Table 3.
Maximal or minimal activity and EC50 or IC50 of pesticides on HG5LN-hPXR and HG5LN-zfPXR.
| Compound | hPXR agonism | zfPXR agonism | zfPXR antagonism | Compound | hPXR agonism | zfPXR agonism | zfPXR antagonism | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| EC50 (µM) | Max (%) | EC50 (µM) | Max (%) | IC50 (µM) | Min (%) | EC50 (µM) | Max (%) | EC50 (µM) | Max (%) | IC50 (µM) | Min (%) | ||
| DMSO | 19 ± 6 | 28 ± 1.7 | DMSO | 19 ± 6 | 28 ± 1.7 | ||||||||
| 2,4’-DDE | 5.5 ± 0.4 | 78 | n.m. | 57 | n.a. | - | Heptachlor endo-epoxide* | 3.4 ± 0.7 | 69 | 2.0 ± 0.9 | 32 | n.a. | - |
| 4,4’-DDE | 5.6 ± 0.3 | 77 | n.a. | - | n.a. | - | Heptachlor exo-epoxide* | 1.9 ± 0.1 | 85 | 1.4 ± 0.04 | 76 | n.a. | - |
| Alachlor | 1.5 ± 0.4 | 76 | 0.67 ± 0.10 | 98 | n.a. | - | Hexachlorobenzene | n.a. | - | n.a. | - | n.a. | - |
| Aldicarb | n.a. | - | n.a. | - | n.a. | - | HPTE | n.a. | - | 1.8 ± 0.04 | 37 | n.a. | - |
| Aldrin | 7.6 ± 0.3 | 70 | 10 ± 4.5 | 65 | n.a. | - | Imazalil* | 10 ± 1.4 | 39 | 9.8 ± 2.6 | 43 | n.a. | - |
| Azimsulfuron | n.a. | - | n.a. | - | n.a. | - | Lindane* | 10 ± 1.8 | 62 | 14 ± 0.9 | 55 | n.a. | - |
| Bifenox | 4.5 ± 0.7 | 84 | 5.5 ± 0.4 | 80 | n.a. | - | Linuron | 29 ± 3.2 | 40 | n.a. | - | n.a. | - |
| Boscalid | 13 ± 1.1 | 55 | 58 ± 82 | 41 | n.a. | - | Mecoprop | n.a. | - | n.a. | - | n.a. | - |
| Bupirimate* | 1.7 ± 0.1 | 101 | 22 ± 5.1 | 26 | n.a. | - | Metalaxyl | 31 ± 2.6 | 40 | 20 ± 3.1 | 42 | n.a. | - |
| Captan* | n.a. | - | n.a. | - | n.a. | - | Metamitron | n.a. | - | n.a. | - | n.a. | - |
| Chlordecone* | 19 ± 5.6 | 46 | 75 ± 23 | 32 | n.a. | - | Methoxychlor* | 17 ± 1.7 | 49 | n.a. | - | n.a. | - |
| Chlorosulfuron | n.a. | - | n.a. | - | n.a. | - | Metolachlor | 0.68 ± 0.07 | 69 | 0.63 ± 0.03 | 115 | n.a. | - |
| Chlorpropham* | 20 ± 8.6 | 49 | 22 ± 16 | 51 | n.a. | - | Mirex | n.a. | - | n.a. | - | n.a. | - |
| Chlorpyriphos* | 2.7 ± 0.4 | 95 | 3.0 ± 0.3 | 101 | n.a. | - | Nicosulfuron | n.a. | - | n.a. | - | n.a. | - |
| Chlortoluron | n.a. | - | n.a. | - | n.a. | - | Oxadiazon | 1.1 ± 0.0001 | 76 | n.a. | - | n.a. | - |
| Cis-chlordane* | 8.6 ± 3.0 | 87 | 13 ± 0.4 | 53 | n.a. | - | Oxychlordane | 4.3 ± 0.3 | 69 | n.a. | - | n.a. | - |
| Cis-nonachlor* | 7.4 ± 3.8 | 62 | n.a. | - | n.a. | - | Oxyfluorfen | 3.0 ± 0.1 | 86 | n.a. | - | 10 ± 1.2 | 56 |
| λ-Cyhalothrin | 1.7 ± 0.2 | 107 | n.a. | - | 6.8 ± 1.0 | 45 | Penconazol | n.m. | 42 | 1.5 ± 0.1 | 51 | n.a. | - |
| Cypermethrin | 1.6 ± 0.2 | 100 | n.a. | - | 5.0 ± 0.3 | 31 | Pencycuron* | 1.9 ± 0.2 | 98 | n.a. | - | n.a. | - |
| Cyproconazole | n.m. | 44 | n.a. | - | n.a. | - | Pendimethalin* | 3.0 ± 0.1 | 91 | 0.47 ± 0.1 | 104 | n.a. | - |
| Deltamethrin | 1.8 ± 0.2 | 92 | n.a. | - | 1.6 ± 0.2 | 21 | Pirimiphos-methyl | 22 ± 23 | 69 | 1.1 ± 0.1 | 103 | n.a. | - |
| Diclofop-methyl | n.a. | - | n.a. | - | n.m. | 65 | Pretilachlor* | 0.18 ± 0.02 | 94 | 0.58 ± 0.07 | 123 | n.a. | - |
