Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease

© 2017, The Japanese Society of Pharmacognosy and Springer Japan. Abstract: A series of prenylated resveratrol derivatives were designed, semisynthesized and biologically evaluated for inhibition of β-secretase (BACE1) and amyloid-β (Aβ) aggregation as well as free radical scavenging and neuroprotec...

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Main Authors: Thanchanok Puksasook, Shinya Kimura, Sarin Tadtong, Jutamas Jiaranaikulwanitch, Jaturong Pratuangdejkul, Worawan Kitphati, Khanit Suwanborirux, Naoki Saito, Veena Nukoolkarn
Format: Journal
Published: 2018
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http://cmuir.cmu.ac.th/jspui/handle/6653943832/56964
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Institution: Chiang Mai University
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spelling th-cmuir.6653943832-569642018-09-05T03:51:34Z Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease Thanchanok Puksasook Shinya Kimura Sarin Tadtong Jutamas Jiaranaikulwanitch Jaturong Pratuangdejkul Worawan Kitphati Khanit Suwanborirux Naoki Saito Veena Nukoolkarn Chemistry Medicine Pharmacology, Toxicology and Pharmaceutics © 2017, The Japanese Society of Pharmacognosy and Springer Japan. Abstract: A series of prenylated resveratrol derivatives were designed, semisynthesized and biologically evaluated for inhibition of β-secretase (BACE1) and amyloid-β (Aβ) aggregation as well as free radical scavenging and neuroprotective and neuritogenic activities, as potential novel multifunctional agents against Alzheimer’s disease (AD). The results showed that compound 4b exhibited good anti-Aβ aggregation (IC50 = 4.78 µM) and antioxidant activity (IC50 = 41.22 µM) and moderate anti-BACE1 inhibitory activity (23.70% at 50 µM), and could be a lead compound. Moreover, this compound showed no neurotoxicity along with a greater ability to inhibit oxidative stress on P19-derived neuronal cells (50.59% cell viability at 1 nM). The neuritogenic activity presented more branching numbers (9.33) and longer neurites (109.74 µm) than the control, and was comparable to the quercetin positive control. Taken together, these results suggest compound 4b had the greatest multifunctional activities and might be a very promising lead compound for the further development of drugs for AD. 2018-09-05T03:32:43Z 2018-09-05T03:32:43Z 2017-10-01 Journal 18610293 13403443 2-s2.0-85020739007 10.1007/s11418-017-1097-2 https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85020739007&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/56964
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
topic Chemistry
Medicine
Pharmacology, Toxicology and Pharmaceutics
spellingShingle Chemistry
Medicine
Pharmacology, Toxicology and Pharmaceutics
Thanchanok Puksasook
Shinya Kimura
Sarin Tadtong
Jutamas Jiaranaikulwanitch
Jaturong Pratuangdejkul
Worawan Kitphati
Khanit Suwanborirux
Naoki Saito
Veena Nukoolkarn
Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease
description © 2017, The Japanese Society of Pharmacognosy and Springer Japan. Abstract: A series of prenylated resveratrol derivatives were designed, semisynthesized and biologically evaluated for inhibition of β-secretase (BACE1) and amyloid-β (Aβ) aggregation as well as free radical scavenging and neuroprotective and neuritogenic activities, as potential novel multifunctional agents against Alzheimer’s disease (AD). The results showed that compound 4b exhibited good anti-Aβ aggregation (IC50 = 4.78 µM) and antioxidant activity (IC50 = 41.22 µM) and moderate anti-BACE1 inhibitory activity (23.70% at 50 µM), and could be a lead compound. Moreover, this compound showed no neurotoxicity along with a greater ability to inhibit oxidative stress on P19-derived neuronal cells (50.59% cell viability at 1 nM). The neuritogenic activity presented more branching numbers (9.33) and longer neurites (109.74 µm) than the control, and was comparable to the quercetin positive control. Taken together, these results suggest compound 4b had the greatest multifunctional activities and might be a very promising lead compound for the further development of drugs for AD.
format Journal
author Thanchanok Puksasook
Shinya Kimura
Sarin Tadtong
Jutamas Jiaranaikulwanitch
Jaturong Pratuangdejkul
Worawan Kitphati
Khanit Suwanborirux
Naoki Saito
Veena Nukoolkarn
author_facet Thanchanok Puksasook
Shinya Kimura
Sarin Tadtong
Jutamas Jiaranaikulwanitch
Jaturong Pratuangdejkul
Worawan Kitphati
Khanit Suwanborirux
Naoki Saito
Veena Nukoolkarn
author_sort Thanchanok Puksasook
title Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease
title_short Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease
title_full Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease
title_fullStr Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease
title_full_unstemmed Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease
title_sort semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for alzheimer’s disease
publishDate 2018
url https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85020739007&origin=inward
http://cmuir.cmu.ac.th/jspui/handle/6653943832/56964
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