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Use of bromphenol compound in protein-tyrosine phosphonatease inhibitor

A tyrosine phosphatase and compound technology, applied in the field of bromophenol compounds, can solve problems such as few research reports on the chemical composition of seaweed, and achieve the effect of treating and preventing diabetes and obesity

Inactive Publication Date: 2006-11-01
INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the 1960s, people systematically studied the bromophenol compounds in the same seaweed Rhodomela larix, and in the following 20 years, there were few research reports on the chemical constituents of this genus seaweed

Method used

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  • Use of bromphenol compound in protein-tyrosine phosphonatease inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the extraction of bromophenol compound

[0023] Get 15 kg of pine knotweed after air-drying, soak and extract 3 times with 95% ethanol at room temperature, each time for 72 hours; Ethyl acetate extraction. Ethyl acetate extracts were subjected to silica gel column chromatography, first with petroleum ether-acetone (100:0~1:1) and chloroform-methanol (100:0~0~100) gradient elution, and thin layer chromatography to check the same fraction . Chloroform:methanol 5:1 eluted fraction, chloroform:methanol 3:1 eluted fraction, petroleum ether:acetone 2:1 eluted fraction, petroleum ether:acetone 1:1 eluted fraction were subjected to repeated silica gel column chromatography to obtain the compound I (1082 mg), II (1171 mg), III (2644 mg), IV (776 mg).

Embodiment 2

[0024] Embodiment 2: Bromophenol compounds inhibit protein tyrosine phosphatase activity test in vitro:

[0025] PTP1B: GST fusion protein expressed and purified in Escherichia coli;

[0026] Substrate: PNPP

[0027] Positive reference substance: sodium orthovanadate (2μM)

[0028] Test principle: The product obtained by hydrolyzing the phospholipid of the substrate PNPP by PTP1B has a strong light absorption at 410nm, so the change of absorption at 410nm can be directly detected to observe the change of enzyme activity and the inhibitory effect of the compound on it.

[0029] Test method: Take the above-mentioned 4 kinds of bromophenol compounds, and prepare 2 solutions of 200 μM and 20 μM of test products with phosphate buffer solution respectively.

[0030] Sample serial number

[0031] The test results show that the sample is significantly higher than the traditional protein tyrosine phosphatase inhibitor orthovanadate in inhibiting the activity of protein tyros...

Embodiment 3

[0032] Example 3 In vivo hypoglycemic test of the total bromophenol compounds of Pinus chinensis

[0033] Animals: 40 Kunming white mice.

[0034] Model: mouse diabetes model induced by streptozotocin

[0035] The specific operation is as follows:

[0036] Take 40 Kunming mice weighing 20-24g, and divide them into normal control group, test product 1 (4.0 g / kg), test product 2 (2.0 g / kg) group. The normal control group was intraperitoneally injected with normal saline, and the rest of the groups were intraperitoneally injected with streptozotocin (130 mg / kg). After 48 hours, blood was collected from the orbital vein of the mice, and the serum was separated to measure the serum glucose level. Then the administration group was intragastrically administered once a day, and the normal control group and the model group were given equal volumes of distilled water for 10 consecutive days. After fasting for 16 hours on the 11th day, blood was collected from the orbital venous plexu...

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Abstract

An application of the bromophenol compounds chosen from bis-(2,3-bibromo-4,5- dihydroxybenzyl)-ether, 2,2',3,3'-tetrabromo-4,4',5,5'-tetrahydroxydiphenyl methane, 2,2',3- tribromo-3',4,4',5-tetrahydroxy-6'-ethoxymethyl diphenylmethane, 3-bromo-4,5-bis-(2,3-dibromo -4,5-dihydroxybenzyl)-catechol, their pharmacologically acceptable derivatives, and their mixture in preparing the depressant of protein tyrosine phosphatase for treating diabetes and obesity is disclosed.

Description

technical field [0001] The present invention relates to a bromophenol compound (and their pharmaceutically acceptable salts, esters, ethers and other obvious chemical equivalents) used as protein tyrosine phosphatase inhibitor, and its preparation and application. These compounds and their derivatives are inhibitors of protein tyrosine phosphatase and can be used for treating and preventing diabetes and obesity. Background technique [0002] Protein tyrosine phosphorylation is an important way of protein post-translational modification, and cells can regulate signal transduction through protein tyrosine phosphorylation. Tyrosine phosphorylation is a reversible dynamic process regulated by a pair of opposing enzymes, protein tyrosine kinase (PTK) and protein tyrosine kinase (PTP). PTK, PTP and their corresponding substrates together form a signaling network to regulate cell growth, differentiation, metabolism, cell cycle, intercellular communication, cell migration, gene tra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/055A61K9/02A61K9/08A61K9/10A61K9/20A61K9/48A61P3/04A61P3/10
Inventor 范晓马成俊韩丽君史大永柳全文
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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