Molecules (Sep 2023)

Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development

  • Camilla Pecoraro,
  • Francesca Terrana,
  • Giovanna Panzeca,
  • Barbara Parrino,
  • Stella Cascioferro,
  • Patrizia Diana,
  • Elisa Giovannetti,
  • Daniela Carbone

DOI
https://doi.org/10.3390/molecules28186450
Journal volume & issue
Vol. 28, no. 18
p. 6450

Abstract

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The marine environment is an excellent source of molecules that have a wide structural diversity and a variety of biological activities. Many marine natural products (MNPs) have been established as leads for anticancer drug discovery. Most of these compounds are alkaloids, including several chemical subclasses. In this review, we focus on the bis-indolyl alkaloid Nortopsentins and their derivatives with antiproliferative properties. Nortopsentins A–C were found to exhibit in vitro cytotoxicity against the P388 murine leukaemia cell line. Their structural manipulation provided a wide range of derivatives with significant anti-tumour activity against human cell lines derived from different cancer types (bladder, colon, gastric, CNS, liver, lung, breast, melanoma, ovarian, pancreatic, prostate, pleural mesothelioma, renal, sarcoma, and uterus). In vivo assays on animal models also proved that Nortopsentins and related bis-indolyl compounds have potent anti-inflammatory activity. These remarks set the foundation for future investigations into the development of new Nortopsentin derivatives as new anticancer and anti-inflammatory agents.

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