Tang, Sheng; Wang, Can; Li, Ying-Hong; Niu, Tian-Yu; Zhang, Yuan-Hui; Pang, Yu-Dong; Wang, Yan-Xiang; Kong, Wei-Jia; Song, Dan-Qing published the artcile< Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy>, Electric Literature of 6882-68-4, the main research area is diabetic nephropathy tricyclic matrinic hypoglycemic SAR pharmacodynamics glycolysis; Diabetic nephropathy; Hypoglycemic; Pharmacodynamics; Tricyclic matrinic; structure−activity relationship.
Forty-three tricyclic matrinic derivatives with a unique scaffold were prepared and evaluated for their stimulation effects on glucose consumption in HepG2 cells. The structure-activity relationship was systematically elucidated for the first time. Among them, compound 17a(I) exhibited the most promising potency, and dose-dependently increased glucose consumption in L6 myotubes. It significantly lowered blood glucose, glucosylated Hb and AGE level, and improved glucose tolerance and insulin resistance in KK-Ay mice as well. More importantly, 17a effectively ameliorated diabetic nephropathy (DN), as indicated by the improvement of renal function and pathol. changes, and decrease of urinary protein. Furthermore, 17a could induce glycolysis but suppressed aerobic oxidation of glucose, in a similar mechanism to Metform. Our results indicated that in addition to hyperglycemia, 17a may be developed to treat diabetic complication such as DN.
European Journal of Medicinal Chemistry published new progress about Advanced glycosylation end products Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Electric Literature of 6882-68-4.
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem