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Application of diterpenoids in the preparation of antiviral drugs

A technology of antiviral drugs and compounds, applied in the directions of antiviral agents, resistance to vector-borne diseases, anhydride/acid/halide active ingredients, etc., to achieve the effects of reliable curative effect, abundant resources, and no toxic side effects

Active Publication Date: 2021-07-16
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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Problems solved by technology

[0004] Among the compounds involved in the present invention, the patent JPH04210630A shows that compound F21-1 has a good peripheral vasodilation and promoting effect on vertebral artery blood flow, and can be used as a therapeutic and preventive agent for various diseases caused by insufficient blood circulation , but there are no reports about the effects of compounds F21-1 and F21-2 on anti-picornaviridae viruses, especially hand-foot-mouth virus and rhinovirus

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  • Application of diterpenoids in the preparation of antiviral drugs
  • Application of diterpenoids in the preparation of antiviral drugs
  • Application of diterpenoids in the preparation of antiviral drugs

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[0020] (1) Experimental method

[0021] 1. Isolation and identification of active compounds:

[0022] Firstly, 22 fractions were obtained by roughly fractionating the ethyl acetate extraction layer of the traditional Chinese medicine Forsythia forsythia with preparative medium-pressure liquid; then further antibacterial test screening showed that No. 21 fraction (F21) had the best antibacterial activity. Continue to separate the monomer compounds in this component in detail by high performance liquid chromatography. The mobile phase is acetonitrile-water (90:10) and acetonitrile, and the following separation conditions are used: 0.0–30.0 min, 95% A, 30.0 – 40.0 min, 95% –20% A, 40.0 –50.0 min, 20% A, 50 – 55 min, 20% – 95% A. The flow rate was 10 mL / min, and the injection volume was 100 μl of 20 mg / mL sample. The signal of the ultraviolet detector was received at 225 nm. Finally, compounds 1 and 2 were separated and analyzed by mass spectrometry and nuclear magnetic resonan...

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Abstract

The application of diterpenoids in the preparation of antiviral drugs belongs to the technical field of drug screening. The compound is applied to the preparation of drugs against the family of single-stranded positive-strand picornaviruses, which include rhinoviruses that cause colds, enteroviruses EV71 that cause hand-foot-mouth disease in children, coxsackievirus A16, and Human virus infection such as card virus, yellow fever virus and hepatitis C virus can also be used in similar virus infection drugs that cause animal foot-and-mouth disease and other diseases. The half inhibitory concentrations of compound F21‑1 to EV71 virus, CA16 virus and rhinovirus were 53.46 μM, 50.26 μM and 53.53 μM, respectively; the half inhibitory concentrations of compound F21‑2 to EV71 virus, CA16 virus and rhinovirus were 30.25 μM, 32.47 μM and 23.03 μM. The application of the diterpenoid compound in the preparation of antiviral drugs has the advantages of reliable curative effect, no toxic and side effects, abundant resources, low price and the like.

Description

technical field [0001] The present invention relates to the application of diterpenoids with different substituents in the preparation of medicines, which is characterized in that compounds with the following similar structures are used in the preparation of anti-single-strand positive-sense small RNA virus families, including rhinoviruses that cause colds, and children's hand-foot The enterovirus EV71 of mouth disease can infect human viruses such as Coxsackie virus A16, Zika virus, yellow fever virus, and hepatitis C virus, and it can be used in similar virus infection drugs that cause animal foot-and-mouth disease and other diseases. Background technique [0002] Since the 1970s, there have been many large-scale outbreaks of hand-foot-and-mouth disease (HFMD) in dozens of countries or regions around the world. Hand, foot and mouth disease is an acute pediatric infectious disease characterized by rashes, herpes, and blisters on the hands, feet, and mouth, often accompanied...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/194A61K31/19A61P31/14A61P31/16
CPCA61K31/19A61K31/194A61P31/14A61P31/16Y02A50/30
Inventor 麻彤辉马骁驰
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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