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从雷公藤的茎和枝中分离得到的多样二氢沉香呋喃倍半萜衍生物。

Diverse dihydroagarofuran sesquiterpene derivatives from the stem and branch of Tripterygium wilfordii.

机构信息

Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, China.

Department of Pharmacology, School of Medicine, Guangdong Clinical Translation Center for Targeted Drug, Jinan University, Guangzhou, China.

出版信息

Fitoterapia. 2022 Jul;160:105205. doi: 10.1016/j.fitote.2022.105205. Epub 2022 May 7.

Abstract

Ten new dihydroagarofuran sesquiterpene polyol esters, tripterdines A-J (1-10) were isolated from the stem and branch of Tripterygium wilfordii. The structures of new compounds were elucidated on the basis of extensive spectroscopic analyses, including UV, IR, HRESIMS, NMR, and CD exciton chirality method. The structures of compounds 1, 3, and 6 were confirmed by X-ray crystallographic analyses. The anti-inflammatory and cytotoxic activities were assessed for all the compounds (1-10). Compounds 3, 5 and 10 exhibited potent anti-inflammatory activities with the secretion level of TNF-α ranging from 43.86% to 51.27%, and the IL-6 ranging from 32.44% to 50.64%. In addition, compounds 1, 3, 7 and 9 showed weak cytotoxicities against three human tumor cell lines (Huh7, MCF-7 and HCT-116).

摘要

从雷公藤的茎和枝部分离得到了 10 个新的二氢沉香呋喃倍半萜多元醇酯,即雷公藤啶 A-J(1-10)。基于广泛的光谱分析,包括 UV、IR、HRESIMS、NMR 和 CD 外消旋手性方法,确定了新化合物的结构。通过 X 射线晶体学分析确定了化合物 1、3 和 6 的结构。评估了所有化合物(1-10)的抗炎和细胞毒性活性。化合物 3、5 和 10 表现出较强的抗炎活性,TNF-α 的分泌水平范围为 43.86%-51.27%,IL-6 的分泌水平范围为 32.44%-50.64%。此外,化合物 1、3、7 和 9 对三种人肿瘤细胞系(Huh7、MCF-7 和 HCT-116)表现出较弱的细胞毒性。

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