title: Identification and evaluation of apoptotic compounds from Garcinia oligantha.
abstract: Four new compounds, oliganthins A-D (1-4), and one known caged xanthone gaudichaudione H (5) were isolated from the stems of Garcinia oligantha. The structures of the new compounds were elucidated by spectroscopic evidences. All of the five compounds were evaluated for their apoptosis-inducing effects using HeLa-C3 cells which have been genetically engineered to produce a fluorescent biosensor capable of detecting caspase-3 activation. All of them induced cell apoptosis at 10 μM or lower concentrations. The apoptotic activity of oliganthins A, B and gaudichaudione H were further confirmed by detecting the cleavage of PARP, which is the substrate of activated caspase-3, in these compounds-treated cells using the method of Western blot. Moreover, the values of IC(50) were measured for all five compounds on HeLa cells using the MTT assay. Among them, gaudichaudione H had the lowest IC(50) value of 0.90 μM, while the other four new compounds had IC(50) values of 1.58, 1.52, 4.15, and 7.82 μM, respectively. These results show that gaudichaudione H has the strongest apoptosis-inducing effect and cell growth inhibition effect among these xanthones and it may have the potential to be developed into a new anticancer agent.
authors.affiliation: Key Laboratory of Ethnic Medicine Resource Chemistry, State Ethnic Affairs Commission & Ministry of Education, Yunnan University of Nationalities, Kunming, Yunnan, People's Republic of China. gao_xuemei@hotmail.com
authors.forename: Xue-Mei
authors.initials: XM
authors.lastname: Gao
authors.forename: Ting
authors.initials: T
authors.lastname: Yu
authors.forename: Ming-zhu
authors.initials: MZ
authors.lastname: Cui
authors.forename: Jian-Xin
authors.initials: JX
authors.lastname: Pu
authors.forename: Xue
authors.initials: X
authors.lastname: Du
authors.forename: Quan-bin
authors.initials: QB
authors.lastname: Han
authors.forename: Qiu-fen
authors.initials: QF
authors.lastname: Hu
authors.forename: Tian-Cheng
authors.initials: TC
authors.lastname: Liu
authors.forename: Kathy Qian
authors.initials: KQ
authors.lastname: Luo
authors.forename: Hong-Xi
authors.initials: HX
authors.lastname: Xu
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D015153:Blotting, Western; D053148:Caspase 3 / Q000235:genetics / Q000378:metabolism; D005260:Female; D029760:Garcinia / Q000737:chemistry*; D015870:Gene Expression; D017930:Genes, Reporter; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010936:Plant Extracts / Q000737:chemistry; D018547:Plant Stems / Q000737:chemistry; D011065:Poly(ADP-ribose) Polymerases / Q000235:genetics / Q000378:metabolism; D002583:Uterine Cervical Neoplasms / Q000188:drug therapy / Q000473:pathology; D014966:Xanthenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D044004:Xanthones / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts; D014966:Xanthenes; D044004:Xanthones; D011065:Poly(ADP-ribose) Polymerases; D053148:Caspase 3