Devil's club Falcarinol inhibits human glioblastoma cell proliferation and tumor progression in xenografts

Abstract

BackgroundEffective treatment for human glioblastoma is lacking and a novel effective therapeutic agent is urgently needed. It is known that falcarinol-type polyacetylenes (FC-type PAs) are bioactive ingredients in ginseng and other plants from the Araliaceae family. Our earlier study showed that polyacetylene Falcarinol (FC), 1,2-dihydrofalcarinol (FCH) and 3-acetoxyfalcarinol (FCA) are potent proliferation inhibitors of human pancreatic ductal cancer cell lines. MethodsIn this study we evaluated the bioactivities of these synthetic FC-type polyacetylenes (FC-type PAs) on human glioblastoma DBTRG-05MG cell line with cell viability, cell proliferation, cell migration, wound healing and clonogenic assays. We further evaluated synthetic FC on inhibition of DBTRG tumor bearing NOD-Prkdcem26Il2rgem26/Nju (NCG) mice. ResultsFC dose dependently shifted DBTRG-05MG cells toward apoptosis as well as necrosis. FC and FCA, but not FCH, at near IC50 concentration inhibited colony formation in a 3-week clonogenic assay. Twice weekly intra-peritoneal injection of FC at 10 mg/kg significantly reduced tumor growth and tumor size compared to untreated control animals. ConclusionsSynthetic FC inhibits human glioblastoma cancer cell proliferation in vitro and in vivo. The availability of synthetic FC and other FC-type PAs in sufficient quantity and consistent quality would facilitate and expedite further research leading to potential clinical applications.