title: Inhibition of phospholipase cgamma1 and cancer cell proliferation by triterpene esters from Uncaria rhynchophylla.
abstract: Investigation of the hooks of Uncaria rhynchophylla resulted in isolation of six phospholipase Cgamma1 (PLCgamma1) inhibitors (1-6). The structures of these compounds were elucidated as pentacyclic triterpene esters by spectroscopic and chemical analysis. Three of them, namely uncarinic acids C (1), D (2), and E (3), are newly reported as natural products. All the compounds showed dose-dependent inhibitory activities against PLCgamma1 in vitro with IC(50) values of 9.5-44.6 microM and inhibited the proliferation of human cancer cells with IC(50) values of 0.5-6.5 microg/mL.
authors.affiliation: College of Pharmacy, Seoul National University, Seoul 151-742, Korea, Korea Research Institute of Bioscience and Biotechnology, P.O. Box 115, Yusong, Taejon 305-600, Korea.
authors.forename: J S
authors.initials: JS
authors.lastname: Lee
authors.forename: J
authors.initials: J
authors.lastname: Kim
authors.forename: B Y
authors.initials: BY
authors.lastname: Kim
authors.forename: H S
authors.initials: HS
authors.lastname: Lee
authors.forename: J S
authors.initials: JS
authors.lastname: Ahn
authors.forename: Y S
authors.initials: YS
authors.lastname: Chang
mesh_terms: D016475:3T3 Cells; D000818:Animals; D002455:Cell Division / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology; D004952:Esters / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D051379:Mice; D009369:Neoplasms / Q000201:enzymology / Q000473:pathology*; D051966:Phospholipase C gamma; D010946:Plants, Medicinal / Q000737:chemistry*; D019666:Rubiaceae / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000302:isolation & purification* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured; D010738:Type C Phospholipases / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D004952:Esters; D007527:Isoenzymes; D014315:Triterpenes; C412669:uncarinic acid-C; C412670:uncarinic acid-D; C412671:uncarinic acid-E; D010738:Type C Phospholipases; D051966:Phospholipase C gamma