Boron-based hybrids as novel scaffolds for the development of drugs with neuroprotective properties

TY - JOUR

T1 - Boron-based hybrids as novel scaffolds for the development of drugs with neuroprotective properties

AU - Cacciatore, Ivana

AU - Turkez, Hasan

AU - Di Rienzo, Annalisa

AU - Ciulla, Michele

AU - Mardinoglu, Adil

AU - Di Stefano, Antonio

N1 - Funding Information: This study was supported by the Italian Ministry of Education, University and Research (University “G. d‘Annunzio” of Chieti-Pescara) FAR 2019. Publisher Copyright: © The Royal Society of Chemistry.

PY - 2021/11

Y1 - 2021/11

N2 - Novel boron-based compounds (BBCs) were synthesized and evaluated as potential candidates for the development of novel drugs against Alzheimer's disease (AD). The neuroprotective profile of novel BBCs was evaluated using Aβ1-42-treated-SH-SY5Y cells while their antioxidant activity was evaluated by total antioxidant capacity (TAC) and total oxidative status (TOS) assays. Results showed that (a novel boron-based hybrid containing an antioxidant portion) inhibited cell death induced by Aβ1-42-exposure in differentiated SH-SY5Y cells, resulting in an increase in cell viability by 25-33% (MTT assay) and by 63-71% (LDH assay) in a concentration range of 25-100 μM. Antioxidant assays demonstrated a good capability of to counteract the oxidative status. Moreover, possessed a significant ability to inhibit acetylcholinesterase (AChE) (22.96% at 50 μM), an enzyme whose enzymatic activity is increased in AD patients. In the present work, absorption and distribution properties of boron-based hybrids were predicted using Pre-ADMET software. preliminary results suggested that boron-based hybrids could be new structural scaffolds for the development of novel drugs for the management of AD. [Abstract copyright: This journal is © The Royal Society of Chemistry.]

AB - Novel boron-based compounds (BBCs) were synthesized and evaluated as potential candidates for the development of novel drugs against Alzheimer's disease (AD). The neuroprotective profile of novel BBCs was evaluated using Aβ1-42-treated-SH-SY5Y cells while their antioxidant activity was evaluated by total antioxidant capacity (TAC) and total oxidative status (TOS) assays. Results showed that (a novel boron-based hybrid containing an antioxidant portion) inhibited cell death induced by Aβ1-42-exposure in differentiated SH-SY5Y cells, resulting in an increase in cell viability by 25-33% (MTT assay) and by 63-71% (LDH assay) in a concentration range of 25-100 μM. Antioxidant assays demonstrated a good capability of to counteract the oxidative status. Moreover, possessed a significant ability to inhibit acetylcholinesterase (AChE) (22.96% at 50 μM), an enzyme whose enzymatic activity is increased in AD patients. In the present work, absorption and distribution properties of boron-based hybrids were predicted using Pre-ADMET software. preliminary results suggested that boron-based hybrids could be new structural scaffolds for the development of novel drugs for the management of AD. [Abstract copyright: This journal is © The Royal Society of Chemistry.]

UR - http://www.scopus.com/inward/record.url?scp=85119981104&partnerID=8YFLogxK

U2 - 10.1039/d1md00177a

DO - 10.1039/d1md00177a

M3 - Article

AN - SCOPUS:85119981104

SN - 2632-8682

VL - 12

SP - 1944

EP - 1949

JO - RSC Medicinal Chemistry

JF - RSC Medicinal Chemistry

IS - 11

ER -