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Application of bromine phenolic compound in preparing medicament for treating type 2 diabetes or adiposis

A type 2 diabetes mellitus and compound technology, which is applied in the application field of preparing medicines for treating type 2 diabetes mellitus or obesity, can solve the problems such as no research report on bromophenol compounds, increase skeletal muscle uptake, and few researches, etc., and achieve curative effect. Significant, high bioavailability, high bioavailability effect

Inactive Publication Date: 2009-01-14
INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Studies have found that the expression of PTP1B and LARPTP in the insulin target tissues of patients with insulin resistance is increased, and the increased expression of these two PTPs can block the activation of insulin receptor tyrosine and the signal transduction of insulin; PTP1B gene knockout mice can improve insulin secretion. Sensitivity, and this sensitization effect is tissue-specific, it can increase the uptake of glucose by skeletal muscle, but has no significant effect on adipose tissue, these results confirm the negative regulation of PTP1B in insulin signal transduction, its activity Increased, may be a pathogenic factor of insulin resistance and impaired insulin receptor signaling, therefore, the search for small molecule inhibitors of PTP1B may lead to the development of effective new drugs against type 2 diabetes and obesity
[0006] There are not many studies on PTP1B inhibitors in the world, mainly including the following categories: antisense oligonucleotide compounds, difluro-methylenePhosPhaonates, methoxybenzoic acid (2-carbometh -oxybenzoic acids), oxalyaminobenzoic acids, benzbromarone, ABDF (the fluorogenic reagent4-(aminosulfonyl)-7-fluoro-2,1,3-benzoxa-diazole); but There is no research report on bromophenol compounds as PTP1B inhibitors in anti-diabetes

Method used

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  • Application of bromine phenolic compound in preparing medicament for treating type 2 diabetes or adiposis
  • Application of bromine phenolic compound in preparing medicament for treating type 2 diabetes or adiposis
  • Application of bromine phenolic compound in preparing medicament for treating type 2 diabetes or adiposis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Extraction, separation and structural identification of embodiment 1 bromophenol compound

[0026] Air-dried Rhodomela confervoides sample 14.4kg (dry weight) was pulverized and extracted three times with 10L 95% ethanol, each time for 72 hours; the combined extracts were 723g of ethanol extract concentrated under reduced pressure at 40°C, the concentrate Suspended with 10 times the weight of distilled water, extracted with ethyl acetate (volume ratio 1:1), and concentrated under reduced pressure to obtain 594.6 g of ethyl acetate phase extract. The ethyl acetate extraction part was subjected to silica gel column chromatography, and petroleum ether-acetone Gradient elution (volume ratio from 500:1 to 1:1), chloroform-methanol gradient elution (volume ratio from 20:1 to 1:1), and finally elution with 95% ethanol, thin layer chromatography check, The eluents with similar components were combined and concentrated under reduced pressure to obtain 14 fractions L 1 ~ L 14 ....

Embodiment 2

[0034] Example 2 Protein tyrosine phosphatase (PTP1B) activity inhibitory activity test

[0035] Experimental principle:

[0036] PTP1B is the first identified protein tyrosine phosphatase (protein tyrosine phosphatase). Through gene knockout experiments, it has been shown that PTP1B plays a negative regulatory role in insulin signaling and leptin signaling, and plays a role in regulating insulin sensitivity. and play a key role in glucose metabolism.

[0037] The catalytic activity domain of human protein tyrosine phospholipase 1B (hPTP1B) was expressed in Escherichia coli by means of molecular biology. The purified hPTP1B recombinant protein can hydrolyze the phospholipid bond of the substrate pNPP, and the obtained product has a strong wavelength at 410nm. Strong light absorption, therefore, the change of light absorption at 410nm can be directly detected to observe the change of enzyme activity and the inhibition of the compound to the enzyme activity, and calculate the i...

Embodiment 3

[0043] Example 3 In vivo anti-diabetic activity test of turpentine ethanol extract

[0044] (1), animal grouping and treatment

[0045] The high-fat diet STZ-DM model (streptozotocin-induced type 2 diabetes rat model) was used to conduct in vivo anti-diabetic activity tests on the ethanol extracts of Sarcodon sp. In vivo hypoglycemic activity of extracts.

[0046] 1, type 2 diabetes model preparation

[0047] 70 Wistar rats were reared for 3 days after environmental adaptation, and 10 rats (half male and half male) were randomly selected as the normal control group. After fasting for 24 h, the remaining rats were given a one-time intraperitoneal injection of streptozotocin (dissolved) at 35 mg / kg. In 0.1mol / L sodium citrate solution, pH=4.5), induce diabetes model. After 3 days of fasting for 12 hours, blood was collected from the tail vein, and the fasting blood glucose was measured by a blood glucose meter. If the blood glucose was greater than 16.7mmol / L, it was determin...

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PUM

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Abstract

The invention relates to a medicine for treating type 2 diabetes and obesity, in particular to an application of three bromophenol compounds to the preparation of the medicine for treating type 2 diabetes and obesity. The bromophenol compounds of the invention have inhibitory activity against protein tyrosine phosphatase (PTP1B), and can be used for treating the type 2 diabetes and the obesity.

Description

technical field [0001] The invention relates to a medicine for treating type 2 diabetes and obesity, in particular to the application of bromophenol compounds in the preparation of medicines for treating type 2 diabetes or obesity, including the preparation, pharmacological activity and pharmaceutical use of three marine bromophenol compounds. The compound acts as a protein tyrosine phosphatase (PTP1B) inhibitor and can be used for treating type 2 diabetes and obesity. Background technique [0002] Diabetes mellitus is a common multiple endocrine disease. Its pathogenesis is due to relative or absolute insulin deficiency and decreased sensitivity of target cells to insulin. It can be divided into insulin-dependent diabetes (type 1) and non-insulin-dependent diabetes (type 2). More than 90% of clinical patients with type 2 diabetes. [0003] Insulin resistance is a key factor in the pathogenesis of type 2 diabetes. Insulin binds to the extracellular α subunit of the receptor...

Claims

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Application Information

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IPC IPC(8): A61K31/09A61K31/343A61P3/04A61P3/10C07C43/178C07C41/38C07D307/87
Inventor 史大永韩丽君范晓许凤袁兆慧
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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