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Antidiarrheal ligan compound A with antibacterial activity and application thereof

A technology for antidiarrheal lignans and compounds, applied in the field of medicine, can solve the problems of drug resistance of drug-resistant bacteria, increased mortality and other problems

Inactive Publication Date: 2015-07-29
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main reason for the increase in the fatality rate is the difficulty of drug use caused by drug-resistant bacteria

Method used

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  • Antidiarrheal ligan compound A with antibacterial activity and application thereof
  • Antidiarrheal ligan compound A with antibacterial activity and application thereof
  • Antidiarrheal ligan compound A with antibacterial activity and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 20Kg of Zixie Muzi was heated and refluxed with 10 times the volume fraction of 75% ethanol-water solution for 3 times, 1 hour each time, the extract was filtered, and the ethanol was recovered under reduced pressure to obtain the extract. The extract part (1009) was subjected to repeated silica gel adsorption column chromatography, and gradient elution was carried out with dichloromethane-methanol (100:1-1:100) system, and SephadexLH-20 column chromatography was performed with methanol-water (10:1-1 :10), dichloromethane-methanol (5:1-1:1) or pure methanol for elution, HPLC for gradient elution with methanol-water (5:95-95:5) system, combined with recrystallization, etc. Means separation and purification to obtain antidiarrheal lignan A.

Embodiment 2

[0028] (1) The antidiarrheal Muzi extract was chromatographed on a HPD600 macroporous resin column, followed by gradient elution with water and volume fractions of 60% ethanol, 70% ethanol, 80% ethanol, 90% ethanol and 100% ethanol;

[0029] (2) The eluate obtained in step (1) with a volume fraction of 80% ethanol was separated by silica gel column chromatography, and gradient eluted with dichloromethane:methanol 100:1, 100:4, 100:8, 100:16 (volume mixing ratio) to obtain the compound Crystallization, chemical properties and spectral data (see Table 1) identified as a lignan. Its structure is:

[0030]

Embodiment 3

[0031] Embodiment 3: the inhibitory activity of antidiarrheal lignan A to 2 kinds of bacterial strains

[0032] According to the American Clinical Laboratory Standardization Committee CLSI (formerly NCCLS) drug susceptibility test protocol, the in vitro antibacterial activity of the compound antidiarrheal lignan A was determined.

[0033] Instruments and materials:

[0034] Analytical balance for instruments and reagents; 721-2000 spectrophotometer (Shangdong Gaomi Rainbow Analytical Instrument Co., Ltd.); ZHJH-C luxury ultra-clean workbench (Shanghai Zhicheng Analytical Instrument Manufacturing Co., Ltd.); LDZX vertical pressure steam Sterilizer (Shanghai Shen'an Medical Instrument Factory); WMK-02 electric thermostat incubator (Hubei Province Huangshi Medical Instrument Factory); No. 11 MSSA (methicillin-sensitive Staphylococcus aureus); No. 27 MRSA (resistant to Methicillin and vancomycin-resistant Staphylococcus aureus); MH medium (Beijing Aoboxing Biotechnology Co., Ltd....

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PUM

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Abstract

The invention belongs to the technical field of medicines and discloses a structure of an antidiarrheal ligan compound A with natural bacteriostatic activity and application of the antidiarrheal ligan compound A to bacteriostasis. In-vitro culture screening experiments and in-vitro bacteriostatic activity tests show that the antidiarrheal ligan compound A has a relatively obvious inhibitory activity on two selected bacteriostatic strains. The specific data is that the antidiarrheal ligan compound A has an extremely strong inhibitory effect on methicillin-sensitive staphylococcus aureus, and the MIC (Minimal Inhibitory Concentration) is 128 [mu]g / mL; the antidiarrheal ligan compound A also has an extremely strong inhibitory effect on methicillin-resistant and vancomycin-resistant staphylocccus aureus, and the MIC value is 128 [mu]g / mL.

Description

technical field [0001] The present invention relates to the technical field of medicine, relates to compound antidiarrheal lignan A and its use in the field of pharmacy, and specifically discloses a new compound obtained from plants, Chinese medicinal materials or Chinese medicinal pieces or obtained by synthetic and semi-synthetic means. Antidiarrheal lignan A, a natural antibacterial active lignan compound, and its use in antibacterial aspects. Background technique [0002] Due to the over-reliance and abuse of antibiotics in recent years, the types of drug-resistant bacteria have increased rapidly, and new strains with multi-drug resistance have been rapidly derived. These multi-drug-resistant bacteria are juxtaposed with tuberculosis and HIV. Three pathogenic microorganisms that pose a major threat to human health. In the 1950s and 1960s, known as the "golden age" of antibiotics, about 7 million people died of infectious diseases worldwide every year, and this number ro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04A61K31/34A61P31/04
CPCC07D493/04
Inventor 孙博航董婷婷葛晓磊晋敦青金颖
Owner SHENYANG PHARMA UNIVERSITY
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