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采用假孕大鼠黄体细胞体外培养和孕酮放射免疫(RIA)测定法,比较通式为 pGlu~1-His~2-Trp-Ser~4-A~5-B~6-C~7-D~8-Pro~9-Gly~10-NH_2的七种不同结构的 LHRH 类似物抑制黄体细胞分泌孕酮作用的强弱,初步分析其构效关系。结果表明:(1)5位以 His 取代优于5位不取代者;(2)8位 Gln 取代优于 Leu 取代;(3)6位 D 型氨基酸取代提高活性的顺序是 D-Trp~6>D-Leu~6>D-Ala~6、D_2Nal~6。本文结果提示大鼠黄体细胞培养法可取代垂体细胞培养法作为 LHRH 类似物生物活性的初步定量。
In vitro culture of rat luteal cells and progesterone radioimmunoassay (RIA) were used to detect the expression of pGlu1-His2-Trp-Ser4-A5-B6-C7- The LHRH analogues of D ~ 8-Pro ~ 9-Gly ~ 10-NH_2 inhibited the secretion of progesterone by luteal cells, and their structure-activity relationship was analyzed preliminarily. The results showed that: (1) His substitution at position 5 was better than that at position 5; (2) Gln substitution at position 8 was better than Leu substitution; (3) D-Trp ~ 6 > D-Leu ~ 6> D-Ala ~ 6, D_2Nal ~ 6. Our results suggest that rat luteal cell culture can replace the pituitary cell culture method as a preliminary quantitative LHRH analogue biological activity.