title: Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent.
abstract: A novel anti-tumor agent, 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride (TAS-103), effectively inhibits both topoisomerase I and II activities. To enhance anti-tumor efficacy and to reduce the side effects of the agent, liposomalization of TAS-103 was performed. TAS-103 was effectively entrapped in liposomes by a remote-loading method, and was stable at 4 degrees C and in the presence of 50% serum. To evaluate the anti-tumor efficacy of liposomal TAS-103, the growth inhibition against Lewis lung carcinoma cells in vitro and the therapeutic efficacy against solid tumor-bearing mice in vivo were examined. Liposomal TAS-103 showed strong cytotoxic effect against Lewis lung carcinoma cells in a dose dependent manner and effectively suppressed solid tumor growth accompanying longer survival time of tumor-bearing mice in comparison with the mice treated with free TAS-103. These results suggest that liposomal TAS-103 is useful for cancer therapy.
authors.affiliation: Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Japan.
authors.forename: Kosuke
authors.initials: K
authors.lastname: Shimizu
authors.forename: Miki
authors.initials: M
authors.lastname: Takada
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Asai
authors.forename: Koichi
authors.initials: K
authors.lastname: Kuromi
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Baba
authors.forename: Naoto
authors.initials: N
authors.lastname: Oku
mesh_terms: D000634:Aminoquinolines / Q000008:administration & dosage*; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy / Q000201:enzymology; D004305:Dose-Response Relationship, Drug; D007192:Indenes / Q000008:administration & dosage*; D008081:Liposomes; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D015996:Survival Rate; D059005:Topoisomerase II Inhibitors; D023041:Xenograft Model Antitumor Assays / Q000379:methods
chemical_list: D000634:Aminoquinolines; D000970:Antineoplastic Agents; D007192:Indenes; D008081:Liposomes; D059005:Topoisomerase II Inhibitors; C106647:6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one