Sung Hyun Kim¹, Dong Seok Lee^{1, 2,}

Cynaroside (luteolin-7-O-glucoside) is a flavone glycoside compound that has been reported to possess strong anti-oxidant activities. However, the integrative study for anti-inflammatory and anti-cancer activities of cynaroside alone or together with some flavonoids from medicinal herbs is rare. This study demonstrated anti-oxidant, anti-inflammatory, and anti-pancreatic cancer activities of cynaroside and n-butanol fraction derived from Orostachys japonicus (OJB). HPLC analysis indicated that OJB contained three different types of flavonoid glycosides; the major component among them was cynaroside. The anti-oxidant activities of cynaroside and OJB were validated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays and confirmed through analyzing the expression levels of heme oxygenase-1 (HO-1). The anti-inflammatory effects of them were certified by observing the decrease of lipopolysaccharide (LPS)-stimulated nitric oxide (NO) in RAW 264.7 cells. Additionally, the anti-proliferative activities of them were confirmed by 3-[4,5-dimethylthiazol-2-yl]-5-[3-carboxymethoxyphenyl]-2-[4-sulfophenyl]-2H-tetrazolium (MTS) assays in PANC-1 cells. Apoptotic bodies induced by them were clearly proven by DAPI staining. The cell cycle arrest at G1/S phase provoked by OJB was affirmed using flow cytometry. The effective activation of caspase -9, -8, -3 and inhibition of CDK2 and CDK4 by OJB were verified analyzing the protein levels measured using western blot. Such results indicated that both cynaroside and OJB effectively exerted anti-cancer effects on PANC-1 cells. In conclusion, the OJB containing cynaroside as a major flavonoid compound has the potential to be utilized as effectual anti-oxidant, anti-inflammatory, and anti-cancer agents in the future.

Orostachys japonicus, cynaroside, anti-oxidant, anti-inflammatory, anti-cancer