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首页> 外文期刊>RSC Advances >Pharmacokinetic profile and metabolite identification of bornyl caffeate and caffeic acid in rats by high performance liquid chromatography coupled with mass spectrometry
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Pharmacokinetic profile and metabolite identification of bornyl caffeate and caffeic acid in rats by high performance liquid chromatography coupled with mass spectrometry

机译：高效液相色谱法与质谱相偶联大鼠二烷基咖啡因和咖啡酸的药代动力学曲线和代谢物鉴定

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摘要

Bornyl caffeate was initially discovered as a bioactive compound in medicinal plants. Despite the promising pharmacological activities including anti-tumor and antibacterial activities, the pharmacokinetics of the compound remain open. This work developed a high performance liquid chromatography-tandem mass spectrometric method for the determination of bornyl caffeate and caffeic acid (major metabolite and a main unit of bornyl caffeate) in vivo. Successful application of the method included identification of its metabolites and investigation on the drug pharmacokinetics. A total of 30 compounds were identified as the metabolites of bornyl caffeate in rats. We attributed these metabolites to phase I metabolic routes of reduction, oxidation, hydrolysis and phase II metabolic reactions of glucuronidation, sulfation, Omethylation and glycine. Glucuronidation, sulfation, O-methylation and reduction were the main metabolic pathways of bornyl caffeate. The method presented a linear range of 1-4000 ng mL(-1). The pharmacokinetic profile of bornyl caffeate was found to be a three compartment open model, while caffeic acid fitted to a two compartment open model when it was administered alone or served as the main metabolite of bornyl caffeate. The time to peak concentration (T-max) and the maximum plasma concentration (C-max) of bornyl caffeate were 0.53 h and 409.33 ng mL(-1). Compared with original caffeic acid, the compound displayed an increased half-life of elimination (T-1/2 beta), area under the concentration time curve from 0 to t (AUC(0-infinity)) and area under the concentration time curve from 0 to infinity (AUC(0-infinity)), a decreased half-life of absorption (T-1/2 alpha) and an identical C-max. Taking together, we concluded that bornyl caffeate is able to rapidly initiate therapeutic effect and last for a relatively long time in rats; metabolic pathways of O-methylation and reduction is key to interpret the mechanism and toxicity of bornyl caffeate.
机译：最初在药用植物中发现Bordel咖啡因作为生物活性化合物。尽管有前途的药理学活动，包括抗肿瘤和抗菌活性，但该化合物的药代动力学仍然是开放的。这项工作开发了一种高效液相色谱 - 串联质谱法，用于测定Bordyl咖啡因和咖啡酸（主要代谢物和Bornyl Caffeate的主要单位）体内。该方法的成功应用包括其代谢物的鉴定和对药物药代动力学的调查。共鉴定了总共30种化合物作为大鼠咖啡因的代谢产物。我们将这些代谢产物归因于葡萄糖醛，硫化，亚甲基化和甘氨酸的氧化物，氧化，水解和期代谢反应的I代谢物。葡萄糖醛酸化，硫化，O-甲基化和还原是Bordell Caffeate的主要代谢途径。该方法呈现1-4000ng ml（-1）的线性范围。发现二蚕的药代动力学谱是三个隔室开放模型，而咖啡酸在单独给药时适合两个隔室开放式模型，或者作为Bordyl咖啡因的主要代谢物。峰浓度（T-MAX）的时间（T-MAX）和BOLYL咖啡因的最大血浆浓度（C-MAX）为0.53小时和409.33ng mL（-1）。与原始咖啡酸相比，化合物显示出消除（T-1 /2β）的半衰期增加（T-1 /2β），浓度时间曲线下的面积（AUC（0-无穷大）和面积在浓度时间曲线下从0到无穷大（AUC（0-无穷大），减少的吸收半衰期（T-1/2α）和相同的C-MAX。在一起，我们得出结论，Bornyl Caffeate能够迅速启动治疗效果，并在大鼠中持续相对较长的时间; O-甲基化和还原的代谢途径是解释Bordyl咖啡因的机制和毒性的关键。

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  • 来源
    《RSC Advances》 |2019年第7期|共13页
  • 作者

    Shi Baimei; Yang Lingjian; Gao Tian; Ma Cuicui; Li Qiannan; Nan Yefei; Wang Shixiang; Xiao Chaoni; Jia Pu; Zheng Xiaohui;

  • 作者单位

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

    Northwest Univ Coll Life Sci Minist Educ Key Lab Resource Biol &

    Biotechnol Western China 195 Mail Box 229 Northern Taibai Rd Xian 710069 Shaanxi Peoples R China;

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