Inhibition of bromophenols against PTP1B and anti-hyperglycemic effect of Rhodomela confervoides extract in diabetic rats
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- 作者：DaYong Shi (1)
Feng Xu (2)
Juan He (2)
Jing Li (1)
Xiao Fan (1)
LiJun Han (1) - 关键词：bromophenol derivatives ; Rhodomela confervoides ; inhibition against PTP1B ; anti ; hyperglycemic
- 刊名：Chinese Science Bulletin
- 出版年：2008
- 出版时间：August 2008
- 年：2008
- 卷：53
- 期：16
- 页码：2476-2479
- 全文大小：611KB
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Feng Xu (2)
Juan He (2)
Jing Li (1)
Xiao Fan (1)
LiJun Han (1)
1. Institute of Oceanology, Chinese Academy of Sciences, Qingdao, 266071, China
2. The Affiliated Hospital of Medical College, Qingdao University, Qingdao, 266003, China - ISSN：1861-9541
文摘
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 streptozotocin-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 inhibitory actions against PTP1B of the bromophenol derivatives and that may be of clinical importance in improving the management of type 2 diabetes mellitus.