WATER-SOLUBLE DERIVATIVES OF GOSSYPOL

一种有效的口服男性抗生育药物，既无毒又 可逆，目前不可用。棉酚，最有希望的 非类固醇男性抗生育铅，具有不可接受的狭窄 治疗比率。 我们建议可以通过改变治疗方案来提高治疗比例。 水溶作用的药代动力学和生物利用度。 因此，几种精心挑选的棉酚水溶性衍生物 都会做好准备。然后将在体外对这些化合物进行这两种测试 杀精活性和体内抗生育活性。体内试验 将从疗效和毒性两方面进行评估。 一种与棉酚相同药效的化合物的鉴定 没有毒性的影响将为进一步的研究提供基础 最终开发一种安全有效的男性抗生育药物 探员。

An effective oral male antifertility agent, which is both non-toxic and reversible, is not currently available. Gossypol, the most promising non-steroidal male antifertility lead, has an unacceptably narrow therapeutic ratio. We propose that the therapeutic ratio may be improved by alteration of the pharmaco-kinetics and bioavailability through water-solubilization. Accordingly, several carefully chosen water-soluble derivatives of gossypol will be prepared. These compounds will then be tested for both in vitro spermicidal activity and in vivo antifertility activity. The in vivo tests will be evaluated both in terms of efficacy and toxicity. The identification of a compound with the same efficacy as gossypol but without the toxic effects would provide the basis for further study leading to the eventual development of a safe and effective male antifertility agent.