Acetylcholinesterase (AChE) and β-secretase (BACE-1) have become attractive therapeutic targets for Alzheimer’s disease (AD). Flavones are flavonoid derivatives with various bioactive effects, including AChE and BACE-1 inhibition. In the present work, a series of 14 flavone derivatives was synthesized in relatively high yields (35–85%). Six of the synthetic flavones (B4, B5, B6, B8, D6 and D7) had completely new structures. The AChE and BACE-1 inhibitory activities were tested, giving pIC50 3.47–4.59 (AChE) and 4.15–5.80 (BACE-1). Three compounds (B3, D5 and D6) exhibited the highest biological effects on both AChE and BACE-1. A molecular docking investigation was conducted to explain the experimental results. These molecules could be employed for further studies to discover new structures with dual action on both AChE and BACE-1 that could serve as novel therapies for AD.

Alzheimer’s disease (AD) is an irreversible neurodegenerative disease that affects many older people adversely. AD has been putting a huge socioeconomic burden on the healthcare systems of many developed countries with aging populations. The need for new therapies that can halt or reverse the progression of the disease is now extremely great. A research approach in the finding new treatment for AD that has attracted much interest from scientists for a long time is the reestablishment of cholinergic transmission through inhibition of acetylcholinesterase (AChE). Naringenin is a flavonoid with the potential inhibitory activity against AChE. From naringenin, many other flavonoid derivatives, such as flavanones and chalcones, can be synthesized. In this study, by applying the Williamson method, nine flavonoid derivatives were synthesized, including four flavanones and five chalcones. The evaluation of AChE inhibitory activity by the Ellman method showed that there were four substances (2, 4, 5, and 7) with relatively good biological activities (IC50 < 100 μM), and these biological activities were better than that of naringenin. The molecular docking revealed that strong interactions with amino acid residue Ser200 of the catalytic triad and those of the peripheral region of the enzyme were crucial for strong effects against AChE. Compound 7 had the strongest AChE inhibitory activity (IC50 13.0 ± 1.9 μM). This substance could be used for further studies.

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The vegetable leaf miner, Liriomyza sativae (Blanchard) is a serious insect pest on vegetable and ornamental crops in the whole of Vietnam. It was controlled by a wide range of conventional insecticides. Since there is a limited recommendation on insecticide application, growers continue to use whatever is available. This study was carried out at Entomology Laboratory, Faculty of Agronomy, University of Agriculture and Forestry, Hue University, Vietnam during 2021-22 to determine the susceptibility of larval and adult stages of L. sativae to four insecticides (e.g., lambda-cyhalothrin, abamectin, cypermethrin and clothianidin) currently used for the management of the leaf miner. Among four tested insecticides, abamectin was highly effective on larvae and moderately effective on adults of L. satiave. Lambda-cyhalothrin and cypermethrin were moderately effective on either larvae and adults of the leaf miner. Clothianidin was least effective against the leaf miner. These results suggest that abamectin, lambda-cyhalothrin and cypermethrin can be rotationally used for the management of L. sativae.