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 Novelα-Glucosidase Inhibitor in Rats

作　　者：曾嘉程 肖品鑑 聂嘉文 凌丽娟 林萍[1] 唐道邦[2] 张清峰[1] 陈继光[1] 尹忠平[1] ZENG Jiacheng;XIAO Pinjian;NIE Jiawen;LING Lijuan;LIN Ping;TANG Daobang;ZHANG Qingfeng;CHEN Jiguang;YIN Zhongping(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;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)

机构地区：[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　　处：《食品科学》2022年第9期103-110,共8页Food Science

基　　金：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)。

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(halflife in the terminal phase,T_(1/2))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(0.0156%);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%。The absorption and metabolism of a 1-deoxynojirimycin and hydroxychalcone heterocomplex(DC-5)as a novel potentα-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(T_(1/2))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(0.0156%).The results of pharmacokinetics test showed that the bioavailability of DC-5 in rats was 1.47%.

关 键 词：Α-葡萄糖苷酶抑制剂 代谢 吸收 生物利用度 

分 类 号：TS201.4[轻工技术与工程—食品科学]