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Natural Prenylchalconaringenins and Prenylnaringenins as Antidiabetic Agents: α-Glucosidase and α-Amylase Inhibition and in Vivo Antihyperglycemic and Antihyperlipidemic Effects.
  • Hua Sun, Dong Wang, +8 authors Peng Yu
  • Chemistry, Medicine
  • Journal of agricultural and food chemistry
  • 17 February 2017
Results suggest that compound 2 has dual inhibitory activity against α-glucosidase and α-amylase and alleviates diabetic hyperglycemia and hyperlipidemia, making it a potential functional food ingredient and drug candidate for management of type 2 diabetes. Expand
Design, synthesis and evaluation of novel metalloproteinase inhibitors based on L-tyrosine scaffold.
A series of novel L-tyrosine derivatives were designed, synthesized and assayed for their inhibitory activities on matrix metalloproteinase 2 and histone deacetylase 8 and showed inhibitory profiles against MMP-2 and HDAC-8. Expand
SAHA-based novel HDAC inhibitor design by core hopping method.
This work provided an approach to design novel high-efficiency HDAC inhibitors with better ADMET properties and molecular dynamics simulation of the representative compound 101 was performed to study the stability of HDAC8-inhibitor system. Expand
Novel Inhibitor Design for Hemagglutinin against H1N1 Influenza Virus by Core Hopping Method
It has been shown through the subsequent molecular docking studies and molecular dynamic simulations that Neo6 not only assumes more favorable conformation at the binding pocket of HA but also has stronger binding interaction with its receptor. Expand
Find novel dual-agonist drugs for treating type 2 diabetes by means of cheminformatics
Ten novel compounds found by targeting peroxisome proliferator-activated receptors (PPARs) using virtual screening and core hopping approaches are reported, finding that these novel dual agonists not only possessed the same function as ragaglitazar did in activating PPARα and PPARγ, but they also had more favorable conformation for binding to the two receptors. Expand
Identification of novel multitargeted PPARα/γ/δ pan agonists by core hopping of rosiglitazone
Molecular dynamics simulation of the representative Cpd#1 showed more favorable binding conformation for PPARs receptor than the original ligand, which could act as a PPARα/γ/δ pan agonist for novel antidiabetic drug research. Expand
Synthesis, α-glucosidase inhibitory and molecular docking studies of prenylated and geranylated flavones, isoflavones and chalcones.
Three series of prenylated and/or geranylated flavonoids were synthesized and evaluated for their α-glucosidase inhibitory activity and showed that 3',5'-digeranylated chalcone exhibited a competitive inhibitory mode. Expand
The design of novel inhibitors for treating cancer by targeting CDC25B through disruption of CDC25B-CDK2/Cyclin A interaction using computational approaches
This research focused on identifying potential compounds in theory which are able to disrupt transient interactions between CDC25B and its CDK2/Cyclin A substrate and selected the comp#1, as a representative, to be synthesized and assayed for theirCDC25B inhibitory activities. Expand
Multitargeted bioactive ligands for PPARs discovered in the last decade
This review updated and generalized the development of PPARγ partial agonist rosiglitazone,PPARγ antagonists, PPARα/γ dual agonists, PP ARδ partial agonists), PPARδ antagonists,PParα/δ dual agonist, PParγ/ Δ dual agonism, and PPAR α/γ/ δ pan‐agonists published in recent decade. Expand
Efficient enzymatic synthesis of L-rhamnulose and L-fuculose.
Purity of L-rhamnulose or L-fuculose with purity exceeding 99% in more than 80% yield (gram scale) is demonstrated. Expand