Use of benzoyl polyhydroxycyclohexene in the preparation of pharmaceutical compositions

A technology of benzoyl polyhydroxycyclohexene and a composition is applied in the field of preparing a pharmaceutical composition with the synergistic effect of anti-external pump-resistant Staphylococcus aureus, and can solve the problems of serious bacterial resistance and the like

Inactive Publication Date: 2017-11-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also because of the wide application of norfloxacin in clinical and animal husbandry, bacteria have developed serious drug resistance to it, thus limiting the application of norfloxacin [4]

Method used

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  • Use of benzoyl polyhydroxycyclohexene in the preparation of pharmaceutical compositions
  • Use of benzoyl polyhydroxycyclohexene in the preparation of pharmaceutical compositions
  • Use of benzoyl polyhydroxycyclohexene in the preparation of pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1. Isolation of synergistic compounds EllipeiopsolB and Zeylenol from the leaves of Piper betel

[0036] Take 3.5g extract from the chloroform extract of the 95% ethanol extract of Piperbetle, mix it with 200-300 mesh silica gel for column chromatography, and use 20mL as a fraction. It was eluted with chloroform-acetone (9:1), and fractions 32-36 were collected and marked as Fr02-32. Fr02-32 was separated and eluted with chloroform-methanol (95:5). Fraction 4-5 was collected and recorded as Fr02-32-4, and weighed 430 mg after evaporating to dryness under reduced pressure. Continue to separate Fr02-32-4, elute with chloroform-acetone (9:1), collect fractions 2-5 and fractions 6-10 respectively, and record them as Fr02-32-4-2 and Fr02-32-4 -6, evaporated to dryness under reduced pressure and weighed 160mg and 220mg respectively. Fr02-32-4-2 and Fr02-32-4-6 were purified several times respectively to obtain a white solid Fr02-32-4-2 weighing 20 mg and Fr02-32-4-6...

Embodiment 2

[0037] Embodiment 2, isolating synergistic compound EllipeiopsolB and Zeylenol from plant floret purple jade disc

[0038] 3.34Kg of the dried aerial part of the plant of the genus Uvaria rufa was extracted with chloroform to obtain 482g of green extract. Part of this extract (150 g) was extracted and layered with 50% petroleum ether-alcohol / water solution, and then the alcohol / water layer was extracted with chloroform to obtain 104 g of chloroform sub-extract. 104g of the extract was separated by column chromatography and eluted with chloroform-acetone to obtain five components of Fr-1 to Fr-5. Fr-3 (5 g) was separated by silica gel column chromatography and eluted with chloroform-methanol to obtain nine components of Fr-3-1~Fr-3-9. Fr-3-5 (2.89 g) was further separated by silica gel column chromatography and eluted with dichloromethane-acetone to obtain thirteen components from Fr-3-5-1 to Fr-3-5-13. Fr-3-5-7 (1.22g) was further separated and purified by reverse phase sili...

Embodiment 3

[0043] Embodiment 3, synergistic compound Zeylenol is synthesized with simple chemical raw material

[0044] synthetic route:

[0045]

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PUM

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Abstract

The invention belongs to the field of pharmacy, and relates to a benzoyl polyhydroxycyclohexene compound and its synergistic antibacterial effect on drug-resistant Staphylococcus aureus of an efflux pump. The compound of the present invention itself does not have the effect of inhibiting bacterial growth. When it is compatible with the antibiotic norfloxacin, the fluoroquinolone-resistant methicillin-resistant Staphylococcus aureus containing the NorA gene is adopted by targeting the bacterial efflux pump (efflux) resistance mechanism. Experimental drug-resistant bacteria SA1199B was tested, and the results showed that the compounds Zeylenol and Ellipeiopsol B reduced the minimum inhibitory concentration values ​​of norfloxacin by 4 times and 16 times, respectively. The compound Zeylenol involved in the present invention has the same inhibitory effect on the efflux pump of bacteria as the positive control drug. The compounds involved in the invention can be used to prepare antibiotic synergistic drugs.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to the use of benzoyl polyhydroxycyclohexene in the preparation of pharmaceutical compositions, in particular to the use of benzoyl polyhydroxycyclohexene in the preparation of synergistic effects of anti-external pump drug-resistant Staphylococcus aureus; especially benzoyl polyhydroxycyclohexene The use of acyl polyhydroxycyclohexene in the preparation of fluoroquinolone-resistant methicillin-resistant Staphylococcus aureus (MRSA) drugs. Background technique [0002] Methicillin-resistant Staphylococcus aureus (MRSA) is one of the most common infectious bacteria in hospitals. Today, MRSA is resistant to all lactam antibiotics such as penicillin, but also to macrolides, fluoroquinolones, tetracyclines, etc., making its infection more difficult to treat. Currently, only vancomycin is the only antibiotic available for the treatment of MRSA. Unfortunately, in 2002, MRSA strains completely resi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K31/235A61P31/04
Inventor 孙仲琳穆青王双英西蒙.吉本斯
Owner FUDAN UNIV
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