蓝指海星Linckia laevigata中次级代谢产物及其生物活性研究进展

对蓝指海星Linckia laevigata中次级代谢产物及生物活性进行了综述。蓝指海星富含甾体皂苷和神经鞘糖脂类化合物,已从中分离鉴定了50余个化合物,其中甾体皂苷为主要化合物。药理活性研究表明,这类甾体皂苷能单独或协同神经生长因子(NGF)诱导PC12细胞神经突的生长,其活性与皂苷上连有的糖基密切相关,尤其是支链上单糖单元的存在提高了其活性。神经鞘糖脂类化合物的糖单元具有极其复杂的结构,限制了其分离与结构鉴定等研究工作。该类化合物能协同NGF诱导PC12细胞神经突的生长。本文对海星皂苷及鞘糖脂类化合物的构效关系研究具有参考价值。     

化学合成具有抗肿瘤活性甾体皂苷的研究进展

甾体皂苷是天然产物中～类重要的生物活性物质，人们已经发现了许多具有抗肿瘤活性的甾体皂苷化合物，对该类化合物的合成、结构改造及药理活性的研究也取得了一些进展，并初步总结出一些构效关系的规律。对进一步开发抗癌新药具有指导作用。该文对近10年来，化学合成的具有抗肿瘤活性的甾体皂苷的研究情况进行综述。     

C21甾体皂苷研究

甾体化合物是一类具有生物活性的天然产物,其中C21甾体皂苷生物活性较显著,本文对C21甾体皂苷分布状态、提取分离、结构鉴定和药理活性研究进行总结。     

盾叶薯蓣中甾体皂苷的分离与结构鉴定

目的对盾叶薯蓣根茎中甾体皂苷类的化学成分进行研究。方法利用常规柱层析法与制备型HPLC法相结合对盾叶薯蓣中的活性成分进行分离纯化,通过1 H-NMR、13 C-NMR和MS等光谱法鉴定单体化合物的结构。结果从盾叶薯蓣根茎中共分离得到了20个甾体皂苷化合物,其中7个化合物为首次从该植物中发现。结论盾叶薯蓣根茎中主要含有螺甾烷型和呋甾烷型甾体皂苷。     

一类新型高芳香胆甾烷型甾体皂苷元的NMR特征

目的 研究一类新型的高芳香胆甾烷型甾体皂苷元的NMR特征.方法 采用1D-和2D-NMR技术测定高芳香胆甾烷皂苷元的NMR数据,并结合文献数据进行分析.结果 对该类型化合物苷元的全部NMR信号进行了明确归属.结论 高芳香胆甾烷型甾体皂苷元的NMR特征明确,可为该类型的化合物结构鉴定提供重要参考.     

延龄草中主要化学成分的波谱特征

延龄草为我国传统中药材,甾体皂苷类是其主要活性成分。本文对延龄草中的甾体皂苷的化学结构和波谱学特征进行了归纳,为今后这类化合物的结构鉴定和核磁波谱数据归属提供了参考依据。     

薯蓣皂苷元药理活性及其机制研究进展

薯蓣皂苷元（diosgenin,Dio）作为一种重要的甾体皂苷元,是生产甾体激素类药物的主要原料,其来源广泛,抗肿瘤、抗炎、心血管保护等活性显著,具有很高的药用价值,日益引起国内外学者的关注。本文重点综述了国际上近年来有关薯蓣皂苷元药理活性及其作用机制的研究进展,以供参考。     

胡芦巴来源的甾体皂苷研究进展

中药胡芦巴是豆科一年生草本植物胡芦巴（Trigonellafoenum—graecumL．）的干燥种子,富含甾体皂苷。本实验室对胡芦巴中甾体皂苷进行了系统研究,包括原生呋甾皂苷及其酶解产物的分离鉴定、利用液质联用技术对甾体皂苷类成分的快速表征与结构分析,以及利用超临界流体色谱技术对螺甾皂苷C-25R／S异构体的分析、制备分离等。本文对本实验室相关研究进行总结,以期有助于胡芦巴的开发与利用,也为今后中药的化学成分研究工作提供借鉴。     

