Quercetin (cas 117-39-5) based derivatives as sirtuin inhibitors
-
Add time:09/02/2019 Source:sciencedirect.com
Polyphenols synthesized by plants and fungi have various pharmacological effects. The ability of polyphenols to modulate sirtuins has gained considerable interest due to the role of sirtuins in aging, insulin sensitivity, lipid metabolism, inflammation, and cancer. In particular, sirtuin 6 (SIRT6) has gained importance in regulating a variety of cellular processes, including genomic stability and glucose metabolism. On the other hand, Quercetin (cas 117-39-5) has been demonstrated to modulate sirtuins and to protect against several chronic diseases. In this study, two quercetin derivatives, diquercetin and 2-chloro-1,4-naphtoquinone-quercetin, were identified as promising SIRT6 inhibitors with IC50 values of 130 μM and 55 μM, respectively. 2-Chloro-1,4-naphtoquinone-quercetin also showed potent inhibition against SIRT2, with an IC50 value of 14 μM. Diquercetin increased the Km value of NAD+, whereas 2-chloro-1,4-naphthoquinone-quercetin increased the Km value of the acetylated substrate. Molecular docking studies suggest that diquercetin prefers the binding site of the nicotinamide (NAM) moiety, whereas 2-chloro-1,4-naphtoquinone-quercetin prefers to dock into the substrate binding site. Overall, the results of in vitro studies and molecular modeling indicate that diquercetin competes with nicotinamide adenine dinucleotide (NAD+), whereas 2-chloro-1,4-naphthoquinone-quercetin competes with the acetylated substrate in the catalytic site of SIRT6. Natural polyphenolic compounds targeting sirtuins show promise as a new approach in the search for novel and effective treatments for age-related diseases.
We also recommend Trading Suppliers and Manufacturers of Quercetin (cas 117-39-5). Pls Click Website Link as below: cas 117-39-5 suppliers
Prev:In silico and in vitro approach of Allium cepa and isolated Quercetin (cas 117-39-5) against MDR bacterial strains and Mycobacterium smegmatis
Next:Antioxidant activity of Quercetin (cas 117-39-5) in Eudragit-coated liposomes for intestinal delivery) - 【Back】【Close 】【Print】【Add to favorite 】
- Related Information
- Quercetin (cas 117-39-5) suppressed NADPH oxidase-derived oxidative stress via heme oxygenase-1 induction in macrophages09/04/2019
- Antioxidant activity of Quercetin (cas 117-39-5) in Eudragit-coated liposomes for intestinal delivery09/03/2019
- In silico and in vitro approach of Allium cepa and isolated Quercetin (cas 117-39-5) against MDR bacterial strains and Mycobacterium smegmatis09/01/2019
- Quercetin (cas 117-39-5) glycosides prevent dexamethasone-induced muscle atrophy in mice08/31/2019
- Supercritical CO2 impregnation of silica microparticles with Quercetin (cas 117-39-5)08/30/2019
- Quercetin (cas 117-39-5) inhibited mesangial cell proliferation of early diabetic nephropathy through the Hippo pathway08/29/2019
- Original articleAntioxidant, antimicrobial and cytotoxic activities of gold nanoparticles capped with Quercetin (cas 117-39-5)08/28/2019
- Research ArticleIn vitro bioaccessibility and bioavailability of Quercetin (cas 117-39-5) from the Quercetin (cas 117-39-5)-fortified bread products with reduced glycemic potential08/27/2019
- Original articleRedox properties of individual Quercetin (cas 117-39-5) moieties08/26/2019