雷公藤内酯酮的半合成方法研究

Study on Semisynthesis of Triptonide

雷公藤环氧二萜内酯类化合物,是植物雷公藤(Tripterygium wilfordii Hook f.)中起抗炎免疫及雄性抗生育活性的主要一类化合物。药理试验表明,在这类化合物中,雷公藤内酯酮(triptonide,Ⅰ)反映的两类活性效价的差值最大,其抗生育单剂量效价比免疫抑制活性高约12倍,具有一定的雄性抗生育活性优势,展现了一定的抗生育前景。

Triptonide(Ⅰ) is one of the epoxide diterpenes isolated from Tripterygium wilfordii Hook f. (TW). Pharmacologic assay showed that triptonide possesses a potent male antifertility effect, and its dose ratio of antifertility action to immunosuppressive action is lower than that of any other known epoxide diterpene from TW. It is inferred that triptonide may be developed into a male contraceptive. but the content of triptonide is very low in TW. We have semi-synthesized triptonide by the oxidation of triptolide (Ⅱ) isolated from TW. It is clear from the data of some oxidation methods that the condition of oxidation with K_2Cr_2O_7/CrO_3/H_2SO_4/H_2O/(CH_3)_2CO is better. Triptolide was conversed into triptonide by 97%.