Beta,beta-dimethyl-acry-lalkannin and application in preparing medicines for inhibiting drug-resistant bacteria

A technology of drugs and bacteria, applied in the field of pharmacy, can solve the problems of treatment spread and epidemic difficulties

Inactive Publication Date: 2009-12-09
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The multidrug resistance of MRSA makes it very difficult to trea

Method used

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  • Beta,beta-dimethyl-acry-lalkannin and application in preparing medicines for inhibiting drug-resistant bacteria
  • Beta,beta-dimethyl-acry-lalkannin and application in preparing medicines for inhibiting drug-resistant bacteria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1 prepares compound AE02-7-2

[0038] 1.0 kg root of Arnebia euchroma plant, crushed, soaked in 95% ethanol below 45°C for extraction, combined extracts were concentrated under reduced pressure until all ethanol volatilized, and solid-phase extracted with chloroform. The remaining part was separated by silica gel and RP-18 forward and reverse phase column chromatography several times to obtain purple red solid compound AE02-7-2. Mix 2.0 g of the sample with 100-200 mesh silica gel, and evaporate the residual solvent. Take 250 grams of 200-300 mesh silica gel and put it into a glass column with a diameter of 2.0 cm, add the above-mentioned sample that has been mixed with silica gel and evaporated to dryness, and add mobile phase for separation. The mobile phase of silica gel column chromatography was chloroform-petroleum ether (1:1); the same fractions were combined and evaporated under reduced pressure to remove the solvent. Detect gained sample purity with...

Embodiment 2

[0041] Example 2 Compound AE02-7-2 Pharmacological activity test on SA1199B

[0042] Determine the minimum inhibitory concentration: Norfloxacin (norfloxacin) was purchased from Sigma Chemical Co. (Sigma Chemical Co.) Mueller-Hinton broth (Mueller-Hinton broth, MHB; Oxoid) adjusted to contain 20 mg of calcium ions and Magnesium ions. Bacterial cultures were formulated to 5 x 10 by comparison to McFarland standards 5 Inoculum at cfu / ml density. Norfloxacin and compound AE02-7-2 were dissolved in DMSO solvent and diluted in MHB to an initial concentration of 512 μg / ml. Use a Nunc type 96 microwell plate, add 125 microliters of MHB into wells 1-11; add 125 microliters of compound or norfloxacin (control drug) into well 1 and serially dilute, leaving well 11 without compound or Drugs served as bacterial growth controls. The final volume was added to well 12, which contained no broth as a sterile control. Finally, bacterial inoculum (125 microliters) was added to wells 1-11, r...

Embodiment 3

[0045] The pharmacological activity test of embodiment 3 compound AE02-7-2 to drug-resistant bacteria Xu212 and

[0046] Bacteria were cultured in the same manner as in Example 2, with norfloxacin as the positive control drug, and the experimental steps of Example 2 were repeated to detect the minimum inhibitory concentration of AE02-7-2 to drug-resistant strain Xu212. The strain Xu212 is a tetracycline-resistant Staphylococcus aureus strain with TetK tetracycline efflux protein (Richardson JF, Reith S. Journal of Hospital Infection, 1993, 25: 45-52.).

[0047] The results showed that the compound AE02-7-2 had an inhibitory effect on tetracycline-resistant Staphylococcus aureus strain Xu212 with TetK tetracycline efflux protein, and the minimum inhibitory concentration was 4 μg / ml (10.8 μM), which was comparable to that of the positive control drug norflu The antibacterial activity of Floxacin is comparable, 4 micrograms / ml (12.5μM).

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Abstract

The invention belongs to the pharmaceutical field, relates to beta,beta-dimethyl-acry-lalkannin and an application in preparing medicines for inhibiting drug-resistant bacteria. The invention can provide a natural inhibitor for inhibiting efflux pump multidrug methicillin-resistant staphylococcus aureus. The compound has good inhibiting effect on multidrug staphylococcus aureus resistance strain with NorA efflux pump protein and the antibacterial effect is 13 times of positive contrastive drug norfloxacin. The compound can both inhibit tetracycline-resistant staphylococcus aureus strain Xu212with TetK tetracycline efflux pump protein and macrolide-resistant staphylococcus aureus strain RN4220 with MsrA macrolide efflux pump protein, and the minimal inhibitory concentration is 10.8mu m. The compound of the invention can be prepared to medicines for inhibiting multidrug resistance bacteria and produced to antibacterial injection or external medicine preparation.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a natural naphthoquinone compound for inhibiting external pump-type multidrug-resistant bacteria, in particular to the compound β,β-dimethylacryloylarkanin and its use in the preparation of drugs for inhibiting multidrug-resistant bacteria use Background technique [0002] The discovery of antibiotics at the beginning of the 20th century made leprosy, typhoid, cholera, tuberculosis and other infectious diseases that were difficult to treat no longer terminal illnesses. However, with the continuous advent of antimicrobials and their widespread use worldwide, the resistance of bacteria to antibiotics has become increasingly prominent, and has developed into a serious public health problem by the end of the 1980s. According to reports, Methicillin-Resistant Staphylococcus aureus (MRSA) has become a common and serious infectious pathogen in hospitals. Except for methicillin, MRSA is resistant...

Claims

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Application Information

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IPC IPC(8): C07C69/533A61K31/222A61P31/04
Inventor 穆青叶佳西蒙·吉本斯穆合苏尔·热合曼
Owner FUDAN UNIV
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