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来自苦豆子的喹诺里西啶生物碱及其抗炎活性。

Quinolizidine alkaloids from Sophora tonkinensis and their anti-inflammatory activities.

机构信息

Institute of Traditional Chinese Medicine & Natural Products, Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, China; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China.

School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China.

出版信息

Fitoterapia. 2019 Nov;139:104391. doi: 10.1016/j.fitote.2019.104391. Epub 2019 Nov 1.

Abstract

Two new quinolizidine-based alkaloids (2 and 12), along with ten known ones (1, 3-11) were isolated from the roots of S. tonkinensis. Their structures were determined by spectroscopic data (including NMR, MS, IR, and UV), X-ray single crystal diffraction, electronic circular dichroism analyses (ECD), and comparing with related literatures. Compounds 1, 3-12 at non-toxic concentrations exhibited potent anti-inflammatory activities according to in vitro and in vivo anti-inflammatory tests. Among them, (-)-anagyrine (4), sophocarpine (8), 14β-hydroxymatrine (10), and 7β-sophoramine (12) showed more potent in vitro anti-inflammatory activities, and 5α,14β-dihydroxymatrine (2), (-)-anagyrine (4), sophocarpine (8), and 5α-hydroxymatrine (9) exhibited better in vivo anti-inflammatory effects.

摘要

从越南苦参的根部分离得到两个新的喹诺里西啶类生物碱(2 和 12),以及十个已知的生物碱(1、3-11)。它们的结构通过光谱数据(包括 NMR、MS、IR 和 UV)、X 射线单晶衍射、电子圆二色性分析(ECD)和与相关文献的比较来确定。根据体外和体内抗炎试验,化合物 1、3-12 在非毒性浓度下表现出很强的抗炎活性。其中,(-)-阿那格雷(4)、苦参碱(8)、14β-苦参碱(10)和 7β-槐胺碱(12)表现出更强的体外抗炎活性,而 5α,14β-二羟基苦参碱(2)、(-)-阿那格雷(4)、苦参碱(8)和 5α-苦参碱(9)则表现出更好的体内抗炎效果。

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