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Molecules, Volume 17, Issue 5 (May 2012), Pages 4770-6178

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Open AccessCommunication Chiral Bis(Imidazolidine)Pyridine-Cu Complex-Catalyzed Enantioselective [3+2]-Cycloaddition of Azomethine Imines with Propiolates
Molecules 2012, 17(5), 6170-6178; https://doi.org/10.3390/molecules17056170
Received: 27 April 2012 / Revised: 18 May 2012 / Accepted: 21 May 2012 / Published: 24 May 2012
Cited by 41 | PDF Full-text (284 KB) | HTML Full-text | XML Full-text
Abstract
[3+2] Cycloaddition of azomethine imines with electron-deficient terminal alkynes was smoothly catalyzed by a chiral bis(imidazolidine)pyridine-CuOAc complex to give bicyclic pyrazolo[1,2-a]pyrazolone derivatives with up to 74% ee. Full article
(This article belongs to the Special Issue Asymmetric Catalysis)
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Open AccessArticle Chemical Constituents of the Ethyl Acetate Extract of Belamcanda chinensis (L.) DC Roots and Their Antitumor Activities
Molecules 2012, 17(5), 6156-6169; https://doi.org/10.3390/molecules17056156
Received: 19 April 2012 / Revised: 8 May 2012 / Accepted: 14 May 2012 / Published: 24 May 2012
Cited by 40 | PDF Full-text (539 KB) | HTML Full-text | XML Full-text
Abstract
An activity-directed fractionation and purification process was used to isolate antitumor compounds from the roots of Belamcanda chinensis (L.) DC. The ethyl acetate extract showed greater antitumor activities than the other extracts, consequently leading to the isolation of 18 compounds identified as b-
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An activity-directed fractionation and purification process was used to isolate antitumor compounds from the roots of Belamcanda chinensis (L.) DC. The ethyl acetate extract showed greater antitumor activities than the other extracts, consequently leading to the isolation of 18 compounds identified as b-sitosterol (1), dausterol (2), quercetin (3), kampferol (4), shikimic acid (5), gallic acid (6), ursolic acid (7), betulin (8), betulonic acid (9), betulone (10), tectoridin (11), irisflorentin (12), 4′,5,6-trihydroxy-7-methoxyisoflavone (13), tectorigenin (14), irilins A (15), iridin (16), irigenin (17), and iristectongenin A (18). Compounds 310, 13, and 15 were isolated from B. chinensis for the first time. Compounds 4 and 710 showed potent cytotoxic activities against PC3, MGC-803, Bcap-37, and MCF-7 cell lines. The mechanism of the antitumor action of compound 7 was preliminarily investigated through acridine orange/ethidium bromide (AO/EB) staining, Hoechst 33258 staining, and terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay, which indicated the growth inhibition of MGC-803 cells via the induction of tumor cell apoptosis. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Ipomoea aquatica Extract Shows Protective Action Against Thioacetamide-Induced Hepatotoxicity
Molecules 2012, 17(5), 6146-6155; https://doi.org/10.3390/molecules17056146
Received: 1 April 2012 / Revised: 20 April 2012 / Accepted: 23 April 2012 / Published: 22 May 2012
Cited by 17 | PDF Full-text (513 KB) | HTML Full-text | XML Full-text
Abstract
In the Indian system of traditional medicine (Ayurveda) it is recommended to consume Ipomoea aquatica to mitigate disorders like jaundice. In this study, the protective effects of ethanol extract of I. aquatica against liver damage were evaluated in thioacetamide (TAA)-induced chronic hepatotoxicity in
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In the Indian system of traditional medicine (Ayurveda) it is recommended to consume Ipomoea aquatica to mitigate disorders like jaundice. In this study, the protective effects of ethanol extract of I. aquatica against liver damage were evaluated in thioacetamide (TAA)-induced chronic hepatotoxicity in rats. There was no sign of toxicity in the acute toxicity study, in which Sprague-Dawley (SD) rats were orally fed with I. aquatica (250 and 500 mg/kg) for two months along with administration of TAA (i.p injection 200 mg/kg three times a week for two months). The results showed that the treatment of I. aquatica significantly lowered the TAA-induced serum levels of hepatic enzyme markers (ALP, ALT, AST, protein, albumin, bilirubin and prothrombin time). The hepatic content of activities and expressions SOD and CAT that were reduced by TAA were brought back to control levels by the plant extract supplement. Meanwhile, the rise in MDA level in the TAA receiving groups also were significantly reduced by I. aquatica treatment. Histopathology of hepatic tissues by H&E and Masson trichrome stains displayed that I. aquatica has reduced the incidence of liver lesions, including hepatic cells cloudy swelling, infiltration, hepatic necrosis, and fibrous connective tissue proliferation induced by TAA in rats. Therefore, the results of this study show that the protective effect of I. aquatica in TAA-induced liver damage might be contributed to its modulation on detoxification enzymes and its antioxidant and free radical scavenger effects. Moreover, it confirms a scientific basis for the traditional use of I. aquatica for the treatment of liver disorders. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle A QSAR Study of Environmental Estrogens Based on a Novel Variable Selection Method
Molecules 2012, 17(5), 6126-6145; https://doi.org/10.3390/molecules17056126
Received: 10 March 2012 / Revised: 19 April 2012 / Accepted: 26 April 2012 / Published: 21 May 2012
Cited by 10 | PDF Full-text (718 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A large number of descriptors were employed to characterize the molecular structure of 53 natural, synthetic, and environmental chemicals which are suspected of disrupting endocrine functions by mimicking or antagonizing natural hormones and may thus pose a serious threat to the health of
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A large number of descriptors were employed to characterize the molecular structure of 53 natural, synthetic, and environmental chemicals which are suspected of disrupting endocrine functions by mimicking or antagonizing natural hormones and may thus pose a serious threat to the health of humans and wildlife. In this work, a robust quantitative structure-activity relationship (QSAR) model with a novel variable selection method has been proposed for the effective estrogens. The variable selection method is based on variable interaction (VSMVI) with leave-multiple-out cross validation (LMOCV) to select the best subset. During variable selection, model construction and assessment, the Organization for Economic Co-operation and Development (OECD) principles for regulation of QSAR acceptability were fully considered, such as using an unambiguous multiple-linear regression (MLR) algorithm to build the model, using several validation methods to assessment the performance of the model, giving the define of applicability domain and analyzing the outliers with the results of molecular docking. The performance of the QSAR model indicates that the VSMVI is an effective, feasible and practical tool for rapid screening of the best subset from large molecular descriptors. Full article
(This article belongs to the Special Issue QSAR and Its Applications)
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Open AccessArticle Preussianone, a New Flavanone-Chromone Biflavonoid from Garcinia preussii Engl.
