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Application of Protoporphyrin Derivatives in Preparation of Enveloped Virus Blocking Agent

An enveloped virus, protoporphyrin technology, used in antiviral agents, resistance to vector-borne diseases, medical preparations containing active ingredients, etc., to achieve the effect of improving survival rate and survival time

Active Publication Date: 2022-01-04
广州肽山生物科技有限公司
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

According to the existing literature, there is no detailed mechanism of action to predict or show that protoporphyrin and its derivatives have the ability to block enveloped virus infection.

Method used

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  • Application of Protoporphyrin Derivatives in Preparation of Enveloped Virus Blocking Agent
  • Application of Protoporphyrin Derivatives in Preparation of Enveloped Virus Blocking Agent
  • Application of Protoporphyrin Derivatives in Preparation of Enveloped Virus Blocking Agent

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Embodiment Construction

[0053] In the previous research of the inventor, a porphyrin derivative—pyropheophorbide a was discovered and identified from the seafood sea melon seeds through the method of activity tracking. Further biological activity studies have found that the compound has significant anti-influenza virus activity against a series of influenza virus strains. Mechanistic studies have shown that pyropheophytin a acts in the early stages of viral infection to block the entry of enveloped viruses into host cells by interacting with the lipid bilayer of the viral envelope.

[0054] Based on this discovery, the inventors decided to synthesize a series of derivatives with similar structures in order to better study the antiviral effects of these compounds on other enveloped viruses. Therefore, the commercial raw material protoporphyrin (PPIX) with porphyrin compound structure has become a better synthetic starting point molecule. The inventor intends to improve the combination of protoporphyri...

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Abstract

The invention discloses the application of protoporphyrin derivatives in the preparation of an enveloped virus blocking agent. The inventors found that protoporphyrin and its derivatives have broad-spectrum antiviral activity against influenza viruses including LASV, MERS, Ebola, SARS-CoV-2, and a series of different subtypes in vitro experiments, and the half inhibitory concentration is between Between 0.91~1.88μM. The possible mechanism is the biophysical interaction with the envelope lipids of enveloped viruses, thereby inhibiting the formation of a negative bending configuration of the envelope lipids and blocking the fusion between the virus envelope and the host cell membrane. At the same time, the in vivo model of mice infected with A / Puerto Rico / 8 / 34 (H1N1) virus strain was initially used to verify the antiviral effect of protoporphyrin. The results showed that the survival rate and survival time of mice in the administration group were significantly improved. improve. These research results suggest that the inventors can use protoporphyrin as a lead compound to establish an antiviral drug targeting the viral envelope to prevent and treat infectious diseases caused by enveloped virus infection.

Description

technical field [0001] The invention relates to a new application of a class of compounds, in particular to the application of protoporphyrin derivatives in the preparation of enveloped virus blocking agents. Background technique [0002] New highly pathogenic infectious diseases, such as Severe Acute Respiratory Syndrome (SARS), Avian Influenza (AI), Middle East Respiratory Syndrome (MERS), Ebola virus (Ebola) infection, and The COVID-19 caused by the popular SARS-CoV-2 has greatly endangered public health, leading to the urgent need to develop new and effective drugs to deal with the outbreak of such viral infectious diseases. It is worth noting that most of these viruses are enveloped RNA viruses, and about one-third of the currently circulating or recurrent viruses are enveloped RNA viruses. Therefore, drugs with broad-spectrum antiviral activity can be developed by targeting the conserved components in the life process of these viruses. [0003] From a structural poin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/555A61K31/409A61P31/14A61P31/16A61P31/18A61P31/20
CPCA61K31/555A61K31/409A61P31/14A61P31/16A61P31/18A61P31/20Y02A50/30
Inventor 何坚潘晓彦陆盛胜陈黛蔚
Owner 广州肽山生物科技有限公司
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