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Molecules, Volume 20, Issue 8 (August 2015), Pages 13496-15448

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Open AccessArticle Fatty Acid Profile of Milk and Cheese from Dairy Cows Supplemented a Diet with Palm Kernel Cake
Molecules 2015, 20(8), 15434-15448; https://doi.org/10.3390/molecules200815434
Received: 8 July 2015 / Revised: 11 August 2015 / Accepted: 17 August 2015 / Published: 24 August 2015
Cited by 16 | PDF Full-text (697 KB) | HTML Full-text | XML Full-text
Abstract
Lipid supplements (oilseeds vegetables) are included in ruminant diet to increase its energy density and improve fatty acid composition of milk and consequently of fresh cheese. Milk and cheeses were evaluated from crossbred Holstein × Zebu, fed diets enriched with 0%, 25%, 50%,
[...] Read more.
Lipid supplements (oilseeds vegetables) are included in ruminant diet to increase its energy density and improve fatty acid composition of milk and consequently of fresh cheese. Milk and cheeses were evaluated from crossbred Holstein × Zebu, fed diets enriched with 0%, 25%, 50%, and 75% inclusion levels of palm kernel cake in concentrated supplement, which were supplied daily (3.0 kg). Milk and fresh cheese (p = 0.001) fatty acids C12:0 exhibited quadratic negative values. Milk fatty acids C13:0, C20:0, C18:2t10c12, and C20:2n-6 presented positive quadratic values. The milk C18:2n-6 decreased linearly and in fresh cheese exhibited an increasing linear effect (p = 0.016). However, the fatty acids grouped in milk fat were not affected. The medium-chain fatty acids varied negatively and quadratically (p = 0.045). There was no effect on milk and fresh cheese chemical composition (p > 0.05). The milk fat was increased (p = 0.0065) quadratically (minimum point of 24.7%). Thus, the addition of palm kernel cake to cow diets negatively altered the fatty acid profile, it raises the percentage of lauric (C12) and tridecanoic (C13) acids fat which is not beneficial to human health from a nutraceutical perspective, although it did not influence the atherogenicity index. Full article
(This article belongs to the Section Metabolites)
Open AccessReview The Potential Use of Natural and Structural Analogues of Antimicrobial Peptides in the Fight against Neglected Tropical Diseases
Molecules 2015, 20(8), 15392-15433; https://doi.org/10.3390/molecules200815392
Received: 13 July 2015 / Revised: 2 August 2015 / Accepted: 10 August 2015 / Published: 24 August 2015
Cited by 12 | PDF Full-text (1661 KB) | HTML Full-text | XML Full-text | Correction
Abstract
Recently, research into the development of new antimicrobial agents has been driven by the increase in resistance to traditional antibiotics and Emerging Infectious Diseases. Antimicrobial peptides (AMPs) are promising candidates as alternatives to current antibiotics in the treatment and prevention of microbial infections.
[...] Read more.
Recently, research into the development of new antimicrobial agents has been driven by the increase in resistance to traditional antibiotics and Emerging Infectious Diseases. Antimicrobial peptides (AMPs) are promising candidates as alternatives to current antibiotics in the treatment and prevention of microbial infections. AMPs are produced by all known living species, displaying direct antimicrobial killing activity and playing an important role in innate immunity. To date, more than 2000 AMPs have been discovered and many of these exhibit broad-spectrum antibacterial, antiviral and anti-parasitic activity. Neglected tropical diseases (NTDs) are caused by a variety of pathogens and are particularly wide-spread in low-income and developing regions of the world. Alternative, cost effective treatments are desperately needed to effectively battle these medically diverse diseases. AMPs have been shown to be effective against a variety of NTDs, including African trypanosomes, leishmaniosis and Chagas disease, trachoma and leprosy. In this review, the potential of selected AMPs to successfully treat a variety of NTD infections will be critically evaluated. Full article
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Open AccessArticle Structure-Activity Relationships of the Antitumor C5-Curcuminoid GO-Y030
Molecules 2015, 20(8), 15374-15391; https://doi.org/10.3390/molecules200815374
Received: 24 July 2015 / Revised: 19 August 2015 / Accepted: 19 August 2015 / Published: 24 August 2015
Cited by 4 | PDF Full-text (936 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
1,5-Bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one (2) was isolated from Curcuma domestica as a curcumin (1)-related compound, which we named C5-curcumin. Intrigued by the potent antitumor activity of C5-curcumin (2)-related 1,5-bisaryl-1,4-pentadiene-3-ones [bis(arylmethylidene)acetones, termed C5-curcuminoids], we previously conducted a structure–activity relationship study of C5-curcuminoids and showed that highly active
[...] Read more.
