目的 对松节藻中得到的10种化合物进行体外细胞毒活性筛选,并对其醇提取物进行体内抑瘤活性研究。方法 采用碘酰罗丹明B(SRB)蛋白染色法和MTT法对10种化合物进行细胞毒活性筛选;用S₁₈₀荷瘤小鼠模型进行松节藻醇提取物的体内抗肿瘤活性评价,分别测定半数致死量(LD₅₀)、抑瘤率、胸腺指数、脾指数、脾淋巴细胞增殖活性(MTT法)、免疫球蛋白IgA、IgG、IgM和脾淋巴细胞凋亡率等指标,应用软件SPSS进行数据处理。结果 体外活性筛选实验表明4,4′-亚甲基-二(5,6-二溴-1,2-二苯酚)(Ⅰ)、3-溴-4-[2,3-二溴-4,5-二羟基苯基]甲基-5-(甲氧基甲基)-1,2-二苯酚(Ⅱ)、3-溴-4,5-二(2,3-二溴-4,5-二羟基苯甲基)-1,2-二苯酚(Ⅲ)、二(2,3-二溴-4,5-二羟基苯甲基)醚(Ⅳ)和3-溴-4-[2,3-二溴-4,5-二羟基苯基]甲基-5-(乙氧基)-1,2-二苯酚(Ⅴ)5种单体化合物对人肺癌细胞株A-549具有-定的细胞毒活性。松节藻醇提取物中剂量(1g/kg)组表现出较高的抑瘤率,但中剂量组胸腺指数及脾指数均有所升高;松节藻醇提取物各组均可较好抑制脾淋巴细胞增殖;各组免疫球蛋白IgA和IgG无明显变化,而松节藻醇提取物中剂量组IgM含量有明显升高;中、高剂量组脾淋巴细胞凋亡率显著升高。结论 从松节藻中提取的部分化合物表现出-定的细胞毒活性;其醇提取物对肿瘤细胞有-定的抑制作用,并可增强机体免疫功能。

Objective To screen the in vitro cytotoxicity of ten compounds from Rhodomela confervoides and investigate the antitumor activities of ethan01 extract from R.confervoides(EERC)on S₁₈₀ mice.Methods Cytotoxicity of ten compounds was obtained by SRB and MTT assays.S₁₈₀ mice were used to evaluate the antitumor activities in vivo of EERC(Cytoxan as positive drug).LD₅₀,tumor inhibition rate,indices of thymus and spleen,multiplication of spleen lymphocyte(MTT assay),IgA,IgG,IgM,and apoptosis rate of spleen lymphocyte were detected,respectively.The data were analyzed by software SPSS.Results Five compounds as 4,47-methylene-bis[5,6-dibromo-1,2-benzenedi01](I),3-bromo-4-[2,3-dibromo-4,5-dihydroxybenzyl]methyl-5-(methoxymethyl)-1,2-benzenediol(Ⅱ),3-bro-mo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol(Ⅲ),bis(2,3-dibromo-4,5-dihy-droxybenzyl)ether(Ⅳ),and 3-bromo-4-[2,3-dibromo-4,5-dihydroxyphenyl]methyl-5-(ethoxymethyl)1,2-benzenedi01(V)showed cytotoxicity to human lung cancer celllines A-549.Tumor inhibitory rate of EERC in middle-dose group(1 g/kg)was significantly higher than that in the other groups,while the indices of thymus and spleen were increased obviously.Groups of EERC showed inhibition on multiDlication of spleen lymphocyte.Concentration of IgA and IgG maintained a stable level in all groups.IgM was increased significantly in middle-dose group of EERC.Apoptosis rate of spleen lymphocyte was increased in middle-and high-dose groups.Conclusion Some compounds from R.confervoides showed certain cyto-toxicity.The EERC has obvious antitumc r effect on S₁₈₀ mice and can enhance the immune function of organism.

国家863项目(2004AA625030,2001AA620503);中国科学院方向性创新项目(KZCX3-SW-215)