BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling Pathway

Diabetic retinopathy (DR) is one of the microvascular complications of diabetes mellitus and a major pathological feature of neovascular DR. These patients potentially experience vision impairment and blindness. Platelet-derived growth factor receptor β (PDGFRβ), fibroblast growth factor receptor 1...

Full description

Saved in:
Bibliographic Details
Main Authors: Xin Cao, Tao Li, Yongshen Tian, Yajing Tian, Chuang Gao, Dongmei Zhang, Yu Song
Format: Article
Language:English
Published: Wiley 2023-01-01
Series:Journal of Ophthalmology
Online Access:http://dx.doi.org/10.1155/2023/7355039
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1849309006856716288
author Xin Cao
Tao Li
Yongshen Tian
Yajing Tian
Chuang Gao
Dongmei Zhang
Yu Song
author_facet Xin Cao
Tao Li
Yongshen Tian
Yajing Tian
Chuang Gao
Dongmei Zhang
Yu Song
author_sort Xin Cao
collection DOAJ
description Diabetic retinopathy (DR) is one of the microvascular complications of diabetes mellitus and a major pathological feature of neovascular DR. These patients potentially experience vision impairment and blindness. Platelet-derived growth factor receptor β (PDGFRβ), fibroblast growth factor receptor 1 (FGFR1), and vascular endothelial growth factor receptor 2 (VEGFR2) are implicated in the DR pathogenesis. Nintedanib (BIBF1120) is an oral selective dual receptor tyrosine kinase (RTK) inhibitor of VEGFR2, FGFR1, and PDGFRβ. In this study, intravitreal injection of BIBF1120 blocked the phosphorylation of VEGFR2, FGFR1, PDGFRβ, and MAPK signaling pathway proteins in a streptozotocin (STZ)-induced diabetic retinopathy mouse model. In in vitro cell experiments, BIBF1120 did not change cellular activity under normal conditions, while it further suppressed the tube formation, migration, and proliferation of high glucose-induced human retinal microvascular endothelial cells (HRMECs). Additionally, BIBF1120 blocked the phosphorylation of p38, JNK, and ERK1/2 in high glucose-treating HRMECs. Our results indicate that the BIBF1120 treatment can be a novel potential drug to protect against DR.
format Article
id doaj-art-05a1122bae7e4dd89ada6e00363ed1a9
institution Kabale University
issn 2090-0058
language English
publishDate 2023-01-01
publisher Wiley
record_format Article
series Journal of Ophthalmology
spelling doaj-art-05a1122bae7e4dd89ada6e00363ed1a92025-08-20T03:54:16ZengWileyJournal of Ophthalmology2090-00582023-01-01202310.1155/2023/7355039BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling PathwayXin Cao0Tao Li1Yongshen Tian2Yajing Tian3Chuang Gao4Dongmei Zhang5Yu Song6Department of OphthalmologyDepartment of OphthalmologyDepartment of OphthalmologyDepartment of OphthalmologyDepartment of OphthalmologyDepartment of OphthalmologyDepartment of OphthalmologyDiabetic retinopathy (DR) is one of the microvascular complications of diabetes mellitus and a major pathological feature of neovascular DR. These patients potentially experience vision impairment and blindness. Platelet-derived growth factor receptor β (PDGFRβ), fibroblast growth factor receptor 1 (FGFR1), and vascular endothelial growth factor receptor 2 (VEGFR2) are implicated in the DR pathogenesis. Nintedanib (BIBF1120) is an oral selective dual receptor tyrosine kinase (RTK) inhibitor of VEGFR2, FGFR1, and PDGFRβ. In this study, intravitreal injection of BIBF1120 blocked the phosphorylation of VEGFR2, FGFR1, PDGFRβ, and MAPK signaling pathway proteins in a streptozotocin (STZ)-induced diabetic retinopathy mouse model. In in vitro cell experiments, BIBF1120 did not change cellular activity under normal conditions, while it further suppressed the tube formation, migration, and proliferation of high glucose-induced human retinal microvascular endothelial cells (HRMECs). Additionally, BIBF1120 blocked the phosphorylation of p38, JNK, and ERK1/2 in high glucose-treating HRMECs. Our results indicate that the BIBF1120 treatment can be a novel potential drug to protect against DR.http://dx.doi.org/10.1155/2023/7355039
spellingShingle Xin Cao
Tao Li
Yongshen Tian
Yajing Tian
Chuang Gao
Dongmei Zhang
Yu Song
BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling Pathway
Journal of Ophthalmology
title BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling Pathway
title_full BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling Pathway
title_fullStr BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling Pathway
title_full_unstemmed BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling Pathway
title_short BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling Pathway
title_sort bibf1120 protects against diabetic retinopathy through neovascularization related molecules and the mapk signaling pathway
url http://dx.doi.org/10.1155/2023/7355039
work_keys_str_mv AT xincao bibf1120protectsagainstdiabeticretinopathythroughneovascularizationrelatedmoleculesandthemapksignalingpathway
AT taoli bibf1120protectsagainstdiabeticretinopathythroughneovascularizationrelatedmoleculesandthemapksignalingpathway
AT yongshentian bibf1120protectsagainstdiabeticretinopathythroughneovascularizationrelatedmoleculesandthemapksignalingpathway
AT yajingtian bibf1120protectsagainstdiabeticretinopathythroughneovascularizationrelatedmoleculesandthemapksignalingpathway
AT chuanggao bibf1120protectsagainstdiabeticretinopathythroughneovascularizationrelatedmoleculesandthemapksignalingpathway
AT dongmeizhang bibf1120protectsagainstdiabeticretinopathythroughneovascularizationrelatedmoleculesandthemapksignalingpathway
AT yusong bibf1120protectsagainstdiabeticretinopathythroughneovascularizationrelatedmoleculesandthemapksignalingpathway