Xue Bao-Juan, Zhao Wen-Wen, Sun Xiu-Rui, Zhang Zhe, Chen Jian-Hua, Zhang Yu-Jie
School of Chinese Materia Medica, Beijing University of Chinese Medicine Beijing 102488, China Monitoring and Statistical Research Center, National Administration of Traditional Chinese Medicine Beijing 100027, China.
School of Chinese Materia Medica, Beijing University of Chinese Medicine Beijing 102488, China.
Zhongguo Zhong Yao Za Zhi. 2022 Jul;47(14):3908-3914. doi: 10.19540/j.cnki.cjcmm.20220121.201.
Magnoflorine is an important aporphine alkaloid in Coptidis Rhizoma. As reported previously, coexisting components in Coptidis Rhizoma can change the pharmacokinetic characteristics of magnoflorine. To illustrate the interactional links of magnoflorine with its coexisting components in Coptidis Rhizoma, the present study investigated the influence of coexisting components in Coptidis Rhizoma on the excretion of magnoflorine in rat bile, urine, and feces. The rats were dosed with magnoflorine(30 mg·kg(-1)) and water decoction of Coptidis Rhizoma(equivalent to 30 mg·kg(-1) magnoflorine) via intragastric administration, and magnoflorine(10 mg·kg~(-1)) by intravenous administration, respectively, and the excretion of magnoflorine in rat bile, urine, and feces in 24 h was observed. The excretion rates of magnoflorine in bile and urine in 24 h were 0.90% and 37.11% respectively after intravenous administration of magnoflorine, which suggested that urination was the main excretive way of magnoflorine. The excretion rates of magnoflorine in feces were 8.77% and 6.18% respectively after intragastric administration of magnoflorine and water decoction of Coptidis Rhizoma, which indicated that defecation was the main excretion route of magnoflorine. The cumulative excretion rates of magnoflorine in the bile, urine, and feces in the Coptidis Rhizoma water decoction group were 77.78%, 79.44%, and 70.47% of those in the magnoflorine group. The results showed that the cumulative excretion rates of magnoflorine in rat bile, urine, and feces were not high, suggesting that magnoflorine was metabolized significantly in rats. The coexisting components of Coptidis Rhizoma could inhibit the excretion of magnoflorine in rat bile, urine, and feces, which was consistent with the decrease in the elimination rate of magnoflorine in the pharmacokinetics of Coptidis Rhizoma water decoction. It indicated interactions between drugs. This study is expected to provide references for the development of magnoflorine-containing new drugs and rational clinical medication of Coptidis Rhizoma.
小檗碱是黄连中的一种重要阿朴菲生物碱。如先前报道,黄连中的共存成分可改变小檗碱的药代动力学特征。为阐明小檗碱与其在黄连中的共存成分之间的相互作用关系,本研究考察了黄连中的共存成分对大鼠胆汁、尿液和粪便中小檗碱排泄的影响。分别通过灌胃给予大鼠小檗碱(30 mg·kg⁻¹)和黄连水煎液(相当于30 mg·kg⁻¹小檗碱),以及静脉注射给予大鼠小檗碱(10 mg·kg⁻¹),观察24小时内大鼠胆汁、尿液和粪便中小檗碱的排泄情况。静脉注射小檗碱后,24小时内胆汁和尿液中小檗碱的排泄率分别为0.90%和37.11%,这表明排尿是小檗碱的主要排泄途径。灌胃给予小檗碱和黄连水煎液后,粪便中小檗碱的排泄率分别为8.77%和6.18%,这表明排便为小檗碱的主要排泄途径。黄连水煎液组胆汁、尿液和粪便中小檗碱的累积排泄率分别为小檗碱组的77.78%、79.44%和70.47%。结果表明,大鼠胆汁、尿液和粪便中小檗碱的累积排泄率不高,提示小檗碱在大鼠体内有显著代谢。黄连中的共存成分可抑制大鼠胆汁、尿液和粪便中小檗碱的排泄,这与黄连水煎液药代动力学中小檗碱消除率降低一致。这表明药物之间存在相互作用。本研究有望为含小檗碱新药的研发及黄连的合理临床用药提供参考。