摘要 :
In 1863, Diphenylamine (DPA) was prepared by Hoffmann by the destructive distillation ofdifferent triphenylmethane dyes. DPA are naturally occurring compounds, present in onions, leaves ofblack and green tea and peel of citrus fru...
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In 1863, Diphenylamine (DPA) was prepared by Hoffmann by the destructive distillation ofdifferent triphenylmethane dyes. DPA are naturally occurring compounds, present in onions, leaves ofblack and green tea and peel of citrus fruits. DPA derivatives belong to the category of Non SteroidalAnti-inflammatory Drugs (NSAIDs). Diclofenac, chemically called 2-(2,6-dichloranilino) phenylaceticacid, is a well-known NSAID. Other important compounds are tolfenamic acid, flufenamic acid andmefenamic acid, etc. DPA derivatives are claimed for several important biological activities whichinclude anti-microbial, analgesic, anti-inflammatory, anti-convulsant and anti-cancer activities. Manymore compounds have been discovered and many are still being focused.The key goal of this article is to show up the different derivatives and the pharmacological activities ofDPA. Hence, it can be concluded that DPA and its derivatives possess significant therapeutic functionsand many potent derivatives are still to be discovered.
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摘要 :
In 1863, Diphenylamine (DPA) was prepared by Hoffmann by the destructive distillation ofdifferent triphenylmethane dyes. DPA are naturally occurring compounds, present in onions, leaves ofblack and green tea and peel of citrus fru...
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In 1863, Diphenylamine (DPA) was prepared by Hoffmann by the destructive distillation ofdifferent triphenylmethane dyes. DPA are naturally occurring compounds, present in onions, leaves ofblack and green tea and peel of citrus fruits. DPA derivatives belong to the category of Non SteroidalAnti-inflammatory Drugs (NSAIDs). Diclofenac, chemically called 2-(2,6-dichloranilino) phenylaceticacid, is a well-known NSAID. Other important compounds are tolfenamic acid, flufenamic acid andmefenamic acid, etc. DPA derivatives are claimed for several important biological activities whichinclude anti-microbial, analgesic, anti-inflammatory, anti-convulsant and anti-cancer activities. Manymore compounds have been discovered and many are still being focused.The key goal of this article is to show up the different derivatives and the pharmacological activities ofDPA. Hence, it can be concluded that DPA and its derivatives possess significant therapeutic functionsand many potent derivatives are still to be discovered.
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Six new N [(4-aminophenyl) sulfonyl] acetamide based hydroxytriazenes have been synthesized and characterized using elemental analysis, IR, 1H NMR, 13C NMR and MASS spectral analysis. Further, their theoretical predictions for pro...
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Six new N [(4-aminophenyl) sulfonyl] acetamide based hydroxytriazenes have been synthesized and characterized using elemental analysis, IR, 1H NMR, 13C NMR and MASS spectral analysis. Further, their theoretical predictions for probable activities have been taken using PASS (Prediction of Activity Spectra for Substance). Although a number of activities have been predicted but specifically anti-inflammatory, anti-radical, anti-diabetic activities have been experimentally validated which proves that theoretical predictions agree with the experimental results. The object of the Letter is to establish Computer Aided Drug Design (CADD) using our compounds. (C) 2016 Elsevier Ltd. All rights reserved.
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Reaction of ortho phenylenediamine 1 with various organic acids yielded 2-substituted benzimidazole derivatives 2 which Were further treated with nitric acid and sulphuric acid to afford 5-nitro-2-substituted benzimdazoles 3.Coupl...
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Reaction of ortho phenylenediamine 1 with various organic acids yielded 2-substituted benzimidazole derivatives 2 which Were further treated with nitric acid and sulphuric acid to afford 5-nitro-2-substituted benzimdazoles 3.Coupling of this compound with halogenated beta picoline 5 yielded the title compounds.The structures of synthesized compounds were elucidated mainly by spectral evidence.All the compounds were screened for their anti-inflammatory and anti-convulsant potential.The compounds exhibited moderate to significant activities.
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A series of novel compounds were synthesized in reactions of N3-substituted amidrazones with cis-1,2-cyclohexanedicarboxylic anhydride: linear, isoindole, and triazole derivatives. All new structures were confirmed by H1 NMR and I...
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A series of novel compounds were synthesized in reactions of N3-substituted amidrazones with cis-1,2-cyclohexanedicarboxylic anhydride: linear, isoindole, and triazole derivatives. All new structures were confirmed by H1 NMR and IR spectrometry as well as elemental analysis. Potential biological effects of new compounds were predicted with the Prediction of Activity Spectra for Substances (PASS) program. Antiviral, antibacterial, analgesic, and anti-inflammatory activities were experimentally verified.
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摘要 :
A series of novel compounds were synthesized in reactions of N 3-substituted amidrazones with cis-1,2-cyclohexanedicarboxylic anhydride: linear, isoindole, and triazole derivatives. All new structures were confirmed by H 1 NMR and...
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A series of novel compounds were synthesized in reactions of N 3-substituted amidrazones with cis-1,2-cyclohexanedicarboxylic anhydride: linear, isoindole, and triazole derivatives. All new structures were confirmed by H 1 NMR and IR spectrometry as well as elemental analysis. Potential biological effects of new compounds were predicted with the Prediction of Activity Spectra for Substances (PASS) program. Antiviral, antibacterial, analgesic, and anti-inflammatory activities were experimentally verified.
