Antihyperglycemic activity of naphthylchalcones

Brine shrimp lethality assay ‘an effective prescreen’: Microwave-assisted synthesis, BSL toxicity and 3DQSAR studies-based designing, docking and antitumor evaluation of potent chalcones

“…Chalcones are gaining importance for their medicinal value and are extensively investigated for their pharmacological importance. They have shown an impressive array of biological activities, including anti-inflammatory (Furusawa et al, 2009;Won et al, 2005;Yang et al, 2007), antitumor (Ahsanullah et al, 2007;Aryapour et al, 2012;Ducki, 2009;Dyrager et al, 2011;Kong et al, 2010;Na et al, 2009;Zhou et al, 2009), antioxidant (Gacche et al, 2008;Ghosh et al, 2009), antiviral (Deng et al, 2007;Kiat et al, 2006), antibacterial (Ansari et al, 2005(Ansari et al, , 2009Sivakumar et al, 2007Sivakumar et al, , 2009, antileshmanial (Boeck et al, 2006;Kayser & Kiderlen, 2001;Liu et al, 2003), antimalarial (Dominguez et al, 2005a,b;Geyer et al, 2009), antihyperglycemic (Damazio et al, 2010) and antituberculotic (Lin et al, 2002). They are also patented as antiangiogenic agents (Bowen et al, 2005), matrix metalloproteinases (MMP's) inhibitors (Kim et al, 2003) and as anticancer agents (Cai et al, 2007).…”

Triterpene derivative: A potential signaling pathway for the fern-9(11)-ene-2α,3β-diol on insulin secretion in pancreatic islet

“…It is known that different substituents at different positions in core structure of a compound can determine biological activity as well as the specific mode of action. Taking it in mind and based in our previous studies [29,37,38]; it can be observed that electron withdrawing groups, such as nitro group, have significantly improved the antihyperglycemic action; a new derivative compound triterpene 2 with a substituent electron withdrawing group in the Aring was synthesized. This p-nitrobenzoyl derivative exhibited a potency about 10 2 and 10 3 fold than the anti-hyperglycemic effect of the natural triterpene 1.…”

“…Triterpenes can regulate glucose serum homeostasis by increasing insulin secretion (secretagogues action) or by stimulating glucose uptake in insulin dependent-tissues (insulinomimetic action) [16] similar to other exogenous compounds (nutraceutical or hypoglycemic drugs) [22,29,37]. Among steroidal structural core, 1,25-D 3 is one of the terpenoids that have been reported as both antihyperglycemic and hypoglycemic compound [14,16,38].…”

Chalcones and their therapeutic targets for the management of diabetes: Structural and pharmacological perspectives

“…The compounds with nitro group at position 3 in the B ring (84) showed effective antihyperglycemic action on serum glucose levels (Fig. 16) [104]. In another study, a series of nitrochalcones demonstrated their ability to increase insulin secretion, in which compounds (85) and (86) stimulated insulin secretion by about 325% and 265%, respectively when compared with the hyperglycemic control group in the respective time-course of study.…”