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Molecules, Volume 17, Issue 10 (October 2012), Pages 11294-12468

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Open AccessArticle A Sub-Pathway Based Method to Identify Candidate Agents for Ankylosing Spondylitis
Molecules 2012, 17(10), 12460-12468; https://doi.org/10.3390/molecules171012460
Received: 26 June 2012 / Revised: 25 September 2012 / Accepted: 26 September 2012 / Published: 22 October 2012
Cited by 1 | PDF Full-text (219 KB) | HTML Full-text | XML Full-text
Abstract
The need for new therapeutics for Ankylosing Spondylitis (AS) is highlighted by the general lack of efficacy for most agents currently available for this disease. Many recent studies have detailed molecular pathways in AS, and several molecule-targeting agents are undergoing evaluation. We aimed
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The need for new therapeutics for Ankylosing Spondylitis (AS) is highlighted by the general lack of efficacy for most agents currently available for this disease. Many recent studies have detailed molecular pathways in AS, and several molecule-targeting agents are undergoing evaluation. We aimed to explore the mechanism of AS and identify biologically active small molecules capable of targeting the sub-pathways which were disregulated in the development of AS. By using the GSE25101 microarray data accessible from the Gene Expression Omnibus database, we first identified the differentially expressed genes (DEGs) between AS samples and healthy controls, followed by the sub-pathway enrichment analysis of the DEGs. In addition, we propose the use of an approach based on targeting sub-pathways to identify potential agents for AS. A total of 3,280 genes were identified as being significantly different between patients and controls with p-values < 0.1. Our study showed that neurotrophic signaling pathway and some immune-associated pathways may be involved in the development of AS. Besides, our bioinformatics analysis revealed a total of 15 small molecules which may play a role in perturbing the development of AS. Our study proposes the use of an approach based on targeting sub-pathways to identify potential agents for AS. Candidate agents identified by our approach may provide the groundwork for a combination therapy approach for AS. Full article
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Open AccessArticle Acute Toxicity and Gastroprotective Effect of the Schiff Base Ligand 1H-Indole-3-ethylene-5-nitrosalicylaldimine and Its Nickel (II) Complex on Ethanol Induced Gastric Lesions in Rats
Molecules 2012, 17(10), 12449-12459; https://doi.org/10.3390/molecules171012449
Received: 12 September 2012 / Revised: 4 October 2012 / Accepted: 5 October 2012 / Published: 22 October 2012
Cited by 9 | PDF Full-text (355 KB) | HTML Full-text | XML Full-text
Abstract
The present study was performed to evaluate the gastroprotective activity of Schiff base ligand derived from the condensation reaction of tryptamine (an indole derivative) and 5-nitrosalicylaldehyde (TNS) and its nickel (II) complex against ethanol-induced gastric ulcer in rats. The compounds were orally administered
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The present study was performed to evaluate the gastroprotective activity of Schiff base ligand derived from the condensation reaction of tryptamine (an indole derivative) and 5-nitrosalicylaldehyde (TNS) and its nickel (II) complex against ethanol-induced gastric ulcer in rats. The compounds were orally administered with low (30 mg/kg) and high (60 mg/kg) doses to ulcer-induced Sprague-Dawley rats. Macroscopically, the ulcer control group exhibited severe mucosal injury, whereas pre-treatment with either cimetidine or TNS and its nickel (II) complex each resulted in significant protection against gastric mucosal injury. Flattening of gastric mucosal folds was also observed in rats pretreated with TNS and its nickel complex. Histological studies of the gastric wall of ulcer control group revealed severe damage of gastric mucosa, along with edema and leucocytes infiltration of the submucosal layer compared to rats pre-treated with either cimetidine or TNS and its nickel (II) compound, where there was marked gastric protection along with reduction of edema and leucocytes infiltration of the submucosal layer. Acute toxicity study done on mice with a higher dose of 5 g/kg of TNS and its nickel (II) complex did not manifest any toxicological signs. Research finding suggest that TNS and its nickel (II) complex could be considered as effective gastroprotective compounds. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Synthesis, FTIR, 13C-NMR and Temperature-Dependent 1H‑NMR Characteristics of Bis-naphthalimide Derivatives
Molecules 2012, 17(10), 12427-12448; https://doi.org/10.3390/molecules171012427
