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Molecules, Volume 15, Issue 10 (October 2010), Pages 6678-7508

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Open AccessArticle Modulation of Huntingtin Toxicity by BAG1 is Dependent on an Intact BAG Domain
Molecules 2010, 15(10), 6678-6687; doi:10.3390/molecules15106678
Received: 11 August 2010 / Revised: 16 September 2010 / Accepted: 19 September 2010 / Published: 28 September 2010
Cited by 3 | PDF Full-text (444 KB)
Abstract
Huntington´s disease, one of the so-called poly-glutamine diseases, is a dominantly inherited movement disorder characterized by formation of cytosolic and nuclear inclusion bodies and progressive neurodegeneration. Recently, we have shown that Bcl-2-associated athanogene-1 (BAG1), a multifunctional co-chaperone, modulates toxicity, aggregation, degradation and [...] Read more.
Huntington´s disease, one of the so-called poly-glutamine diseases, is a dominantly inherited movement disorder characterized by formation of cytosolic and nuclear inclusion bodies and progressive neurodegeneration. Recently, we have shown that Bcl-2-associated athanogene-1 (BAG1), a multifunctional co-chaperone, modulates toxicity, aggregation, degradation and subcellular distribution in vitro and in vivo of the disease-specific mutant huntingtin protein. Aiming at future small molecule-based therapeutical approaches, we further analysed structural demands for these effects employing the C-terminal deletion mutant BAGDC. We show that disruption of the BAG domain known to eliminate intracellular heat shock protein 70 (Hsp70) binding and activation also precludes binding of Siah-1 thereby leaving nuclear huntingtin translocation unaffected. At the same time BAGDC fails to induce increased proteasomal huntingtin turnover and does not inhibit intracellular huntingtin aggregation, a pre-requisite necessary for prevention of huntingtin toxicity. Full article
(This article belongs to the Special Issue Neuroprotective Strategies)
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Open AccessArticle Hypericum Perforatum L. Hypericaceae/Guttiferae Sunflower, Olive and Palm Oil Еxtracts Attenuate Cold Restraint Stress – Induced Gastric Lesions
Molecules 2010, 15(10), 6688-6698; doi:10.3390/molecules15106688
Received: 10 June 2010 / Revised: 14 September 2010 / Accepted: 20 September 2010 / Published: 28 September 2010
Cited by 6 | PDF Full-text (293 KB)
Abstract
Three Hypericum perforatum L., Hypericaceae (St. John’s Wort) oil extracts (HPE) were prepared according to the prescriptions from traditional medicine – fresh flowering tops were macerated in three different vegetable oils: sunflower (E1), olive (E2) and palm oil (E3) for 40 days, [...] Read more.
Three Hypericum perforatum L., Hypericaceae (St. John’s Wort) oil extracts (HPE) were prepared according to the prescriptions from traditional medicine – fresh flowering tops were macerated in three different vegetable oils: sunflower (E1), olive (E2) and palm oil (E3) for 40 days, exposed to the sunlight. The aim of the study was to investigate the gastroprotective activity of the obtained extracts in respect to their quercetin content. HPLC analysis confirmed the presence of quercetin in all of the investigated HPEs, but in different amounts: 15.1, 5.8 and 21.7 μg/mL in E1, E2, and E3, respectively. Gastroprotective activity was evaluated using cold-restraint stress (CRS) induced rat gastric mucosa lesions test. All of the HPEs showed gastroprotective activity, which was close to that achieved by the one of the most studied anti-ulcer flavonoids, quercetin [percentages of inhibition of ulcer index (UI) were 35, 62 and 40 % in E1, E2 and E3, respectively]. Contrary to the lowest quercetin content, HPE prepared with olive oil (E2) offered the highest protection against gastric damaging action of CRS. It may be assumed that this is due to other constituents of E2, which probably play an additional role in complex gastroprotective activity. Full article
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Open AccessArticle Carotenoids from Mangifera Pajang and Their Antioxidant Capacity
Molecules 2010, 15(10), 6699-6712; doi:10.3390/molecules15106699
Received: 4 August 2010 / Revised: 22 September 2010 / Accepted: 25 September 2010 / Published: 28 September 2010
Cited by 11 | PDF Full-text (342 KB)
Abstract
This study provides new data on the various carotenoids found in bambangan (Mangifera pajang Kosterm.) peel and pulp extracts, such as all-trans-α- and β-carotene, cis-β-carotene, 9-cis-β-carotene, and cryptoxanthin. Chemical and biological antioxidant assays were determined to [...] Read more.
This study provides new data on the various carotenoids found in bambangan (Mangifera pajang Kosterm.) peel and pulp extracts, such as all-trans-α- and β-carotene, cis-β-carotene, 9-cis-β-carotene, and cryptoxanthin. Chemical and biological antioxidant assays were determined to evaluate the antioxidant capacity of bambangan peel and pulp extracts. Bambangan pulp had higher α- and β-carotene contents (7.96 ± 1.53 and 20.04 ± 1.01 mg/100 g) than its peel (4.2 ± 0.14 and 13.09 ± 0.28 mg/100 g); the cryptoxanthin contents of bambangan peel and pulp were 0.60 and 1.18 mg/100 g, respectively. The antioxidant activity results determined by chemical assay using the 2,2-diphenyl-2-picrylhydrazyl (DPPH) method showed that bambangan peel extract had higher DPPH radical scavenging activity than its pulp. In the biological assays bambangan peel and pulp had protective effects against hemoglobin and LDL oxidation at an extract concentration of 1 ppm. Bambangan peel is a therefore a potential source of natural antioxidants and could be utilized as a functional ingredient. Full article
Open AccessArticle Antiphytoviral Activity of Satureja montana L. ssp. variegata (Host) P. W. Ball Essential Oil and Phenol Compounds on CMV and TMV
Molecules 2010, 15(10), 6713-6721; doi:10.3390/molecules15106713
Received: 3 August 2010 / Revised: 8 September 2010 / Accepted: 16 September 2010 / Published: 28 September 2010
Cited by 15 | PDF Full-text (248 KB)
Abstract
The essential oil of Satureja montana L. ssp. variegata (Host) P. W. Ball (Lamiaceae) was characterized by a high concentration of oxygenated monoterpenes (71.3%), among which carvacrol (19.4%) and thymol (16.6%) were the major compounds. When the essential oil was applied on local hosts Chenopodium amaranticolor Coste & Reyn. and Chenopodium quinoa Willd. simultaneously with the infecting virus, the number of local lesions on both Tobacco mosaic virus (TMV) and Cucumber mosaic virus (CMV) infected plants was reduced for 29.2% and 24.1%, respectively. When applied individually for each virus, thymol was more effective in reducing CMV infection (33.2%), while carvacrol was more effective in reducing the TMV infection (34.3%). No synergistic effect of both monoterpenes was observed in the antiviral activity of the oil. Full article
(This article belongs to the Section Natural Products)
Open AccessArticle Antioxidant Activities of Caragana sinica Flower Extracts and Their Main Chemical Constituents
Molecules 2010, 15(10), 6722-6732; doi:10.3390/molecules15106722
Received: 10 August 2010 / Revised: 4 September 2010 / Accepted: 16 September 2010 / Published: 28 September 2010
Cited by 6 | PDF Full-text (269 KB)
Abstract
The edible flowers of Caragana sinica are used in China a kind of health-promoting vegetable. In this study, the antioxidant activities of its ethanol extract, as well as its petroleum ether, ethyl acetate, n-butanol and water fractions, were evaluated through [...] Read more.
The edible flowers of Caragana sinica are used in China a kind of health-promoting vegetable. In this study, the antioxidant activities of its ethanol extract, as well as its petroleum ether, ethyl acetate, n-butanol and water fractions, were evaluated through in vitro model systems including the DPPH, FRAP and β-carotene bleaching methods. Among the C. sinica flower extracts the ethyl acetate fraction was the most effective. Correlation analysis suggested that flavonoids might be the major contributors to the high antioxidant activity of this flower. Six flavonoids including quercetin (1), isoquercitrin (2), rutin (3), quercetin-3′-O-methyl-3-O-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside (4), typhaneoside (5) and quercetin-3-O-β-D-glucopyranosyl(1→2)[α-L-rhamnopyranosyl (1→6)]-β-D-glucopyranoside (6), were isolated from this flower for the first time. Their contents were determined by a HPLC method. Compounds 3 and 4 were found to be the major flavonoids, with concentrations of 1.20 ± 0.07 and 3.94 ± 0.12 mg/g dry sample, respectively. These results demonstrated that the C. sinica flowers may be valuable natural antioxidant sources and are potentially applicable in the health food industry. Full article
(This article belongs to the Special Issue Antioxidants)
Open AccessArticle Two New Pyranoxanthones from Mesua beccariana (Guttiferae)
Molecules 2010, 15(10), 6733-6742; doi:10.3390/molecules15106733
Received: 13 August 2010 / Revised: 20 August 2010 / Accepted: 24 August 2010 / Published: 28 September 2010
Cited by 5 | PDF Full-text (259 KB)
Abstract
Our recent study on the stem bark extracts of Mesua beccariana has led to the isolation of two new pyranoxanthones, mesuarianone  (1) and mesuasinone (2), two anthraquinones, 4-methoxy-1,3,5-trihydroxyanthraquinone (3) and 2,5-dihydroxy-1,3,4-trimethoxyanthraquinone (4), one coumarin, [...] Read more.
Our recent study on the stem bark extracts of Mesua beccariana has led to the isolation of two new pyranoxanthones, mesuarianone  (1) and mesuasinone (2), two anthraquinones, 4-methoxy-1,3,5-trihydroxyanthraquinone (3) and 2,5-dihydroxy-1,3,4-trimethoxyanthraquinone (4), one coumarin, mammea A/AB (5) and three common triterpenes, stigmasterol (6), friedelin (7) and betulinic acid (8). Structural elucidations of these compounds were achieved using 1D and 2D NMR and MS techniques. This is the first report on the phytochemistry of Mesua beccariana. Full article
Open AccessArticle Convenient Synthesis and Antimicrobial Activity of Some Novel Amino Acid Coupled Triazoles
Molecules 2010, 15(10), 6759-6772; doi:10.3390/molecules15106759
Received: 19 July 2010 / Revised: 30 August 2010 / Accepted: 1 September 2010 / Published: 28 September 2010
Cited by 8 | PDF Full-text (193 KB)
Abstract
This study describes a promising one-pot synthesis of [2-(5-benzyl-4-phenyl-4H-[1,2,4]triazol-3-thio)-acetyl]-amino acid methyl esters 6a-h and dipeptides 10a-e, which were successfully synthesized starting from amino acid esters 5a-h, 9a-e and azides 4, 8a,b, respectively. On the other hand, azide 4 underwent [...] Read more.
