title: Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa.
abstract: BACKGROUND
  Natural products represent an important source for agents of cancer prevention and cancer treatment. More than 60% of conventional anticancer drugs are derived from natural sources, particularly from plant-derived materials. In this study, 2α, 3α, 19β, 23β-tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid from the leaves of Sinojackia sarcocarpa, was isolated, and its anticancer activity was investigated both in vitro and in vivo.
  
  
  RESULTS
  THA possessed potent tumor selected toxicity in vitro. It exhibited significantly higher cytotoxicity to the cancer cell lines A2780 and HepG2 than to IOSE144 and QSG7701, two noncancerous cell lines derived from ovary epithelium and liver, respectively. Moreover, THA showed a dose-dependent inhibitory effect on A2780 ovary tumor growth in vivo in nude mice. THA induced a dose-dependent apoptosis and G2/M cell cycle arrest in A2780 and HepG2 cells. The THA-induced cell cycle arrest was accompanied by a downregulation of Cdc2. The apoptosis induced by THA was evident by induction of DNA fragmentation, release of cytoplasmic Cytochrome c from mitochondria, activation of caspases, downregulation of Bcl-2 and upregulation of Bax.
  
  
  CONCLUSIONS
  The primary data indicated that THA exhibit a high toxicity toward two cancer cells than their respective non-cancerous counterparts and has a significant anticancer activity both in vitro and in vivo. Thus, THA and/or its derivatives may have great potential in the prevention and treatment of human ovary tumors and other malignancies.
authors.affiliation: Institute of Genomic Medicine, Wenzhou Medical College, Wenzhou, China.
authors.forename: Ouchen
authors.initials: O
authors.lastname: Wang
authors.forename: Sujun
authors.initials: S
authors.lastname: Liu
authors.forename: Jiawei
authors.initials: J
authors.lastname: Zou
authors.forename: Liting
authors.initials: L
authors.lastname: Lu
authors.forename: Lin
authors.initials: L
authors.lastname: Chen
authors.forename: Sunquan
authors.initials: S
authors.lastname: Qiu
authors.forename: He
authors.initials: H
authors.lastname: Li
authors.forename: Xincheng
authors.initials: X
authors.lastname: Lu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000302:isolation & purification* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D005260:Female; D016195:G2 Phase / Q000187:drug effects; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D051379:Mice; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology; D029644:Styracaceae / Q000737:chemistry*; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; C097138:sericic acid; D009828:Oleanolic Acid