1,5-Bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one (2) was isolated from Curcuma domestica as a curcumin (1)-related compound, which we named C5-curcumin. Intrigued by the potent antitumor activity of C5-curcumin (2)-related 1,5-bisaryl-1,4-pentadiene-3-ones [bis(arylmethylidene)acetones, termed C5-curcuminoids], we previously conducted a structure–activity relationship study of C5-curcuminoids and showed that highly active GO-Y030 [1,5-bis(3,5-bis(methoxymethoxy)phenyl)-1,4-pentadiene-3-one (4)] is the most promising antitumor compound. In this study, a panel of C5-curcuminoids based on GO-Y030, consisting of 30 new and 10 known compounds, was synthesized to elucidate in detail which moiety of GO-Y030 is significant for antitumor activity. The results confirmed that both the cross-conjugated dienone moiety and the 3,5-bis(methoxymethoxy) substituent are important for the antitumor activity. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Phenyllactic Acid from Lactobacillus plantarum PromotesAdipogenic Activity in 3T3-L1 Adipocyte via Up-Regulationof PPAR-γ2
Molecules 2015, 20(8), 15359-15373; https://doi.org/10.3390/molecules200815359
Received: 21 July 2015 / Revised: 17 August 2015 / Accepted: 19 August 2015 / Published: 24 August 2015
Cited by 2 | PDF Full-text (3108 KB) | HTML Full-text | XML Full-text
Abstract
Synthetic drugs are commonly used to cure various human ailments at present. However, the uses of synthetic drugs are strictly regulated because of their adverse effects. Thus, naturally occurring molecules may be more suitable for curing disease without unfavorable effects. Therefore, we investigated
[...] Read more.
Synthetic drugs are commonly used to cure various human ailments at present. However, the uses of synthetic drugs are strictly regulated because of their adverse effects. Thus, naturally occurring molecules may be more suitable for curing disease without unfavorable effects. Therefore, we investigated phenyllactic acid (PLA) from Lactobacillus plantarum with respect to its effects on adipogenic genes and their protein expression in 3T3-L1 pre-adipocytes by qPCR and western blot techniques. PLA enhanced differentiation and lipid accumulation in 3T3-L1 cells at the concentrations of 25, 50, and 100 μM. Maximum differentiation and lipid accumulation were observed at a concentration of 100 μM of PLA, as compared with control adipocytes (p < 0.05). The mRNA and protein expression of PPAR-γ2, C/EBP‑α, adiponectin, fatty acid synthase (FAS), and SREBP-1 were increased by PLA treatment as compared with control adipocytes (p < 0.05). PLA stimulates PPAR-γ mRNA expression in a concentration dependent manner, but this expression was lesser than agonist (2.83 ± 0.014 fold) of PPAR-γ2. Moreover, PLA supplementation enhances glucose uptake in 3T3-L1 pre-adipocytes (11.81 ± 0.17 mM) compared to control adipocytes, but this glucose uptake was lesser than that induced by troglitazone (13.75 ± 0.95 mM) and insulin treatment (15.49 ± 0.20 mM). Hence, we conclude that PLA treatment enhances adipocyte differentiation and glucose uptake via activation of PPAR-γ2, and PLA may thus be the potential candidate for preventing Type 2 Diabetes Mellitus (T2DM). Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle The Influence of Sesquiterpenes from Myrica rubra on the Antiproliferative and Pro-Oxidative Effects of Doxorubicin and Its Accumulation in Cancer Cells
Molecules 2015, 20(8), 15343-15358; https://doi.org/10.3390/molecules200815343
Received: 9 July 2015 / Revised: 6 August 2015 / Accepted: 13 August 2015 / Published: 21 August 2015
Cited by 14 | PDF Full-text (1161 KB) | HTML Full-text | XML Full-text
Abstract
The sesquiterpenes β-caryophyllene, β-caryophyllene oxide (CAO), α-humulene (HUM), trans-nerolidol (NER), and valencene (VAL) are substantial components of the essential oil from Myrica rubra leaves which has exhibited significant antiproliferative effects in several intestinal cancer cell lines, with CaCo-2 cells being the most
[...] Read more.