This study describes a promising one-pot synthesis of [2-(5-benzyl-4-phenyl-4H-[1,2,4]triazol-3-thio)-acetyl]-amino acid methyl esters 6a-h and dipeptides 10a-e, which were successfully synthesized starting from amino acid esters 5a-h, 9a-e and azides 4, 8a,b, respectively. On the other hand, azide 4 underwent Curtius rearrangement to the corresponding isocyanate, which subsequently reacted with selected aliphatic amine and/or aniline derivatives to give the corresponding urea derivatives 11 and 12a,b. Reactions of the isocyanate with secondary amines gave amide derivatives 13a,b. The structural elucidation of products is reported and some of the products were also screened for their antimicrobial activity. Full article
(This article belongs to the Section Organic Synthesis)
Open AccessArticle Synthesis of Lasofoxifene, Nafoxidine and Their Positional Isomers via the Novel Three-Component Coupling Reaction
Molecules 2010, 15(10), 6773-6794; doi:10.3390/molecules15106773
Received: 21 August 2010 / Revised: 13 September 2010 / Accepted: 20 September 2010 / Published: 28 September 2010
Cited by 4 | PDF Full-text (440 KB) | Supplementary Files
Abstract
A Lewis acid-mediated three-component coupling reaction was successfully applied for the synthesis of lasofoxifene (1), nafoxidine (2), and their positional isomers, inv-lasofoxifene (3) and inv-nafoxidine (4). In the presence of HfCl4 [...] Read more.
A Lewis acid-mediated three-component coupling reaction was successfully applied for the synthesis of lasofoxifene (1), nafoxidine (2), and their positional isomers, inv-lasofoxifene (3) and inv-nafoxidine (4). In the presence of HfCl4, the desired one-pot coupling reaction among 4-pivaloyloxybenzaldehyde (5), cinnamyltrimethylsilane (6), and anisole proceeded to afford the corresponding 3,4,4-triaryl-1-butene 7 in high yield. The iodocarbocyclization of the coupling product and the successive elimination of hydrogen iodide forming the olefin part, followed by the migration of the double-bond afforded the common synthetic intermediate of lasofoxifene (1) and nafoxidine (2) via a very concise procedure. Additionally, the syntheses of their positional isomers inv-lasofoxifene (3) and inv-nafoxidine (4) were also achieved through very convenient protocols. Full article
(This article belongs to the Special Issue Diversity Oriented Synthesis)
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Open AccessArticle Synthesis and Antioxidant Activity of Some New Coumarinyl-1,3-Thiazolidine-4-ones
Molecules 2010, 15(10), 6795-6809; doi:10.3390/molecules15106795
Received: 12 June 2010 / Revised: 21 September 2010 / Accepted: 27 September 2010 / Published: 29 September 2010
Cited by 31 | PDF Full-text (263 KB)
Abstract
A series of Schiff’s bases (E)-N-2-aryliden-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetohydrazides 2a-l and N-(2-(substituted phenyl)-4-oxo-thiazolidin-3-yl)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetamides 3a-l were synthesized and evaluated for their antioxidant activity by the phosphomolybdenum method. Most of the Schiff’s bases and thiazolidine-4-ones bearing two hydroxyl [...] Read more.
A series of Schiff’s bases (E)-N-2-aryliden-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetohydrazides 2a-l and N-(2-(substituted phenyl)-4-oxo-thiazolidin-3-yl)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetamides 3a-l were synthesized and evaluated for their antioxidant activity by the phosphomolybdenum method. Most of the Schiff’s bases and thiazolidine-4-ones bearing two hydroxyl groups on the phenyl ring showed excellent antioxidant activity in comparison with ascorbic acid. Preliminary investigation on cytotoxic and antifungal activity was done on some representative samples. Full article
Open AccessArticle Domoic Acid - A New Toxin in the Croatian Adriatic Shellfish Toxin Profile
Molecules 2010, 15(10), 6835-6849; doi:10.3390/molecules15106835
Received: 31 August 2010 / Revised: 25 September 2010 / Accepted: 27 September 2010 / Published: 8 October 2010
Cited by 17 | PDF Full-text (259 KB)
Abstract
This is the first study that presents concentrations of domoic acid detected in the whole shellfish tissue from breeding and harvesting areas along the Croatian coast of the Adriatic Sea during the period 2006 to 2008. Shellfish sample analyses after SAX cleaning [...] Read more.
This is the first study that presents concentrations of domoic acid detected in the whole shellfish tissue from breeding and harvesting areas along the Croatian coast of the Adriatic Sea during the period 2006 to 2008. Shellfish sample analyses after SAX cleaning procedures, using a UV-DAD-HPLC system, showed the presence of domoic acid in four species. The most prevalent of those species were the blue mussel (Mytilus galloprovincialis), followed by European flat oyster (Ostrea edulis), Mediterranean scallop (Pecten jacobaeus) and proteus scallop (Flexopecten proteus). Domoic acid, a potentially lethal phycotoxin that causes amnesic shellfish poisoning (ASP), was detected for the first time in January 2006 with the highest value of 6.5486 μg g-1 in whole shellfish tissue. Pseudo-nitzschia spp. bloom events preceded these high domoic acid concentrations. According to this study, retention of domoic acid in the blue mussel M. galloprovincialis is more than 42 days. This investigation indicates the first presence of domoic acid in Croatian shellfish, but in concentrations under the regulatory limit (20 μg g-1), therefore shellfish consumption was not found to endanger human health. Full article
Open AccessCommunication Synthesis and Anti-Bacterial Activities of Some Novel Schiff Bases Derived from Aminophenazone
Molecules 2010, 15(10), 6850-6858; doi:10.3390/molecules15106850
Received: 20 July 2010 / Revised: 16 August 2010 / Accepted: 18 August 2010 / Published: 8 October 2010
Cited by 29 | PDF Full-text (106 KB)
Abstract
A series of 1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one-containing Schiff bases were synthesized, characterized and screened for their antibacterial activities. The structures of the synthesized compounds were established by spectroscopic (FT-IR, 1H-NMR, 13C-NMR, MS) and elemental analyses. The anti-bacterial activities (with MIC values) [...] Read more.
A series of 1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one-containing Schiff bases were synthesized, characterized and screened for their antibacterial activities. The structures of the synthesized compounds were established by spectroscopic (FT-IR, 1H-NMR, 13C-NMR, MS) and elemental analyses. The anti-bacterial activities (with MIC values) of compounds were evaluated. The anti-bacterial screening results reveal that among the six compounds screened, four compounds showed moderate to good anti-bacterial activity. Among the tested compounds, the most effective compounds against four bacterial strains, viz. Escherichia coli, Staphylococcus aureus, Salmonella typhimurium and Streptococcus pyogenes, are [(2-Chlorobenzylidene)amino]-1,5-dimethyl-2-phenyl-1,2-dihydropyrazol-3-one (4) and [(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylimino)methyl]benzonitrile (5) with MIC values of 6.25 μg/mL. Full article
Open AccessArticle In Vitro Antioxidant Properties, HIV-1 Reverse Transcriptase and Acetylcholinesterase Inhibitory Effects of Traditional Herbal Preparations Sold in South Africa
Molecules 2010, 15(10), 6888-6904; doi:10.3390/molecules15106888
Received: 16 August 2010 / Revised: 27 August 2010 / Accepted: 3 September 2010 / Published: 8 October 2010
Cited by 15 | PDF Full-text (252 KB)
Abstract
The antioxidant potentials for fourteen multipurpose traditional herbal preparations sold in South Africa were determined using the DPPH radical scavenging, ferric reducing power and β-carotene-linoleic acid model system, the anti-HIV-1 reverse transcriptase (RT) enzyme inhibitory effects using an ELISA kit and [...] Read more.
The antioxidant potentials for fourteen multipurpose traditional herbal preparations sold in South Africa were determined using the DPPH radical scavenging, ferric reducing power and β-carotene-linoleic acid model system, the anti-HIV-1 reverse transcriptase (RT) enzyme inhibitory effects using an ELISA kit and acetylcholinesterase (AChE) enzyme inhibition using the microtitre plate assay. Nine of the herbal mixtures (Umzimba omubi, Umuthi wekukhwehlela ne zilonda, Mvusa ukunzi, Umpatisa inkosi, Imbiza ephuzwato, Vusa umzimba, Supreme one hundred, Sejeso herbal mixture Ingwe® and Ingwe® special muti) exhibited higher antioxidant potentials, while only four (Imbiza ephuzwato, Ingwe® muthi mixture, Sejeso herbal mixture Ingwe® and African potato extractTM) showed potent activity against the RT enzyme. Nine mixtures (Imbiza ephuzwato, Umpatisa inkosi, African potato extractTM, Sejeso herbal mixture Ingwe®, Vusa umzimba; Ingwe® muthi mixture, Ibhubezi™, Lion izifozonke Ingwe® and Ingwe® special muti) showed AChE enzyme inhibitory activity greater than 50%. The observed activity exhibited by some of the herbal mixtures gives some credence to the manufacturers’ claims and goes part of the way towards validating their use against certain conditions such as oxidative stress, HIV/AIDS proliferation and some mental conditions. It is however, desirable to carry out further studies to determine the effects of mixing plant species/parts in one mixture on the antioxidant potency as well as isolating active constituents from the herbal mixtures. Full article
(This article belongs to the Special Issue Antioxidants)
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Open AccessArticle Prodigiosin Production by Serratia marcescens UCP 1549 Using Renewable-Resources as a Low Cost Substrate
Molecules 2010, 15(10), 6931-6940; doi:10.3390/molecules15106931
Received: 16 August 2010 / Revised: 6 September 2010 / Accepted: 9 September 2010 / Published: 8 October 2010
Cited by 23 | PDF Full-text (254 KB)
Abstract
A new strain of Serratia marcescens UCP1459 isolated from a semi-arid soil produced the natural red pigment prodigiosin, characterized by an uncommon pyrrolylpyrromethane skeleton. Prodigiosin is a promising drug due to its reported antifungal, immunosuppressive and anti-proliferative activities. The objective of this [...] Read more.
A new strain of Serratia marcescens UCP1459 isolated from a semi-arid soil produced the natural red pigment prodigiosin, characterized by an uncommon pyrrolylpyrromethane skeleton. Prodigiosin is a promising drug due to its reported antifungal, immunosuppressive and anti-proliferative activities. The objective of this work was to indentify a suitable medium to simultaneously enhance S. marcescens growth and pigment production using renewable resources obtained from industrial wastes. S. marcescens produced the highest level of prodigiosin (49.5 g/L) at 48 h of cultivation using 6% “manipueira” (cassava wastewater) supplemented with mannitol (2%) at pH 7 and 28 °C. Carbohydrates in “manipueira” and mannitol play a role in the enhanced cell growth and prodigiosin production. The purified pigment extracted from the biomass was analyzed by mass spectrophotometry and showed the expected molecular weight of 324 Da corresponding to prodigiosin. In conclusion, we have successfully designed a new, economically feasible medium supporting enhanced S. marcescens growth and a high yield production of prodigiosin. Full article
Open AccessArticle Synthesis 1-Acyl-3-(2'-aminophenyl) thioureas as Anti-Intestinal Nematode Prodrugs
Molecules 2010, 15(10), 6941-6947; doi:10.3390/molecules15106941
Received: 4 August 2010 / Revised: 6 September 2010 / Accepted: 25 September 2010 / Published: 8 October 2010
Cited by 14 | PDF Full-text (148 KB)
Abstract
A series of 1-acyl-3-(2'-aminophenyl) thiourea derivatives were designed and synthesized. The structures of all the newly synthesized compounds were identified by IR, elemental analysis, 1H-NMR and 13C-NMR. Their anti-intestinal nematode activities against Nippostrongylus brazilliensis were evaluated in rats by [...] Read more.
