血籽乌桕成分对结核分枝杆菌生长的抑制作用

Mycobacterium tuberculosis growth inhibition by constituents of Sapium haematospermum.

作者信息

Woldemichael Girma M, Gutierrez-Lugo Maria-Teresa, Franzblau Scott G, Wang Yuehong, Suarez Enrique, Timmermann Barbara N

机构信息

Department of Pharmacology and Toxicology, Division of Medicinal and Natural Products Chemistry, College of Pharmacy, University of Arizona, 1703 E. Mabel Street, Tucson, Arizona 85721-0207, USA.

出版信息

J Nat Prod. 2004 Apr;67(4):598-603. doi: 10.1021/np0303411.

DOI:10.1021/np0303411

PMID:15104489

Abstract

Four novel compounds consisting of two new pimaranes, lecheronol A (1) and lecheronol B (2), an acylated cycloartane, 3-O-beta-lauroyl-cycloart-(23E)-en-25-ol (10), and a highly oxygenated novel chalconoid, alpha,beta,3,4,5,2',4',6'-octahydroxydihydrochalcone (12), were isolated along with seven known triterpene derivatives and three flavonol glucosides from Mycobacterium tuberculosis growth-inhibiting fractions of the CH(2)Cl(2)/MeOH (1:1) extract of the aerial parts of Sapium haematospermum. Compounds 1, 3 (3 alpha-hydroxyolean-12-ene), 8 [3 alpha-hydroxylup-20(29)-en], and 9 (cycloartanol) were found most active, with MIC values of 4, 12.2, 13.4, and 8 microg/mL, respectively. Cytotoxicity tests in Vero cells for compounds 1, 3, 8, and 9 gave IC(50) values of 104.8, 127.2, 127.2, and 102.4 microg/mL, respectively.

摘要

从血桐地上部分的二氯甲烷/甲醇（1:1）提取物的结核分枝杆菌生长抑制级分中，分离出四种新化合物，包括两种新的海松烷类化合物，勒氏醇A（1）和勒氏醇B（2），一种酰化环阿尔廷烷，3 - O - β - 月桂酰基 - 环阿尔廷 - （23E） - 烯 - 25 - 醇（10），以及一种高度氧化的新型查耳酮类化合物，α，β，3，4，5，2'，4'，6' - 八羟基二氢查耳酮（12），同时还分离出七种已知的三萜衍生物和三种黄酮醇糖苷。化合物1、3（3α - 羟基齐墩果 - 12 - 烯）、8 [3α - 羟基羽扇 - 20（29） - 烯]和9（环阿尔廷醇）被发现活性最强，其最小抑菌浓度（MIC）值分别为4、12.2、13.4和8微克/毫升。对化合物1、3、8和9在非洲绿猴肾细胞中的细胞毒性测试得到的半数抑制浓度（IC50）值分别为104.8、127.2、127.2和102.