The sesquiterpenes β-caryophyllene, β-caryophyllene oxide (CAO), α-humulene (HUM), trans-nerolidol (NER), and valencene (VAL) are substantial components of the essential oil from Myrica rubra leaves which has exhibited significant antiproliferative effects in several intestinal cancer cell lines, with CaCo-2 cells being the most sensitive. The present study was designed to evaluate the effects of these sesquiterpenes on the efficacy and toxicity of the anticancer drug doxorubicin (DOX) in CaCo-2 cancer cells and in primary culture of rat hepatocytes. Our results showed that HUM, NER, VAL and CAO inhibited proliferation of CaCo-2 cancer cells but they did not affect the viability of hepatocytes. CAO, NER and VAL synergistically potentiated the efficacy of DOX in cancer cells killing. All sesquiterpenes exhibited the ability to selectively increase DOX accumulation in cancer cells and did not affect DOX concentration in hepatocytes. Additionally, CAO and VAL were able to increase the pro-oxidative effect of DOX in CaCo-2 cells. Moreover, CAO mildly ameliorated DOX toxicity in hepatocytes. Based on all results, CAO seems to be the most promising compound for further testing. Full article
(This article belongs to the collection Herbal Medicine Research)
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Open AccessArticle α-Glucosidase Inhibitors from Vauquelinia corymbosa
Molecules 2015, 20(8), 15330-15342; https://doi.org/10.3390/molecules200815330
Received: 4 July 2015 / Revised: 15 August 2015 / Accepted: 18 August 2015 / Published: 21 August 2015
Cited by 7 | PDF Full-text (4048 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The α-glucosidase inhibitory activity of an aqueous extract and compounds from the aerial parts of V. corymbosa was demonstrated with yeast and rat small intestinal α-glucosidases. The aqueous extract inhibited yeast α-glucosidase with a half maximal inhibitory concentration (IC50) of 28.6
[...] Read more.
The α-glucosidase inhibitory activity of an aqueous extract and compounds from the aerial parts of V. corymbosa was demonstrated with yeast and rat small intestinal α-glucosidases. The aqueous extract inhibited yeast α-glucosidase with a half maximal inhibitory concentration (IC50) of 28.6 μg/mL. Bioassay-guided fractionation of the extract led to the isolation of several compounds, including one cyanogenic glycoside [prunasin (1)], five flavonoids [(−)-epi-catechin (2), hyperoside (3), isoquercetin (4), quercitrin (5) and quercetin-3-O-(6′′-benzoyl)-β-galactoside (6)] and two simple aromatic compounds [picein (7) and methylarbutin (8)]. The most active compound was 6 with IC50 values of 30 μM in the case of yeast α-glucosidase, and 437 μM in the case of the mammalian enzyme. According to the kinetic analyses performed with rat and yeast enzymes, this compound behaved as mixed-type inhibitor; the calculated inhibition constants (Ki) were 212 and 50 μM, respectively. Molecular docking analyses with yeast and mammalian α-glucosidases revealed that compound 6 bind differently to these enzymes. Altogether, the results of this work suggest that preparations of V. corymbosa might delay glucose absorption in vivo. Full article
(This article belongs to the collection Bioactive Compounds)
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Open AccessArticle Aqueous Extract of Tomato (Solanum lycopersicum L.) and Ferulic Acid Reduce the Expression of TNF-α and IL-1β in LPS-Activated Macrophages
Molecules 2015, 20(8), 15319-15329; https://doi.org/10.3390/molecules200815319
Received: 8 June 2015 / Revised: 14 August 2015 / Accepted: 17 August 2015 / Published: 21 August 2015
Cited by 16 | PDF Full-text (1028 KB) | HTML Full-text | XML Full-text
Abstract
Acute inflammation is essential for defending the body against pathogens; however, when inflammation becomes chronic, it is harmful to the body and is part of the pathophysiology of various diseases such as Diabetes Mellitus type 2 (DM2) and Cardiovascular Disease (CVD) among others.
[...] Read more.
