title: Synthesis and cytotoxicity of novel ursolic acid derivatives containing an acyl piperazine moiety.
abstract: This study designed and synthesized a series of novel ursolic acid derivatives in an attempt to develop potent antitumor agents. Their structures were confirmed using MS, IR, (1)H NMR and (13)C NMR. The inhibitory activities of the title compounds against the MGC-803 (gastric cancer cell) and Bcap-37 (breast cancer cell) human cancer cell lines were evaluated using standard MTT assay in vitro. The pharmacological results showed that some of the compounds displayed moderate to high levels of antitumor activities against the tested cancer cell lines and that most exhibited more potent inhibitory activities compared with ursolic acid. The mechanism of compound 4b was preliminarily investigated by acridine orange/ethidium bromide staining, Hoechst 33258 staining, TUNEL assay and flow cytometry, which revealed that the compound can induce cell apoptosis in MGC-803 cells.
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China.
authors.forename: Ming-Chuan
authors.initials: MC
authors.lastname: Liu
authors.forename: Sheng-Jie
authors.initials: SJ
authors.lastname: Yang
authors.forename: Lin-Hong
authors.initials: LH
authors.lastname: Jin
authors.forename: De-Yu
authors.initials: DY
authors.lastname: Hu
authors.forename: Wei
authors.initials: W
authors.lastname: Xue
authors.forename: Bao-An
authors.initials: BA
authors.lastname: Song
authors.forename: Song
authors.initials: S
authors.lastname: Yang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured; D000097245:Ursolic Acid
chemical_list: D000970:Antineoplastic Agents; D014315:Triterpenes; D000097245:Ursolic Acid