虎杖苷对LPS作用下心肌细胞β-肾上腺素能受体的调节作用  

The regulation and its mechanism of Polydatin on the β-adrenoreceptor in cardiac myocytes stimulated by lipopolysaccharide

作　　者：赵清[1] 黄海潇[1] 金春华[1] 

机构地区：[1]第一军医大学休克微循环重点实验室,广东广州510515

出　　处：《中国药理学通报》2004年第7期769-772,共4页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目;No 3 9870 93 6

摘　　要：目的　探讨LPS对心肌细胞 β肾上腺素能受体 (β AR)功能的影响以及虎杖苷 (PD)的防治效果。方法　体外培养心肌细胞 ,利用放射配体竞争结合法检测 β AR数量和亲和力 ,同时应用流式细胞术检测 β AR数量。 结果　正常心肌细胞膜上的 β AR最大结合容量 (Bmax)为 (4 14± 1 4 1)fmol·1× 10 5cells-1,解离常数Kd 值为 (4 0 2± 0 5 9)nmol·L-1;LPS刺激后 ,受体Bmax减小为 1 78± 0 12fmol·(1×10 5cells) -1,亲和力下降为 (2 3 88± 2 34)nmol·L-1;当用PD处理后 ,最大结合容量和亲和常数都恢复至接近正常 ,分别为 (3 37± 0 36 )fmol·(1× 10 5cells) -1和 (3 4 4± 0 4 4 )nmol·L-1;单纯用PD处理细胞Bmax和Kd 都与正常组差异无显著性 ,分别为 (2 76± 0 32 )fmol· 1× 10 5cells) -1和(4 6 3± 1 5 4 )nmol·L-1。流式细胞术检测 β AR数量变化与放射配体结合法检测结果一致。结论　LPS可直接引起心肌细胞β AR数量下调、亲和力降低 ,虎杖苷可调节 β AR的功能 ,使其维持正常水平。Aim To observe the effect of polydatin(PD) on the activities of β-AR in cardiomyocytes under the stimulation of LPS. Methods Cardiac myocytes were isolated and cultured from neonatal rats. Radioligand binding assay and flow cytometry were used to detect the function of β-AR. Results In control group, the density of β-AR (B max) was 4.14±1.41 fmol·(1×105 cells) -1 and β-AR affinity (K d) was (4.02±0.59) nmol·L -1. In LPS group, β-AR density was down-regulated 〔B max=1.78±0.12 fmol·(1×105 cells) -1〕 and the affinity decreased (K d=23.88±2.34 nmol·L -1). In LPS+PD group, β-AR B max was recovered to 3.37±0.36 fmol·(1×105 cells) -1 and the affinity increased (K d=3.44±0.44 nmol·L -1). In PD group, β-AR functions had no significant difference with normal group 〔B max=2.76±0.32 fmol·(1×105 cells) -1 and K d=4.63±1.54 nmol·L -1〕. The β-AR amount measured by flow cytometry showed the same change tendency as the radioligand binding assay. Conclusion β-AR activities may be down-regulated during the pathological process of LPS treatment. PD could reverse the effects of LPS by up-regulating β-adrenoreceptors.

关 键 词：虎杖苷 心肌细胞 LPS Β-肾上腺素能受体 

分 类 号：R-332[医药卫生] R282.71