Acute inflammation is essential for defending the body against pathogens; however, when inflammation becomes chronic, it is harmful to the body and is part of the pathophysiology of various diseases such as Diabetes Mellitus type 2 (DM2) and Cardiovascular Disease (CVD) among others. In chronic inflammation macrophages play an important role, mainly through the secretion of proinflammatory cytokines such as Tumor necrosis factor (TNF)-α and Interleukin (IL)-1β, explained in part by activation of the Toll-like receptor 4 (TLR4), a signaling pathway which culminates in the activation of Nuclear factor (NF)-κB, an important transcription factor in the expression of these proinflammatory genes. On the other hand, the benefits on health of a diet rich in fruit and vegetables are well described. In this work, the effects of aqueous extract of tomato and ferulic acid on the expression of proinflammatory cytokines in LPS activated monocyte-derived THP-1 macrophages were investigated. In addition, using Western blot, we investigated whether the inhibition was due to the interference on activation of NF-κB. We found that both the tomato extract and ferulic acid presented inhibitory activity on the expression of TNF-α and IL-1β cytokine by inhibiting the activation of NF-κB. The current results suggest that tomatoes and ferulic acid may contribute to prevention of chronic inflammatory diseases. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Optimization of Micellar Electrokinetic Chromatography Method for the Simultaneous Determination of Seven Hydrophilic and Four Lipophilic Bioactive Components in Three Salvia Species
Molecules 2015, 20(8), 15304-15318; https://doi.org/10.3390/molecules200815304
Received: 4 August 2015 / Revised: 15 August 2015 / Accepted: 18 August 2015 / Published: 21 August 2015
Cited by 5 | PDF Full-text (1062 KB) | HTML Full-text | XML Full-text
Abstract
A micellar electrokinetic chromatography (MEKC) method was developed for the simultaneous determination of seven hydrophilic phenolic acids and four lipophilic tanshinones in three Salvia species. In normal MEKC mode using SDS as surfactant, the investigated 11 compounds could not be well separated. Therefore,
[...] Read more.
A micellar electrokinetic chromatography (MEKC) method was developed for the simultaneous determination of seven hydrophilic phenolic acids and four lipophilic tanshinones in three Salvia species. In normal MEKC mode using SDS as surfactant, the investigated 11 compounds could not be well separated. Therefore, several buffer modifiers including β-cyclodextrins (β-CD), ionic liquid 1-butyl-3-methylimidazolium tetrafluoroborate ([bmim]BF4) and organic solvents have been added to the buffer solution to improve the separation selectivity. Under the optimized conditions (BGE, 15 mM sodium tetraborate with 10 mM SDS, 5 mM β-CD, 10 mM [bmim]BF4 and 15% ACN (v/v) as additives; buffer pH, 9.8; voltage, 20 kV; temperature, 25 °C), the 11 investigated analytes could achieve baseline separation in 34 min. The proposed MEKC was additionally validated by evaluating the linearity (R2 ≥ 0.9965), LODs (0.27–1.39 μg·mL–1), and recovery (94.26%–105.17%), demonstrating this method was reproducible, accurate and reliable. Moreover, the contents of the 11 compounds in three Salvia species, including S. miltiorrhiza, S. przewalskii and S. castanea were analyzed. The result showed that the established MEKC method was simple and practical for the simultaneous determination of the hydrophilic and lipophilic bioactive components in Salvia species, which could be used to effectively evaluate the quality of these valued medicinal plants. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Design and Synthesis of Imidazopyrazolopyridines as Novel Selective COX-2 Inhibitors
Molecules 2015, 20(8), 15287-15303; https://doi.org/10.3390/molecules200815287
Received: 22 July 2015 / Revised: 2 August 2015 / Accepted: 6 August 2015 / Published: 21 August 2015
Cited by 4 | PDF Full-text (1444 KB) | HTML Full-text | XML Full-text
Abstract
The usefulness of non-steroidal anti-inflammatory drugs (NSAIDs) is hampered by their gastrointestinal side effects. Non-selective cyclooxygenases inhibitors interfere with both COX-1 and COX-2 isozymes. Since COX-1 mediates cytoprotection of gastric mucosa, its inhibition leads to the undesirable side effects. On the other hand,
[...] Read more.
