The Cytotoxic Principles ofPrunella vulgaris, Psychotria serpens, andHyptis capitata: Ursolic Acid and Related Derivatives1

Authors:
  • KLKuo-Hsiung Lee
    Kuo-Hsiung Lee
  • YLYuh-Meei Lin
    Yuh-Meei Lin
  • TWTian-Shung Wu
    Tian-Shung Wu
  • DZDe-Cheng Zhang
    De-Cheng Zhang
  • TYTakashi Yamagishi
    Takashi Yamagishi
  • THToshimitsu Hayashi
    Toshimitsu Hayashi
  • IHIris H. Hall
    Iris H. Hall
  • JCJer-Jang Chang
    Jer-Jang Chang
  • RWRong-Yang Wu
    Rong-Yang Wu
  • TYTsang-Hsiung Yang
    Tsang-Hsiung Yang

Abstract
Bioassay-directed fractionation of the cytotoxic antileukemic extracts of Prunella vulgaris, Psychotria serpens, and Hyptis capitata has led to the isolation of ursolic acid as one of the active principles. Ursolic acid showed significant cytotoxicity in the lymphocytic leukemia cells P-388 and L-1210 as well as the human lung carcinoma cell A-549. It also demonstrated marginal cytotoxicity in the KB and the human colon (HCT-8) and mammary (MCF-7) tumor cells. Esterification of the hydroxyl group at C-3 and the carboxyl group at C-17 led to compounds with decreased cytotoxicity in the human tumor cell lines, but with equivalent or slightly increased activity against the growth of L-1210 and P-388 leukemic cells.