Pentacyclic triterpenes. Part 1: The first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases

The semi-synthesis, in vitro and in vivo biological evaluation of corosolic acid ( 1) and maslinic acid ( 2) are described. Compounds 1 and 2 represent a new class of inhibitors of glycogen phosphorylases. The semi-synthesis, in vitro and in vivo biological evaluation of corosolic acid ( 1) and masl...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2005-11, Vol.15 (22), p.4944-4948
Hauptverfasser: Wen, Xiaoan, Sun, Hongbin, Liu, Jun, Wu, Guanzhong, Zhang, Luyong, Wu, Xiaoming, Ni, Peizhou
Format: Artikel
Sprache:eng
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Zusammenfassung:The semi-synthesis, in vitro and in vivo biological evaluation of corosolic acid ( 1) and maslinic acid ( 2) are described. Compounds 1 and 2 represent a new class of inhibitors of glycogen phosphorylases. The semi-synthesis, in vitro and in vivo biological evaluation of corosolic acid ( 1) and maslinic acid ( 2) are described. Compounds 1 and 2 represent a new class of inhibitors of glycogen phosphorylases. Both 1 and 2 inhibit the increase of fasted plasma glucose of diabetic mice induced by adrenaline. It is therefore proposed that naturally occurring pentacyclic triterpenes 1 and 2 might reduce blood glucose, at least in part, through inhibiting hepatic glycogen degradation.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.08.026