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中药成分巴马汀在5个种属肝微粒体中的代谢特征

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目的:研究巴马汀在5个种属的体外肝微粒体代谢差异.方法:采用体外肝微粒体温孵法,在正离子模式下,通过超高效液相色谱-飞行时间质谱(UPLC-Q-TOF-MS)分析比较巴马汀在狗肝微粒体(DLM)、人肝微粒体(HLM)、小鼠肝微粒体(MLM)、猴肝微粒体(MKLM)和大鼠肝微粒体(RLM)的体外代谢途径,流动相0.1%甲酸铵的水溶液-乙腈梯度洗脱.结果:巴马汀的5个种属体外肝微粒体代谢中,鉴定了 11个代谢产物,其中DLM 3个,HLM 8个,MLM 2个,MKLM 3个,RLM 4个,其代谢途径主要是脱甲基化、羟基化、羟基化、脱氢化、甲基化、羟基化.结论:种属间的肝微粒代谢存在差异性,为进一步研究巴马汀体内代谢安全性提供依据.
Metabolism Characteristics Research of Traditional Chinese Medicine Ingredients Palmatine in Five Species Liver Microsomes
Objective:To study in vitro metabolites of Palmatine in liver microsomes are different among of five species.Methods:Using liver microsome incubation method in vitro,UPLC-Q-TOF-MS with positive ion mode was established and applied to identify the metabolites of Palmatine in liver microsomes of dog(DLM),human(HLM),mice(MLM),monkey(MKLM)and rat(RLM),mobile phase was 0.1%ammonium formate and acetonitrile for gradient elution.Results:A total of 11 metabolites,including 3 metabolites in DLM,8 metabolites in HLM,2 metabolites in MLM,3 metabolites in MKLM and 4 metabolites in RLM,were proposed and identified in liver microsomes of five species in vitro respectively,the metabolic pathway of Palmatine in liver microsomes were demonstrated as hydroxylation,dehydrogenation and hydroxylation,dehydrogenation and demethylation,demethylation and hydroxylation.,Conclusion:There are some differences in liver microsomes metabolism between species.Furthermore,the present study provided vital data for further pharmacokinetic and in vivo metabolism study of palmatine.

UPLC-Q-TOF-MSPalmatineLiver MicrosomesMetabolism

廖惠平、谢勇辉、刘晓、邓中华、黄文平、冯育林、李军茂

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吉安市中心人民医院 江西 吉安 343000

吉安县妇幼保健计划生育服务中心 江西 吉安 343000

中药固体制剂制造技术国家工程研究中心 南昌 330006

超高效液相色谱-飞行时间质谱 巴马汀 肝微粒体 代谢

江西省药品监督管理局科研项目

2020JS10

2024

江西中医药大学学报
江西中医学院

江西中医药大学学报

影响因子:0.575
ISSN:2095-7785
年,卷(期):2024.36(4)