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对黄荆叶成分的植物化学和生物活性研究。

Phytochemical and Bioactivity Studies on Constituents of the Leaves of Vitex Quinata.

作者信息

Deng Ye, Chin Young-Won, Chai Hee-Byung, de Blanco Esperanza Carcache, Kardono Leonardus B S, Riswan Soedarsano, Soejarto Djaja D, Farnsworth Norman R, Kinghorn A Douglas

机构信息

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.

出版信息

Phytochem Lett. 2011 Sep 1;4(3):213-217. doi: 10.1016/j.phytol.2011.03.007.

DOI:10.1016/j.phytol.2011.03.007
PMID:21966342
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3182149/
Abstract

A phytochemical investigation of the leaves of Vitex quinata (Lour.) F.N. Williams (Verbenaceae), guided by the MCF-7 human breast cancer cell line, led to the isolation of a new δ-truxinate derivative (1) and a new phytonoic acid derivative (2), together with 12 known compounds. The structures of the new compounds were determined by spectroscopic methods as dimethyl 3,4,3',4'-tetrahydroxy-δ-truxinate (1) and methyl 10R-methoxy-12-oxo-9(13),16E-phytodienoate (2), respectively. In a cytotoxicity assay, (S)-5-hydroxy-7,4'-dimethoxyflavanone (3) was found to be the sole active principle, with ED(50) values of 1.1-6.7 μM, respectively, when tested against a panel of three human cancer cells. Methyl 3,4,5-O-tricaffeoyl quinate (4) showed activity in an enzyme-based ELISA NF-κB p65 assay, with an ED(50) value of 10.3 μM.

摘要

以MCF - 7人乳腺癌细胞系为导向,对黄荆(马鞭草科)叶片进行植物化学研究,从中分离出一种新的δ - 吐昔酸衍生物(1)和一种新的植酮酸衍生物(2),以及12种已知化合物。通过光谱方法确定新化合物的结构分别为3,4,3',4'-四羟基 - δ - 吐昔酸二甲酯(1)和10R - 甲氧基 - 12 - 氧代 - 9(13),16E - 植二烯酸甲酯(2)。在细胞毒性试验中,当针对一组三种人类癌细胞进行测试时,(S)-5 - 羟基 - 7,4'-二甲氧基黄酮(3)被发现是唯一的活性成分,其ED(50)值分别为1.1 - 6.7 μM。3,4,5 - O - 三咖啡酰奎宁酸甲酯(4)在基于酶的ELISA NF - κB p65测定中显示出活性,ED(50)值为10.3 μM。