Apuzzo C Fiore, Sullivan Eirin C, Platt David C, Seger-Held Ian, Jones Marjorie A
Department of Chemistry, Campus Box 4160, Illinois State University, Normal, IL, 61790, USA.
Department of Chemistry, University of North Florida, Jacksonville, FL, 32224, USA.
Heliyon. 2021 Aug 30;7(9):e07896. doi: 10.1016/j.heliyon.2021.e07896. eCollection 2021 Sep.
Novel therapeutics for the treatment of leishmaniasis are of interest as the disease not only is becoming more prevalent, but drug resistance is increasing in certain regions of the world. Reported here is the use of Bi-doped strontium aluminum oxyfluoride phosphors and protease inhibitors to test inhibitory activity against cultured promastigote and effects on secreted acid phosphatase (SAP) activity. Cell viability did not significantly decrease in the presence of 50 μM anti-perovskite compounds, implying limited cytotoxicity. Yet SAP activity did increase in the cell free preparations with time in the presence of strontium compounds. Of interest was the observation that cell free SAP activity did not increase in the presence of protease inhibitors with or without added strontium compounds. Since secreted proteases may play a role in the maturation of SAP and thus be involved with parasite-host infection establishment, this is in further need of evaluation. Nitric oxide production on day 4 post-addition of the strontium compounds was evaluated and showed an approximately 50% decrease in NO production in the presence of two test compounds relative to DMSO control cells. This is the first report of anti-perovskite compound inhibition of NO production by .
由于利什曼病不仅愈发普遍,而且在世界某些地区耐药性也在增加,因此治疗该疾病的新型疗法备受关注。本文报道了使用双掺杂氟氧化锶铝磷光体和蛋白酶抑制剂来测试对培养的前鞭毛体的抑制活性以及对分泌性酸性磷酸酶(SAP)活性的影响。在存在50 μM反钙钛矿化合物的情况下,细胞活力并未显著降低,这意味着细胞毒性有限。然而,在存在锶化合物的情况下,无细胞制剂中的SAP活性会随时间增加。有趣的是,观察到无论有无添加锶化合物,在蛋白酶抑制剂存在的情况下,无细胞SAP活性均未增加。由于分泌的蛋白酶可能在SAP的成熟过程中起作用,从而参与寄生虫 - 宿主感染的建立,因此这一点还需要进一步评估。在添加锶化合物后第4天评估一氧化氮的产生,结果显示相对于二甲基亚砜对照细胞,在存在两种测试化合物的情况下,一氧化氮的产生量减少了约50%。这是关于反钙钛矿化合物抑制一氧化氮产生的首次报道。