A series of 1-acyl-3-(2'-aminophenyl) thiourea derivatives were designed and synthesized. The structures of all the newly synthesized compounds were identified by IR, elemental analysis, 1H-NMR and 13C-NMR. Their anti-intestinal nematode activities against Nippostrongylus brazilliensis were evaluated in rats by an oral route. Among these compounds, at concentrations of 10 mg/kg of rat, compound (1-(2'-furanyl)acyl-3- (2'-aminophenyl) thiourea) (5h) produced the highest activity with 89.4% deparasitization. The present work suggests that 1-acyl-3-(2'-aminophenyl) thiourea derivatives may become useful  lead compounds for anti-intestinal nematode treatment. Full article
Open AccessCommunication Component Analysis and Free Radicals Scavenging Activity of Cicer arietinum L. Husk Pectin
Molecules 2010, 15(10), 6948-6955; doi:10.3390/molecules15106948
Received: 13 August 2010 / Revised: 6 September 2010 / Accepted: 13 September 2010 / Published: 11 October 2010
Cited by 9 | PDF Full-text (230 KB)
Abstract
A pectin (CAP) was extracted from the husk of Cicer arietinum L.. Monosaccharide analysis of CAP revealed the dominance of galacturonic acid and smaller amounts of galactose, arabinose, rhamnose, glucose, xylose and mannose. Viscosimetric analysis showed that the intrinsic viscosity ([η [...] Read more.
A pectin (CAP) was extracted from the husk of Cicer arietinum L.. Monosaccharide analysis of CAP revealed the dominance of galacturonic acid and smaller amounts of galactose, arabinose, rhamnose, glucose, xylose and mannose. Viscosimetric analysis showed that the intrinsic viscosity ([η]) and the molecular weight (MW) of CAP were 296 mL/g and 105 kDa, respectively. The degree of esterification (DE = 10%) was determined by FTIR spectroscopy. CAP exhibited a dose-dependent free radical scavenging activity, as shown by its DPPH radical inhibition. At 1.0 mg/mL CAP exhibited a scavenging rate of 29% on DPPH radicals. The evaluation of antioxidant activity suggested that CAP had good potential for DPPH radical scavenging activity and should be explored as a novel potential antioxidant. Full article
(This article belongs to the Section Natural Products)
Open AccessArticle Evaluation of Antioxidant Capacity and Synergistic Associations of Quinonemethide Triterpenes and Phenolic Substances from Maytenus ilicifolia (Celastraceae)
Molecules 2010, 15(10), 6956-6973; doi:10.3390/molecules15106956
Received: 27 August 2010 / Revised: 13 September 2010 / Accepted: 24 September 2010 / Published: 11 October 2010
Cited by 9 | PDF Full-text (248 KB)
Abstract
This work describes the isolation of the secondary metabolites identified as the quinonemethides maytenin (1) and pristimerin (2) from Maytenus ilicifolia extracts obtained from root barks of adult plants and roots of seedlings and their quantification by high [...] Read more.
This work describes the isolation of the secondary metabolites identified as the quinonemethides maytenin (1) and pristimerin (2) from Maytenus ilicifolia extracts obtained from root barks of adult plants and roots of seedlings and their quantification by high performance liquid chromatography coupled to a diode array detector. The electrochemical profiles obtained from cyclic voltammetry and a coulometric detector coupled to high-performance liquid chromatography contributed to the evaluation of their antioxidant capacity. The antioxidant properties of individual components and the crude extracts of the root barks of Maytenus ilicifolia were compared and the possible synergistic associations of quinonemethide triterpenes and phenolic substances were investigated by using rutin as a model phenolic compound. Full article
(This article belongs to the Special Issue Antioxidants)
Open AccessArticle LYRM1, a Gene that Promotes Proliferation and Inhibits Apoptosis during Heart Development
Molecules 2010, 15(10), 6974-6982; doi:10.3390/molecules15106974
Received: 18 September 2010 / Revised: 28 September 2010 / Accepted: 2 October 2010 / Published: 11 October 2010
Cited by 3 | PDF Full-text (351 KB)
Abstract
Congenital heart disease (CHD) is the most common type of birth defect, but its underlying molecular mechanisms remain unidentified. Previous studies determined that Homo sapiens LYR motif containing 1 (LYRM1) is a novel nucleoprotein expressed at the highest level in [...] Read more.
Congenital heart disease (CHD) is the most common type of birth defect, but its underlying molecular mechanisms remain unidentified. Previous studies determined that Homo sapiens LYR motif containing 1 (LYRM1) is a novel nucleoprotein expressed at the highest level in adipose tissue and in high levels in heart tissue. The LYRM1 gene may play an important role in the development of the human heart. This study was designed to identify the biological characteristics of the LYRM1 gene in heart development. On the basis of expression-specific differentiation markers identified with quantitative real-time RT-PCR and the morphology of LYRM1-overexpressing cells during differentiation, ectopic expression was not found to significantly affect differentiation of P19 cells into cardiomyocytes. MTT assays and cell cycle analysis showed that LYRM1 dramatically increases the proliferation of P19 cells. Furthermore, data from annexin V-FITC binding and caspase-3 activity revealed that LYRM1 can inhibit the apoptosis of P19 cells. Our data suggest that LYRM1 might have the potential to modulate cell growth, apoptosis, and heart development. Full article
Open AccessArticle Targeted Thiazole Orange Derivative with Folate: Synthesis, Fluorescence and in Vivo Fluorescence Imaging
Molecules 2010, 15(10), 6983-6992; doi:10.3390/molecules15106983
Received: 19 August 2010 / Revised: 15 September 2010 / Accepted: 25 September 2010 / Published: 11 October 2010
Cited by 7 | PDF Full-text (1268 KB)
Abstract
A Thiazole Orange conjugated with folate derivative was synthesized in two steps. Firstly, folate was coupled with 1-(3-aminopropyl)-4-methylquinolinium bromide to afford folate-methylquinolinium bromide, which then reacted with benzothiazolium to obtain the title folate-conjugated compound. The compound was evaluated by 1H-NMR MS, [...] Read more.
A Thiazole Orange conjugated with folate derivative was synthesized in two steps. Firstly, folate was coupled with 1-(3-aminopropyl)-4-methylquinolinium bromide to afford folate-methylquinolinium bromide, which then reacted with benzothiazolium to obtain the title folate-conjugated compound. The compound was evaluated by 1H-NMR MS, TG/DTA and fluorescence spectroscopic methods. The title compound could selectively target folate receptor expressing tumors according to the in vivo fluorescence imaging preliminarily performed on nude mice with breast tumors. Full article
Open AccessArticle Analysis of the Chemical Composition of the Essential Oil of Polygonum minus Huds. Using Two-Dimensional Gas Chromatography-Time-of-Flight Mass Spectrometry (GC-TOF MS)
Molecules 2010, 15(10), 7006-7015; doi:10.3390/molecules15107006
Received: 4 August 2010 / Revised: 8 October 2010 / Accepted: 10 October 2010 / Published: 12 October 2010
Cited by 28 | PDF Full-text (267 KB)
Abstract
The essential oil in leaves of Polygonum minus Huds., a local aromatic plant, were identified by a pipeline of gas chromatography (GC) techniques coupled with mass-spectrometry (MS), flame ionization detector (FID) and two dimensional gas chromatography time of flight mass spectrometry (GC×GC–TOF [...] Read more.
The essential oil in leaves of Polygonum minus Huds., a local aromatic plant, were identified by a pipeline of gas chromatography (GC) techniques coupled with mass-spectrometry (MS), flame ionization detector (FID) and two dimensional gas chromatography time of flight mass spectrometry (GC×GC–TOF MS). A total of 48 compounds with a good match and high probability values were identified using this technique. Meanwhile, 42 compounds were successfully identified in this study using GC-MS, a significantly larger number than in previous studies. GC-FID was used in determining the retention indices of chemical components in P. minus essential oil. The result also showed the efficiency and reliability were greatly improved when chemometric methods and retention indices were used in identification and quantification of chemical components in plant essential oil. Full article
Open AccessArticle Synthesis and Reactivity of [1,2,4]Triazolo-annelated Quinazolines
Molecules 2010, 15(10), 7016-7034; doi:10.3390/molecules15107016
Received: 25 September 2010 / Revised: 29 September 2010 / Accepted: 8 October 2010 / Published: 12 October 2010
Cited by 21 | PDF Full-text (177 KB) | Correction | Supplementary Files
Abstract
This paper reports the synthesis of phenyl-substituted 2-alkoxy(methylsulfanyl)-1,2,4-triazolo[1,5-a]quinazolines starting from N-cyanoimidocarbonates and substituted hydrazinobenzoic acids as building blocks. Thionation or chlorination of the inherent lactam moiety in the target compounds followed by treatment with multifunctional nucleophiles provided access to [...] Read more.
This paper reports the synthesis of phenyl-substituted 2-alkoxy(methylsulfanyl)-1,2,4-triazolo[1,5-a]quinazolines starting from N-cyanoimidocarbonates and substituted hydrazinobenzoic acids as building blocks. Thionation or chlorination of the inherent lactam moiety in the target compounds followed by treatment with multifunctional nucleophiles provided access to a variety of derivatives. Full article
Open AccessArticle The Fungicidal Terpenoids and Essential Oil from Litsea cubeba in Tibet
Molecules 2010, 15(10), 7075-7082; doi:10.3390/molecules15107075
Received: 7 September 2010 / Revised: 25 September 2010 / Accepted: 11 October 2010 / Published: 13 October 2010
Cited by 27 | PDF Full-text (154 KB)
Abstract
A new C9 monoterpenoid acid (litseacubebic acid, 1) and a known monoterpene lactone (6R)-3,7-dimethyl-7-hydroxy-2-octen-6-olide (2), along with three known compounds – vanillic acid (3), trans-3,4,5-trimethoxylcinnamyl alcohol (4), and oxonantenine (5) – [...] Read more.
