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Aspidinol compound and application thereof in preparing medicines for resisting drug-resistant bacteria

A compound, the technology of cotton horse phenol, applied in the field of pharmacy, can solve problems such as failure and reduction of drug concentration

Inactive Publication Date: 2012-05-23
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most types of commonly used antibiotic drug molecules are "pumped out" by the bacterial cell in these external pump mechanisms, making the drug less effective in the intracellular concentration

Method used

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  • Aspidinol compound and application thereof in preparing medicines for resisting drug-resistant bacteria
  • Aspidinol compound and application thereof in preparing medicines for resisting drug-resistant bacteria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Take 2 kg of dried hypericum (Hypericum chinense L.) fruit leaves, crush them, soak and extract with 95% ethanol (3 L × 3 times), combine the extracts and evaporate to dryness under reduced pressure to obtain 437 g of extract. The extract was eluted with 200-300 mesh silica gel (6×60 cm silica gel column), petroleum ether-ethyl acetate (100:0 ~ 0:100) gradient, and detected by silica gel thin-layer chromatography. The fractions eluted with petroleum ether-ethyl acetate 70:30 were combined and evaporated to dryness to obtain an orange-yellow waxy solid, which was re-chromatographed on a silica gel column with petroleum ether-acetone (80:20) as the eluent to obtain yellow crystals. Continue to purify by silica gel column chromatography, the eluent is petroleum ether-acetone (90:10), to obtain 10 g of yellow crystals. It was detected as a pure compound by forward and reverse phase silica gel thin-layer chromatography and HPLC, and was identified as aspidinol C by spectral ...

Embodiment 2

[0031] Embodiment 2 antibacterial experiment

[0032] Before the minimum inhibitory concentration (MIC) test, all test strains were inoculated on agar medium (Oxoid) and incubated at 37oC for 24 h. The control antibacterial drug norfloxacin and the test compound samples aspidinol C and aspidinol D solutions were added to the corresponding wells at a certain solubility. The matrix was Cation adjusted Mueller-Hinton broth (CAMHB). Incubate at 37oC for 18 h. For MIC determination, 20 μL of 5 mg / mL bromodimethylthiazolediphenyltetrazolium blue (MTT; Sigma) staining solution was added to each well and incubated for 20 min. Bacterial growth is judged by a color change from yellow to dark blue. Based on observations, the lowest concentration that results in no growth of bacteria is the MIC value.

[0033] The results show that the minimum inhibitory concentration MIC of fluoroquinolones norfloxacin is 32 μg / mL (100 μM), and the MICs of compounds aspidinol C and aspidinol D of t...

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Abstract

The invention, belonging to the field of medicine, relates to an aspidinol compound and an application of the compound in inhibiting the activity of multidrug-resistant Staphylococcus aureus (MRSA). According to the invention, the aspidinol compound having the activity of drug-resistant bacteria is obtained by extracting and separating Hypericum monogynum, and the compound is represented as aspidinol C and D in the formula I. The bacteriostasis experiment shows the aspidinol C and D have a certain inhibiting effect on drug-resistant bacterial strains of six different mechanisms, wherein, the compound has a stronger inhibitory activity against MRSA strain SA-1199 B having fluoroquinolone outer pump protein NorA resistance than norfloxacin as a contrast medicine. The compound can be used for preparing antibiotic medicinal preparations. In the formula I, R represents lower alkyl: C1-C5 straight chain branched chain alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, t-butyl, pentyl, isopentyl, and neo-pentyl.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a cerol compound and its application in the preparation of anti-drug-resistant bacteria drugs, especially the application of inhibiting the activity of multidrug-resistant staphylococcus aureus. Background technique [0002] Bacterial drug resistance has always been a thorny problem that plagues clinical anti-infective treatment. Among them, Multidrug-resistant Staphylococcus aureus has become a common and serious infectious bacteria in hospitals in recent years. In addition to being resistant to all lactam antibiotics, it is resistant to macrolides, Antibiotics such as fluoroquinone and tetracycline have also developed resistance. In 2002, resistant strains of vancomycin, the most powerful antibiotic in use, emerged in the United States. The oxazolinone drug Linezoid (Zyvox TM ) and the streptoxin drug quinupristin / dalfostin mixture were put on the market in 2001, and within a year, Li...

Claims

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Application Information

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IPC IPC(8): C07C49/84C07C45/79A61K31/12A61P31/04
Inventor 穆青王玮曾祎含西蒙.吉本斯卡迪者奥斯曼
Owner FUDAN UNIV
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