霍山石斛抗炎及肿瘤细胞毒活性研究

Anti-inflammatory and Cytotoxic Activity of Dendrobium Huoshanense C.Z.Tang et S.J.Cheng

目的研究霍山石斛提取物及单体化合物的抗炎及肿瘤细胞毒活性。方法利用脂多糖(LPS)诱导小鼠单核巨噬细胞(RAW 264.7)炎症反应模型,检测细胞内ROS水平和NO生成量,评价霍山石斛各组分以及单体化合物的抗炎活性;采用MTS法筛选石斛各组分以及单体化合物对HL-60、A-549、SMMC-7721、MCF-7和SW-480的体外细胞毒活性。结果霍山石斛乙醇提取物及其不同极性部位对降低细胞内ROS水平的作用能力顺序为:正丁醇部位>乙酸乙酯部位>水部位>乙醇提取物>石油醚部位;乙酸乙酯部位对NO生成的抑制作用较强,抑制率为26.39%,其它各部位对NO生成的抑制作用较弱。乙醇提取物和石油醚部位均对除HL-60细胞外的其他细胞具有一定的抑制细胞增殖的作用。从乙醇提取物中获得11个化合物,其中,化合物3,4-二羟基-5-甲氧基苯甲醛(3)和4,4'-二羟基-3,5-二甲氧基联苄(6)对NO生成抑制率分别为21.88%和23.32%,化合物6对HL-60、SMMC-7721和MCF-7细胞的IC50值分别为27.79μmol/L、6.66μmol/L和25.01μmol/L。结论霍山石斛能减少ROS产生、抑制NO生成和肿瘤细胞毒活性,化合物3和6具有较好抗炎和抗肿瘤活性。

Objective To evaluate the anti-inflammatory and cytotoxic activities of extracts and monomeric compounds from the aerial of stems of Dendrobium huoshanense.Methods The anti-inflammatory was determined by the level of intracellular ROS and NO production using a lipopolysaccharide(LPS)-induced RAW 264.7 cells;and the cytotoxic activities were screened for HL-60,A-549,SMMC-7721,MCF-7 and SW-480 cell lines by MTS.Results The ethanolic extract of D.huoshanense and its different polar parts could decrease the level of intracellular ROS in the order of n-butanol fraction,ethyl acetate fraction,water fraction,ethanol extract and petroleum ether fraction.The ethyl acetate fraction inhibited NO production by 26.39%,which was superior to other fractions.The ethanol extract and petroleum ether fraction exhibited cytotoxic activities on A-549,SMMC-7721,MCF-7 and SW-480 cell lines.11 compounds isolated and identified from the ethanolic extracts.Among them,3 and 6 showed antiinflammatory activities with NO production inhibition rates of 21.88%and 23.32%,respectively.The IC50 values of 6 against HL-60,SMMC-7721 and MCF-7 cells were 27.79μmol/L,6.66μmol/L and 25.01μmol/L,respectively.Conclusion D.huoshanense has biological activities of reducing the level of ROS,inhibiting NO production and cytotoxic activity.3 and 6 demonstrated anti-inflammatory and anti-tumor activities.