Molecules 2012, 17(5), 6114-6125; https://doi.org/10.3390/molecules17056114
Received: 20 March 2012 / Revised: 26 April 2012 / Accepted: 14 May 2012 / Published: 21 May 2012
Cited by 20 | PDF Full-text (273 KB) | HTML Full-text | XML Full-text
Abstract
A new flavanone-chromone biflavonoid, preussianone (1), has been isolated from the leaves of Garcinia preussii, along with four known biflavonoids. The absolute stereostructures were elucidated by chemical, spectroscopic, and chiroptical methods. The biological properties of the new biflavonoid against several
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A new flavanone-chromone biflavonoid, preussianone (1), has been isolated from the leaves of Garcinia preussii, along with four known biflavonoids. The absolute stereostructures were elucidated by chemical, spectroscopic, and chiroptical methods. The biological properties of the new biflavonoid against several bacterial strains were evaluated. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents
Molecules 2012, 17(5), 6100-6113; https://doi.org/10.3390/molecules17056100
Received: 5 April 2012 / Revised: 5 May 2012 / Accepted: 7 May 2012 / Published: 21 May 2012
Cited by 18 | PDF Full-text (273 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
In the present work, we report the synthesis and in vitro anticancer and antimicrobial activity evaluation of a new series of 1-substituted-β-carboline derivatives bearing a 4-benzylidene-4H-oxazol-5-one unity at C-3. The compound 2-[1-(4-methoxyphenyl)-9H-β-carbolin-3-yl]-4-(benzylidene)-4H-oxazol-5-one (11) was the
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In the present work, we report the synthesis and in vitro anticancer and antimicrobial activity evaluation of a new series of 1-substituted-β-carboline derivatives bearing a 4-benzylidene-4H-oxazol-5-one unity at C-3. The compound 2-[1-(4-methoxyphenyl)-9H-β-carbolin-3-yl]-4-(benzylidene)-4H-oxazol-5-one (11) was the most active derivative, exhibiting a potent cytotoxic activity against glioma (U251), prostate (PC-3) and ovarian (OVCAR-03) cancer cell lines with IC50 values of 0.48, 1.50 and 1.07 µM, respectively. An in silico study of the ADME properties of the novel synthesized β-carboline derivatives was also performed. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessReview Synthesis and Bioactivity of Secondary Metabolites from Marine Sponges Containing Dibrominated Indolic Systems
Molecules 2012, 17(5), 6083-6099; https://doi.org/10.3390/molecules17056083
Received: 20 April 2012 / Revised: 14 May 2012 / Accepted: 15 May 2012 / Published: 21 May 2012
Cited by 38 | PDF Full-text (293 KB) | HTML Full-text | XML Full-text
Abstract
Marine sponges. (e.g., Hyrtios sp., Dragmacidin sp., Aglophenia pleuma, Aplidium cyaneum, Aplidium meridianum.) produce bioactive secondary metabolites involved in their defence mechanisms. Recently it was demonstrated that several of those compounds show a large variety of biological activities against different
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Marine sponges. (e.g., Hyrtios sp., Dragmacidin sp., Aglophenia pleuma, Aplidium cyaneum, Aplidium meridianum.) produce bioactive secondary metabolites involved in their defence mechanisms. Recently it was demonstrated that several of those compounds show a large variety of biological activities against different human diseases with possible applications in medicinal chemistry and in pharmaceutical fields, especially related to the new drug development process. Researchers have focused their attention principally on secondary metabolites with anti-cancer and cytotoxic activities. A common target for these molecules is the cytoskeleton, which has a central role in cellular proliferation, motility, and profusion involved in the metastatic process associate with tumors. In particular, many substances containing brominated indolic rings such as 5,6-dibromotryptamine, 5,6-dibromo-N-methyltryptamine, 5,6-dibromo-N-methyltryptophan (dibromoabrine), 5,6-dibromo-N,N-dimethyltryptamine and 5,6-dibromo-L-hypaphorine isolated from different marine sources, have shown anti-cancer activity, as well as antibiotic and anti-inflammatory properties. Considering the structural correlation between endogenous monoamine serotonin with marine indolic alkaloids 5,6-dibromoabrine and 5,6-dibromotryptamine, a potential use of some dibrominated indolic metabolites in the treatment of depression-related pathologies has also been hypothesized. Due to the potential applications in the treatment of various diseases and the increasing demand of these compounds for biological assays and the difficult of their isolation from marine sources, we report in this review a series of recent syntheses of marine dibrominated indole-containing products. Full article
(This article belongs to the collection Bioactive Compounds)
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Open AccessArticle Antioxidant, Antimicrobial and Tyrosinase Inhibitory Activities of Xanthones Isolated from Artocarpus obtusus F.M. Jarrett
Molecules 2012, 17(5), 6071-6082; https://doi.org/10.3390/molecules17056071
Received: 5 March 2012 / Revised: 17 April 2012 / Accepted: 20 April 2012 / Published: 21 May 2012
Cited by 24 | PDF Full-text (250 KB) | HTML Full-text | XML Full-text
Abstract
One of the most promising plants in biological screening test results of thirteen Artocarpus species was Artocarpus obtusus FM Jarrett and detailed phytochemical investigation of powdered dried bark of the plant has led to the isolation and identification of three xanthones; pyranocycloartobiloxanthone A
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One of the most promising plants in biological screening test results of thirteen Artocarpus species was Artocarpus obtusus FM Jarrett and detailed phytochemical investigation of powdered dried bark of the plant has led to the isolation and identification of three xanthones; pyranocycloartobiloxanthone A (1), dihydroartoindonesianin C (2) and pyranocycloartobiloxanthone B (3). These compounds were screened for antioxidant, antimicrobial and tyrosinase inhibitory activities. Pyranocycloartobiloxanthone A (1) exhibited a strong free radical scavenger towards DPPH free radicals with IC50 value of 2 µg/mL with prominent discoloration observed in comparison with standard ascorbic acid, α-tocopherol and quercetin, The compound also exhibited antibacterial activity against methicillin resistant Staphylococcus aureus (ATCC3359) and Bacillus subtilis (clinically isolated) with inhibition zone of 20 and 12 mm, respectively. However the other two xanthones were found to be inactive. For the tyrosinase inhibitory activity, again compound (1) displayed strong activity comparable with the standard kojic acid. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Physicochemical Characterization and Cytotoxic Activity Evaluation of Hydroxymethylferrocene:β-Cyclodextrin Inclusion Complex
