A comprehensive review on the antiviral activities of chalcones

Abstract

Some viral outbreaks have plagued the world since antiquity, including the most recent COVID-19 pandemic. The continuous spread and emergence of new viral diseases have urged the discovery of novel treatment options that can overcome the limitations of currently marketed antiviral drugs. Chalcones are natural open chain flavonoids that are found in various plants and can be synthesised in labs. Several studies have shown that these small organic molecules exert a number of pharmacological activities, including antiviral, anti-inflammatory, antimicrobial and anticancer. The purpose of this review is to provide a summary of the antiviral activities of chalcones and their derivatives on a set of human viral infections and their potential for targeting the most recent COVID-19 disease. Accordingly, we herein review chalcones activities on the following human viruses: Middle East respiratory syndrome coronavirus, severe acute respiratory syndrome coronavirus, human immunodeficiency, influenza, human rhinovirus, herpes simplex, dengue, human cytomegalovirus, hepatitis B and C, Rift Valley fever and Venezuelan equine encephalitis. We hope that this review will pave the way for the design and development of potentially potent and broad-spectrum chalcone based antiviral drugs.

Chalcones: Synthetic Chemistry Follows Where Nature Leads

“…A docking study suggested that the antiviral activity of (190) might depend on its strong binding affinity to tobacco mosaic virus coat protein (TMV-CP). There are several other reports on antiviral properties of synthetic chalcone derivatives available in the literature to date, including a few excellent review articles on this topic [108][109][110].…”

The Unique Australian Flora, A Veritable Pandora’s Pharmacopeia of Compounds with Therapeutic Biomedical Potential: Are the Chalcones the Geni in The Box?

“…Interaction of these flavonoids with ACE2 may also impede the binding of SARS-CoV-2 spike protein and is in line with the anti-viral properties of these compounds [149].The interaction of flavonoids with Mpro, Spike receptor binding domain (Spike-RBD), RNA -dependent RNA polymerase (RdRp or Nsp12), non-structural protein 15 (Nsp15) and the host ACE-2 spike-RBD binding domain have been examined using advanced computation molecular docking techniques. These en-silicoSARS-CoV-2 binding studies indicated that tribuloside, legalon and isosilybin had anti-viral antiinfective properties, warranting further evaluation to determine how effective they are in the inhibition of SARS-CoV-2 infectivity [150].A range of chalcone derivatives have been evaluated using molecular docking methods to assess the effectiveness of these re-purposed compounds on the prevention of the infectivity and replication of SARS-CoV-2 [151][152][153][154][155].…”

Adsorption and selectivity studies of direct and magnetite-cored molecularly imprinted polymers (MIPs and magMIPs) towards chosen chalcones investigated with various analytical methods

“…2 Up to now, chalcones have been postulated for multiple therapeutic effects, especially anticancer, anti-inammatory, antioxidant, antitumor, anti-bacterial, antiviral, and anti-fungal activities. [3][4][5][6][7][8] Moreover, several chalcone-derivatives have been investigated and proved for efficient inhibition of key enzymes responsible for viral replication of SARS-CoV, HIV, HBV, or HCV. 9 The bioactivity of chalcones is undoubtedly based on their structural features, especially the position and the type of substituents in both phenyl rings, such as saturated or unsaturated hydrocarbon groups, halogens atoms, additional aromatic or heteroaromatic rings, bulky cyclopropyl or adamantane domains, as well as hydroxyl, carboxylic or amide groups.…”