PMID- 19166016 OWN - NLM STAT- MEDLINE DCOM- 20090508 LR - 20240109 IS - 1001-5302 (Print) IS - 1001-5302 (Linking) VI - 33 IP - 19 DP - 2008 Oct TI - [PTP1B inhibitory activities of bromophenol derivatives from algae]. PG - 2238-40 AB - OBJECTIVE: To 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. METHOD: Bromophenols 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. RESULT: Three 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. CONCLUSION: The 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. FAU - Shi, Da-Yong AU - Shi DY AD - Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China. FAU - Xu, Feng AU - Xu F FAU - Li, Jing AU - Li J FAU - Guo, Shu-Ju AU - Guo SJ FAU - Su, Hua AU - Su H FAU - Han, Li-Jun AU - Han LJ LA - chi PT - English Abstract PT - Journal Article PL - China TA - Zhongguo Zhong Yao Za Zhi JT - Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica JID - 8913656 RN - 0 (Phenols) RN - EC 3.1.3.48 (Protein Tyrosine Phosphatase, Non-Receptor Type 1) SB - IM MH - Diabetes Mellitus, Type 2/drug therapy/metabolism MH - Eukaryota/*chemistry MH - Phaeophyceae/chemistry MH - Phenols/*chemistry/*therapeutic use MH - Protein Tyrosine Phosphatase, Non-Receptor Type 1/*antagonists & inhibitors MH - Rhodophyta/chemistry EDAT- 2009/01/27 09:00 MHDA- 2009/05/09 09:00 CRDT- 2009/01/27 09:00 PHST- 2009/01/27 09:00 [entrez] PHST- 2009/01/27 09:00 [pubmed] PHST- 2009/05/09 09:00 [medline] PST - ppublish SO - Zhongguo Zhong Yao Za Zhi. 2008 Oct;33(19):2238-40.