A new C9 monoterpenoid acid (litseacubebic acid, 1) and a known monoterpene lactone (6R)-3,7-dimethyl-7-hydroxy-2-octen-6-olide (2), along with three known compounds – vanillic acid (3), trans-3,4,5-trimethoxylcinnamyl alcohol (4), and oxonantenine (5) – were isolated with bioassay-guided purification from the fruit extract of Litsea cubeba collected in Tibet. The structure of 1 was elucidated by MS, 1H-NMR, 13C-NMR, COSY, HSQC, HMBC, NOE spectral data as 2,6-dimethyl-6-hydroxy-2E,4E-hepta-2,4-diene acid. Additionally 33 compounds were identified from the essential oil of L. cubeba. The preliminary bioassay results showed that 1 and 2 have good fungicidal activities against Sclerotinia sclerotiorum, Thanatephorus cucumeris, Pseudocer-cospora musae and Colletotrichum gloeosporioides at the concentration of 588 and 272 μM, and the essential oil has good fungicidal activities against T. cucumeris and S. sclerotiorum, with IC50 values of 115.58 and 151.25 μg/mL, repectively. Full article
Open AccessArticle Two New Alkaloids from Narcissus serotinus L.
Molecules 2010, 15(10), 7083-7089; doi:10.3390/molecules15107083
Received: 15 September 2010 / Revised: 5 October 2010 / Accepted: 11 October 2010 / Published: 14 October 2010
Cited by 8 | PDF Full-text (138 KB)
Abstract
The Amaryllidaceae family is well known for the presence of an exclusive group of alkaloids with a wide range of biological activities. Narcissus serotinus L. is a plant belonging to this family and its geographical distribution is mainly located along the Mediterranean [...] Read more.
The Amaryllidaceae family is well known for the presence of an exclusive group of alkaloids with a wide range of biological activities. Narcissus serotinus L. is a plant belonging to this family and its geographical distribution is mainly located along the Mediterranean coast. In the present work, specimens collected near Casablanca (Morocco) were used to study the alkaloid content of this species. Starting with 350 g of the whole plant we used standard extraction and purification procedures to obtain fractions and compounds for GC-MS and NMR analysis. As well as five known alkaloids, we isolated two new compounds: 1-O-(3´-acetoxybutanoyl)lycorine and narseronine. The latter has been previously published, but with an erroneous structure. Full article
(This article belongs to the Section Natural Products)
Open AccessArticle A New Xanthone from the Bark Extract of Rheedia acuminata and Antiplasmodial Activity of Its Major Compounds
Molecules 2010, 15(10), 7106-7114; doi:10.3390/molecules15107106
Received: 21 August 2010 / Revised: 23 September 2010 / Accepted: 3 October 2010 / Published: 14 October 2010
Cited by 8 | PDF Full-text (205 KB)
Abstract
Bioassay-guided fractionation of the ethyl acetate bark extract of Rheedia acuminata led to the isolation of the new compound 1,5,6-trihydroxy-3-methoxy-7-geranyl-xanthone (1), together with four known compounds 2-5. These compounds were tested in vitro for their antiplasmodial activity [...] Read more.
Bioassay-guided fractionation of the ethyl acetate bark extract of Rheedia acuminata led to the isolation of the new compound 1,5,6-trihydroxy-3-methoxy-7-geranyl-xanthone (1), together with four known compounds 2-5. These compounds were tested in vitro for their antiplasmodial activity on a chloroquine-resistant strain of Plasmodium falciparum (FcB1) and for their cytotoxicity against the human diploid embryonic lung cell line MRC-5. Full article
Open AccessArticle Inhibitory Effects of Resveratrol on the Epstein-Barr Virus Lytic Cycle
Molecules 2010, 15(10), 7115-7124; doi:10.3390/molecules15107115
Received: 7 September 2010 / Revised: 11 October 2010 / Accepted: 13 October 2010 / Published: 14 October 2010
Cited by 18 | PDF Full-text (232 KB)
Abstract
Reactivation of Epstein-Barr virus (EBV) from latency to the lytic cycle is required for the production of viral particles. Here, we examine the capacity of resveratrol to inhibit the EBV lytic cycle. Our results show that resveratrol inhibits the transcription of EBV [...] Read more.
Reactivation of Epstein-Barr virus (EBV) from latency to the lytic cycle is required for the production of viral particles. Here, we examine the capacity of resveratrol to inhibit the EBV lytic cycle. Our results show that resveratrol inhibits the transcription of EBV immediate early genes, the expression of EBV lytic proteins, including Rta, Zta, and EA-D and reduces viron production, suggesting that this compound may be useful for preventing the proliferation of the virus. Full article
(This article belongs to the Section Natural Products)
Open AccessArticle Effects of Different Maturity Stages on Antioxidant Content of Ivorian Gnagnan (Solanum indicum L.) Berries
Molecules 2010, 15(10), 7125-7138; doi:10.3390/molecules15107125
Received: 2 September 2010 / Revised: 28 September 2010 / Accepted: 12 October 2010 / Published: 15 October 2010
Cited by 8 | PDF Full-text (276 KB)
Abstract
Gnagnan (Solanum indicum L.) is a spontaneous plant widely distributed in Ivory Coast. During ripening stages, Solanum indicum L. presents different colours (green, yellow and red) and is reported to contain several albeit poorly characterized antioxidant compounds. This paper describes in [...] Read more.
Gnagnan (Solanum indicum L.) is a spontaneous plant widely distributed in Ivory Coast. During ripening stages, Solanum indicum L. presents different colours (green, yellow and red) and is reported to contain several albeit poorly characterized antioxidant compounds. This paper describes in detail the antioxidant profile (ascorbic acid, carotenoids and polyphenols), antioxidant capacity (FRAP test and Folin-Ciocalteau assay) and the colour changes of Gnagnan berries at different ripening levels. Ascorbic acid content was similar in green and yellow berries, but significantly lower in red ones. Red berries showed a higher content of carotenoids compared to green and yellow ones. Regarding polyphenols, several phenolic acids and flavonoids were found in all berries. The content of caffeoylquinic acids, caffeic acid, flavonol glycosides and naringenin was higher in red berries, while the content of p-coumaric acid and feruloylquinic acids was similar among the three colours. The FRAP assay increased with the ripening process, whereas total polyphenols were similar among berries. Significant differences were found for the colorimetric indexes among products of different degrees of ripening. The present results show the important role of the ripening stage in increasing the antioxidant content of Gnagnan berries. Full article
(This article belongs to the Special Issue Antioxidants)
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Open AccessArticle Anti-Adhesive Activities of Flavan-3-ols and Proanthocyanidins in the Interaction of Group A-Streptococci and Human Epithelial Cells
Molecules 2010, 15(10), 7139-7152; doi:10.3390/molecules15107139
Received: 19 September 2010 / Revised: 13 October 2010 / Accepted: 14 October 2010 / Published: 15 October 2010
Cited by 8 | PDF Full-text (233 KB)
Abstract
Bacterial adhesion to epithelial cells is a key step in infections, allowing subsequent colonization, invasion and internalization of pathogens into tissues. Anti-adhesive agents are therefore potential prophylactic tools against bacterial infections. The range of anti-adhesive compounds is largely confined to carbohydrate analogues. [...] Read more.
Bacterial adhesion to epithelial cells is a key step in infections, allowing subsequent colonization, invasion and internalization of pathogens into tissues. Anti-adhesive agents are therefore potential prophylactic tools against bacterial infections. The range of anti-adhesive compounds is largely confined to carbohydrate analogues. Tannins are generously recognized as potent antimicrobials, but little data exist on their anti-adherence potency. Using a model for mucosal pathogenesis with labeled group A-streptococci (GAS) and human laryngeal HEp-2 cells, a series of flavan-3-ols (epicatechin, epigallocatechin, epigallocatechin-3-O-gallate) and highly purified and chemically characterized proanthocyanidin samples including procyanidins based on epicatechin, catechin or ‘mixed’ constituent flavanyl units, prodelphinidins made up of (epi)gallocatechin monomeric unts as well as oligomers possessing A-type units in their molecules was evaluated for anti-adhesive effects. Reduced microbial adherence was observed exclusively for prodelphinidins, suggesting that pyrogallol-type elements, i.e., (epi)gallocatechin units are important structural features. This is the first report on structure-activity relationships regarding the anti-adhesive potency of proanthocyanidins. In addition, the structures of the first chemically defined proanthocyanidins from Pelargonium sidoides are disclosed. Full article
(This article belongs to the Section Natural Products)
Open AccessArticle Mechanisms of the Gastric Antiulcerogenic Activity of Anacardium humile St. Hil on Ethanol-Induced Acute Gastric Mucosal Injury in Rats
Molecules 2010, 15(10), 7153-7166; doi:10.3390/molecules15107153
Received: 9 September 2010 / Revised: 8 October 2010 / Accepted: 14 October 2010 / Published: 15 October 2010
Cited by 13 | PDF Full-text (443 KB)
Abstract
Leaves and bark infusions Anacardium humile St. Hil. (Anacardiaceae), known as in Brazil as “cajuzinho do cerrado”, have been used in folk medicine as an alternative treatment for ulcers and gastritis. This study evaluated the gastroprotective activity of an ethyl acetate extract [...] Read more.
Leaves and bark infusions Anacardium humile St. Hil. (Anacardiaceae), known as in Brazil as “cajuzinho do cerrado”, have been used in folk medicine as an alternative treatment for ulcers and gastritis. This study evaluated the gastroprotective activity of an ethyl acetate extract of the leaves of A. humile (AcF) and the mechanism involved in this gastroprotection. Pretreatment concentrations (50, 100, 200 mg.kg−1) were administered by gavage. Following a 60 min. period, all the rats were orally administered 1 mL of absolute ethanol. One hour after the administration of ethanol, all groups were sacrificed, and the gastric ulcer index was calculated. Prostaglandin PGE2 concentration, gastric adherent mucous, and the participation of nitric oxide (NO) and sulfhydryl compounds in the gastroprotection process were also analyzed using the most effective tested dose (50 mg·kg−1). A histological study of the glandular stomach for the evaluation of the epithelial damage and mucus content was also performed. AcF significantly reduced the gastric damage produced by ethanol. This effect was statistically significant for the 50 mg·kg−1 group compared to control. Also, it significantly increased the PGE2 (by 10-fold) and mucous production, while pretreatment with NG-nitro-L-arginine methyl ester (L-NAME) or N-ethylmaleimide (NEM) completely abolished the gastroprotection. AcF has a protective effect against ethanol, and this effect, might be due to the augmentation of the protective mechanisms of mucosa. Full article
(This article belongs to the Section Natural Products)
Open AccessArticle Preparation of a Carbon-Based Solid Acid Catalyst by Sulfonating Activated Carbon in a Chemical Reduction Process
Molecules 2010, 15(10), 7188-7196; doi:10.3390/molecules15107188
Received: 14 September 2010 / Revised: 11 October 2010 / Accepted: 13 October 2010 / Published: 18 October 2010
Cited by 42 | PDF Full-text (222 KB)
Abstract
Sulfonated (SO3H-bearing) activated carbon (AC-SO3H) was synthesized by an aryl diazonium salt reduction process. The obtained material had a SO3H density of 0.64 mmol·g-1 and a specific surface area of 602 m2·g-1 [...] Read more.
