Detoxification of paraquat poisoning: Effects of alkylsulfates and alkylsulfonates on paraquat poisoning in mice and rats

Article abstract of DOI:10.1248/bpb.18.523

The study revealed that high molecular polyvinyl sulfate (PVP) or sulfonate (PVS), and low molecular alkyldisulfonates (NaO₃S(CH₂)(n)SO₃Na, n = 2-5: EDS, TDS, BDS and PDS) can alleviate acute toxicity of the herbicide, paraquat dichloride (PQ) in mice. Their activity as antidotes and the mode of the action varied depending on molecular size. The survival rate for mice receiving PQ at 200 mg/kg alone was increasingly improved when the dose of antidotes was increased from 8 to 10 times the dose of PQ; all the test compounds, except EDS (70% survival), achieved a survival rate of 100%. When test compounds were orally dosed to mice in a mixture with PQ, they improved LD₅₀ of PQ alone. With the low molecular compounds EDS, TDS, BDS and PDS, the value increased to about 2 to 3 times (300-458 mg/kg) over that of PQ alone (140 mg/kg). With high molecular PVS and PVP, the combination reached about a 7 fold (900-1000 mg/kg) increase in LD₅₀ value. The formation of lipid peroxide in lungs of rats due to PQ tended to be suppressed by concomitant administration of carbohydrate sulfate (DS and GS). PVP, BDS and TDS were more effective in depressing synthesis of lipid peroxide than DS or GS in the lungs, although BDS and TDS were less effective in suppressing PQ absorption from the rat small intestine than DS, GS or PVP. The results of these experiments indicate that the main mechanism for the detoxification of a high molecular alkylsulfate or sulfonate, and a low molecular alkyldisulfonate must be suppression of PQ absorption from the intestine, similar to that of carbohydrate sulfate. In addition, a low molecular alkyldisulfonate (BDS and TDS) was also proved to be significantly effective in suppressing the formation of lipid peroxide in the lungs.

Full text of DOI:10.1248/bpb.18.523

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