176652-07-6

Crystalline Solid

Active antimalarial constituent of the tradional Chinese medicinal herb Artemisia annua L., Compositae, which has been known for almost 2000 years as Qinghao. Antimalarial

Artemisinin-d₃ is intended for use as an internal standard for the quantification of artemisinin . Artemisinin is an endoperoxide antimalarial agent with anticancer activity. It reduces the growth of various P. falciparum strains in vitro (IC₅₀s = 3.98-20.36 nM) and reduces parasitemia in mice infected with P. falciparum with a curative dose (CD₅₀) value of 140 mg/kg. It also reduces P. berghei infection in mice (ED₅₀ = 5.6 mg/kg per day). Artemisinin (100-400 μM) induces cell cycle arrest in the G₀/G₁ phase and apoptosis and inhibits growth of SK-N-AS, BE(2)-C, SK-N-DZ, and SHEP1 neuroblastoma cells in a time- and concentration-dependent manner. It also suppresses BE(2)-C cell colony formation in a soft agar assay and reduces tumor growth in a BE(2)-C mouse xenograft model. Formulations containing artemisinin have been used in combination therapies for the treatment of malaria.

Plasmodium

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[1] MONIQUE AKOACHERE. In vitro assessment of methylene blue on chloroquine-sensitive and -resistant Plasmodium falciparum strains reveals synergistic action with artemisinins.[J]. Antimicrobial Agents and Chemotherapy, 2005: 4592-4597. DOI: 10.1128/aac.49.11.4592-4597.2005
[2] SHUNQIN ZHU. Artemisinin reduces cell proliferation and induces apoptosis in neuroblastoma.[J]. Oncology reports, 2014, 32 3: 1094-1100. DOI: 10.3892/or.2014.3323
[3] ANNE ROBERT. The antimalarial drug artemisinin alkylates heme in infected mice.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102 38: 13676-13680. DOI: 10.1073/pnas.0500972102
[4] A.N. CHAWIRA. The effect of combinations of qinghaosu (artemisinin) with standard antimalarial drugs in the suppressive treatment of malaria in mice[J]. Transactions of The Royal Society of Tropical Medicine and Hygiene, 1987, 81 4: Pages 554-558. DOI: 10.1016/0035-9203(87)90404-4