YM0501手性异构体对大鼠良性前列腺增生的治疗作用  

Therapeutical effects of YM0501 enantiomers on BPH model rats in vivo

作　　者：朱着 申青 何雪兰 徐静仪 许芳 袁牧 ZHU Zhuo;SHEN Qing;HE Xuelan;XU Jingyi;XU fang;YUAN Mu(School of Pharmaceutical Science, Guangzhou Medical University, Guangzhou, Guangdong,511436 P. R. China)

机构地区：[1]广州医科大学药学院

出　　处：《华西药学杂志》2018年第3期263-266,共4页West China Journal of Pharmaceutical Sciences

基　　金：广东省自然科学基金资助项目(2015A030313464)

摘　　要：目的研究YM0501手性异构体在大鼠体内抗良性前列腺增生（BPH）活性的差异。方法建立大鼠尿生殖窦（UGS）诱导BPH模型,考察α1-肾上腺素受体拮抗剂YM0501消旋体及其手性异构体对BPH的治疗作用。称量湿重、计算湿重指数;于大鼠右侧腹前叶切片,在光镜下观察其组织形态学特征,并进行组织形态计量分析;采用免疫组化定量考察间充质特异表达蛋白波形蛋白（vimentin）及α-平滑肌动蛋白（α-SMA）的阳性表达率。结果与模型组比较,异构体A及异构体B各剂量组的宿主叶湿重、湿重指数均明显减小;异构体B对宿主叶湿重、前列腺上皮细胞增生程度、间质增生程度及vimentin蛋白的抑制作用优于异构体A。结论异构体A及异构体B对模型大鼠含UGS的宿主叶间质增生均有抑制作用,异构体B抗BPH的作用优于相同剂量的异构体A。OBJECTIVE To study the therapeutic effect of two enantiomers of YM0501 on sieving the homogeneous urogenital sinus （UGS） model. METHODS The benign prostatic hyperplasia （BPH） model of rat was induced by UGS to evaluate the therapeutical effects of two enantiomers of YM0501. UGS were obtained to measure the wet weight and wet weight index of right ventral prostate ,the histomorphology features were observed under microscope with prostate slice. Morphometry was used to image analysis device. Vimentin and a -SMA expressed only in mesenchymal tissue were studied by Immunohistochemistry method. RESULTS Both enantiomer A and enantiomer B, the wet weight, wet weight index, epithelial ceils height and the mesenchymal specific expressed protein of right ventral prostate decreased in UGS model. The inhibitory effect of enantiomer B was stronger. CONCLUSION Both enantiomer A and enantiomer B can inhibit the growth and the proliferation of prostate, which is more potent than that of YM0501. Enantiomer B may exhibit higher efficacy for treating benign prostatic hyperplasia in clinic than that of racemic naftopidil.

关 键 词：YM0501 手性异构体 良性前列腺增生 尿生殖窦 组织形态学 Α1-肾上腺素受体 亚型选择性 手性药物 

分 类 号：R96[医药卫生—药理学]