Antitubercular activity of triterpenoids from Asteraceae flowers.
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.
Akihisa
Toshihiro
T
College of Science and Technology, Nihon University, Tokyo, Japan. akihisa@chem.cst.nihon-u.ac.jp
Franzblau
Scott G
SG
Ukiya
Motohiko
M
Okuda
Hiroki
H
Zhang
Fangqiu
F
Yasukawa
Ken
K
Suzuki
Takashi
T
Kimura
Yumiko
Y
D000818:Animals; D000995:Antitubercular Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D019659:Asteraceae; D002522:Chlorocebus aethiops; D035264:Flowers; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000254:growth & development; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D014315:Triterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014709:Vero Cells
D000995:Antitubercular Agents; D010936:Plant Extracts; D014315:Triterpenes