王德心, 王妮, 鲁桂琛, 徐庆柴, 王乃功, 关慕贞. 酪氨酸相关肽的合成及抗孕酮生成活性J. 药学学报, 1994, 29(6): 438-442.
引用本文: 王德心, 王妮, 鲁桂琛, 徐庆柴, 王乃功, 关慕贞. 酪氨酸相关肽的合成及抗孕酮生成活性J. 药学学报, 1994, 29(6): 438-442.
DX Wang, N Wang .GC Lu, QC Xu, NGWang ,MZGuan, . SYNTHESIS OF TYROSINE-RELATED PEPTIDE AND THEIR EFFECT ON PROGESTERONE PRODUCTIONJ. Acta Pharmaceutica Sinica, 1994, 29(6): 438-442.
Citation: DX Wang, N Wang .GC Lu, QC Xu, NGWang ,MZGuan, . SYNTHESIS OF TYROSINE-RELATED PEPTIDE AND THEIR EFFECT ON PROGESTERONE PRODUCTIONJ. Acta Pharmaceutica Sinica, 1994, 29(6): 438-442.

酪氨酸相关肽的合成及抗孕酮生成活性

SYNTHESIS OF TYROSINE-RELATED PEPTIDE AND THEIR EFFECT ON PROGESTERONE PRODUCTION

  • 摘要: 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。

     

    Abstract: Twenty peptides containing hydroxy- amino acids have been synthesized manually by stepwise solid-phase procedure.The chloromethyl resin and MBHA resin were used as solid supports.A new reagent of 0.5 mol·L-1 DDSi/1.5mol·L-1 phenol/ DCM was applied for the removal of Na-Boc group.TFMSA was the cleaving reagent.After purification by C-18 column,allproducts were assayed according to amino acid analysis·The bioactivity of synthetic peptides was tested for the effect on progesterone production in uitro.Eight peptides, GlyTyrAiaLys,( SarSer )2Lys and its metftyl ester,TyrLys,HisTyr-NH2,ThrProTyrLys-NH2 TyrThrProArgLys and AspHisProThrPheLys showed significant effect on inhibiting hCG-induced progesterone production,and first three of them could also inhibit basal progesterone secretion. However,peptide GlySerTyr exhibited stimulative activity on basal proges- erone secretion,So far,no reasonable relationship between structure and bioactivity was found。

     

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