Protein tyrosine phosphatase 1B inhibitory activities of ursane- and lupane-type triterpenes from Sorbus pohuashanensis

D Li, W Li, K Higai, K Koike - Journal of natural medicines, 2014 - Springer
D Li, W Li, K Higai, K Koike
Journal of natural medicines, 2014Springer
Protein tyrosine phosphatase 1B (PTP1B) is a non-transmembrane protein tyrosine
phosphatase, and has received much attention as a molecular target for the treatment of
insulin resistance diseases because of its critical roles in negatively regulating insulin-and
leptin-signaling cascades. Six ursane-type triterpenes, 3β-acetoxy-urs-12-ene-28-oic acid
(1), pomolic acid-3β-acetate (2), pomolic acid (3), ursolaldehyde (4), euscaphic acid (5) and
3β-acetoxy-urs-11-en-28, 13-olide (6), and a lupane-type triterpene, betulinic acid (7), from …
Abstract
Protein tyrosine phosphatase 1B (PTP1B) is a non-transmembrane protein tyrosine phosphatase, and has received much attention as a molecular target for the treatment of insulin resistance diseases because of its critical roles in negatively regulating insulin- and leptin-signaling cascades. Six ursane-type triterpenes, 3β-acetoxy-urs-12-ene-28-oic acid (1), pomolic acid-3β-acetate (2), pomolic acid (3), ursolaldehyde (4), euscaphic acid (5) and 3β-acetoxy-urs-11-en-28,13-olide (6), and a lupane-type triterpene, betulinic acid (7), from the fruits of Sorbus pohuashanensis, exhibited significant PTP1B inhibitory activity, with IC50 values ranging from 3.5 to 54.8 μM. Kinetics analyses revealed that compounds 2, 3, and 7 are non-competitive PTP1B inhibitors, and compounds 1 and 6 are mixed-type PTP1B inhibitors.
Springer