Received: 5 September 2012 / Revised: 17 October 2012 / Accepted: 18 October 2012 / Published: 22 October 2012
Cited by 3 | PDF Full-text (1010 KB) | HTML Full-text | XML Full-text
Abstract
Chemotherapy is still the most important method of cancer treatment. To make this method more effective and safe, new drugs to destroy cancer cells are needed. Some bis-naphthalimide derivatives show potential anticancer activity via an intercalation mechanism. A higher degree of DNA intercalation
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Chemotherapy is still the most important method of cancer treatment. To make this method more effective and safe, new drugs to destroy cancer cells are needed. Some bis-naphthalimide derivatives show potential anticancer activity via an intercalation mechanism. A higher degree of DNA intercalation corresponds to better therapeutic effects. The degree of intercalation of naphthalimides depends on their structure, molecular dynamics and intermolecular interactions with DNA. In order to apply any active substance as a drug, its molecular dynamics as well as possible interactions with target molecules have to be examined in exhaustive details. This paper describes a practical preparation of some novel bis-naphthalimide derivatives with different functional groups and their FTIR and 1H- and 13C-NMR spectral characteristics. To determine the molecular dynamics of the obtained compounds the temperature, their 1H-NMR spectra were measured. It has been clearly proven in this paper that the unusual temperature-dependent 1H-NMR behavior of the aromatic protons of phthalimide derivatives, previously described in the literature as “hypersensitivity” and explained by n-π interactions and molecular motions of aromatic amide rings, is a result of temperature driven changes of the geometry of carbonyl groups. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle The Effect of Curcumin on Human Bronchial Epithelial Cells Exposed to Fine Particulate Matter: A Predictive Analysis
Molecules 2012, 17(10), 12406-12426; https://doi.org/10.3390/molecules171012406
Received: 12 July 2012 / Revised: 15 October 2012 / Accepted: 16 October 2012 / Published: 22 October 2012
Cited by 5 | PDF Full-text (2059 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Fine particulate matter (PM2.5) has been associated in humans with inflammation, oxidative stress and cancer. Studies had shown that curcumin could potentially inhibit these effects; however, there had been no in vivo or in vitro reports about the effects of curcumin
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Fine particulate matter (PM2.5) has been associated in humans with inflammation, oxidative stress and cancer. Studies had shown that curcumin could potentially inhibit these effects; however, there had been no in vivo or in vitro reports about the effects of curcumin on organisms exposed to PM2.5. This predictive study explored the possible biological functions and pathways involved in the mechanism of curcumin inhibition of the hazardous effects of PM2.5. For predictive analysis, microarray data were used to investigate the effect of PM2.5 on human bronchial epithelial cells (HBEC), and human target proteins of curcumin were retrieved from PubChem. Two protein-protein interaction (PPI) networks were established based upon differential genes and target proteins, respectively, and the common network of these two networks was found. Functional and pathway analysis of the common network was performed using the Ingenuity Pathways Analysis (IPA) software. The results suggested that the predictive effects of curcumin on HBEC exposed to PM2.5 were involved in bio-functions, including inflammatory response of airway, cancerogenesis, and apoptosis, and in pathways such as cancer, glucocorticoid receptor signaling, and NF-kappaB signaling. This study predicted for the first time that curcumin could be a potential therapeutic agent for protecting the human airway from the hazardous effects of PM2.5. Full article
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Open AccessArticle trans-Resveratrol in Nutraceuticals: Issues in Retail Quality and Effectiveness
Molecules 2012, 17(10), 12393-12405; https://doi.org/10.3390/molecules171012393
Received: 31 August 2012 / Revised: 13 September 2012 / Accepted: 15 October 2012 / Published: 22 October 2012
Cited by 26 | PDF Full-text (398 KB) | HTML Full-text | XML Full-text
Abstract
Fourteen brands of resveratrol-containing nutraceuticals were evaluated in order to verify their actual resveratrol content and to control if their health-promoting properties are related to manufacturing quality. Products included pure resveratrol capsules or multi-ingredient formulations with standardized amounts of resveratrol and other phytochemicals.
