Inhibition of phospholipase cgamma1 and cancer cell proliferation by triterpene esters from Uncaria rhynchophylla.
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.
Lee
J S
JS
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.
Kim
J
J
Kim
B Y
BY
Lee
H S
HS
Ahn
J S
JS
Chang
Y S
YS
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*
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