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In this study, the anti-oxidative, anti-inflammatory, anti-melanogenic activities of Endlicheha anomala (Nees) Mez methanol extract (EAME) were evaluated by use of in vitro assays and cell culture model systems. The results reveal...
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In this study, the anti-oxidative, anti-inflammatory, anti-melanogenic activities of Endlicheha anomala (Nees) Mez methanol extract (EAME) were evaluated by use of in vitro assays and cell culture model systems. The results revealed that EAME scavenges various radicals such as 1,1 -diphenyl-2-picryl hydrazyl hydrogen peroxide induced reactive oxygen species, and lipopolysaccharide induced nitric oxide. Furthermore, EAME induced the expression of anti-oxidative enzymes such as heme oxygenase 1, thioredoxin reductase 1, NAD(P)H dehydrogenase 1, and their upstream transcription factor, nuclear factors-related factor 2. Moreover, EAME inhibited in vitro DQPA oxidation and 3-isobutyl-1-methylxanthine induced melanogenesis in B16F10 cells. Its anti-melanogenic activity will have originated from the inhibition of tyrosinase enzyme activity and melanogenesis related protein expression. Taken together, these results provide the important new insight that E. anomala possesses various biological activities such as anti-oxidative, anti-inflammatory, and anti-melanogenic. Therefore, it might be utilized as a promising material in the fields of nutraceuticals and cosmetics.
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This study was designed to explore new nutraceutical and cosmetic resources possessing biological activities from the plant kingdom. To fulfill this purpose, we analyzed the anti-oxidative, anti-mel-anogenic, and anti-inflammatory...
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This study was designed to explore new nutraceutical and cosmetic resources possessing biological activities from the plant kingdom. To fulfill this purpose, we analyzed the anti-oxidative, anti-mel-anogenic, and anti-inflammatory activities of Zanthoxylum schinifolium extract (ZSE) and its solvent fractions using in vitro assays and cell culture model systems. Three kinds of ZSE treated with methanol, ethanol, and water exhibited potent anti-oxidative activities through DPPH radical scavenging capacity, and inhibited in vitro DOPA oxidation. Furthermore, Z schinifolium methanol extract (ZSME) inhibited the a-melanocyte stimulating hormone, which induces melanin contents in B16F10 cells. Its anti-melanogenic activity originates from the inhibition of tyrosinase enzyme activity and melanogenesis related protein expression. Moreover, lipopolysaccharide induced nitric oxide production in the RAW 264.7 cell line was also ameliorated by ZSME treatment in a dose dependent manner. Among the four solvent fractions of ZSME treated with dichloromethane, ethyl acetate, n-butanol, and water, three fractions, except water, showed significant anti-melanogenic and anti-inflammatory activities. Taken together, these results provide important new insights into Z schinifolium, indicating that it possesses numerous biological activities such as anti-oxidative, anti-melanogenic, and anti-inflammatory activities. Therefore, it may well serve as a promising material in the field of nutraceuticals and cosmetics.
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In this study, biological activities of methanolic extracts from Artemisia herba-alba, Ruta chalpensis L. and Peganum harmala L. plants, collected in Centre of Tunisia, were investigated. Results showed an important phenolic compo...
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In this study, biological activities of methanolic extracts from Artemisia herba-alba, Ruta chalpensis L. and Peganum harmala L. plants, collected in Centre of Tunisia, were investigated. Results showed an important phenolic composition of Artemisia herba-alba (123.95. ±. 4.3. g GAE/kg of dry mass). The extract of this plant showed, using different antioxidant assays (DPPH, ABTS and AAPH/linoleic acid methods) and an IFN-γ/LPS induced RAW 264.7 murine macrophages' assay, the highest antioxidant (IC50 (DPPH assay) 20.64. ±. 0.84. mg/L) and anti-inflammatory (72% inhibition at 150. mg/L) activities, respectively. Excepting Peganum harmala L. extract, the two other extracts showed a high anticancer activity against several cell lines (human bladder carcinoma RT112, human laryngeal carcinoma Hep2 and human myelogenous leukemia K562), for A. herba-laba IC50 = 81.59. ±. 4.4, 59.05. ±. 3.66 and 90.96. mg/L respectively, but not on normal peripheral blood mononuclear cells. All these biological activities are well correlated with the phenolic contents of these extracts. These findings demonstrate the remarkable potential of these plants as valuable source of antioxidants with exhibit original and interesting anti-inflammatory and anticancer capacities.
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Ethnopharmacological relevance: Periploca sepium Bunge (P. sepium) is used in traditional Chinese medicine (TCM) for the treatment of autoimmune diseases, particularly rheumatoid arthritis. Periploca sepium periplosides (PePs), is...
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Ethnopharmacological relevance: Periploca sepium Bunge (P. sepium) is used in traditional Chinese medicine (TCM) for the treatment of autoimmune diseases, particularly rheumatoid arthritis. Periploca sepium periplosides (PePs), isolated from the root bark of P. sepium, characterized as the cardiac glycosides-free pregnane glycosides fraction, is expected to possess therapeutic potential on inflammatory arthritis.
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