The widespread application of triazole fungicides makes people attach great concern over its adverse effects in mammalian. In this paper, cytotoxic effects of triazole alcohol fungicides (TAFs) were assessed on human HeLa, A549, HCT116 and K562 cells, and the potential mechanism of TAFs cytotoxicity was studied preliminarily. Results showed that TAFs had cytotoxicity on human cells with different level and cytotoxic selectivity. TAFs cytotoxicity was resonated with a typical hormetic biphasic dose action that produced a complex pattern of stimulatory or inhibitory effects on cell viability. Among the five TAFs, diniconazole revealed a widest range of cytotoxicity to inhibit the viability of the adherent and the suspension cells, causing HeLa cells shrinkage, A549 cells shrunken, and K562 cells collapse, and showed stronger cytotoxicity than hexaconazole. Moreover, the involvement of ROS generation in the cytotoxicity of TAFs on human cells was observed, and the apoptosis of HeLa cells and the formation of apoptotic body in K562 cells induced by diniconazole were characterized. The results indicated the cytotoxicity of TAFs with different structures on human cells was depended on their own property and cell specificity, K562 cells were the most susceptible to TAFs and diniconazole was the strongest toxic.

三唑类杀真菌剂的广泛应用使人们对其在哺乳动物中的不良影响高度关注。本文研究了三唑醇类杀菌剂（TAFs）对人HeLa，A549，HCT116和K562细胞的细胞毒性作用，并初步研究了TAFs细胞毒性的潜在机制。结果表明，TAF对人细胞具有不同程度和细胞毒性选择性的细胞毒性。TAFs的细胞毒性与典型的双相药性剂量作用共鸣，该剂量作用对细胞活力产生了复杂的刺激或抑制作用。在这5种TAF中，迪尼康唑显示出最广泛的细胞毒性，可抑制粘附细胞和悬浮细胞的活力，从而导致HeLa细胞萎缩，A549细胞萎缩和K562细胞崩溃，并且显示出比六康唑更强的细胞毒性。此外，观察到ROS的产生与TAFs对人细胞的细胞毒性有关，并表征了地尼康唑诱导的HeLa细胞凋亡和K562细胞凋亡小体的形成。结果表明，不同结构的TAF对人细胞的细胞毒性取决于其自身特性和细胞特异性，K562细胞对TAF最敏感，而迪尼康唑的毒性最强。