关键词: 何首乌, 虎杖, 大黄, 游离蒽醌, 肝细胞毒性, 细胞凋亡

Abstract: OBJECTIVE: To investigate correlations between toxicity in HepaRG cells and free anthraquinone contents in aqueous extracts from Polygoni Multiflori Radix (PMR),Polygoni Cuspidati Rhizoma et Radix (PCRER) and Rhei Radix et Rhizoma (RRER). METHODS: High performance liquid chromatography was used to detect the content of emodin,physcion,aloe emodin,rhein and chrysophanol from the three aqueous extracts. MTT assay was employed to measure HepaRG cell viability following treatment with theextracts in different concentrations (1.0,1.5,2.0,2.5,3.0 mg/mL) for 48 h. HepaRG cells were also treated in concentrations of 1.5,2.0,2.5 mg/mL for the detection of apoptosis by AnnexinⅤ/PI dual staining for FCM. RESULTS: The contents of free anthraquinoneins in the three extracts were 0.229%,0.545%,2.593% respectively. The survival rate of HepaRG cells was down-regulated by PMR (2.0,2.5,3.0 mg/mL),PCRER (1.5,2.0,2.5,3.0 mg/mL) and RRER (1.0,1.5,2.0,2.5,3.0 mg/mL) in dose-dependent manners. The degree of inhibition was positively correlated with the content of free anthraquinones. The same trend was observed in apoptosis cell proportion in which the concentrations of extracts were 1.5,2.0,2.5 mg/mL. CONCLUSION: The contents of free anthraquinones in the three aqueous extracts from low to high degree were PMR,PCRER and RRER. The content was positively correlated with cytotoxicity in vitro,which suggests that free anthraquinones might be the important component inducing toxicity in these three traditional Chinese medicines.

Key words: Polygoni Multiflori Radix, Polygoni Cuspidati Rhizoma et Radix, Rhei Radix et Rhizoma, free anthraquinones, hepatotoxicity, apoptosis