L-Canaline, a nonprotein amino acid found in many leguminous plants, exhibits potent anticancer and antiproliferative effects. It effectively inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. Additionally, L-Canaline acts as a cytotoxic metabolite produced from L-canavanine through arginase catalysis and serves as a potent and irreversible inhibitor of ornithine aminotransferase.

P. falciparum:297 nM

L-Canaline is slightly less toxic to PBMCs stimulated via the mixed lymphocyte reaction (IC50 of 0.54 mM). L-canaline inhibits L-lysine flux competitively (Ki of 4.6 mM) in astrocytes and astrocytoma cells.L-Canaline treatment inhibits the proliferation of PBMCs after stimulation by phorbol 12-myristate-13-acetate (PMA) or via the mixed lymphocyte reaction.?The greatest effect is seen with PMA-stimulated cells, where L-canaline has an IC50 of 0.26 mM.

Intraseptal injection of 100 μg of L-canaline into male Sprague-Dawley rats causes a 90% decrease in the omithine aminotransferase activity of the septum tissues evaluated from animals killed 1 h later.L-Canaline decreases the aspartic acid content of tissues of the medulla oblongata of male Wistar rats, but it does not affect the evoked release of this nonprotein amino acid into these tissues.