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Published on: May 3, 2021
Experimental Study on the Inhibitory Effect of Eupatilin on Osteosarcoma by the NBR2/miR-129-5p/FKBP11 Regulatory
Xinzhe Zhang1, Jihui Zhou2, Jingtao Wu3
1Maoming People's Hospital, Southern Medical University, Guangzhou, Guangdong, China.
Background:
Osteosarcoma is a malignant bone tumor primarily composed of interstitial cells; there is an urgent need to develop effective treatments to improve patient prognosis. Traditional Chinese medicine offers a promising direction for research. This study explores the inhibitory effects and mechanisms of eupatilin on osteosarcoma, as well as the feasibility of using exosomes loaded with eupatilin in the treatment of osteosarcoma.
Methods:
The cell counting kit-8 (CCK-8) assay was utilized to determine the optimal experimental concentration of eupatilin and assess its effect on cell proliferation. Cell apoptosis, migration, and invasion were evaluated through flow cytometry, wound healing assay, transwell assay, and colony formation assay. The expression of neighbor of BRCA1 gene 2 (NBR2), microRNA-129-5p (miR-129-5p), and FKBP prolyl isomerase 11 (FKBP11) were assessed using real-time quantitative polymerase chain reaction and Western blot. Extracellular exosomes from bone marrow mesenchymal stem cells were extracted via ultracentrifugation. Exosomes overexpressing miR-129-5p were obtained by transfecting the stem cells, and exosomes loaded with eupatilin were prepared through co-incubation. The inhibitory effects of different exosome treatments were observed.
Results:
Cytological experiments demonstrated that eupatilin significantly enhances the apoptosis rate of osteosarcoma cells, suppresses cell viability, and markedly diminishes the capacities for colony formation, migration, and invasion. PCR and WB analyses revealed that the expression levels of NBR2, FKBP11 gene, and protein were notably reduced, whereas the expression level of miR-129-5p was significantly elevated. Exosome-based therapy exhibited a pronounced inhibitory effect on osteosarcoma cells.
Conclusion:
Eupatilin exerts a reliable inhibitory effect on osteosarcoma cells through the NBR2/miR-129-5p/FKBP11 regulatory axis. Exosomes can effectively carry both eupatilin and miR-129-5p, enhancing their therapeutic efficacy.
Insights
Eupatilin shows promise in treating osteosarcoma by inducing cell death and reducing tumor growth. Exosomes loaded with eupatilin and miR-129-5p enhance its therapeutic effect against bone cancer.
Area of Science:
- Oncology
- Biotechnology
- Pharmacology
Background:
- Osteosarcoma is a challenging bone cancer requiring novel treatments.
- Traditional Chinese medicine offers potential therapeutic avenues.
- Eupatilin's efficacy and exosome-based delivery for osteosarcoma warrant investigation.
Purpose of the Study:
- To explore the inhibitory effects of eupatilin on osteosarcoma cells.
- To elucidate the underlying molecular mechanisms of eupatilin's action.
- To assess the therapeutic potential of exosomes loaded with eupatilin for osteosarcoma treatment.
Main Methods:
- Cell counting kit-8 (CCK-8) assay for proliferation and optimal concentration.
- Flow cytometry, wound healing, transwell, and colony formation assays for apoptosis, migration, and invasion.
- Real-time PCR and Western blot to analyze NBR2, miR-129-5p, and FKBP11 expression; exosome extraction and loading via ultracentrifugation and co-incubation.
Main Results:
- Eupatilin significantly increased osteosarcoma cell apoptosis and suppressed viability, colony formation, migration, and invasion.
- NBR2 and FKBP11 expression decreased, while miR-129-5p expression increased following eupatilin treatment.
- Exosome-based delivery of eupatilin and miR-129-5p demonstrated significant inhibition of osteosarcoma cells.
Conclusions:
- Eupatilin effectively inhibits osteosarcoma via the NBR2/miR-129-5p/FKBP11 pathway.
- Exosomes serve as an effective delivery vehicle for eupatilin and miR-129-5p, enhancing therapeutic outcomes.
- This study highlights a novel therapeutic strategy for osteosarcoma leveraging natural compounds and advanced drug delivery systems.

