title: A Novel 1,2-Dihydroquinoline Anticancer Agent and Its Delivery to Tumor Cells Using Cationic Liposomes.
abstract: We screened nine 1,2-dihydro-quinolines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HepG2 and SMMC cells and identified ethyl-2-cyano-2-(2- (methoxycarbonyl)allyl)quinoline-1(2H)-carboxylate (compound 5) as a potential anticancer agent. In order to further develop its anticancer therapeutic potential, we incorporated this agent into cationic liposomes for delivery to tumor cells. The characteristics of liposomes, their cytotoxicity and cellular uptake by tumor cells were investigated. We demonstrated that cationic 1,2-dioleoyl-3- trimethyl-ammonium-propane containing liposomes (cLips) loaded with compound 5 has superior antitumor activity compared to neutral liposomes. These data suggest cLip-compound 5 to be a promising agent that warrants further evaluation.
authors.affiliation: School of Pharmaceutical Sciences, Jilin University, Changchun, Jilin, P.R. China.
authors.forename: Xiaoyuan
authors.initials: X
authors.lastname: Ma
authors.affiliation: School of Pharmaceutical Sciences, Jilin University, Changchun, Jilin, P.R. China.
authors.forename: Y I
authors.initials: YI
authors.lastname: Wu
authors.affiliation: School of Life Sciences, Jilin University, Changchun, Jilin, P.R. China.
authors.forename: Xuewei
authors.initials: X
authors.lastname: Yang
authors.affiliation: School of Life Sciences, Jilin University, Changchun, Jilin, P.R. China.
authors.forename: Shuang
authors.initials: S
authors.lastname: Yang
authors.affiliation: School of Life Sciences, Jilin University, Changchun, Jilin, P.R. China.
authors.forename: Yuhuan
authors.initials: Y
authors.lastname: Li
authors.affiliation: College of Agricultural and Life Sciences, University of Florida, Gainesville, FL, U.S.A.
authors.forename: Yushen
authors.initials: Y
authors.lastname: Huang
authors.affiliation: School of Life Sciences, Jilin University, Changchun, Jilin, P.R. China Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH, U.S.A..
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Lee
authors.affiliation: College of Computer Science and Technology, Jilin University, Changchun, Jilin, P.R. China baitian@jlu.edu.cn luoyungang@sohu.com.
authors.forename: Tian
authors.initials: T
authors.lastname: Bai
authors.affiliation: The Second Hospital of Jilin University, Changchun, Jilin, P.R. China baitian@jlu.edu.cn luoyungang@sohu.com.
authors.forename: Yungang
authors.initials: Y
authors.lastname: Luo
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage*; D002412:Cations; D045744:Cell Line, Tumor; D006801:Humans; D008081:Liposomes; D018613:Microscopy, Confocal; D011809:Quinones / Q000008:administration & dosage*
chemical_list: C403008:1,4-dihydroquinone; D000970:Antineoplastic Agents; D002412:Cations; D008081:Liposomes; D011809:Quinones
keywords: Dihydroquinoline; cationic liposomes; drug delivery; liposomes