| 新型α-葡萄糖苷酶抑制剂1-脱氧野尻霉素-羟基查耳酮杂合体在大鼠体内的吸收与代谢 |
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| 引用本文： | 曾嘉程,肖品鑑,聂嘉文,凌丽娟,林萍,唐道邦,张清峰,陈继光,尹忠平.新型α-葡萄糖苷酶抑制剂1-脱氧野尻霉素-羟基查耳酮杂合体在大鼠体内的吸收与代谢[J].食品科学,2022,43(9):103-110. |
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| 作者姓名： | 曾嘉程 肖品鑑 聂嘉文 凌丽娟 林萍 唐道邦 张清峰 陈继光 尹忠平 |
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| 作者单位： | （1.江西农业大学食品科学与工程学院，江西省天然产物与功能食品重点实验室，江西省农产品加工与安全控制工程实验室，江西 南昌 330045；2.广东省农业科学院蚕业与农产品加工研究所，农业农村部功能食品重点实验室，广东省农产品加工重点实验室，广东 广州 510610） |
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| 基金项目： | 国家自然科学基金地区科学基金项目（31460436）；广州市科技计划项目（201909020001）；
江西省食品药品监督管理局科技项目（2017SP05） |
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| 摘 要： | 本实验研究了新型、高效α-葡萄糖苷酶抑制剂1-脱氧野尻霉素-羟基查耳酮杂合体（DC-5）在大鼠体内的吸收与代谢。超高效液相色谱-四极杆-飞行时间串联质谱（ultra-performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry，UPLC-Q-TOF-MS/MS）检测结果表明，DC-5灌胃后大鼠血液中出现了加氢还原、甲基化、磺酸化及葡萄糖醛酸化4 种代谢产物；灌胃后0.5 h，大鼠血液、心、肝、肺、胃、小肠中的DC-5含量达到峰值，而脾和肾中则在灌胃后1 h达到最高值；大鼠血液中DC-5的峰值质量浓度为162.76 ng/mL，半衰期（half-life in the terminal phase，T1/2）为30.66 h，平均驻留时间（mean residence time，MRT）为11.41 h；粪便是DC-5的主要排泄途径，24 h内排泄量为灌胃量的2.26%，显著高于24 h内尿液中的排泄量（0.015 6%）；药代动力学分析结果表明，DC-5在大鼠体内的生物利用度为1.47%。
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| 关 键 词： | α-葡萄糖苷酶抑制剂 代谢 吸收 生物利用度 |
Absorption and Metabolism of a 1-Deoxynojirimycin and Hydroxychalcone Heterocomplex as a Novel α-Glucosidase Inhibitor in Rats |
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| ZENG Jiacheng,XIAO Pinjian,NIE Jiawen,LING Lijuan,LIN Ping,TANG Daobang,ZHANG Qingfeng,CHEN Jiguang,YIN Zhongping.Absorption and Metabolism of a 1-Deoxynojirimycin and Hydroxychalcone Heterocomplex as a Novel α-Glucosidase Inhibitor in Rats[J].Food Science,2022,43(9):103-110. |
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| Authors: | ZENG Jiacheng XIAO Pinjian NIE Jiawen LING Lijuan LIN Ping TANG Daobang ZHANG Qingfeng CHEN Jiguang YIN Zhongping |
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| Affiliation: | (1. Jiangxi Key Laboratory of Natural Products and Functional Foods, Jiangxi Agro-processing and Safety Control Engineering Laboratory, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, China; 2. Key Laboratory of Functional Foods, Ministry of Agriculture and Rural Affairs, Guangdong Key Laboratory of Agricultural Products Processing, Sericultural & Agri-food Research Institute, Guangdong Academy of Agricultural Sciences, Guangzhou 510610, China) |
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| Abstract: | The absorption and metabolism of a 1-deoxynojirimycin and hydroxychalcone heterocomplex (DC-5) as a novel potent α-glucosidase inhibitor was investigated in rats. A total of four metabolites derived from DC-5 were identified in the blood of rats gavaged with DC-5 using ultra-performance liquid chromatography quadrupole time-of-flight tandem mass micrometry (UPLC-Q-TOF-MS/MS), including hydrogenated, methylated, sulfonated, and glucuronidated metabolites of DC-5. The concentration of DC-5 in the blood, heart, liver, lung, stomach and small intestine all peaked at 0.5 h after oral administration, while the peak concentration appeared at 1 h in the spleen and kidney. The peak concentration of DC-5 in the blood was 162.76 ng/mL, with a half-life in the terminal phase (T1/2) of 30.66 h and mean residence time (MRT) of 11.41 h. DC-5 was mainly excreted via feces, and a total of 2.26% of the intragastrical DC-5 was found in feces, which was significantly higher than that in urine (0.015 6%). The results of pharmacokinetics test showed that the bioavailability of DC-5 in rats was 1.47%. |
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| Keywords: | α-glucosidase inhibitor metabolism absorption bioavailability |
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