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Progress in Chemistry 2018, Vol. 30 Issue (8): 1067-1081 DOI: 10.7536/PC171231 Previous Articles   Next Articles

• Review •

Studies on Structure and Biological Activity of Indole Diketopiperazine Alkaloids

Bin Jia, Yangmin Ma*, Di Chen, Pu Chen, Yan Hu   

  1. Shaanxi Key Laboratory of Chemical Additives for Industry, Shaanxi University of Science and Technology, Xi'an 710021, China
  • Received: Revised: Online: Published:
  • Supported by:
    The work was supported by the Scientific Research Project for Key Laboratory of Shaanxi Province Education Department, China(No.16JS010).
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Indole diketopiperazine alkaloids(Indole DKPs) are natural products isolated from secondary metabolites of endophytic fungi, especially in the genera Aspergillus and Penicillium of the phylum Ascomycota or sac fungi, showing diverse chemical structures, which contain two moieties indole and cyclic dipeptides and are derived from several amino acids, such as L -tryptophan、L -proline and L -alanine. They not only have a class of naturally occurring privileged structures but also exhibit a broad spectrum of biological activities that make them attractive scaffolds for drug discovery. Recently, many studies have shown that the sealkaloids having significant biological activities such as anticancer, antibacterial, immunomodulatory, antioxidant, and insecticidal activities. And the discovery of these activities has spawned numerous investigations into their synthesis. Meanwhile, the discovery of increasing numbers of new indole DKPs have led to an expanding range of bioactivities. The review summarizes briefly the considerable progress on bioactivities of these alkaloids isolated from various fungal strains in recent years. In addition, we also investigate structure-activity relationship of some compounds.The aim is to give an overview to provide useful reference for the extraction, synthesis and drug discovery of these compounds.
Contents
1 Introduction
2 Structure and classification of Indole DKPs
3 Biological activities of Indole DKPs
3.1 Anticancer and antitumor activity
3.2 Antibacterial activity
3.3 Antioxidant activity
3.4 Insecticidal activity
3.5 Other activities
4 Conclusion
Key words: indole diketopiperazine alkaloids, endophytic fungi, secondary metabolites, biological activities

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