Antitubercular activity of triterpenoids from Asteraceae flowers

被引:58
作者
Akihisa, T
Franzblau, SG
Ukiya, M
Okuda, H
Zhang, FQ
Yasukawa, K
Suzuki, T
Kimura, Y
机构
[1] Nihon Univ, Coll Sci & Technol, Chiyoda Ku, Tokyo 1018308, Japan
[2] Univ Illinois, Coll Pharm, Inst TB Res, Chicago, IL 60612 USA
[3] Nihon Univ, Coll Pharm, Funabashi, Chiba 2748555, Japan
关键词
triterpenoid; Chrysanthemum morifolium; chrysanthemum flower; Mycobacterium tuberculosis; antituberculosis; antimycobacterial;
D O I
10.1248/bpb.28.158
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 H(37)Rv using the Microplate Alamar Blue Assay (MABA). Fifteen compounds showed a minimum inhibitory concentration (MIC) in the range of 4-64 mug/ml, among which maniladiol (9; MIC 4 mug/ml), 3-epilupeol (17; 4 mug/ml), and 4,5 alpha-epoxyhelianol (27; 6 mug/ml) exhibited the highest activity. Cytotoxicity of compound 17 against Vero cells gave an IC50 value of over 62.5 mug/ml, suggesting some degree of selectivity for M. tuberculosis.
引用
收藏
页码:158 / 160
页数:3
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