The in vitro drug efficacy (IC50) of auranofin was investigated by haemocytometry and the CellTiter-Glo assay methods and the ex vivo drug efficacy (IC50) by light microscopic examination of Giemsa-stained slides. Also, the cytotoxic activity (CC50) of auranofin was examined by the CellTiter-Glo assay. The selectivity index (SI) was calculated for auranofin.
According to IC50, CC50 and SI data, auranofin did not exhibit cytotoxic activity on Vero cells, but exhibited antiprotozoal activity on epimastigotes and intracellular amastigotes of T. cruzi, promastigotes and intracellular amastigotes of L. tropica and intracellular tachyzoites of T. gondii (p<0.05).
The detection antiprotozoal activity of auranofin on T. cruzi, L. tropica and T. gondii according to the IC50, CC50 and SI values is considered an important and promising development. This is significant because auranofin may be an effective alternative treatment for Chagas disease, leishmaniasis and toxoplasmosis in the future.
方法:通过血细胞计数和CellTiter-Glo测定方法研究了金诺芬的体外药效(IC50),并通过Giemsa染色的载玻片进行光学显微镜检查研究了离体药效(IC50)。此外,通过CellTiter-Glo测定法检查了金诺芬的细胞毒性活性(CC50)。计算了金诺芬的选择性指数(SI)。
结果:根据IC50、CC50和SI数据,金诺芬对Vero细胞没有细胞毒活性,但是对T.Cruzi的epimastigotes和细胞内amastigotes表现出抗原生动物活性,热带乳杆菌的前鞭毛和细胞内的阿马斯泰格和弓形虫的细胞内速殖子(p<0.05)。
结论:检测金诺芬对克氏毛虫的抗原活性,根据IC50,CC50和SI值,热带念珠菌和弓形虫被认为是重要且有前途的发展。这一点很重要,因为金诺芬可能是南美锥虫病的有效替代疗法,未来的利什曼病和弓形虫病。