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Fourteen brands of resveratrol-containing nutraceuticals were evaluated in order to verify their actual resveratrol content and to control if their health-promoting properties are related to manufacturing quality. Products included pure resveratrol capsules or multi-ingredient formulations with standardized amounts of resveratrol and other phytochemicals. Samples were analyzed for total trans-resveratrol, flavonoids, procyanidin, polyphenol content and the results were compared with the content declared on-label. Only five out of 14 brands had near label values, compliant with Good Manufacturing Practices (GMP) requirements (95–105% content of active constituent), four products were slightly out of this range (83–111%) and three were in the 8–64% range. Two samples were below the limit of detection. The greater the difference between actual and labeled resveratrol content, the lower was the antioxidant and antiproliferative activity strength. Dietary supplements containing pure trans-resveratrol exhibited a greater induction of differentiation towards human leukemic K562 cells when compared to multicomponent products. Great differences currently exist among resveratrol food supplements commercially available and GMP-grade quality should not be taken for granted. On the other side, dosages suggested by most “pure”, “high-dosage” supplements may allow a supplementation level adequate to obtain some of the purported health benefits. Full article
(This article belongs to the Special Issue Methods in Polyphenol Analysis)
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Open AccessArticle Synthesis of a Cholesteryl-HEG Phosphoramidite Derivative and Its Application to Lipid-conjugates of the Anti-HIV 5'TGGGAG3' Hotoda’s Sequence
Molecules 2012, 17(10), 12378-12392; https://doi.org/10.3390/molecules171012378
Received: 19 September 2012 / Revised: 16 October 2012 / Accepted: 17 October 2012 / Published: 22 October 2012
Cited by 5 | PDF Full-text (316 KB) | HTML Full-text | XML Full-text
Abstract
A novel phosphoramidite derivative of cholesterol, with an ether-linked hexaethylene glycol (HEG) spacer arm, has been obtained through simple and reproducible solid phase modified oligonucleotide synthesis manipulations. This building block and the known phosphoramidite derivative of 3b-(2-hydroxyethoxy)cholesterol have been exploited in standard oligonucleotide
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A novel phosphoramidite derivative of cholesterol, with an ether-linked hexaethylene glycol (HEG) spacer arm, has been obtained through simple and reproducible solid phase modified oligonucleotide synthesis manipulations. This building block and the known phosphoramidite derivative of 3b-(2-hydroxyethoxy)cholesterol have been exploited in standard oligonucleotide synthesis protocols for the preparation of 5'- conjugates of the G-quadruplex-forming 5'TGGGAG3' oligomer, known as the Hotoda’s sequence, to produce new potential anti-HIV agents. Full article
(This article belongs to the Special Issue Nucleic Acid Analogs)
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Open AccessArticle Phenylmethimazole Blocks dsRNA-Induced IRF3 Nuclear Translocation and Homodimerization
Molecules 2012, 17(10), 12365-12377; https://doi.org/10.3390/molecules171012365
Received: 5 October 2012 / Revised: 16 October 2012 / Accepted: 19 October 2012 / Published: 22 October 2012
Cited by 7 | PDF Full-text (856 KB) | HTML Full-text | XML Full-text
Abstract
Previous studies revealed that phenylmethimazole (C10) inhibits IRF3 signaling, preventing dsRNA-induction of type 1 interferon gene expression, production, and downstream signaling. In the present study, we investigated the molecular basis for C10 inhibition of dsRNA-stimulated IRF3 signaling. IRF-3 Trans-AM assays were used to
[...] Read more.
Previous studies revealed that phenylmethimazole (C10) inhibits IRF3 signaling, preventing dsRNA-induction of type 1 interferon gene expression, production, and downstream signaling. In the present study, we investigated the molecular basis for C10 inhibition of dsRNA-stimulated IRF3 signaling. IRF-3 Trans-AM assays were used to measure C10 effects on dsRNA induction of IRF3 DNA binding. Green fluorescent protein-labeled IRF3 was used to measure C10 effects on dsRNA-induced IRF3 nuclear translocation. Native PAGE, SDS PAGE, and western blotting were used to identify effects of C10 on IRF3 homodimer formation and phosphorylation, respectively. There was a significant impairment of dsRNA-induced IRF3 DNA binding activity in human embryonic kidney and pancreatic cancer cells with C10 treatment. C10 also blocked dsRNA-induced IRF3 nuclear translocation and homodimer formation without blocking serine 396 phosphorylation of IRF3. Together, these results indicate that C10 interferes with IRF3 signaling by blocking dsRNA-induced IRF3 homodimer formation, a prerequisite for nuclear translocation and DNA binding activities. Full article
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Open AccessArticle Two New Cholic Acid Derivatives from the Marine Ascidian-Associated Bacterium Hasllibacter halocynthiae
Molecules 2012, 17(10), 12357-12364; https://doi.org/10.3390/molecules171012357
Received: 13 August 2012 / Revised: 8 October 2012 / Accepted: 17 October 2012 / Published: 22 October 2012
Cited by 2 | PDF Full-text (251 KB) | HTML Full-text | XML Full-text
Abstract
The investigation of secondary metabolites in liquid cultures of a recently discovered marine bacterium, Hasllibacter halocynthiae strain KME 002T, led to the isolation of two new cholic acid derivatives. The structures of these compounds were determined to be 3,3,12-trihydroxy-7-ketocholanic acid (
[...] Read more.
