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作 者:杨波[1,2] 陈虹[3] 贺文彬[1] 李芳[1] 陈乃宏[1]
机构地区:[1]中国医学科学院北京协和医学院药物研究所,北京100050 [2]天津武警医学院附属医院药剂科,天津300162 [3]天津武警医学院生药教研室,天津300162
出 处:《中国新药杂志》2009年第8期724-727,754,共5页Chinese Journal of New Drugs
摘 要:目的:探讨贯叶金丝桃提取物及其制剂金玉康胶囊对5-HT受体的影响及其对细胞内钙离子的改变,揭明贯叶金丝桃提取物抗抑郁的作用机理。方法:采用放射配体受体结合法和Western blot检测5-HT1a受体表达,激光共聚焦检测细胞内游离钙离子变化。结果:贯叶金丝桃提取物、金玉康胶囊与5-HT1受体有较高的亲和力;金玉康胶囊可以上调5-HT1a受体的表达;金玉康胶囊、金丝桃素可以分别增加细胞内游离钙离子浓度4倍和5倍。结论:贯叶金丝桃提取物及制剂金玉康胶囊可能是通过与脑内5-HT1受体结合;上调5-HT1a受体表达;提高细胞内游离钙离子浓度,调节细胞内钙依赖的神经递质的释放,产生抗抑郁作用。Objective: To study the effect of Hypericum perforatum extracts and its preparation, Jinyukang capsule (JYK) , on the changes in serotonin receptor and the intracellular calcium, and to reveal the mechanism underlying the anti-depressant effect of Hypericum perforatum extracts. Methods: Ligand-receptor binding radioassay and Western blotting were used to analyze the expression of 5-HT1 receptor, and confocal microscopy was applied to detect the intracellular free calcium. Results: Both Hypericum perforatum extracts and JYK had a high affinity with 5-HT1 receptors. JYK up-regulated the expression of 5-HT1a receptors. JYK and Hypericin increased the concentration of free calcium by 4-fold and 5-fold. Conclusion: Hypericum perforatum extracts and JYK may exert the anti-depressant effect through binding to brain 5-HT1 receptors, up-regulating 5-HT1a receptors, increasing the concentration of intracellular free calcium and adjusting the calcium dependent release of neurotransmitter.
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