| Dieldrin* | 9.2 ± 1.4 | 62 | n.a. | - | 19 ± 8.8 | 63 | Prochloraz* | 1.8 ± 0.1 | 71 | n.a. | - | 11 ± 5.6 | 50 |
| Diethofencarb* | 19 ± 2.4 | 45 | n.a. | - | n.a. | - | Propiconazole | 13 ± 1.5 | 58 | 1.0 ± 0.1 | 33 | n.a. | - |
| Diflubenzuron | n.a. | - | n.a. | - | n.a. | - | Propyzamide | 22 ± 1.7 | 45 | n.a. | - | n.a. | - |
| Diuron | n.a. | - | n.a. | - | n.a. | - | Tebuconazole | 6.8 ± 0.4 | 71 | n.a. | - | 24 ± 4.3 | 62 |
| Endosulfan | 5.7 ± 0.4 | 72 | 11 ± 1.5 | 57 | n.a. | - | Tefluthrin | 4.4 ± 0.9 | 76 | 4.2 ± 1.1 | 32 | n.a. | - |
| Endrin* | 6.9 ± 1.2 | 66 | 14 ± 1.2 | 57 | n.a. | - | Terbutylazine | n.a. | - | n.a. | - | n.a. | - |
| Epoxiconazole | 8.1 ± 0.2 | 72 | 1.6 ± 0.1 | 68 | n.a. | - | Thiabendazole* | n.a. | - | n.a. | - | 10 ± 0.7 | 49 |
| Ethoprophos | n.m. | 33 | n.m. | 38 | n.a. | - | Thiacloprid | n.a. | - | n.a. | - | n.a. | - |
| Etofenprox | 3.0 ± 0.2 | 81 | n.a. | - | n.a. | - | Thiophanate-methyl | 35 ± 7.3 | 46 | n.a. | - | n.a. | - |
| Fenamiphos | 1.7 ± 0.2 | 76 | 0.70 ± 0.21 | 103 | n.a. | - | Tolclofos-methyl | 11 ± 0.3 | 59 | 2.5 ± 0.1 | 88 | n.a. | - |
| Fenarimol | 13 ± 2.2 | 56 | n.a. | - | 24 ± 7.1 | 66 | Toxaphene* | 0.75 ± 0.03 | 89 | 0.15 ± 0.01 | 68 | n.a. | - |
| Fenbuconazole* | 32 ± 13 | 43 | n.m. | 43 | n.a. | - | Trans-chlordane* | 4.3 ± 0.3 | 92 | 16 ± 0.8 | 50 | n.a. | - |
| Fenvalerate* | 1.7 ± 0.05 | 79 | n.a. | - | n.m. | 66 | Trans-nonachlor | 5.3 ± 0.2 | 70 | 29 ± 5.5 | 43 | n.a. | - |
| Fipronil* | n.m. | 39 | n.a. | - | n.a. | - | Triclosan* | 11 ± 3.9 | 62 | n.a. | - | n.a. | - |
| Fipronil sulfone* | 5.4 ± 0.4 | 73 | n.a. | - | n.a. | - | Triflurnizole | 21 ± 14 | 51 | 6.0 ± 0.8 | 48 | n.a. | - |
| Flufenoxuron* | n.m. | 49 | 8.9 ± 0.6 | 63 | n.a. | - | Vinclozolin | n.a. | - | n.m. | 30 | n.a. | - |
| Fluvalinate | 1.1 ± 0.1 | 74 | n.a. | - | n.a. | - | Vinclozolin M2 | 39 ± 9.6 | 35 | n.a. | - | n.a. | - |
| Heptachlor | n.m. | 43 | 7.4 ± 1.8 | 44 | n.a. | - | Ziram* | n.a. | - | n.a. | - | n.a. | - |
n.a., not active; n.m., not modellable; max, maximal activity of the chemicals obtained at 10 µM except for compounds that were not tested above 3 µM because of toxicity or non-specificity*; min, minimal activity of the chemicals obtained at 10 µM except for compounds that were not tested above 3 µM because of toxicity or non-specificity*.
Maximal activities of the chemicals obtained at 10 µM are expressed as a percentage of the maximal induced by 3 µM SR 12813 and 1 µM clotrimazole for HG5LN-hPXR and HG5LN-zfPXR, respectively. Antagonism assays were performed in coexposure with 0.3 µM SR 12813 in HG5LN-hPXR cells and 0.03 µM clotrimazole in HG5LN-zfPXR cells. Minimal activities of the chemicals obtained at 10 µM are expressed as a percentage of the maximal induced by 3 µM SR 12813 and 1 µM clotrimazole for HG5LN-hPXR and HG5LN-zfPXR, respectively.