Antiprotozoal alkaloid principles of the plant family Amaryllidaceae

Bioorg Med Chem Lett. 2019 Oct 15;29(20):126642. doi: 10.1016/j.bmcl.2019.126642. Epub 2019 Aug 26.

Abstract

Protozoan-borne diseases are prominent amongst diseases caused by parasites. Given their alarming morbidity and mortality statistics, there is ever growing interest in new therapies against these diseases. Whilst synthetic drugs such as benznidazole and melarsoprol have had a profound influence on the clinical setup, there has been significant interest in the phytochemical platform to also deliver such drug candidates. The plant family Amaryllidaceae is recognizable for its isoquinoline alkaloids, which exhibit attractive molecular architectures and interesting biological properties. This survey focuses on the antiprotozoal activities of 73 of such substances described in 18 different species of the Amaryllidaceae. Of these, 2-O-acetyllycorine was identified as the most potent (IC50 0.15 μg/mL against Trypansoma brucei brucei). Also considered are structure-activity relationships which have served to modulate activities, as well as the plausible mechanisms that underpin these effects and afford insight to the Amaryllidaceae alkaloid antiprotozoal pharmacophore.

Keywords: Alkaloid; Amaryllidaceae; Antiparasitic; Antiprotozoal; Medicinal plant.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amaryllidaceae / chemistry*
  • Amaryllidaceae Alkaloids / chemistry*
  • Amaryllidaceae Alkaloids / pharmacology
  • Antiprotozoal Agents / chemistry*
  • Antiprotozoal Agents / pharmacology
  • Diterpenes / chemistry
  • Drug Evaluation, Preclinical
  • Humans
  • Isoquinolines / chemistry*
  • Isoquinolines / pharmacology
  • Molecular Structure
  • Phytochemicals / chemistry
  • Phytochemicals / pharmacology
  • Plant Extracts / chemistry*
  • Plant Extracts / pharmacology
  • Structure-Activity Relationship
  • Trypanosoma brucei brucei / drug effects

Substances

  • 2-O-acetylorochrine
  • Amaryllidaceae Alkaloids
  • Antiprotozoal Agents
  • Diterpenes
  • Isoquinolines
  • Phytochemicals
  • Plant Extracts
  • isoquinoline