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首页> 外文期刊>Journal of Pharmaceutical and Biomedical Analysis: An International Journal on All Drug-Related Topics in Pharmaceutical, Biomedical and Clinical Analysis >Screening and profiling stilbene-type natural products with angiotensin-converting enzyme inhibitory activity from Ampelopsis brevipedunculata var. hancei (Planch.) Rehder
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Screening and profiling stilbene-type natural products with angiotensin-converting enzyme inhibitory activity from Ampelopsis brevipedunculata var. hancei (Planch.) Rehder

机译:从Ampelopsis brevipedunculata var中筛选和分析具有血管紧张素转化酶抑制活性的二苯乙烯型天然产物。汉西(Planch。)Rehder

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In this study, we screened 10 resveratrol derivatives isolated from Ampelopsis brevipedunculata var. hancei (Planch.) Rehder (ABH) for angiotensin I converting enzyme (ACE) inhibitory (ACEI) activity. Among these compounds, (+)-hopeaphenol and (+)-vitisin A showed the lowest IC50 values (similar to 1.5 mu M) toward ACE. In addition, the compounds' abundances and distributions in ABH were profiled using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Interestingly, trimers and tetramers of resveratrol were mainly obtained from the bark of ABH when 90% ethanol was used for extraction. This result implies that the antihypertension effect of ABH extract may be mainly contributed by (+)-hopeaphenol (F1) and (+)-vitisin A (F2) in the ABH bark due to their remarkable ACE inhibitions. Moreover, the sizes and structures of these compounds were further correlated to their affinities toward ACE using molecular docking calculations. The results showed that resveratrol tetramers interact with ACE more favorably than other smaller oligomers. (C) 2015 Elsevier B.V. All rights reserved.
机译:在这项研究中,我们筛选了10种从白术Ampelopsis brevipedunculata var中分离的白藜芦醇衍生物。 hancei(Planch。)Rehder(ABH)具有血管紧张素I转换酶(ACE)抑制(ACEI)活性。在这些化合物中,(+)-胡豆酚和(+)-葡萄红素A对ACE的IC50值最低(约1.5μM)。此外,使用液相色谱-串联质谱法(LC-MS / MS)对化合物在ABH中的丰度和分布进行了分析。有趣的是,当使用90%乙醇萃取时,白藜芦醇的三聚体和四聚体主要来自ABH的树皮。该结果表明,ABH提取物的抗高血压作用可能主要是由ABH树皮中的(+)-hopeaphenol(F1)和(+)-vitisin A(F2)引起的,因为它们具有显着的ACE抑制作用。此外,使用分子对接计算,将这些化合物的大小和结构与它们对ACE的亲和力进一步关联。结果表明,白藜芦醇四聚体比其他较小的低聚体与ACE的相互作用更有利。 (C)2015 Elsevier B.V.保留所有权利。

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