Professor Youyou Tu discovered that the plant Artemisia annua had been used in many traditional Chinese medicine recipes for the treatment of malaria. Using historical texts to devise an extraction method, Tu was able to isolate artemisinin from the plant leaves. This compound was highly effective in killing Plasmodium, a malaria-carrying parasite, in various animal models. Since this finding, artemisinin and its derivatives have been used successfully to reduce the mortality rate of malaria infection by nearly half worldwide. Artemisinin is thought to kill parasites by increasing levels of reactive oxygen species and inducing oxidative stress.
Professor Satoshi Ōmura used his background in natural product isolation to isolate and characterize a new strain of Streptomyces. This new strain was found in soil near a golf course in Japan and upon characterization, was found to exhibit antimicrobial activity. The bacterial culture was sent to Dr. William C. Campbell to explore its efficacy in animal models of parasitic infection. After Ōmura refined the culturing conditions for the bacteria, Campbell characterized the active component avermectin B1. A semi-synthetic derivative of this compound, ivermectin, was examined in further animal and clinical studies, showing efficacy against a variety of worms and nematodes. Although the mechanism of action is unknown, it is thought to involve glutamate-gated chloride channels and GABA-activated chloride channels.
For more information on the 2015 Nobel Prize in Medicine, click here
LKT carries several avermectins and artemisinin-related compounds! For more information on these, please click the representative links below.
- A6970 Artemether
- A6978 Artemisinin (Qinghaosu)
- A6982 Artesunate
- A6979 Dihydroartemisinin
- A0501 Abamectin
- E4902 Emamectin B1 Benzoate
- E6470 Eprinomectin
- I8618 Ivermectin
Estrada-Mondragon A, Lunch JW. Functional characterization of ivermectin binding sites in α1β2γ2L GABA(A) receptors. Front Mol Neurosci. 2015 Sep 25;8:55. PMID: 26441518.
Ōmura S. Microbial metabolites: 45 years of wandering, wondering and discovering. Tetrahedron. 2011; 67: 6420-59.
Cui L, Su X. Discovery, mechanisms of action and combination therapy of artemisinin. Expert Rev Anti Infect Ther. 2009 Oct; 7(8): 999-1013. PMID: 19803708
Tu YY. The constituents of young Artemisia annua. Zhong Yao Tong Bao. 1985 Sep;10(9):35-6, 18. PMID: 2935314.