一般描述 | Artesunate(青蒿琥酯) is a water-soluble, semi-synthetic derivative of the sesquiterpine lactone artemisinin with anti-malarial, anti-shistosomiasis, antiviral, and potential anti-neoplastic activities. |
生物活性/药理作用 | Artesunate is an artemisinin drug capable of killing all erythrocytic stages of the malaria parasite including the ring stage, late schizonts, and the gametocytes responsible for transmission of
malaria [L891]. It also increases splenic clearance of infected erythrocytes by reducing cytoadherence. Artesunate and the artemisinins are the most rapid
acting anti-malarial drugs. This class of drugs is ineffective against extra-erythrocytic forms, sporozoites, liver schizonts, and merozoites. Artesunate is a water-soluble, semi-synthetic derivative of the sesquiterpine lactone artemisinin with anti-malarial, anti-shistosomiasis, antiviral, and potential anti-neoplastic activities. Upon hydrolysis of artesunate's active endoperoxide bridge moiety
by liberated heme in parasite-infected red blood cells, reactive oxygen species and carbon-centered radicals form, which have been shown to damage
and kill parasitic organisms. Additionally, in vitro studies demonstrate that this agent induces DNA breakage in a dose-dependent manner. Artesunate has also been shown to stimulate cell differentiation, arrest the cell cycle in the G1 and G2/M phases, inhibit cell proliferation, and induce apoptosis
through mitochondrial and caspase signaling pathways. Artemisinin is isolated from the plant Artemisia annua. |