Molecules 2012, 17(5), 6056-6070; https://doi.org/10.3390/molecules17056056
Received: 24 April 2012 / Revised: 14 May 2012 / Accepted: 15 May 2012 / Published: 21 May 2012
Cited by 17 | PDF Full-text (662 KB) | HTML Full-text | XML Full-text
Abstract
An inclusion complex of hydroxymethylferrocene (FeMeOH) with β-cyclodextrin (β-CD) was prepared in the solid state by different techniques such as physical mixture, coprecipitation, kneading and freeze-drying. The formation of the inclusion complex was confirmed by X-ray Powder Diffractometry and Fourier Transform-Infrared spectroscopy. In
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An inclusion complex of hydroxymethylferrocene (FeMeOH) with β-cyclodextrin (β-CD) was prepared in the solid state by different techniques such as physical mixture, coprecipitation, kneading and freeze-drying. The formation of the inclusion complex was confirmed by X-ray Powder Diffractometry and Fourier Transform-Infrared spectroscopy. In aqueous solution, the 1:1 stoichiometry was established by a Job plot. The inclusion complex formation was also investigated by NMR and the stability constant (Kb) of the complex was determined to be 478 M−1, which is in agreement with that obtained with UV-Vis tritation (Kb = 541.3 M−1). The phase solubility study showed a diagram classified as BS type and that the solubility of FeMeOH was slightly increased in the presence of β-CD. Furthermore, utilizing phase solubility diagram data, the Kb was estimated to be equal to 528.0 M−1. The cytotoxic activity of FeMeOH and its complexation product with β-CD was determined using the MTT-assay on MDA-MB-231 cell line, showing that the inclusion complex has a higher capability of inhibiting cell growth compared to that of pure FeMeOH. Full article
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Open AccessArticle Effect of Soluble Sulfide on the Activity of Luminescent Bacteria
Molecules 2012, 17(5), 6046-6055; https://doi.org/10.3390/molecules17056046
Received: 23 February 2012 / Revised: 11 May 2012 / Accepted: 14 May 2012 / Published: 21 May 2012
Cited by 5 | PDF Full-text (476 KB) | HTML Full-text | XML Full-text
Abstract
Sulfide is an important water pollutant widely found in industrial waste water that has attracted much attention. S2−, as a weak acidic anion, is easy hydrolyzed to HS and H2S in aqueous solution. In this study, biological tests
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Sulfide is an important water pollutant widely found in industrial waste water that has attracted much attention. S2−, as a weak acidic anion, is easy hydrolyzed to HS and H2S in aqueous solution. In this study, biological tests were performed to establish the toxicity of sulfide solutions on luminescent bacteria. Considering the sulfide solution was contained three substances—S2−, HS and H2S—the toxicity test was performed at different pH values to investigate which form of sulfide increased light emission and which reduced light emission. It was shown that the EC50 values were close at pH 7.4, 8.0 and 9.0 which were higher than pH 5 and 10. The light emission and sulfide concentrations displayed an inverse exponential dose-response relationship within a certain concentration range at pH 5, 6.5 and 10. The same phenomenon occurred for the high concentration of sulfide at pH 7.4, 8 and 9, in which the concentration of sulfide was HS >> H2S > S2−. An opposite hormesis-effect appeared at the low concentrations of sulfide. Full article
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Open AccessArticle Protective Effect of T. violacea Rhizome Extract Against Hypercholesterolemia-Induced Oxidative Stress in Wistar Rats
Molecules 2012, 17(5), 6033-6045; https://doi.org/10.3390/molecules17056033
Received: 29 March 2012 / Revised: 27 April 2012 / Accepted: 28 April 2012 / Published: 21 May 2012
Cited by 21 | PDF Full-text (368 KB) | HTML Full-text | XML Full-text
Abstract
The present study examines the effect of methanolic extract of T. violacea rhizomes on high cholesterol (2%) diet fed rats (HCD). At the end of 4 weeks, serum total protein, albumin, reduced glutathione (GSH), and markers of oxidative stress viz., catalase (CAT), superoxide
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The present study examines the effect of methanolic extract of T. violacea rhizomes on high cholesterol (2%) diet fed rats (HCD). At the end of 4 weeks, serum total protein, albumin, reduced glutathione (GSH), and markers of oxidative stress viz., catalase (CAT), superoxide dismutase (SOD), thiobarbituric acid reactive substances (TBARS—a marker of lipid peroxidation), glutathione-S-transferase (GST) and glutathione peroxidase (GPx) in the serum, aorta, liver and heart of HCD and normal rats were assessed and compared. A significant (p < 0.05) elevation in TBARS, and a reduction (p < 0.05) in serum total protein, albumin, GSH and antioxidant enzyme activities was observed in tissues of HCD fed rats compared with the normal group. Co-administration of crude extracts of T. violacea rhizomes protected the liver, heart, serum and aorta against HCD-induced lipid peroxidation in a dose dependant manner. The activities of the extract (500 mg/kg) compared favorably with gemfibrozil. The extracts also protected against HCD-induced reduction in serum total protein, GSH and restored the activities of antioxidant tissues (liver, heart and aorta) enzymes to near normal values. This result suggested that consumption of T. violacea rhizome may help to protect against hypercholesterolemia- induced oxidative stress diseases in the heart and liver. Full article
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Open AccessArticle Chemical Composition of Artemisia annua L. Leaves and Antioxidant Potential of Extracts as a Function of Extraction Solvents
Molecules 2012, 17(5), 6020-6032; https://doi.org/10.3390/molecules17056020
Received: 12 April 2012 / Revised: 9 May 2012 / Accepted: 11 May 2012 / Published: 21 May 2012
Cited by 21 | PDF Full-text (237 KB) | HTML Full-text | XML Full-text
Abstract
This study was conducted to investigate the chemical and nutritional composition of Artemisia annua leaves in addition to determination of antioxidant potential of their extracts prepared in different solvents. Chemical composition was determined by quantifying fat, protein, carbohydrate, fiber, tocopherol, phytate, and tannin
