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Planta Med 1988; 54(4): 308-311
DOI: 10.1055/s-2006-962441
Papers

© Georg Thieme Verlag Stuttgart · New York

The Cytotoxic Principles of Prunella vulgaris, Psychotria serpens, and Hyptis capitata: Ursolic Acid and Related Derivatives1

Kuo-Hsiung Lee2 , Yuh-Meei Lin2 , Tian-Shung Wu2 , De-Cheng Zhang2 , Takashi Yamagishi2 , Toshimitsu Hayashi2 , Iris H. Hall2 , Jer-Jang Chang3 , Rong-Yang Wu4 , Tsang-Hsiung Yang5
  • 2Natural Products Laboratory, Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27514, U.S.A.
  • 3Division of Laboratory Animal Medicine, School of Medicine, University of North Carolina, Chapel Hill, North Carolina 27514, U.S.A.
  • 4Institute of Botany, Academia Sinica, Nankang, Taipei, Taiwan, Republic of China.
  • 5School of Pharmacy, Taipei Medical College, Taipei, Taiwan, Republic of China.
1 Antitumor Agents; LXXXVIII. For paper LXXXVII in this series, see Fukamiya, N., Okano, M., Aratani, T., Negoro, K., Lin, Y.-M., Lee, K.-H. (1987) Planta Med. 53, 140.
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Publication History

1987

Publication Date:
24 January 2007 (online)

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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.