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Application of leonurine to preparation of medicament for treating 2-type diabetes

A technology for type 2 diabetes and leonurine, which is used in drug combinations, antipyretics, metabolic diseases, etc.

Inactive Publication Date: 2012-07-18
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Leonurine is one of the main alkaloids in the traditional Chinese medicine Leonurus, so far there is no report on the therapeutic effect of Leonurine on type 2 diabetes

Method used

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  • Application of leonurine to preparation of medicament for treating 2-type diabetes
  • Application of leonurine to preparation of medicament for treating 2-type diabetes
  • Application of leonurine to preparation of medicament for treating 2-type diabetes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Blood glucose monitoring, oral glucose tolerance test

[0019] (1) Experimental animals

[0020] 42 male C57BLKS / J db / db mice and 5 C57BLKS / J db / m mice (db / m mice were used as normal controls) were kept in their SPF grade animal room. The light alternated between light and dark every 12 hours, and they had free access to food and water. During the feeding and experiment process, the relevant guidelines for the management and protection of experimental animals were followed. The experimental animals used in this experiment were purchased from Shanghai Ruizhi Chemical Research Co., Ltd. The db / db mouse is a typical animal model of spontaneous type 2 diabetes. Its pathogenesis is caused by mutations in leptin receptors, and it is autosomal recessive. It has the characteristics of metabolic disorders similar to human type 2 diabetes: hyperglycemia, hyperinsulinemia, polyuria, diabetes and obesity.

[0021] (2) Experimental grouping and processing

[002...

Embodiment 2

[0027] Example 2 Detection of plasma indicators

[0028] Experimental animals and experimental grouping and treatment are the same as in Example 1.

[0029] Blood samples were collected in test tubes containing heparin, and centrifuged at 3000g for 15 minutes at 4°C; plasma insulin content was detected by ELISA; plasma triglyceride, total cholesterol, high-density lipoprotein and low-density lipoprotein were detected by Hitachi 7080 automatic biochemical analyzer Density lipoprotein and liver function indicators aspartate aminotransferase and alanine aminotransferase.

[0030] The results of plasma index detection showed that the plasma insulin content of the motherwortine (SCM-198) 100mg / kg, 200mg / kg treatment group was significantly improved compared with the db / db vehicle group; the motherwortine (SCM-198) 200mg / kg treatment Compared with the db / db vehicle group, the triglycerides in the group were significantly lower, while the high-density lipoprotein was significantly...

Embodiment 3

[0034] Example 3 Leonurine ( SCM-198) Effect on the expression of glucokinase (GK) gene, glucose-6-phosphatase (G6pase) and phosphoenolpyruvate carboxylase (PEPCK) gene

[0035] Experimental animals and experimental grouping and treatment are the same as in Example 1.

[0036] Glucokinase (GK) is the first rate-limiting enzyme in the glycolysis process, and the increase in its expression will promote the utilization of glucose and play a role in lowering blood sugar. Glucose-6-phosphatase (G6pase) and phosphoenolpyruvate carboxylase (PEPCK) are two key rate-limiting enzymes in the process of gluconeogenesis, and their increased expression will increase the process of gluconeogenesis and the production of glycogen. break down, and the result is an increase in blood sugar. In this example, the effect of motherwortine (SCM-198) on the expression of glucokinase (GK) gene, glucose-6-phosphatase (G6pase) and phosphoenolpyruvate carboxylase (PEPCK) gene was detected according t...

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Abstract

The invention belongs to the field of traditional Chinese medicine manufacturing, and relates to application of leonurine to preparation of a medicament for treating 2-type diabetes. Animal experiments prove that the fasting blood glucose of a 2-type diabetes mouse, i.e., a db / db mouse, can be lowered by the leonurine, and the tolerance of oral glucose is improved; and meanwhile, fasting plasma insulin is increased, the plasma triglyceride is reduced and the content of the plasma high-density lipoprotein is increased. Experiment results also show that the expression of liver glucose metabolic enzymes such as glucokinase, glucose-6-phosphatase and phosphoenolpyruvate carboxyl enzyme is adjusted by the leonurine in an Akt dependent mode; and the biological response of an inflammatory mediator, such as generation of TNF (Tumor Necrosis Factor)-alpha, degradation of IkB-alpha and subsequent phosphorylation of NF-kBp65, is suppressed. Through the leonurine, the inflammatory state of the 2-type diabetes can be corrected, and the symptoms of the 2-type diabetes can be improved; and the leonurine can be used as a treatment medicament to be applied to the treatment of the 2-type diabetes.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a new application of leonurine (SCM-198) in pharmacy, in particular to the application of leonurine (SCM-198) in the preparation of drugs for treating type 2 diabetes. Background technique [0002] The prior art discloses that diabetes has become a disease that seriously threatens human health. In recent years, with the transformation of human life style, its incidence is rising rapidly at an alarming rate. According to the estimates of the International Diabetes Federation (IDF), the number of adults with diabetes in the world reached 285 million in 2010, and more than 90% of them were type 2 diabetes patients. Currently, the clinically used drugs for the treatment of type 2 diabetes mainly include sulfonylureas, glinides, biguanides, thiazolidinones and α-glucosidase inhibitors. However, the above-mentioned hypoglycemic drugs have been reported to have side effects. Therefore, it is im...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/235A61P3/10A61P29/00A61P3/06
Inventor 朱依谆黄慧辛宏
Owner FUDAN UNIV
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