Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7041-4. doi: 10.1016/j.bmcl.2011.09.097. Epub 2011 Oct 1.

Abstract

From the methanol extract of the bulbs of Pancratium illyricum L., three phenanthridine type alkaloids, ungeremine (1), (-)-lycorine (2) and (+)-vittatine (3) were isolated. For the evaluation of their anticancer and antibacterial potential, compounds 1-3 were tested against human (I, IIα) and bacterial (IA, IV) topoisomerases. Our data demonstrated that ungeremine impairs the activity of both, human and bacterial topoisomerases. Remarkably, ungeremine was found to largely increments the DNA cleavage promoted by bacterial topoisomerase IA, a new target in antimicrobial chemotherapy.

MeSH terms

  • Amaryllidaceae Alkaloids / pharmacology*
  • Animals
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Bacteria* / drug effects
  • Bacteria* / enzymology
  • Bacterial Proteins / metabolism
  • Drug Delivery Systems
  • Humans
  • Indolizines / pharmacology*
  • Inhibitory Concentration 50
  • Liliaceae / chemistry
  • Models, Molecular
  • Molecular Structure
  • Topoisomerase I Inhibitors / chemistry
  • Topoisomerase I Inhibitors / pharmacology*
  • Topoisomerase II Inhibitors / chemistry
  • Topoisomerase II Inhibitors / pharmacology*

Substances

  • Amaryllidaceae Alkaloids
  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Bacterial Proteins
  • Indolizines
  • Topoisomerase I Inhibitors
  • Topoisomerase II Inhibitors
  • ungeremine