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This study was conducted to investigate the chemical and nutritional composition of Artemisia annua leaves in addition to determination of antioxidant potential of their extracts prepared in different solvents. Chemical composition was determined by quantifying fat, protein, carbohydrate, fiber, tocopherol, phytate, and tannin contents. Extraction of A. annua leaves, for antioxidant potential evaluation, was carried out using five solvents of different polarities, i.e., hexane, chloroform, ethyl acetate, methanol and water. Antioxidant potential was evaluated by estimating total phenolic (TPC), flavonoid (TFC) contents, ferric reducing antioxidant power (FRAP), Trolox equivalent antioxidant capacity (TEAC), DPPH radical scavenging activity and lipid peroxidation. Efficiency of different solvents was compared for the yield of antioxidant extracts from leaf samples and a clear variation was observed. The highest TPC, TFC, TEAC, DPPH radical scavenging and lowest lipid peroxidation were observed in MeOH extracts, whereas aqueous extract exhibited high ferric reducing antioxidant power; suggesting MeOH to be the most favorable extractant. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Green and Highly Efficient Synthesis of 2-Arylbenzothiazoles Using Glycerol without Catalyst at Ambient Temperature
Molecules 2012, 17(5), 6011-6019; https://doi.org/10.3390/molecules17056011
Received: 27 March 2012 / Revised: 9 May 2012 / Accepted: 10 May 2012 / Published: 18 May 2012
Cited by 25 | PDF Full-text (175 KB) | HTML Full-text | XML Full-text
Abstract
A one-pot and clean synthesis of 2-arylbenzothiazoles via the ambient temperature reaction of 2-aminothiophenols and aromatic aldehydes without catalyst in glycerol as a green solvent has been reported. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle Metathesis Transformations of Natural Products: Cross-Metathesis of Natural Rubber and Mandarin Oil by Ru-Alkylidene Catalysts
Molecules 2012, 17(5), 6001-6010; https://doi.org/10.3390/molecules17056001
Received: 16 March 2012 / Revised: 30 April 2012 / Accepted: 3 May 2012 / Published: 18 May 2012
Cited by 18 | PDF Full-text (245 KB) | HTML Full-text | XML Full-text
Abstract
This study reports on the degradation of natural rubber (NR) via cross-metathesis with mandarin oil and d-limonene, an abundant compound in essential oils; that were used as chain transfer agents (CTAs) and green solvents. Reactions were performed in the presence of the
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This study reports on the degradation of natural rubber (NR) via cross-metathesis with mandarin oil and d-limonene, an abundant compound in essential oils; that were used as chain transfer agents (CTAs) and green solvents. Reactions were performed in the presence of the ruthenium-alkylidene catalysts (PCy3)2(Cl)2Ru=CHPh (I) and (1,3-dimesityl-4,5-dihydroimidazol-2-ylidene) (PCy3)Cl2Ru=CHPh (II), respectively. Catalyst II bears an N-heterocyclic carbene ligand (NHC) bounded to the ruthenium atom, which has a strong basic character; therefore it is more active toward trisubstituted olefins in comparison with catalyst I. In both cases, isolated monoterpene-terminated isoprene oligomers were obtained as products of the cross-metathesis degradation of NR. In the presence of catalyst II molecular weight values around Mn × 102 and yields of 80% were obtained; whereas with catalyst I, the molecular weights of products were about Mn × 104 with yields ranging 70 to 74%. The composition and yield of NR degradation products were determined by GC/MS (EI) analysis and it was found that the oligomers obtained have primarily one vinyl group and one terpene-monocyclic group at the chain end, with isoprene units Am = 2, 3 y 4. Full article
(This article belongs to the Special Issue Olefin Metathesis and Its Application)
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Open AccessArticle A Sandwich HIV p24 Amperometric Immunosensor Based on a Direct Gold Electroplating-Modified Electrode
Molecules 2012, 17(5), 5988-6000; https://doi.org/10.3390/molecules17055988
Received: 8 March 2012 / Revised: 25 April 2012 / Accepted: 9 May 2012 / Published: 18 May 2012
Cited by 31 | PDF Full-text (590 KB) | HTML Full-text | XML Full-text
Abstract
Acquired immune deficiency syndrome (AIDS) is a severe communicable immune deficiency disease caused by the human immune deficiency virus (HIV). The analysis laboratory diagnosis of HIV infection is a crucial aspect of controlling AIDS. The p24 antigen, the HIV-1 capsid protein, is of
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Acquired immune deficiency syndrome (AIDS) is a severe communicable immune deficiency disease caused by the human immune deficiency virus (HIV). The analysis laboratory diagnosis of HIV infection is a crucial aspect of controlling AIDS. The p24 antigen, the HIV-1 capsid protein, is of considerable diagnostic interest because it is detectable several days earlier than host-generated HIV antibodies following HIV exposure. We present herein a new sandwich HIV p24 immunosensor based on directly electroplating an electrode surface with gold nanoparticles using chronoamperometry, which greatly increased the conductivity and reversibility of the electrode. Under optimum conditions, the electrochemical signal showed a linear relationship with the concentration of p24, ranging from 0.01 ng/mL to 100 ng/mL (R > 0.99), and the detection limit was 0.008 ng/mL. Compared with ELISA, this method increased the sensitivity by more than two orders of magnitude (the sensitivity of ELISA for p24 is about 1 ng/mL). This immunosensor may be broadly applied to clinical samples, being distinguished by its ease of use, mild reaction conditions, guaranteed reproducibility, and good anti-interference ability. Full article
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Open AccessArticle Preparation of Curcumin-Loaded Liposomes and Evaluation of Their Skin Permeation and Pharmacodynamics
Molecules 2012, 17(5), 5972-5987; https://doi.org/10.3390/molecules17055972
Received: 9 April 2012 / Revised: 8 May 2012 / Accepted: 9 May 2012 / Published: 18 May 2012
Cited by 100 | PDF Full-text (708 KB) | HTML Full-text | XML Full-text
Abstract
This study aimed to investigate the in vitro skin permeation and in vivo antineoplastic effect of curcumin by using liposomes as the transdermal drug-delivery system. Soybean phospholipids (SPC), egg yolk phospholipids (EPC), and hydrogenated soybean phospholipids (HSPC) were selected for the preparation of