Sulfonated (SO3H-bearing) activated carbon (AC-SO3H) was synthesized by an aryl diazonium salt reduction process. The obtained material had a SO3H density of 0.64 mmol·g-1 and a specific surface area of 602 m2·g-1. The catalytic properties of AC-SO3H were compared with that of two commercial solid acid catalysts, Nafion NR50 and Amberlyst-15. In a 10-h esterification reaction of acetic acid with ethanol, the acid conversion with AC-SO3H (78%) was lower than that of Amberlyst-15 (86%), which could be attributed to the fact that the SO3H density of the sulfonated carbon was lower than that of Amberlyst-15 (4.60 mmol·g-1). However, AC-SO3H exhibited comparable and even much higher catalytic activities than the commercial catalysts in the esterification of aliphatic acids with longer carbon chains such as hexanoic acid and decanoic acid, which may be due to the large specific surface area and mesoporous structures of the activated carbon. The disadvantage of AC-SO3H is the leaching of SO3H group during the reactions. Full article
Open AccessArticle Small Interfering RNA Effectively Inhibits the Expression of SARS Coronavirus Membrane Gene at Two Novel Targeting Sites
Molecules 2010, 15(10), 7197-7207; doi:10.3390/molecules15107197
Received: 1 September 2010 / Accepted: 15 September 2010 / Published: 18 October 2010
Cited by 5 | PDF Full-text (682 KB)
Abstract
Small interfering RNA (siRNA) is a class of duplex RNA molecules of 21-25 nt nucleotides in length functioning post-transcriptionally to downregulate targeted gene expression. The membrane (M) protein of severe acute respiratory syndrome-associated coronavirus (SARS-CoV) is highly abundant during viral infections and [...] Read more.
Small interfering RNA (siRNA) is a class of duplex RNA molecules of 21-25 nt nucleotides in length functioning post-transcriptionally to downregulate targeted gene expression. The membrane (M) protein of severe acute respiratory syndrome-associated coronavirus (SARS-CoV) is highly abundant during viral infections and is a critical element for viral assembly. Nucleotide substitution in the viral genome occurs frequently during SARS-CoV infection. In the current study, we analyzed the M gene sequences derived from 15 SARS-CoV isolates and uncovered six nucleotide substitutions among these isolates. Interestingly, these nucleotide substitutions are all located at the 5’ half of the M gene. Based on this information and previous reports, we created two novel siRNAs targeting two unexploited and well conserved regions in the M gene. The effects of these two siRNAs were tested by semi-quantitative RT-PCR and EGFP-M fusion gene expression. The results demonstrated that both siRNAs effectively and specifically blocked the targeted gene expression. Real time quantitative RT-PCR (qRT-PCR) revealed that siRNA targeting the 3’ half of the M gene (si-M2) induced more potent inhibition than that targeting the 5’ half (si-M1). Both si-M1 and si-M2 significantly downregulated M gene mediated upregulation of interferon b expression. Thus, our results indicate that SARS-CoV M gene specific siRNA might function in a sequence-dependent manner. Full article
(This article belongs to the Special Issue Catalytic Nucleic Acids)
Open AccessArticle The Beneficial Effect of Vanillic Acid on Ulcerative Colitis
Molecules 2010, 15(10), 7208-7217; doi:10.3390/molecules15107208
Received: 1 September 2010 / Revised: 8 October 2010 / Accepted: 18 October 2010 / Published: 19 October 2010
Cited by 27 | PDF Full-text (318 KB)
Abstract
Vanillic acid, an oxidized form of vanillin, is a benzoic acid derivative used as a flavoring agent. The objective of this study was to determine whether vanillic acid has beneficial effects against dextran sulfate sodium (DSS)-induced ulcerative colitis. Our results showed that [...] Read more.
Vanillic acid, an oxidized form of vanillin, is a benzoic acid derivative used as a flavoring agent. The objective of this study was to determine whether vanillic acid has beneficial effects against dextran sulfate sodium (DSS)-induced ulcerative colitis. Our results showed that vanillic acid reduced the severity of the clinical signs of DSS-induced colitis, including weight loss and shortening of colon length, and the disease activity index. The results of this study showed that vanillic acid significantly suppressed the expression of cyclooxygenase-2 and the activation of transcription nuclear factor-kB p65 in DSS-treated colon tissues. In addition, we observed that the plasma levels of interleukin (IL)-6 were higher in the DSS-treated group than in the control group, but these increased levels were reduced by the administration of vanillic acid. Taken together, these findings suggest that vanillic acid has a beneficial effect on DSS-induced ulcerative colitis, thereby indicating its usefulness in the regulation of chronic intestinal inflammation. Full article
Open AccessArticle Anthraquinones with Antiplasmodial Activity from the Roots of Rennellia elliptica Korth. (Rubiaceae)
Molecules 2010, 15(10), 7218-7226; doi:10.3390/molecules15107218
Received: 24 August 2010 / Revised: 6 October 2010 / Accepted: 11 October 2010 / Published: 20 October 2010
Cited by 16 | PDF Full-text (222 KB)
Abstract
Dichloromethane root extract of Rennellia elliptica Korth. showed strong inhibition of Plasmodium falciparum growth in vitro with an IC50 value of 4.04 µg/mL. A phytochemical study of the dichloromethane root extract has led to the isolation and characterization of a new [...] Read more.
Dichloromethane root extract of Rennellia elliptica Korth. showed strong inhibition of Plasmodium falciparum growth in vitro with an IC50 value of 4.04 µg/mL. A phytochemical study of the dichloromethane root extract has led to the isolation and characterization of a new anthraquinone, 1,2-dimethoxy-6-methyl-9,10-anthraquinone (1), and ten known anthraquinones: 1-hydroxy-2-methoxy-6-methyl-9,10-anthraquinone (2), nordamnacanthal (3), 2-formyl-3-hydroxy-9,10-anthraquinone (4), damnacanthal (5), lucidin-ω-methyl ether (6), 3-hydroxy-2-methyl-9,10-anthraquinone (7), rubiadin (8), 3-hydroxy-2-methoxy-6-methyl-9,10-anthraquinone (9), rubiadin-1-methyl ether (10) and 3-hydroxy-2-hydroxymethyl-9,10-anthraquinone (11). Structural elucidation of all compounds was accomplished by modern spectroscopic methods, notably 1D and 2D NMR, IR, UV and HREIMS. The new anthraquinone 1, 2-formyl-3-hydroxy-9,10-anthraquinone (4) and 3-hydroxy-2-methyl-9,10-anthraquinone (7) possess strong antiplasmodial activity, with IC50 values of 1.10, 0.63 and 0.34 µM, respectively. Full article
(This article belongs to the Section Natural Products)
Open AccessCommunication Efficient Microwave-Assisted Synthesis of 5-Deazaflavine Derivatives
Molecules 2010, 15(10), 7227-7234; doi:10.3390/molecules15107227
Received: 16 September 2010 / Revised: 30 September 2010 / Accepted: 3 October 2010 / Published: 20 October 2010
Cited by 2 | PDF Full-text (174 KB)
Abstract A series of pyrimido[4,5-b]quinolines  (5-deazaflavines), were synthesized by microwave assisted intramolecular cyclization. The N4-substituted-2,4-diamino-6-chloro-pyrimidine-5-carbaldehydes, were prepared by selective monoamination of 2-amino-4,6-dichloropyrimidine-5-carbaldehyde with aliphatic and aromatic amines. Full article
(This article belongs to the Section Organic Synthesis)
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Open AccessArticle Antioxidant-Prooxidant Properties of a New Organoselenium Compound Library
Molecules 2010, 15(10), 7292-7312; doi:10.3390/molecules15107292
Received: 21 September 2010 / Revised: 18 October 2010 / Accepted: 20 October 2010 / Published: 21 October 2010
Cited by 33 | PDF Full-text (686 KB)
Abstract
The present study describes the biological evaluation of a library of 59 organo-selenium compounds as superoxide (O2) generators and cytotoxic agents in human prostate cancer cells (PC-3) and in breast adenocarcinoma (MCF-7). In order to corroborate that the biological [...] Read more.
The present study describes the biological evaluation of a library of 59 organo-selenium compounds as superoxide (O2) generators and cytotoxic agents in human prostate cancer cells (PC-3) and in breast adenocarcinoma (MCF-7). In order to corroborate that the biological activity for selenium compounds depends on the chemical form, a broad structural variety is presented. These structures include selenocyanates, diselenides, selenoalkyl functional moieties and eight newly synthesized symmetrically substituted dithioselenites and selenylureas. Eleven of the derivatives tested showed high levels of superoxide generation in vitro via oxidation of reduced glutathione (GSH) and nine of them were more catalytic than the reference compound, diselenodipropionic acid. Eighteen of the library compounds inhibited cell growth more than or similar to reference chemotherapeutic drugs in PC-3 and eleven were more potent cytotoxic agents than etoposide in the MCF-7 cell line. Considering both parameters (superoxide generation and cell cytotoxicity) compounds B1, C6 and C9 displayed the best therapeutic profiles. Considering that many diselenide compounds can generate superoxide (O2) in vitro via oxidation of GSH and other thiols, the analogue B1, that contains a diselenide moiety, was selected for a preliminary mechanistic investigation, which . revealed that B1 has apoptogenic effects similar to camptothecin mediated by reactive oxygen species (ROS) in lymphocytic leukemia cells (CCRF-CEM) and affected the MCF-7 cell-cycle in G2/M and S-phases. Full article
(This article belongs to the Special Issue Antioxidants)
Open AccessArticle Tetrabutylammonium Bromide Media Aza-Michael Addition of 1,2,3,6-Tetrahydrophthalimide to Symmetrical Fumaric Esters and Acrylic Esters under Solvent-Free Conditions
Molecules 2010, 15(10), 7353-7362; doi:10.3390/molecules15107353
Received: 19 September 2010 / Revised: 11 October 2010 / Accepted: 11 October 2010 / Published: 21 October 2010
Cited by 6 | PDF Full-text (184 KB)
Abstract
The aza-Michael addition of 1,2,3,6-tetrahydrophthalimide with symmetrical fumaric esters has been performed efficiently in a solvent-free system at 100 °C and using 1,4-diazabicyclo[2.2.2]octane (DABCO) as a base in the presence of tetrabutylammonium bromide (TBAB). The products were obtained in good to high [...] Read more.
The aza-Michael addition of 1,2,3,6-tetrahydrophthalimide with symmetrical fumaric esters has been performed efficiently in a solvent-free system at 100 °C and using 1,4-diazabicyclo[2.2.2]octane (DABCO) as a base in the presence of tetrabutylammonium bromide (TBAB). The products were obtained in good to high yields within 2.5-7.0 h. This reaction worked well on linear alkyl fumarates and was not effective with nonlinear alkyl fumarates. Although the reaction was also applicable to acrylates such as n-butyl acrylate, methacrylates and crotonates were not suitable Michael acceptors for this reaction. Full article
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Open AccessArticle Chemometric Studies on Natural Products as Potential Inhibitors of the NADH Oxidase from Trypanosoma cruzi Using the VolSurf Approach
Molecules 2010, 15(10), 7363-7377; doi:10.3390/molecules15107363
Received: 16 September 2010 / Revised: 5 October 2010 / Accepted: 11 October 2010 / Published: 21 October 2010
Cited by 19 | PDF Full-text (667 KB)
Abstract
Natural products have widespread biological activities, including inhibition of mitochondrial enzyme systems. Some of these activities, for example cytotoxicity, may be the result of alteration of cellular bioenergetics. Based on previous computer-aided drug design (CADD) studies and considering reported data on structure-activity [...] Read more.
