epi-maslinic-acid has been researched along with maslinic-acid* in 3 studies
3 other study(ies) available for epi-maslinic-acid and maslinic-acid
| Article | Year |
|---|---|
Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.
A series of maslinic acid derivatives have been synthesized by introducing various fused heterocyclic rings at C-2 and C-3 positions. Their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Most of the compounds exhibited a dramatic increase in inhibitory potency and selectivity, the two most potent PTP1B inhibitors 20 (IC(50)=0.61 microM) and 29 (IC(50)=0.64 microM) showed about 10-fold more potent than lead compound maslinic acid. More importantly, 29 possesses the best selectivity of 6.9-fold for PTP1B over TCPTP. Topics: Dose-Response Relationship, Drug; Drug Design; Enzyme Inhibitors; Molecular Conformation; Protein Tyrosine Phosphatase, Non-Receptor Type 1; Stereoisomerism; Structure-Activity Relationship; Triterpenes | 2009 |
Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: synthesis, structure-activity relationships, and X-ray crystallographic studies.
Twenty-five naturally occurring pentacyclic triterpenes, 15 of which were synthesized in this study, were biologically evaluated as inhibitors of rabbit muscle glycogen phosphorylase a (GPa). From SAR studies, the presence of a sugar moiety in triterpene saponins resulted in a markedly decreased activity ( 7, 18- 20) or no activity ( 21, 22). These saponins, however, might find their value as potential natural prodrugs which are much more water-soluble than their corresponding aglycones. To elucidate the mechanism of GP inhibition, we have determined the crystal structures of the GPb-asiatic acid and GPb-maslinic acid complexes. The X-ray analysis indicates that the inhibitors bind at the allosteric activator site, where the physiological activator AMP binds. Pentacyclic triterpenes represent a promising class of multiple-target antidiabetic agents that exert hypoglycemic effects, at least in part, through GP inhibition. Topics: Adenosine Monophosphate; Allosteric Site; Animals; Binding Sites; Crystallography, X-Ray; Glycogen Phosphorylase; Hypoglycemic Agents; Kinetics; Models, Molecular; Muscles; Oleanolic Acid; Pentacyclic Triterpenes; Protein Binding; Protein Conformation; Rabbits; Stereoisomerism; Structure-Activity Relationship; Triterpenes | 2008 |
Pentacyclic triterpenes. Part 2: Synthesis and biological evaluation of maslinic acid derivatives as glycogen phosphorylase inhibitors.
The synthesis of a series of maslinic acid derivatives is described and their effect on rabbit muscle glycogen phosphorylase a evaluated. Within this series of compounds, 15 (IC(50)=7 microM) is the most potent GPa inhibitor. SAR of the maslinic acid derivatives are discussed. Topics: Animals; Enzyme Inhibitors; Glycogen Phosphorylase, Muscle Form; Muscles; Rabbits; Structure-Activity Relationship; Triterpenes | 2006 |