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Application of tiacumicin derivatives in preparation of medicines for treating related diseases and/or symptoms caused by dengue virus infection

A technology of taigamycin and dengue virus, applied in the field of medicine, can solve problems such as lack of effective drugs, and achieve the effects of high safety, high inhibition of dengue virus activity, and strong binding ability

Active Publication Date: 2020-05-26
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is a lack of clinically approved effective drugs against dengue virus

Method used

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  • Application of tiacumicin derivatives in preparation of medicines for treating related diseases and/or symptoms caused by dengue virus infection
  • Application of tiacumicin derivatives in preparation of medicines for treating related diseases and/or symptoms caused by dengue virus infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Anti-DENV activity of tiacomycin derivatives at the cellular level

[0022] Virus strain: Dengue virus DENV2 (NGC)

[0023] Cell Line: A549

[0024] Detection method:

[0025] 50% Effective Concentration, EC 50 ): DMSO, gradient concentration of tiacomycin derivatives to saturate cells 1h in advance, after virus infection for 2h, change to virus-free medium containing the corresponding concentration of drug for 48h; collect cell supernatant, extract viral RNA in the supernatant, use qRT- The number of DENV2 virus RNA copies in the supernatant was detected by PCR.

[0026] Inhibition rate (%) = (1-the number of viral RNA copies in the administration group / the number of viral RNA copies in the solvent control group) 100%, calculated by the Forcast formula of EXCEL 2013, when the inhibition rate is equal to 50%, the corresponding tyacomycin derivative concentration of the substance, as EC 50 . Three repeated experiments were averaged.

[0027] 50% Cytotox...

Embodiment 2

[0031] Example 2 Inhibitory activity of taigamycin derivatives on DENV2-prM protein in A549 cell line

[0032] Virus strain: Dengue virus DENV2 (NGC)

[0033] Cell Line: A549

[0034] Detection method:

[0035] DMSO, 1, 5, and 10 μM tiacomycin derivatives were used to saturate cells for 1 h in advance. After virus infection for 2 h, the virus-free medium containing the corresponding concentration of drugs was changed for 48 h; cell pellets were collected, and cells under different treatments were detected by western blot electrophoresis. The relative expression of internal DENV2(NGC)-prM protein, with GAPDH as the internal reference protein. like figure 1 . Tiacumycin derivatives Compound 1 and Compound 2 can effectively inhibit the expression of DENV2prM protein at a concentration of 1~5μM, and the expression of DENV2prM protein, which is an important structural protein, is inhibited, indicating that the reproduction of DENV2 has been inhibited.

Embodiment 3

[0036] Example 3 Surface plasmon resonance detection of the affinity of tyacomycin derivatives with DENV2-NS5 protein

[0037] This method uses GE's Biacore T100 instrument and CM5 chip for experiments. First, the purified DENV2(NGC)-NS5 protein amino group is coupled to the CM5 chip, and then it flows through different concentrations of taigamycin derivatives, and the instrument detects The mass change of the substance adsorbed on the chip surface was calculated to calculate the affinity rate of the compound (K a ) and the dissociation rate (K d ). Affinity = dissociation equilibrium constant (K D ), this value describes the binding strength between small molecules and protein molecules. The biological significance is that when small molecules bind to proteins 1:1, let 50% of the small molecules saturate the concentration of protein molecules. The smaller the value, the stronger the binding. Usually, the small molecules and protein affinity molecules calculated by this met...

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Abstract

The invention discloses an application of a tiacumicin derivative to preparation of a medicine for treating related diseases and / or symptoms caused by dengue virus infection. Tiacumicin serving as a clostridium difficile infection resisting medicine clinically approved for use is high in safety, and the tiacumicin derivative can remarkably inhibit dengue viruses, is high in activity, has strong binding capacity with dengue virus non-structural protein NS5 and can be expected to be a novel effective dengue virus infection resisting medicine.

Description

technical field [0001] The invention belongs to the field of medicine, and more particularly relates to the application of tiacomycin derivatives in the preparation of medicines for treating related diseases and / or symptoms caused by dengue virus infection. Background technique [0002] Tiacumicins is a general term for a series of 18-membered macrolide antibiotics, and is an important class of therapeutic antibiotics. [0003] Dengue virus belongs to the Flaviviridae family of Flaviviruses. It is an RNA positive-strand virus. It is transmitted by mosquitoes and can cause systemic fever, rash, arthritis and other symptoms. In severe cases, shock and death may occur. [0004] DENV-NS5 is an RNA-dependent RNA polymerase that performs viral genome replication and plays a crucial role in viral replication. Inhibiting the activity of this enzyme can achieve the effect of killing dengue virus. [0005] Currently, there is a lack of clinically approved effective drugs for dengue ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61P31/14
CPCA61K31/7048Y02A50/30
Inventor 张长生黎孟枫张海波朱义广张光涛袁洁朱勋于暕辰
Owner SUN YAT SEN UNIV
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