1571-72-8Relevant articles and documents
Novel SIRT1 activator MHY2233 improves glucose tolerance and reduces hepatic lipid accumulation in db/db mice
Kim, Min Jo,An, Hye Jin,Kim, Dae Hyun,Lee, Bonggi,Lee, Hye Jin,Ullah, Sultan,Kim, Su Jeong,Jeong, Hyoung Oh,Moon, Kyoung Mi,Lee, Eun Kyeong,Yang, Jungho,Akter, Jinia,Chun, Pusoon,Moon, Hyung Ryong,Chung, Hae Young
, p. 684 - 688 (2018)
The NAD+-dependent deacetylase SIRT1, which is associated with the improvement of metabolic syndromes, such as type 2 diabetes, is a well-known longevity-related gene. Several in vitro and in vivo studies have shown the known protective effects of SIRT1 activators, such as resveratrol and SRT1720, on diabetes- or obesity-induced fatty liver and insulin resistance. Here, we newly synthesized 18 benzoxazole hydrochloride derivatives based on the structure of resveratrol and SRT1720. We performed an in vitro SIRT1 activity assay to identify the strongest SIRT1 activator. The assay confirmed MHY2233 to be the strongest SIRT1 activator (1.5-fold more potent than resveratrol), and docking simulation showed that the binding affinity of MHY2233 was higher than that of resveratrol and SRT1720. To investigate its beneficial effects, db/db mice were orally administered MHY2233 for 1 month, and various metabolic parameters were assessed in the serum and liver tissues. MHY2233 markedly ameliorated insulin signaling without affecting body weight in db/db mice. In particular, the mRNA expression of lipogenic genes, such as acetyl CoA carboxylase, fatty acid synthase, and sterol regulatory element-binding protein, which increased in db/db mice, decreased following oral treatment with MHY2233. In conclusion, the novel SIRT1 activator MHY2233 reduced lipid accumulation and improved insulin resistance. This finding may contribute toward therapeutic approaches for fatty liver disease and glucose tolerance.
Novel SIRT 1 activator and medical use thereof
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Paragraph 0084; 0283; 0286; 0288; 0289, (2018/11/27)
The present invention relates to an SIRT 1 activator and a medical purpose thereof. According to the present invention, the novel SIRT 1 activator based on a benzo[d]oxazole frame, a hydrate thereof, a crystal form thereof, and salt thereof are manufactured. According to the present invention, it is confirmed that the SIRT 1 activator has improvement effects on obesity, insulin resistance, and dyslipidemia, improvement effect on fatty liver, prevention effects on cell aging and oxidation stress, and collagen composition and wrinkle improvement effect. Therefore, the novel SIRT 1 activator having the same effect can be usefully used as a pharmaceutical composition for preventing or treating a metabolic and liver diseases, a cosmetic composition for preventing or treating wrinkles, and a health food composition for preventing cell aging, wherein the metabolic disease includes obesity, diabetes, and dyslipidemia and the liver disease includes an alcoholic or nonalcoholic fatty liver and fatty hepatitis.COPYRIGHT KIPO 2018
Amino-benzoic acids and derivatives, and methods of use
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, (2008/06/13)
The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.