ABSTRACT
BACE1 (β-secretase, memapsin 2, Asp2) has emerged as a promising target for the treatment of Alzheimer's disease (AD). BACE1 is an aspartic protease which works in the initial step of the amyloidogenic pathway, stimulating the creation and deposition of amyloid-β peptides (Aβ). BACE1 inhibition has direct ramifications in AD pathology without generally influencing viability. However, inhibition of BACE1, specifically through in-vivo models, has introduced numerous challenges for the researchers. Since the identification of BACE1 in 2000, inhibitors covering a wide range of auxiliary classes have been isolated or created. These inhibitors have been classified into either peptidomimetic or non-peptidic inhibitors. Advances in these fields have brought about targeted drug therapy, that may reduce deposition of A plaque in the brain. Natural product derivatives have always been a potential source of chemicals or lead chemicals in the drug discovery process and they are considered to be safe and economical. Natural BACE1 inhibitors are predominantly flavonoids. Citrus bioflavonoids are distinguished as potential non‐competitive BACE1 inhibitors. Furthermore, xanthones exhibited inhibition of Aβ conglomeration and BACE1 activity in vitro and in cells, in addition to their free radical scavenging and metal chelation activities. From this foundation, an efficient survey has been set up to deliver an effective screening program for a wide range of phytoextracts and their derivatives for BACE1 inhibitory potential, to contribute to AD treatment. Electronic databases have been utilized to screen data from studies performed on plants decades ago.
