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Tigliane Diterpenoids as a New Type of Antiadipogenic Agents Inhibit GRα-Dexras1 Axis in Adipocytes.
A mechanistic study indicated that 1 and 1a could inhibit the glucocorticoid receptor α-Dexras1 axis in adipocyte, leading to the retardation of cell differentiation at the early stage, and may provide a new type of lipid-lowering agents for future antiobesity drug development.
Analogues of xanthones--Chalcones and bis-chalcones as α-glucosidase inhibitors and anti-diabetes candidates.
Discovery of natural alkaloid bouchardatine as a novel inhibitor of adipogenesis/lipogenesis in 3T3-L1 adipocytes.
Natural alkaloid bouchardatine ameliorates metabolic disorders in high‐fat diet‐fed mice by stimulating the sirtuin 1/liver kinase B‐1/AMPK axis
The therapeutic effects of the newly identified bouchardatine (Bou) on obesity‐associated metabolic disorders and the molecular mechanisms of these effects are evaluated.
Design, Synthesis and Evaluation of New Quinazolinone Derivatives that Inhibit Bloom's Syndrome Protein (BLM) Helicase, Trigger DNA damage at the Telomere Region and Synergize with PARP Inhibitors.
- Chen-Xi Wang, Zi-Lin Zhang, Zhishu Huang
- Biology, ChemistryJournal of medicinal chemistry
- 22 July 2020
Compound 9h inhibited the proliferation of the colorectal cell line HCT116 by significantly triggering DNA damage in the telomere region and inducing apoptosis, especially in combination with a PARP inhibitor, suggesting a synthetic lethal effect between the BLM and PARP inhibitors in DDR pathways.
Synthesis and Biological Evaluation of Novel Bouchardatine Derivatives as Potential Adipogenesis/Lipogenesis Inhibitors for Antiobesity Treatment.
The mechanism studies revealed that 3d blocked TG accumulation via activation of the LKB1-AMPK signaling pathway, efficiently down-regulating the expression of key regulators of adipogenesis/lipogenesis, suggesting that3d may be a promising agent for the treatment of obesity and related metabolic disorders.
Euphorhelipanes A and B, Triglyceride-Lowering Euphorbia Diterpenoids with a Bicyclo[4.3.0]nonane Core from Euphorbia helioscopia.
Euphorhelipanes A and B represent the first examples of Euphorbia diterpenoids with a 5/6 fused carbon ring system, and their plausible biosynthetic pathways originating from jatrophanes are proposed.
Bouchardatine analogue alleviates non‐alcoholic hepatic fatty liver disease/non‐alcoholic steatohepatitis in high‐fat fed mice by inhibiting ATP synthase activity
The pharmacological effects of R17 in a model of NAFLD/NASH and its mode of action are examined, which shows benefits in the metabolic syndrome but not in the liver.
Gut Akkermansia muciniphila ameliorates metabolic dysfunction-associated fatty liver disease by regulating the metabolism of L-aspartate via gut-liver axis
Data indicate that the anti-MAFLD activity of A. muciniphila correlated with lipid oxidation and improved gut–liver interactions through regulating the metabolism of L-aspartate, suggesting that the gut bacterium could be a potential agent for clinical intervention in MAFLD.