含羟基氨基酸小肽的合成及其抗孕酮生成活性

SYNTHESIS OF SMALL PEPTIDES CONTAINING HYDROXY-AMINO-ACID, AND ITS EFFECTS ON PROGESTERONE PRODUCTION

用固相、逐步接肽法合成了十一个含羟基氨基酸小肽。在肽树脂裂解反应中比较了HF及TFMSA(三氟甲磺酸)两种方法,裂解收率基本相同。全部产物经C-18反相柱纯化后,氨基酸组成数值均符合预期结构要求。对孕酮分泌影响的活性筛选表明Gly-Tyr-NH_2,Gly-Tyr-Lys-OH及Gly-Ser-Lys-OH有明显的抑制hCG诱发孕酮分泌的活性(P<0.01)。

Eleven peptides containing hydroxy-amino-acid have been synthesized manually by stepwise solid - phase method. Three of them were started on BHA - resin, the others on M errifield - resin. TFM SA/TFA/p -cresol were used as cleaving reagent in all peptide - resin(1～11) cleavage. Furthermore, HF cleaving procedure was also used paralleily to five of those peptide-resins for contrast. No conspicuous difference in yield was tbund between TFM SA and HF. The purity of all products was checked by the profiles of analytical reversed phase HP LC (C-18)and the data of amino acid analysis.All synthetic peptides were tested for the effect on progesterone production by rat corpus luteum in vitro. Among them, three peptides, GlyTyr-NH_2, LysTyr-NH_2 and GlySer Lys-OH, showed significant effect (p<0.01) on inhibiting hCG-induced progesterone production.