title: α-Glucosidase and α-Amylase Inhibitors from Arcytophyllum thymifolium.
abstract: Three new coumarins (1-3), a prenylated flavanone (4), and two iridoids (5 and 6), together with 17 known secondary metabolites, were isolated from the aerial parts of Arcytophyllum thymifolium. The structures of the new compounds were elucidated on the basis of their spectroscopic data. The potential hypoglycemic properties of the new and known compounds were evaluated by measuring their α-amylase and α-glucosidase inhibitory effects. The iridoid asperulosidic acid (15) and the flavonoid rhamnetin (13) showed the highest activities versus α-amylase (IC50 = 69.4 ± 3.1 and 73.9 ± 5.9 μM, respectively). In turn, the new eriodictyol derivative 4 exhibited the most potent effect as an α-glucosidase inhibitor, with an IC50 value of 28.1 ± 2.6 μM, and was more active than acarbose, used as a positive control. Modeling studies were also performed to suggest the interaction mode of compound 4 in the α-glucosidase enzyme active site.
authors: Dipartimento di Scienze, Università degli Studi della Basilicata , Viale dell'Ateneo Lucano 10, 85100 Potenza, Italy.
authors: Luigi
authors: L
authors: Milella
authors: Dipartimento di Farmacia, Università di Pisa , Via Bonanno 6 and 33, 56126 Pisa, Italy.
authors: Stella
authors: S
authors: Milazzo
authors: Dipartimento di Farmacia, Università di Pisa , Via Bonanno 6 and 33, 56126 Pisa, Italy.
authors: Marinella
authors: M
authors: De Leo
authors: Departamento de Ciencias de la Vida, Universidad de las Fuerzas Armadas, ESPE , Avenida General Rumiñahui s/n, Sangolqui, Ecuador.
authors: Mariela Beatriz
authors: MB
authors: Vera Saltos
authors: Dipartimento di Scienze, Università degli Studi della Basilicata , Viale dell'Ateneo Lucano 10, 85100 Potenza, Italy.
authors: Immacolata
authors: I
authors: Faraone
authors: Dipartimento di Farmacia, Università di Pisa , Via Bonanno 6 and 33, 56126 Pisa, Italy.|Centro Interdipartimentale di Ricerca "Nutraceutica e Alimentazione per la Salute", Università di Pisa , Via del Borghetto 80, 56124 Pisa, Italy.
authors: Tiziano
authors: T
authors: Tuccinardi
authors: Dipartimento di Farmacia, Università di Pisa , Via Bonanno 6 and 33, 56126 Pisa, Italy.
authors: Margherita
authors: M
authors: Lapillo
authors: Dipartimento di Farmacia, Università degli Studi di Salerno , Via Giovanni Paolo II 132, 84084 Fisciano (SA), Italy.
authors: Nunziatina
authors: N
authors: De Tommasi
authors: Dipartimento di Farmacia, Università di Pisa , Via Bonanno 6 and 33, 56126 Pisa, Italy.|Centro Interdipartimentale di Ricerca "Nutraceutica e Alimentazione per la Salute", Università di Pisa , Via del Borghetto 80, 56124 Pisa, Italy.
authors: Alessandra
authors: A
authors: Braca
mesh_terms: D020909:Acarbose / Q000494:pharmacology; D000465:Algorithms; D003374:Coumarins / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004484:Ecuador; D004791:Enzyme Inhibitors / Q000737:chemistry; D044950:Flavanones; D005419:Flavonoids / Q000302:isolation & purification* / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D039823:Iridoids / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D011794:Quercetin / Q000031:analogs & derivatives / Q000494:pharmacology; D019666:Rubiaceae / Q000737:chemistry*; D000516:alpha-Amylases / Q000037:antagonists & inhibitors*; D000520:alpha-Glucosidases / Q000378:metabolism*
chemical_list: C000617761:(2'R)-7-hydroxy-8-(2',3'-dihydroxyisopentyl)-6-methoxycoumarin; C000617760:(2S)-7-prenyloxyeriodictyol; C000617763:5'-hydroxy-3'-dehydrotoddanin; C000617762:6-demethyl-5'-hydroxy-3'-dehydrotoddanin; D003374:Coumarins; D004791:Enzyme Inhibitors; D044950:Flavanones; D005419:Flavonoids; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D039823:Iridoids; C063423:rhamnetin; D011794:Quercetin; D000516:alpha-Amylases; D000520:alpha-Glucosidases; D020909:Acarbose