Component for forming bacterium-resisting and efficacy-enhancing inclusion compound together with vancomycin and preparation method and application thereof

A vancomycin, antibacterial and synergistic technology, applied in the direction of non-active components of polymer compounds, glycopeptide components, antibacterial drugs, etc., can solve the problem of decreased sensitivity of vancomycin

Inactive Publication Date: 2012-10-31
SHANGHAI RUICHUANG MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the abuse of antibiotics, clinically, the sensitivity of vancomycin to MRSA has a tendency to decline rapidly.

Method used

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  • Component for forming bacterium-resisting and efficacy-enhancing inclusion compound together with vancomycin and preparation method and application thereof
  • Component for forming bacterium-resisting and efficacy-enhancing inclusion compound together with vancomycin and preparation method and application thereof
  • Component for forming bacterium-resisting and efficacy-enhancing inclusion compound together with vancomycin and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Vancomycin, 6-[(L-phenylalanyl)-amino]-β-cyclodextrin hydrochloride ( 1 ) and its inclusion complex in vitro antibacterial activity test

[0027] Test 6-[(L-phenylalanyl)-amino]-β-cyclodextrin hydrochloride ( 1 ), positive control drug Linezolid, vancomycin, 1:1 molar solubility of vancomycin: 6-[(L-phenylalanyl)-amino]-β-cyclodextrin hydrochloride ( 1 ) antibacterial activity against nine clinically common bacterial strains, the results are shown in figure 1 .

Embodiment 2

[0029]6-[(L-phenylalanyl)-amino]-β-cyclodextrin hydrochloride ( 1 ), vancomycin and clathrates 1 H NMR Spectrum, Chemical Conformation Analysis and Antibacterial Synergistic Mechanism

[0030] 6-[(L-phenylalanyl)-amino]-β-cyclodextrin hydrochloride ( 1 ) and vancomycin were directly prepared with 0.9% normal saline heavy water, the concentration was 0.016 moles, respectively for 1 H NMR determination; compound 1 Prepare with vancomycin at a molar ratio of 1:1 with 0.9% normal saline heavy water, the concentration is 0.016 molar, and carry out one hour after mixing 1 H NMR determination. See the test results figure 2 and 3 . 6-[(L-phenylalanyl)-amino]-β-cyclodextrin hydrochloride ( 1 ) and vancomycin, the chemical conformation analysis of the inclusion complex and its antibacterial synergistic mechanism are shown in Figure 4 , Figure 5 .

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Abstract

The invention aims to provide a component of an inclusion compound capable of increasing the antibacterial activity of vancomycin and a preparation method. The inclusion compound is formed by taking a beta-cyclodextrin derivative, i.e., 6-[(L-phenylalanyl)-amino]-beta-cyclodextrin as a host compound and taking vancomycin as a guest compound. As proved by an in-vitro antibacterial activity experiment of the inclusion compound, vancomycin has the efficacy-enhancing effect of 4-8 times of minimum bacteriostasis solubility on the antibacterial activities of multiple bacterium strains, particularly methicillin resistant staphylococcus aureus (MRSA). The bacterium-resisting and efficacy-enhancing mechanisms of the inclusion compound formed by vancomycin and 6-[(L-phenylalanyl)-amino]-beta-cyclodextrin are explained by performing a 1HNMR (1h Nuclear Magnetic Resonance) experiment, analyzing the chemical structural conformation of the inclusion compound and combining the original biochemical acting mechanism of the antibacterial activity of vancomycin. The inclusion compound for increasing the antibacterial activity of vancomycin can be applied to antibacterial treatment of pathogenic bacteria which are insensitive to vancomycin or have low antibacterial activities. The component can be developed into a novel vancomycin synergistic agent for constituting a novel medicament together with vancomycin.

Description

[0001] technical field [0002] The present invention relates to vancomycin vancomycin and β-cyclodextrin derivative 6-[(L-phenylalanyl)-amino]-β-cyclodextrin Per-6-[(phenylalanyl)-amino]-b- The preparation method of inclusion compound formed by cyclodextrin hydrochloride, chemical conformation analysis, antibacterial synergistic effect and synergistic mechanism, and the application of this vancomycin inclusion complex antibacterial synergistic effect. Background technique [0003] Vancomycin is currently the clinical treatment for methicillin-resistant staphylococcus aureus (methicillin-resistant Staphylococcu saureus , referred to as MRSA), which belongs to the glycopeptide antibiotics with a relatively complex structure. The antibacterial mechanism of vancomycin has been confirmed to form hydrogen bonds and combine with the five sites of L-Lys-D-Ala-D-Ala on the C-terminal of the bacterial cell wall NAM / NAG peptides, thereby inhibiting bacteria The synthesis of the cell...

Claims

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Application Information

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IPC IPC(8): A61K38/14A61K47/40A61K9/19A61P31/04
Inventor 邓京振
Owner SHANGHAI RUICHUANG MEDICAL TECH
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