Tổng hợp và đánh giá tác động ức chế lipase tuỵ của các dẫn chất methylxanthin thế ở N7

Methylxanthines such as caffeine, theobromine, and theophylline were reported to exhibit pancreatic lipase inhibitory activity. In this study, methylxanthine derivatives with imine and ester functional group at N7 were synthesized to explore their ability to inhibit lipase. Three imine derivatives were synthesized from theophylline-7-acetaldehyde and corresponding amines. Four ester derivatives were from acefylline and corresponding alcohols. The structures of the compounds were characterized by IR, MS and NMR spectroscopy. Their in vitro pancreatic lipase inhibitory activities were determined using porcine pancreatic lipase and p-nitrophenyl palmitate as substrate. Out of 7 compounds, 2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)acetaldehyde oxime (1a) showed the most potential pancreatic lipase inhibitory activity (IC₅₀ = 18.76 µM), 13 times higher than caffeine.

Keywords: Pancreatic lipase inhibition, obesity, methylxanthine, enzymatic assay.

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