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莎草科物种是天然哺乳动物精氨酸酶抑制剂的潜在来源,对血管功能有积极影响。

Cyperaceae Species Are Potential Sources of Natural Mammalian Arginase Inhibitors with Positive Effects on Vascular Function.

机构信息

PEPITE EA4267, University of Bourgogne Franche-Comté , 25000 Besançon, France.

MIB-UR Œnologie, EA 4577, USC 1366 INRA, University of Bordeaux, ISVV , 33882 Villenave-d'Ornon, France.

出版信息

J Nat Prod. 2017 Sep 22;80(9):2432-2438. doi: 10.1021/acs.jnatprod.7b00197. Epub 2017 Aug 24.

Abstract

The inhibition of arginase is of substantial interest for the treatment of various diseases of public health interest including cardiovascular diseases. Using an ex vivo experiment on rat aortic rings and an in vitro assay with liver bovine purified arginase, it was demonstrated that several polyphenolic extracts from Cyperus and Carex species possess vasorelaxant properties and mammalian arginase inhibitory capacities. Phytochemical studies performed on these species led to the identification of eight compounds, including monomers, dimers, trimers, and tetramers of resveratrol. The potential of these stilbenes as inhibitors of mammalian arginase was assessed. Five compounds, scirpusin B (5), ε-viniferin (4), cyperusphenol B (6), carexinol A (7), and the new compound virgatanol (1), showed significant inhibition of arginase, with percentage inhibition ranging from 70% to 95% at 100 μg/mL and IC values between 12.2 and 182.1 μM, confirming that these stilbenes may be useful for the development of new pharmaceutical products.

摘要

精氨酸酶的抑制作用对于治疗各种具有公共卫生意义的疾病具有重要意义,包括心血管疾病。通过对大鼠主动脉环的离体实验和牛肝纯化精氨酸酶的体外测定,证明了来自香蒲属和薹草属的几种多酚提取物具有血管舒张特性和哺乳动物精氨酸酶抑制能力。对这些物种进行的植物化学研究鉴定出了 8 种化合物,包括白藜芦醇的单体、二聚体、三聚体和四聚体。评估了这些芪类化合物作为哺乳动物精氨酸酶抑制剂的潜力。五种化合物,即蒲黄素 B(5)、ε-viniferin(4)、香蒲酚 B(6)、薹草醇 A(7)和新化合物 virgatanol(1),对精氨酸酶表现出显著的抑制作用,在 100μg/mL 时抑制率在 70%至 95%之间,IC 值在 12.2 和 182.1μM 之间,证实这些芪类化合物可能有助于开发新的药物产品。

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