Natural Compounds as Therapeutic Agents: The Case of Human Topoisomerase IB

Int J Mol Sci. 2021 Apr 16;22(8):4138. doi: 10.3390/ijms22084138.

Abstract

Natural products are widely used as source for drugs development. An interesting example is represented by natural drugs developed against human topoisomerase IB, a ubiquitous enzyme involved in many cellular processes where several topological problems occur due the formation of supercoiled DNA. Human topoisomerase IB, involved in the solution of such problems relaxing the DNA cleaving and religating a single DNA strand, represents an important target in anticancer therapy. Several natural compounds inhibiting or poisoning this enzyme are under investigation as possible new drugs. This review summarizes the natural products that target human topoisomerase IB that may be used as the lead compounds to develop new anticancer drugs. Moreover, the natural compounds and their derivatives that are in clinical trial are also commented on.

Keywords: cancer; natural products; topoisomerase.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Biological Products / chemistry
  • Biological Products / pharmacology*
  • Biological Products / therapeutic use
  • Clinical Trials as Topic
  • DNA Topoisomerases, Type I / chemistry
  • DNA Topoisomerases, Type I / metabolism
  • Humans
  • Neoplasms / drug therapy*
  • Topoisomerase I Inhibitors / chemistry
  • Topoisomerase I Inhibitors / pharmacology*
  • Topoisomerase I Inhibitors / therapeutic use

Substances

  • Antineoplastic Agents
  • Biological Products
  • Topoisomerase I Inhibitors
  • DNA Topoisomerases, Type I