TY  - JOUR
TI  - Anticancer Profiling of Gambogic Acid as a Target Specific RANKL Inhibitor in Osteosarcoma Cell Line
AB  - 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.
AU  - DUMAN, ESRA
AU  - Ozgur, Aykut
DO  - 10.18185/erzifbed.928668
PY  - 2021
JO  - Erzincan Üniversitesi Fen Bilimleri Enstitüsü Dergisi
VL  - 14
IS  - 2
SN  - 1307-9085
SP  - 442
EP  - 452
DB  - TRDizin
UR  - http://search/yayin/detay/479544
ER  -