Medicinal composition containing resveratrol and being capable of inhibiting drug-resisting staphylococcus aureus

A technology of resveratrol and Staphylococcus aureus, which is applied in the field of pharmacy, can solve the problem that the antibacterial effect of resveratrol has not been seen yet, and achieve the effect of improving sensitivity

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

AI Technical Summary

Problems solved by technology

[0006] So far, there has been no report on the antibacterial effect of

Method used

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  • Medicinal composition containing resveratrol and being capable of inhibiting drug-resisting staphylococcus aureus
  • Medicinal composition containing resveratrol and being capable of inhibiting drug-resisting staphylococcus aureus
  • Medicinal composition containing resveratrol and being capable of inhibiting drug-resisting staphylococcus aureus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 prepares compound Resveratrol

[0034] Take 202.6 g of dried roots of Sophora davidii, crush them, soak them in 95% ethanol (3 L x 3 times), combine the extracts and evaporate to dryness under reduced pressure to obtain 18.5 g of extract. The extract was sequentially extracted with petroleum ether, chloroform, and methanol, wherein 13.9 g of the methanol part was obtained, and the methanol part was separated by silica gel column chromatography, and the eluent was dichloromethane-methanol (100:0-0:100), gradient washing After removal, silica gel thin-layer chromatography detection, the fractions were collected to obtain 570.4 mg of mixture 9, and mixture 9 obtained 27.2 mg of colorless needle crystals through repeated column chromatography on gel and silica gel, which was detected as a pure compound by silica gel thin-layer chromatography and HPLC. Identified as Resveratrol by spectral data.

Embodiment 2

[0035] Embodiment 2 prepares compound Resveratrol

[0036] Utilize high-speed countercurrent chromatography (TBE-300 type high-speed countercurrent chromatography) to separate and purify resveratrol in Polygonum cuspidatum (Polygonumcuspidatum), select the solvent system as: chloroform: methanol: water = 4: 3: 2, rotating speed 850r / min, flow rate 2ml / min, and the ultraviolet detection wavelength is 280nm; under this condition, the yield of resveratrol is 0.186%, and the purity is greater than 96%.

Embodiment 3

[0037] Embodiment 3 prepares compound Resveratrol

[0038] With 3,5-dimethoxybenzaldehyde (1) as starting material, obtain 3 through demethylation reaction under the effect of anhydrous aluminum trichloride, 5-dihydroxybenzaldehyde (2), then with p- Hydroxyphenylacetic acid undergoes Perkin condensation under the action of acetic anhydride and triethylamine to obtain (E)-2-(4'-hydroxyphenyl)-3-(3',5'-dihydroxyphenyl)acrylic acid (4) , and finally the target compound resveratrol (5) was obtained through synchronous decarboxylation-isomerization reaction with a total yield of 41.9%.

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Abstract

The invention belongs to the field of pharmacy, and relates to compound 3, 4',5-trihydroxy-diphenyl (resveratrol) and applications of the compound 3, 4',5-trihydroxy-diphenyl (resveratrol) in preparing sensitivity enhancing medicines of methicillin-resistant staphylococcus aureus capable of resisting fluoroquinolones. The compound 3, 4',5- trihydroxy-diphenyl (resveratrol) is wide in distribution,at present, resveratrol has been found in plants of at least 21 families, 31 categories and 72 kinds, wherein the contents in grape, polygonum cuspidatum and peanut are relatively high, and no obvious toxic and side effects exist. The antibacterial test shows that the compound has the pharmacological activity of improving the sensitivity of the multidrug-resisting staphylococcus aureus for norfloxacin, especially aiming at the methicillin-resistant staphylococcus aureus SA1199B containing fluoroquinolones-resisting gene NorA, the MIC value of norfloxacin can be reduced by 16 times after the compound and norfloxacin are mixed for use, and further, the composition can be used for preparing antibiotic synergistic medicines.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a pharmaceutical composition for inhibiting drug-resistant Staphylococcus aureus, in particular to the compound 3,4', 5-trihydroxystilbene (Resveratrol) and its preparation of anti-fluoroquinolone-resistant Methicillin Staphylococcus aureus drug use. Background technique [0002] The prior art discloses that Methicillin-Resistant Staphylococcus aureus (MRSA) is one of the most common infectious bacteria in hospitals. In addition to superficial skin infection, it can also cause deep infection inside the human body. Clinical practice shows that MRSA, which is resistant to all lactam antibiotics such as penicillin, has also developed resistance to antibiotics such as macrolides, fluoroquinolones, and tetracyclines, which makes its infection more severe. Difficult to treat. Currently, only vancomycin is the only antibiotic available for the treatment of MRSA. Unfortunately, MRSA strains that ...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61K31/496C07C39/21A61P31/04
CPCA61K31/05A61K31/496C07C39/21A61K2300/00
Inventor 陈杰桃穆青王锐
Owner FUDAN UNIV
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