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This study aimed to investigate the in vitro skin permeation and in vivo antineoplastic effect of curcumin by using liposomes as the transdermal drug-delivery system. Soybean phospholipids (SPC), egg yolk phospholipids (EPC), and hydrogenated soybean phospholipids (HSPC) were selected for the preparation of different kinds of phospholipids composed of curcumin-loaded liposomes: C-SPC-L (curcumin-loaded SPC liposomes), C-EPC-L (curcumin-loaded EPC liposomes), and C-HSPC-L (curcumin-loaded HSPC liposomes). The physical properties of different lipsomes were investigated as follows: photon correlation spectroscopy revealed that the average particle sizes of the three types of curcumin-loaded liposomes were 82.37 ± 2.19 nm (C-SPC-L), 83.13 ± 4.89 nm (C-EPC-L), and 92.42 ± 4.56 nm (C-HSPC-L), respectively. The encapsulation efficiency values were found to be 82.32 ± 3.91%, 81.59 ± 2.38%, and 80.77 ± 4.12%, respectively. An in vitro skin penetration study indicated that C-SPC-L most significantly promoted drug permeation and deposition followed by C-EPC-L, C-HSPC-L, and curcumin solution. Moreover, C-SPC-L displayed the greatest ability of all loaded liposomes to inhibit the growth of B16BL6 melanoma cells. Therefore, the C-SPC-L were chosen for further pharmacodynamic evaluation. A significant effect on antimelanoma activity was observed with C-SPC-L, as compared to treatment with curcumin solution in vivo. These results suggest that C-SPC-L would be a promising transdermal carrier for curcumin in cancer treatment. Full article
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Open AccessArticle Antibacterial Evaluation of Some Schiff Bases Derived from 2-Acetylpyridine and Their Metal Complexes
Molecules 2012, 17(5), 5952-5971; https://doi.org/10.3390/molecules17055952
Received: 27 March 2012 / Revised: 13 May 2012 / Accepted: 15 May 2012 / Published: 18 May 2012
Cited by 26 | PDF Full-text (436 KB) | HTML Full-text | XML Full-text
Abstract
A series of Schiff bases derived from 2-acetylpyridne and their metal complexes were characterized by elemental analysis, NMR, FT-IR and UV-Vis spectral studies. The complexes were screened for anti-bacterial activity against Methicillin-resistant Staphylococcus aureus (MRSA), Acinetobacter baumanni (AC), Klebsiella pneumonie (KB) and Pseudomonas
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A series of Schiff bases derived from 2-acetylpyridne and their metal complexes were characterized by elemental analysis, NMR, FT-IR and UV-Vis spectral studies. The complexes were screened for anti-bacterial activity against Methicillin-resistant Staphylococcus aureus (MRSA), Acinetobacter baumanni (AC), Klebsiella pneumonie (KB) and Pseudomonas aeruginosa (PA) using the disc diffusion and micro broth dilution assays. Based on the overall results, the complexes showed the highest activities against MRSA while a weak antibacterial activity was observed against A. baumanii and P. aeruginosa. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessCommunication Inhibitory Effect and Mechanism on Antiproliferation of Isoatriplicolide Tiglate (PCAC) from Paulownia Coreana
Molecules 2012, 17(5), 5945-5951; https://doi.org/10.3390/molecules17055945
Received: 28 April 2012 / Revised: 11 May 2012 / Accepted: 14 May 2012 / Published: 18 May 2012
Cited by 3 | PDF Full-text (599 KB) | HTML Full-text | XML Full-text | Correction
Abstract
Paulownia coreana has traditionally been used as the medicine and health food in the treatment of cancer and infectious diseases. In the present study, a new antiproliferation agent, isoatriplicolide tiglate (PCAC) was isolated from the chloroform soluble fraction of the leaves of Paulownia
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Paulownia coreana has traditionally been used as the medicine and health food in the treatment of cancer and infectious diseases. In the present study, a new antiproliferation agent, isoatriplicolide tiglate (PCAC) was isolated from the chloroform soluble fraction of the leaves of Paulownia coreana. The antiproliferation activities of PCAC plant extract was examined in breast and cervical cancer cell lines in a time-and dose-dependent manners. Our in vitro experiments showed that PCAC suppresses the cell growth and proliferation of cancer cells at a relatively low concentration ( < 10 µg/mL) and induces apoptosis at a high concentration ( > 50 µg/mL). Western blot analysis showed that concentration higher than 50 µg/mL induces a time-dependent increase in the percentage of apoptotic cells. In this case, PCAC uses both extrinsic and intrinsic pathways for the apoptosis. PCAC treatment decreased the expression of pro-caspase 8, 9, and 3, the main regulators of apoptotic cell death, in MDA-MB-231 cells, accompanied by the activation of caspase 8, 9, and 3. More importantly, PCAC inhibited the in vitro proliferation of six other human breast and cervical cancer cell lines. In conclusion, our data strongly suggest that PCAC acts as an antiproliferation agents particularly against breast and cervical cancers by inducing cell cycle arrest in the S/G2 phase and caspase dependent apoptosis at relatively low ( < 10 μg/mL) and high ( > 50 µg/mL) concentrations, respectively. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle The Vasorelaxant Mechanisms of a Rho Kinase Inhibitor DL0805 in Rat Thoracic Aorta
Molecules 2012, 17(5), 5935-5944; https://doi.org/10.3390/molecules17055935
Received: 26 March 2012 / Revised: 11 May 2012 / Accepted: 11 May 2012 / Published: 18 May 2012
Cited by 11 | PDF Full-text (402 KB) | HTML Full-text | XML Full-text
Abstract
Rho-kinase has been suggested as a potential therapeutic target in the treatment of cardiovascular diseases. The Rho-kinase signaling pathway is substantially involved in vascular contraction. The aim of the present study was to evaluate the vasorelaxant effects of Rho kinase inhibitor DL0805 in
