马钱子碱在大鼠体内的组织分布研究

Tissue Distribution of Brucine in Rats

目的考察马钱子碱的体内分布特征。方法建立HPLC法测定大鼠体内组织和血浆中马钱子碱浓度的方法。大鼠静脉注射马钱子碱5 mg·kg-1,测定不同时间点(5,20,60,120,180 min)马钱子碱在组织和血浆中的浓度。结果马钱子碱在肾组织中分布最多(22%),其次是脾(18%)、小肠(16%),在性腺中亦有一定分布(11%),在脑中的分布最少(1%)。结论马钱子碱具有很高的组织亲和性,而且在不同组织中的分布差异较大,肾组织浓度最高,提示肾脏很可能是其主要的排泄途径;脾组织浓度也较高,可能与马钱子碱具有免疫调节作用有关;在性腺中亦有一定分布。

Objective To invesligate the tissue distribution properties of brucine. Methods To determine the concentrations of brucine in the tissues and plasma, the HPLC method was validated. Following intravenous injection, brucine concentrations in different tissues and plasma were measured at time points of 5, 20, 60, 120 and 180 min, respectively. Results The highest AUC（area under the curve）was obtained in the kidney（22 %）. And high distribution was also found in the spleen（ 18 %）, small intestine（ 16 %） and gonad（ll %）. The lowest AUC of brucine was found in the brain（ 1% ）. Conclusion Brucine possesses high tissue affinity, and its concentrations vary significantly among different tissues. The highest distribution of brucine in the kidney suggests that urine excretion might be its main elimination route. And the high distribution in the spleen might be associated with its immunomodulatory efficacy. More attention should be paid to the potential toxicity of reproductive system due to its high AUC.