Inhibition of bromophenols against PTP1B and anti-hyperglycemic effect of Rhodomela confervoides extract in diabetic rats  

作　　者：SHI DaYong XU Feng HE Juan LI Jing FAN Xiao HAN LiJun 

机构地区：[1]Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China [2]The Affiliated Hospitai of Medical College, Qingdao University, Qingdao 266003, China

出　　处：《Chinese Science Bulletin》2008年第16期2476-2479,共4页

基　　金：the National 863 Projects of China (Grant Nos.2007AA09Z410 and 2007AA091604);Key Innovative Project of the Chinese Academy of Sciences (Grant No. KZCX2-YW-209)

摘　　要：Protein tyrosine phosphatase 1B (PTP1B) plays an important role as a negative regulator in insulin signaling pathways. PTP1B is an effective target for the treatment of type 2 diabetes mellitus. Four bromophenol derivatives from red algae Rhodomela confervoides, 2,2′,3,3′-tetrabromo-4,4′,5,5′-tetra- hydroxydiphenyl methane (1), 3-bormo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl) pyrocatechol (2), bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (3) and 2,2′,3-tribromo-3′,4,4′,5-tetrahydroxy-6′-ethyloxy- methyldiphenylmethane (4) showed significant inhibitory activity against PTP1B (IC50 were 2.4, 1.7, 1.5 and 0.84 μmol/L, respectively) as potential therapeutical agents for the treatment of type 2 diabetes mellitus. The anti-hyperglycemic effects of the ethanol extracts from R. confervoides on streptozoto- cin-induced diabetes (STZ-diabetes) in male Wistar rats fed with high fat diet were investigated. The STZ-diabetic rats treated with medium-dose and high-dose alga extracts showed remarkable reductions in fasting blood glucose (FBG) as compared with the STZ-diabetic control. The results indicate that the in vivo anti-hyperglycemic activity of the R. confervoides extracts can be partially attributed to the in- hibitory actions against PTP1B of the bromophenol derivatives and that may be of clinical importance in improving the management of type 2 diabetes mellitus.Protein tyrosine phosphatase 1B （PTPIB） plays an important role as a negative regulator In insulin signaling pathways. PTPIB is an effective target for the treatment of type 2 diabetes mellitus. Four bromophenol derivatives from red algae Rhodomela confervoides, 2,2＇,3,3＇-tetrabromo-4,4＇,5,5＇-tetrahydroxydiphenyl methane （1）, 3-bormo-4,5-bis（2,3-dibromo-4,5-dihydroxybenzyl） pyrocatechol （2）, bis（2,3-dibromo-4,5-dihydroxybenzyl） ether （3） and 2,2＇,3-tribromo-3＇,4,4＇,5-tetrahydroxy-6＇-ethyloxymethyldiphenylmethane （4） showed significant inhibitory activity against PTPIB （IC50 were 2.4, 1.7, 1.5 and 0.84 μmol/L, respectively） as potential therapeutical agents for the treatment of type 2 diabetes mellitus. The anti-hyperglycemic effects of the ethanol extracts from If. confervoides on streptozotocin-induced diabetes （STZ-diabetes） in male Wistsr rats fed with high fat diet were investigated. The STZ-diabetic rats treated with medium-dose and high-dose alga extracts showed remarkable reductions in fasting blood glucose （FBG） as compared with the STZ-diabetic control. The results indicate that the in vivo anti-hyperglycemic activity of the R. confervoides extracts can be partially attributed to the inhibitory actions against PTPIB of the bromophenol derivatives and that may be of clinical Importance in improving the management of type 2 diabetes mellitus.

关 键 词：溴苯酚 抑制作用 萃取液 糖尿病 

分 类 号：R587.1[医药卫生—内分泌]