Akihisa Toshihiro, Franzblau Scott G, Ukiya Motohiko, Okuda Hiroki, Zhang Fangqiu, Yasukawa Ken, Suzuki Takashi, Kimura Yumiko
College of Science and Technology, Nihon University, Tokyo, Japan.
Biol Pharm Bull. 2005 Jan;28(1):158-60. doi: 10.1248/bpb.28.158.
Twenty-eight 3-hydroxy triterpenoids of taraxastane- (1-7), oleanane- (8-12), ursane- (13-15), lupane- (16,18,19), taraxane- (20), cycloartane- (21-25), tirucallane- (26-28), and dammarane-types (29) isolated from the non-saponifiable lipid fraction of the flower extract of chrysanthemum (Chrysanthemum morifolium) and one lupane-type 3alpha-hydroxy triterpenoid (17) derived from 16 were tested for their antitubercular activity against Mycobacterium tuberculosis strain H37Rv using the Microplate Alamar Blue Assay (MABA). Fifteen compounds showed a minimum inhibitory concentration (MIC) in the range of 4-64 microg/ml, among which maniladiol (9; MIC 4 microg/ml), 3-epilupeol (17; 4 microg/ml), and 4,5alpha-epoxyhelianol (27; 6 microg/ml) exhibited the highest activity. Cytotoxicity of compound 17 against Vero cells gave an IC50 value of over 62.5 microg/ml, suggesting some degree of selectivity for M. tuberculosis.
从菊花（Chrysanthemum morifolium）花提取物的不皂化脂质部分分离出28种蒲公英烷型（1 - 7）、齐墩果烷型（8 - 12）、乌苏烷型（13 - 15）、羽扇豆烷型（16、18、19）、蒲公英赛烷型（20）、环阿尔廷烷型（21 - 25）、四环三萜型（26 - 28）和达玛烷型（29）的3 - 羟基三萜类化合物，以及1种由16衍生而来的羽扇豆烷型3α - 羟基三萜类化合物（17），采用微孔板阿拉玛蓝法（MABA）检测它们对结核分枝杆菌H37Rv菌株的抗结核活性。15种化合物的最低抑菌浓度（MIC）在4 - 64微克/毫升范围内，其中马尼拉二醇（9；MIC 4微克/毫升）、3 - 表羽扇豆醇（17；4微克/毫升）和4,5α - 环氧半日花醇（27；6微克/毫升）表现出最高活性。化合物17对Vero细胞的细胞毒性给出的IC50值超过62.5微克/毫升，表明对结核分枝杆菌有一定程度的选择性。
