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目的研究小鼠口服天然冰片后脑内冰片含量的变化以及对氨基酸类神经递质含量的影响。方法小鼠灌胃天然冰片,于给药前及给药后0.083,0.167,0.25,0.333,0.5,0.75,1,1.5,2,2.5,3,4 h分别取脑,采用GC-MS法测定冰片含量,HPLC-FLD法测定氨基酸类神经递质含量。结果小鼠口服天然冰片1.2 g/kg后5 min开始出现兴奋症状,持续10~15 min转为抑制状态。天然冰片给药后5 min即可在脑内测得,60 min达到峰值,消除半衰期1.66 h,AUC为326.7μg.h.g-1。脑内天门冬氨酸从给药后0.083 h至1 h含量显著增加,谷氨酸在给药后0.333 h含量显著增加,在给药后1.5 h至4 h含量显著降低,γ-氨基丁酸从给药后0.167 h至4 h含量均显著增加,甘氨酸含量无明显变化。结论天然冰片对中枢神经系统具有兴奋/抑制的双向作用,其作用机制与其对中枢兴奋/抑制性氨基酸类神经递质释放的调控作用有关。
Objective To study the changes of content of borneol and the effect on amino acid neurotransmitters in mice after oral administration of natural borneol. Methods Mice were intragastrically administered with natural borneol and the brain was harvested before and at 0.083,0.167,0.25,0.333,0.5,0.75,1,1.5,2,2.5,3,4 h after administration, respectively, and determined by GC-MS Borneol content, HPLC-FLD method for the determination of amino acid neurotransmitter content. Results The mice began to show excitement symptoms 5 min after oral administration of 1.2 g / kg of natural borneol, and the mice were challenged for 10-15 min. Natural borneol measured 5 min after administration in the brain, peaked at 60 min, elimination half-life 1.66 h, AUC 326.7μg.h.g-1. The content of aspartate in brain increased significantly from 0.083 h to 1 h after administration, the content of glutamate increased significantly at 0.333 h after administration, and decreased significantly from 1.5 h to 4 h after administration, From 0.167 h to 4 h after administration, the contents of glycine were significantly increased, while the contents of glycine did not change significantly. CONCLUSION Natural borneol has a bidirectional effect on the central nervous system (CNS). Its mechanism of action is related to its regulation on the release of central excitatory / inhibitory amino acid neurotransmitters.