应用放射配基结合法研究黄连素对α~1和β肾上腺素能受体的作用

STUDY OF BERBERINE EFFECTS ON ALPHA 1 AND BETA ADRENOCEPTORS WITH RADIOLIGAND BINDING ASSAY

本文报告黄连素与放射配基3H-prazosin和3H-DHA竞争结合α_1受体和β_1受体的实验。结果显示黄连素对α-1受体具有很强的亲和力(IC50为4.15×10^(-7),其作用强度与经典的酚妥拉明相似(IC50为2.65×10^(-1)M);对β受体具有微弱的亲和力(IC50为1.59×10^(-5)M)。上述结果提示黄连素可通过α受体及β受体而产生药理作用。

This report is to communicate the competitive binding effect in alpha 1-adrenoceptors of Wistar rat liver and beta-adrenoceptors of Wistar rat lung between berberine and 3H-prazosin and 3H-dihydro-alprenolol respectively. The results showed that berberine exhibited potent binding effect to alpha-1-adrenoceptors of Wistar rat liver. The concentration of drugs producing a 50% inhibition of specific binding (Ic50 values) was 4.15 ×10^(-7)M for berberine and 2.65×10^(-7)M for phentolamine. To beta-adrenoccptors of Wistar rat lung, berberine only had mild binding effect, the Ic50 value was 1.59×10~5M. The above results suggested that the pharmacologic effects of berberine might be carried out through alpha and beta adrenoreceptors.