l-
Phosphinothricin (
glufosinate or 2-amino-4-((hydroxy(methyl) phosphinyl)
butyric acid ammonium salt (AHPB)), which is a structural analog of
glutamate, is a recognized
herbicide that acts on weeds through inhibition of
glutamine synthetase. Due to the structural similarity between
phosphinothricin and some
bisphosphonates (BPs), this study focuses on investigating the possibility of repurposing
phosphinothricin as a
bisphosphonate analogue, particularly in two medicine-related activities: image probing and as an anti-
cancer drug. As BP is a competitive inhibitor of human
farnesyl pyrophosphate synthase (HFPPS), in silico molecular docking and dynamic simulations studies were established to evaluate the binding and stability of
phosphinothricin with HFPPS, while the results showed good binding and stability in the active site of the
enzyme in relation to
alendronate. For the purpose of inspecting bone-tissue accumulation of
phosphinothricin, a
technetium (99mTc)-
phosphinothricin complex was developed and its stability and tissue distribution were scrutinized. The radioactive complex showed rapid, high and sustained uptake into bone tissues. Finally, the cytotoxic activity of
phosphinothricin was tested against breast and
lung cancer cells, with the results indicating cytotoxic activity in relation to
alendronate. All the above results provide support for the use of
phosphinothricin as a potential anti-
cancer drug and of its
technetium complex as an imaging probe.