Mini-review
A review of anti-infective and anti-inflammatory chalcones

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Abstract

Chalcones, considered as the precursors of flavonoids and isoflavonoids, are abundant in edible plants, and have also been shown to display a diverse array of pharmacological activities. The purpose of this review is to provide an overview of the pharmacological activity of synthetic and naturally occurring chalcones. This review is complementary to earlier reviews and covers more recent reports of antimicrobial activity of chalcones (antibacterial and antifungal), as well as antileishmanial, antimalarial, antiviral and anti-inflammatory activities of these compounds.

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This review covers recent reports of antimicrobial (antibacterial and antifungal), antileishmanial, antimalarial, antiviral as well as anti-inflammatory activities of (E)-chalcones.

Section snippets

Antibacterial properties

The antibacterial activity of chalcones is being increasingly documented. Many research groups either isolated and identified the structure of chalcones that possess antibacterial activity, or synthesized or modified natural chalcones. The bactericidal effects have been related to the ability of the α,β-unsaturated ketone to undergo a conjugated addition to a nucleophilic group like a thiol group in an essential protein.

Liquorice (root and rhizome of Glycyrrhiza spp.) is currently used in the

Antileishmanial properties

Leishmaniasis is a group of prevalent diseases caused by protozoan parasites belonging to the genus Leishmania. Recently, a series of synthetic and naturally occurring chalcone derivatives have been reported to be potential agents against Leishmania in a number of in vitro and in vivo assays. Though a large number of synthetic compounds have been tested, licochalcone A still remains one of the few naturally occurring chalcones under investigation. Various species of the protozoan parasite

Antimalarial properties

Plasmodium falciparum and Plasmodium vivax are the two major human malaria parasites. P. falciparum is responsible for most deaths, and it has developed resistance to nearly all available drugs. No wonder that the antimalarial activity of chalcones has generated great interest. Many chalcones have been described for their high antimalarial activity, probably as a result of a Michael addition of nucleophilic species to the double bond of the enone [44], [45].

Licochalcone A 1A isolated from

Antifungal properties

Since dermatophytes are a group of fungi which characteristically infect the keratinized areas of the body and dermatomycoses are very difficult to eradicate, it is very interesting to note that chalcone derivatives showed activity against dermatophytes and not against other types of fungi. Lopez et al. [60] tested chalcones 6164 against a panel of human opportunistic pathogenic fungi, using the agar dilution method. Regarding the influence of the substituents on ring A, an interesting

Antiviral properties

Antiviral properties of chalcones were discovered in studies on inhibition of plant viruses and human rhinoviruses. The variable antiviral activity of chalcones suggests that the activity of each chalcone depends on specific substitution patterns. A hydroxy and methoxy substituted chalcone derivatives were investigated by Onyilagha et al. [68], [69] for activity against tomato ringspot nepovirus (ToRSV) infectivity. Hydroxylation of ring B at 2′,3′,4′, and ring A at C-4-positions activates

Anti-inflammatory properties

The inhibition of prostaglandin E2 (PGE2) and nitric oxide (NO) production has been proposed as a potential therapy for different inflammatory disorders. Large amounts of NO may lead to tissue damage. In inflammatory diseases such as rheumatoid arthritis, excessive NO production by activated macrophages has been observed. Therefore, it would be interesting to develop potent and selective inhibitors of NO for potential therapeutic use.

Herencia et al. [79], [80], [81], [82] tested a series of

Conclusions

Chalcone is a unique template that is associated with several biological activities. The radical quenching properties of the phenolic groups present in many chalcones have raised interest in using the compounds or chalcone rich plant extracts as drugs or food preservatives. The anti-infective and anti-inflammatory activities of a variety of chalcones have been presented in this review article. The literature is analysed to provide a meaningful overview of the structural requirements for

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