Synthetic chemistry fuels interdisciplinary approaches to the production of artemisinin

Nat Prod Rep. 2015 Mar;32(3):359-66. doi: 10.1039/c4np00113c.

Abstract

In the developing world, multi-drug resistant malaria caused by the parasite Plasmodium falciparum is an epidemic that claims the lives of 1-3 million people per year. Artemisinin, a naturally occurring small molecule that has seen little resistance from malarial parasites, is a valuable weapon in the fight against this disease. Several easily accessible artemisinin derivatives, including artesunate and artemether, display potent antimalarial activity against drug-resistant malaria strains; however, the global supply of artemisinin from natural sources alone remains highly inconsistent and unreliable. As a result, several approaches to artemisinin production have been developed, spanning areas such as total synthesis, flow chemistry, synthetic biology, and semi-synthesis. This review highlights achievements in all areas, in addition to the interplay between synthetic biology and synthetic chemistry that has fueled the recent industrial-scale production of artemisinin.

Publication types

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

MeSH terms

  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology
  • Artemether
  • Artemisinins / chemical synthesis*
  • Artemisinins / chemistry
  • Artemisinins / pharmacology
  • Artesunate
  • Drug Resistance, Microbial / drug effects
  • Malaria / drug therapy*
  • Molecular Structure
  • Plasmodium falciparum / drug effects

Substances

  • Antimalarials
  • Artemisinins
  • Artesunate
  • artemisinin
  • Artemether