Simmen U, Schweitzer C, Burkard W, Schaffner W, Lundstrom K
Dept. of Pharmaceutical Biology, University of Basel, Switzerland.
Pharm Acta Helv. 1998 Jun;73(1):53-6. doi: 10.1016/s0031-6865(97)00049-6.
The effects of Hypericum perforatum extracts on in vitro [3H]naloxone binding to the human mu- and rat kappa-opioid receptors were studied in chinese hamster ovary (CHO) cells using the Semliki Forest virus (SFV) expression system. Binding of [3H]naloxone to the mu- and kappa-opioid receptor was inhibited in the presence of Hypericum extracts showing IC50 values of approximately 25 and 90 micrograms/ml, respectively. In contrast, extracts of Valeriana officinalis did not inhibit binding to the mu-opioid receptor. Also, single constituents of H. perforatum like the flavonoids quercetin and kaempferol and the glycosilated flavonoid quercitrin did not inhibit [3H]naloxone binding to the mu-opioid receptor up to a concentration of 10 microM. The present in vitro data may suggest a new possible mechanism for the anti-depressant effect of H. perforatum.
利用辛德毕斯病毒（SFV）表达系统，在中国仓鼠卵巢（CHO）细胞中研究了贯叶连翘提取物对体外[³H]纳洛酮与人μ-阿片受体和大鼠κ-阿片受体结合的影响。在贯叶连翘提取物存在的情况下，[³H]纳洛酮与μ-和κ-阿片受体的结合受到抑制，IC50值分别约为25和90微克/毫升。相比之下，缬草提取物不抑制与μ-阿片受体的结合。此外，贯叶连翘的单一成分如黄酮类化合物槲皮素、山奈酚和糖基化黄酮芦丁，在浓度高达10微摩尔时不抑制[³H]纳洛酮与μ-阿片受体的结合。目前的体外数据可能提示了贯叶连翘抗抑郁作用的一种新的可能机制。
