Synthesis and evaluation of enzyme inhibitory potential of some derivatives of scopolamine

Authors : Durre SHAHWAR, Muhammad Asam RAZA, Tania KHAN

Pages : 257-266

Doi:10.3906/sag-1206-94

View : 21 | Download : 8

Publication Date : 0000-00-00

Article Type : Research Paper

Abstract :This study was designed to synthesize and evaluate derivatives of scopolamine insert ignore into journalissuearticles values(1); as acetylcholine esterase and protease inhibitors. Scopolamine insert ignore into journalissuearticles values(1); was extracted from the aerial parts of Datura innoxia through bioassay guided fractionation. Five different derivatives of scopolamine insert ignore into journalissuearticles values(1); were synthesized, and identified through spectroscopic studies. Their acetylcholine esterase insert ignore into journalissuearticles values(AChE); and trypsin inhibitory potentials were determined through standard protocols and evaluated from the perspective of structure-activity relationship. The synthesized scopolamine derivatives insert ignore into journalissuearticles values(2-6); showed remarkable AChE inhibitory activity, except for scopoline insert ignore into journalissuearticles values(6);. The results showed higher enzyme inhibition potential of the synthesized compounds insert ignore into journalissuearticles values(2-5); as compared to scopolamine insert ignore into journalissuearticles values(1);. Maximum inhibition was exhibited by scopolamine N-oxide insert ignore into journalissuearticles values(89.9 \pm 1.2%, IC50 = 37.4 \pm 1.1 m M););, followed by scopolamine sulfonic acid insert ignore into journalissuearticles values(70.3 \pm 0.8%, IC50 = 46.9 \pm 1.0 m M); and O-methyl scopolamine insert ignore into journalissuearticles values(66.1 \pm 1.2%, IC50 = 94.7 \pm 0.8 m M);. All derivatives showed moderate activity against trypsin; maximum activity was exhibited by 6 insert ignore into journalissuearticles values(54.0 \pm 1.4%); with IC50 = 621.2 \pm 3.7 m M.
Keywords : Enzyme inhibition, scopolamine, Datura innoxia