Department of Medicine, Washington University School of Medicine, St. Louis, MO 63110, USA.
Toxicol Appl Pharmacol. 2010 Mar 15;243(3):315-22. doi: 10.1016/j.taap.2009.11.023. Epub 2009 Dec 11.
Silver is a centuries-old antibiotic agent currently used to treat infected burns. The sensitivity of a wide range of drug-resistant microorganisms to silver killing suggests that it may be useful for treating refractory lung infections. Toward this goal, we previously developed a methylated caffeine silver acetate compound, SCC1, that exhibits broad-spectrum antimicrobial activity against clinical strains of bacteria in vitro and when nebulized to lungs in mouse infection models. Preclinical testing of high concentrations of SCC1 in primary culture mouse tracheal epithelial cells (mTEC) showed selective ciliated cell death. Ciliated cell death was induced by both silver- and copper-containing compounds but not by the methylated caffeine portion of SCC1. We hypothesized that copper transporting P-type ATPases, ATP7A and ATP7B, play a role in silver detoxification in the airway. In mTEC, ATP7A was expressed in non-ciliated cells, whereas ATP7B was expressed only in ciliated cells. The exposure of mTEC to SCC1 induced the trafficking of ATP7B, but not ATP7A, suggesting the presence of a cell-specific silver uptake and detoxification mechanisms. Indeed, the expression of the copper uptake protein CTR1 was also restricted to ciliated cells. A role of ATP7B in silver detoxification was further substantiated when treatment of SCC1 significantly increased cell death in ATP7B shRNA-treated HepG2 cells. In addition, mTEC from ATP7B(-/-) mice showed enhanced loss of ciliated cells compared to wild type. These studies are the first to demonstrate a cell type-specific expression of the Ag+/Cu+ transporters ATP7A, ATP7B, and CTR1 in airway epithelial cells and a role for ATP7B in detoxification of these metals in the lung.
银是一种具有数百年历史的抗生素药物,目前用于治疗感染性烧伤。多种耐药微生物对银的敏感性表明,它可能对治疗难治性肺部感染有用。为此,我们之前开发了一种甲基化咖啡因的醋酸银化合物 SCC1,该化合物对体外临床细菌菌株和在小鼠感染模型中雾化到肺部时具有广谱抗菌活性。SCC1 的高浓度在原代培养的小鼠气管上皮细胞 (mTEC) 中的临床前测试显示出选择性纤毛细胞死亡。纤毛细胞死亡是由含银和含铜的化合物引起的,但不是由 SCC1 的甲基化咖啡因部分引起的。我们假设铜转运 P 型 ATP 酶 ATP7A 和 ATP7B 在气道中的银解毒中起作用。在 mTEC 中,ATP7A 在非纤毛细胞中表达,而 ATP7B 仅在纤毛细胞中表达。mTEC 暴露于 SCC1 诱导 ATP7B 的转运,但不诱导 ATP7A 的转运,表明存在细胞特异性的银摄取和解毒机制。事实上,铜摄取蛋白 CTR1 的表达也仅限于纤毛细胞。当用 SCC1 处理时,ATP7B shRNA 处理的 HepG2 细胞中的细胞死亡显著增加,进一步证实了 ATP7B 在银解毒中的作用。此外,与野生型相比,ATP7B(-/-) 小鼠的 mTEC 显示出增强的纤毛细胞丢失。这些研究首次证明了 Ag+/Cu+ 转运蛋白 ATP7A、ATP7B 和 CTR1 在气道上皮细胞中的细胞类型特异性表达,以及 ATP7B 在肺部这些金属解毒中的作用。