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April 26, 2026Theranostics0 citationsOpen Access

Multi-functional Small Molecule for Regenerative Healing of Avascular Meniscus Tears: Modulation of Inflammation, Differentiation, and Multi-Tissue Crosstalk

MFMeng FengDPD D PelleiMWMing Wang

Key Points

  • This research aims to evaluate the efficacy of 4-PPBP in promoting the healing of avascular meniscus tears through modulation of inflammation and differentiation.
  • In vitro analysis of 4-PPBP's effects on proliferation, migration, and differentiation of meniscus cells and synovial mesenchymal stem cells.
  • Ex vivo and in vivo assessments of healing efficacy using 4-PPBP-loaded bioglue.
  • Single injection evaluation of outcomes related to meniscal gapping and gait performance.
  • 4-PPBP significantly enhanced meniscus healing in ex vivo settings and minimized meniscal gapping in vivo.
  • Gait performance was improved in the treatment group compared to controls, with enhanced fibrocartilaginous tissue integration.
  • Pro-inflammatory gene expression in macrophages was reduced, while differentiation and matrix synthesis genes were elevated in fibroblasts and chondrocytes.

Abstract

Avascular meniscus tears are a major contributor to mechanical joint locking, compromised gait and function, and the initiation and progression of post-traumatic osteoarthritis.Unfortunately, the avascular meniscus tears hardly heal.Here, we report a novel small molecule, 4-PPBP, a sigma-1 receptor (1R) agonist, exhibiting significant potential to promote avascular meniscus healing by activating synovial mesenchymal stem cells (syMSCs) and modulating macrophage-regulated inflammation via multi-tissue crosstalk.In vitro, 4-PPBP promoted the proliferation and migration of meniscus cells and syMSCs, exhibited anti-inflammatory effects, and induced fibrochondrogenic differentiation.4-PPBP significantly promoted the healing of avascular meniscus tears ex vivo.In vivo, a single injection of 4-PPBP-loaded bioglue minimized meniscal gapping, with improved meniscus healing and gait performance.In contrast to the degenerative changes in the untreated control, 4-PPBP/bioglue application resulted in integrated fibrocartilaginous tissues.scRNA-seq and CellChat analyses revealed 4-PPBP-activated cell-cell communications leading to inflammatory regulation and cell differentiation.Macrophages showed a robust reduction in pro-inflammatory genes, and fibroblasts, chondrocytes, and fibrochondrocytes increased genes associated with differentiation and matrix synthesis in response to 4-PPBP.Anti-inflammatory cell-cell communication signals were significantly elevated between adipocytes and macrophages.Together, this study demonstrates the notable potential of 4-PPBP as a multi-functional therapeutic for avascular meniscus tears.

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Cite This Study

Feng et al. (2026) studied this question.

synapsesocial.com/papers/69edab424a46254e215b3603https://doi.org/10.7150/thno.132326
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