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利用固相法合成了二十个含羟基氨基酸的小肽。其中,以0.5mol·L-1二甲二氯硅烷/1.5mol·L-1苯酚/DCM*为脱除Boc试剂,以TFMSA为切除树脂试剂。经C-18反相柱纯化后,全部产物均通过氨基酸分析要求。体外黄体细胞分泌孕酮实验表明有八个肽化物GlyTyrAlaLys,(SarSer)2Lys及其申酯,TyrLys,HisTyr-NH2,ThrProTyrLys-NH2,TyrThrProArgLys,AspHisProThr-PheLys显示较强的抑制hCG致孕酮分泌的活性,而且前三个肽还能显著抑制基础孕酮的分泌,相反,GlySerTyr能刺激基础孕酮的分泌。目前尚未建立合理的结构一活性关系。
Twenty hydroxyl-terminated amino acids were synthesized by solid-phase method. Among them, the Boc reagent was removed with 0.5 mol·L-1 dichlorodichlorosilane / 1.5 mol·L-1 phenol / DCM *, and TFMSA was used as the excision resin reagent. After purification by C-18 reverse phase column, all products were required for amino acid analysis. In vitro progesterone secretion assay showed that there are eight peptides GlyTyrAlaLys, (SarSer) 2Lys and their esters, TyrLys, HisTyr-NH2, ThrProTyrLys-NH2, TyrThrProArgLys, AspHisProThr-PheLys showed stronger inhibition of hCG-induced progesterone secretion Activity, and the first three peptides also significantly inhibited the secretion of basal progesterone, whereas GlySerTyr stimulated the secretion of basal progesterone. At present, no reasonable structure-activity relationship has been established.