Inhibitory activity against acetylcholinesterase

Phytochemical study of Knema pachycarpa leaves led to the isolation of ten compounds. Their chemical structures were determined as (7''R, 8''R)-hydnocarpin D, (7''R, 8''R)-hydnocarpin, sinaicitin, (-)-globulol, β-caryolanol, phytol, biochanin A, chrysoeriol, tanoside II and astragalin using NMR and MS spectral data. Among the isolates, (7''R, 8''R)-hydnocarpin showed good cytotoxic activity against KB, HepG-2, Lu and MCF-7 cancer cell lines with IC50 values from 13.99±0.62 ug/mL to 30.65±1.44 ug/mL.

6p dianmotminh02 03-05-2024 1 1   Download

The compounds were identified by the use of 1D- and 2D-NMR and UV spectroscopic techniques and by comparisons with the reported data. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the acetone, methanol, and water extracts of the plant and of the flavones penduletin and apigenin were evaluated at 200 µg/mL. The water extract exhibited better activity against the enzyme AChE as compared to both the acetone and the methanol extracts. Penduletin (1) showed significant activity against BChE (66.

9p langthannam 29-12-2021 10 0   Download

Tanacetum mucroniferum Hub.-Mor. & Grierson was collected from Sakaltutan in Erzincan Province of Turkey. Comparative phytochemical investigation was carried out on the ethyl acetate and methanol extracts of the plant. The secondary metabolites were isolated and purified by chromatographic methods such as column chromatography, medium pressure liquid chromatography, high-performance thin-layer chromatography, and preparative thin-layer chromatography.

7p tudichquannguyet 29-11-2021 9 1   Download

In this study, a new series of Mannich bases, 3-(aminomethyl)-6-{3-[4-(trifluoromethyl)phenyl]acryloyl}-2(3H)- benzoxazolones (1a–g), were synthesized by the Mannich reaction. Inhibitory effects of the newly synthesized compounds towards carbonic anhydrases (CAs) and acetylcholinesterase (AChE) enzymes were evaluated to find out new potential drug candidate compounds. According to the inhibitory activity results, Ki values of the compounds 1 and 1a–g were in the range of 12.3 ± 1.2 to 154.0 ± 9.3 nM against hCA I, and they were in the range of 8.6 ± 1.9 to 41.0 ± 5.5 nM against hCA II.

14p tudichquannguyet 29-11-2021 6 1   Download

In this study, the synthesis of new monostyryl (BDPY-2) and distyryl BODIPY dyes (BDPY-4, BDPY-5) containing pyridine groups has been reported for the first time. The acetylcholinesterase from Electrophorus electricus (AChE), butyrylcholinesterase from equine serum (BuChE), α-glucosidase from Saccharomyces cerevisiae and DNA hydrolytic cleavage actions of BDPY-2, BDPY-4, BDPY5 were investigated using various techniques. The results indicated that the compounds had varying inhibition properties against AChE, BuChE, and α-glucosidase.

14p tudichquannguyet 29-11-2021 3 1   Download