Abstract

The indole scaffold is one of the most important heterocyclic ring systems for pharmaceutical development, and serves as an active moiety in several clinical drugs. Fungi derived from marine origin are more liable to produce novel indole-containing natural products due to their extreme living environments. The indole alkaloids from marine fungi have drawn considerable attention for their unique chemical structures and significant biological activities. This review attempts to provide a summary of the structural diversity of marine fungal indole alkaloids including prenylated indoles, diketopiperazine indoles, bisindoles or trisindoles, quinazoline-containing indoles, indole-diterpenoids, and other indoles, as well as their known biological activities, mainly focusing on cytotoxic, kinase inhibitory, antiinflammatory, antimicrobial, anti-insecticidal, and brine shrimp lethal effects. A total of 306 indole alkaloids from marine fungi have been summarized, covering the references published from 1995 to early 2021, expecting to be beneficial for drug discovery in the future.

Highlights

  • IntroductionThe indole fragment is a valuable unit in a wide range of clinical drugs for treating various diseases, such as sunitinib (anticancer), nintedanib (anti-idiopathic pulmonary fibrosis), reserpine (antihypertension), indomethacin (antiinflammation), amedalin (antidepression), atevirdine (antihuman immunodeficiency virus), zafirlukast (antiasthma), etc. (►Fig. 1).[1,2,3,4,5,6,7] This ring system is one of the most important heterocycles for pharmaceutical development[8,9] and widely distributed in bioactive heterocyclic natural products.[10]

  • The indole fragment is a valuable unit in a wide range of clinical drugs for treating various diseases, such as sunitinib, nintedanib, reserpine, indomethacin, amedalin, atevirdine, zafirlukast, etc. (►Fig. 1).[1,2,3,4,5,6,7] This ring system is one of the most important heterocycles for pharmaceutical development[8,9] and widely distributed in bioactive heterocyclic natural products.[10]

  • We reviewed the chemical diversity and biological properties of marine fungal indole alkaloids, expecting to provide clear evidence that these metabolites possess potential of application as lead compounds in the drug innovation and discovery

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Summary

Introduction

The indole fragment is a valuable unit in a wide range of clinical drugs for treating various diseases, such as sunitinib (anticancer), nintedanib (anti-idiopathic pulmonary fibrosis), reserpine (antihypertension), indomethacin (antiinflammation), amedalin (antidepression), atevirdine (antihuman immunodeficiency virus), zafirlukast (antiasthma), etc. (►Fig. 1).[1,2,3,4,5,6,7] This ring system is one of the most important heterocycles for pharmaceutical development[8,9] and widely distributed in bioactive heterocyclic natural products.[10]. (►Fig. 1).[1,2,3,4,5,6,7] This ring system is one of the most important heterocycles for pharmaceutical development[8,9] and widely distributed in bioactive heterocyclic natural products.[10] The marine fungi are a rich underexploited source to produce novel indole-containing secondary metabolites for drug discovery, due to their extreme marine living conditions.[11,12,13,14] the indole alkaloids from marine fungi have drawn considerable attention for their unique chemical structures and significant biological activities.[13,15,16] In the light of the increasing attention paid on the marine fungal indoles, it is necessary to give a comprehensive summary on these indoles from the specific source. We reviewed the chemical diversity and biological properties of marine fungal indole alkaloids, expecting to provide clear evidence that these metabolites possess potential of application as lead compounds in the drug innovation and discovery

Marine Fungal Indole Alkaloids
Conclusion
Aspergillus versicolor
Cytotoxicity Cytotoxicity Inhibitory against drug efflux Cytotoxicity
Penicillium janthinellum Biourge Penicillium citrinum
Antibiofilm formation Antimicrobial effect
Findings
Antimicrobial effect
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