title: Cytotoxic cardenolide and sterols from Calotropis gigantea.
abstract: The dichloromethane extract from the leaves of Calotropis gigantea Linn. was strongly cytotoxic against non-small cell lung carcinoma (A549), colon carcinoma (HCT 116) and hepatocellular carcinoma (Hep G2), and non toxic to Chinese hamster ovary (AA8). The extract afforded uscharin (1), 3,5,8-trihydroxy-24-methylcholest-6,22-diene (2), a mixture of (24R)-3beta-hydroxy-24-ethylcholest-5-en-7-one (3a) and 6beta-hydroxy-24-ethylcholest-4,22-dien-3-one (3b), and another mixture of (24R)-24-ethylcholest-4-en-3-one (4a) and (24S)-24-ethylcholest-4,22-dien-3-one (4b). Cardenolide 1 exhibited extreme toxicity to A549, HCT 116 and Hep G2 with IC50 values of 0.003 microg/mL, 0.013 microg/mL, and 0.018 microg/mL, respectively, while sample 3 exhibited an IC50 of 1.35 microg/mL, 4.46 microg/mL, and 3.83 microg/mL, respectively.
authors.affiliation: Institute of Biology, College of Science, University of the Philippines, Diliman, Quezon City, Philippines.
authors.forename: Sonia D
authors.initials: SD
authors.lastname: Jacinto
authors.forename: Eunice Alexis C
authors.initials: EA
authors.lastname: Chun
authors.forename: Anthony Sebastian
authors.initials: AS
authors.lastname: Montuno
authors.forename: Chien-Chang
authors.initials: CC
authors.lastname: Shen
authors.forename: Dinah L
authors.initials: DL
authors.lastname: Espineli
authors.forename: Consolacion Y
authors.initials: CY
authors.lastname: Ragasa
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology; D031107:Calotropis / Q000737:chemistry*; D002298:Cardenolides / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D006801:Humans; D018515:Plant Leaves / Q000737:chemistry; D013261:Sterols / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002298:Cardenolides; D013261:Sterols