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Medicinal use of (3,4-dihydroxyl-5-nitrophenyl)-(4-methylphenyl)ketone

A technology of nitrophenyl and methylphenyl, applied in the field of pharmaceutical compounds

Active Publication Date: 2020-03-24
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It is clinically used as an adjuvant treatment for primary Parkinson's disease who receive combination therapy of levodopa and carbidopa. No studies have shown that it can inhibit seminal amyloid fibrils and their mediated Ebola or HIV-1 transmission. Efficacy of sexual transmission

Method used

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  • Medicinal use of (3,4-dihydroxyl-5-nitrophenyl)-(4-methylphenyl)ketone
  • Medicinal use of (3,4-dihydroxyl-5-nitrophenyl)-(4-methylphenyl)ketone
  • Medicinal use of (3,4-dihydroxyl-5-nitrophenyl)-(4-methylphenyl)ketone

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Experimental program
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Embodiment Construction

[0033] In the following in vitro experiments, (3,4-dihydroxy-5-nitrophenyl)-(4-methylphenyl)methanone inhibits the formation of SEVI, inhibits the binding of SEVI to virus particles, and interrupts the fiber morphology, thereby antagonizing the promotion of SEVI. Virus infectivity was verified.

[0034] Effect of (3,4-dihydroxy-5-nitrophenyl)-(4-methylphenyl)methanone on the formation of SEVI

[0035] Congo red staining: peptide PAP 248-286(220μM) mixed with various concentrations of (3,4-dihydroxy-5-nitrophenyl)-(4-methylphenyl)methanone (5×, 7.5×, 11×) or PBS, placed at 37 React at 1400rpm in a shaker at ℃, take out 10μL samples at different time points (2h, 4h, 8h, 12h, 24h, 48h) and mix with 90μL Congo red solution (Sigma), react in the dark for 15min, centrifuge at 12000rpm, remove the supernatant , the precipitate was dissolved in 50 μL DMSO, and the absorbance value at 490 nm was measured, and the reference wavelength was 650 nm.

[0036] Virus infection enhancement ...

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Abstract

The invention discloses medicinal use of (3,4-dihydroxyl-5-nitrophenyl)-(4-methylphenyl)ketone. Discovered through researches by the inventor, the (3,4-dihydroxyl-5-nitrophenyl)-(4-methylphenyl)ketoneeffectively inhibits semen amyloid fibers from forming, breaks forms of the semen amyloid fibers and inhibits the semen amyloid fibers from being bonded to viruses, thus, the action that the semen amyloid fibers promote sexual propagation of virus HIV-1, virus Ebola and the like is blocked, and the (3,4-dihydroxyl-5-nitrophenyl)-(4-methylphenyl)ketone is an ideal microbicide.

Description

technical field [0001] The present invention relates to a new application of a pharmaceutical compound, in particular to (3,4-dihydroxy-5-nitrophenyl)-(4-methylphenyl)methanone in the preparation of antimicrobial agents for inhibiting semen amyloid fibers Applications. Background technique [0002] There is a type of amyloid fiber in human semen, which can significantly promote the infection of many sexually transmitted pathogens, including HIV-1, Ebola, cytomegalovirus, etc. The most studied is the promotion of HIV-1 infection. Professor Münch of Ulm University in Germany found that there are some degraded polypeptide fragments in semen, and these hydrolyzed polypeptide fragments can form amyloid deposits, thereby promoting HIV-1 infection of target cells. They named this amyloid fiber that enhances virus infection as Semen-derived Enhancer of Virus Infection (SEVI). The mechanism of SEVI's promotion of viral infection is mainly related to its strong cationic properties....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61P15/00A61P31/00A61P31/18A61P31/14
CPCA61K31/12A61P15/00A61P31/00A61P31/18A61P31/14Y02A50/30
Inventor 谭穗懿邱梦婕陈玉柳李钊锋刘叔文
Owner SOUTHERN MEDICAL UNIVERSITY
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