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A kind of compound antidiarrheal lignan a with anti-drug resistance activity and use thereof

A technology of antidiarrheal lignans and compounds, applied in the field of medicine, can solve problems such as difficulty in drug-resistant bacteria and increased mortality

Inactive Publication Date: 2017-06-30
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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  • A kind of compound antidiarrheal lignan a with anti-drug resistance activity and use thereof
  • A kind of compound antidiarrheal lignan a with anti-drug resistance activity and use thereof
  • A kind of compound antidiarrheal lignan a with anti-drug resistance activity and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The antidiarrheal muzi 20Kg was extracted 3 times with 10 times the volume fraction of 75% ethanol-water solution by heating and refluxing for 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 Sephadex LH-20 column chromatography was carried out with methanol-water (10:1-1:100). :10), dichloromethane-methanol (5:1-1:1) or pure methanol for elution, HPLC with methanol-water (5:95-95:5) system for gradient elution, combined with recrystallization, etc. Means of separation and purification to obtain antidiarrheal lignan A.

Embodiment 2

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

[0029] (2) The volume fraction obtained in step (1) is 80% ethanol. The eluate is separated by silica gel column chromatography and eluted with a gradient of 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) were identified as a lignan. Its structure is:

[0030]

Embodiment 3

[0031] Example 3: Inhibitory activity of antidiarrheal lignan A on two bacterial strains

[0032] Refer to the US Clinical Laboratory Standardization Committee CLSI (formerly NCCLS) drug susceptibility test protocol to determine the in vitro antibacterial activity of the compound antidiarrheal lignan A.

[0033] Instruments and materials:

[0034] Instrument and reagent analytical balance; 721-2000 type 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 Equipment Factory); WMK-02 electric heating constant temperature incubator (Hubei Huangshi Medical Equipment Factory); No. 11 MSSA (methicillin-sensitive Staphylococcus aureus); No. 27 MRSA (resistant Methicillin and vancomycin-resistant Staphylococcus aureus); MH medium (Beijing Obosing Biotechnology Co., Ltd.); BHI broth (Beijing Obosing Bi...

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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, and relates to the compound antidiarrheal lignan A and its use in the pharmaceutical field. Specifically, it discloses a novel compound obtained from plants, Chinese medicinal materials or Chinese medicinal pieces or obtained by synthetic and semi-synthetic methods. Natural antibacterial activity lignan compound antidiarrheal lignan A 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 have been side by side with tuberculosis and HIV and have become The three major 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...

Claims

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Application Information

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Patent Type & Authority Patents(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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