title: Bile acids, carriers of hepatoma-targeted drugs?
abstract: Previous studies display that bile acids (Bas) could be used as carriers and pharmaceutical excipients. In this study, the selective cytotoxicity of 6 bile acids (BAs) was evaluated against hepatoma cell line HepG2, human colon carcinoma cell line HT-29, gastric cancer cell line BGC823, cervical cancer cell line Hela and hepatocyte line L02. Our study suggested that most of the BAs showed cytotoxicity against a broader spectrum of tumor cells and display high cell selectivity toward HepG2. In particular, chenodeoxy- cholic acid (CDCA) exerted the most potent selective cytotoxicity against HepG2 (IC₅₀ = 54.62 ± 3.5 µM) and low toxicity on L02 cells (IC₅₀ >200 µM). According to the structure-activity relationship, the position, configuration and number of OH groups in BAs could affect cell proliferation and selectivity. Moreover, the pre-mechanism of CDCA on HepG2 cells was studied by Giemsa staining, DAPI staining, AO/EB staining, apoptosis analysis and mitochondrial membrane potential assay. Results showed that CDCA could induce apoptosis and loss of mitochondrial transmembrane potential in HepG2 cells. The study inferred that CDCA might be a carrier and parent pharmaceutical excipient for hepatic carcinoma targeting drug.
authors.forename: Yan
authors.initials: Y
authors.lastname: Gong
authors.forename: Xiaoqian
authors.initials: X
authors.lastname: Zhang
authors.forename: Yuzhong
authors.initials: Y
authors.lastname: Zhang
authors.forename: Fuhao
authors.initials: F
authors.lastname: Chu
authors.forename: Guoliang
authors.initials: G
authors.lastname: Li
authors.forename: Haibo
authors.initials: H
authors.lastname: Zhang
authors.forename: Bing
authors.initials: B
authors.lastname: Xu
authors.forename: Huazheng
authors.initials: H
authors.lastname: Zhang
authors.forename: Bi
authors.initials: B
authors.lastname: Li
authors.forename: Penglong
authors.initials: P
authors.lastname: Wang
authors.forename: Haimin
authors.initials: H
authors.lastname: Lei
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001647:Bile Acids and Salts / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D016503:Drug Delivery Systems; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy*; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001647:Bile Acids and Salts; D004337:Drug Carriers