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Applications of sesquiterpene lactone compound and derivative of sesquiterpene lactone compound in treatment of diabetes

A technology for diabetes and compounds, which is used in medical preparations containing active ingredients, metabolic diseases, drug combinations, etc.

Inactive Publication Date: 2014-03-12
龙海波
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is no report about the application of the compound of formula (I) or its pharmaceutical composition in the prevention, treatment or auxiliary treatment of diabetes, diabetic chronic complications and its application in the preparation of drugs for the prevention, treatment or auxiliary treatment of diabetes and diabetic chronic complications

Method used

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  • Applications of sesquiterpene lactone compound and derivative of sesquiterpene lactone compound in treatment of diabetes
  • Applications of sesquiterpene lactone compound and derivative of sesquiterpene lactone compound in treatment of diabetes
  • Applications of sesquiterpene lactone compound and derivative of sesquiterpene lactone compound in treatment of diabetes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the preparation method of compound 1-50

[0027] Preparation of Compound 1:

[0028] Parthenolide (50 mg, 0.2 mmol) was dissolved in 2.5 mL of dichloromethane, and p-toluenesulfonic acid (5 mg, 0.026 mmol) was added. The reaction system was left at room temperature and stirred overnight. Transfer the reaction solution to NaHCO 3 (10mL) in a saturated solution, collect the organic phase, extract the aqueous phase with a small amount of dichloromethane, combine the organic phases, and wash with Na 2 SO 4 After drying and filtering, the organic solvent was distilled under reduced pressure with a rotary evaporator, and purified on a silica gel column to obtain compound 1 (45 mg, yield 90%). 1 H NMR (CDCl3 , 400MHz) δ6.20(d, J=3.2Hz, 1H) 5.49(d, J=3.2Hz, 1H) 3.81(t, J=10.4Hz, 1H), 2.70(d, J=10.4Hz, 1H) , 2.65-2.62(m, 2H), 2.40-2.34(m, 1H), 2.07-2.26(m, 4H), 1.73-1.86(m, 2H), 1.68(s, 3H), 1.36-1.28(m, 4H); 13 C NMR (CDCl 3 , 100MHz) δ169.8, 138.7, 131.7,...

Embodiment 2

[0158] Example 2: Anti-diabetes and diabetes chronic complications activity test of compound 1-50

[0159] Chronic complications of diabetes are the main cause of disability and death in DM. Its pathogenesis involves polyol bypass, protein kinase C, hexosamine activation, and production of advanced glycation end products. In recent years, it has been found that hyperglycemia-induced mitochondrial response Increased production of sexual oxidation products is a possible common basis. Activation of reduced nicotinamide adenine dinucleotide oxidase is increasingly recognized as the central link in high glucose-induced oxidative stress. High glucose leads to protein uncoupling by causing Overexpression of mitochondrial peroxides causes oxidative stress and ultimately DNA damage. At the same time, from in vitro model tests and pathological examinations to epidemiological studies, many evidences have shown that inflammation is also one of the main pathogenesis of chronic complication...

Embodiment 3

[0172] Embodiment 3: injection

[0173] Compound 1-50 prepared in Example 1 was dissolved in a small amount of DMSO, added water for injection as usual, finely filtered, potted and sterilized to make an injection.

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Abstract

The invention relates to applications of a sesquiterpene lactone compound and a derivative of the sesquiterpene lactone compound in treatment of diabetes, belongs to the technical field of medicine, and specifically relates to applications of a compound represented by formula (I) in prevention, therapy or adjuvant therapy of diabetes and diabetic chronic complications, and in preparation of medicines used for prevention, therapy or adjuvant therapy of the diabetes and diabetic chronic complications.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular, it relates to the application of sesquiterpene lactone compounds and their derivatives in the prevention, treatment or auxiliary treatment of diabetes and chronic complications of diabetes, and the use of them as active ingredients or pharmaceutical compositions Application in preparation of medicines for preventing, treating or assisting treating diabetes and chronic complications of diabetes. Background technique [0002] With the improvement of living standards, population aging, and changes in lifestyle, the prevalence of diabetes mellitus (DM) has increased rapidly, and it has become the third largest non-communicable disease in developed countries after cardiovascular disease and tumors. The incidence of DM in my country is also increasing year by year. According to statistics, the total number of DM patients nationwide in 2001 was about 30 million; in 2008, a survey organi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/366A61K31/4192A61K31/655A61K31/4025A61K31/4525A61K31/496A61K31/5377A61P3/10A61P29/00
Inventor 龙海波
Owner 龙海波
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