Cytotoxic activity of amooranin and its derivatives.
Amooranin, 25-hydroxy-3-oxoolean-12-en-28-oic acid, is a triterpene acid isolated from Amoora rohituka stem bark. The cytotoxic effects of amooranin and its derivatives were studied. Amooranin and its methyl ester showed greater cytotoxicity against MCF-7 and HeLa cells derived from tumour tissues with a 50% inhibitory concentration (IC(50)) of 1.8-3.4 microg/mL, compared with Chang liver cells from normal tissue with an IC(50) of 6.2-6.4 microg/mL, but amooranin exhibited no activity on HEp-2 and L-929 cells. However, its monoacetate derivative showed no inhibitory activity at 1-10 microg/mL dose levels. Of the cytotoxic isolates, the methyl ester derivative was inactive in in vivo evaluations in the Ehrlich ascites tumour cells at 50 and 100 mg/kg/day, demonstrating T/C values of 106% and 114%, respectively.
Rabi
T
T
Research Division, Regional Cancer Centre, Thiruvananthapuram 695 011, India. rcctvm@md2.vsnl.net.in
Karunagaran
D
D
Krishnan Nair
M
M
Bhattathiri
V N
VN
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D002478:Cells, Cultured / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans; D020128:Inhibitory Concentration 50; D008099:Liver / Q000166:cytology / Q000187:drug effects*; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy*; D008517:Phytotherapy; D024301:Plant Bark; D010946:Plants, Medicinal; D014315:Triterpenes / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000972:Antineoplastic Agents, Phytogenic; D014315:Triterpenes; C453733:amooranin