Stagkos-Georgiadis Alkiviadis, Baffour-Duah Bright, Tralau Tewes, Bloch Denise
Department of Pesticides Safety, German Federal Institute for Risk Assessment (BfR), Max-Dohrn-Str. 8-10, 10589, Berlin, Germany.
Department of Nutritional Toxicology, Institute of Nutritional Science, University of Potsdam, Arthur-Scheunert-Alle 114-116, 14558, Nuthetal, Germany.
Arch Toxicol. 2025 Jul 2. doi: 10.1007/s00204-025-04078-0.
Plant protection products (PPPs) contain one or more active substances (AS) as well as a varying number of co-formulants. Whilst AS are amongst the most data-rich and well-investigated substances in toxicology, possibly toxic co-formulants and PPPs with potentially relevant mixture effects are not considered in risk assessment. This especially applies to operators who come in contact with the undiluted product. In this study, we investigated this concern by prioritising co-formulants and PPPs for further testing using new approach methodologies (NAMs). We combined in silico predictions of co-formulant nephrotoxicity and hepatotoxicity with AS and co-formulant kinetic interaction prediction and thus identified 427 PPPs for further investigation. In a next step, six PPPs were there assessed for their comparative AS and PPP toxicity in liver cells. One product displayed more than additive effects and was thus tested for in silico predicted kinetic interactions. Whilst permeability glycoprotein (P-gp) interaction could not be confirmed, the observed effect may likely be attributed to CYP2C19 interaction. In summary, the findings highlight that the use of in silico tools as a screening step is useful to limit the number of PPPs for further testing. Subsequent in vitro testing of a limited number of PPPs supported the application of the additivity concept and highlighted that prioritised co-formulants contribute additively. We propose the integration of such co-formulants into the Hazard Index (HI) approach currently applied in active substance combined risk assessment.
植物保护产品(PPPs)含有一种或多种活性物质(AS)以及数量不等的辅助配方成分。虽然活性物质是毒理学中数据最丰富且研究最充分的物质之一,但在风险评估中并未考虑可能有毒的辅助配方成分以及具有潜在相关混合效应的植物保护产品。这尤其适用于接触未稀释产品的操作人员。在本研究中,我们通过使用新方法学(NAMs)对辅助配方成分和植物保护产品进行优先级排序以进行进一步测试,从而调查了这一问题。我们将辅助配方成分肾毒性和肝毒性的计算机模拟预测与活性物质和辅助配方成分的动力学相互作用预测相结合,从而确定了427种需要进一步研究的植物保护产品。下一步,对六种植物保护产品在肝细胞中进行了活性物质和植物保护产品的比较毒性评估。一种产品表现出超加和效应,因此对其进行了计算机模拟预测的动力学相互作用测试。虽然无法证实其与通透性糖蛋白(P - gp)的相互作用,但观察到的效应可能归因于与CYP2C19的相互作用。总之,研究结果突出表明,使用计算机模拟工具作为筛选步骤有助于限制需要进一步测试的植物保护产品数量。随后对有限数量的植物保护产品进行的体外测试支持了加和性概念的应用,并突出表明经过优先级排序的辅助配方成分具有加和作用。我们建议将此类辅助配方成分纳入目前在活性物质联合风险评估中应用的危害指数(HI)方法中。