Zhou Ying, Fomovska Alina, Muench Stephen, Lai Bo-Shiun, Mui Ernest, McLeod Rima
The University of Chicago, Chicago, Illinois, USA.
Antimicrob Agents Chemother. 2014;58(3):1789-92. doi: 10.1128/AAC.02225-13. Epub 2013 Dec 23.
Here, we show that spiroindolone, an effective treatment for plasmodia, is also active against Toxoplasma gondii tachyzoites. In vitro, spiroindolone NITD609 is cidal for tachyzoites (50% inhibitory concentration [IC50], 1μM) and not toxic to human cells at ≥10μM. Two daily oral doses of 100 mg/kg of body weight reduced the parasite burden in mice by 90% (P=0.002), measured 3 days after the last dose. This inhibition of T. gondii tachyzoites in vitro and in vivo indicates that spiroindolone is a promising lead candidate for further medicine development.
在此，我们表明，对疟原虫有效的治疗药物螺环吲哚酮对刚地弓形虫速殖子也有活性。在体外，螺环吲哚酮NITD609对速殖子具有杀伤作用（半数抑制浓度[IC50]为1μM），且在浓度≥10μM时对人细胞无毒。每天口服两次，每次100mg/kg体重，末次给药3天后检测发现，小鼠体内的寄生虫负荷降低了90%（P = 0.002）。螺环吲哚酮在体外和体内对刚地弓形虫速殖子的这种抑制作用表明，它是进一步药物开发的一个有前景的潜在候选药物。
