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QSAR,docking studies and pharmacophore identification of phenylmethyl phenoxy propyl amino propanoic acid derivatives as leukotriene A_4 hydrolase inhibitors

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药学学报 2010年第5期45卷 615-623页

作者： SONAWANE Lalit V BARI Sanjaykumar B Drug Design and Development R. C. Patel Institute of Pharmaceutical Education and Research Karwand Naka Shirpur Dist. - Dhule Maharashtra State 425405 India

The enzyme leukotriene A4 (lta4) plays an important role as precursor of slow reactive substances as LTC4, LTD4, and LTE4. It is an attractive target for molecular modeling and QSAR study. Our effort is mainly focused on exploring the SAR for inhibitors of the lta4 hydrolase through docking study, pharmacophore modeling and molecular descriptor study. The binding of these small molecules on lta4 hydrolase enzyme was described by the models developed on 2D molecular descriptors, with good predictive power (39 compounds, 6 descriptors, r2 0.98, SEE 0.167, F-value 268.53, q2 0.90, r2adj 0.97, P-value lta4 hydrolase through techniques of QSAR, docking and pharmacophore.

关键词： lta4 hydrolase QSAR molecular descriptor docking pharmacophore

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Protective effects of Dioscin on TNF-α-induced collagen-induced arthritis rat fibroblast-like synoviocytes involves in regulating the LTB4/BLT pathway

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BIOCELL 2021年第4期45卷 1005-1012页

作者： ZHIPING WEI YAJUN LIU MEIWEN YANG MENGDI LI KEXIN LI LUXI ZHENG HUIQIONG GUO FENFANG HONG SHULONG YANG Department of Physiology College of MedicineNanchang UniversityNanchang330006China Henan Vocational College of Nursing Anyan455000China Nanchang University Hospital Nanchang330031China Department of Experimental Teaching Center Nanchang UniversityNanchang330031China

Background and Objective:LTB4 has been shown to be involved in rheumatoid arthritis(RA)*** effect of Dioscin(Dio)on the LTB4 pathway of RA have not been reported *** study aimed at further exploring whether Dioscin’s effects on TNF-αinduced collagen-induced arthritis(CIA)rat fibroblast-like synoviocytes(FLS)connected with the LTB4 and its receptor ***&Methods:In this experiment,control group,TNF-αgroup,and different concentrations of Dioscin groups were *** viability was evaluated using MTT *** levels of LTB4 in the samples of above groups were measured using *** mRNA expression levels of lta4H,BLT1,and BLT2 were detected by quantitative real time PCR,while the expression level of lta4H proteins were detected using western *** distribution of lta4H was assessed by immunofluorescence ***:the LTB4 level of TNF-αgroup in sample supernatant was higher than both control group and Dioscin groups with decreased LTB4 levels(plta4H was significantly increased in TNF-αgroup(plta4H expressions were significantly decreased in all Dioscin groups when compared to TNF-αgroup(p4 production by down-regulating lta4H expression,and may inhibit its downstream pathway by decreasing LTB4 receptors *** findings suggest that dioscin produces a potential therapeutic effects for RA via its influencing lta4H/LTB4/BLT pathway.

关键词： Rheumatoid arthritis Dioscin Fibroblast-like synoviocytes Leukotriene B4 lta4 hydrolase Leukotriene B4 receptor

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