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1.
Int J Mol Sci ; 22(23)2021 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-34884795

RESUMO

Compounds of natural origin, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovering new medicines. In this review, we summarize the naturally occurring ellagitannins, sanguiins, which are bioactive constituents of various traditional medicinal plants, especially from the Rosaceae family. In-depth studies of sanguiin H-6 as an antimicrobial, antiviral, anticancer, anti-inflammatory, and osteoclastogenesis inhibitory agent have led to potent drug candidates. In addition, recently, virtual screening studies have suggested that sanguiin H-6 might increase resistance toward SARS-CoV-2 in the early stages of infection. Further experimental investigations on ADMET (absorption, distribution, metabolism, excretion, and toxicity) supplemented with molecular docking and molecular dynamics simulation are still needed to fully understand sanguiins' mechanism of action. In sum, sanguiins appear to be promising compounds for additional studies, especially for their application in therapies for a multitude of common and debilitating ailments.


Assuntos
Antivirais/química , Antivirais/farmacologia , Taninos Hidrolisáveis/química , Taninos Hidrolisáveis/farmacologia , Animais , Antifúngicos/química , Antifúngicos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Farmacocinética , Rosaceae/química , SARS-CoV-2/efeitos dos fármacos , Tratamento Farmacológico da COVID-19
2.
J Enzyme Inhib Med Chem ; 36(1): 1016-1028, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33980119

RESUMO

Elastase is a proteolytic enzyme belonging to the family of hydrolases produced by human neutrophils, monocytes, macrophages, and endothelial cells. Human neutrophil elastase is known to play multiple roles in the human body, but an increase in its activity may cause a variety of diseases. Elastase inhibitors may prevent the development of psoriasis, chronic kidney disease, respiratory disorders (including COVID-19), immune disorders, and even cancers. Among polyphenolic compounds, some flavonoids and their derivatives, which are mostly found in herbal plants, have been revealed to influence elastase release and its action on human cells. This review focuses on elastase inhibitors that have been discovered from natural sources and are biochemically characterised as flavonoids. The inhibitory activity on elastase is a characteristic of flavonoid aglycones and their glycoside and methylated, acetylated and hydroxylated derivatives. The presented analysis of structure-activity relationship (SAR) enables the determination of the chemical groups responsible for evoking an inhibitory effect on elastase. Further study especially of the in vivo efficacy and safety of the described natural compounds is of interest in order to gain better understanding of their health-promoting potential.


Assuntos
Inibidores Enzimáticos/farmacologia , Flavonoides/farmacologia , Elastase de Leucócito/antagonistas & inibidores , Neutrófilos/enzimologia , COVID-19/metabolismo , Inibidores Enzimáticos/química , Flavonoides/química , Humanos , Elastase de Leucócito/metabolismo , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Neutrófilos/efeitos dos fármacos , Relação Estrutura-Atividade , Tratamento Farmacológico da COVID-19
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