@article{article_928668, title={Anticancer Profiling of Gambogic Acid as a Target Specific RANKL Inhibitor in Osteosarcoma Cell Line}, journal={Erzincan University Journal of Science and Technology}, volume={14}, pages={442–452}, year={2021}, DOI={10.18185/erzifbed.928668}, author={Özgür, Aykut and Duman, Esra}, keywords={Osteosarcoma, Saos-2, Gambogic acid, RANK, RANKL, OPG}, abstract={Osteosarcoma is a common cancer type among the youth population and usually develops in growing bones. Approximately twenty percent of osteosarcoma cases show tendency to metastases and patients with osteosarcoma have a low survival rate after treatment. RANK/RANKL/OPG key regulator triad of bone remodeling play critical roles in tumourigenesis of osteosarcoma. Anti-proliferative activity of the gambogic acid was determined in Saos-2 cell line by XTT assay. To understand the anticancer activities of the gambogic acid, molecular docking calculations were also performed with RANK-RANKL complex. The expression levels of the RANKL and OPG was measured at gene and protein level with RT-PCR and ELISA assays. Its potential anti-invasive property in-vitro against osteosarcoma cells was evaluated using wound healing assay. Experimental assays indicated that gambogic acid suppressed cell proliferation, cell migration, and decreased protein expression ratio of RANKL/OPG in Saos-2 cells. Gambogic acid binds to RANK-RANKL complex with Kd value of 549.38 nM and with estimated free energy of binding -8.54 kcal/mol. Gambogic acid is found to be significant drug template for target specific osteosarcoma treatment.}, number={2}, publisher={Erzincan Binali Yildirim University}, organization={Tokat Gaziosmanpaşa University}