Patel Alpa, Panter Grace H, Trollope Henry T, Glennon Yohanna C, Owen Stewart F, Sumpter John P, Rand-Weaver Mariann
Biosciences, Institute of Environment, Health and Societies, Brunel University London, Uxbridge, Middlesex, UB8 3PH, United Kingdom.
AstraZeneca, Brixham Environmental Laboratory, Freshwater Quarry, Brixham, Devon, TQ5 8BA, United Kingdom.
Chemosphere. 2016 Nov;163:592-600. doi: 10.1016/j.chemosphere.2016.08.041. Epub 2016 Aug 28.
Human pharmaceuticals present in the environment have the potential to cause adverse effects on non-target organisms. The "read-across hypothesis" stipulates that pharmaceuticals will exhibit similar biological effects across species (e.g. human and fish) if the molecular target has been conserved and the effective drug concentrations are reached (Cmax). We tested this hypothesis by evaluating if ibuprofen, a non-selective inhibitor of prostaglandins and the cyclooxygenase (COX) enzyme, can mimic its primary effect in humans, on fish, at comparable plasma concentrations. The endpoints, prostaglandin E metabolite (PGEM) levels and the mRNA expression of COX (ptgs) gene, were measured in the gills of control and exposed fathead minnows (Pimephales promelas), using enzyme-immunoassay and quantitative real-time PCR (qPCR). Fish were exposed, for 24-72 h, to measured water concentrations of 9 (n = 12), 370 (n = 40) and 470 μg ibuprofen/L (n = 12). Water and blood plasma concentrations were determined using LC-MS/MS. Results showed that PGEM levels in fish exposed to 370 and 470 μg ibuprofen/L were significantly decreased compared to control fish, when mean plasma ibuprofen concentrations were 1.8-5.6-fold below the Cmax. The plasma ibuprofen concentrations and PGEM levels varied greatly between individuals. In fish exposed to 9 μg ibuprofen/L, when the mean plasma ibuprofen concentration was 224-fold below Cmax, no change in PGEM levels was observed. These data provide evidence for the read-across hypothesis, but suggest establishing a direct dose-response between internal plasma and PGEM is difficult, and would require significantly larger numbers of fish to overcome the inter-individual variation.
环境中存在的人类用药品有可能对非目标生物产生不利影响。“类推假设”规定,如果分子靶点保守且达到有效药物浓度(Cmax),药品将在不同物种(如人类和鱼类)间表现出相似的生物学效应。我们通过评估布洛芬(一种前列腺素和环氧化酶(COX)的非选择性抑制剂)在可比血浆浓度下能否在鱼类中模拟其在人类中的主要效应,来验证这一假设。使用酶免疫测定法和定量实时聚合酶链反应(qPCR),在对照和暴露的黑头呆鱼(Pimephales promelas)的鳃中测量了前列腺素E代谢物(PGEM)水平和COX(ptgs)基因的mRNA表达等终点指标。将鱼类暴露于9(n = 12)、370(n = 40)和470 μg布洛芬/升的测量水体浓度中24 - 72小时。使用液相色谱 - 串联质谱法测定水体和血浆浓度。结果显示,暴露于370和470 μg布洛芬/升的鱼类中,PGEM水平与对照鱼相比显著降低,此时平均血浆布洛芬浓度比Cmax低1.8 - 5.6倍。个体间血浆布洛芬浓度和PGEM水平差异很大。在暴露于9 μg布洛芬/升的鱼类中,当平均血浆布洛芬浓度比Cmax低224倍时,未观察到PGEM水平变化。这些数据为类推假设提供了证据,但表明在血浆和PGEM之间建立直接的剂量反应关系很困难,并且需要大量更多的鱼类来克服个体间差异。