升麻中环阿尔廷烷型三萜皂苷及其抗肿瘤活性研究

从我国中草药的潜在区域特异性出发,对目前很少涉及的西北地区甘肃产升麻进行了较系统的化学成分及其生物活性研究。通过正、反相硅胶等色谱技术从升麻根茎的乙酸乙酯萃取物中分离得到15个环阿尔廷烷型三萜皂苷;根据单体化合物的波谱学数据、理化性质将其分别鉴定为25-脱水升麻醇-3-O-β-D-吡喃木糖苷(1),25-O-乙酰基-升麻醇-3-O-β-D-吡喃木糖苷(2),25-O-乙酰基-7,8-去氢升麻醇-3-O-β-D-吡喃木糖苷(3),25-O-乙酰基-升麻醇-3-O-α-L-吡喃阿拉伯糖苷(4{ST),asiaticoside A(5),asiaticoside B(6),isocimipodocarpaside(7),cimicidanol(8),26-Deoxyactein(9),升麻醇-3-O-β-D-吡喃木糖苷(10),24-O-acetylisodahurinol-3-O-β-D-xylopyranoside(11),23-O-acetylshengmanol-3-O-β-D-xylopyranoside(12),26-deoxycimicifugoside(13),升麻苷H-1(14),以及升麻苷H-2(15)。其中,化合物6为首次从该属植物中分离得到,化合物3,7,11为首次从该种植物中分离得到。选择人宫颈癌细胞(HeLa)和人乳腺癌细胞(MCF-7)以MTT法对分离得到的化合物进行了肿瘤细胞毒活性评价,化合物2~6对两种肿瘤细胞都具有显著活性。研究结果进一步丰富了我国升麻中药的化学多样性,同时为其药效的物质基础及其构效关系提供了理论依据。     

不同方法制备的海星皂甙细胞毒性评价

考察超临界CO2萃取、乙醇萃取两种方法制备的南海产多棘海星皂甙的溶血过程,采用分光光度法测定溶血指数,结合红细胞形态血观察,评价其细胞毒性。结果显示,两种方法制备的海星皂甙都具有明显溶血作用,超临界CO2萃取、溶剂萃取的海星皂甙溶血指数分别为19231,12821,超临界CO2萃取的海星皂甙保持了更强的细胞毒性,这为海星皂甙制备工艺的选择,探索其物质基础提供了参考依据。     

茶皂素在血吸虫病防治上的应用研究 I.茶皂素对血吸虫中间宿主钉螺的杀灭效果

用茶皂素对日本血吸虫中间宿主钉螺进行杀灭试验,初步结果表明,不同产地的茶皂素浸杀成螺、幼螺、蜾卵均有较好的杀灭效果。其中,茶皂素Ⅰ 2.5mg/L,茶皂素Ⅱ,Ⅲ 5.0mg/L,浸杀钉螺的效果均为100%。喷杀成蜾所需浓度较高,效果也稍差。茶皂素对淡水鱼类虽有一定的毒性,但比氯硝柳胺毒性低得多:茶皂素Ⅰ在1.6mg/L以下,茶皂素Ⅱ,Ⅲ在4.0mg/L以下,水温在28℃,48h,鲢鱼全部存活。茶皂素资源丰富,价格低廉,对环境无污染，是具有开发前景的植物杀螺剂。文中还对不同产地的茶皂素的毒性差异原因、使用浓度和方法进行了讨论。     

皂素生产废水后续处理方法的选择

用EM菌—活性污泥法和混凝法两种方法对经一次处理过的皂素生产废水进行二次处理,比较两种方法的处理效果。结果表明,在最佳条件下EM菌-活性污泥法对废水处理效果较好,最后出水可达排放标准;而混凝方法对废水处理的效果甚小,可以得出皂素生产废水不宜用混凝方法来预处理或后处理。     

Isolation,Identification, and Quantitative Determination of Saponin in Apostichopus japonicus by HPLC-DAD

Apostichopus japonicus is an important invertebrate that is widely used as a tonic food in Asian countries.The purpose of this study is to purify and identify a class of compound,the saponins,from the body wall of A.japonicus,and to establish a new me-thod to determine the quantity of saponins in the sea cucumber.In this study,the saponins of A.japonicus,cladoloside A(CA),were ob-tained from 80%ethanol extract by column chromatography for the first time and were characterized using the spectral method.The resulting purified saponins were then profiled using ¹HNMR,¹³CNMR,and ESI-MS,which revealed the CA molecular formula of C₅₃H₈₂O₂ and contained a triterpenoid backbone,a methylglucopyranosyl moiety,a quinovopyranosyl,and two xylopyranosyls.A me-thod for the quantitative determination of CA,comprising microwave-assisted extraction,high-performance liquid chromatography,and diode array detector method,was established.Extraction efficiency was optimized by changing microwave power,extraction sol-vent,volume,time,and temperature.Results showed that under the optimum conditions(extraction time of 10 min,temperature of 45℃,and solvent of 25 mL 70%ethanol under 400 W),the detection limit of CA was 0.0015 mg mL^?1,and the recoveries of CA from samples at spiking levels of 10,20,and 50μg g^?1 ranged from 90.1%-104%.The proposed method was successfully applied to ana-lyze the saponins in different tissues of A.japonicus collected in different seasons.The method developed in this study can provide quantitative technical support for the quality control of A.japonicus.     

甲基Funlioside B的合成

完成呋喃甾烷型甾体皂苷甲基Funlioside B的合成。在三氟化硼乙醚促进下,薯蓣皂苷元与乙酸酐反应以55%的产率得到3,16-二-氧-乙酰基-22-羟基-胆甾烷13。以三甲基硅基三氟甲磺酸酯为促进剂,化合物13与葡萄糖三氯亚胺酯给体11进行糖苷化反应以83%的产率得到单糖苷15。最后,在甲醇中,用氢氧化锂脱除酰基保护基团后并在无水甲醇中回流反应,以95%的产率得到甲基Funlioside B。