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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

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【作者】 王德心鲁桂琛刘文王迺功关慕贞赵玉连王晓宁程治平

【Author】 DX Wang, GS Lu, W Liu, NG Wang, MZ Guan, YL Zhao~*, XN Wang~* and ZP Cheng~*(Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050; ~* Harbin Medical University, Harbin 150086)

【机构】 中国医学科学院药物研究所哈尔滨医科大学哈尔滨医科大学 北京 10005北京 10005哈尔滨 150086哈尔滨 150086

【摘要】 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-NH2,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)。

【Abstract】 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-NH2, LysTyr-NH2 and GlySer Lys-OH, showed significant effect (p<0.01) on inhibiting hCG-induced progesterone production.

【基金】 国家科委“七五”重点科技攻关项目;第六十五项节育技术中有关的科研基金
  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1991年01期
  • 【被引频次】1
  • 【下载频次】46
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