PTP1B inhibitory activities of bromophenol derivatives from algae.
- Author:
Da-Yong SHI
1
;
Feng XU
;
Jing LI
;
Shu-Ju GUO
;
Hua SU
;
Li-Jun HAN
Author Information
- Publication Type:Journal Article
- MeSH: Diabetes Mellitus, Type 2; drug therapy; metabolism; Eukaryota; chemistry; Phaeophyta; chemistry; Phenols; chemistry; therapeutic use; Protein Tyrosine Phosphatase, Non-Receptor Type 1; antagonists & inhibitors; Rhodophyta; chemistry
- From: China Journal of Chinese Materia Medica 2008;33(19):2238-2240
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo study the protein tyrosine phosphatase-1B (PTP1B) inhibitory activity of natural products from algae aiming at searching for new way for the treatment of type 2 diabetes mellitus (T2DM) and obesity.
METHODBromophenols derivatives from algae were screened against the PTP1B by the colorimetric assay with GST/PTP1B fusion protein. The Me2SO was distributed as the full enzyme activity, and Na3VO4 (IC50 2 micromol L(-1)) was distributed as the positive control. Inhibition rate was assayed and IC50 were calculated by LOGIT method.
RESULTThree bromophenols from Rhodomela confervoides and Leathesia nana, 3, 4-dibromo-5-(methoxymethyl)-1, 2-benzenediol (1), 2-methyl-3-(2, 3-dibromo4, 5-dihydroxy)-propylaldehyde (2) and 3-(2, 3-dibromo-4, 5-dihydroxy-phenyl)-4-bromo-5, 6-dihydroxy-1, 3-dihydroiso-benzofuran (3) showed significant inhibitory activity against PTP1B. IC50 values were 3.4 +/- micromol L(-1), 4.5 micromol L(-1) and 2.8 micromol L(-1), respectively.
CONCLUSIONThe results prove that three bromophenol derivatives from algae with significant inhibitory activity against PTP1B were potential and effective therapeutic agents for treatment of T2DM and obesity.
