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

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Issued Date

2017

Resource Type

Article

File Type

application/pdf

ISSN

13403443

DOI

10.1007/s11418-017-1097-2

Other identifier(s)

2-s2.0-85020739007

Rights Holder(s)

มหาวิทยาลัยศรีนครินทรวิโรฒ

Bibliographic Citation

Journal of Natural Medicines. Vol 71, No.4 (2017), p.665-682

Suggested Citation

Puksasook T., Kimura S., Tadtong S., Jiaranaikulwanitch J., Pratuangdejkul J., Kitphati W., Suwanborirux K., Saito N., Nukoolkarn V. Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease. Journal of Natural Medicines. Vol 71, No.4 (2017), p.665-682. doi:10.1007/s11418-017-1097-2 Retrieved from: https://hdl.handle.net/20.500.14740/4072

Title

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

Author(s)

Puksasook T.
 Kimura S.
 Tadtong S.
 Jiaranaikulwanitch J.
 Pratuangdejkul J.
 Kitphati W.
 Suwanborirux K.
 Saito N.
 Nukoolkarn V.

Abstract

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. © 2017, The Japanese Society of Pharmacognosy and Springer Japan.

Subject(s)

3 ethoxy 4',5 hydroxystilbene
 3 methoxy 4',5 hydroxystilbene
 3,4' diethoxy 5 hydroxystilbene
 3,4' dimethoxy 5 hydroxystilbene
 3,5,4' tri(methoxymethoxy) 4 prenylstilbene
 3,5,4' tri(methoxymethoxy)stilbene
 3,5,4' triethoxystilbene
 3,5,4' trihydroxy 2 geranylstilbene
 3,5,4' trihydroxy 2 prenylstilbene
 3,5,4' trihydroxy 2,6 geranylstilbene
 3,5,4' trihydroxy 2,6 prenylstilbene
 3,5,4' trihydroxy 4 geranylstilbene
 3,5,4' trihydroxy 4 prenylstilbene
 3,5,4' trimethoxystilbene
 4' ethoxy 3,5 dihydroxystilbene
 4' methoxy 3,5 dihydroxystilbene
 Ascorbic acid
 Beta secretase
 Beta secretase inhibitor
 Calbiochem
 Curcumin
 Quercetin
 Resveratrol
 Unclassified drug
 Amyloid beta protein
 Antioxidant
 Neuroprotective agent
 Plant extract
 Resveratrol
 Secretase
 Stilbene derivative
 Alzheimer disease
 Animal cell
 Antioxidant activity
 Article
 Cell viability
 Cell viability assay
 Controlled study
 Drug structure
 Drug synthesis
 Embryo
 IC50
 Molecular docking
 Mouse
 Nerve cell
 Nerve cell differentiation
 Neurite
 Neuroprotection
 Nonhuman
 Oxidative stress
 P19 cell line
 Alzheimer disease
 Antagonists and inhibitors
 Cell culture technique
 Drug effects
 Human
 Metabolism
 Prenylation
 Alzheimer Disease
 Amyloid beta-Peptides
 Amyloid Precursor Protein Secretases
 Antioxidants
 Cell Culture Techniques
 Humans
 Neurites
 Neurons
 Neuroprotective Agents
 Oxidative Stress
 Plant Extracts
 Prenylation
 Stilbenes

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URI

https://hdl.handle.net/20.500.14740/4072

Collections

Scopus: Year 1983-2021

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