Nano-based drug delivery systems used as vehicles to enhance polyphenols therapeutic effect for diabetes mellitus treatment

LC-MS/HRMS Analysis, Anti-Cancer, Anti-Enzymatic and Anti-Oxidant Effects of Boerhavia diffusa Extracts: A Potential Raw Material for Functional Applications

“…For example, acetylcholinesterase is a pharmaceutical target in the treatment of Alzheimer’s disease and its inhibition could help to increase cognitive functions in Alzheimer’s patients [ 54 ]. As another example, amylase and glucosidase are important players in diabetes mellitus and their inhibition is closely related to the control of blood glucose level [ 55 ]. Overall, enzyme inhibitory agents are gaining in importance in the medicinal and pharmaceutical fields.…”

An In Silico and an In Vitro Inhibition Analysis of Glycogen Phosphorylase by Flavonoids, Styrylchromones, and Pyrazoles

“…2-Styrylchromones (16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28)(29) share the styryl group backbone as displayed in the 4-(1-9) and 5-styrylpyrazoles (10)(11)(12)(13)(14)(15). However, no relevant inhibitory activities were found in pyrazole groups.…”

“…Furthermore, different substitutions were assessed at N-1 of the pyrazole moiety, including the phenyl (12) and tosyl groups (13)(14)(15). In the third set of compounds, 2-styrylchromones (16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28)(29), which hold a styryl group at C-2 of the chromone core, nine were hydroxylated (16)(17)(18)(19)(20)(21)(22)(23)(24); one was hydroxylated and methoxylated (25), and four were only methoxylated (26)(27)(28)(29). Among the group 2-styrylchromone-related derivatives (30)(31)(32)(33)(34)(35), which display a 4-arylbuta-1,3-dien-1-yl at the C-2 of the chromone core, three compounds were hydroxylated (30)(31)(32), two were hydroxylated and methoxylated (33)(34), and one was only methoxylated (35).…”

“…The other hydroxylated 2-styrylchromones, 16-20, and 24, also exhibited low or no inhibitory activities at the maximum tested concentrations. Within the hydroxylated and methoxylated derivative (25) and the methoxylated derivatives only (26)(27)(28)(29), low or no inhibitory activities were observed at the highest tested concentration, such as with 2-styrylchromone 26, which has methoxy substituents at C-5 and C-7 of the A ring and C-3 and C-4 of the B ring, with an inhibitory activity of 42.2 ± 5.6%. Therefore, methoxy substituents seem to be disadvantageous for GPa inhibitory activity in the 2-styrylchromone scaffold.…”

“…Flavonoids, are the most abundant polyphenols in the human diet, holding a chromone core. This is a class of plant secondary metabolites widely distributed in nature and are well recognized by their ability to modulate a large number of DM targets [22][23][24][25]. 2-Styrylchromones and 2-styrylchromone-related derivatives [2-(4-arylbuta-1,3-dien-1-yl)chromones], which are structurally related to flavonoids, also belong to the chromone family, and hold a styryl and a 4-arylbuta-1,3-dien-1-yl moiety, respectively, at C-2 of the chromone core.…”