Chemical Properties
White to off-white solid
Uses
Picolinamide was used as template in preparation of molecular imprinting polymer. Picolinamide was used in a study to evaluate kinetics and mechanism of liberation of picolinamide from chromium(III)-picolinamide complexes in HClO
4.
Uses
A nicotinic acid derivative for prevention and treatment of cancer by activating RUNX3 gene.
Definition
ChEBI: A pyridinecarboxamide that is the monocarboxylic acid amide derivative of picolinic acid.
Biological Activity
picolinamide is a poly (adp-ribose) synthetase (parp) inhibitor.parp inhibitors, a group of pharmacological inhibitors of the enzyme poly adp ribose polymerase (parp), are developed for multiple indications, especially for the treatment of cancer.
Biochem/physiol Actions
Picolinamide is potential inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. Picolinamide acts as bidentate ligand and forms complexes with lanthanide nitrates, thiocyanates and perchlorates.
in vitro
the pathway of oxidation of picolinamide by a gram-negative rod has been elucidated. results showed that under high ph conditions, whole cells could release 2,5-dihydroxypyridine into culture supernatants. moreover, sodium arsenite was able to cause whole cells to accumulate 6-hydroxypicolinate in the culture media. in addition, whole cells were found to oxidize picolinamide, without lag. it was also found that cell-free extracts could convert picolinamide into picolinate, and hydroxylate picolinate into 6-hydroxypicolinate [1].
in vivo
picolinamide was used in a previous study to evaluate the possibility that the inhibition of na+/phosphate cotransport might be associated with the inhibition of nad hydrolyzing enzymes. results showed that the overnight treatment of rats with picolinamide, administered as a single injection (4 mmol/kg), could inhibit na+/phosphate cotransport by isolated renal brush border membrane vesicles. similar to nicotinamide, the inhibition caused by picolinamide occurred in thyroparathyroidectomized rats, was specific for na+/phosphate cotransport. unlike nicotinamide, there was only a small 1.5-fold increase in renal cortical nad content after picolinamide treatment [2].
References
[1] c. g. orpin,m. knight, and w. c. evans. the bacterial oxidation of picolinamide, a photolytic product of diquatbiochem j. 1972 may; 127(5): 819–831.
[2] campbell pi, al-mahrouq ha,abraham mi,kempson sa. specific inhibition of rat renal na+/phosphate cotransport by picolinamide. j pharmacol exp ther.1989 oct;251(1):188-92.
