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Vinca alkaloids and analogues as anti-cancer agents: Looking back, peering ahead

Emanuela Martino1, Giuseppe Casamassima2, Sonia Castiglione2

  • 1Department of Earth and Environmental Sciences, University of Pavia, Via S. Epifanio 14, 27100 Pavia, Italy.

Bioorganic & Medicinal Chemistry Letters
|August 21, 2018
PubMed

Insights

Vinca alkaloids (VAs), derived from natural sources, are crucial microtubule-targeting agents (MTAs) for cancer treatment. This review covers their mechanisms, properties, and advancements in overcoming drug resistance.

Area of Science:

  • Oncology
  • Pharmacology
  • Natural Products Chemistry

Background:

  • Cancer remains a significant global health burden, necessitating effective antiproliferative therapies.
  • Natural products are a vital source of anticancer agents, contributing to 60% of current drugs.
  • Microtubule-targeting agents (MTAs) show high therapeutic potential by disrupting cancer cell division.

Purpose of the Study:

  • To provide a comprehensive review of Vinca alkaloids (VAs), a key class of MTAs.
  • To discuss the mechanism of action, pharmacokinetics, therapeutic relevance, and toxicological profile of VAs.
  • To explore technological strategies for improving VA properties and overcoming drug resistance, including new derivative discovery.

Main Methods:

  • Literature review of existing research on Vinca alkaloids.
  • Analysis of VAs' mechanism of action, focusing on interference with mitotic division.
  • Examination of pharmacokinetic properties, therapeutic efficacy, and toxicological data.

Main Results:

  • Vinca alkaloids are among the earliest developed and clinically approved MTAs for treating hematological and lymphatic neoplasms.
  • VAs exert their antiproliferative effects by disrupting microtubule dynamics, crucial for cancer cell mitosis.
  • The review highlights the established therapeutic value alongside the toxicological considerations of VAs.

Conclusions:

  • Vinca alkaloids remain essential in cancer chemotherapy, particularly for hematological malignancies.
  • Ongoing research focuses on enhancing VA pharmacological profiles and circumventing drug resistance through technological innovations.
  • The discovery of novel VA derivatives holds promise for future cancer treatment strategies.
Keywords:
Antimitotic agentsEmerging vinblastine-related compoundsMicrotubule-targeting agentsVinca alkaloids

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