Natural products have widespread biological activities, including inhibition of mitochondrial enzyme systems. Some of these activities, for example cytotoxicity, may be the result of alteration of cellular bioenergetics. Based on previous computer-aided drug design (CADD) studies and considering reported data on structure-activity relationships (SAR), an assumption regarding the mechanism of action of natural products against parasitic infections involves the NADH-oxidase inhibition. In this study, chemometric tools, such as: Principal Component Analysis (PCA), Consensus PCA (CPCA), and partial least squares regression (PLS), were applied to a set of forty natural compounds, acting as NADH-oxidase inhibitors. The calculations were performed using the VolSurf+ program. The formalisms employed generated good exploratory and predictive results. The independent variables or descriptors having a hydrophobic profile were strongly correlated to the biological data. Full article
(This article belongs to the Special Issue Phenolics and Polyphenolics)
Open AccessArticle Synthesis, Gastroprotective Effect and Cytotoxicity of New Amino Acid Diterpene Monoamides and Diamides
Molecules 2010, 15(10), 7378-7394; doi:10.3390/molecules15107378
Received: 9 August 2010 / Revised: 5 October 2010 / Accepted: 14 October 2010 / Published: 21 October 2010
Cited by 6 | PDF Full-text (212 KB)
Abstract
Following our studies on the gastroprotective effect and cytotoxicity of terpene derivatives, new amides were prepared from the diterpene 8(17)-labden-15,19-dioic acid (junicedric acid) and its 8(9)-en isomer with C-protected amino acids (amino acid esters). The new compounds were evaluated for their gastroprotective [...] Read more.
Following our studies on the gastroprotective effect and cytotoxicity of terpene derivatives, new amides were prepared from the diterpene 8(17)-labden-15,19-dioic acid (junicedric acid) and its 8(9)-en isomer with C-protected amino acids (amino acid esters). The new compounds were evaluated for their gastroprotective effect in the ethanol/HCl-induced gastric lesions model in mice, as well as for cytotoxicity using the following human cell lines: normal lung fibroblasts (MRC-5), gastric adenocarcinoma cells (AGS) and liver hepatocellular carcinoma (Hep G2). A dose-response experiment showed that at 25 mg/kg the C-15 leucyl and C-15,19-dileucylester amides of junicedric acid reduced gastric lesions by about 65.6 and 49.6%, respectively, with an effect comparable to lansoprazole at 20 mg/kg (79.3% lesion reduction). The comparison of the gastroprotective effect of 18 new amino acid ester amides was carried out at a single oral dose of 25 mg/kg. Several compounds presented a strong gastroprotective effect, reducing gastric lesions in the 70.9-87.8% range. The diprolyl derivative of junicedric acid, the most active product of this study (87.8% lesion reduction at 25 mg/kg) presented a cytotoxicity value comparable with that of the reference compound lansoprazole. The structure-activity relationships are discussed. Full article
(This article belongs to the Section Medicinal Chemistry)
Open AccessArticle Antibacterial Activity of Phytochemicals Isolated from Atractylodes japonica against Methicillin-Resistant Staphylococcus aureus
Molecules 2010, 15(10), 7395-7402; doi:10.3390/molecules15107395
Received: 7 September 2010 / Accepted: 19 October 2010 / Published: 21 October 2010
Cited by 11 | PDF Full-text (304 KB)
Abstract
Methicillin-resistant Staphylococcus aureus (MRSA) has been emerging worldwide as one of the most important problems in communities and hospitals. Therefore, new agents are needed to treat acute oral infections from MRSA. In this study, antibacterial compounds from the roots of Atractylodes japonica [...] Read more.
Methicillin-resistant Staphylococcus aureus (MRSA) has been emerging worldwide as one of the most important problems in communities and hospitals. Therefore, new agents are needed to treat acute oral infections from MRSA. In this study, antibacterial compounds from the roots of Atractylodes japonica (A. japonica) were isolated and characterized. The compounds were isolated from the root extracts using HPLC-piloted activity-guided fractionations. Four A. japonica compounds were isolated and identified as atractylenolide III (1), atractylenolide I (2), diacetylatractylodiol [(6E,12E)-tetradeca-6,12-diene-8,10-diyne-1,3-diol diacetate, TDEYA, 3). and (6E,12E)-tetradecadiene-8,10-diyne-1,3-diol (TDEA, 4), which was obtained by hydrolysis of TDEYA. The minimum inhibitory concentrations (MICs) was determined in the setting of clinical MRSA isolates. Compound 4 showed anti-MRSA activity with a MIC value of 4-32 μg/mL. The overall results provide promising baseline information for the potential use of the extract of A. japonica as well as some of the isolated compounds in the treatment of bacterial infections. Full article
(This article belongs to the collection Bioactive Compounds)
Open AccessArticle The Pharmacological Effects of Morroniside and Loganin Isolated from Liuweidihuang Wan, on MC3T3-E1 Cells
Molecules 2010, 15(10), 7403-7414; doi:10.3390/molecules15107403
Received: 6 September 2010 / Revised: 18 October 2010 / Accepted: 19 October 2010 / Published: 21 October 2010
Cited by 10 | PDF Full-text (292 KB)
Abstract
Liuweidihuang Wan (LW), initially a well-known formula for curing “wu chi wu ruan”, is commonly used nowadays for clinical treatment of Postmenopausal Osteoporosis (PO), but the identity of the effective substance(s) remains unclear. The present study was designed to evaluate the effects [...] Read more.
Liuweidihuang Wan (LW), initially a well-known formula for curing “wu chi wu ruan”, is commonly used nowadays for clinical treatment of Postmenopausal Osteoporosis (PO), but the identity of the effective substance(s) remains unclear. The present study was designed to evaluate the effects of morroniside and loganin isolated from LW on the proliferation, differentiation and apoptosis of MC3T3-E1 cells, as well as the possible mechanism of action. Morroniside and loganin had no effects on the proliferation of MC3T3-E1 cells, but both susbtances could improve the activity of alkaline phosphatase (ALP), and increase the contents of collagen type I and osteocalcin. Simultaneously, the mRNA expression of caspase-3, capase-9, RANKL was down-regulated and that of bcl-2 was up-regulated, which partially explains the anti-osteoporosis mechanism in MC3T3-E1 cells. In conclusion, morroniside and loganin may directly promote the differentiation and inhibit the apoptosis of MC3T3-E1 cells, and accordingly indirectly reduce bone resorption, which makes them promising natural drugs leads for treating PO in the near future. Full article
Open AccessArticle Evaluation on Anti-hepatitis Viral Activity of Vitis vinifer L
Molecules 2010, 15(10), 7415-7422; doi:10.3390/molecules15107415
Received: 20 August 2010 / Revised: 15 October 2010 / Accepted: 19 October 2010 / Published: 22 October 2010
Cited by 6 | PDF Full-text (199 KB)
Abstract
Suosuo grape (Vitis vinifer L) is traditionally used as a therapeutic agent for measles and hepatitis by the ethnic Uighurs. This work aimed to investigate the anti-HBV effect of total triterpene (VTT), total flavonoids (VTF) and total polysaccharides (VTP) from Suosuo [...] Read more.
Suosuo grape (Vitis vinifer L) is traditionally used as a therapeutic agent for measles and hepatitis by the ethnic Uighurs. This work aimed to investigate the anti-HBV effect of total triterpene (VTT), total flavonoids (VTF) and total polysaccharides (VTP) from Suosuo grape, and their synergistic effects were also tested. The viral antigens of cellular secretion, HBsAg and HBeAg, were determined by enzyme linked immunosorbent assay (ELISA).The quantity of HBV-DNA released in the supernatant was assayed by real-time PCR. It was found that it effectively suppressed the secretion of HBsAg and HBeAg from HepG2.2.15 cells in a dose-dependent manner, as well as the HBV DNA. The results of orthogonal design experiment showed that the combination of VTT 20 μg/mL, VTF 50 μg/mL and VTP 50 μg/mL had the best optimistic inhibitory effects on HBeAg secretion. Full article
Open AccessArticle One-Pot Synthesis of 2,3,4-Triarylquinolines via Suzuki-Miyaura Cross-Coupling of 2-Aryl-4-chloro-3-iodoquinolines with Arylboronic Acids
Molecules 2010, 15(10), 7423-7437; doi:10.3390/molecules15107423
Received: 16 September 2010 / Revised: 12 October 2010 / Accepted: 18 October 2010 / Published: 22 October 2010
Cited by 6 | PDF Full-text (226 KB)
Abstract Palladium–catalyzed Suzuki cross-coupling of 2-aryl-4-chloro-3-iodoquinolines with excess arylboronic acids (2.5 equiv.) in the presence of tricyclohexylphosphine afforded the 2,3,4-triarylquinolines in one-pot operation. The incipient 2,3-diaryl-4-chloroquinolines were also prepared and transformed to the primary 4-amino-2,3-diarylquinolines and 2,3-diarylquinolin-4(1H)-ones. Full article
Open AccessArticle Prenylated Xanthones from the Bark of Garcinia xanthochymus and Their 1,1-Diphenyl-2-picrylhydrazyl (DPPH) Radical Scavenging Activities
Molecules 2010, 15(10), 7438-7449; doi:10.3390/molecules15107438
Received: 25 September 2010 / Revised: 7 October 2010 / Accepted: 11 October 2010 / Published: 22 October 2010
Cited by 9 | PDF Full-text (244 KB)
Abstract
Garcinia xanthochymus has been widely used in traditional Chinese medicine for expelling worms and removing food toxins. Bioassay-guided fractionation of an EtOAc-soluble extract of G. xanthochymus stem bark led to the isolation of six new xanthones. Their structures were elucidated by spectroscopic [...] Read more.
Garcinia xanthochymus has been widely used in traditional Chinese medicine for expelling worms and removing food toxins. Bioassay-guided fractionation of an EtOAc-soluble extract of G. xanthochymus stem bark led to the isolation of six new xanthones. Their structures were elucidated by spectroscopic methods, especially 2D-NMR techniques. Free-radical-scavenging activities of the isolated compounds were elucidated through DPPH method. Most of the isolated compounds showed considerable free radical scavenging activity on DPPH assay. Compound 1 exhibited effective antioxidant scavenging activity against DPPH radical with an IC50 value of 19.64 μM, and compound 6 showed the lowest activity among all the tested molecules, with an IC50 value of 66.88 μM. These findings support the notion that the plant genus Garcinia is a good source of bioactive compounds. Full article
(This article belongs to the Section Natural Products)
Open AccessArticle Creation of a Databank for Content of Antioxidants in Food Products by an Amperometric Method
Molecules 2010, 15(10), 7450-7466; doi:10.3390/molecules15107450
Received: 20 September 2010 / Accepted: 20 October 2010 / Published: 22 October 2010
Cited by 4 | PDF Full-text (181 KB)
Abstract
Oxidative stress, i.e. excessive content of reactionary, oxygen, and nitrogen compounds (ROAC), including free radicals, is one of the causes of various dangerous diseases as well as premature aging. The adverse effect of free radicals can be neutralized by antioxidants. In order [...] Read more.
