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The chemistry and pharmacology of citrus limonoids

The chemistry and pharmacology of citrus limonoids

Gualdani, Roberta, Cavalluzzi, Maria, Lentini, Giovanni and Habtemariam, Solomon (2016) The chemistry and pharmacology of citrus limonoids. Molecules, 21 (11):1530. pp. 1-39. ISSN 1420-3049 (Print), 1420-3049 (Online) (doi:

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Citrus limonoids (CLs) are a group of highly oxygenated terpenoid secondary metabolites found mostly in the seeds, fruits and peel tissues of citrus fruits such as lemons, limes, oranges, pumellos, grapefruits, bergamots, and mandarins. Represented by limonin, the aglycones and glycosides of CLs have shown to display numerous pharmacological activities including anticancer, antimicrobial, antioxidant, antidiabetic and insecticidal among others. In this review, the chemistry and pharmacology of CLs are systematically scrutinised through the use of medicinal chemistry tools and structure-activity relationship approach. Synthetic derivatives and other structurally-related limonoids from other sources are include in the analysis. With the focus on literature in the past decade, the chemical classification of CLs, their physico-chemical properties as drugs, their biosynthesis and enzymatic modifications, possible ways of enhancing their biological activities through structural modifications, their ligand efficiency metrics and systematic graphical radar plot analysis to assess their developability as drugs are among those discussed in detail

Item Type: Article
Additional Information: © 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (
Uncontrolled Keywords: Citrus limonoids; Tetranortriterpenoids; Lead compound; Structure-activity relationships; Ligand efficiency metrics; Developability; Antimicrobial; Anticancer; antioxidant; Antiinflammatory; Insecticidal; Antidiabetic
Subjects: Q Science > QD Chemistry
R Medicine > RM Therapeutics. Pharmacology
Faculty / School / Research Centre / Research Group: Faculty of Engineering & Science
Faculty of Engineering & Science > School of Science (SCI)
Last Modified: 05 Sep 2017 11:16

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