Teubner Wera, Mehling Anette, Schuster Paul Xaver, Guth Katharina, Worth Andrew, Burton Julien, van Ravenzwaay Bennard, Landsiedel Robert
BASF Schweiz AG, Basel, Switzerland.
Regul Toxicol Pharmacol. 2013 Dec;67(3):468-85. doi: 10.1016/j.yrtph.2013.09.007. Epub 2013 Sep 30.
National legislations for the assessment of the skin sensitization potential of chemicals are increasingly based on the globally harmonized system (GHS). In this study, experimental data on 55 non-sensitizing and 45 sensitizing chemicals were evaluated according to GHS criteria and used to test the performance of computer (in silico) models for the prediction of skin sensitization. Statistic models (Vega, Case Ultra, TOPKAT), mechanistic models (Toxtree, OECD (Q)SAR toolbox, DEREK) or a hybrid model (TIMES-SS) were evaluated. Between three and nine of the substances evaluated were found in the individual training sets of various models. Mechanism based models performed better than statistical models and gave better predictivities depending on the stringency of the domain definition. Best performance was achieved by TIMES-SS, with a perfect prediction, whereby only 16% of the substances were within its reliability domain. Some models offer modules for potency; however predictions did not correlate well with the GHS sensitization subcategory derived from the experimental data. In conclusion, although mechanistic models can be used to a certain degree under well-defined conditions, at the present, the in silico models are not sufficiently accurate for broad application to predict skin sensitization potentials.
各国用于评估化学品皮肤致敏潜力的立法越来越多地基于全球协调系统(GHS)。在本研究中,根据GHS标准对55种非致敏化学品和45种致敏化学品的实验数据进行了评估,并用于测试计算机(虚拟)模型预测皮肤致敏的性能。对统计模型(Vega、Case Ultra、TOPKAT)、机理模型(Toxtree、经合组织(Q)SAR工具箱、DEREK)或混合模型(TIMES-SS)进行了评估。在各种模型的个体训练集中发现了三到九种评估的物质。基于机理的模型比统计模型表现更好,并且根据域定义的严格程度给出了更好的预测能力。TIMES-SS实现了最佳性能,预测完美,但其可靠性域内仅包含16%的物质。一些模型提供了效力模块;然而,预测结果与从实验数据得出的GHS致敏亚类相关性不佳。总之,虽然在明确界定的条件下,机理模型在一定程度上可以使用,但目前,虚拟模型在广泛应用中预测皮肤致敏潜力的准确性还不够高。