Biological evaluation of de-O-sulfonated analogs of salacinol, the role of sulfate anion in the side chain on the α-glucosidase inhibitory activity

Hypoglycemic Effect of 13-Membered Ring Thiocyclitol, a Novel α-Glucosidase Inhibitor from Kothala-himbutu (Salacia reticulata)

“…It was confirmed that 13-MRT showed more potent -glucosidase inhibitory activities (IC 50 : maltase, 0.23 mM; sucrase, 0.19 mM) than those of salacinol (IC 50 : maltase, 9.6 mM; sucrase, 2.5 mM). 7) This evidence suggested that 13-MRT might be a contributive constituent in the anti-hyperglycemic effect of Kothalahimbutu. In this study, we investigated the effect of 13-MRT on postprandial glucose levels in maltose-and sucrose-loaded rats.…”

Design, synthesis and anti-diabetic activity of some novel xanthone derivatives targeting α-glucosidase

“…Since the discovery of acarbose, first -glucosidase inhibitor lots of synthetic Tanabe et al, 2007;Liu et al, 2007) and natural molecules (Luo et al, 2007;Saludes et al, 2007;Du et al, 2006) reported for the management of type 2 diabetes, but continuous administration of these agents causing adverse effects like diarrhea, abdominal discomfort, flatulence (Campbell et al, 2000), and hepatotoxicity (Hsiao et al, 2006). So, the research continues to find other problem solving alternatives.…”

Synthesis of phosphate derivatives related to the glycosidase inhibitor salacinol

“…In addition, Tanabe et al concluded that the internal sulfate counterion is not necessary for activity since the de-O-sulfonated analogues 27 and 28 showed almost equal inhibitory activities against intestinal a-glucosidases when compared to salacinol (1). 39 Thus, it is likely that an exact phosphate analogue of salacinol (1) will be required in order to provide a definite answer as to whether the presence of a phosphate moiety or the lack of the hydroxyl group at C-2 0 and hydroxymethyl moiety at C-3 0 is the cause of the low activities of compounds 11 and 12 against MGA. …”