尿囊素雌激素样作用  

Estrogen-like effect of allantoin

作　　者：郑晓珂[1,2] 张贝贝 曾梦楠[1] 李苗 克迎迎[1] 吴广操 冯卫生[1,2] 

机构地区：[1]河南中医药大学药学院,河南郑州450046 [2]河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心,河南郑州450046

出　　处：《药学学报》2018年第1期68-73,共6页Acta Pharmaceutica Sinica

基　　金：中央领导地方科技发展专项资助项目(14204349)

摘　　要：筛选尿囊素雌激素样活性,并初步探讨其作用特点。采用小鼠子宫增重实验和人乳腺癌细胞(MCF-7)增殖实验对尿囊素雌激素样活性进行筛选,同时ELISA法检测小鼠血清雌二醇(E2)、黄体生成素(LH)、卵泡刺激素(FSH)水平的变化;采用特异性雌激素受体阻断剂(ICI182,780)、雌激素受体α阻断剂(MPP)、雌激素受体β阻断剂(THC)、雌激素膜受体GPR30阻断剂(G15)拮抗实验及Western blot探讨其作用机制。结果显示,尿囊素可显著性提高未成熟雌性小鼠的子宫指数、血清E2与FSH水平(P<0.05);且能够促进MCF-7细胞的增殖(P<0.05),但促增殖作用可被ICI182,780、MPP、G15所抑制;Western blot结果显示,尿囊素可以显著增加小鼠子宫ERα、GPR30的表达。本研究首次发现尿囊素具有雌激素样活性,且通过雌激素受体ERα、GPR30共同介导。The study was designed to test the estrogen-like effects about allantoin. The activity of the allantoin was investigated by mouse uterine weight gain test and MCF-7 cell proliferation assay. The levels of E2, FSH and LH were also measured. ICI182,780, MPP, THC and G15 antagonnist assay and Western blot were adopted to explore the mechanism of allantoin. Allantoin increased the uterus index of premature female mice, the levels of E2 and FSH, and the expression of ERα and GPR30, compared with the control group. Allantoin also promoted the proliferation of MCF-7 cells. Co-incubation of MCF-7 cells with estrogen receptor blockers, ICI182,780, MPP and G15 abolished the inductive effect of the proliferation. These results suggest that allantoin has estrogenic activities, which are mainly mediated by ERα, GPR30.

关 键 词：尿囊素 雌激素样活性 子宫指数 拮抗剂 雌激素受体 

分 类 号：R965[医药卫生—药理学]