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Rho-kinase has been suggested as a potential therapeutic target in the treatment of cardiovascular diseases. The Rho-kinase signaling pathway is substantially involved in vascular contraction. The aim of the present study was to evaluate the vasorelaxant effects of Rho kinase inhibitor DL0805 in isolated rat aortic rings and to investigate its possible mechanism(s). It was found that DL0805 exerted vasorelaxation in a dose-dependent manner in NE or KCl-induced sustained contraction and partial loss of the vasorelaxation under endothelium-denuded rings. The DL0805-induced vasorelaxation was significantly reduced by the nitric oxide synthase inhibitor Nω-nitro-L-arginine methyl ester, the guanylate cyclase inhibitor methylene blue and the cyclooxygenase inhibitor indomethacin. The voltage-dependent K+ channel blocker 4-aminopyridine remarkably attenuated DL0805-induced relaxations. However, the ATP-sensitive K+ channel blocker glibenclamide and Ca2+-activated K+ channel blocker tetraethylammonium did not affect the DL0805-induced relaxation. In the endothelium-denuded rings, DL0805 also reduced NE-induced transient contraction and inhibited contraction induced by increasing external calcium. These findings suggested that DL0805 is a novel vasorelaxant compound associated with inhibition of Rho/ROCK signaling pathway. The NO-cGMP pathway may be involved in the relaxation of DL0805 in endothelium-intact aorta. The vasorelaxant effect of DL0805 is partially mediated by the opening of the voltage-dependent K+ channels. Full article
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Open AccessArticle Scope and Limitations of a Novel Synthesis of 3-Arylazonicotinates
Molecules 2012, 17(5), 5924-5934; https://doi.org/10.3390/molecules17055924
Received: 27 January 2012 / Revised: 13 May 2012 / Accepted: 15 May 2012 / Published: 18 May 2012
Cited by 5 | PDF Full-text (214 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The reaction of 3-oxo-3-phenyl-2-phenylhydrazonal with functionally substituted and heteroaromatic substituted acetonitrile to yield arylazonicotinic acid derivatives and 5-arylsubstituted pyridines was established. In some cases the produced nicotinates could not be isolated as they underwent thermally induced 6π-electrocyclization yielding polynuclear pyridine derivatives. Full article
(This article belongs to the Special Issue Heterocycles)
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Open AccessArticle Tropical Plant Extracts as Potential Antihyperglycemic Agents
Molecules 2012, 17(5), 5915-5923; https://doi.org/10.3390/molecules17055915
Received: 7 April 2012 / Revised: 28 April 2012 / Accepted: 30 April 2012 / Published: 18 May 2012
Cited by 17 | PDF Full-text (605 KB) | HTML Full-text | XML Full-text
Abstract
Preliminary investigations on 14 plant extracts (obtained by ethanolic and aqueous extraction) identified those having high antioxidant and a significant total phenolic content. Antihyperglycemic, a-amylase and a-glucosidase inhibition activities were also observed. A correlation between the antihyperglycemic activity, total phenolic content and antioxidant
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Preliminary investigations on 14 plant extracts (obtained by ethanolic and aqueous extraction) identified those having high antioxidant and a significant total phenolic content. Antihyperglycemic, a-amylase and a-glucosidase inhibition activities were also observed. A correlation between the antihyperglycemic activity, total phenolic content and antioxidant (DPPH scavenging) activity was established. To further substantiate these findings, the possibility of tannins binding non-specifically to enzymes and thus contributing to the antihyperglycemic activity was also investigated. Our study clearly indicated that the antihyperglycemic activity observed in the plant extracts was indeed not due to non-specific tannin absorption. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessReview Modifications on the Basic Skeletons of Vinblastine and Vincristine
Molecules 2012, 17(5), 5893-5914; https://doi.org/10.3390/molecules17055893
Received: 30 March 2012 / Revised: 9 May 2012 / Accepted: 10 May 2012 / Published: 18 May 2012
Cited by 33 | PDF Full-text (940 KB) | HTML Full-text | XML Full-text
Abstract
The synthetic investigation of biologically active natural compounds serves two main purposes: (i) the total synthesis of alkaloids and their analogues; (ii) modification of the structures for producing more selective, more effective, or less toxic derivatives. In the chemistry
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The synthetic investigation of biologically active natural compounds serves two main purposes: (i) the total synthesis of alkaloids and their analogues; (ii) modification of the structures for producing more selective, more effective, or less toxic derivatives. In the chemistry of dimeric Vinca alkaloids enormous efforts have been directed towards synthesizing new derivatives of the antitumor agents vinblastine and vincristine so as to obtain novel compounds with improved therapeutic properties. Full article
(This article belongs to the Special Issue Advances in Heteroaromatic Chemistry)
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Open AccessArticle Synthesis of 1,2,3-Triazole Derivatives and in Vitro Antifungal Evaluation on Candida Strains
Molecules 2012, 17(5), 5882-5892; https://doi.org/10.3390/molecules17055882
Received: 12 April 2012 / Revised: 3 May 2012 / Accepted: 5 May 2012 / Published: 16 May 2012
Cited by 32 | PDF Full-text (230 KB) | HTML Full-text | XML Full-text
Abstract
1,2,3-Triazoles have been extensively studied as compounds possessing important biological activities. In this work, we describe the synthesis of ten 2-(1-aryl-1H-1,2,3-triazol-4-yl)propan-2-ols via copper catalyzed azide alkyne cycloaddition (CuAAc or click chemistry). Next the in vitro antifungal activity of these ten
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1,2,3-Triazoles have been extensively studied as compounds possessing important biological activities. In this work, we describe the synthesis of ten 2-(1-aryl-1H-1,2,3-triazol-4-yl)propan-2-ols via copper catalyzed azide alkyne cycloaddition (CuAAc or click chemistry). Next the in vitro antifungal activity of these ten compounds was evaluated using the microdilution broth method against 42 isolates of four different Candida species. Among all tested compounds, the halogen substituted triazole 2-[1-(4-chlorophenyl)-1H-(1,2,3)triazol-4-yl]propan-2-ol, revealed the best antifungal profile, showing that further modifications could be done in the structure to obtain a better drug candidate in the future. Full article
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Open AccessArticle Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines
Molecules 2012, 17(5), 5870-5881; https://doi.org/10.3390/molecules17055870
Received: 28 April 2012 / Revised: 10 May 2012 / Accepted: 11 May 2012 / Published: 16 May 2012
Cited by 11 | PDF Full-text (303 KB) | HTML Full-text | XML Full-text
Abstract
Two series of novel 2-substituted-4-amino-6-halogenquinolines 8al and 13ah were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl substituents
