Diverse host-associated fungal systems as a dynamic source of novel bioactive anthraquinones in drug discovery: Current status and future perspectives

Graphical abstract

Highlights

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  Diversity and distribution of host-living fungi producing AQs in the terrestrial ecosystem are assembled.

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  AQs biosynthesis and their SAR are elucidated to guide the approaches in novel drugs design and development.

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  Several examples of true endophytic fungi producing AQs like their different host plants have been reported as interesting alternative sources of drugs.

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  The review recapitulates the novel AQs with rare chemical skeleton that could open future venues for investigation of their biological activities.

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  Lichens are assembled as unique source of several bioactive classes of AQs.

Abstract

Background

Despite, a large number of bioactive anthraquinones (AQs) isolated from host-living fungi, only plant-derived AQs were introduced in the global consumer markets. Host-living fungi represents renewable and extendible resources of diversified metabolites to be exploited for bioactives production. Unique classes of AQs from fungi include halogenated and steroidal AQs, and absent from planta are of potential to explore for biological activity against urging diseases such as cancer and multidrug-resistant pathogens. The structural diversity of fungal AQs, monomers, dimers, trimers, halogenated, etc… results in a vast range of pharmacological activities.

Aim of review

The current study capitalizes on uncovering the diversity and distribution of host-living fungal systems producing AQs in different terrestrial ecosystems ranging from plant endophytes, lichens, animals and insects. Furthermore, the potential bioactivities of fungal derived AQs i.e., antibacterial, antifungal, antiviral (anti-HIV), anticancer, antioxidant, diuretic and laxative activities are assembled in relation to their structure activity relationship (SAR). Analyzing for structure–activity relationship among fungal AQs may facilitate bioengineering of more potential analogues. Withal, elucidation of AQs biosynthetic pathways in fungi is discussed from different fungal hosts to open up new possibilities for potential biotechnological applications. Such comprehensive review unravels terrestrial host-living fungal systems as a treasure trove in drug discovery, in addition to future perspectives and trends for their exploitation in pharmaceutical industries.

Key Scientific Concepts of Review

Such comprehensive review unravels terrestrialhost-living fungal systems as a treasure trove in drug discovery, in addition to future perspectives and trends for their exploitation in pharmaceutical industries.