Publication: Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease
3
Issued Date
2017-10-01
Resource Type
ISSN
18610293
13403443
13403443
Other identifier(s)
2-s2.0-85020739007
Rights
Mahidol University
Rights Holder(s)
SCOPUS
Bibliographic Citation
Journal of Natural Medicines. Vol.71, No.4 (2017), 665-682
Suggested Citation
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. Journal of Natural Medicines. Vol.71, No.4 (2017), 665-682. doi:10.1007/s11418-017-1097-2 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/42199
Research Projects
Organizational Units
Authors
Journal Issue
Thesis
Title
Semisynthesis and biological evaluation of prenylated resveratrol derivatives as multi-targeted agents for Alzheimer’s disease
Abstract
© 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.