The usefulness of non-steroidal anti-inflammatory drugs (NSAIDs) is hampered by their gastrointestinal side effects. Non-selective cyclooxygenases inhibitors interfere with both COX-1 and COX-2 isozymes. Since COX-1 mediates cytoprotection of gastric mucosa, its inhibition leads to the undesirable side effects. On the other hand, COX-2 is undetectable in normal tissues and selectively induced by inflammatory stimuli. Therefore, it is strongly believed that the therapeutic benefits derive from inhibition of COX-2 only. The presence of a strong connection between reported COX-2 inhibitors and cardiac toxicity encourages medicinal chemists to explore new scaffolds. In the present study, we introduced imidazopyrazolopyridines as new potent and selective COX-2 inhibitors that lack the standard pharmacophoric binding features to hERG. Starting from our lead compound 5a, structure-based drug-design was conducted and more potent analogues were obtained with high COX-2 selectivity and almost full edema protection, in carrageenan-induced edema assay, in case of compound 5e. Increased bulkiness around imidazopyrazolopyridines by adding a substituted phenyl ring(s) afforded less active compounds. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle Ultrasound-Assisted Aqueous Two-Phase System for Extraction and Enrichment of Zanthoxylum armatum Lignans
Molecules 2015, 20(8), 15273-15286; https://doi.org/10.3390/molecules200815273
Received: 16 June 2015 / Revised: 2 August 2015 / Accepted: 17 August 2015 / Published: 20 August 2015
Cited by 9 | PDF Full-text (1116 KB) | HTML Full-text | XML Full-text
Abstract
In the study, an aqueous two phase system (ATPS) coupled with ultrasound was employed to extract lignans from Zanthoxylum armatum. Three standard lignans, namely (−)-fargesin, sesamin and L-asarinin, were used as marker compounds, and extraction was optimized and projected by response surface
[...] Read more.
In the study, an aqueous two phase system (ATPS) coupled with ultrasound was employed to extract lignans from Zanthoxylum armatum. Three standard lignans, namely (−)-fargesin, sesamin and L-asarinin, were used as marker compounds, and extraction was optimized and projected by response surface methodology (RSM) and artificial neural network (ANN). The optimal condition for ATPS with 20% n-propanol and 24% (NH4)2SO4 coupled with ultrasonic-assisted extraction including a solvent to solid ratio of 15:1, a temperature of 40 °C, and a treatment time of 55 min was obtained. Under the condition, the yield of (−)-fargesin increased 15.12%, and the purities of (−)-fargesin, sesamin and L-asarinin reached 2.222%, 1.066%, and 1.583%, with an increase of 44.38%, 25.70%, and 26.34% compared to those extracted with 95% ethanol, respectively. Coefficient of the determined (0.9855) and mean squared error (0.0018) of ANN model suggested good fitness and generalization of the ANN. Taken together, the results showed that ultrasonic-assisted ATPS can be a suitable method for extraction and enrichment of lignans from Z. armatum. Full article
(This article belongs to the Special Issue New Technologies for the Recovery of Natural Products)
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Open AccessReview Optimal Energy Transfer in Light-Harvesting Systems
Molecules 2015, 20(8), 15224-15272; https://doi.org/10.3390/molecules200815224
Received: 22 June 2015 / Revised: 3 August 2015 / Accepted: 14 August 2015 / Published: 20 August 2015
Cited by 11 | PDF Full-text (4102 KB) | HTML Full-text | XML Full-text
Abstract
Photosynthesis is one of the most essential biological processes in which specialized pigment-protein complexes absorb solar photons, and with a remarkably high efficiency, guide the photo-induced excitation energy toward the reaction center to subsequently trigger its conversion to chemical energy. In this work,
[...] Read more.
Photosynthesis is one of the most essential biological processes in which specialized pigment-protein complexes absorb solar photons, and with a remarkably high efficiency, guide the photo-induced excitation energy toward the reaction center to subsequently trigger its conversion to chemical energy. In this work, we review the principles of optimal energy transfer in various natural and artificial light harvesting systems. We begin by presenting the guiding principles for optimizing the energy transfer efficiency in systems connected to dissipative environments, with particular attention paid to the potential role of quantum coherence in light harvesting systems. We will comment briefly on photo-protective mechanisms in natural systems that ensure optimal functionality under varying ambient conditions. For completeness, we will also present an overview of the charge separation and electron transfer pathways in reaction centers. Finally, recent theoretical and experimental progress on excitation energy transfer, charge separation, and charge transport in artificial light harvesting systems is delineated, with organic solar cells taken as prime examples. Full article
(This article belongs to the Special Issue Light-Harvesting Complexes)
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Open AccessArticle Synthesis and Evaluation of Selected Benzimidazole Derivatives as Potential Antimicrobial Agents
Molecules 2015, 20(8), 15206-15223; https://doi.org/10.3390/molecules200815206
Received: 28 June 2015 / Revised: 9 August 2015 / Accepted: 10 August 2015 / Published: 20 August 2015
Cited by 16 | PDF Full-text (782 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial
[...] Read more.
