title: Cytotoxicity of lissoclibadins and lissoclinotoxins, isolated from a tropical ascidian Lissoclinum cf. badium, against human solid-tumor-derived cell lines.
abstract: The in vitro growth inhibitory activity of lissoclibadins and lissoclinotoxins isolated from the tropical ascidian Lissoclinum cf. badium against nine human cancer cell lines was examined to evaluate their potential anticancer efficacy. Lissoclibadins 1 (1) and 2 (2), and lissoclinotoxin F (4) showed the strongest activity of the six compounds tested, which were more potent than the anticancer drug cisplatin. Compound 1 has a trimeric structure, and compounds 2 and 4 are structural isomers possessing dimeric structures connected by disulfide and sulfide bonds of trans- and cis-orientations, respectively. Lissoclibadin 3 (3), a dimeric compound connected by two sulfide bonds, and two monomeric compounds (5, 6) were less active than 1, 2, and 4. Lissoclibadin 2 (2) was the most interesting compound possessing potent inhibitory activity against colon (DLD-1 and HCT116), breast (MDA-MB-231), renal (ACHN), and non-small-cell lung (NCI-H460) cancer cell lines and showing no toxicity following a 50 mg/kg single treatment to mice, and preferable stability in rat plasma.
authors.affiliation: Kyoritsu University of Pharmacy, Tokyo, Japan. oda-ti@kyoritsu-ph.ac.jp
authors.forename: Taiko
authors.initials: T
authors.lastname: Oda
authors.forename: Keiichi
authors.initials: K
authors.lastname: Kamoshita
authors.forename: Sakiko
authors.initials: S
authors.lastname: Maruyama
authors.forename: Kuniko
authors.initials: K
authors.lastname: Masuda
authors.forename: Masakazu
authors.initials: M
authors.lastname: Nishimoto
authors.forename: Jinzhong
authors.initials: J
authors.lastname: Xu
authors.forename: Kazuyo
authors.initials: K
authors.lastname: Ukai
authors.forename: Remy Emile Petrus
authors.initials: RE
authors.lastname: Mangindaan
authors.forename: Michio
authors.initials: M
authors.lastname: Namikoshi
mesh_terms: D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D014561:Urochordata / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents