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止得咳颗粒在大鼠体内的代谢产物研究

Study on metabolites derived from Zhideke granules in rats in vivo

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【作者】 梁洁郑飘雪陈辉华黄春燕梁炎丽陆春莲谢晶晶马玉明彭嘉文赵立春陈日兰

【Author】 LIANG Jie;ZHENG Piaoxue;CHEN Huihua;HUANG Chunyan;LIANG Yanli;LU Chunlian;XIE Jingjing;MA Yuming;PENG Jiawen;ZHAO Lichun;CHEN Rilan;School of Pharmacy, Guangxi University of Chinese Medicine;Guangxi Universities Laboratory of TCM Extraction,Purification and Quality Analysis;National Engineering Research Center South China Branch of TCM Solid Preparation Manufacturing Technology;Guangxi Zhuang Yao Medicine Engineering Technology Research Center;Qinzhou Inspection and Testing Center;Dept. of Pharmacy, Ruikang Hospital Affiliated to Guangxi University of Chinese Medicine;

【通讯作者】 陈日兰;

【机构】 广西中医药大学药学院广西高校中药提取纯化与质量分析重点实验室中药固体制剂制造技术国家工程研究中心华南分中心广西壮瑶药工程技术研究中心钦州市检验检测中心广西中医药大学附属瑞康医院药剂科

【摘要】 目的 分析止得咳颗粒在大鼠体内的代谢产物并推测其代谢途径。方法 将雄性SD大鼠随机分为空白组、给药组(止得咳颗粒,9.45 g/kg),每组灌胃超纯水或相应药液,每天2次,每次灌胃间隔6~8 h,连续3 d。收集各组大鼠血清、粪便、尿液样品,利用超高效液相色谱-四极杆-静电场轨道阱高分辨质谱(UPLC-Q-Exactive-MS)技术鉴定大鼠灌胃止得咳颗粒后上述生物样品中的代谢产物,并推测其代谢途径。结果 大鼠灌胃止得咳颗粒后,在其血清、尿液、粪便样品中共鉴定出16个原型成分(如野鸢尾黄素、黄芩素、绿原酸等)和11个代谢产物(如山柰酚或木犀草素水合产物、绿原酸甲基化产物、黄芩苷羟基化产物)。其中,血清样品中鉴定出8个原型成分和4个代谢产物;尿液样品中鉴定出10个原型成分和7个代谢产物;粪便样品中鉴定出8个原型成分和5个代谢产物。结论 止得咳颗粒在大鼠体内的代谢成分主要包括黄芩苷、野鸢尾黄素、绿原酸,主要涉及甲基化、羟基化、葡萄糖醛酸化等代谢途径。

【Abstract】 OBJECTIVE To analyze the metabolites of Zhideke granules and speculate its metabolic pathway in rats in vivo.METHODS Male SD rats were randomly divided into blank group and administration group(Zhideke granules, 9.45 g/kg); they were given ultrapure water or relevant medicine, twice a day, every 6-8 h, for 3 consecutive days. Serum, urine and feces samples of rats were collected, and their metabolites were identified by UPLC-Q-Exactive-MS technique after intragastric administration of Zhideke granules; their metabolic pathways were speculated. RESULTS After intragastric administration of Zhideke granules, 16prototype components(i.g. irisflorentin, baicalin, chlorogenic acid) and 11 metabolites(i.g. hydration products of kaempferol or luteolin, methylation products of chlorogenic acid, and hydroxylation products of baicalin) were identified in serum, urine and feces of rats. Among them, 8 prototype components and 4 metabolites were identified in serum samples; 10 prototype components and 7 metabolites were identified in urine samples; 8 prototype components and 5 metabolites were identified in the fecal samples. CONCLUSIONS The metabolites of Zhideke granules in rats mainly include baicalin, irisflorentin, chlorogenic acid, and the main metabolic pathways included methylation, hydroxylation, glucuronidation.

【基金】 广西创新驱动发展专项(科技重大专项)(No.桂科AA17202046);广西壮族自治区民族药资源与应用工程研究中心项目(No.桂发改高技函[2020]2605号);广西中医药重点学科(壮药学)项目(No.GZXK-Z-20-64);广西高等学校千名中青年骨干教师培育计划项目(No.桂教人[2019]5号);广西中医药大学第三批“歧黄工程”高层次人才团队培育项目
  • 【文献出处】 中国药房 ,China Pharmacy , 编辑部邮箱 ,2024年02期
  • 【分类号】R285.5
  • 【被引频次】1
  • 【下载频次】284
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