Intersting SAR studies of pregnane alkaloids isolated from genus Sarcococca against cholinesterase enzymes

Abstract

The genus Sarcococca is widely distributed in South-East Asia and it comprises 14 species. The genus is traditionally used for gastrointestinal ulcers, infections, pain and in rheumatic fevers. Recently, our group has derived a comprehensive SAR relationship picture for a new series of natural cholinesterase inhibitors isolated from Sarcococca saligna (syn. S. pruniformis, Buxaceae). The fractionation and purification of the active constitutents is based on bioassay-guided screening by using cholinesterase enzyme inhibition assay. These new cholinesterase inhibitors may act as potential leads in the discovery of clinically useful inhibitors for nervous system disorders, particularly by reducing memory deficiency in Alzheimer disease patients by potentiating and affecting the cholinergic transmission process. The cholinesterase inhibitory potential, kinetics and docking studies of pure compounds were accomplished and will be discussed in detail