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Effect of DL111-IT on progesterone biosynthesis and viability of rat luteal cells in vitro 被引量:1

Effect of DL111 IT on progesterone biosynthesis and viability of rat luteal cells in vitro
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摘要 目的:研究抗孕唑(DL111IT)对离体大鼠黄体细胞孕酮合成和存活率的影响.方法:体外培养大鼠黄体细胞,用细胞计数和放射免疫法.结果:DL111IT使黄体细胞存活率随剂量上升而下降,ED50为77(71-85)mg·L-1.DL111IT3mg·L-1使黄体细胞基础黄体酮分泌下降25%,并可显著抑制弗司扣林(cAMP激动剂)10μmol·L-1和孕烯醇酮(可被3βHSD催化成黄体酮)10μmol·L-1的促孕酮分泌作用,抑制率分别为43%和155%,但不抑制hCG10IU·L-1的促黄体酮分泌作用.结论:DL111IT抗早孕作用是在cAMP和3βHSD水平上影响基础黄体酮分泌功能,并于高剂量降低黄体细胞成活率. IM: To study the influence of DL111 IT on progesterone biosynthesis of cultured luteal cells (LC). METHODS: LC viability was assessed with trypan blue dye exclusion and progesterone concentration was measured with radio ̄immuno ̄assay. RESULTS: DL111 IT decreased the viability of LC after 24 h incubation, its ED 50 being 7 7 (95 % confidence limits: 7 1-8 5) mg·L -1 . DL111 IT inhibited basal secretion of progesterone in a concentration dependent manner, and 3 mg ·L -1 decreased progesterone concentration by 25 % vs control. DL111 IT 3 mg·L -1 also inhibited the stimulatory effect of forskolin (cAMP activator) 10 μmol·L -1 and pregnenolone [converted to proges ̄ter ̄one by 3β hydroxysteroid dehydrogenase isomerase complex (3β HSD)] 10 μmol·L -1 on progesterone production in cultured LC, and their inhibitory rates were 43 % and 155 % , respec ̄tively. At the same concentration, DL111 IT did not influence hCG induced progesterone production. CONCLUSION: DL111 IT inhibited progesterone synthesis by suppressing the conversion of pregnenolone to progesterone (inactivating 3β HSD) and suppressed the activity of cAMP. DL111 IT 6-24 mg·L -1 decreased the viability of LC.
出处 《中国药理学报》 CSCD 1997年第4期361-370,共10页 Acta Pharmacologica Sinica
关键词 抗孕唑 黄体 黄体酮 细胞存活 生物合成 DL111 IT corpus luteum progesterone pregnenolone forskolin cultured cells cell survival chorionic gonadotropins
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