PMID- 28811203
OWN - NLM
STAT- MEDLINE
DCOM- 20180709
LR  - 20180709
IS  - 1879-0003 (Electronic)
IS  - 0141-8130 (Linking)
VI  - 106
DP  - 2018 Jan
TI  - BPN, a marine-derived PTP1B inhibitor, activates insulin signaling and improves 
      insulin resistance in C2C12 myotubes.
PG  - 379-386
LID - S0141-8130(17)31187-X [pii]
LID - 10.1016/j.ijbiomac.2017.08.042 [doi]
AB  - Insulin resistance is a key feature of type 2 diabetes mellitus (T2DM) and is 
      characterized by defects in insulin signaling. Protein tyrosine phosphatase 1B 
      (PTP1B) is a major negative regulator of insulin signaling cascade and has 
      attracted intensive investigation in recent T2DM therapy study. BPN, a 
      marine-derived bromophenol compound, was isolated from the red alga Rhodomela 
      confervoides. This study investigated the effects of BPN on the insulin signaling 
      pathway in insulin-resistant C2C12 myotubes by inhibiting PTP1B. Molecular 
      docking study and analysis of small- molecule interaction with PTP1B all showed 
      BPN inhibited PTP1B activity via binding to the catalytic site through hydrogen 
      bonds. We then found that BPN permeated into C2C12 myotubes, on the one hand, 
      activated insulin signaling in an insulin-independent manner in C2C12 cells; on 
      the other hand, ameliorated palmitate-induced insulin resistance through 
      augmenting insulin sensitivity. Moreover, our studies also showed that PTP1B 
      inhibition by BPN increased glucose uptake in normal and insulin-resistant C2C12 
      myotubes through glucose transporter 4 (GLUT4) translocation. Taken together, BPN 
      activates insulin signaling and alleviates insulin resistance and represents a 
      potential candidate for further development as an antidiabetic agent.
CI  - Copyright (c) 2017 Elsevier B.V. All rights reserved.
FAU - Xu, Qi
AU  - Xu Q
AD  - Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese 
      Academy of Sciences, Qingdao, China; The University of Chinese Academy of 
      Sciences, Beijing, China; Laboratory for Marine Drugs and Bioproducts, Qingdao 
      National Laboratory for Marine Science and Technology, Qingdao, China.
FAU - Luo, Jiao
AU  - Luo J
AD  - Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese 
      Academy of Sciences, Qingdao, China; The University of Chinese Academy of 
      Sciences, Beijing, China; Laboratory for Marine Drugs and Bioproducts, Qingdao 
      National Laboratory for Marine Science and Technology, Qingdao, China.
FAU - Wu, Ning
AU  - Wu N
AD  - Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese 
      Academy of Sciences, Qingdao, China; Laboratory for Marine Drugs and Bioproducts, 
      Qingdao National Laboratory for Marine Science and Technology, Qingdao, China.
FAU - Zhang, Renshuai
AU  - Zhang R
AD  - Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese 
      Academy of Sciences, Qingdao, China; Laboratory for Marine Drugs and Bioproducts, 
      Qingdao National Laboratory for Marine Science and Technology, Qingdao, China.
FAU - Shi, Dayong
AU  - Shi D
AD  - Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese 
      Academy of Sciences, Qingdao, China; The University of Chinese Academy of 
      Sciences, Beijing, China; Laboratory for Marine Drugs and Bioproducts, Qingdao 
      National Laboratory for Marine Science and Technology, Qingdao, China. Electronic 
      address: shidayong@qdio.ac.cn.
LA  - eng
PT  - Journal Article
DEP - 20170812
PL  - Netherlands
TA  - Int J Biol Macromol
JT  - International journal of biological macromolecules
JID - 7909578
RN  - 0 (Glucose Transporter Type 4)
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (Insulin)
RN  - 0 (Phenols)
RN  - 0 (Slc2a4 protein, mouse)
RN  - 2V16EO95H1 (Palmitic Acid)
RN  - EC 3.1.3.48 (Protein Tyrosine Phosphatase, Non-Receptor Type 1)
RN  - EC 3.1.3.48 (Ptpn1 protein, mouse)
RN  - IY9XDZ35W2 (Glucose)
SB  - IM
MH  - Animals
MH  - Catalytic Domain
MH  - Cell Line, Transformed
MH  - Gene Expression Regulation
MH  - Glucose/metabolism/pharmacology
MH  - Glucose Transporter Type 4/genetics/metabolism
MH  - Hydrogen Bonding
MH  - Hypoglycemic Agents/chemistry/isolation & purification/*pharmacology
MH  - Insulin/agonists/*metabolism
MH  - Insulin Resistance
MH  - Mice
MH  - Molecular Docking Simulation
MH  - Myoblasts/*drug effects/metabolism/pathology
MH  - Palmitic Acid/antagonists & inhibitors/pharmacology
MH  - Phenols/chemistry/isolation & purification/*pharmacology
MH  - Protein Binding
MH  - Protein Conformation, alpha-Helical
MH  - Protein Conformation, beta-Strand
MH  - Protein Interaction Domains and Motifs
MH  - Protein Tyrosine Phosphatase, Non-Receptor Type 1/*antagonists & 
      inhibitors/chemistry/genetics/metabolism
MH  - Rhodophyta/*chemistry
MH  - Signal Transduction/drug effects
OTO - NOTNLM
OT  - BPN
OT  - C2C12 myotubes
OT  - Insulin resistance
OT  - Insulin signaling
OT  - Protein tyrosine phosphatase 1B
EDAT- 2017/08/16 06:00
MHDA- 2018/07/10 06:00
CRDT- 2017/08/17 06:00
PHST- 2017/04/01 00:00 [received]
PHST- 2017/08/03 00:00 [revised]
PHST- 2017/08/04 00:00 [accepted]
PHST- 2017/08/16 06:00 [pubmed]
PHST- 2018/07/10 06:00 [medline]
PHST- 2017/08/17 06:00 [entrez]
AID - S0141-8130(17)31187-X [pii]
AID - 10.1016/j.ijbiomac.2017.08.042 [doi]
PST - ppublish
SO  - Int J Biol Macromol. 2018 Jan;106:379-386. doi: 10.1016/j.ijbiomac.2017.08.042. 
      Epub 2017 Aug 12.