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Planta Med 1991; 57(4): 309-314
DOI: 10.1055/s-2006-960104
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© Georg Thieme Verlag Stuttgart · New York

Disposition of an Antineoplastic Sesquiterpene Lactone, [3 H]-Plenolin, in BDF1 Mice

Anne A. Grippo1 , 3 , Steven D. Wyrick1 , Kuo-Hsiung Lee1 , Robert P. Shrewsbury2 , Iris H. Hall1
  • 1Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7360, U.S.A.
  • 2Division of Pharmaceutics, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7360, U.S.A.
  • 3Dairy Breeding Research Center, The Pennsylvania State University, University Park, PA 16801, U.S.A.
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Publication History

1990

Publication Date:
05 January 2007 (online)

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Abstract

The pharmacokinetics of a radiolabelled analog of helenalin, [3 H]-plenolin ([3 H]-11,13-dihydrohelenalin), was determined in BDF1 mice following intravenous, intraperitoneal, and oral administration. A two-compartment pharmacokinetic model predicted that the maximum terminal (beta) half-life of [3 H]-plenolin was 57.3 hours. Urinary excretion accounted for 40.3% to 64.4% of the administered radioactivity, while fecal excretion accounted for 9.3% to 39.7%. The fecal excretion data also suggested that [3 H]-plenolin was secreted in the bile. Following intraperitoneal administration of [3 H]-plenolin, no radioactivity was sequestered in the major organs. However, radioactivity was sustained in the carcass and skin for 24 days. [3 H]-Plenolin was rapidly taken up by murine tumor cells and human fibroblasts. The drug did not significantly associate with DNA, RNA, or protein of P388 leukemia or human fibroblast cells.

Key words

Antineoplastic sesquiterpene - pharmacokinetics - helanalin - [3 H]-plenolin - Helenium genus