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Screening for Thermotoga maritima Membrane-Bound Pyrophosphatase Inhibitors
Published on: November 23, 2019
[PTP1B inhibitory activities of bromophenol derivatives from algae]
Da-Yong Shi1, Feng Xu, Jing Li
1Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China.
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.
