Preliminary tests in rats have shown that the title complex is an efficient insulin mimic, which may be the first example of polyoxomatalates possessing insulin mimetic activity.
AIM： To identify the glucose lowering ability and chronic treatment effects of a novel coumarin-glucagon-like peptide-1 （GLP-1） conjugate H J07. METHOD： A receptor activation experiment was performed in HEK 293 ce...AIM： To identify the glucose lowering ability and chronic treatment effects of a novel coumarin-glucagon-like peptide-1 （GLP-1） conjugate H J07. METHOD： A receptor activation experiment was performed in HEK 293 cells and the glucose lowering ability was evaluated with hypoglycemic duration and glucose stabilizing tests. Chronic treatment was performed by daily injection of exendin-4, saline, and HJ07. Body weight and HbAlc were measured every week, and an intraperitoneal glucose tolerance test was performed before treatment and after treatment. RESULTS： HJ07 showed well-preserved receptor activation efficacy. The hypoglycemic duration test showed that HJ07 possessed a long-acting, glucose-lowering effect and the glucose stabilizing test showed that the antihyperglycemic activity of H J07 was still evident at a predetermined time （12 h） prior to the glucose challenge （0 h）. The long time glucose-lowering effect of H J07 was bet- ter than native GLP-1 and exendin-4. Furthermore, once daily injection of HJ07 to db/db mice achieved long-term beneficial effects on HbA 1 c lowering and glucose tolerance. CONCLUSION： The biological activity results of H J07 suggest that H J07 is a potential long-acting agent for the treatment of type 2 diabetes.展开更多
基金Supported by the National Natural Science Foundation of China(No. 30 1710 11)
文摘Preliminary tests in rats have shown that the title complex is an efficient insulin mimic, which may be the first example of polyoxomatalates possessing insulin mimetic activity.
基金supported by the NationalNatural Science Foundation of China(Nos.81172932,81273376)Natural Science Foundation of Jiangsu Province(No.BK 2012356)
文摘AIM： To identify the glucose lowering ability and chronic treatment effects of a novel coumarin-glucagon-like peptide-1 （GLP-1） conjugate H J07. METHOD： A receptor activation experiment was performed in HEK 293 cells and the glucose lowering ability was evaluated with hypoglycemic duration and glucose stabilizing tests. Chronic treatment was performed by daily injection of exendin-4, saline, and HJ07. Body weight and HbAlc were measured every week, and an intraperitoneal glucose tolerance test was performed before treatment and after treatment. RESULTS： HJ07 showed well-preserved receptor activation efficacy. The hypoglycemic duration test showed that HJ07 possessed a long-acting, glucose-lowering effect and the glucose stabilizing test showed that the antihyperglycemic activity of H J07 was still evident at a predetermined time （12 h） prior to the glucose challenge （0 h）. The long time glucose-lowering effect of H J07 was bet- ter than native GLP-1 and exendin-4. Furthermore, once daily injection of HJ07 to db/db mice achieved long-term beneficial effects on HbA 1 c lowering and glucose tolerance. CONCLUSION： The biological activity results of H J07 suggest that H J07 is a potential long-acting agent for the treatment of type 2 diabetes.
