Application of histamine receptor inhibitor and derivatives thereof in preparation of anti-Zika virus drugs

A histamine receptor and Zika virus technology, applied in the field of medicine, can solve problems such as the application of histamine receptor inhibitors and their derivatives that have not been seen

Active Publication Date: 2020-01-17
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Studies have shown that histamine receptor inhibitors have anti-Ebola and influenza virus activity, but there is no a

Method used

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  • Application of histamine receptor inhibitor and derivatives thereof in preparation of anti-Zika virus drugs
  • Application of histamine receptor inhibitor and derivatives thereof in preparation of anti-Zika virus drugs
  • Application of histamine receptor inhibitor and derivatives thereof in preparation of anti-Zika virus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] (1) Cell culture

[0027] Take Vero E6 cells for culture. After the cells fill the culture flask, discard the old medium and digest with digestive juice. When the cells become round, discard the digestion solution, immediately add the culture medium, and gently blow the bottom of the bottle with a straw to completely separate the cells from the bottom of the bottle and disperse them into a single-cell suspension. After counting on a hemocytometer, the cell suspension was inoculated in a 6-well plate at a density of 2.5×10 5 individual / mL.

[0028] (2) Determination of compound's inhibitory activity against Zika virus

[0029] In this example, 23 kinds of histamine receptor inhibitors were selected (see Table 1 for specific compound information), and their inhibitory effects on Zika virus RNA and Zika virus protein were determined respectively.

[0030] Table 1 Compound information of 23 histamine receptor inhibitors

[0031]

[0032]

[0033] a. Inhibitory eff...

Embodiment 2

[0052] The EC50 and CC50 of four compounds, which have good inhibitory effect on Zika virus, mehaltraline naphthalene disulfonate, cyproheptadine hydrochloride, JNJ-7777120 and desloratadine, are respectively determined, and the results are shown in Table 3.

[0053] Table 3 EC50 and CC50 of four compounds

[0054] compound EC50(μM) CC50(μM) SI (CC50 / EC50) Mehaldriline naphthalene disulfonate 3.3 50.5 15.3 Cyproheptadine Hydrochloride 8.6 33 3.8 JNJ-7777120 1.2 64.2 53.5 Desloratadine 0.7 23.7 33.9

[0055] It can be seen from Table 3 that the four compounds of mehaldriline naphthalene disulfonate, cyproheptadine hydrochloride, JNJ-7777120 and desloratadine all have strong anti-Zika virus effects and low cytotoxicity. Suitable candidates for anti-Zika virus drugs.

Embodiment 3

[0057] Infect the cells with the Zika virus of different MOI, measure respectively according to the method identical with embodiment 1 four kinds of compounds of mehaldriline naphthalene disulfonate, cyproheptadine hydrochloride, JNJ-7777120 and desloratadine to Zika The inhibitory effect of viral RNA and the inhibitory effect on Zika virus protein, the results are as follows Figure 3-6 shown. It can be seen that the four compounds mehaldriline naphthalene disulfonate, cyproheptadine hydrochloride, JNJ-7777120 and desloratadine can all inhibit Zika virus at different MOI.

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Abstract

The invention provides a histamine receptor inhibitor and derivatives thereof in the preparation of anti-Zika virus drugs. The histamine receptor inhibitor is preferably one or more of mebhydrolin napadisylate, ketotifen fumarate, flunarizine hydrochloride, cyproheptadinehydrochloride, JNJ-7777120, desloratadine, brompheniramine maleate, brompheniramine maleate, chlorpheniramine maleate and cetirizine hydrochloride. The invention brings forward for the first time that the histamine receptor inhibitor and its derivatives have clear anti-Zika virus effect and can significantly inhibit the expression level of Zika virus protein and Zika virus RNA. The invention also screens out histamine receptor inhibitors with better inhibitory effect on Zika virus, including mebhydrolin napadisylate, cyproheptadinehydrochloride, JNJ-7777120, desloratadine, etc., whose inhibition effect on Zika virus at a concentration of 10 uM is equivalent to inhibition effect of ribavirin at a concentration of 40 uM.The histamine receptor inhibitor and the derivatives can be used as good candidate drugs for anti-Zika virus drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, and more specifically, relates to the application of a histamine receptor inhibitor and its derivatives in the preparation of anti-Zika virus drugs. Background technique [0002] Zika virus is a mosquito-borne flavivirus. The genome is a single-stranded positive-sense RNA with a total length of about 11kb, which encodes an open reading frame (ORF) that can form a polyprotein. Zika virus was first isolated in Ugandan rhesus monkeys in 1947. The first recorded case of human infection with Zika virus was in 1952. In 2007, there was an outbreak of Zika virus on Yap Island in the Pacific Ocean. According to data released by the World Health Organization (WHO) in 2016, Zika virus infection occurred in 73 countries or regions. After a person is infected with Zika virus, the main clinical manifestations are rash, fever, muscle pain, non-suppurative conjunctivitis, and headache. In addition, after th...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/437A61K31/4535A61K31/495A61K31/4418A61K31/496A61K31/4545A61K31/4402A61P31/14
CPCA61K31/437A61K31/4402A61K31/4418A61K31/4535A61K31/4545A61K31/495A61K31/496A61K45/00A61P31/14Y02A50/30
Inventor 岑山周睿李晓宇李艳萍李卓荣
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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