The investigation of secondary metabolites in liquid cultures of a recently discovered marine bacterium, Hasllibacter halocynthiae strain KME 002T, led to the isolation of two new cholic acid derivatives. The structures of these compounds were determined to be 3,3,12-trihydroxy-7-ketocholanic acid (1) and 3,3,12-trihydroxy-7-deoxycholanic acid (2) through HRFABMS and NMR data analyses. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Comparison of the Phenolic Compounds, Carotenoids and Tocochromanols Content in Wheat Grain under Organic and Mineral Fertilization Regimes
Molecules 2012, 17(10), 12341-12356; https://doi.org/10.3390/molecules171012341
Received: 21 July 2012 / Revised: 26 September 2012 / Accepted: 9 October 2012 / Published: 19 October 2012
Cited by 17 | PDF Full-text (364 KB) | HTML Full-text | XML Full-text
Abstract
A field study was performed to evaluate the effect of mineral (NPK) and organic-based fertilizers such as compost (C), manure (FYM) and meat and bone meal (MBM) on the appearance (dimensions and color) of spring wheat kernels and on the total content in
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A field study was performed to evaluate the effect of mineral (NPK) and organic-based fertilizers such as compost (C), manure (FYM) and meat and bone meal (MBM) on the appearance (dimensions and color) of spring wheat kernels and on the total content in grain of main its phytochemicals (polyphenols, carotenoids and tocochromanols) and phenolic acids composition. Total phenolic compounds were determined using the Folin-Ciocalteu assay after alkaline hydrolysis of grain and carotenoids were analyzed spectrophotometrically. Composition of tocochromanols and phenolic acids was determined using RP-HPLC techniques. Only insignificant differences in the appearance of kernels and small changes in the content and composition of grain phytochemicals were noted between the studied fertilization systems. Among the analyzed phytochemicals the greatest variation was observed in the group of polyphenol compounds, with a stated increase of their total content of 6.7 and 11.2% in grain fertilized with MBM and compost, respectively. Simultaneously the grain from organic fertilization contained significantly less phenolic acids, and the decrease in their content ranged from 10.0% for FYM to 24.8% for MBM+EM-1. Organically and conventionally fertilized grain had similar amounts of tocochromanols and carotenoids. Comparison of MBM and MBM+EM-1 variants showed that application of effective microorganisms decreased carotenoids and tocochromanols content by 8.5 and 9.7%, respectively. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Phenolic and Lignan Glycosides from the Butanol Extract of Averrhoa carambola L. Root
Molecules 2012, 17(10), 12330-12340; https://doi.org/10.3390/molecules171012330
Received: 26 September 2012 / Revised: 11 October 2012 / Accepted: 12 October 2012 / Published: 19 October 2012
Cited by 19 | PDF Full-text (213 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Fifteen compounds, which included six chiral lignans and nine phenolic glycosides, were separated from the butanol fraction of Averrhoa carambola L. root and identified. All of the compounds, namely 3,4,5-trimethoxyphenol-1-O-β-D-glucopyranoside (1), benzyl-1-O-β-
[...] Read more.
