抑制素β_A亚基片段的合成及活性的初步测定  

SYNTHESES AND PRELIMINARY BIOASSAYS OF INHIBIN SEGMENTS /

作　　者：刘爱民[1] 鲁桂琛[1] 

机构地区：[1]中国医学科学院药物研究所,北京100050

出　　处：《药学学报》1990年第4期260-266,共7页Acta Pharmaceutica Sinica

摘　　要：以固相多肽合成方法合成了抑制素β_A亚基的六个片段:Ⅰb-βA(37～39)-NH_2(Ⅰ),Ⅰb-βA(34～39)-NH_2(Ⅱ),Ⅰb-β_A(30～39)-NH_2(Ⅲ),Ⅰb-β_A(23～39)-NH_2(Ⅳ),Ⅰb-β_A(16～39)-NH_2(Ⅴ)和Ⅰb-β_A(14-39)-NH_2(Ⅵ),对产物进行了分离纯化。用垂体细胞培养方法对其中Ⅰ,Ⅱ和Ⅲ进行生物活性测定,表明它们不能抑制由LHRH诱导的FSH分泌,Ⅳ,Ⅴ和Ⅵ三个太肽片段由于难溶于中性介质,需要寻求其它方法对其进行生物活性测定。Six segments within the subunit beta-A of the follicular inhibin have been synthesized by an improved solid phase procedure on p-methyl-benzhydrylamine (1% divinylbenzene) resin. The courses of the syntheses were monitored by quantitative ninhydrin assays and amino acid analyses. Following the cleavage by HF-pcresol (9:1 V/V), the peptides were extracted with anhydrous trifluoroacetic acid containing 1% dithiothreitol and precipitated with dry ethyl ether. The purification was achieved uniquely by reverse phase HPLC and final products were craracserized by several TLC systems, analytical HPLC and amino acid analyses. Pituitary cell culture bioassays were performed to ascertain their biological activities. However, among these synthetic peptides, the small peptides Ib-β_A(37～39)NH_2(Ⅰ), Ib-β_A(34～39)NH_2(Ⅱ), and ib-β_A(30～39)NH_2(Ⅲ)showed no significant supression on the LHRH-induced FSH secretion; the large peptides Ib-β_A(23～39)NH_2(Ⅳ), Ib-β_A(16～39)NH_2(Ⅴ), and Ib-β_A(14～39)NH_2(Ⅵ)lack adequate solubility in neutral media, and other methods are to be sought to test their bioactivities.

关 键 词：抑制素βA 亚基片段 高效液相色谱 

分 类 号：TQ467.92[化学工程—制药化工]