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目的研究黑乳海参中化合物nobiliside B及单乙酰化衍生物体外抗肿瘤活性及溶血作用。方法no-biliside B溶于吡啶,冰浴中与醋酐反应15 min,室温反应5h,应用多种色谱技术对反应产物分离纯化,根据化合物的理化性质和波谱数据鉴定其结构。采用磺酰罗单明B法,测定化合物的体外抗肿瘤活性。结果确定nobiliside B单乙酰化衍生物结构为:3-O-[6″-乙酰氧基-β-D-吡喃葡萄糖-(1(3)-4′-O-磺酸钠-β-D-吡喃木糖]-海参烷-9-烯22,25-环氧-3β,17α-二醇(2);活性测试结果表明,化合物2在保持抗肿瘤活性的同时,溶血活性显著降低。结论通过结构修饰,得到1个活性强,毒副作用小的新化合物。为进一步研发海参皂苷类化合物抗肿瘤新药提供了试验依据。
Objective To study the antitumor activity and hemolysis of compound nobiliside B and monoacetylated derivatives in black milk sea cucumber. Method No-biliside B was dissolved in pyridine, reacted with acetic anhydride for 15 min in ice bath, and reacted at room temperature for 5 h. The products were separated and purified by a variety of chromatographic techniques. Their structures were identified by physicochemical properties and spectral data. The sulfonylurea B method was used to determine the in vitro antitumor activity of the compounds. As a result, it was confirmed that the structure of nobiliside B monoacetylated derivative was 3-O- [6 "-acetoxy-β-D-glucopyranosyl- (1 - xylopyranose] -HP-22,25-epoxy-3β, 17α-diol (2). The results of the activity test showed that compound 2 showed a significant decrease in hemolytic activity while maintaining antitumor activity. Conclusion A new compound with strong activity and little side effect was obtained through structural modification, which provided the experimental basis for further research on antitumor drugs of sea cucumber saponins.