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Application of castanospermine to preparation of antibacterial drugs

An anti-bacterial and drug technology, applied in anti-bacterial drugs, resistance to vector-borne diseases, pharmaceutical formulations, etc., can solve problems such as irritation, dizziness, allergies, and strong accumulation of antibacterial drugs

Inactive Publication Date: 2016-02-03
ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Antibacterial drugs have been widely used in the treatment of AIDS, organ transplantation and chronic wasting diseases (such as cancer, diabetes, uremia, etc.) , but these antibacterial drugs have strong cumulative toxicity, often causing liver and kidney damage, gastrointestinal irritation, dizziness, allergies, etc., so looking for new antibacterial drugs with unique mechanism of action has become one of the hot spots in drug research and development today

Method used

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  • Application of castanospermine to preparation of antibacterial drugs
  • Application of castanospermine to preparation of antibacterial drugs
  • Application of castanospermine to preparation of antibacterial drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Embodiment 1: the preparation of the compound Castanospermine tablet involved in the present invention:

[0011] Take 5 grams of the compound Castanospermine, add 195 grams of dextrin, mix well, and make 1000 tablets by conventional compression.

Embodiment 2

[0012] Embodiment 2: the preparation of the compound Castanospermine capsules involved in the present invention:

[0013] Take 5 grams of the compound Castanospermine, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.

[0014] The following pharmacodynamic experiments will further illustrate its drug activity.

experiment example 1

[0015] Experimental example 1: Experimental research on the antibacterial activity of Castanospermine

[0016] The antibacterial activity experiment is the method of concentration dilution, and each measurement is repeated three times. The test pathogens include Escherichia coli, Pseudomonas fluorescens, Staphylococcus aureus, Proteus, and Cryptococcus neoformans, and the concentration of the bacteria solution is 10 5 individual / mL. The initial concentration of Castanospermine was 50.0 μg / mL (5% dimethyl sulfoxide DMSO), and it was serially diluted to 0.098 μg / mL. The equal volume of bacterial liquid and test samples were mixed and cultured in a 96-well plate, and the bacterial culture temperatures were respectively 37°C, observe after 24 hours of incubation, if no colonies are found, it is the lowest antibacterial concentration of the sample, that is, the MIC value. The positive control of this experiment was amikacin sulfate, and the antibacterial results of Castanospermine...

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PUM

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Abstract

The invention relates to application of castanospermine to preparation of antibacterial drugs. Castanospermine has strong effects of inhibiting escherichia coli, pseudomonas fluorescens, staphylococcus aureus, proteus vulgaris and cryptococcus neoformans, can serve as an antibacterial compound, is disclosed for the first time, is high in bacteriostasis activity, has an outstanding substantive feature, and obviously makes remarkable progress in preventing and treating bacterial infection.

Description

technical field [0001] The present invention relates to a new application of the compound Castanospermine, in particular to the application of Castanospermine in the preparation of antibacterial drugs. Background technique [0002] Antibacterial drugs have been widely used in the treatment of AIDS, organ transplantation and chronic wasting diseases (such as cancer, diabetes, uremia, etc.) , but these antibacterial drugs have strong cumulative toxicity, often causing liver and kidney damage, gastrointestinal irritation, dizziness, allergies, etc., so looking for new antibacterial drugs with unique mechanism of action has become one of the hot spots in drug research and development today. [0003] The compound Castanospermine involved in the present invention is a new compound published in 2013 (VijayDhand, et al., AShort, Organocatalytic Formal Synthesis of (-)-Swainsonine and Related Alkaloids. Organic Letters, 2013, 15 (8) 1914-1917.), which has a new skeleton type , the c...

Claims

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Application Information

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IPC IPC(8): A61K31/437A61P31/04C07D471/04
CPCY02A50/30
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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