ABSTRACT
Hispolon (HISP) is a bioactive compound isolated from Phellinu linteus. It has various pharmacological activities, including antioxidant, anti-inflammatory, and anti-cancer. However, its anti-osteoclastogenic activity has not yet been reported. Hence, in the current study, we have explored the anti-osteoclastogenic activity of HISP and elucidated the molecular mechanisms. HISP inhibited the RANKL induced differentiation of RAW 264.7 cells into osteoclasts in a dose-dependent manner. Mechanistic studies showed that HISP inhibited RANKL-mediated activation of NF-κB and MAPK signaling pathways in osteoclast precursors RAW 264.7 cells. In addition, Hispolon also downregulated the expression of master transcriptional factors essential for osteoclast differentiation, such as NFATc1 and c-FOS. In conclusion, these findings establish molecular mechanisms behind the anti-osteoclastogenic activity of HISP.
Subject(s)
Catechols/pharmacology , Cell Differentiation/drug effects , Osteoclasts/cytology , Osteoclasts/drug effects , Osteoclasts/metabolism , RANK Ligand/metabolism , Actins/metabolism , Animals , Biomarkers , Catechols/chemistry , Cell Survival/drug effects , Cells, Cultured , Fluorescent Antibody Technique , MAP Kinase Signaling System , Mice , Osteogenesis , RAW 264.7 Cells , Reactive Oxygen Species/metabolismABSTRACT
AIM@#Sargassum wightii Greville is a marine brown alga belonging to the Sargassaceae family which has about 200 species. The ethanolic extract of the whole dry plant powder contained numerous phytoconstituents, including flavonoids. The study was focused on the anticancer activity of Sargassum wightii in mice.@*METHOD@#The ethanolic extract of Sargassum wightii (EESW) at two dose levels was used to examine the anticancer activity in mice using DAL cell lines to induce cancer. The body weight, viable and non-viable tumor cell count, mean survival time, increase in life span, and hematological parameters were observed for anticancer activity of EESW.@*RESULTS@#The intraperitoneal inoculation of DAL cells in mice significantly increased cancer cell count. The decrease in the cancer cell number observed in the EESW-treated group cancer animals indicates that the test drug has a significant inhibitory effect on the tumor cell proliferation. Treatment with EESW also showed a significant decrease in tumor weight, and hence increased the lifespan of DAL-treated mice. In addition, EESW administration significantly restored the hematological parameters in DAL-treated mice.@*CONCLUSION@#The present study results suggest that administration of extract offers enhanced antioxidant potential. Therefore it can be concluded from this study that EESW possesses anticancer activity.
