Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.
CIIMAR/CIMAR-Interdisciplinary Center for Marine and Environmental Research, University of Porto, 4450-208 Matosinhos, Portugal.
Molecules. 2022 Aug 17;27(16):5247. doi: 10.3390/molecules27165247.
Antifouling (AF) coatings containing booster biocides are used worldwide as one of the most cost-effective ways to prevent the attachment of marine organisms to submerged structures. Nevertheless, many of the commercial biocides, such as Econea (tralopyril), are toxic in marine environments. For that reason, it is of extreme importance that new efficient AF compounds that do not cause any harm to non-target organisms and humans are designed. In this study, we measured the half-maximal inhibitory concentration (IC) of a promising nature-inspired AF compound, a triazolyl glycosylated chalcone (compound ), in an immortalized human retinal pigment epithelial cell line (hTERT-RPE-1) and compared the results with the commercial biocide Econea. We also investigated the effects of these biocides on the cellular lipidome following an acute (24 h) exposure using liquid chromatography quadrupole time-of-flight mass spectrometry (LC-Q-TOF/MS). Our results showed that compound did not affect viability in hTERT-RPE-1 cells at low concentrations (1 μM), in contrast to Econea, which caused a 40% reduction in cell viability. In total, 71 lipids were found to be regulated upon exposure to 10 µM of both compounds. Interestingly, both compounds induced changes in lipids involved in cell death, membrane modeling, lipid storage, and oxidative stress, but often in opposing directions. In general, Econea exposure was associated with an increase in lipid concentrations, while compound exposure resulted in lipid depletion. Our study showed that exposure to human cells at sublethal Econea concentrations results in the modulation of several lipids that are linked to cell death and survival.
含增效型杀生物剂的防污(AF)涂料作为防止海洋生物附着在水下结构物上的最具成本效益的方法之一,在全球范围内得到了广泛应用。然而,许多商业杀生物剂,如 Econea(tralopyril),在海洋环境中是有毒的。因此,设计出不会对非目标生物和人类造成任何伤害的新的高效 AF 化合物是至关重要的。在这项研究中,我们测量了一种有前途的仿生 AF 化合物,即三唑基糖基查尔酮(化合物)在永生化人视网膜色素上皮细胞系(hTERT-RPE-1)中的半最大抑制浓度(IC),并将结果与商业杀生物剂 Econea 进行了比较。我们还使用液相色谱四极杆飞行时间质谱(LC-Q-TOF/MS)研究了这些杀生物剂在急性(24 小时)暴露后对细胞脂类组的影响。我们的研究结果表明,与 Econea 相比,化合物在低浓度(1 μM)下不会影响 hTERT-RPE-1 细胞的活力,而 Econea 则导致细胞活力降低 40%。总共发现有 71 种脂质在暴露于 10 μM 的两种化合物时发生了调节。有趣的是,两种化合物都诱导了与细胞死亡、膜建模、脂质储存和氧化应激相关的脂质发生变化,但通常是相反的方向。一般来说,Econea 暴露会导致脂质浓度增加,而化合物暴露则导致脂质耗尽。我们的研究表明,在亚致死 Econea 浓度下暴露于人类细胞会导致与细胞死亡和存活相关的几种脂质发生调制。