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新型 Esculentoside A 及其苷元原薯蓣皂甙元衍生物的合成及溶血活性和脂多糖诱导的一氧化氮产生抑制作用的评价。

Synthesis of novel derivatives of esculentoside A and its aglycone phytolaccagenin, and evaluation of their haemolytic activity and inhibition of lipopolysaccharide-induced nitric oxide production.

机构信息

School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China.

出版信息

Chem Biodivers. 2011 Oct;8(10):1833-52. doi: 10.1002/cbdv.201000339.

Abstract

A series of 46 compounds derived from esculentoside A and its aglycone were synthesized and characterized. The effect of these compounds on lipopolysaccharide (LPS)-induced NO production, haemolytic activity, and cell viability was evaluated. Structure-activity relationship was established by comparing the derivatives of esculentoside A with its aglycone derivatives. Both the aglycone and its derivatives showed higher inhibitory effects on LPS-induced NO production, and lower haemolytic activities than esculentoside A and its derivatives.

摘要

合成并表征了一系列来源于毛蕊花糖苷 A 及其苷元的 46 种化合物。评价了这些化合物对脂多糖(LPS)诱导的 NO 生成、溶血活性和细胞活力的影响。通过比较毛蕊花糖苷 A 及其苷元衍生物的衍生物,建立了构效关系。苷元和其衍生物对 LPS 诱导的 NO 生成的抑制作用均高于毛蕊花糖苷 A 及其衍生物,溶血活性则较低。

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