ScienceAsia 10 (1984): 197-206 |doi: 10.2306/scienceasia1513-1874.1984.10.197

MOLECULAR MECHANISM OF THE ANTIFERTILITY EFFECTS OF GOSSYPOL: A REVIEW

NONGNUJ TANPHAICHITR,^a M.R. JISNUSON SVASTI^b AND PRASERT SOBHON^c

ABSTRACT: Gossypol, a plant disesquiterpene, has been used as a male contraceptive in China. After oral administration, gossypol can be taken up by several tissues, including liver, muscle and testes. Force-feeding of rats with gossypol causes degeneralion of the plasma membrane, mitochondria and axial filaments of epididymal sperm, nuclear vacuolalion and milochondrial swelling in spermatocytes and spermatids, and intercellular and intracellular vacuolation of Sertoli cells. Chemically, gossypol has been shown to react with macromolecules, such as proteins, and to form chelates with ferrous ions. It has direct effects on spermatozoa, decreasing the motility very markedly, and inhibiting the activities of several enzymes, including mitochondria-related enzymes. In addition, gossypol adversely affects the proliferation of primary cultures of Sertoli cells and transformed Sertoli cell tumor lines: in the case of the rat tumor cell line, protein synthesis was also shown to be inhibited. Similar to spermatozoa. mitochondrial transmembrane potential is diminished, as assessed by rhodamine-123 incorporation.

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a. Laboratory of Human Reproduction and Reporductive Biology, Harvard Medical School, 45 Shalluck St., Boston, MA 02115, U.S.A.
b. Department of Biochemistry and
c. Department of Anatomy, Faculty of Science, Mahidol University, Rama VI Rd., Bangkok 10400, Thailand.

Received 7 September 1984