review · Molecules
Xanthones are oxygenated heterocyclic compounds found in higher plants, marine organisms, and lower microorganisms, notably within plant families such as Caryophyllaceae, Guttiferae, and Gentianaceae. Structurally characterised by two benzene rings linked by a central gamma-pyrone core, they originate through shikimate-acetate or acetate-malonate biosynthetic pathways. These compounds display structural diversity, categorised by their ring oxidation levels into monomers, dimers, and heterodimers, as well as by their oxygenation patterns and functional groups. Because of these distinct chemical scaffolds, xanthones demonstrate significant biological actions, showing promise as antioxidant, antifungal, antimicrobial, and anticancer agents. Structure-activity relationship studies indicate that specific carbon positions, particularly C-1, C-3, C-6, and C-8, alongside substituents such as prenyl, hydroxyl, glycosyl, furan, and pyran groups, strongly govern their bioactivity. Mapping these relationships supports the identification of lead molecules as potential drug candidates.
Understanding how natural compounds combat disease is essential for therapeutic discovery. Xanthones present versatile chemical frameworks with verified activities against fungi, microbes, and cancer cells. Defining the specific molecular positions and chemical groups responsible for these medicinal effects gives drug developers a clear foundation to optimise natural scaffolds into more potent and targeted treatments for various health conditions.
This research informs early-stage pharmaceutical discovery by highlighting xanthone scaffolds and structure-activity relationships for development as antifungal, antimicrobial, and anticancer drugs. The primary users are medicinal chemists and drug discovery teams screening or designing natural product derivatives. Because the findings focus on structural classifications and lead identification, the work represents foundational, early-stage research that remains distant from clinical application and commercial drug development.
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Xanthones are chemical substances in higher plants, marine organisms, and lower microorganisms. The most prevalent naturally occurring sources of xanthones are those belonging to the families Caryophyllaceae, Guttiferae, and Gentianaceae. Structurally, xanthones (9H xanthan-9-one) are heterocyclic compounds with oxygen and a γ-pyrone component. They are densely packed with a two-benzene ring structure. The carbons in xanthones are numbered from their nucleus and biosynthetic construct. They have mixed shikimate-acetate (higher plants) and acetate-malonate (lower organisms) biosynthetic origins, which influence their classification. Based on the level of oxidation of the C-ring, they are classified into monomers, dimers, and heterodimers. While based on the level of oxygenation or the type of ring residue, they can be categorized into mono-, di-, tri-, tetra-, penta- and hexa-oxygenated xanthones, bis-xanthones, prenylated and related xanthones, xanthonolignoids, and other miscellaneous xanthones. This structural diversity has made xanthones exhibit considerable biological properties as promising antioxidant, antifungal, antimicrobial, and anticancer agents. Structure-activity relationship studies suggest C-1, C-3, C-6, and C-8 as the key positions that influence the biological activity of xanthones. Furthermore, the presence of functional groups, such as prenyl, hydroxyl, glycosyl, furan, and pyran, at the key positions of xanthones, may contribute to their spectrum of biological activity. The unique chemical scaffolds of xanthones, their notable biological activities, and the structure-activity relationships of some lead molecules were discussed to identify lead molecules as possible drug candidates.
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DOI: 10.3390/molecules29174241
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