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Method for inhibiting protein intron activity and application thereof in medicine preparation

A protein intron, active technology, applied in the direction of organic active ingredients, antibacterial drugs, pharmaceutical formulations, etc., to achieve the effect of simplifying clinical trial work

Inactive Publication Date: 2010-01-06
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on the inhibitory effect of platinum compounds on Intein

Method used

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  • Method for inhibiting protein intron activity and application thereof in medicine preparation
  • Method for inhibiting protein intron activity and application thereof in medicine preparation
  • Method for inhibiting protein intron activity and application thereof in medicine preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The fusion protein of RecA Intein and green fluorescent protein GFP in Mycobacterium tuberculosis was expressed by Escherichia coli. Due to the insertion of RecA Intein, the luminescent effect of the green fluorescent protein GFP is completely eliminated. If RecA Intein can exert its protein splicing function and connect the two ends of the GFP protein, the luminescence of the fluorescent protein is restored. The presence of intein activity inhibitors will suppress fluorescence. Thus, the change in fluorescence intensity can be used to detect the efficiency of the intein activity inhibitor.

[0038] We dissolve the fusion protein from the inclusion body with complex buffer (8M urea, 0.5M sodium chloride, 20mM sodium phosphate, pH=7.5), then adsorb the fusion protein through a metal affinity column and elute other foreign proteins to remove it. The phosphate buffer containing 0.5M sodium chloride was used for step-by-step gradient elution. After the urea was completely...

Embodiment 2

[0044] The specific experimental method and principle are the same as in Example 1, and the inhibitory effect of the platinum complex diaminocyclobutane dihydroxy acid platinum is detected, and its IC 50 About 30μM. The structural formula of platinum dihydrocyclobutane dihydroxy acid is:

[0045]

Embodiment 3

[0047] Concrete experimental method and principle are with embodiment 1, detect the platinum compound chloride monochlorine diamine imidazolium platinum ([cis-Pt(NH 3 ) 2 (im)Cl]Cl) inhibition, its IC 50 About 77μM. The structural formula of chlorine chloride diamine imidazolium platinum is:

[0048]

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PUM

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Abstract

The invention provides a method for inhibiting protein intron activity, which is characterized by comprising the steps: acting a platinum composition on a microorganism with protein intron; inhibiting an internal protein cutting function of the microorganism by directly inhibiting the protein intron activity; thereby inhibiting the maturation and the function of the corresponding protein. The method for inhibiting protein intron activity has low use concentration of an inhibitor and wide application and is not easy to generate drug resistance. In masses of diseases which are related to microorganisms, the method for inhibiting protein intron activity has good application prospect on a tubercle bacillus resisting aspect particularly. The invention also provides the application of a platinum composition for preparing medicines which are used for treating diseases related to the protein intron activity, in particular to the application for preparing tuberculosis treating medicines.

Description

technical field [0001] The invention relates to a method for inhibiting protein intron activity and its application, in particular to a method for using a platinum complex to inhibit protein intron activity and its application in pharmacy. Background technique [0002] Intein is a class of enzymes discovered in 1990, and introns exist in the three major biological systems (eukaryotes, eubacteria, and archaea). And the nuclei and organelles of eukaryotes are distributed, indicating the extensive distribution of introns. At present, the protein splicing function of Intein has been widely used in protein engineering. Studies have shown that the biological activity of Intein is the same as that caused by bacteria such as tuberculosis (Mycobacterium tuberculosis), leprosy (Bacillus leprae), and infections caused by bacteria such as Mycobacterium avium, Mycobacterium laevis, and Cryptococcus neoformans, and Aspergillus fumigatus, constitutive Asthma or infectious diseases caused...

Claims

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Application Information

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IPC IPC(8): A61K33/24A61K31/282A61K31/194A61K31/555A61K31/4164A61K31/4745A61K31/44A61P31/04A61P31/10A61P31/06
Inventor 刘扬中张立云罗昭锋
Owner UNIV OF SCI & TECH OF CHINA
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