Description
Artesunate is a sesquiterpene lactone derived from Artemisia. Artesunate exhibits anticancer chemotherapeutic, antiviral, anti-angiogenic, and anti-parasitic activities. Artemisinins such as artesunate are best known for their antimalarial activity. Artesunate induces G0/G1 phase cell cycle arrest, increases levels of Bax and caspase 3, and decreases levels of Bcl-2, inhibiting tumor growth in animal models of breast cancer. In models of cervical cancer, artesunate inhibits production of prostaglandin E2 (PGE2) and decreases the number of Treg cells, also inhibiting tumor growth. Artesunate induces cell cycle arrest and inhibits replication of Polyoma virus as well. Additionally, this compound inhibits neovascularization and inflammation in corneas, increasing the Bax/Bcl-2 ratio and ROS levels, decreasing the mitochondrial membrane potential, and activating p38 MAPK.
References
Zhang LX, Liu ZN, Ye J, et al. Artesunate exerts an anti-immunosuppressive effect on cervical cancer by inhibiting PGE2 production and Foxp3 expression. Cell Biol Int. 2014 May;38(5):639-46. PMID: 24446394.
Dong HY, Wang ZF. Antitumor effects of artesunate on human breast carcinoma MCF-7 cells and IGF-IR expression in nude mice xenografts. Chin J Cancer Res. 2014 Apr;26(2):200-7. PMID: 24826061.
Sharma BN, Marschall M, Henriksen S, et al. Antiviral effects of artesunate on polyomavirus BK replication in primary human kidney cells. Antimicrob Agents Chemother. 2014 Jan;58(1):279-89. PMID: 24145549.
Cheng R, Li C, Li C, et al. The artemisinin derivative artesunate inhibits corneal neovascularization by inducing ROS-dependent apoptosis in vascular endothelial cells. Invest Ophthalmol Vis Sci. 2013 May 15;54(5):3400-9. PMID: 23611999.
Gomes TC, de Andrade Júnior HF, Lescano SA, et al. In vitro action of antiparasitic drugs, especially artesunate, against Toxoplasma gondii. Rev Soc Bras Med Trop. 2012 Jul-Aug;45(4):485-90. PMID: 22930046.
Haynes RK, Chan WC, Wong HN, et al. Facile oxidation of leucomethylene blue and dihydroflavins by artemisinins: relationship with flavoenzyme function and antimalarial mechanism of action. ChemMedChem. 2010 Aug 2;5(8):1282-99. PMID: 20629071.