Application of fenticonazole nitrate to preparation of anti-diabetic drug
A technology for fenticonazole nitrate and diabetes drug, applied in the field of medicine, can solve the problems of cardiomegaly, obesity, hinder the application of thiazolidinediones, etc., and achieve the effect of low toxicity and side effects
Active Publication Date: 2021-08-06
GUANGZHOU MEDICAL UNIV
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Problems solved by technology
Long-term use of thiazolidinediones can lead to side effects such as obesity, weight gain, edema, bladder cancer, enlarged heart, and heart failure
These side effects have seriously hindered the clinical application of thiazolidinediones
Method used
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Embodiment 1
[0023] 1. Detecting the ability of fenticonazole nitrate to activate PPARγ (luciferase activity assay)
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Abstract
The invention discloses an application of fenticonazole nitrate to preparation of an anti-diabetic drug. Under the action of the concentration of 10 [mu] M, the fenticonazole nitrate has relatively strong affinity with PPAR gamma. Experiments show that compared with rosiglitazone, the fenticonazole nitrate has a relatively weak capability of inducing adipocyte differentiation, and the fenticonazole nitrate weakly activates expression of a PPAR gamma downstream adipogenic gene. In a db / db model mouse, the fenticonazole nitrate does not cause increase of the weight of the mouse and does not generate obvious side effects on all internal organs of the mouse. Besides, under the concentration of 10mg / kg, a very good hypoglycemic effect is also achieved. It is found for the first time that the fenticonazole nitrate has an efficient hypoglycemic effect, has low toxic and side effects, and can be developed as an anti-diabetic drug.
Description
technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of fenticonazole nitrate in the preparation of antidiabetic drugs. Background technique [0002] Diabetes mellitus is a common metabolic disease that is increasing at an alarming rate in the world's population, characterized by hyperglycemia and its associated symptoms caused by insufficient insulin secretion, insufficient insulin action, or both. Non-insulin-dependent type 2 diabetes accounts for more than 90% of all diabetic patients. In patients with type 2 diabetes, hyperglycemia is caused by insulin resistance in the liver and peripheral tissues. Diabetic patients need more insulin to maintain the physiological balance of glucose metabolism in the body, which can be achieved by increasing insulin secretion from islets (endogenous production) or directly Injection of recombinant peptides to lower blood sugar levels. However, both processes lead ...
Claims
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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4174A61P3/10
CPCA61K31/4174A61P3/10
Inventor 易伟马磊周志侯宁唐君源
Owner GUANGZHOU MEDICAL UNIV
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