Semysinthetic biflavonoid Morelloflavone-7,4′,7″,3‴,4‴-penta-O-butanoyl is a more potent inhibitor of Proprotein Convertases Subtilisin/Kexin PC1/3 than Kex2 and Furin

Souza, Aline Aparecida de; Andrade, Débora Martins de; Siqueira, Fábio da Silva; Iório, Juliana Fortes Di; Veloso, Márcia Paranho; Coelho, Camila; Viegas, Cláudio; Gontijo, Vanessa Silva; Santos, Marcelo Henrique dos; Meneghetti, Maria Cecília Zorél; Nader, Helena B.; Tersariol, Ivarne L.S.; Juliano, Luiz; Juliano, María A.; Júdice, Wagner Alves de Souza

doi:10.1016/j.bbagen.2021.130016

Cited by 2 publications

(1 citation statement)

References 75 publications

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“…The identification of TM-PRSS2 (transmembrane serine protease 2), TMPRSS4 and furin cleavage sites in the Spike glycoprotein, which prime it for fusion with the host cell plasma membrane, have identified further targets of interest in anti-viral strategies. Phytochemical inhibitors of TMPRSS2 and furin have also now been identified [100].…”

Section: Screening For Anti-viral Phytochemicalsmentioning

confidence: 99%

Natural and Semi-Synthetic Flavonoid Anti-SARS-CoV-2 Agents for the Treatment of Long COVID-19 Disease and Neurodegenerative Disorders of Cognitive Decline

Melrose¹,

Smith²

2022

Front. Biosci. (Elite Ed)

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The aim of this review is to highlight the beneficial attributes of flavonoids, a diverse family of widely-distributed polyphenolic phytochemicals that have beneficial cell and tissue protective properties. Phytochemicals are widely distributed in plants, herbs and shrubs used in traditional complimentary medical formulations for centuries. The bioactive components that convey beneficial medicinal effects in these complex herbal preparations are now being identified using network pharmacology and molecular docking procedures that identify their molecular targets. Flavonoids have anti-oxidant, anti-inflammatory, antiviral, antibacterial and anti-cancer properties that have inspired the development of potent multifunctional derivatised flavonoids of improved efficacy. The antiviral properties of flavonoids and the emergence of the severe acute respiratory syndrome (SARS-CoV-2) pandemic has resulted in a resurgence of interest in phytochemicals in the search for efficacious compounds that can prevent viral infection or replication, with many promising plant compounds identified. Promising semi-synthetic flavonoid derivatives have also been developed that inhibit multiple pathological neurodegenerative processes; these offer considerable promise in the treatment of diseases of cognitive decline. Clinical trials are currently being undertaken to evaluate the efficacy of dietary supplements rich in flavonoids for the treatment of virally-mediated diseases. Such trials are expected to identify flavonoids with cell and tissue protective properties that can be harnessed in biomedical applications that may serve as supportive adjunctive procedures to conventional anti-viral drug therapies against diseases such as COVID-19.

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Section: Screening For Anti-viral Phytochemicalsmentioning

confidence: 99%

Natural and Semi-Synthetic Flavonoid Anti-SARS-CoV-2 Agents for the Treatment of Long COVID-19 Disease and Neurodegenerative Disorders of Cognitive Decline

Melrose¹,

Smith²

2022

Front. Biosci. (Elite Ed)

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Morelloflavone as Phytomedicine-An Ethnopharmacological Review on the Therapeutical Properties, Biological Efficacy and Pharmacological Activity

Patel

2023

AIA

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Background: Flavonoids are low molecular weight class secondary metabolites found to be present throughout the plant kingdom. Structurally, flavonoid class phytochemicals consist of C6-C3-C6 chemical structures with different substitution patterns and have drug-like nature. Morelloflavone is a biflavonoid class phytochemical found to be present abundantly in the Garcinia genus. Morelloflavone has been investigated in the scientific field for its numerous pharmacological activities. The present work aims to discuss the scientific progress of health beneficial aspects and pharmacological potential of morelloflavone in medicine. Methods: The purpose of this work is to provide scientific information about the biological potential and health beneficial effects of flavonoids in medicine with special reference to the morelloflavone. In this work, we have collected the scientific data of morelloflavone for the biological potential and pharmacological activities against different types of human illnesses with their mechanism of action from Google, Google Scholar, Science Direct and PubMed and analyzed. Further, the preventive role of morelloflavone against various types of human illnesses and the mechanism of action have also been discussed in the present work. This work will provide up-to-date information on the health beneficial aspects of morelloflavone in medicine for the prevention and treatment of human complications. Results: Morelloflavone exhibited a wide-range of pharmacologic activity in regulating numerous kinds of human disorders. Present work revealed the health beneficial aspects and pharmacological activities of morelloflavone for the prevention and treatment of human disorders due to its anti-microbial, anti-plasmodial, anti-oxidant, anti-atherosclerosis, anti-inflammatory, anti-tumor anti-restenosis, anti-HIV, aphrodisiac, Alzheimer's disease and apoptotic potential in the medicine. Further, its biological potential on phospholipase A2, melanin, kallikreins, monoamine oxidase, aromatase, Eg5 Inhibition and proprotein convertases have been also analyzed in the present work. Analytical data signified the importance of modern analytical tools for the separation and isolation of morelloflavone in medicine. Conclusion: Present work revealed the detailed pharmacological activities of morelloflavone that can be utilized in the future for the development of new pharmacologic agents.

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Semysinthetic biflavonoid Morelloflavone-7,4′,7″,3‴,4‴-penta-O-butanoyl is a more potent inhibitor of Proprotein Convertases Subtilisin/Kexin PC1/3 than Kex2 and Furin

Cited by 2 publications

References 75 publications

Natural and Semi-Synthetic Flavonoid Anti-SARS-CoV-2 Agents for the Treatment of Long COVID-19 Disease and Neurodegenerative Disorders of Cognitive Decline

Natural and Semi-Synthetic Flavonoid Anti-SARS-CoV-2 Agents for the Treatment of Long COVID-19 Disease and Neurodegenerative Disorders of Cognitive Decline

Morelloflavone as Phytomedicine-An Ethnopharmacological Review on the Therapeutical Properties, Biological Efficacy and Pharmacological Activity

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