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Two series of novel 2-substituted-4-amino-6-halogenquinolines 8al and 13ah were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl substituents exhibited good to excellent antiproliferative activity. Among them, compound 8e was a considered promising lead for further structural modifications with IC50 values of 0.03 μM, 0.55 μM, 0.33 μM and 1.24 μM, which was 2.5- to 186-fold more active than gefitinib and compound 1. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Effects of Citrus aurantium (Bitter Orange) Fruit Extracts and p-Synephrine on Metabolic Fluxes in the Rat Liver
Molecules 2012, 17(5), 5854-5869; https://doi.org/10.3390/molecules17055854
Received: 21 March 2012 / Revised: 7 May 2012 / Accepted: 12 May 2012 / Published: 16 May 2012
Cited by 20 | PDF Full-text (363 KB) | HTML Full-text | XML Full-text
Abstract
The fruit extracts of Citrus aurantium (bitter orange) are traditionally used as weight-loss products and as appetite supressants. An important fruit component is p-synephrine, which is structurally similar to the adrenergic agents. Weight-loss and adrenergic actions are always related to metabolic changes
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The fruit extracts of Citrus aurantium (bitter orange) are traditionally used as weight-loss products and as appetite supressants. An important fruit component is p-synephrine, which is structurally similar to the adrenergic agents. Weight-loss and adrenergic actions are always related to metabolic changes and this work was designed to investigate a possible action of the C. aurantium extract on liver metabolism. The isolated perfused rat liver was used to measure catabolic and anabolic pathways, including oxygen uptake and perfusion pressure. The C. aurantium extract and p-synephrine increased glycogenolysis, glycolysis, oxygen uptake and perfusion pressure. These changes were partly sensitive to a- and b-adrenergic antagonists. p-Synephrine (200 mM) produced an increase in glucose output that was only 15% smaller than the increment caused by the extract containing 196 mM p-synephrine. At low concentrations the C. aurantium extract tended to increase gluconeogenesis, but at high concentrations it was inhibitory, opposite to what happened with p-synephrine. The action of the C. aurantium extract on liver metabolism is similar to the well known actions of adrenergic agents and can be partly attributed to its content in p-synephrine. Many of these actions are catabolic and compatible with the weight-loss effects usually attributed to C. aurantium. Full article
(This article belongs to the collection Bioactive Compounds)
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Open AccessArticle Chemical Investigation of Saponins in Different Parts of Panax notoginseng by Pressurized Liquid Extraction and Liquid Chromatography-Electrospray Ionization-Tandem Mass Spectrometry
Molecules 2012, 17(5), 5836-5853; https://doi.org/10.3390/molecules17055836
Received: 12 April 2012 / Revised: 3 May 2012 / Accepted: 11 May 2012 / Published: 16 May 2012
Cited by 28 | PDF Full-text (527 KB) | HTML Full-text | XML Full-text
Abstract
A pressurized liquid extraction (PLE) and high performance liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS) method was developed for the qualitative determination of saponins in different parts of P. notoginseng, including rhizome, root, fibre root, seed, stem, leaf and flower. The samples
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A pressurized liquid extraction (PLE) and high performance liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS) method was developed for the qualitative determination of saponins in different parts of P. notoginseng, including rhizome, root, fibre root, seed, stem, leaf and flower. The samples were extracted using PLE. The analysis was achieved on a Zorbax SB-C18 column with gradient elution of acetonitrile and 8 mM aqueous ammonium acetate as mobile phase. The mass spectrometer was operated in the negative ion mode using the electrospray ionization, and a collision induced dissociation (CID) experiment was also carried out to aid the identification of compounds. Forty one saponins were identified in different parts of P. notoginseng according to the fragmentation patterns and literature reports, among them, 21 saponins were confirmed by comparing the retention time and ESI-MS data with those of standard compounds. The results showed that the chemical characteristics were obviously diverse in different parts of P. notoginseng, which is helpful for pharmacological evaluation and quality control of P. notoginseng. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessReview Recent Advances in Photoinduced Electron Transfer Processes of Fullerene-Based Molecular Assemblies and Nanocomposites
Molecules 2012, 17(5), 5816-5835; https://doi.org/10.3390/molecules17055816
Received: 29 March 2012 / Revised: 3 May 2012 / Accepted: 8 May 2012 / Published: 16 May 2012
Cited by 86 | PDF Full-text (919 KB) | HTML Full-text | XML Full-text
Abstract
Photosensitized electron-transfer processes of fullerenes hybridized with electron donating or other electron accepting molecules have been surveyed in this review on the basis of the recent results reported mainly from our laboratories. Fullerenes act as photo-sensitizing electron acceptors with respect to a wide
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Photosensitized electron-transfer processes of fullerenes hybridized with electron donating or other electron accepting molecules have been surveyed in this review on the basis of the recent results reported mainly from our laboratories. Fullerenes act as photo-sensitizing electron acceptors with respect to a wide variety of electron donors; in addition, fullerenes in the ground state also act as good electron acceptors in the presence of light-absorbing electron donors such as porphyrins. With single-wall carbon nanotubes (SWCNTs), the photoexcited fullerenes act as electron acceptor. In the case of triple fullerene/porphyrin/SWCNT architectures, the photoexcited porphyrins act as electron donors toward the fullerene and SWCNT. These mechanisms are rationalized with the molecular orbital considerations performed for these huge supramolecules. For the confirmation of the electron transfer processes, transient absorption methods have been used, in addition to time-resolved fluorescence spectral measurements. The kinetic data obtained in solution are found to be quite useful to predict the efficiencies of photovoltaic cells. Full article
