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

doi:10.7506/spkx1002-6630-20210204-085

食品科学 ›› 2022, Vol. 43 ›› Issue (9): 103-110.doi: 10.7506/spkx1002-6630-20210204-085

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

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

（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）

出版日期:2022-05-15 发布日期:2022-05-27
基金资助:
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）

Absorption and Metabolism of a 1-Deoxynojirimycin and Hydroxychalcone Heterocomplex as a Novel α-Glucosidase Inhibitor in Rats

ZENG Jiacheng, XIAO Pinjian, NIE Jiawen, LING Lijuan, LIN Ping, TANG Daobang, ZHANG Qingfeng, CHEN Jiguang, YIN Zhongping

(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)

Online:2022-05-15 Published:2022-05-27

摘要/Abstract

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%。

关键词: α-葡萄糖苷酶抑制剂；代谢；吸收；生物利用度

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%.

Key words: α-glucosidase inhibitor; metabolism; absorption; bioavailability

中图分类号:

TS201.4

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.

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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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

Absorption and Metabolism of a 1-Deoxynojirimycin and Hydroxychalcone Heterocomplex as a Novel α-Glucosidase Inhibitor in Rats

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