Therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approach

Abstract Articular cartilage has a limited regenerative capacity, resulting in poor spontaneous healing of damaged tissue. Despite various scientific efforts to enhance cartilage repair, no single method has yielded satisfactory results. With rising drug development costs, drug repositioning has eme...

Full description

Saved in:
Bibliographic Details
Main Authors: Jun-Ku Lee, Hyunjeong Yeo, Sujin Choi, Kyeong Mi Kim, Hannah Kim, Sung-Sahn Lee, Hyun Il Lee, Younghoon Jeong, Hyun-Ju An, Soonchul Lee
Format: Article
Language:English
Published: Nature Portfolio 2024-12-01
Series:Scientific Reports
Online Access:https://doi.org/10.1038/s41598-024-82177-1
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850102904105467904
author Jun-Ku Lee
Hyunjeong Yeo
Sujin Choi
Kyeong Mi Kim
Hannah Kim
Sung-Sahn Lee
Hyun Il Lee
Younghoon Jeong
Hyun-Ju An
Soonchul Lee
author_facet Jun-Ku Lee
Hyunjeong Yeo
Sujin Choi
Kyeong Mi Kim
Hannah Kim
Sung-Sahn Lee
Hyun Il Lee
Younghoon Jeong
Hyun-Ju An
Soonchul Lee
author_sort Jun-Ku Lee
collection DOAJ
description Abstract Articular cartilage has a limited regenerative capacity, resulting in poor spontaneous healing of damaged tissue. Despite various scientific efforts to enhance cartilage repair, no single method has yielded satisfactory results. With rising drug development costs, drug repositioning has emerged as a viable alternative. This study aimed to identify a drug capable of improving cartilage defects by analyzing chondrogenesis-related microarray data from the Gene Expression Omnibus (GEO) public database. We utilized datasets GSE69110, GSE107649, GSE111822, and GSE116173 to identify genes associated with cartilage differentiation, employing StringTie for differential gene expression analysis and extracting drug data from the Drug-Gene Interaction database. Additionally, we aimed to verify the cartilage regeneration potential of the identified drug through experiments using cellular and animal models. We evaluated the effects of aripiprazole on adipose-derived mesenchymal stem cells (ADMSCs) and chondrocytes using qRT-PCR and a 3D pellet culture system. In vivo, we assessed cartilage restoration by combining aripiprazole with a scaffold and implanting it into artificially induced cartilage defects in Sprague-Dawley rats. Subsequent mRNA sequencing provided insights into the mechanistic pathways involved. Our results showed that aripiprazole significantly increased mRNA expression of COL2A1 and SOX9, markers of chondrogenesis, and promoted chondrogenic condensation in vitro. Furthermore, aripiprazole effectively enhanced cartilage regeneration in the rat model. KEGG pathway and Gene Ontology Biological Processes (GOBP) analyses of the mRNA sequencing data revealed that aripiprazole upregulated genes related to ribosomes and cytoplasmic translation, thereby facilitating chondrogenesis. In conclusion, our findings suggest that aripiprazole is a promising candidate for improving damaged cartilage, offering a novel approach to cartilage regeneration.
format Article
id doaj-art-16d570f293cd4308b7d11dfd288273e3
institution DOAJ
issn 2045-2322
language English
publishDate 2024-12-01
publisher Nature Portfolio
record_format Article
series Scientific Reports
spelling doaj-art-16d570f293cd4308b7d11dfd288273e32025-08-20T02:39:40ZengNature PortfolioScientific Reports2045-23222024-12-0114111110.1038/s41598-024-82177-1Therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approachJun-Ku Lee0Hyunjeong Yeo1Sujin Choi2Kyeong Mi Kim3Hannah Kim4Sung-Sahn Lee5Hyun Il Lee6Younghoon Jeong7Hyun-Ju An8Soonchul Lee9Department of Orthopedic Surgery, National Health Insurance Service Ilsan HospitalDepartment of Orthopaedic Surgery, CHA Bundang Medical Center, CHA University School of MedicineDepartment of Orthopaedic Surgery, CHA Bundang Medical Center, CHA University School of MedicineDepartment of Laboratory Medicine, CHA Ilsan Medical Center, CHA University School of MedicineDepartment of Orthopaedic Surgery, CHA Bundang Medical Center, CHA University School of MedicineDepartment of Orthopedic Surgery, Ilsan Paik Hospital, Inje UniversityDepartment of Orthopedic Surgery, Ilsan Paik Hospital, Inje UniversityDepartment of Orthopaedic Surgery, CHA Bundang Medical Center, CHA University School of MedicineDepartment of Orthopaedic Surgery, CHA Bundang Medical Center, CHA University School of MedicineDepartment of Orthopaedic Surgery, CHA Bundang Medical Center, CHA University School of MedicineAbstract Articular cartilage has a limited regenerative capacity, resulting in poor spontaneous healing of damaged tissue. Despite various scientific efforts to enhance cartilage repair, no single method has yielded satisfactory results. With rising drug development costs, drug repositioning has emerged as a viable alternative. This study aimed to identify a drug capable of improving cartilage defects by analyzing chondrogenesis-related microarray data from the Gene Expression Omnibus (GEO) public database. We utilized datasets GSE69110, GSE107649, GSE111822, and GSE116173 to identify genes associated with cartilage differentiation, employing StringTie for differential gene expression analysis and extracting drug data from the Drug-Gene Interaction database. Additionally, we aimed to verify the cartilage regeneration potential of the identified drug through experiments using cellular and animal models. We evaluated the effects of aripiprazole on adipose-derived mesenchymal stem cells (ADMSCs) and chondrocytes using qRT-PCR and a 3D pellet culture system. In vivo, we assessed cartilage restoration by combining aripiprazole with a scaffold and implanting it into artificially induced cartilage defects in Sprague-Dawley rats. Subsequent mRNA sequencing provided insights into the mechanistic pathways involved. Our results showed that aripiprazole significantly increased mRNA expression of COL2A1 and SOX9, markers of chondrogenesis, and promoted chondrogenic condensation in vitro. Furthermore, aripiprazole effectively enhanced cartilage regeneration in the rat model. KEGG pathway and Gene Ontology Biological Processes (GOBP) analyses of the mRNA sequencing data revealed that aripiprazole upregulated genes related to ribosomes and cytoplasmic translation, thereby facilitating chondrogenesis. In conclusion, our findings suggest that aripiprazole is a promising candidate for improving damaged cartilage, offering a novel approach to cartilage regeneration.https://doi.org/10.1038/s41598-024-82177-1
spellingShingle Jun-Ku Lee
Hyunjeong Yeo
Sujin Choi
Kyeong Mi Kim
Hannah Kim
Sung-Sahn Lee
Hyun Il Lee
Younghoon Jeong
Hyun-Ju An
Soonchul Lee
Therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approach
Scientific Reports
title Therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approach
title_full Therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approach
title_fullStr Therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approach
title_full_unstemmed Therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approach
title_short Therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approach
title_sort therapeutic role of aripiprazole in cartilage defects explored through a drug repurposing approach
url https://doi.org/10.1038/s41598-024-82177-1
work_keys_str_mv AT junkulee therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT hyunjeongyeo therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT sujinchoi therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT kyeongmikim therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT hannahkim therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT sungsahnlee therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT hyunillee therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT younghoonjeong therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT hyunjuan therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach
AT soonchullee therapeuticroleofaripiprazoleincartilagedefectsexploredthroughadrugrepurposingapproach