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Application of etravirine in preparing anti-bacterial and anti-inflammation drug

An etravirine, antibacterial and anti-inflammatory technology, which is applied in the directions of antibacterial drugs, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as no reports on the application of etravirine antibacterial and anti-inflammatory drugs.

Inactive Publication Date: 2019-04-05
GENERAL HOSPITAL OF PLA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, according to the prior art, etravirine is mainly used in the preparation of drugs for the treatment of HIV, and there is no report on the application of etravirine in the preparation of antibacterial and anti-inflammatory drugs

Method used

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  • Application of etravirine in preparing anti-bacterial and anti-inflammation drug
  • Application of etravirine in preparing anti-bacterial and anti-inflammation drug
  • Application of etravirine in preparing anti-bacterial and anti-inflammation drug

Examples

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Embodiment Construction

[0025] The following examples are provided to further illustrate but not limit the present invention.

[0026] 1. Materials and methods:

[0027] 1.1 Bacteria and cells

[0028] Fusobacterium nucleatum (F. nucleatum, Fn, ATCC 25586) was obtained from the frozen bacterial strain bank of the Key Laboratory of Oral Tissue Regeneration in Shandong Province.

[0029] Gingival fibroblasts (HGF): isolated from 6 volunteer patients aged 18-30 who underwent extraction of impacted teeth.

[0030] 1.2 Reagents

[0031]Defibrinated sheep blood (Haibo Bio Company, Qingdao, Shandong, China), PBS (Soleibao, Beijing, China), hemin-vitamin K1 (Haibo Bio Company, Qingdao, Shandong, China), brain Heart infusion blood culture medium (Suolaibao, Beijing, China), BHI liquid medium (Suolaibao, Beijing, China), type I collagenase (Suolaibao, Beijing, China), DispaseII dispase (Invitrogen, Carlsbad, CA, USA), intracellular reactive oxygen species detection kit (Bebo, Shanghai), etravirine (Selleck...

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Abstract

The invention discloses application of etravirine in preparing an anti-bacterial and anti-inflammation drug. A list of candidate drugs with anti-bacterial and anti-inflammation effects is obtained through RNA-seq (Ribonucleic Acid-sequencing) transcriptome analysis on human cells infected by bacteria and based on a coexpression channel and a drug gene set enrichment analysis method, finding that the list contains a plurality of marketed drugs with the anti-bacterial and anti-inflammation effects, the etravirine with the anti-bacterial and anti-inflammation effects, which is not discovered before, is among the marketed drugs, and the effect of the etravirine is verified to be stronger than the effects of common anti-bacterial and anti-inflammation drugs-metranidazole and gentamicin at a cellular level, so that the etravirine can be applied to prepare the anti-bacterial and anti-inflammation drugs.

Description

technical field [0001] The invention relates to a new application of medicine, in particular to the application of etravirine in the preparation of antibacterial and anti-inflammatory drugs, and belongs to the field of biomedicine. Background technique [0002] Etravirine (brand name Intelence, formerly known as TMC125 and R-165335) is a drug used to treat HIV. Its molecular weight is 435.28, and its CAS code is 269055-15-4. It is soluble in DMSO and insoluble in water and ethanol. [0003] Etravirine is highly effective against wild-type HIV-1, with EC50 of 1.4nM to 4.8nM, and also exhibits certain activity against HIV-2, with EC50 of 3.5μM (see Das K, Clark AJ, Lewi PJ, Heeres J, De Jonge MR, KoymansLM, Vinkers HM, Daeyaert F, Ludovici DW, Kukla MJ, et al: Roles of conformational and positional adaptability in structure-based design of TMC125-R165335(etravirine) and related non-nucleotide reverse transcriptase inhibitors that are highly potent and effective against wild-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61P31/04
CPCA61K31/513A61P31/04
Inventor 贾志龙何昆仑冯强康文燕王卫东石金龙赵晓静贾倩刘春蕾
Owner GENERAL HOSPITAL OF PLA
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