Probing the possible molecular origin of the highly selective toxicity of antimalarial peroxide qinghaosu (artemisinin)

Yikang Wu; He-Hua Liu

doi:10.1021/tx034133k

Probing the possible molecular origin of the highly selective toxicity of antimalarial peroxide qinghaosu (artemisinin)

Chem Res Toxicol. 2003 Oct;16(10):1202-6. doi: 10.1021/tx034133k.

Authors

Yikang Wu¹, He-Hua Liu

Affiliation

¹ State Key Laboratory of Bio-Organic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, China. yikangwu@mail.sioc.ac.cn

PMID: 14565761
DOI: 10.1021/tx034133k

Abstract

The radicals derived from qinghaosu (artemisinin) showed strong tendency for intramolecular reactions and thus are unlikely to cause so much damage to cells as simple alkyl radicals, giving a clue to the extraordinarily low toxicity of this radical precursor at therapeutic doses.

Publication types

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

MeSH terms

Animals
Antimalarials / administration & dosage
Antimalarials / chemistry*
Antimalarials / toxicity*
Artemisinins / administration & dosage
Artemisinins / chemistry*
Artemisinins / toxicity*
Lethal Dose 50
Mice
Molecular Structure
Peroxides / chemistry
Rats
Sesquiterpenes / administration & dosage
Sesquiterpenes / chemistry*
Sesquiterpenes / toxicity*
Structure-Activity Relationship

Substances

Antimalarials
Artemisinins
Peroxides
Sesquiterpenes
artemisinin