Chongqing Engineering Research Center of Pharmaceutical Sciences, Chongqing Medical and Pharmaceutical College, Chongqing, 401331, PR China; Collaborative Innovation Centre for Brain Science, Chongqing University, Chongqing, 400030, PR China. Electronic address: [Email]
BACKGROUND : Breynia fruticosa is a folk medicine in China, traditionally used to treat gastroenteritis, sore throat, eczema and arthritis. However, the bioactive ingredients are unknown. OBJECTIVE : To identify and isolate the anti-inflammatory ingredients of B. fruticosa. METHODS : B. fruticosa extracts were fractioned by Amberchrom CG161M and Toyopearl HW40C resins. Acetic acid-induced capillary permeability mice model was used to evaluate the anti-inflammation activities of fractions. The anti-inflammatory ingredients were identified by high performance liquid chromatography/mass spectroscopy (HPLC-MS). On-line two dimensional liquid chromatography system was constructed to remove the tannins and enrich the breynins. The breynins were purified by preparative HPLC and evaluated for their anti-arthritis activities using complete Freund's adjuvant (CFA) induced arthritis rats model. RESULTS : The anti-inflammatory ingredients of B. fruticosa are sulfur containing sesquiterpenoids (breynins). The on-line two dimensional preparative liquid chromatography system can effectively remove the tannins and enrich the bioactive ingredients in large scale within 1 h. Four major breynins were purified, and their structures were elucidated by analysis of MS and NMR data. Breynins can significantly prevent the rats' arthritis deterioration, with inhibition ratio 50% at dose 0.2 mg kg-1, comparable with that of indomethacin at dose 2 mg kg-1. CONCLUSIONS : The breynins have strong anti-arthritis activities, which is responsible to the anti-inflammatory effects of B. fruticosa. However, breynins are also toxic components of B. fruticosa.