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Pharmacokinetics of Five Alkaloids and their Metabolites in Normal and Diabetic Rats after Oral Administration of Rhizoma coptidis
Planta Medica ( IF 2.7 ) Pub Date : 2021-06-10 , DOI: 10.1055/a-1506-1627
Xinchi Feng 1 , Kun Wang 1, 2 , Shijie Cao 2 , Liqin Ding 2 , Feng Qiu 1, 2
Affiliation  

Rhizoma coptidis has been clinically used for a long time for the treatment of various diseases in China, such as hypertension, diabetes, and inflammation. Previous studies have shown that alkaloid components of Rhizoma coptidis extract could be extensively metabolized and the metabolites were also considered to be the therapeutic material basis. However, until now, pharmacokinetic studies of the in vivo metabolites have not been revealed yet. The aim of the present study was to characterize the pharmacokinetics and excretions of five main alkaloids (berberine, jatrorrhizine, palmatine, epiberberine, and coptisine) and their seven metabolites (berberrubine, demethyleneberberine, jatrorrhizine-3-O-β-D-glucuronide, thalifendine-10-O-β-D-glucuronide, berberrubine-9-O-β-D-glucuronide, demethyleneberberine-2-O-sulfate, and demethyleneberberine-2-O-β-D-glucuronide) in rats after oral administration of Rhizoma coptidis extract. Meanwhile, comparative pharmacokinetics and excretions of these analytes in diabetic model rats were also investigated, since Rhizoma coptidis is widely used for the treatment of diabetes. Our results showed that the in vivo existing forms of alkaloid components were phase II metabolites, highlighting the glucuronidation metabolic pathway. In diabetic model rats, the utilization of Rhizoma coptidis alkaloids was significantly increased and the biotransformation of berberine into berberrubine was significantly inhibited.

中文翻译:

五种生物碱及其代谢物在正常和糖尿病大鼠口服黄连后的药代动力学

黄连在我国临床上长期用于治疗高血压、糖尿病、炎症等多种疾病。以往的研究表明,黄连提取物的生物碱成分可以被广泛代谢,代谢物也被认为是治疗的物质基础。然而,到目前为止,尚未揭示体内代谢物的药代动力学研究。本研究的目的是表征五种主要生物碱(小檗碱、药根碱、巴马汀、表小檗碱和黄连碱)及其七种代谢物(小檗红碱、脱亚甲基小檗碱、药根碱-3-O-β-D-葡糖苷酸、塔利芬定-10-O-β-D-葡糖苷酸、小檗红素-9-O-β-D-葡糖苷酸、脱亚甲基小檗碱-2-O-硫酸盐、和 demethylberberine-2-O-β-D-glucuronide) 在大鼠口服黄连提取物后。同时,还研究了这些分析物在糖尿病模型大鼠中的比较药代动力学和排泄物,因为黄连广泛用于治疗糖尿病。我们的研究结果表明,生物碱成分的体内存在形式是 II 期代谢物,突出了葡萄糖醛酸化代谢途径。在糖尿病模型大鼠中,黄连生物碱的利用显着增加,黄连素向小檗红碱的生物转化受到显着抑制。因为黄连被广泛用于治疗糖尿病。我们的研究结果表明,生物碱成分的体内存在形式是 II 期代谢物,突出了葡萄糖醛酸化代谢途径。在糖尿病模型大鼠中,黄连生物碱的利用显着增加,黄连素向小檗红碱的生物转化受到显着抑制。因为黄连被广泛用于治疗糖尿病。我们的研究结果表明,生物碱成分的体内存在形式是 II 期代谢物,突出了葡萄糖醛酸化代谢途径。在糖尿病模型大鼠中,黄连生物碱的利用显着增加,黄连素向小檗红碱的生物转化受到显着抑制。
更新日期:2021-06-11
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