生物活性 | |||
---|---|---|---|
描述 | The 8-aminoquinoline (8AQ) class of anti-malarial compounds is extremely important in the fight against malaria, as this class of molecules is unique due to the efficacy against relapsing forms of malaria. Tafenoquine (TQ) is an 8-aminoquinoline (8AQ) that is currently in late stage development as an anti-malarial prophylactic agent. In the CYP 2D knock-out mouse model, there was no luminescence signal at either 48 or 72 hr post-infection indicating that TQ at its ED100 (3 mg/kg) prevented P. berghei infection. TQ was tested at two times its ED100 in the humanized/CYP 2D6 knock-in mouse strain. The results showed that there was less luminescence signal in all five mice at 48 hr (as compared to WT-infected controls) and no detectable luminescence signal at 72 hr post-inoculation. Five out of five WT mice treated with TQ had no detectable parasite burden after 31 days, in comparison to the WT infection control or the CYP 2D knock-out mice treated with TQ. Those results illustrated that TQ is active in the presence of the CYP 2D gene cluster[3]. |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.16mL 0.43mL 0.22mL |
10.79mL 2.16mL 1.08mL |
21.58mL 4.32mL 2.16mL |
参考文献 |
---|