Oxidative stress, i.e. excessive content of reactionary, oxygen, and nitrogen compounds (ROAC), including free radicals, is one of the causes of various dangerous diseases as well as premature aging. The adverse effect of free radicals can be neutralized by antioxidants. In order to carry out antioxidant therapy, one needs to know the contents of antioxidants in food products. We have created the databank for the contents of antioxidants in 1,140 food products, beverages, etc. Apart from water-soluble antioxidants, fat-soluble antioxidants in dairy and fish products, cacao, chocolate, nuts etc. were determined for the first time using an amperometric method. Full article
Open AccessArticle A New Natural Ceramide from Trollius chinensis Bunge
Molecules 2010, 15(10), 7467-7471; doi:10.3390/molecules15107467
Received: 16 August 2010 / Revised: 20 September 2010 / Accepted: 18 October 2010 / Published: 25 October 2010
Cited by 6 | PDF Full-text (137 KB)
Abstract A new natural product named trolliamide was isolated from Trollius chinensis Bunge. Its structure was determined as 2-hydroxy-tetracosanoic acid(2,3-dihydroxy-1-hydroxymethyl-heptadec-7-enyl)-amide by spectroscopic methods, including UV, IR, MS and NMR. This is the first report of a ceramide isolated from Trollius chinensis. Full article
Open AccessArticle Synthesis of Novel 1-[(2,6-Dichloro-4-trifluoromethyl)phenyl]-3-aryl-1H-pyrazole-4-carbaldehydes
Molecules 2010, 15(10), 7472-7481; doi:10.3390/molecules15107472
Received: 7 September 2010 / Revised: 29 September 2010 / Accepted: 2 October 2010 / Published: 25 October 2010
Cited by 10 | PDF Full-text (117 KB)
Abstract A series of novel 1-[(2,6-dichloro-4-trifluoromethyl)phenyl]-3-aryl-1H-pyrazole-4-carbaldehydes 6a-i were synthesized using the Vilsmeier-Haack reagent. The structures of all the title compounds have been confirmed by elemental analysis, 1H-NMR and 13C-NMR and in addition, the structure of intermediate 5b was investigated by X-ray crystallography. Full article
Open AccessArticle Lead Contamination in Selected Foods from Riyadh City Market and Estimation of the Daily Intake
Molecules 2010, 15(10), 7482-7497; doi:10.3390/molecules15107482
Received: 29 August 2010 / Revised: 7 October 2010 / Accepted: 11 October 2010 / Published: 25 October 2010
Cited by 14 | PDF Full-text (224 KB)
Abstract
This study was carried out to determine lead contamination in 104 of the representative food items in the Saudi diet and to estimate the dietary lead intake of Saudi Arabians. Three samples of each selected food items were purchased from the local [...] Read more.
This study was carried out to determine lead contamination in 104 of the representative food items in the Saudi diet and to estimate the dietary lead intake of Saudi Arabians. Three samples of each selected food items were purchased from the local markets of Riyadh city, the capital of Saudi Arabia. Each pooled sample was analyzed in triplicate by ICP-AES after thorough homogenization. Sweets (0.011–0.199 μg/g), vegetables (0.002–0.195 μg/g), legumes (0.014–0.094 μg/g), eggs (0.079 μg/g), meat and meat products (0.013–0.068 μg/g) were the richest sources of lead. Considering the amounts of each food consumed, the major food sources of lead intake for Saudi can be arranged as follows: vegetables (25.4%), cereal and cereal products (24.2%), beverages (9.7%) sweets (8.2%), legumes (7.4%), fruits (5.4%) milk and milk products (5.1%). The daily intake of lead was calculated taking into account the concentration of this element in the edible part of the daily consumption data which were derived from two sources, (a) the KSA food sheet provided by the Food and Agriculture Organization (FAO) and (b) from questionnaires distributed among 300 families in Riyadh city. The results showed that the daily intakes of lead according to the two sources are 22.7 and 24.5 μg/person/day respectively, which are lower than that mentioned by The Joint Expert Committee on Food Additives (JECFA), whereas it is comprabale with that of other countries. Full article
Open AccessArticle Synthesis of New Azo Compounds Based on N-(4-Hydroxypheneyl)maleimide and N-(4-Methylpheneyl)maleimide
Molecules 2010, 15(10), 7498-7508; doi:10.3390/molecules15107498
Received: 1 October 2010 / Revised: 14 October 2010 / Accepted: 18 October 2010 / Published: 25 October 2010
Cited by 12 | PDF Full-text (502 KB)
Abstract
Maleic anhydride was reacted with p-aminophenol and p-toluidine in the presence of di-phosphorus pentoxide (P2O5) as a catalyst to produce two compounds: N-(4-hydroxy-phenyl)maleimide (I) and N-(4-methylphenyl)maleimide (II). The new azo [...] Read more.
Maleic anhydride was reacted with p-aminophenol and p-toluidine in the presence of di-phosphorus pentoxide (P2O5) as a catalyst to produce two compounds: N-(4-hydroxy-phenyl)maleimide (I) and N-(4-methylphenyl)maleimide (II). The new azo compounds I(a-c) and II(a-c) were prepared by the reaction of I and II with three different aromatic amines, namely aniline, p-aminophenol and p-toluidine. The structures of these compounds were confirmed by CHN, FT-IR, 1H-NMR, 13C-NMR, mass spectrum and UV/Vis spectroscopy. Full article

Review

Jump to: Research

Open AccessReview Stem Cells for the Treatment of Neurodegenerative Diseases
Molecules 2010, 15(10), 6743-6758; doi:10.3390/molecules15106743
Received: 13 August 2010 / Revised: 6 September 2010 / Accepted: 8 September 2010 / Published: 27 September 2010
Cited by 5 | PDF Full-text (116 KB)
Abstract
Neurodegenerative diseases are characterized by neurodegenerative changes or apoptosis of neurons involved in networks, leading to permanent paralysis and loss of sensation below the site of the injury. Cell replacement therapy has provided the basis for the development of potentially powerful new [...] Read more.
Neurodegenerative diseases are characterized by neurodegenerative changes or apoptosis of neurons involved in networks, leading to permanent paralysis and loss of sensation below the site of the injury. Cell replacement therapy has provided the basis for the development of potentially powerful new therapeutic strategies for a broad spectrum of human neurological diseases. In recent years, neurons and glial cells have successfully been generated from stem cells, and extensive efforts by investigators to develop stem cell-based brain transplantation therapies have been carried out. We review here notable previously published experimental and preclinical studies involving stem cell-based cell for neurodegenerative diseases and discuss the future prospects for stem cell therapy of neurological disorders in the clinical setting. Steady and solid progress in stem cell research in both basic and preclinical settings should support the hope for development of stem cell-based cell therapies for neurological diseases. Full article
Open AccessReview The Roles of Phytochemicals in Bronchial Asthma
Molecules 2010, 15(10), 6810-6834; doi:10.3390/molecules15106810
Received: 9 August 2010 / Revised: 16 September 2010 / Accepted: 30 September 2010 / Published: 4 October 2010
Cited by 8 | PDF Full-text (324 KB)
Abstract
Despite gaps in our knowledge of how phytochemicals interfere with cellular functions, several natural plant products are utilized to prevent or treat a wide range of diseases. Identification of an agent with therapeutic potential requires multiple steps involving in vitro studies, efficacy [...] Read more.
Despite gaps in our knowledge of how phytochemicals interfere with cellular functions, several natural plant products are utilized to prevent or treat a wide range of diseases. Identification of an agent with therapeutic potential requires multiple steps involving in vitro studies, efficacy and toxicity studies in animal models, and then human clinical trials. This review provides a brief introduction on natural products that may help to treat and/or prevent bronchial asthma and describes our current understanding of their molecular mechanisms based on various in vitro, in vivo, and clinical studies. We focus on the anti-inflammatory and anti-vascular actions of the plant products and other roles beyond the anti-oxidative effects. Full article
(This article belongs to the Special Issue Antioxidants)
Open AccessReview Dealing with Misfolded Proteins: Examining the Neuroprotective Role of Molecular Chaperones in Neurodegeneration
Molecules 2010, 15(10), 6859-6887; doi:10.3390/molecules15106859
Received: 19 August 2010 / Revised: 6 September 2010 / Accepted: 8 September 2010 / Published: 8 October 2010
Cited by 21 | PDF Full-text (2865 KB)
Abstract
Human neurodegenerative diseases arise from a wide array of genetic and environmental factors. Despite the diversity in etiology, many of these diseases are considered "conformational" in nature, characterized by the accumulation of pathological, misfolded proteins. These misfolded proteins can induce cellular stress [...] Read more.
Human neurodegenerative diseases arise from a wide array of genetic and environmental factors. Despite the diversity in etiology, many of these diseases are considered "conformational" in nature, characterized by the accumulation of pathological, misfolded proteins. These misfolded proteins can induce cellular stress by overloading the proteolytic machinery, ultimately resulting in the accumulation and deposition of aggregated protein species that are cytotoxic. Misfolded proteins may also form aberrant, non-physiological protein-protein interactions leading to the sequestration of other normal proteins essential for cellular functions. The progression of such disease may therefore be viewed as a failure of normal protein homeostasis, a process that involves a network of molecules regulating the synthesis, folding, translocation and clearance of proteins. Molecular chaperones are highly conserved proteins involved in the folding of nascent proteins, and the repair of proteins that have lost their typical conformations. These functions have therefore made molecular chaperones an active area of investigation within the field of conformational diseases. This review will discuss the role of molecular chaperones in neurodegenerative diseases, highlighting their functional classification, regulation, and therapeutic potential for such diseases. Full article
(This article belongs to the Special Issue Neuroprotective Strategies)
Open AccessReview Natural Antioxidants: Fascinating or Mythical Biomolecules?
Molecules 2010, 15(10), 6905-6930; doi:10.3390/molecules15106905
Received: 26 August 2010 / Revised: 9 September 2010 / Accepted: 14 September 2010 / Published: 8 October 2010
Cited by 87 | PDF Full-text (327 KB)
Abstract
Research on the use, properties, characteristics and sources of antioxidants especially phenolic compounds, flavonoids, vitamins, synthetic chemicals and some micronutrients began in the late 18th century. Since then antioxidant research has received considerable attention and over a hundred thousand papers have [...] Read more.
