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黄花远志亚种黄花远志的成分及其作为人乳酸脱氢酶抑制剂的活性

Constituents of Polygala flavescens ssp. flavescens and Their Activity as Inhibitors of Human Lactate Dehydrogenase.

作者信息

De Leo Marinella, Peruzzi Lorenzo, Granchi Carlotta, Tuccinardi Tiziano, Minutolo Filippo, De Tommasi Nunziatina, Braca Alessandra

机构信息

Dipartimento di Farmacia, Università di Pisa , Via Bonanno 6 and 33, 56126 Pisa, Italy.

Centro Interdipartimentale di Ricerca "Nutraceutica e Alimentazione per la Salute", Università di Pisa , Via del Borghetto 80, 56124 Pisa, Italy.

出版信息

J Nat Prod. 2017 Jul 28;80(7):2077-2087. doi: 10.1021/acs.jnatprod.7b00295. Epub 2017 Jul 10.

Abstract

Four new flavonol glycosides (1-4), two oligosaccharides (5, 6), one α-ionone (7), and three triterpenoid saponins (8-10), together with four known secondary metabolites (11-14), were isolated from the aerial parts of Polygala flavescens ssp. flavescens. All structures were elucidated on the basis of their spectroscopic and spectrometric data. The isolates were assayed for their inhibitory activity against isoform 5 of human lactate dehydrogenase, and compound 11 (3,6'-di-O-sinapoylsucrose) showed an IC value of 90.4 μM. Modeling studies were carried out to suggest the putative interaction mode of compound 11 in the enzyme active site.

摘要

从黄花远志亚种黄花远志的地上部分分离得到了4个新的黄酮醇苷(1 - 4)、2个寡糖(5, 6)、1个α-紫罗兰酮(7)和3个三萜皂苷(8 - 10),以及4个已知的次生代谢产物(11 - 14)。所有结构均根据其光谱和波谱数据确定。对分离得到的化合物进行了对人乳酸脱氢酶同工酶5的抑制活性测定,化合物11(3,6'-二-O-芥子酰基蔗糖)的IC值为90.4 μM。进行了模型研究以推测化合物11在酶活性位点的假定相互作用模式。

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