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瑞香狼毒茎中的生物活性二萜。

Bioactive Diterpenoids from the Stems of Euphorbia royleana.

机构信息

State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research , Nankai University , Tianjin 300350 , People's Republic of China.

College of Chemistry and Environmental Sciences, Laboratory of Xinjiang Native Medicinal and Edible Plant Resources Chemistry , Kashgar University , Kashgar 844000 , People's Republic of China.

出版信息

J Nat Prod. 2019 Feb 22;82(2):183-193. doi: 10.1021/acs.jnatprod.8b00493. Epub 2019 Feb 7.

Abstract

Two ingenane- (1 and 2), two ent-atisane- (3 and 4), two ent-kaurane- (5 and 6), two ent-abietane- (7 and 8), and one ent-isopimarane-type (9) diterpenoid and 12 known analogues have been isolated from the methanolic extract of the stems of Euphorbia royleana. Their structures, including absolute configurations, were determined by extensive spectroscopic methods and ECD data analysis. The nitric oxide inhibitory activities of those diterpenoids were examined biologically in lipopolysaccharide-stimulated BV-2 cells, with compounds 1, 2, 5-7, 10, and 12 having IC values lower than 40 μM. Molecular docking was used to investigated the possible mechanism of compounds 1, 2, 5-7, 10, and 12.

摘要

从大戟属植物罗勒茎的甲醇提取物中分离得到了两个 ingenane- (1 和 2)、两个 ent-atisane- (3 和 4)、两个 ent-kaurane- (5 和 6)、两个 ent-abietane- (7 和 8) 和一个 ent-isopimarane-type (9) 二萜类化合物和 12 个已知类似物。通过广泛的光谱方法和 ECD 数据分析确定了它们的结构,包括绝对构型。这些二萜类化合物的一氧化氮抑制活性在脂多糖刺激的 BV-2 细胞中进行了生物检测,化合物 1、2、5-7、10 和 12 的 IC 值低于 40 μM。分子对接用于研究化合物 1、2、5-7、10 和 12 的可能作用机制。

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