环苯丙-精二肽盐酸盐水合物的合成及生理活性研究

The Study on the Synthesis and Pharmacological Activities of Cyclo-Phe-Arg Hydrochloride from the Chinese Soft Coral Sinularia sp.

本文报道了环苯丙-精二肽盐酸盐水合物1的合成及其生理活性研究。作者首次使用DCC/Na_2CO_3合成肽键,无需复杂的纯化,产品纯度较高,产率达83％。本文用此法合成了另外6种二肽。药理试验显示,1对免疫系统有广泛的增强作用并显示出较强的抗肿瘤活性,其机制可能与其免疫促进作用有关。

Cyclo-Phe-Arg hydrochloride 1 from the Chinese soft coral sinularia sp.was synthesized from Z-Phe and NO_2-Arg-OMe with the method of DCC/Na_2CO_3,which haven't been reported. The product had high purity without complicated purification. The yield was 70～80%. The synthesis of seven dipeptides containing NO_2-ArgOMe with the same method was studied. Pharmacological tests showed that 1 had marked immunopotentiation and antitumor activity in animals. We suggest that there might be a relation between these two activities.