A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. In particular, some compounds displayed antibacterial activity against two methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) comparable to the widely-used drug ciprofloxacin. The compounds have some common features; three possess 5-halo substituents; two are derivatives of (S)-2-ethanaminebenzimidazole; and the others are derivatives of one 2-(chloromethyl)-1H-benzo[d]imidazole and (1H-benzo[d]imidazol-2-yl)methanethiol. The results from the antifungal screening were also very interesting: 23 compounds exhibited potent fungicidal activity against the selected fungal strains. They displayed equivalent or greater potency in their MIC values than amphotericin B. The 5-halobenzimidazole derivatives could be considered promising broad-spectrum antimicrobial candidates that deserve further study for potential therapeutic applications. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessEditorial Protein-Carbohydrate Interactions, and Beyond …
Molecules 2015, 20(8), 15202-15205; https://doi.org/10.3390/molecules200815202
Received: 17 August 2015 / Revised: 17 August 2015 / Accepted: 19 August 2015 / Published: 20 August 2015
Cited by 2 | PDF Full-text (630 KB) | HTML Full-text | XML Full-text
Abstract
Carbohydrates are ubiquitous and play an intriguing role inside the cell as well as on the cell surface.[...] Full article
(This article belongs to the Special Issue Protein-Carbohydrate Interactions, and Beyond)
Open AccessArticle A New Ionone Glycoside and Three New Rhemaneolignans from the Roots of Rehmannia glutinosa
Molecules 2015, 20(8), 15192-15201; https://doi.org/10.3390/molecules200815192
Received: 25 June 2015 / Revised: 13 August 2015 / Accepted: 14 August 2015 / Published: 20 August 2015
Cited by 6 | PDF Full-text (1199 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A new ionone glycoside, frehmaglutoside I (1), and three new rhemaneolignans AC (24) were isolated from the 95% EtOH extract of the roots of Rehmannia glutinosa. Their structures were determined by extensive spectroscopic (UV, IR,
[...] Read more.
A new ionone glycoside, frehmaglutoside I (1), and three new rhemaneolignans AC (24) were isolated from the 95% EtOH extract of the roots of Rehmannia glutinosa. Their structures were determined by extensive spectroscopic (UV, IR, HR-ESI-MS, 1D and 2D NMR) analyses. In addition, these compounds were evaluated for their protective effects on cardiocytes impaired by doxorubicin in H9c2 cells. Among them, compounds 13 exhibited protective effects against DOX-induced cardiotoxicity. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Characterization of the Sublimation and Vapor Pressure of 2-(2-Nitrovinyl) Furan (G-0) Using Thermogravimetric Analysis: Effects of Complexation with Cyclodextrins
Molecules 2015, 20(8), 15175-15191; https://doi.org/10.3390/molecules200815175
Received: 3 July 2015 / Revised: 15 August 2015 / Accepted: 17 August 2015 / Published: 19 August 2015
Cited by 2 | PDF Full-text (2312 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
In the present work, the sublimation of crystalline solid 2-(2-nitrovinyl) furan (G-0) in the temperature range of 35 to 60 °C (below the melting point of the drug) was studied using thermogravimetric analysis (TGA). The sublimated product was characterized using Fourier-transformed-infrared spectroscopy (FT-IR)
[...] Read more.
In the present work, the sublimation of crystalline solid 2-(2-nitrovinyl) furan (G-0) in the temperature range of 35 to 60 °C (below the melting point of the drug) was studied using thermogravimetric analysis (TGA). The sublimated product was characterized using Fourier-transformed-infrared spectroscopy (FT-IR) and thin layer chromatography (TLC). The sublimation rate at each temperature was obtained using the slope of the linear regression model and followed apparent zero-order kinetics. The sublimation enthalpy from 35 to 60 °C was obtained from the Eyring equation. The Gückel method was used to estimate the sublimation rate and vapor pressure at 25 °C. Physical mixtures, kneaded and freeze-dried complexes were prepared with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and sulfobutyl ether-β-cyclodextrin (SBE-β-CD) and analyzed using isothermal TGA at 50 °C. The complexation contributed to reducing the sublimation process. The best results were achieved using freeze-dried complexes with both cyclodextrins. Full article
(This article belongs to the collection Poorly Soluble Drugs)
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