HPN, a Synthetic Analogue of Bromophenol from Red Alga Rhodomela confervoides: Synthesis and Anti-Diabetic Effects in C57BL/KsJ-db/db Mice
作者： Dayong Shi , Shuju Guo , Bo Jiang , Chao Guo , Tao Wang
DOI: 10.3390/MD11020350
关键词:
摘要: 3,4-Dibromo-5-(2-bromo-3,4-dihydroxy-6-(isopropoxymethyl)benzyl)benzene-1,2-diol (HPN) is a synthetic analogue of 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(ethoxymethyl) benzyl)benzene-1,2-diol (BPN), which isolated from marine red alga Rhodomela confervoides with potent protein tyrosine phosphatase 1B (PTP1B) inhibition (IC50 = 0.84 mu mol/L). The in vitro assay showed that HPN exhibited enhanced inhibitory activity against PTP1B IC50 0.63 mol/L and high selectivity other PTPs (T cell (TCPTP), leucocyte antigen-related (LAR), Src homology 2-containing phosphatase-1 (SHP-1) SHP-2). results antihyperglycemic using db/db mouse model demonstrated significantly decreased plasma glucose (P < 0.01) after eight weeks treatment period. lowered serum triglycerides total cholesterol concentration dose-dependent manner. Besides, both the medium dose groups remarkably HbA1c levels 0.05). group markedly insulin level compared to 0.05), whereas effects were less than positive drug rosiglitazone. Western blotting pancreatic tissue. Last but not least, an intraperitoneal tolerance test Sprague-Dawley rats indicate have similar as therefore potential for development treatments Type 2 diabetes.
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