Antitubercular activity of triterpenoids from Asteraceae flowers
Antitubercular activity of triterpenoids from Asteraceae flowers
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DOI：
10.1248/bpb.28.158
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发表时间：
2005-01-01
影响因子：
2
通讯作者：
Kimura, Y
中科院分区：
文献类型：
--
作者：
Akihisa, T;Franzblau, SG;Kimura, Y
共分离得到28个3-羟基三萜类化合物，分别为蒲公英烷-（1-7）、齐墩果烷-（8-12）、乌索烷-（13-15）、羽扇烷-（16，18，19），蒲公英烷-（20），环阿糖胞苷-（21-25），三茂卡烷-（26-28），和从菊花提取物的不可皂化脂质部分分离的达玛烷型（29）用微量板碱性蓝法（MABA）测定了16个化合物和一个羽扇烷型3 α-羟基三萜（17）对结核分枝杆菌菌株H（37）Rv的抗结核活性。15种化合物显示出4-64 μ g/ml范围内的最小抑制浓度（MIC），其中马尼拉二醇（9; MIC 4 μ g/ml）、3-Epilupeol（17; 4 μ g/ml）和4，5 α-环氧向日葵醇（27; 6 μ g/ml）显示出最高活性。化合物17对Vero细胞的细胞毒性给出超过62.5 μ g/ml的IC 50值，表明对M有一定程度的选择性。结核
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.