title: Three new C-27-carboxylated-lupane-triterpenoid derivatives from Potentilla discolor Bunge and their in vitro antitumor activities.
abstract: Three new lupane-triterpenoids (1-3) along with six known compounds (4-9) were isolated from the ethanolic extract of whole plant of Potentilla discolor Bunge. The structures of Compounds 1-3 were established by extensive 1D and 2D NMR together with other spectrum analysis, indicating that their C-27 positions were highly oxygenated, which were rarely found in nature. Their in vitro anti-proliferative activities against HepG-2, MCF-7 and T-84 cell lines were evaluated by Cell Counting Kit-8 (CCK-8) assay, and the results showed different activities for three cell lines with IC50 values ranging from 17.84 to 40.64 μM. In addition, the results from Hoechst 33258 and AO/EB staining as well as annexinV-FITC assays exhibited Compound 1 caused a markedly increased HepG-2 cellular apoptosis in a dose-dependent manner. The further mechanisms of Compound 1-induced cellular apoptosis were confirmed that 1 induced the production of ROS and the alteration of pro- and anti-apoptotic proteins, which led to the dysfunction of mitochondria and activation of caspase-9 and caspase-3 and finally caused cellular apoptosis. These results would be useful in search for new potential antitumor agents and for developing semisynthetic lupane-triterpenoid derivatives with high antitumor activity.
authors.affiliation: Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, P. R. China.|Institute of Agro-Food Science and Technology/Key Laboratory of Agro-Products Processing Technology of Shandong Province, Shandong Academy of Agricultural Sciences, Jinan, P. R. China.
authors.forename: Jing
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Institute of Agro-Food Science and Technology/Key Laboratory of Agro-Products Processing Technology of Shandong Province, Shandong Academy of Agricultural Sciences, Jinan, P. R. China.
authors.forename: Chao
authors.initials: C
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, P. R. China.
authors.forename: Ri-Zhen
authors.initials: RZ
authors.lastname: Huang
authors.affiliation: Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, P. R. China.
authors.forename: Hui-Feng
authors.initials: HF
authors.lastname: Chen
authors.affiliation: Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, P. R. China.
authors.forename: Zhi-Xin
authors.identifier: http://orcid.org/0000-0001-6569-366X
authors.initials: ZX
authors.lastname: Liao
authors.affiliation: Institute of Agro-Food Science and Technology/Key Laboratory of Agro-Products Processing Technology of Shandong Province, Shandong Academy of Agricultural Sciences, Jinan, P. R. China.
authors.forename: Jin-Yue
authors.initials: JY
authors.lastname: Sun
authors.affiliation: Biotechnology Center, Shandong Academy of Sciences, Jinan, P. R. China.
authors.forename: Xue-Kui
authors.initials: XK
authors.lastname: Xia
authors.affiliation: Institute of Shandong River Wetlands, Laiwu, P. R. China.
authors.forename: Feng-Xiang
authors.initials: FX
authors.lastname: Wang
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D031987:Potentilla / Q000737:chemistry*; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D053978:Pentacyclic Triterpenes
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002264:Carboxylic Acids; D014315:Triterpenes; C480546:lupane; D053978:Pentacyclic Triterpenes