Acetytlcholinesterase is a neurotransferase enzyme which decomposes acetylcholine into acetyl and choline. The fact that the concentration of acetylcholine is found to be decreased in the brains of Alzheimer patients has lead us to focus to the inhibi...
Acetytlcholinesterase is a neurotransferase enzyme which decomposes acetylcholine into acetyl and choline. The fact that the concentration of acetylcholine is found to be decreased in the brains of Alzheimer patients has lead us to focus to the inhibition of AChE for the developmental research of the Alzheimer disease treatment.
In this report, we confirmed that the fluorinated or hydroxynated porphyrin compounds have excellent AChE inhibition effect. These compounds are rather large molecules, so it is a very interesting result considering tht they can hardly reach the active site of AChE through the narrow and long passage in AChE. Similar porphyrin compounds was found to be ineffective in the AChE inhibition, which suggests that the presence of fluorine atoms or hydroxy group in the compounds is critical in the process of the enzyme inhibition.
Various porphyrin compounds were synthesized and purified as the potential AChE inhibitors, whose enzyme inhibition activities were checked by the Ellman's coupled enyme using the Michaelis-Menten kinetics. The assay result showed that Various porphyrin compounds have relatively low K₁(enzyme inhibition constant) values. The type of enzyme inhibition was cheked by the Lineweaver-Burk plot. So we were found to inhibition type of various porphyrin compounds. For instance ADD16, the increase of Kim and the decrease of V? were observed, verifying that it acts as a reversible mixed type inhibitor.