Fifteen compounds, which included six chiral lignans and nine phenolic glycosides, were separated from the butanol fraction of Averrhoa carambola L. root and identified. All of the compounds, namely 3,4,5-trimethoxyphenol-1-O-β-D-glucopyranoside (1), benzyl-1-O-β-D-glucopyranoside (2), (+)-5'-methoxyisolariciresinol 3α-O-β-D-gluco-pyranoside (3), (+)-isolariciresinol 3α-O-β-D-glucopyranoside (4), koaburaside (5), (+)-lyoniresinol 3α-O-β-D-glucopyranoside (6), (−)-lyoniresinol 3α-O-β-D-glucopyranoside (7), (−)-5'-methoxyisolariciresinol 3α-O-β-D-glucopyranoside (8), (−)-isolariciresinol 3α-O-β-D-glucopyranoside (9), 3,5-dimethoxy-4-hydroxyphenyl 1-O-β-apiofuranosyl (1''→6')-O-β-D-glucopyranoside (10), 3,4,5-trimethoxyphenyl 1-O-β-apiofuranosyl (1''→6')-β-gluco-pyranoside (11), methoxyhydroquinone-4-β-D-glucopyranoside (12), (2S)-2-O-β-D-gluco-pyranosyl-2-hydroxyphenylacetic acid (13), 3-hydroxy-4-methoxyphenol 1-O-D-apio-furanosyl-(1''→6')-O-β-D-glucopyranoside (14) and 4-hydroxy-3-methoxyphenol 1-O-D-apiofuranosyl-(1''→6')-O-β-D-glucopyranoside (15) were isolated from this plant for the first time. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Bioassays Against Pinewood Nematode: Assessment of a Suitable Dilution Agent and Screening for Bioactive Essential Oils
Molecules 2012, 17(10), 12312-12329; https://doi.org/10.3390/molecules171012312
Received: 21 September 2012 / Revised: 10 October 2012 / Accepted: 10 October 2012 / Published: 19 October 2012
Cited by 13 | PDF Full-text (231 KB) | HTML Full-text | XML Full-text
Abstract
Acetone was investigated and found to be an appropriate alternative to Triton X-100 as a solvent of essential oils in bioassays aimed to investigate their effects on pinewood nematode (Bursaphelenchus xylophilus) mortality. Therefore it was used as dilution agent to screen
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Acetone was investigated and found to be an appropriate alternative to Triton X-100 as a solvent of essential oils in bioassays aimed to investigate their effects on pinewood nematode (Bursaphelenchus xylophilus) mortality. Therefore it was used as dilution agent to screen the effectiveness of fifty two essential oils against this pest. Thirteen essential oils were highly effective, resulting in more than 90% pinewood nematode mortality at 2 mg/mL, with six of them resulting in 100% mortality. LC100 values ranged between 0.50 mg/mL and 0.83 mg/mL for the essential oils of Origanum vulgare and Satureja montana, respectively. Essential oils were submitted to gas chromatography and gas chromatography-mass spectrometry analysis and their chemical composition established. Data from essential oils with 100% mortality at 2 mg/mL and other essential oils previously found to have LC100 ≤ 2 mg/mL was combined, their chemical profiles investigated by correspondences analysis plus automatic classification. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle TLC Screening for Antioxidant Activity of Extracts from Fifteen Bamboo Species and Identification of Antioxidant Flavone Glycosides from Leaves of Bambusa. textilis McClure
Molecules 2012, 17(10), 12297-12311; https://doi.org/10.3390/molecules171012297
Received: 10 September 2012 / Revised: 19 September 2012 / Accepted: 12 October 2012 / Published: 19 October 2012
Cited by 24 | PDF Full-text (317 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Interest in the antioxidant activity of bamboo leaves is growing. To discover new sources of natural antioxidants, a TLC bioautography method combined with a new image processing method was developed to evaluate the antioxidant activity of leaf extracts from 15 different species of
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Interest in the antioxidant activity of bamboo leaves is growing. To discover new sources of natural antioxidants, a TLC bioautography method combined with a new image processing method was developed to evaluate the antioxidant activity of leaf extracts from 15 different species of bamboo. The results showed that the methanolic extract of Bambusa. textilis McClure possessed the highest antioxidant activity among the selected bamboo species. To rapidly identify the antioxidant compounds, the crude extract of B. textilis McClure was analysed by HPLC-UV, and HPLC-micro-fractionation of the extract was carried out. Based on TLC bioautography-guided fractionation, three antioxidant fractions were isolated from B. textilis McClure by preparative chromatography. These three antioxidant compounds were identified as isoorientin 4''-O β-D-xylopyranoside (1), isoorientin 2''-O-α-L-rhamnoside (2) and isoorientin (3) according to their UV, MS, and NMR data. The proposed TLC screening method could therefore be an easy way to evaluate the antioxidant activity of bamboo leaves, and the results achieved should prove very helpful for promoting their utilization, as B. textilis McClure can be considered a promising plant source of natural antioxidants. Full article
(This article belongs to the Special Issue Antioxidants 2012)
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Open AccessArticle Interaction Profile of Diphenyl Diselenide with Pharmacologically Significant Thiols
Molecules 2012, 17(10), 12287-12296; https://doi.org/10.3390/molecules171012287
