2024-03-28T10:27:44Z
https://u-ryukyu.repo.nii.ac.jp/oai
oai:u-ryukyu.repo.nii.ac.jp:02012160
2023-08-03T05:31:23Z
1642838163960:1642838338003
1642838403551:1642838407312
Anti-Inflammatory, Anti-Diabetic, and Anti-Alzheimer’s Effects of Prenylated Flavonoids from Okinawa Propolis: An Investigation by Experimental and Computational Studies
Shahinozzaman, Md
Taira, Nozomi
Ishii, Takahiro
Halim, Mohammad A
Hossain, Amzad Md
Tawata, Shinkichi
open access
Okinawa propolis
prenylated flavonoids
inflammation
α-glucosidase
acetylcholinesterase
molecular docking
density functional theory
p21-activated kinase 1
Okinawa propolis (OP) and its major ingredients were reported to have anti-cancer effects and lifespan-extending effects on Caenorhabditis elegans through inactivation of the oncogenic kinase, p21-activated kinase 1 (PAK1). Herein, five prenylated flavonoids from OP, nymphaeol-A (NA), nymphaeol-B (NB), nymphaeol-C (NC), isonymphaeol-B (INB), and 3′-geranyl-naringenin (GN), were evaluated for their anti-inflammatory, anti-diabetic, and anti-Alzheimer’s effects using in vitro techniques. They showed significant anti-inflammatory effects through inhibition of albumin denaturation (half maximal inhibitory concentration (IC50) values of 0.26–1.02 µM), nitrite accumulation (IC50 values of 2.4–7.0 µM), and cyclooxygenase-2 (COX-2) activity (IC50 values of 11.74–24.03 µM). They also strongly suppressed in vitro α-glucosidase enzyme activity with IC50 values of 3.77–5.66 µM. However, only INB and NA inhibited acetylcholinesterase significantly compared to the standard drug donepezil, with IC_50 values of 7.23 and 7.77 µM, respectively. Molecular docking results indicated that OP compounds have good binding affinity to the α-glucosidase and acetylcholinesterase proteins, making non-bonded interactions with their active residues and surrounding allosteric residues. In addition, none of the compounds violated Lipinski’s rule of five and showed notable toxicity parameters. Density functional theory (DFT)-based global reactivity descriptors demonstrated their high reactive nature along with the kinetic stability. In conclusion, this combined study suggests that OP components might be beneficial in the treatment of inflammation, type 2 diabetes mellitus, and Alzheimer’s disease.
論文
MDPI
2018-09-17
eng
journal article
VoR
http://hdl.handle.net/20.500.12000/44786
http://hdl.handle.net/20.500.12000/44786
https://u-ryukyu.repo.nii.ac.jp/records/2012160
https://doi.org/10.3390/molecules23102479
10.3390/molecules23102479
1420-3049
Molecules
23
10
1
18
https://u-ryukyu.repo.nii.ac.jp/record/2012160/files/vol23_n10_p1.pdf