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Medical purpose of holarrhine B

A technology for antidiarrheal wood and drugs, applied in the field of medicine, can solve problems such as heavy responsibilities and long way to go in research and development

Inactive Publication Date: 2019-02-12
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, some compounds with bacterial efflux pump inhibitory activity have been found, but none of them can be used for clinical treatment, and the research and development of efflux pump inhibitor drugs has a long way to go

Method used

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  • Medical purpose of holarrhine B
  • Medical purpose of holarrhine B
  • Medical purpose of holarrhine B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Effects of antidiarrhea B on the efflux pump of methicillin-resistant Staphylococcus aureus (MRSA)

[0026] Materials and Methods

[0027] Experimental strain:

[0028] Two strains, 73111 and 73127, are both methicillin-resistant Staphylococcus aureus (MRSA). These strains were subcultured and then used in this example. Drugs and reagents:

[0029] Ethidium bromide (EtBr): Sigma-Aldrich;

[0030] Carbonyl cyanochlorophenylhydrazone (CCCP): Sigma-Aldrich;

[0031] Pyronin Y: Sigma-Aldrich;

[0032] Phosphate buffered saline: self-made;

[0033] Glucose: Dalian Meilun Biotechnology Co., Ltd.;

[0034] 4-Hydroxyethylpiperazineethanesulfonic acid buffer (HEPES): Beijing Suo Laibao Technology Co., Ltd.;

[0035] Sodium formate: Tianjin Bodi Chemical Co., Ltd.;

[0036] 96-well ELISA plate: Guangzhou Jiete Biofiltration Co., Ltd.

[0037] laboratory apparatus:

[0038] Analytical balance; UV-1700 ultraviolet spectrophotometer (Shimadzu, Japan); ZHJH-C1112B double ve...

Embodiment 2

[0057] Comparison of in vitro synergistic antibacterial activity of antidiarrhealine B combined with penicillin against methicillin-resistant Staphylococcus aureus (MRSA)

[0058] According to the drug susceptibility test protocol of the American Committee for Clinical Laboratory Standardization CLSI (formerly NCCLS), the in vitro antibacterial activity of the compound antidiarrhea B combined with penicillin was determined.

[0059] Materials and Methods

[0060] Experimental strains:

[0061] MRSA (methicillin-resistant Staphylococcus aureus), these strains were subcultured and then used in this example.

[0062] Subculture steps:

[0063] 1. Take out the bacteria-containing glycerol tube from the -80°C refrigerator, inoculate it in the nutrient broth medium aseptically, and culture it with vibration for 18-24 hours.

[0064] 2. Heat the Erlenmeyer flask containing broth agar medium until fully melted. After the culture medium is cooled to about 50°C, the aseptic method i...

Embodiment 3

[0093] Embodiment 3: the preparation of capsule

[0094] Take 50g of antidiarrhealine B, add 200g of fine starch powder, 10g of talcum powder, 5g of magnesium stearate, mix well, granulate, dry, put into capsules, and make 1000 capsules, 3 times a day, 2 times each time piece.

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PUM

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Abstract

The invention belongs to the technical field of medicines, relates to a medical purpose of holarrhine B, and particularly relates to application of a natural compound holarrhine B in the preparation of an efflux pump inhibitor. The inhibitor is used for reversing the drug resistance of a drug-resistant strain, and particularly for reversing the drug resistance of a drug-resistant bacterium. According to the application, by utilizing experiments on the cumulants of ethidium bromide (EtBr) and pyronin Y (Pyronin Y), the exertion of an efflux pump inhibiting effect by the holarrhine B is evaluated. Results show that the holarrhine B with the concentration of 0.25 mmol / ml to 2.0 mmol / ml can be used for obviously increasing the cumulants of the EtBr and the pyronin Y in the thallus of methicillin resistant staphylococcus aureus (MRSA); and the holarrhine B is capable of effectively inhibiting the efflux of an antibiotic in the thallus of the MRSA. The holarrhine B in the invention can exerta synergistic and antibacterial effect as the efflux pump inhibitors (EPIs); a clue is provided for searching the EPIs with application prospects; and thus, a drug resistance reverser with clinical significance is developed.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to the medical application of antidiarrhea B, in particular to the application of the compound antidiarrhea B in the preparation of active drugs for inhibiting microbial efflux pumps. Background technique [0002] With the widespread use of antibiotics, bacterial drug resistance is becoming more and more serious, especially multi-drug resistance (Multi-drug resistance, MDR) has become a very serious medical problem, and various types of bacterial efflux pumps (Efflux pumps) Existence is an important mechanism of bacterial multidrug resistance. [0003] Staphylococcus aureus is one of the main pathogens of nosocomial infection, especially the emergence of MRSA, which makes clinical treatment more difficult. MRSA infection has been tied with hepatitis B and acquired immunodeficiency syndrome to become the three most difficult infectious diseases in the world. The efflux function of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K31/43A61P31/04
CPCA61K31/43A61K31/58A61P31/04A61K2300/00
Inventor 孙博航周丽娜杨宇庞林月麻露萍谢海花郭建艳连敬杰
Owner SHENYANG PHARMA UNIVERSITY