(This article belongs to the Special Issue Fullerene Chemistry)
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Open AccessArticle A Study of Proline Metabolism in Canola (Brassica napus L.) Seedlings under Salt Stress
Molecules 2012, 17(5), 5803-5815; https://doi.org/10.3390/molecules17055803
Received: 7 March 2012 / Revised: 25 April 2012 / Accepted: 26 April 2012 / Published: 16 May 2012
Cited by 20 | PDF Full-text (279 KB) | HTML Full-text | XML Full-text
Abstract
Expression analysis of crop plants has improved our knowledge about the veiled underlying mechanisms for salt tolerance. In order to observe the time course effects of salinity stress on gene expression for enzymes regulating proline metabolism, we comparatively analyzed the expression of specific
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Expression analysis of crop plants has improved our knowledge about the veiled underlying mechanisms for salt tolerance. In order to observe the time course effects of salinity stress on gene expression for enzymes regulating proline metabolism, we comparatively analyzed the expression of specific genes for proline metabolism in root and shoot tissues of salt-tolerant (cv. Dunkled) and salt-sensitive (cv. Cyclone) canola (Brassica napus L.) cultivars through reverse-transcriptase polymerase chain reaction (RT-PCR); following the NaCl treatment for various durations. Both lines showed an increase in ∆1-pyrroline-5-carboxylate synthase1 (P5CS1) gene expression after induction of salt stress with enhanced expression in the root tissue of the tolerant line, while maximum expression was noted in the shoot tissues of the sensitive line. We observed a much reduced proline dehydrogenase (PDH) expression in both the root and shoot tissues of both canola lines, with more marked reduction of PDH expression in the shoot tissues than that in the root ones. To confirm the increase in P5CS1 gene expression, total proline content was also measured in the root and shoot tissues of both the canola lines. The root tissues of canola sensitive line showed a gradually increasing proline concentration pattern with regular increase in salinity treatment, while an increase in proline concentration in the tolerant line was noted at 24 h post salinity treatment after a sudden decrease at 6 h and 12 h of salt treatment. A gradually increasing concentration of free proline content was found in shoot tissues of the tolerant canola line though a remarkable increase in proline concentration was noted in the sensitive canola line at 24 h post salinity treatment, indicating the initiation of proline biosynthesis process in that tissue of sensitive canola. Full article
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Open AccessArticle A New Facile Synthesis of D4-Pterosin B and D4-Bromopterosin, Deuterated Analogues of Ptaquiloside
Molecules 2012, 17(5), 5795-5802; https://doi.org/10.3390/molecules17055795
Received: 26 April 2012 / Revised: 9 May 2012 / Accepted: 14 May 2012 / Published: 16 May 2012
Cited by 5 | PDF Full-text (218 KB) | HTML Full-text | XML Full-text
Abstract
Ptaquiloside (Pta) is a potent carcinogen present in bracken fern and in soil matrices, that can potentially leach to the aquatic environment. More recently its presence in the milk of different farm animals has been reported. Pterosin B (Ptb) and bromopterosin (BrPt) represent
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Ptaquiloside (Pta) is a potent carcinogen present in bracken fern and in soil matrices, that can potentially leach to the aquatic environment. More recently its presence in the milk of different farm animals has been reported. Pterosin B (Ptb) and bromopterosin (BrPt) represent the most convenient analogues in the detection of ptaquiloside by mass spectrometry. Pterosin sesquiterpenes are also involved in many patented biomedical protocols. In this work we introduce a new and convenient approach to the synthesis in three steps and more than 80% yield of d4-pterosin B (d4-Ptb) and d4-bromopterosin (d4-BrPt), useful as internal standards in the quantification of ptaquiloside. Full article
(This article belongs to the Special Issue Challenges in Synthetic Chemistry)
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Open AccessArticle Luffa echinata Roxb. Induces Human Colon Cancer Cell (HT-29) Death by Triggering the Mitochondrial Apoptosis Pathway
Molecules 2012, 17(5), 5780-5794; https://doi.org/10.3390/molecules17055780
Received: 19 March 2012 / Revised: 9 May 2012 / Accepted: 11 May 2012 / Published: 16 May 2012
Cited by 22 | PDF Full-text (582 KB) | HTML Full-text | XML Full-text
Abstract
The antiproliferative properties and cell death mechanism induced by the extract of the fruits of Luffa echinata Roxb. (LER) were investigated. The methanolic extract of LER inhibited the proliferation of human colon cancer cells (HT-29) in both dose-dependent and time-dependent manners and caused
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The antiproliferative properties and cell death mechanism induced by the extract of the fruits of Luffa echinata Roxb. (LER) were investigated. The methanolic extract of LER inhibited the proliferation of human colon cancer cells (HT-29) in both dose-dependent and time-dependent manners and caused a significant increase in the population of apoptotic cells. In addition, obvious shrinkage and destruction of the monolayer were observed in LER-treated cells, but not in untreated cells. Analysis of the cell cycle after treatment of HT-29 cells with various concentrations indicated that LER extracts inhibited the cellular proliferation of HT-29 cells via G2/M phase arrest of the cell cycle. The Reactive oxygen species (ROS) level determination revealed that LER extracts induced apoptotic cell death via ROS generation. In addition, LER treatment led to a rapid drop in mitochondrial membrane potential (MMP) as a decrease in fluorescence. The transcripts of several apoptosis-related genes were investigated by RT-PCR analysis. The caspase-3 transcripts of HT-29 cells significantly accumulated and the level of Bcl-XL mRNA was decreased after treatment with LER extract. Furthermore, the ratio of mitochondria-dependent apoptosis genes (Bax and Bcl-2) was sharply increased from 1.6 to 54.1. These experiments suggest that LER has anticancer properties via inducing the apoptosis in colon cancer cells, which provided the impetus for further studies on the therapeutic potential of LER against human colon carcinoma. Full article
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