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Published on: October 12, 2012
Non-anticoagulant heparin derivatives for COVID-19 treatment
Min Cao1, Meng Qiao1, Muhammad Sohail1
1School of Food Science and Pharmaceutical Engineering, Nanjing Normal University, Wenyuan Road 1, Nanjing 210023, China.
Insights
Heparin shows promise for treating COVID-19 (coronavirus disease 2019) by inhibiting viral entry and inflammation. However, non-anticoagulant heparin derivatives may offer safer alternatives by targeting specific mechanisms without side effects.
Area of Science:
- Biochemistry
- Virology
- Pharmacology
Background:
- COVID-19 (coronavirus disease 2019), caused by SARS-CoV-2, triggers severe inflammatory responses, particularly in the lungs and kidneys.
- Exogenous heparin has demonstrated potential in mitigating COVID-19 severity through anticoagulant and non-anticoagulant pathways.
- Known heparin drawbacks include structure-activity relationship complexities, contamination risks, and anticoagulant side effects.
Purpose of the Study:
- To explore the therapeutic potential of heparin and its derivatives in managing COVID-19.
- To address the limitations and side effects associated with conventional heparin therapy.
- To investigate non-anticoagulant heparin derivatives as targeted treatments for COVID-19 and other inflammatory conditions.
Main Methods:
- Review of existing evidence on heparin's mechanisms of action in COVID-19.
- Detailed analysis of heparin therapy's drawbacks, including anticoagulant activity and structure-activity relationships.
- Consideration of chemically modified and enzymatically depolymerized heparin derivatives.
Main Results:
- Heparin exhibits multiple non-anticoagulant mechanisms beneficial against COVID-19, such as heparanase inhibition and viral entry blocking.
- Heparin therapy presents significant drawbacks, including potential contamination and undesirable anticoagulant effects.
- Non-anticoagulant heparin derivatives show promise for targeted antiviral and anti-inflammatory effects.
Conclusions:
- Targeting non-anticoagulant mechanisms of heparin offers a promising therapeutic strategy for COVID-19.
- Development of specific non-anticoagulant heparin derivatives could overcome the limitations of traditional heparin therapy.
- Further research into structure-activity relationships of heparin derivatives is crucial for optimizing treatments for COVID-19 and inflammatory disorders.
Abstract:
The ongoing pandemic of COVID-19, caused by the infection of SARS-CoV-2, has generated significant harm to the world economy and taken numerous lives. This syndrome is characterized by an acute inflammatory response, mainly in the lungs and kidneys. Accumulated evidence suggests that exogenous heparin might contribute to the alleviation of COVID-19 severity through anticoagulant and various non-anticoagulant mechanisms, including heparanase inhibition, chemokine and cytokine neutralization, leukocyte trafficking interference, viral cellular-entry obstruction, and extracellular cytotoxic histone neutralization. However, the side effects of heparin and potential drawbacks of administering heparin therapy need to be considered. Here, the current heparin therapy drawbacks were covered in great detail: structure-activity relationship (SAR) mystery, potential contamination, and anticoagulant activity. Considering these unfavorable effects, specific non-anticoagulant heparin derivatives with antiviral activity could be promising candidates to treat COVID-19. Furthermore, a structurally diverse library of non-anticoagulant heparin derivatives, constructed by chemical modification and enzymatic depolymerization, would contribute to a deeper understanding of SAR mystery. In short, targeting non-anticoagulant mechanisms may produce better therapeutic effects, overcoming the side effects in patients suffering from COVID-19 and other inflammatory disorders.
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