Abstract
An organic layer prepared from the Chinese crude drug 'Sang-Bai-Pi' (Morus root bark) was studied in order to identify the inhibitory compounds for protein tyrosine phosphatase 1B (PTP1B). Bioassay-guided fractionation resulted in the isolation of sanggenon C (1), sanggenon G (2), mulberrofuran C (3) and kuwanon L (4) as PTP1B inhibitors, along with moracin O (5) and moracin P (6). Compounds 1-4 inhibited PTP1B with IC(50) values ranging from 1.6+/-0.3 microM to 16.9+/-1.1 microM.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Drugs, Chinese Herbal / chemistry
-
Drugs, Chinese Herbal / pharmacology
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / isolation & purification*
-
Enzyme Inhibitors / pharmacology*
-
Humans
-
Inhibitory Concentration 50
-
Kinetics
-
Morus / chemistry*
-
Plant Bark / chemistry
-
Plant Roots / chemistry*
-
Protein Tyrosine Phosphatase, Non-Receptor Type 1
-
Protein Tyrosine Phosphatases / antagonists & inhibitors*
-
Protein Tyrosine Phosphatases / metabolism
Substances
-
Drugs, Chinese Herbal
-
Enzyme Inhibitors
-
PTPN1 protein, human
-
Protein Tyrosine Phosphatase, Non-Receptor Type 1
-
Protein Tyrosine Phosphatases