PEGlyated Chinese trichosannthes root protein medicine and its preparation

A trichosanthin protein and PEGylation technology, which is applied in the direction of drug combination, pharmaceutical formula, peptide/protein composition, etc., can solve the problems of singleness and poor uniformity of modified products, inability to obtain clinical application products, difficult separation and purification, etc., to achieve Low anti-HIV activity and anti-tumor activity, easy industrial production, easy purification and separation

Inactive Publication Date: 2007-07-04
ANHUI ANKE BIOTECHNOLOGY (GRP) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The patent No. PCT / US94 / 01618 (Ribosome inactivating protein compositions having reduced antigenicity) discloses a method for modifying TCS using mPEG-SC with a molecular weight of 5000. Separation and purification, and the yield is very low, the stability is poor, and it is impossible to obtain products that meet clinical applications

Method used

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  • PEGlyated Chinese trichosannthes root protein medicine and its preparation
  • PEGlyated Chinese trichosannthes root protein medicine and its preparation
  • PEGlyated Chinese trichosannthes root protein medicine and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0026] The trichosanthin protein used in each embodiment is obtained from the root of the natural plant Trichosanthes chinensis, the purity is greater than 99%, and it maintains high biological activity. The molecular weight of mPEG-ALD is 20000Da. Dissolve TCS in pH 6.0, 100mmol / L phosphate buffer, add mPEC-ALD in the weight ratio shown in the table below, after dissolving, add Na CNBH 3 , so that the final concentration was 10 mM, and reacted at room temperature at 20° C. for 24 hours.

[0027]

serial number

mPEG-ALD / TCS (w / w)

Yield of target product PEG-TCS

(%)

Example 1

0.4

Difference

Example 2

0.5

poor

Example 3

1.0

Can

Example 4

4.0

it is good

Example 5

6.0

it is good

Example 6

7.0

most

Example 7

8.0

most

Example 8

10.0

it is good

Example 9

13.0

better

Example 10 ...

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PUM

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Abstract

The invention provides a polyethylene glycol and Chinese trichosannthes root protein medicine and its preparation, wherein the medicine is bonded by polyethylene glycol and N ends of Chinese trichosannthes root through amine bonds, the preparing process comprises subjecting the polyethylene glycol and Chinese trichosannthes root to deoxidized alkylation, the weight ratio (W / W) being in the range of 0.5-20, the pH of the cushion architecture between 3-8, the reaction temperature between 4-37 deg. C, the reaction time being 4-48 hours. The prepared product has good unitarity and homogeneity.

Description

technical field [0001] The technical solution to be protected by the present invention belongs to the technical field of pegylated trichosanthin medicine and its production process. Background technique [0002] Trichosanthin (TCS) is a protein extracted from the tuber root of Trichosanthes kirilowii Maxim. It has a variety of biological and pharmaceutical functions, and is clinically used in the treatment of induction of labor and ectopic pregnancy, hydatidiform mole and choriocarcinoma. In 1989, American scholar McGrath et al. found that TCS, a traditional traditional Chinese medicine for labor induction in my country, could not only inhibit the replication of HIV in T lymphocytes in vitro, but also inhibit the replication of HIV in monocytes / macrophages. Phase I and Phase II clinical trials conducted in the United States in the early 1990s proved that TCS from China can not only effectively inhibit the replication of HIV in T lymphocytes, but also inhibit the replication...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/16A61P15/00
Inventor 宋礼华戎隆富王荣海
Owner ANHUI ANKE BIOTECHNOLOGY (GRP) CO LTD
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