合成冰片影响血脑屏障开放促槲皮素脑吸收的研究

目的:观察冰片对正常小鼠血脑屏障(blood brain barrier,BBB)开放性的影响及其促进槲皮素脑组织吸收的作用,为芳香开窍药的促BBB开放作用应用于脑部疾病的治疗提供依据。方法:小鼠随机分为单用槲皮素给药组、冰片加槲皮素组、P-糖蛋白抑制剂加槲皮素给药组、5-羟色胺抑制剂加槲皮素给药组等,空白组为对照,各组小鼠分别灌胃给予相应的药物3天后,断头取血和脑组织;采用高效液相色谱法测定小鼠血浆及脑组织中槲皮素含量。结果:与单用槲皮素给药组(50 mg/kg)相比较,冰片(200mg/kg)加槲皮素组(50 mg/kg)、P-糖蛋白抑制剂(56mg/kg)加槲皮素给药组(50 mg/kg)的脑组织槲皮素含量均显著升高(P<0.05),而5-羟色胺抑制剂(25mg/kg)加槲皮素给药组(50 mg/kg)的脑组织槲皮素含量显著下降(P<0.05);与单用槲皮素给药组(50 mg/kg)相比较,冰片(200mg/kg)加槲皮素组(50 mg/kg)、P-糖蛋白抑制剂(56mg/kg)加槲皮素给药组(50 mg/kg)槲的血浆药物浓度均显著下降(P<0.05)。结论:冰片对小鼠生理状态下的血脑屏障具有一定的开放效应,可能是该类药物通过影响P-糖蛋白与5-羟色胺的含量使血脑屏障细胞膜通透性增加从而促进药物吸收,其促血脑屏障开放的机制可能为芳香走窜、引药上行功效的药理基础之一。

Study on the effect of borneol influence on BBB opening for promoting the cerebral absorption of quercetin

Objective: To investigate aromatic drugs for inducing resuscitation of borneol influence on blood brain barrier(BBB) opening for the cerebral absorption of quercetin and provide a basis for the effect of aromatic drugs for inducing resuscitation promoting BBB opening in the treatment of of cerebral disease.Methods: Kunming mice were randomly divided into 8 groups(quercetin group,borneol add quercetin group,P-gp inhibitor add quercetin group,5-HT inhibitor add quercetin group,et al)and blank group as control.The determination of content of quercetin in mice plasma and brain tissue by HPLC.Results: The contents of quercetin in mice brain tissue in borneol add quercetin group and P-gp inhibitor add quercetin group were significant higher than that of quercetin group(P<0.05),however,the content of quercetin in mice brain tissue in 5-HT inhibitor add quercetin group was significant lower than that of quercetin group(P<0.05).The contents of quercetin in mice plasma in borneol add quercetin group and P-gp inhibitor add quercetin group were significant lower than that of quercetin group(P<0.05).Conclusion: Borneol has the effect of promoting BBB opening in mice under physiologic condition,and the mechanism of improving the absorption of quercetin in mice brain tissue probobly was influence on the contents of P-gp and 5-HT,which so as to provide pharmacology foundation for functions of guide medicine to go ahead.