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具有抗炎作用的罕见双酰胺型苦参碱类生物碱。

Uncommon Bis-Amide Matrine-type Alkaloids From With Anti-inflammatory Effects.

作者信息

Luo Ding, Tu Zhenchao, Yin Wenjing, Fan Chunlin, Chen Nenghua, Wu Zhongnan, Ding Weilong, Li Yaolan, Wang Guocai, Zhang Yubo

机构信息

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

Department of Neurosurgery, The First Affiliated Hospital of Jinan University, Guangzhou, China.

出版信息

Front Chem. 2021 Sep 15;9:740421. doi: 10.3389/fchem.2021.740421. eCollection 2021.

Abstract

Four new alkaloids (1-4) belonging to rare examples of bis-amide matrine-type were isolated from the seeds of sophora alopecuroides. Their structures including absolute configuration were determined by extensive spectroscopic analysis, electronic circular dichroism (ECD) interpretation, and X-ray diffraction crystallography. Chemically, bis-amide matrine-type alkaloids can provide new molecular template for structural modification. Compounds 3-4 displayed obvious anti-inflammatory effects based on the inhibition of two key pro-inflammatory cytokines [tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6)] in a dose-dependent manner, with IC50 values from 35.6 to 45.8 μm.

摘要

从苦豆子种子中分离出四种新的生物碱(1-4),它们属于罕见的双酰胺苦参碱型。通过广泛的光谱分析、电子圆二色性(ECD)解释和X射线衍射晶体学确定了它们的结构,包括绝对构型。从化学角度来看,双酰胺苦参碱型生物碱可为结构修饰提供新的分子模板。化合物3-4基于对两种关键促炎细胞因子[肿瘤坏死因子-α(TNF-α)和白细胞介素-6(IL-6)]的抑制作用,呈剂量依赖性地显示出明显的抗炎效果,IC50值为35.6至45.8μm。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51fd/8479178/0026bad3d86c/fchem-09-740421-g001.jpg

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