钩藤提取物与阿片受体结合特点分析

Study of Gouteng Aqueous Extract for Its Combining Potency with Morphine Subtype-Receptors(μ、δ、κ)

用放射配体结合实验方法确定钩藤提取物是否能与阿片受体发生相互作用,具体以3H-diprenorphine为标记配体,反应体系及反应条件同饱和结合实验,选用不同浓度的吗啡（10^-10-10^-5nmol/L）或钩藤提取物（0.125-4mg/mL）为竞争药物,考察钩藤提取物与转染阿片受体的结合水平.结果表明,钩藤提取物（0.125-4 mg/mL）浓度依赖地竞争3H-diprenorphine（1nmol/L）与μ、δ、κ3种阿片受体的结合,其IC50值分别为（1.27±0.86）mg/mL（n=3）（、0.59±0.21）mg/mL（n=4）和（1.20±0.24）mg/mL（n=3）,其Ki值分别为（0.41±0.27）mg/mL（n=3）、（0.26±0.09）mg/mL（n=4）和（0.38±0.08）mg/mL（n=3）,说明钩藤提取物非选择性地与μ、δ、κ三种阿片受体结合.

Radio ligand-receptor assay was used to test if Gouteng aqueous extract combined with morphine subtype receptors （μ、δ、κ）. Methods： Using 3H-diprenorphine as radio ligand and morphine（ 10^-10～10^-5 nmol/L） as positive control, the ligand-receptor assay was established. Then the Gouteng aqueous extract was added into the reaction system and its combining potency with three morphine subtype receptors（μ、δ、κ） was tested. Results： Gouteng aqueous extract（0.125 -4 mg/mL） was found to inhibit the combining of 3H-diprenorphine with morphine subtype receptors（μ、δ、κ）. And the inhibition potency was concentrated dependent.The IC50 value were as follows：μ： （1.27 ＋ 0.86）mg/mL（n = 3） ;δ：（0.59 ＋ 0.21）mg/mL（n = 4） ; κ： （1.20±0.24）mg/mL（n = 3） .The Ki value were： （0.41±0.27）mg/mL（n = 3） for μ. （0.26±0.09）mg/mL （n=4） for δ and （0.38±0.08mg/mL（n = 3） for κ.