New uses of myricetin and its derivatives and a microbicide against HIV infection

A technology of microbicides and myricetin, which is applied in the direction of antiviral agents, medical preparations containing active ingredients, active ingredients of heterocyclic compounds, etc., can solve problems such as failure and unsatisfactory clinical inhibitory effect of microbicides, and achieve Good clinical anti-HIV infection efficacy, good anti-HIV activity effect

Active Publication Date: 2020-07-28
广州南方医大科技园有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, about 20 microbicide products have entered various stages of clinical trials, and most of the polyanionic and surfactant microbicides have unsatisfactory clinical inhibitory effects or certain safety problems. Both have successively declared failure or been suspended

Method used

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  • New uses of myricetin and its derivatives and a microbicide against HIV infection
  • New uses of myricetin and its derivatives and a microbicide against HIV infection
  • New uses of myricetin and its derivatives and a microbicide against HIV infection

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0024] Experimental example 1, Thioflavin T staining method to observe the effect of myricetin on the formation of SEVI amyloid fibrils

[0025] (1) Gradiently diluted myricetin (final concentrations are 75, 37.5, 18.75 and 0 μg / mL) mixed with 3 mg / mL PAP248-286 solution, placed in a constant temperature oscillator, 37 ° C, 1400 rpm constant temperature oscillation;

[0026] (2) At different time points of oscillation (0, 6, 12, 18, 24 and 48h), take out 10 μL samples and mix them with 190 μL Thioflavin T solution, and measure the fluorescence intensity with a fluorescent microplate reader (excitation wavelength is 440 nm, emission wavelength is 485nm).

[0027] Experimental results such as figure 1 As shown, 75 μg / mL myricetin can completely inhibit the self-aggregation of PAP248-286 to form SEVI amyloid fibrils within 48 hours.

experiment example 2

[0028] Experimental Example 2, Transmission Electron Microscopy Observation of the Effect of Myricetin on the Morphology of SEVI Amyloid Fibrils

[0029] (1) Gradiently diluted myricetin (75, 37.5, 18.75 and 0 μg / mL) was mixed with 3 mg / mL PAP248-286 solution, placed in a constant temperature oscillator, and oscillated at a constant temperature at 37 ° C and 1400 rpm;

[0030] (2) At different time points (0, 12 and 24h), take 5 μL samples and drop them on the copper grid, and after 2 minutes, use filter paper to absorb excess liquid from the edge of the copper grid;

[0031] (3) Add phosphotungstic acid (3%, pH 7.0) dropwise to the copper grid, and use filter paper to absorb excess dye solution from the edge of the copper grid after 2 minutes;

[0032] (4) Add pure water dropwise to the copper grid, use filter paper to absorb excess water from the edge of the copper grid, and use it for electron microscope observation after drying.

[0033] Experimental results such as fig...

experiment example 3

[0034] Experimental example 3. Circular dichroism method to detect the influence of myricetin on the secondary structure of mature SEVIβ-sheet

[0035] (1) Gradiently diluted myricetin (500, 250, 125 and 0 μg / mL) was mixed with 3 mg / mL preformed SEVI solution, placed in a constant temperature oscillator, and reacted at 37 ° C and 1400 rpm;

[0036] (2) At different time points (1min, 24h and 48h), take out the sample and mix it with PBS and dilute it until the final concentration of the peptide is 300μg / mL;

[0037] (3) Scan the spectrogram in the 200-260 nm band on the circular dichroism spectrometer.

[0038] Experimental results such as image 3 As shown, after myricetin was treated for 1 min, the peak at 220 nm of the amyloid fibril characteristic structure β-sheet disappeared, indicating that myricetin could rapidly destroy the secondary structure of mature SEVI.

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Abstract

The invention discloses a novel application of myricetin and derivatives thereof and an anti-HIV infection microbicide. The myricetin can inhibit formation of SEVI, destroy a mature SEVI structure and directly block off HIV infection enhancement caused by the SEVI; and in addition, the myricetin, which also has a good anti-HIV activity, can be developed into the dual-function microbicide capable of antagonizing the SEVI and resisting HIV, so as to prevent possibility that a poor clinical curative effect is caused due to existence of amyloid fibers in seminal fluid to the greatest extent; with the presence of the seminal fluid, the myricetin can coordinate with any one anti-retroviral agent, which is selected from azidothymidine, raltegravir, maraviroc, tenofovir, nevirapine and efavirenz, so as to resist the HIV; the multi-component anti-HIV infection microbicide, which contains the myricetin and the anti-retroviral agent, can be developed; and the microbicide can simultaneously act on two aspects, namely the seminal fluid and viruses, so that a better anti-HIV infection clinical curative effect can be developed.

Description

technical field [0001] The invention relates to the field of microbicides, in particular to the new application of myricetin and its derivatives and a microbicide against HIV infection. Background technique [0002] AIDS (AIDS) is a viral sexually transmitted disease caused by human immunodeficiency virus (HIV), and sexual transmission is the main transmission route of HIV. Although in theory, the best means to prevent HIV infection is to use AIDS vaccine; however, the AIDS vaccine Research still needs a long time to explore, and it is difficult to come out with an effective AIDS vaccine in the short term. [0003] Microbicide is a kind of gel, cream, suppository, medicine film or sponge containing anti-HIV ingredients, which is inserted into the vagina or anus before sexual intercourse to prevent the sexual transmission of HIV and other sexually transmitted diseases. Effective measures to prevent HIV sexual transmission controlled by women are of great significance for pre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K31/7072A61K31/513A61K31/46A61K31/675A61K31/551A61K31/536A61P31/18
CPCA61K31/352A61K31/46A61K31/513A61K31/536A61K31/551A61K31/675A61K31/7072A61K2300/00
Inventor 李琳任茹霞张萱萱殷淑文丁永桢梁太珍刘叔文
Owner 广州南方医大科技园有限公司
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