Natural naphthoquinone dimer and its application in the preparation of antibacterial drugs
A naphthoquinone dimer, antibacterial drug technology, applied in the field of pharmacy, can solve serious drug resistance and other problems
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Embodiment 1
[0046] Take 1 kg of the roots of Arnebiaeuchroma (purchased from Medicinal Materials Company), crush them, soak and extract with 95% ethanol below 45 degrees Celsius, combine the extracts under reduced pressure and concentrate until all the ethanol has evaporated, add water to the extract and suspend it with acetic acid After extraction with ethyl ester, the organic phase was evaporated to dryness under reduced pressure, and then separated by silica gel and RP-18 forward-reverse phase column chromatography several times to obtain a purple solid compound. Among them, the NMR spectrum data of compounds 2 and 3 are shown in Table 2.
[0047] Table 2. NMR spectrum data of compounds 2 and 3
[0048]
Embodiment 2
[0049] Example 2: Synergistic antibacterial and synergistic effect of EMRSA-16 compound on antibiotics against Staphylococcus aureus
[0050] The synergistic antibacterial test of the compound and antibiotics was carried out at different concentrations formed by the two-fold dilution method on a 96-well plate.
[0051] Dissolve an appropriate amount of norfloxacin in DMSO to prepare an antibiotic mother solution, take an appropriate amount of norfloxacin mother solution and dissolve in the broth to prepare a norfloxacin stock solution, take an appropriate amount of compound sample to dissolve in DMSO to prepare a mother solution, and dilute with the broth. The initial inhibitory concentrations of the compound and the antibiotic were 128 and 256 μg / mL, respectively. An orthogonal experiment was performed to record the concentration of norfloxacin corresponding to each row of microwells where bacteria did not grow. The MIC value of the star. The experimental results are shown in Tab...
Embodiment 3
[0052] Example 3. Direct antibacterial effect of the compound on Staphylococcus aureus
[0053] The standard Staphylococcus aureus strain ATCC25922 and the resistant strains SA1199B, RN4220, EMRSA-15 and Xu212 were taken for microporous antibacterial experiments. The synergistic antibacterial test of the compound and antibiotics was carried out at different concentrations formed by the two-fold dilution method on a 96-well plate. Take an appropriate amount of Norfloxacin and dissolve it in DMSO to prepare an antibiotic mother solution, and take an appropriate amount of Norfloxacin and dissolve it in a broth to prepare a Norfloxacin stock solution. Take an appropriate amount of the compound sample and dissolve it in DMSO to prepare the mother liquor. Diluted with broth, norfloxacin was used as a control drug, and the minimum inhibitory concentration of the compound on the tested strains was greater than 128 μg / mL. None of the compounds showed the activity of inhibiting the growt...
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