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Radiolabeling and Quantification of Cellular Levels of Phosphoinositides by High Performance Liquid Chromatography-coupled Flow Scintillation
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Phakellistatins: An Underwater Unsolved Puzzle.

Alessandra Meli1, Consiglia Tedesco2, Giorgio Della Sala3

  • 1Department of Chemistry and Biology "A. Zambelli", University of Salerno, Via Giovanni Paolo II, 132-84081 Fisciano (SA), Italy. alemeli87@gmail.com.

Marine Drugs
|March 25, 2017
PubMed
Summary

Marine natural products called phakellistatins (1-19) are proline-rich cyclopeptides with cytotoxic properties. This summary covers their discovery, synthesis, and challenges in reproducing their biological activity.

Keywords:
marine spongepeptide synthesispharmacological activityproline-rich cyclopeptide

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Area of Science:

  • Marine natural product chemistry
  • Medicinal chemistry
  • Organic synthesis

Background:

  • Phakellistatins are a family of nineteen cytotoxic proline-rich cyclopeptides isolated from marine sources.
  • These natural products exhibit significant biological activity, making them attractive targets for research.

Purpose of the Study:

  • To provide a critical summary of the discovery and characterization of phakellistatins 1-19.
  • To review the isolation, structural elucidation, and biological properties of these marine cyclopeptides.
  • To discuss the total syntheses and challenges in the reproducibility of their cytotoxic activity.

Main Methods:

  • Literature review and critical analysis of published data on phakellistatins.
  • Summary of isolation and structural determination techniques (e.g., NMR, Mass Spectrometry).
  • Overview of synthetic strategies employed in total synthesis and biological assays.

Main Results:

  • Nineteen members of the phakellistatin family have been identified and characterized.
  • Diverse structural features and sizes of these natural macrocycles have been elucidated.
  • Total synthesis efforts have been reported, alongside challenges in consistent cytotoxic activity assessment.

Conclusions:

  • Phakellistatins represent a significant class of marine-derived cytotoxic agents.
  • Understanding their structure-activity relationships and synthetic accessibility is crucial.
  • Further research is needed to address the reproducibility issues in their biological evaluation.