title: Antitubercular activity of triterpenoids from Asteraceae flowers.
abstract: 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.
authors.affiliation: College of Science and Technology, Nihon University, Tokyo, Japan. akihisa@chem.cst.nihon-u.ac.jp
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Akihisa
authors.forename: Scott G
authors.initials: SG
authors.lastname: Franzblau
authors.forename: Motohiko
authors.initials: M
authors.lastname: Ukiya
authors.forename: Hiroki
authors.initials: H
authors.lastname: Okuda
authors.forename: Fangqiu
authors.initials: F
authors.lastname: Zhang
authors.forename: Ken
authors.initials: K
authors.lastname: Yasukawa
authors.forename: Takashi
authors.initials: T
authors.lastname: Suzuki
authors.forename: Yumiko
authors.initials: Y
authors.lastname: Kimura
mesh_terms: 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
chemical_list: D000995:Antitubercular Agents; D010936:Plant Extracts; D014315:Triterpenes