New Synthesized tri-peptide as Inhibitor of krait (Bungarus sindanus) venom acetylcholinesterase

In the current study, the cyclopeptide alkaloid discarine D derived tri-peptides fragments were manufactured and then investigated for their inhibitory potential against krait ( Bungarus sindanus ) venom acetylcholinesterase (AChE) enzyme. The tri-peptides L-Leu- threo -D-Pheser-L-Phe and L-Leu- threo -L-Pheser-L-Phe were chemically synthesized by a conventional method using the benzyloxycarbonyl group for the alpha-amino (α-amino) safety and the methyl esters an amino acids derivative used safety for the carboxyl group. The present paper described that the general synthetic strategy of tri-peptide allows the tri-peptide sequence to be acquired with the N-terminal extreme protected. Kinetic studies using the Lineweaver Burk plot indicated that tri-peptides fragments cause an un-competitive type of inhibition i.e. both K m and V max values decreased with the increase of tri-peptides fragment concentration (13.5-22.5 µM). The estimated K i and IC50 for krait venom AChE were found to be 17.5 µM and 19.5 µM, respectively. It is concluded from the present paper clarified that the freshly produced tri-peptides fragment can be deliberated as a beneficial mediator for the inhibition of krait venom AChE.