基于UHPLC-Q Exactive MS的分子网络技术快速分析龙葵叶物质成分

龙葵(Solanum nigrum L.)全草均可入药。本研究采用UHPLC-Q Exactive高分辨质谱结合GNPS分子网络(global natural products social molecular networking),对龙葵叶的化学成分进行快速表征。通过与文献报道数据比较,并结合质谱裂解特征规律分析,以及GNPS分子网络中已知和未知节点的关联分析,从龙葵叶中共鉴定157个化合物,包括甾体生物碱30个,甾体皂苷61个,黄酮类35个,氨基酸、有机酸等其他类型化合物31个。与龙葵果和龙葵茎相比,龙葵叶中甾体皂苷、甾体生物碱、黄酮类成分的种类均较为丰富,本研究结果为龙葵药材资源的精准利用奠定了基础。     

海星化学成分及其活性的研究进展

海星含皂苷，甾醇、蒽醌，生物碱和脂类等物质，海星的提取物及其提纯的化合物药理活性多样，包括对正常细胞和肿瘤细胞的体外细胞毒性，及抗菌，抗病毒，溶血，降压，抗炎等活性。     

海星甾醇保护樟柳碱处理的小鼠免致学习记忆障碍

海星甾醇〔己二酸 ( 5-雄甾烯 - 1 7-酮 - 3β-羟基 )二酯〕6.4,1 9.2 ,57.6mg·kg-1·d-1ig,每日 1次 ,共 30 d后 ,采用“Y”型迷宫实验 ,跳台实验 ,避暗法测定其对樟柳碱致小鼠学习记忆获得和再现障碍的影响 .结果表明 ,海星甾醇明显缩短 Y型迷宫实验小鼠到达安全区的时间 ,减少跳台实验中的错误次数 ,延长潜伏期 ,延长避暗法实验小鼠进入暗箱的潜伏期 ,减少错误次数 ,2 4 h后重复测试得到类似结果 ,与樟柳碱对照组有显著差别 ,达到或优于正常对照组水平 .结果说明海星甾醇能保护樟柳碱处理的小鼠免致学习记忆获得和再现障碍 .     

利用稻瘟霉分生孢子跟踪分离面包海星中的海星皂苷活性成分

目的研究面包海星中的海星皂苷活性成分。方法以稻瘟霉模型进行活性监测，采用多种层析手段和波谱技术对海星皂苷活性成分跟踪分离并鉴定其结构。结果分离获得14个海星皂苷，鉴定了其中12个结构(1～12)，包括7个新的海星皂苷(6～12)。其中大多对稻瘟霉显示活性且对K-562和BEL-7402肿瘤细胞株显示显著或中等强度的细胞毒性，2个皂苷有溶血作用。结论利用稻瘟霉模型对海星皂苷活性成分进行跟踪分离是可行的，该研究也为进一步开发抗肿瘤新药提供了有价值的先导化合物和科学依据。     

Two new steroidal compounds from starfish Asterias amurensis Lutken

Two new sulfated steroidal compounds (1 and 2), along with three known steroidal saponins (3, 4, and 5) were isolated from the starfish Asterias amurensis Lutken. The structures of new compounds were elucidated as 3beta-O-sulfated-cholest-5-ene-7alpha-ol (1) and (E) 25-O-beta-d-xylopyranosyl-26, 27-dinor-24(S)-methyl-22-ene-15alpha-O-sulfated-5alpha-cholest-3beta,6alpha-ol (2) by extensive NMR experiments and chemical evidence. Their effects on UMR106 cell proliferation were screened by MTT method. The results indicated that compounds 2 and 2a (0.01-100 microM) significantly promoted the osteoblastic proliferation. The initial structure-activity relationship analysis suggests that the sugar moiety is the necessary group for the activity.     

