A newly identified specific biological activity of glyphosate – inhibition of RGD-binding integrins

Gémes, Borbála Letícia and Takács, Eszter and Székács, Inna and Farkas, Enikő and Horváth, Róbert and Klátyik, Szandra and Székács, András (2022) A newly identified specific biological activity of glyphosate – inhibition of RGD-binding integrins. In: Proceedings of the 28th International Symposium on Analytical and Environmental Problems. Szegedi Tudományegyetem, Szeged, pp. 147-151. ISBN 9789633069042

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Abstract

In this study we investigated the inhibitory effect of the widely used broad-spectrum herbicide active ingredient glyphosate and its related analogues on αVβ3 integrin binding to the shortest oligopeptide recognizing motif of integrins, the arginine-glycine-aspartic acid (RGD) sequence. Integrin binding characteristics were assessed in a modified enzyme linked immunosorbent assay (ELISA) and by a label-free optical biosensor technique. At 22 mM, glyphosate reached full inhibition of αVβ3, and the inhibitory activity of its main metabolite, aminomethylphosphonic acid (AMPA) was also above 95%, while another environmentally relevant metabolite, sarcosine exerted only a weaker effect, approximately 35% inhibition. In turn, the half maximal inhibitory concentration (IC50) of glyphosate and AMPA were reported to be 2.7±0.5 mM and 1.3±0.2 mM, respectively. The inhibitory effects of the other related compounds investigated (acetylglycine, glycine and iminodiacetic acid) at the same concentration, 22 mM were below 50%. Inhibitory effects on cell adhesion to RGD-modified surfaces by whole cells containing several types of RGD-binding integrins including αVβ3 were detected using the biosensor technique, where the integrin antagonist activity of glyphosate was also demonstrated.

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