Abstract: The researches of pharmacology of polyprenyl phosphate (PPH) from Ginkgo biloba L.on antitumor in vitro and in vivo were carried out. After extracting,separating and purifying the mixs of polyprenols (C₇₅-C₁₁₀) from leaves of G. biloba L., polyprenyl monophosphates were synthesized from polyprenols with POCl₃ and triethanylamide. In contrast to 5-Fu,the antitumor activities were studied in vitro with SGC-7901,LoVo and Hela, and in vivo with mice transplanted tumors of Heps,S₁₈₀ and EC Heps, S₁₈₀ and EC. The pharmacologic experiments were done by various doses of PPH.Results show that PPH have the inhibition of 60%-80% against SGC-7901,LoVo and Hela in vitro at high concentration of 0.400:g/L after 72:h,and have the inhibition of 50%-65% against transplanted Heps,S₁₈₀ and EC. This shows that PPH from leaves of G. biloba L. has distinct antitumor biological activity.

Key words: Ginkgo biloba L., polyprenols, polyprenyl phosphates, antitumor