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Application of spiroketal polyacetylene compounds in preparing sensitizing medicines for resisting efflux pump resistant staphylococcus aureus

A polyalkyne and spiroketal technology, applied in the field of pharmacy, can solve the problems of severe drug resistance of bacteria and limit the clinical application of oxacillin

Active Publication Date: 2018-04-24
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is precisely because of the wide application of oxacillin in clinical and animal husbandry that bacteria have developed serious drug resistance, thus limiting the clinical application of oxacillin

Method used

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  • Application of spiroketal polyacetylene compounds in preparing sensitizing medicines for resisting efflux pump resistant staphylococcus aureus
  • Application of spiroketal polyacetylene compounds in preparing sensitizing medicines for resisting efflux pump resistant staphylococcus aureus
  • Application of spiroketal polyacetylene compounds in preparing sensitizing medicines for resisting efflux pump resistant staphylococcus aureus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1. Isolation of synergistic compounds Rupesdiyne A and Rupesdiyne B from plant Artemisia xinjiang

[0026] 27.3 g of petroleum ether extract from the 95% ethanol extract of Artemisia rupestris L., a plant of the genus Artemisia in the genus Compositae, was mixed with 200-300 mesh silica gel for column chromatography, and each 20 mL was a fraction. It was eluted with petroleum ether-dichloromethane (7:3), and fractions 8-54 were collected and marked as Fr01-12. Fr01-8 was separated and eluted with petroleum ether-dichloromethane (7:3), and fractions 10-18 and fractions 18-35 were collected and designated as Fr01-8-10 and Fr01-8-18, respectively. After being evaporated to dryness under reduced pressure, the weights were 3.2 g and 2.4 g, respectively. Fr01-12-2 and Fr01-12-23 were purified several times respectively to obtain a white solid Fr01-8-10-2 weighing 37.1mg, and a light yellow solid Fr01-8-18-6 weighing 68.9mg, which were obtained by thin-layer chromatog...

Embodiment 2

[0027] Example 2. Isolation of synergistic compounds Rupesdiyne A and Rupesdiyne B from the plant Chrysanthemum schizophrenia.

[0028]Ajania przewalskii Poljak (Ajania przewalskii Poljak), a plant of the genus Asteraceae, is dried and pulverized, and then repeatedly extracted with a ternary mixed solvent (petroleum ether: ether: methanol = 1:1:1) 36g of extract. Part of this extract (26 g) was mixed with 200-300 mesh silica gel for column chromatography, and was eluted with a gradient of petroleum ether-acetone system to obtain six components of Fr-1 to Fr-6. Fr-3 (1.9g) was further separated by silica gel column chromatography, and eluted with petroleum ether-dichloromethane (8:2) to obtain eight components of Fr-3-1~Fr-3-8. Fr-3-4 (820 mg) was separated by silica gel column chromatography, eluted with petroleum ether-dichloromethane, separated and purified repeatedly, and finally further purified by reverse phase silica gel column chromatography and normal phase silica gel ...

Embodiment 3

[0033] Embodiment 3, the synergistic effect test of the combination of compound and oxacillin

[0034] The synergistic antibacterial test of compounds and antibiotics was carried out on a 96-well plate at different concentrations formed by the double dilution method;

[0035] An appropriate amount of oxacillin is dissolved in DMSO to prepare an antibiotic mother solution, and an appropriate amount of oxacillin mother solution is dissolved in broth to prepare an oxacillin stock solution. Samples of compounds Rupesdiyne A and Rupesdiyne B were dissolved in DMSO according to the calculated amount to prepare mother liquor. Diluted in broth, the initial inhibitory concentrations of the compound and antibiotic were 512 and 256 μg / mL, respectively. Carry out an orthogonal experiment with this, and record the concentration of oxacillin corresponding to the microwells where bacteria do not grow in each row is the MIC value of oxacillin when used in combination with the compound sample...

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Abstract

The invention belongs to the field of pharmacy, and relates to an application of spiroketal polyacetylene compounds in preparing sensitizing medicines for resisting efflux pump resistant staphylococcus aureus. Based upon results of bacteriostasis experiments, the spiroketal polyacetylene compounds, in the mode of a synergistic effect, can generate an antibacterial synergistic action on oxacillin;and especially, through combined use of the spiroketal polyacetylene compounds and the oxacillin, the minimum inhibitory concentration of the oxacillin can be obviously reduced, and a resistant staphylococcus aureus synergistic action can be taken on the oxacillin. The spiroketal polyacetylene compounds can be applied to the sensitizing medicines for resisting a multi-drug resistant staphylococcusaureus strain EMRSA-16 containing an mecA efflux pump drug resistance gene, as well as to a pharmaceutical composition which is prepared from the compounds and the oxacillin and has a resistant staphylococcus aureus resisting effect.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to the use of spiroketal polyacetylene compounds in the preparation of anti-efflux pump drug-resistant Staphylococcus aureus sensitization drugs, especially the use of spiroketal polyacetylene compounds in anti-mecA efflux pump resistance Use of pharmacogenes in the sensitization of multidrug-resistant Staphylococcus aureus strain EMRSA-16. Background technique [0002] Methicillin-Resistant Staphylococcus aureus (MRSA) is one of the most common infectious bacteria in hospitals. Studies have shown that MRSA is resistant to all lactam antibiotics such as penicillin and other antibiotics, and also resistant to macrolides, fluoroquinolones, tetracyclines and other antibiotics, which makes its Infections become more difficult to treat. Currently, only vancomycin is the only antibiotic available for the treatment of MRSA. Unfortunately, in 2002, MRSA strains completely resistant to vancomycin app...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/35A61K31/431A61P31/04C07D493/10C07D493/20
CPCA61K31/35A61K31/431C07D493/10C07D493/20A61K2300/00
Inventor 蓝江儿李晓瑾孙仲琳顾娟穆青
Owner FUDAN UNIV
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