Selectively cytotoxic diterpenes from Euphorbia poisonii

  • J Med Chem. 1996 Feb 16;39(4):1005-8. doi: 10.1021/jm950509i.
M O Fatope  1 ,  L Zeng ,  J E Ohayaga ,  G Shi ,  J L McLaughlin
Affiliations
  • 1. Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 49707, USA.
PMID: 8632402 DOI: 10.1021/jm950509i
Abstract

Bioactivity-guided fractionation of the latex of Euphorbia poisonii Pax. (Euphorbiaceae) led to the isolation and characterization of a new tigliane diterpene, 12-deoxyphorbol 13-(9,10-methylene)undecanoate (3), together with five known diterpenes (1,2,4-6). When evaluated for cytotoxicity in a panel of six human solid tumor cell lines, the diterpene esters, 1-3, 5, and 6, were selectively cytotoxic for the human kidney carcinoma (A-498) cell line with potencies for 2 and 3 exceeding that of adriamycin by ten thousand times. Details of the isolations, structural analyses, and cytotoxic activities are described.