Abstract
BackgroundGlyphosate-based herbicides (GBHs) are the most widely used pesticides worldwide, and glyphosate is the active ingredient of such herbicides, including the formulation known as Roundup. The massive and increasing use of GBHs results in not only the global burden of occupational exposures, but also increased exposure to the general population. The current pilot study represents the first phase of a long-term investigation of GBHs that we are conducting over the next 5 years. In this paper, we present the study design, the first evaluation of in vivo parameters and the determination of glyphosate and its major metabolite aminomethylphosphonic acid (AMPA) in urine.MethodsWe exposed Sprague-Dawley (SD) rats orally via drinking water to a dose of glyphosate equivalent to the United States Acceptable Daily Intake (US ADI) of 1.75 mg/kg bw/day, defined as the chronic Reference Dose (cRfD) determined by the US EPA, starting from prenatal life, i.e. gestational day (GD) 6 of their mothers. One cohort was continuously dosed until sexual maturity (6-week cohort) and another cohort was continuously dosed until adulthood (13-week cohort). Here we present data on general toxicity and urinary concentrations of glyphosate and its major metabolite AMPA.ResultsSurvival, body weight, food and water consumption of the animals were not affected by the treatment with either glyphosate or Roundup. The concentration of both glyphosate and AMPA detected in the urine of SD rats treated with glyphosate were comparable to that observed in animals treated with Roundup, with an increase in relation to the duration of treatment. The majority of glyphosate was excreted unchanged. Urinary levels of the parent compound, glyphosate, were around 100-fold higher than the level of its metabolite, AMPA.ConclusionsGlyphosate concentrations in urine showed that most part of the administered dose was excreted as unchanged parent compound upon glyphosate and Roundup exposure, with an increasing pattern of glyphosate excreted in urine in relation to the duration of treatment. The adjuvants and the other substances present in Roundup did not seem to exert a major effect on the absorption and excretion of glyphosate. Our results demonstrate that urinary glyphosate is a more relevant marker of exposure than AMPA in the rodent model.
Highlights
Glyphosate-based herbicides (GBHs) are the most widely used pesticides worldwide, and glyphosate is the active ingredient of such herbicides, including the formulation known as Roundup
In the United States (US) glyphosate is contained in over 750 products, herbicides used for intensive genetically modified (GM) crops that have built-in tolerance to glyphosate, and in other products used in agriculture, forestry, urban, and home applications [5]
A few data on the use of individual pesticides are available for certain countries in the European Union (EU), making it difficult to find out how much glyphosate is being used by farmers [7]
Summary
Glyphosate-based herbicides (GBHs) are the most widely used pesticides worldwide, and glyphosate is the active ingredient of such herbicides, including the formulation known as Roundup. Glyphosate [IUPAC chemical name N-(phosphonomethyl)glycine] is the most widely applied pesticide worldwide and it is an active ingredient of all glyphosate-based herbicides (GBHs), including in the formulation “Roundup” [1, 2]. It is mainly marketed as a broad-spectrum systemic herbicide and crop desiccant [3]. The Asia-Pacific region represents the largest supplier of glyphosate active ingredient worldwide in terms of production. The EU has a strict regulation regarding the planting of GM crops (Directive EU 2015/412) [11] and GBHs are mainly applied to cereals for post-harvest desiccation purposes (wheat, rye, triticale, barley and oats), oilseeds (rapeseed, mustard seed and linseed), orchards and vineyards [12]
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