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. 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.
Wen
Xiaoan
X
Department of Medicinal Chemistry, College of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
Sun
Hongbin
H
Liu
Jun
J
Wu
Guanzhong
G
Zhang
Luyong
L
Wu
Xiaoming
X
Ni
Peizhou
P
D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D003500:Cyclization; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000145:classification* / Q000494:pharmacology; D005215:Fasting; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D051379:Mice; D015394:Molecular Structure; D009132:Muscles / Q000187:drug effects / Q000201:enzymology; D051381:Rats; D014315:Triterpenes / Q000737:chemistry* / Q000494:pharmacology*
D001786:Blood Glucose; D004791:Enzyme Inhibitors; D014315:Triterpenes; D024981:Glycogen Phosphorylase