Sodium-glucose cotransporter 2 (SGLT2) inhibitor and application thereof

• Main Authors: LIU MIN, LI XINGAN, YIN FEI, LIU JIANHUI, WANG LUJING, WU YUCUI
• Format: Patent
• Language: Chinese; English
• Published: 12.03.2019
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SUGARS

The invention provides a sodium-glucose cotransporter 2 (SGLT2) inhibitor. The SGLT2 inhibitor is trilobatin, and the specific structure of the trilobatin is shown as the following formula (please seethe specifications for the formula); and the trilobatin and the SGLT2 interact with each other, the trilobatin is in hydrogen bond connection with ASn75 and Tyr290 sites of the SGLT2, and thus the trilobatin can significantly inhibit glucose reabsorption, lowers the overall blood glucose level of an experimental subject, and meanwhile, can further improve insulin resistance of the experimental subject effectively. 本发明提供种钠-葡萄糖协同转运蛋白2抑制剂，该抑制剂三叶苷，其具体结构如下式所示，三叶苷与SGLT2蛋白之间存在相互作用，其与SGLT2的ASn75和Tyr290位点有氢键连接，因此，三叶苷能够与显著抑制葡萄糖重吸收，降低实验对象的整体血糖水平，同时，还能有效改善对实验对象的胰岛素抵抗。