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Molecules 2016, 21(11), 1530; doi:10.3390/molecules21111530

The Chemistry and Pharmacology of Citrus Limonoids

1
Department of Chemistry ”U. Shiff”, University of Florence, Via della Lastruccia 3, Florence 50019, Italy
2
Department of Pharmacy-Drug Sciences, University of Studies of Bari Aldo Moro, Via E. Orabona n. 4, Bari 70126, Italy
3
Pharmacognosy Research Laboratories & Herbal Analysis Services, University of Greenwich, Central Avenue, Charham-Maritime, Kent ME4 4TB, UK
*
Authors to whom correspondence should be addressed.
Received: 17 October 2016 / Accepted: 10 November 2016 / Published: 13 November 2016
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Abstract

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. View Full-Text
Keywords: citrus limonoids; tetranortriterpenoids; lead compound; structure-activity relationships; ligand efficiency metrics; developability; antimicrobial; anticancer; antioxidant; antiinflammatory; insecticidal; antidiabetic citrus limonoids; tetranortriterpenoids; lead compound; structure-activity relationships; ligand efficiency metrics; developability; antimicrobial; anticancer; antioxidant; antiinflammatory; insecticidal; antidiabetic
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MDPI and ACS Style

Gualdani, R.; Cavalluzzi, M.M.; Lentini, G.; Habtemariam, S. The Chemistry and Pharmacology of Citrus Limonoids. Molecules 2016, 21, 1530.

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