Please use this identifier to cite or link to this item: https://ir.swu.ac.th/jspui/handle/123456789/29351
ชื่อเรื่อง: Design, Synthesis, and Neuroprotective Activity of Phenoxyindole Derivatives on Antiamyloid Beta (Aβ) Aggregation, Antiacetylcholinesterase, and Antioxidant Activities
ผู้แต่ง: Laivut S.
Moongkarndi P.
Kitphati W.
Rukthong P.
Sathirakul K.
Sripha K.
Keywords: Alzheimer’s disease
antiamyloid beta aggregation
antioxidant
indole-based scaffold
neuroprotective activity
วันที่เผยแพร่: 2023
สำนักพิมพ์: MDPI
บทคัดย่อ: In this investigation, a number of phenoxyindole derivatives were designed, synthesized, and tested for their neuroprotective ability on SK-N-SH cells against Aβ42-induced cell death and biologically specific activities involved in anti-Aβ aggregation, anti-AChE, and antioxidant effects. The proposed compounds, except compounds 9 and 10, could protect SK-N-SH cells at the IC50 of anti-Aβ aggregation with cell viability values ranging from 63.05% ± 2.70% to 87.90% ± 3.26%. Compounds 3, 5, and 8 demonstrated striking relationships between the %viability of SK-N-SH cells and IC50 values of anti-Aβ aggregation and antioxidants. No significant potency of all synthesized compounds against AChE was found. Among them, compound 5 showed the strongest anti-Aβ and antioxidant properties with IC50 values of 3.18 ± 0.87 and 28.18 ± 1.40 μM, respectively. The docking data on the monomeric Aβ peptide of compound 5 demonstrated good binding at regions involved in the aggregation process, and the structural feature made it possible to be a superior radical scavenger. The most effective neuroprotectant belonged to compound 8, with a cell viability value of 87.90% ± 3.26%. Its unique mechanisms for enhancing the protective impact may serve additional purposes since it demonstrated mild biological-specific effects. In silico prediction of CNS penetration shows strong passive penetration ability across the blood–brain barrier from blood vessels to the CNS for compound 8. In light of our findings, compounds 5 and 8 appeared as potentially intriguing lead compounds for new therapeutic approaches to Alzheimer’s disease. More in vivo testing will be revealed in due course. © 2023 by the authors.
URI: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85152464722&doi=10.3390%2fph16030355&partnerID=40&md5=7e004d9ca21175641fb337eb6fb9d817
https://ir.swu.ac.th/jspui/handle/123456789/29351
Appears in Collections:Scopus 2023

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