Pharmacotherapeutics Applications and Chemistry of Chalcone Derivatives

Jagjit Singh Dhaliwa, - and Said Moshawih, - and Khang Wen Goh, - and Mei Jun Loy, - and Sanower Hossain, - and Andi Hermansyah, - and Vijay Kotra, - and Nurolaini Kifli, - and Hui Poh Goh, - and Sachinjeet Kaur Sodhi Dhaliwal, - and Hayati Yassin, - and Long Chiau Ming, - (2022) Pharmacotherapeutics Applications and Chemistry of Chalcone Derivatives. Molecules, 27 (20). pp. 1-24. ISSN 1420-3049

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Official URL: https://www.mdpi.com/1420-3049/27/20/7062

Abstract

Chalcones have been well examined in the extant literature and demonstrated antibacterial, antifungal, anti-inflammatory, and anticancer properties. A detailed evaluation of the purported health benefits of chalcone and its derivatives, including molecular mechanisms of pharmacological activities, can be further explored. Therefore, this review aimed to describe the main characteristics of chalcone and its derivatives, including their method synthesis and pharmacotherapeutics applications with molecular mechanisms. The presence of the reactive α,β-unsaturated system in the chalcone’s rings showed different potential pharmacological properties, including inhibitory activity on enzymes, anticancer, anti-inflammatory, antibacterial, antifungal, antimalarial, antiprotozoal, and anti-filarial activity. Changing the structure by adding substituent groups to the aromatic ring can increase potency, reduce toxicity, and broaden pharmacological action. This report also summarized the potential health benefits of chalcone derivatives, particularly antimicrobial activity. We found that several chalcone compounds can inhibit diverse targets of antibiotic-resistance development pathways; therefore, they overcome resistance, and bacteria become susceptible to antibacterial compounds. A few chalcone compounds were more active than conventional antibiotics, like vancomycin and tetracycline. On another note, a series of pyran-fused chalcones and trichalcones can block the NF-B signaling complement system implicated in inflammation, and several compounds demonstrated more potent lipoxygenase inhibition than NSAIDs, such as indomethacin. This report integrated discussion from the domains of medicinal chemistry, organic synthesis, and diverse pharmacological applications, particularly for the development of new anti-infective agents that could be a useful reference for pharmaceutical scientists.

Item Type: Article
Uncontrolled Keywords: antimicrobial agent; infectious disease; cancer; cardiovascular disease; health benefits; pharmacology
Subjects: R Medicine
R Medicine > RS Pharmacy and materia medica
R Medicine > RS Pharmacy and materia medica > RS1-441 Pharmacy and materia medica
R Medicine > RS Pharmacy and materia medica > RS200-201 Pharmaceutical dosage forms
Divisions: 05. Fakultas Farmasi > Farmasi Komunitas
Creators:
CreatorsNIM
Jagjit Singh Dhaliwa, --
Said Moshawih, --
Khang Wen Goh, --
Mei Jun Loy, --
Sanower Hossain, --
Andi Hermansyah, -NIDN0027098303
Vijay Kotra, --
Nurolaini Kifli, --
Hui Poh Goh, --
Sachinjeet Kaur Sodhi Dhaliwal, --
Hayati Yassin, --
Long Chiau Ming, --
Depositing User: Mr M. Fuad Sofyan
Date Deposited: 26 Apr 2023 06:16
Last Modified: 26 Apr 2023 06:16
URI: http://repository.unair.ac.id/id/eprint/124018
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