Moracin derivatives from Morus Radix as dual BACE1 and cholinesterase inhibitors with antioxidant and anti-glycation capacities

Life Sciences
Su Hui SeongJae Sue Choi

Abstract

Morus, a member of the family Moraceae and commonly known as the mulberry, comprises a pharmaceutically important plant group whose major constituents are the moracins. Moracin derivatives have received great attention because they exhibit a diverse range of biological functionalities. However, no studies have considered the anti-Alzheimer's disease (AD) and anti-glycation potential of moracin derivatives. We designed the current study to explore the anti-AD activity of moracin derivatives via in vitro inhibition of BACE1 and cholinesterase, their antioxidant activity via scavenging ONOO- and ABTS+ radicals, and their anti-diabetic activity through inhibition of advanced glycation end-products (AGEs) formation. Moreover, to define the mechanism of action of moracin derivatives in depth, we performed in silico molecular modeling using a computer-assisted drug design and modeling program. Among the four Morus-derived moracins tested, moracin S, which has a prenyl moiety in the 2-aryl benzofuran scaffold, possessed the highest BACE1 inhibitory activity. It also, in a dose-dependent fashion, decreased ONOO--mediated bovine serum albumin (BSA) nitration and formation of AGEs and amyloid cross-β structures in the glycated BSA system,...Continue Reading

Citations

Aug 10, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Srijan ShresthaJae Sue Choi
Mar 29, 2020·Free Radical Research·Houssem Boulebd
Jun 7, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Piya TemviriyanukulUthaiwan Suttisansanee
Sep 29, 2019·Expert Opinion on Therapeutic Patents·Kamal M Dawood
May 11, 2021·Frontiers in Chemistry·Angela PariseNino Russo
Jul 21, 2021·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Lingrong WenBao Yang

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