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Article

A Synthetic Cell-Penetrating Heparin-Binding Peptide Derived from BMP4 with Anti-Inflammatory and Chondrogenic Functions for the Treatment of Arthritis

1
School of Biological Sciences, College of Natural Sciences, Chungbuk National University, Cheongju 28644, Korea
2
Central Research Institute, Nano Intelligent Biomedical Engineering Corporation (NIBEC), School of Dentistry, Seoul National University, Seoul 03080, Korea
3
Department of Dental Regenerative Bioengineering and Dental Research Institute, School of Dentistry, Seoul National University, Seoul 03080, Korea
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(12), 4251; https://doi.org/10.3390/ijms21124251
Received: 27 May 2020 / Revised: 11 June 2020 / Accepted: 12 June 2020 / Published: 15 June 2020
(This article belongs to the Special Issue Membrane–Peptide Interactions: From Basics to Current Applications)
We report dual therapeutic effects of a synthetic heparin-binding peptide (HBP) corresponding to residues 15–24 of the heparin binding site in BMP4 in a collagen-induced rheumatic arthritis model (CIA) for the first time. The cell penetrating capacity of HBP led to improved cartilage recovery and anti-inflammatory effects via down-regulation of the iNOS-IFNγ-IL6 signaling pathway in inflamed RAW264.7 cells. Both arthritis and paw swelling scores were significantly improved following HBP injection into CIA model mice. Anti-rheumatic effects were accelerated upon combined treatment with Enbrel® and HBP. Serum IFNγ and IL6 concentrations were markedly reduced following intraperitoneal HBP injection in CIA mice. The anti-rheumatic effects of HBP in mice were similar to those of Enbrel®. Furthermore, the combination of Enbrel® and HBP induced similar anti-rheumatic and anti-inflammatory effects as Enbrel®. We further investigated the effect of HBP on damaged chondrocytes in CIA mice. Regenerative capacity of HBP was confirmed based on increased expression of chondrocyte biomarker genes, including aggrecan, collagen type II and TNFα, in adult human knee chondrocytes. These findings collectively support the utility of our cell-permeable bifunctional HBP with anti-inflammatory and chondrogenic properties as a potential source of therapeutic agents for degenerative inflammatory diseases. View Full-Text
Keywords: anti-inflammatory peptide; cell permeable peptide; heparin-binding peptide; collagen-induced arthritis; inducible nitric oxide; interferon gamma; interleukin-6; Enbrel anti-inflammatory peptide; cell permeable peptide; heparin-binding peptide; collagen-induced arthritis; inducible nitric oxide; interferon gamma; interleukin-6; Enbrel
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MDPI and ACS Style

Choi, D.H.; Lee, D.; Jo, B.S.; Park, K.-S.; Lee, K.E.; Choi, J.K.; Park, Y.J.; Lee, J.-Y.; Park, Y.S. A Synthetic Cell-Penetrating Heparin-Binding Peptide Derived from BMP4 with Anti-Inflammatory and Chondrogenic Functions for the Treatment of Arthritis. Int. J. Mol. Sci. 2020, 21, 4251. https://doi.org/10.3390/ijms21124251

AMA Style

Choi DH, Lee D, Jo BS, Park K-S, Lee KE, Choi JK, Park YJ, Lee J-Y, Park YS. A Synthetic Cell-Penetrating Heparin-Binding Peptide Derived from BMP4 with Anti-Inflammatory and Chondrogenic Functions for the Treatment of Arthritis. International Journal of Molecular Sciences. 2020; 21(12):4251. https://doi.org/10.3390/ijms21124251

Chicago/Turabian Style

Choi, Da Hyeon, Dongwoo Lee, Beom Soo Jo, Kwang-Sook Park, Kyeong Eun Lee, Ju Kwang Choi, Yoon Jeong Park, Jue-Yeon Lee, and Yoon Shin Park. 2020. "A Synthetic Cell-Penetrating Heparin-Binding Peptide Derived from BMP4 with Anti-Inflammatory and Chondrogenic Functions for the Treatment of Arthritis" International Journal of Molecular Sciences 21, no. 12: 4251. https://doi.org/10.3390/ijms21124251

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