Research on the use, properties, characteristics and sources of antioxidants especially phenolic compounds, flavonoids, vitamins, synthetic chemicals and some micronutrients began in the late 18th century. Since then antioxidant research has received considerable attention and over a hundred thousand papers have been published on the subject. This has led to a rampant use of antioxidants in order to try to obtain and preserve optimal health. A number of nutraceuticals and food supplements are frequently fortified with synthetic or natural antioxidants. However, some research outcomes have led to the belief that antioxidants exist as mythical biomolecules. This review provides a critical evaluation of some common in vitro antioxidant capacity methods, and a discussion on the role and controversies surrounding non-enzymatic biomolecules, in particular phenolic compounds and non-phenolic compounds, in oxidative processes in an attempt of stemming the tidal wave that is threatening to swamp the concept of natural antioxidants. Full article
(This article belongs to the Special Issue Antioxidants)
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Open AccessReview Cherry Antioxidants: From Farm to Table
Molecules 2010, 15(10), 6993-7005; doi:10.3390/molecules15106993
Received: 10 August 2010 / Revised: 29 September 2010 / Accepted: 11 October 2010 / Published: 12 October 2010
Cited by 49 | PDF Full-text (216 KB)
Abstract
The dietary consumption of fruits and vegetables is associated with a lower incidence of degenerative diseases such as cardiovascular disease and certain types of cancers. Most recent interest has focused on the bioactive phenolic compounds found in vegetable products. Sweet and sour [...] Read more.
The dietary consumption of fruits and vegetables is associated with a lower incidence of degenerative diseases such as cardiovascular disease and certain types of cancers. Most recent interest has focused on the bioactive phenolic compounds found in vegetable products. Sweet and sour cherries contain several antioxidants and polyphenols that possess many biological activities, such as antioxidant, anticancer and anti-inflammation properties. The review describes the effect of environment and other factors (such as production, handling and storage) on the nutritional properties of cherries, with particular attention to polyphenol compounds. Moreover the health benefits of cherries and their polyphenols against human diseases such as heart disease, cancers, diabetes are reviewed. Full article
(This article belongs to the Special Issue Antioxidants)
Open AccessReview Potential of the Dietary Antioxidants Resveratrol and Curcumin in Prevention and Treatment of Hematologic Malignancies
Molecules 2010, 15(10), 7035-7074; doi:10.3390/molecules15107035
Received: 6 September 2010 / Revised: 2 October 2010 / Accepted: 11 October 2010 / Published: 12 October 2010
Cited by 53 | PDF Full-text (793 KB)
Abstract
Despite considerable improvements in the tolerance and efficacy of novel chemotherapeutic agents, the mortality of hematological malignancies is still high due to therapy relapse, which is associated with bad prognosis. Dietary polyphenolic compounds are of growing interest as an alternative approach, especially [...] Read more.
Despite considerable improvements in the tolerance and efficacy of novel chemotherapeutic agents, the mortality of hematological malignancies is still high due to therapy relapse, which is associated with bad prognosis. Dietary polyphenolic compounds are of growing interest as an alternative approach, especially in cancer treatment, as they have been proven to be safe and display strong antioxidant properties. Here, we provide evidence that both resveratrol and curcumin possess huge potential for application as both chemopreventive agents and anticancer drugs and might represent promising candidates for future treatment of leukemia. Both polyphenols are currently being tested in clinical trials. We describe the underlying mechanisms, but also focus on possible limitations and how they might be overcome in future clinical use – either by chemically synthesized derivatives or special formulations that improve bioavailability and pharmacokinetics. Full article
(This article belongs to the Special Issue Antioxidants)
Open AccessReview Bignoniaceae Metabolites as Semiochemicals
Molecules 2010, 15(10), 7090-7105; doi:10.3390/molecules15107090
Received: 5 August 2010 / Revised: 7 September 2010 / Accepted: 22 September 2010 / Published: 14 October 2010
Cited by 8 | PDF Full-text (77 KB)
Abstract
Members of the family Bignoniaceae are mostly found in tropical and neo-tropical regions in America, Asia and Africa, although some of them are cultivated in other regions as ornamentals. Species belonging to this family have been extensively studied in regard to their [...] Read more.
Members of the family Bignoniaceae are mostly found in tropical and neo-tropical regions in America, Asia and Africa, although some of them are cultivated in other regions as ornamentals. Species belonging to this family have been extensively studied in regard to their pharmacological properties (as extracts and isolated compounds). The aim of this review is to summarize the reported scientific evidence about the chemical properties as well as that of the extracts and isolated compounds from species of this family, focusing mainly in insect-plant interactions. As it is known, this family is recognized for the presence of iridoids which are markers of oviposition and feeding preference to species which have became specialist feeders. Some herbivore species have also evolved to the point of been able to sequester iridoids and use them as defenses against their predators. However, iridoids also exhibit anti-insect properties, and therefore they may be good lead molecules to develop botanical pesticides. Other secondary metabolites, such as quinones, and whole extracts have also shown potential as anti-insect agents. Full article
(This article belongs to the Special Issue Phytochemicals with Signaling, Medicinal and Therapeutic Properties)
Open AccessReview Role of Oxidant Scavengers in the Prevention of Ca2+ Homeostasis Disorders
Molecules 2010, 15(10), 7167-7187; doi:10.3390/molecules15107167
Received: 1 July 2010 / Revised: 9 September 2010 / Accepted: 14 October 2010 / Published: 15 October 2010
Cited by 13 | PDF Full-text (173 KB)
Abstract
A number of disorders, such as Alzheimer disease and diabetes mellitus, have in common the alteration of the redox balance, resulting in an increase in reactive oxygen species (ROS) generation that might lead to the development of apoptosis and cell death. It [...] Read more.
A number of disorders, such as Alzheimer disease and diabetes mellitus, have in common the alteration of the redox balance, resulting in an increase in reactive oxygen species (ROS) generation that might lead to the development of apoptosis and cell death. It has long been known that ROS can significantly alter Ca2+ mobilization, an intracellular signal that is involved in the regulation of a wide variety of cellular functions. Cells have a limited capability to counteract the effects of oxidative stress, but evidence has been provided supporting the beneficial effects of exogenous ROS scavengers. Here, we review the effects of oxidative stress on intracellular Ca2+ homeostasis and the role of antioxidants in the prevention and treatment of disorders associated to abnormal Ca2+ mobilization induced by ROS. Full article
(This article belongs to the Special Issue Antioxidants)
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Open AccessReview Protecting Groups in Carbohydrate Chemistry: Influence on Stereoselectivity of Glycosylations
Molecules 2010, 15(10), 7235-7265; doi:10.3390/molecules15107235
Received: 5 September 2010 / Accepted: 15 October 2010 / Published: 20 October 2010
Cited by 38 | PDF Full-text (1029 KB)
Abstract
Saccharides are polyhydroxy compounds, and their synthesis requires complex protecting group manipulations. Protecting groups are usually used to temporarily mask a functional group which may interfere with a certain reaction, but protecting groups in carbohydrate chemistry do more than protecting groups usually [...] Read more.
Saccharides are polyhydroxy compounds, and their synthesis requires complex protecting group manipulations. Protecting groups are usually used to temporarily mask a functional group which may interfere with a certain reaction, but protecting groups in carbohydrate chemistry do more than protecting groups usually do. Particularly, protecting groups can participate in reactions directly or indirectly, thus affecting the stereochemical outcomes, which is important for synthesis of oligosaccharides. Herein we present an overview of recent advances in protecting groups influencing stereoselectivity in glycosylation reactions, including participating protecting groups, and conformation-constraining protecting groups in general. Full article
(This article belongs to the Special Issue Protecting Group in Organic Synthesis)
Open AccessReview The Nrf2 System as a Potential Target for the Development of Indirect Antioxidants
Molecules 2010, 15(10), 7266-7291; doi:10.3390/molecules15107266
Received: 19 September 2010 / Revised: 18 October 2010 / Accepted: 20 October 2010 / Published: 20 October 2010
Cited by 120 | PDF Full-text (1002 KB)
Abstract
Oxidative stress causes damage to multiple cellular components such as DNA, proteins, and lipids, and is implicated in various human diseases including cancer, neurodegeneration, inflammatory diseases, and aging. In response to oxidative attack, cells have developed an antioxidant defense system to maintain [...] Read more.
Oxidative stress causes damage to multiple cellular components such as DNA, proteins, and lipids, and is implicated in various human diseases including cancer, neurodegeneration, inflammatory diseases, and aging. In response to oxidative attack, cells have developed an antioxidant defense system to maintain cellular redox homeostasis and to protect cells from damage. The thiol-containing small molecules (e.g. glutathione), reactive oxygen species-inactivating enzymes (e.g. glutathione peroxidase), and phase 2 detoxifying enzymes (e.g. NAD(P)H: quinine oxidoreductase 1 and glutathione-S-transferases) are members of this antioxidant system. NF-E2-related factor 2 (Nrf2) is a CNC-bZIP transcription factor which regulates the basal and inducible expression of a wide array of antioxidant genes. Following dissociation from the cytosolic protein Keap1, a scaffolding protein which binds Nrf2 and Cul3 ubiquitin ligase for proteasome degradation, Nrf2 rapidly accumulates in the nucleus and transactivates the antioxidant response element in the promoter region of many antioxidant genes. The critical role of Nrf2 has been demonstrated by various animal studies showing that mice with a targeted disruption of the nrf2 gene are prone to develop lesions in response to environmental toxicants/carcinogens, drugs, and inflammatory insults. In this review, we discuss the role of the Nrf2 system, with particular focus on Nrf2-controlled target genes and the potential pleiotropic effects of Nrf2 activation of indirect antioxidants. Full article
(This article belongs to the Special Issue Antioxidants)
Open AccessReview Plant Phenolics: Extraction, Analysis and Their Antioxidant and Anticancer Properties
Molecules 2010, 15(10), 7313-7352; doi:10.3390/molecules15107313
Received: 10 September 2010 / Revised: 15 October 2010 / Accepted: 19 October 2010 / Published: 21 October 2010
Cited by 553 | PDF Full-text (441 KB)
Abstract
Phenolics are broadly distributed in the plant kingdom and are the most abundant secondary metabolites of plants. Plant polyphenols have drawn increasing attention due to their potent antioxidant properties and their marked effects in the prevention of various oxidative stress associated diseases [...] Read more.
Phenolics are broadly distributed in the plant kingdom and are the most abundant secondary metabolites of plants. Plant polyphenols have drawn increasing attention due to their potent antioxidant properties and their marked effects in the prevention of various oxidative stress associated diseases such as cancer. In the last few years, the identification and development of phenolic compounds or extracts from different plants has become a major area of health- and medical-related research. This review provides an updated and comprehensive overview on phenolic extraction, purification, analysis and quantification as well as their antioxidant properties. Furthermore, the anticancer effects of phenolics in-vitro and in-vivo animal models are viewed, including recent human intervention studies. Finally, possible mechanisms of action involving antioxidant and pro-oxidant activity as well as interference with cellular functions are discussed. Full article
(This article belongs to the Special Issue Antioxidants)

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