Qinghaosu (Artemisinin): an Antimalarial Drug from China

Abstract

The herb Artemisia annua has been used for many centuries in Chinese traditional medicine as a treatment for fever and malaria. In 1971, Chinese chemists isolated from the leafy portions of the plant the substance responsible for its reputed medicinal action. This compound, called qinghaosu (QHS, artemisinin), is a sesquiterpene lactone that bears a peroxide grouping and, unlike most other antimalarials, lacks a nitrogen-containing heterocyclic ring system. The compound has been used successfully in several thousand malaria patients in China, including those with both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum . Derivatives of QHS, such as dihydroqinghaosu, artemether, and the water-soluble sodium artesunate, appear to be more potent than QHS itself. Sodium artesunate acts rapidly in restoring to consciousness comatose patients with cerebral malaria. Thus QHS and its derivatives offer promise as a totally new class of antimalarials.

Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

“…Artemisinin (Qinghaosu) is a sesquiterpene 1, 2, 4-trioxane (sesquiterpene lactone endoperoxide) isolated from the Chinese medicinal herb qinghao (Artemisia annua L.). It has been shown to be an effective antimalarial against chloroquineresistant strains of P. falciparum [14]. This compound and its derivatives, such as artemether (ART), dihydroartemisinin, arteether, and artesunate, are effective against both chloroquineresistant and chloroquine-sensitive strains of P. falciparum, as well as against cerebral malaria [14].…”

“…It has been shown to be an effective antimalarial against chloroquineresistant strains of P. falciparum [14]. This compound and its derivatives, such as artemether (ART), dihydroartemisinin, arteether, and artesunate, are effective against both chloroquineresistant and chloroquine-sensitive strains of P. falciparum, as well as against cerebral malaria [14]. Artemether, a potent rapidly-acting schizonticide is practically insoluble in water.…”

Water deficit effect on the accumulation of biomass and artemisinin in annual wormwood(Artemisia annua L., Asteraceae)

“…The leaves of Artemisia annua (L.) are a rich source of artemisinin, a sesquiterpene lactone used as the raw material for the production of semi-synthetic derivatives that are more stable, bioavailable, and effective against chloroquine-resistant strains of Plasmodium falciparum (Klayman, 1985;Luo and Shen, 1987;Balint, 2001;Enserink, 2005;WHO 2005. Besides its antimalarial activity, artemisinin has proved effective against cancer (Posner et al, 1999;Singh and Lai, 2004;Efferth, 2005), Eimeria spp., Babesia spp., Leishmania spp., Neospora caninum, Trypanosoma brucei rhodesiense (Mishina et al, 2007), and Schistosoma spp.…”

Avaliação da eficácia do artesunato associado à tetraciclina na terapêutica da malária falciparum

“…Em referência à resistência do Plasmodium falciparum, esta já foi amplamente documentada com relação a muitas drogas em diferentes países do mundo 9 10 23 35 . Considerando esta situação, a Organização Mundial da Saúde (OMS) determinou prioritário o desenvolvimento de esquizonticidas sanguíneos de ação rápida derivados da artemisinina para o tratamento da malária grave e/ou complicada e para o controle das cepas multirresistentes de P. falciparum.A medicina tradicional chinesa usou por mais de 2.000 anos, uma planta conhecida como Artemisia annua L, com o propósito de "controlar e reduzir as febres" 17 …”

“…A medicina tradicional chinesa usou por mais de 2.000 anos, uma planta conhecida como Artemisia annua L, com o propósito de "controlar e reduzir as febres" 17 …”