Sarsasapogenin: A steroidal saponin from Asparagus racemosus as multi target directed ligand in Alzheimer’s Disease

Publication date: Available online 28 October 2019Source: SteroidsAuthor(s): Priya Kashyap, Kalaivani Muthusamy, Manisha Niranjan, Shweta Trikha, Suresh KumarAbstractAlzheimer’s Disease (AD) is multi-factorial disorder characterized by impaired memory and cognition deficit. AD is characterized by impaired cholinergic transmission, extracellular amyloid beta deposits , neurofibillary tangles and oxidative stress. A multi-target directed ligand (MTDL) approach is required to devise a therapeutic strategy against AD. In the present study, Asparagus racemosus aqueous extract was chosen, as it possess abundant medicinal properties including nootropic effect mentioned in ancient Ayurvedic texts. Moreover, its secondary metabolite sarsasapogenin (SRS) was also selected for this multi-target study for the very first time. The current study demonstrated that sarsasapogenin significantly inhibits key enzymes involved in pathogenesis of AD which are acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), BACE1 and MAO-B in a concentration dependent manner. SRS also exhibited anti-amyloidogenic, anti-oxidant and neuroprotective effects by in vitro studies. The IC50 values of SRS is 7.7μM and 23.4μM for AChE and BuChE respectively. SRS also significantly inhibited Aβ42 fibrilisation up to 68% at 40μM concentration as compared to control. TEM visualization showed Aβ aggregates as short and scattered fibril clearly indicating SRS significantly inhibited peptide nucleation and fib...
Source: Steroids - Category: Drugs & Pharmacology Source Type: research