Use of 2,4-thiazolidinedione compound K145 in preparation of diabetes treatment drug

A technology for thiazolidinediones and diabetes drugs, applied in the field of pharmaceutical preparations, can solve problems such as unreported effects, and achieve the effects of lowering fasting blood sugar, good hypoglycemic effect, and enhanced glucose output capacity of liver tissue

Inactive Publication Date: 2018-12-18
天津医科大学代谢病医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a thiazolidinedione analogue, K145 has been found to have obvious anticancer effects, but its role in the treatment of diabetes has not been reported

Method used

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  • Use of 2,4-thiazolidinedione compound K145 in preparation of diabetes treatment drug
  • Use of 2,4-thiazolidinedione compound K145 in preparation of diabetes treatment drug
  • Use of 2,4-thiazolidinedione compound K145 in preparation of diabetes treatment drug

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] 2,4-thiazolidinedione compound K145 is added with pharmaceutically acceptable excipients to prepare various dosage forms according to conventional methods, such as liquid injections of various specifications, powder injections, emulsions for injection, tablets, pills, capsules, Ointments, creams, patches, liniments, powders, sprays, implants, drops, suppositories, ointments, confectionery, etc.

[0015] The route of administration includes various routes of administration: oral administration, injection administration, implant administration, intracavity administration, sublingual administration, anal administration, transdermal administration, internal and external application, etc.

[0016] In order to prove the technical means, purpose and experimental effect of the experimental invention, the following will further illustrate the present invention with specific experimental examples.

experiment example 1

[0017] Experimental example 1: The effect of the target compound of the present invention on ob / ob diabetic mice

[0018] Animal group processing and detection indicators: 6-7 weeks old diabetic ob / ob mice, male, weighing 35-40g (provided by Nanjing Institute of Biomedicine, Nanjing University), free drinking and eating, randomly divided into DMSO intervention control group and K145 The intervention model was given by intraperitoneal injection for 17 days, once a day, with a dose of 15 mg / kg. Insulin tolerance analysis (ITT) was performed by intraperitoneal injection of 0.75IU / kg body weight of insulin; overnight starvation, intraperitoneal injection of 2g / kg body weight of aD-glucose, tail vein blood test (IPGTT); mice fasted overnight, tail removed Venous blood was used to measure fasting blood glucose and fasting insulin (RIA, Millipore, USA); according to the formula HOMA-IR = fasting blood glucose (mg / dl) X fasting insulin (mU / ml) / 405, calculate the HOMA-IR value.

[0019] Th...

experiment example 2

[0020] Experimental Example 2: Effect of the target compound of the present invention on db / db diabetic mice

[0021] Animal group processing and detection indicators: 6-7 weeks old diabetic db / db mice, male, weight 34-37g (provided by Nanjing Institute of Biomedicine, Nanjing University), free drinking and eating, randomly divided into DMSO intervention control group and K145 In the intervention model, the drug dissolution method is as follows: after 2% DMSO is dissolved, it is prepared into a suspension with hydroxymethyl cellulose, which is given by intragastric administration for 30 days, once a day, at a dosage of 30 mg / kg. Insulin tolerance analysis (ITT) was performed by intraperitoneal injection of 0.75IU / kg body weight of insulin; overnight starvation, intraperitoneal injection of 2g / kg body weight of aD-glucose, tail vein blood test (IPGTT); mice fasted overnight, tail removed Fasting blood glucose was measured by venous blood, and fasting insulin (RIA, Millipore, USA) ...

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Abstract

The invention discloses a use of a 2,4-thiazolidinedione compound K145 in the preparation of a diabetes treatment drug. Diabetic ob / ob and db / db mice are intervened with the K145 by intraperitoneal injection and intragastric administration, a result of detection shows that the fasting blood-glucose values of two groups of the diabetic mice are significantly reduced, the insulin resistance of peripheral tissues is enhanced, the glucose output capability of liver tissues is enhanced, the expression of hepatic gluconeogenesis-related genes PEPCK and G6Pase is reduced, and after the K145 is addedto hepatocytes, the phosphorylation level of a hepatocyte insulin signaling molecule Akt rises, and the expression of the hepatic gluconeogenesis-related genes is reduced. A result of blood glucose lowering experiments of experimental animals shows that the compound has a good blood sugar lowering effect on the diabetic mice.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and particularly relates to the use of 2,4-thiazolidinedione analogues in the preparation of medicines for treating diabetes. Background technique [0002] With the continuous improvement of living standards, the incidence of human diabetes is increasing year by year. Diabetes has become the third killer threatening human health after cardiovascular diseases and cancer. The International World Health Organization reported in 2017 that the number of diabetes patients increased from 108 million in 1980 to 422 million in 2014, and the global prevalence of diabetes among adults over 18 years of age increased from 4.7% in 1980 to 8.5% in 2014. Middle income The prevalence of diabetes is rising faster in low-income countries, and diabetes is the main cause of blindness, kidney failure, heart disease, stroke, and lower limb amputation. In 2015, nearly 1.6 million people died of diabetes and 2.2 mi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/426A61P3/10
CPCA61K31/426A61P3/10
Inventor 袁继红史亚男穆标闫丽辉乔家运
Owner 天津医科大学代谢病医院
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