Preparation of tellurium contained transparent acid with activity of high glutathione peroxidase

A technology of glutathione peroxide and hyaluronic acid, applied in the field of biochemistry, can solve the problems of large side effects, low drug efficacy, cyclodextrin does not have the effect of targeted drug carrier, etc., and achieves fewer synthesis steps, The product is easy to purify and the effect of high yield

Inactive Publication Date: 2008-06-04
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent 03119443.5 discloses the pharmaceutical use and pharmaceutical composition of cyclodextrin derivatives, but compared with hyaluronic acid, cyclodextrin does not have the role of a targeted drug carrier, and cyclodextrin is synthesized as a substrate containing Selenium compounds are used in clinical treatment, and have the characteristics of large side effects and low drug efficacy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 The synthetic route of tellurium-containing hyaluronic acid:

[0017] (1) Preparation of benzenesulfonyl hyaluronate

[0018] Take 2.0g hyaluronic acid and dissolve it in 80ml NaOH (0.15mol / L) solution, add p-TsCL acetonitrile solution (8.0g / 20ml) dropwise at room temperature, add 1mol / L NaOH continuously during the dropping process to make the solution pH > 12.5 After 3 hours of dropwise addition, stir for 1 hour, adjust to neutral with 1mol / L HCl, add 100ml of methanol, filter off the insoluble matter, evaporate the methanol to 80ml under reduced pressure, put it in a refrigerator at 5°C, and salt will precipitate out after eight days, filter Remove insoluble matter, dialyze in distilled water for 2 days, and set aside.

[0019] (2) Preparation of Sodium Telluride Hydride (NaHTe)

[0020] Add 2.54g of tellurium powder and 1.8g of sodium borohydride to 40ml of absolute ethanol, and gas is generated accompanied by heat release. The system was kept free of o...

Embodiment 2

[0025] Example 2 Determination of Hyaluronic Acid Telluride Activity

[0026] 1. GPX activity of hyaluronic acid telluride

[0027] 500ul bioassay system, containing 50mmol / L potassium phosphate buffer, pH7.0, 1mmol / L sodium azide. 1mmol / L glutathione, 0.25mmol / L coenzyme (NADPH), 1U glutathione reductase, 0.5mmol / L hydrogen peroxide was added to start the reaction, and the absorbance change of NADPH being oxidized was monitored at 340nm. When measuring enzyme activity, distilled water was used instead of tellurium-containing polysaccharide as a blank control. The enzyme activity unit is defined as one micromole of NADPH consumed per micromole of tellurium-containing polysaccharide per minute. Finally, the specific activity of the tellurium-containing polysaccharide obtained under the above conditions was determined to be 174.2 U / umol.

[0028] 2. Antioxidant activity of hyaluronic acid telluride

[0029] The bioassay system is 3ml, take 100ul of the tellurized hyaluronic ...

Embodiment 3

[0030] The influence of embodiment 3 activation conditions on product GPX activity

[0031]According to the technical process of Example 1, the mass ratios of hyaluronic acid and p-toluenesulfonyl chloride are respectively 1:1, 1:2, 1:3, 1:4, and 1:5. The GPX activity of the obtained tellurium-containing hyaluronic acid was measured according to the detection method in Example 2, and the results were 62.5, 91.3, 130.5, 174.2, and 178.3 U / umol. Except for the ratio of 1:1, the results are all greater than the result of 75.2 U / umol in the background technology. Finally, in the activation process, the optimal mass ratio of hyaluronic acid to p-toluenesulfonyl chloride is 1:4, and the product of tellurium-containing hyaluronic acid has the characteristics of high GPX activity and high utilization rate of p-toluenesulfonyl chloride.

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Abstract

Production of transparent acid containing tellurium with high glutathione oxide enzyme activity is artificial enzyme process with GPX activity. It consists of transparent acid activating, tellurium sodium hydride preparing, transparent acid tellurium reacting, tellurium transparent acid oxidizing and after processing. The production is carried out by activating transparent acid with tolylsulfonyl chlorin, preparing transparent acid benzene sulfonyl ester, dialyzing in distilled water, adding tellurium powder and sodium borohydride into anhydrous alcohol, heating and reverse flowing in nitrogen system, adding anaerobic glacial acetic acid, preparing alcohol solution of tellurium sodium hydride preparing, alcohol of tellurium sodium hydride reacting with transparent acid benzene sulfonyl ester solution, obtaining transparent acid containing the, the reacting system expose in air, centrifugal oxidizing, alcohol settling, and washing. It achieves simple process, high output, higher resistance to oxidation and GPX activity.

Description

technical field [0001] The invention belongs to the field of biochemistry, and relates to a method for preparing an artificial enzyme with higher glutathione peroxidase activity, in particular, the invention relates to a chemical preparation method of tellurized hyaluronic acid. Background technique [0002] Hyaluronic acid has a strong water retention effect; it can thicken and stabilize in cosmetics; it can remove active oxygen free radicals in the skin and play a role in sun protection. Therefore, hyaluronic acid has many applications in the field of cosmetics. Hyaluronic acid and its derivatives are also used as carriers in compound preparations composed of basic drugs and various therapeutic drugs, directing and retaining different therapeutic drugs in the pathological parts of the human body, so that the drugs can act on more precise targets, greatly While increasing the curative effect, systemic side effects of the drug are avoided. Anti-cancer targeted drugs with h...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/08
Inventor 陈智博刘兰英冯德日洪水声陈佳初雨卓
Owner JILIN UNIV
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