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CYC31, A Natural Bromophenol PTP1B Inhibitor, Activates Insulin Signaling and Improves Long Chain-Fatty Acid Oxidation in C2C12 Myotubes

by Jiao Luo 1, Yufei Hou 1, Mengyue Xie 1, Wanli Ma 1, Dayong Shi 2,3,* and Bo Jiang 2,4,*
1
School of Public Health, Qingdao University, Qingdao 266071, China
2
Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, 7 Nanhai Road, Qingdao 266071, China
3
State Key Laboratory of Microbial Technology, Shandong University, Jinan 250100, China
4
Center for Ocean Mega-Science, Chinese Academy of Sciences, 7 Nanhai Road, Qingdao 266071, China
*
Authors to whom correspondence should be addressed.
Mar. Drugs 2020, 18(5), 267; https://doi.org/10.3390/md18050267
Received: 22 February 2020 / Revised: 10 April 2020 / Accepted: 22 April 2020 / Published: 19 May 2020
3-bromo-4,5-Bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (CYC31) is a bromophenol protein tyrosine phosphatase 1B (PTP1B) inhibitor isolated from the red alga Rhodomela confervoides. Here, the effect of CYC31 on the insulin signaling and fatty-acid-induced disorders in C2C12 myotubes was investigated. Molecular docking assay showed that CYC31 was embedded into the catalytic pocket of PTP1B. A cellular study found that CYC31 increased the activity of insulin signaling and promoted 2-NBDG uptake through GLUT4 translocation in C2C12 myotubes. Further studies showed that CYC31 ameliorated palmitate-induced insulin resistance in C2C12 myotubes. Moreover, CYC31 treatment significantly increased the mRNA expression of carnitine palmitoyltransferase 1B (CPT-1B) and fatty acid binding protein 3 (FABP3), which was tightly linked with fatty acid oxidation. These findings suggested that CYC31 could prevent palmitate-induce insulin resistance and could improve fatty acid oxidation through PTP1B inhibition. View Full-Text
Keywords: CYC31; PTP1B inhibitor; insulin resistance; fatty acid oxidization; C2C12 CYC31; PTP1B inhibitor; insulin resistance; fatty acid oxidization; C2C12
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MDPI and ACS Style

Luo, J.; Hou, Y.; Xie, M.; Ma, W.; Shi, D.; Jiang, B. CYC31, A Natural Bromophenol PTP1B Inhibitor, Activates Insulin Signaling and Improves Long Chain-Fatty Acid Oxidation in C2C12 Myotubes. Mar. Drugs 2020, 18, 267.

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