【作者】 王啸洋； 汤海峰； 程光；

【Author】 WANG Xiao-yang1,TANG Hai-feng1,CHENG Guang2(1.Department of Pharmacy,Xijing Hospital,Fourth Military Medical University,Xi’an 710032;2.Department of Neurosurgery,Xijing Hospital,Fourth Military Medical University,Xi’an 710032)

【机构】 第四军医大学西京医院药剂科； 第四军医大学西京医院脑科医院；

【摘要】 目的研究陕西特有药用植物太白银莲花中具有抗肿瘤活性的三萜皂苷成分。方法应用多种色谱手段和波谱方法分离和鉴定化合物。采用MTT法测定肿瘤细胞毒性。结果分离鉴定了30个化合物(1～30),包括10个新化合物(12,14,18,19,24,26～30)和1个新天然产物(8),其中27个为三萜皂苷类化合物;所有化合物均为首次从本种得到。皂苷6,7,10,11,12,14对HL-60,Hep-G2和U251MG等肿瘤细胞显示显著细胞毒性。结论 4个新皂苷(18,19,26,27)含有天然届少见的siaresinolic acid苷元,该苷元在银莲花属植物中首次发现。构效关系分析表明:齐墩果烷型三萜皂苷的苷元C-3位成氧苷同时C-28为游离羧基是其肿瘤细胞毒活性较强的必须条件,而C-23位羟基的存在致使活性下降;C-3位糖链含Rha(1→2)Ara-片段的皂苷活性最强。本研究填补了对太白银莲花化学成分的研究空白,为开发这一陕西特有药用资源提供了科学依据,部分成分显著的肿瘤细胞毒性为进一步开发抗肿瘤新药提供了有价值的先导化合物。更多还原

【Abstract】 OBJECTIVE To study the anti-tumor triterpenoid saponins from the medicinal plant Anemone taipaiensis distributed locally in Shaanxi Province.METHODS A combination of multi-chromatography as well as spectral analysis were employed for the separation and determination of the compounds from the plant.The cytotoxicities against human tumor cells were determined using the MTT assays.RESULTS Thirty compounds(1-30),including twenty-seven triterpenoid saponins were obtained and elucidated from the plant for the first time,among which ten are new compounds(12,14,18,19,24,26-30) and one is new natural product(8).Six saponins(6,7,10,11,12,14) showed in vitro cytotoxicity against HL-60,Hep-G2 and U251MG cells.CONCLUSION Four new saponins(18,19,26,27) possessed siaresinolic acid as aglycone,which was found in genus Anemone for the first time.The characteristic structural features of potent cytotoxic saponins were to have α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl group at C-3 and a free carboxylic acid at C-28 of the oleanane skeleton,and the hydroxyl group at C-23 had a negative effect on the cytotoxic activity.Our studies focused on cytotoxic saponins of A.taipaiensis have provided valuable leads for pursuing new anti-tumor drugs,and established a homebase for further development of the title plant distributed locally in Shaanxi Province.更多还原