a Unidad de Toxicología Experimental , Universidad de Ciencias Médicas de Villa Clara , Santa Clara , Villa Clara , Cuba.
b Departament de Biología Funcional i Antropología Física , Universitat de València , Burjassot , Spain.
SAR QSAR Environ Res. 2017 Sep;28(9):735-747. doi: 10.1080/1062936X.2017.1376705.
The phenols are structurally heterogeneous pollutants and they present a variety of modes of toxic action (MOA), including polar narcotics, weak acid respiratory uncouplers, pro-electrophiles, and soft electrophiles. Because it is often difficult to determine correctly the mechanism of action of a compound, quantitative structure-activity relationship (QSAR) methods, which have proved their interest in toxicity prediction, can be used. In this work, several QSAR models for the prediction of MOA of 221 phenols to the ciliated protozoan Tetrahymena pyriformis, using Chemistry Development Kit descriptors, are reported. Four machine learning techniques (ML), k-nearest neighbours, support vector machine, classification trees, and artificial neural networks, have been used to develop several models with higher accuracies and predictive capabilities for distinguishing between four MOAs. They showed global accuracy values between 95.9% and 97.7% and area under Receiver Operator Curve values between 0.978 and 0.998; additionally, false alarm rate values were below 8.2% for training set. In order to validate our models, cross-validation (10-folds-out) and external test-set were performed with good behaviour in all cases. These models, obtained with ML techniques, were compared with others previously reported by other researchers, and the improvement was significant.
酚类是结构多样的污染物,具有多种毒性作用模式(MOA),包括极性麻醉剂、弱酸呼吸解偶联剂、亲电试剂和亲核试剂。由于通常难以正确确定化合物的作用机制,因此可以使用已证明在毒性预测方面具有意义的定量构效关系(QSAR)方法。在这项工作中,使用 Chemistry Development Kit 描述符,报告了用于预测 221 种苯酚对纤毛原生动物梨形四膜虫的 MOA 的几个 QSAR 模型。使用了四种机器学习技术(ML),即 k-最近邻、支持向量机、分类树和人工神经网络,开发了几个具有更高准确性和预测能力的模型,可用于区分四种 MOA。它们显示出的全局准确性值在 95.9%至 97.7%之间,接收器操作曲线下的面积在 0.978 至 0.998 之间;此外,训练集的误报率值低于 8.2%。为了验证我们的模型,在所有情况下都进行了交叉验证(10 折-out)和外部测试集,表现良好。与其他研究人员之前报告的其他模型相比,使用 ML 技术获得的这些模型有了显著改进。