三种甾体皂苷元对心肌细胞M受体的影响  

The effect of three steroidal saponins from Yin-tonic herbal medicince on muscarinic cholinergic receptors of cultured rat myocardiac cells

作　　者：包.照日格图[1] 胡雅儿[2] 夏宗勤[2] 易宁育[2] 

机构地区：[1]云南中医学院中药系,云南昆明650200 [2]上海第二医科大学细胞调控研究室,上海200025

出　　处：《中国药理学通报》2005年第9期1140-1142,共3页Chinese Pharmacological Bulletin

摘　　要：目的观察3种甾体皂苷元对大鼠心肌细胞自然减少的M胆碱受体的调节作用。方法培养大鼠原代心肌细胞,观察其M-胆碱受体数量随培养时间变化情况;知母皂苷元(ZMS),其C-25甲基立体异构体(XMS)和薯蓣皂苷元(D IO)的终浓度分别为10-7,10-6,10-5mol.L-1,培养d 12开始给药,连续4 d。放射配基结合分析M受体的数量。结果心肌细胞M受体数时相曲线显示,培养心肌细胞M受体数在培养时间的d 10开始下降,到d 16达低水平。放射配基结合分析表明D IO未呈现M受体上调作用;ZMS和XMS均显示明显的对M受体的上调作用,并且呈现浓度依赖性。XMS的作用强度比ZMS更强,即XMS在浓度为10-7,10-6,10-5mol.L-1时都显示对M受体显著的上调作用(P<0.05,P<0.01,P<0.01),而ZMS仅在浓度为10-5mol.L-1时方呈现明显的上调作用(P<0.01)。结论滋阴中药知母有效成分知母皂苷元立体构型R型在低浓度时呈现与高浓度的S构型同分异构体相近的M受体上调作用。Aim To observe the effect of three steroidal saponins on the M-cholinoceptor density of cultured rat myocardiac cells. Methods The time course of M- cholinoceptor density was observed and diosgenin （ DIO）, timosaponin aglycone （ ZMS, S-configuration ） and XMS, a stereoisomeric compound of ZMS in C-25 methyl group, R-configuration） were added to the culture medium from the 12th day of culture at three final concentration of 10^-7,10^-6 and 10^-5 mol·L^-1, and the M-cholinoceptor density was measured on the 16th day with radioligand binding assay. Results The density of M-cholinoceptor increased gradually at the beginning of culture, reached a plateau at 4 - 10 days, and then dropped gradually. On the 16th day of culture, the M-cholinoceptor density was about 60% of theplateau value. The up-regulation effect of ZMS on the density of cultured rat myocardiac cells on the 16 th day was only significant at a final concentration of 10^-5 mol·L^-1. On the contrary, XMS was effective even when its final concentration was as low as 10^-7 mol·L^-1 DIO showed no effect on the M-cholinoceptor density at any of its three concentration. Conclusion The above results indicate that XMS with lower concentration showed similar effect on the M-cholinoceptor density of cultured mylcardiac cells as that of ZMS with more higher concentration.

关 键 词：M乙酰胆碱受体 体外培养心肌细胞 薯蓣皂苷元 放射配基结合分析 知母皂苷元 C-25甲基立体异构体 

分 类 号：R-332[医药卫生] R284.1