Received: 24 August 2012 / Revised: 27 September 2012 / Accepted: 29 September 2012 / Published: 19 October 2012
Cited by 10 | PDF Full-text (269 KB) | HTML Full-text | XML Full-text
Abstract
Diphenyl diselenide has shown interesting biological activities in various free-radical-induced damage models and can be considered as a potential candidate drug against oxidative stress. Apart from its anti-oxidant activity, this compound can oxidize various thiols. However there are no detailed studies in the
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Diphenyl diselenide has shown interesting biological activities in various free-radical-induced damage models and can be considered as a potential candidate drug against oxidative stress. Apart from its anti-oxidant activity, this compound can oxidize various thiols. However there are no detailed studies in the literature about the thiol oxidase-like activity of this compound against biologically significant mono and di-thiols with respect to various pH conditions. Keeping in mind the scarcity of data in this area of organochalcogen chemistry, we report for the first time the kinetics of thiol oxidation by diphenyl diselenide, which was carried out in a commonly used phosphate buffer, not only at physiological pH, but also at a number of acidic values. The relative reactivities of the different thiols with diphenyl diselenide were independent of the pKa of the thiol group, such that at pH 7.4, cysteine and dithiothreitol were the most reactive, while 2,3-dimercapto-1-propanesulfonic acid and glutathione were weakly reactive and extremely low reactivity was observed with dimercaptosuccinic acid. Rate of oxidation was dependent on the pH of the incubation medium. The results obtained will help us in the design of rational strategies for the safe pharmacological use of diphenyl diselenide. Full article
(This article belongs to the Section Molecular Diversity)
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Open AccessReview Antimicrobial Peptides for Therapeutic Applications: A Review
Molecules 2012, 17(10), 12276-12286; https://doi.org/10.3390/molecules171012276
Received: 12 September 2012 / Revised: 8 October 2012 / Accepted: 17 October 2012 / Published: 18 October 2012
Cited by 148 | PDF Full-text (179 KB) | HTML Full-text | XML Full-text
Abstract
Antimicrobial peptides (AMPs) have been considered as potential therapeutic sources of future antibiotics because of their broad-spectrum activities and different mechanisms of action compared to conventional antibiotics. Although AMPs possess considerable benefits as new generation antibiotics, their clinical and commercial development still have
[...] Read more.
Antimicrobial peptides (AMPs) have been considered as potential therapeutic sources of future antibiotics because of their broad-spectrum activities and different mechanisms of action compared to conventional antibiotics. Although AMPs possess considerable benefits as new generation antibiotics, their clinical and commercial development still have some limitations, such as potential toxicity, susceptibility to proteases, and high cost of peptide production. In order to overcome those obstacles, extensive efforts have been carried out. For instance, unusual amino acids or peptido-mimetics are introduced to avoid the proteolytic degradation and the design of short peptides retaining antimicrobial activities is proposed as a solution for the cost issue. In this review, we focus on small peptides, especially those with less than twelve amino acids, and provide an overview of the relationships between their three-dimensional structures and antimicrobial activities. The efforts to develop highly active AMPs with shorter sequences are also described. Full article
(This article belongs to the Special Issue Advances in Medicinal Chemistry of Antibiotics)
Open AccessArticle Design, Synthesis and in Vivo Anti-inflammatory Activities of 2,4-Diaryl-5-4H-imidazolone Derivatives
Molecules 2012, 17(10), 12262-12275; https://doi.org/10.3390/molecules171012262
Received: 22 August 2012 / Revised: 12 September 2012 / Accepted: 11 October 2012 / Published: 18 October 2012
Cited by 19 | PDF Full-text (318 KB) | HTML Full-text | XML Full-text
Abstract
A series of 2,4-diaryl-5(4H)-imidazolones were prepared and evaluated for their anti-inflammatory activities. Some selected 2,4-diaryl-5(4H)-imidazolones exhibited excellent anti-inflammatory activity in the carrageenan-induced rat paw edema model. Structure Activity Relationships within the series were studied. The substitution at the N
[...] Read more.
A series of 2,4-diaryl-5(4H)-imidazolones were prepared and evaluated for their anti-inflammatory activities. Some selected 2,4-diaryl-5(4H)-imidazolones exhibited excellent anti-inflammatory activity in the carrageenan-induced rat paw edema model. Structure Activity Relationships within the series were studied. The substitution at the N-sulfonamide moiety by a small hydrophilic acetyl group resulted in compounds with superior in vivo anti-inflammatory properties. As expected from their COX-2 selectivity, most of the active compounds lacked gastrointestinal toxicity in vivo in rats after a 3-day treatment of 25 mg/kg/day. Full article
(This article belongs to the Section Medicinal Chemistry)
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