Abstract
For years, fungi have served as repositories of bioactive secondary metabolites that form the backbone of many existing drugs. With the global rise in infections associated with antimicrobial resistance, in addition to the growing burden of non-communicable disease, such as cancer, diabetes and cardiovascular ailments, the demand for new drugs that can provide an improved therapeutic outcome has become the utmost priority. The exploration of microbes from understudied and specialized niches is one of the promising ways of discovering promising lead molecules for drug discovery. In recent years, a special class of plant-associated fungi, namely, fungal endophytes, have emerged as an important source of bioactive compounds with unique chemistry and interesting biological activities. The present review focuses on endophytic fungi and their classification, rationale for selection and prioritization of host plants for fungal isolation and examples of strategies that have been adopted to induce the activation of cryptic biosynthetic gene clusters to enhance the biosynthetic potential of fungal endophytes.
Highlights
Natural products, known as secondary metabolites (SMs), are a diverse group of mainly low-molecular-weight and structurally diverse chemical entities that are produced by almost all living organisms, but mostly by microbes [1]
Prospects Endophytic fungi have emerged as promising resources with enormous potential in drug discovery
With only a small fraction of the more than 1 million estimated fungal endophytes investigated for their biosynthetic capacity, fungal endophytes remain a largely understudied resource for the discovery novel bioactive molecules
Summary
Known as secondary metabolites (SMs), are a diverse group of mainly low-molecular-weight and structurally diverse chemical entities that are produced by almost all living organisms, but mostly by microbes [1]. While plants have a long history as a source of beneficial SMs, microorganisms have played a key role in the evolution of drug discovery due to their impressive diversity, ease of growth and amenability to genetic manipulation. In the early days of microbial-based drug discovery, the soil microbiota was the principal source of bioactive compounds [3,4]. With the increase in the rate of rediscovery of known compounds from soil microbes, there has been a need to widen the horizon in search of new sources of microbes with greater potential for discovery of novel therapeutic candidates. Already, fascinating compounds with great therapeutic value such as anticancer agents, antibiotics, antiviral, antidiabetic and immunosuppressive compounds have been isolated from these largely untapped microbes [5,6,7,8]
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