Biological activity of saponins and saponin-like compounds from starfish and brittle-stars

Twenty-four saponins and saponin-like compounds, isolated from starfish and brittle-stars, have been tested in four in vitro tests, based upon bacterial and cell tissue cultures. Saponin-like compounds from brittle-stars have previously not been tested for biological activity. In an antibacterial test based on an agar diffusion test, the Gram positive bacterium S. aureus was affected by the polyhydroxylated steroidal glycosides, polyhydroxylated sterols and disulfated sterols. However, none of the 21 compounds tested were active against the Gram negative bacterium E. coli. In a cytotoxicity test all 21 compounds tested influenced the cells at a concentration of 100 micrograms/ml, while the cells were unaffected at 1 microgram/ml. In an antitumor test, 16 compounds were tested on two lymphoma cell lines. Inhibition of cell growth, at a concentration of 5 ng/ml, was seen for three polyhydroxylated sterols, in one cell line. Weak activity was seen in an antiviral test at a concentration of 10 micrograms/ml.     

A novel polyhydroxyl sterol from Asterina pectinifera

A novel polyhydroxyl sterol (1) along with one known polyhydroxyl sterol (2), and two known monoglycosides, asterosaponin P1 (3) and its desulfated monoglycoside (4), have been isolated from the whole bodies of a common Pacific starfish Asterina pectinifera. The structure of the new polyhydroxyl sterol was determined as 15beta,16beta-isopropylidenedioxy-5alpha-cholestane-3beta,4beta,6alpha,7alpha,8,26-hexaol by spectroscopic methods, including FABMS, HR-FABMS, 1D and 2D NMR techniques.     

ISCOMs and other saponin based adjuvants

Saponins are chemically a heterogeneous group of sterol glycosides and triterpene glycosides which are common constituents of plants. One source of triterpenoid saponins obtained from the bark of Quillaia saponaria Molina (the soap bark tree) have been known to cause substantial enhancement of immune responses since the 1920s. Despite their use in animal vaccines, the development of saponin-based formulations for human vaccines has been impeded by their complexity and concerns about toxicity. This review briefly covers the use of saponins for animal vaccines but focuses mainly on the development of these adjuvants for use in man. Important aspects include preparation of purified or highly defined saponin fractions, improved understanding of the relationships between adjuvant activity, toxicity and structure of saponins and formulation of saponins into structures with reduced toxicity such as ISCOMs. Recent developments in the understanding of cellular interactions, cytokine induction and the in vivo localisation of saponin containing formulations will also be reviewed.     

Triterpenoidal saponins: bioactive secondary metabolites from Zygophyllum coccineum

Phytochemical investigation of the aerial parts of Zygophyllum coccineum L. led to the isolation of nine ursane-type triterpene saponins (1- 9), including the new one; zygophylloside S (1), together with a known flavonoid glycoside (10) and a sterol glycoside (11). The isolated compounds were tested for antifungal activity against several important plant pathogens and for insecticidal activity against two important mosquito species. Among the isolated compounds 1, 3, 5, 6, and 9 showed 32-77 % fungal growth inhibition at a concentration of 30 μM against Phomopsis viticola. Compound 9 showed 90 % and 80 % mosquitocidal activity at 3.1 μg/0.5 μL against Aedes aegypti and Culex quinquefasciatus, respectively.     

Separation and purification of saponins from Semen Ziziphus jujuba and their sedative and hypnotic effects

Semen Ziziphus jujuba (SZJ) has long been used in Chinese traditional medicine for the treatment of anxiety and insomnia because of its effect of decreasing monoaminergic system activity; saponins are thought to be the main bioactive factors. To investigate the sedative and hypnotic effects of saponins from SZJ, silica gel column chromatography and thin-layer chromatography were used to purify the crude extract of total saponins from SZJ. High-performance liquid chromatography showed that saponins from SZJ comprised two components, compounds I and II. Animal tests were conducted using these two compounds to compare their sedative and hypnotic effects. Results showed that both compounds had a significant effect (P < 0.05, P < 0.01) on walking time compared with that of the control group. Compound I had a significant effect on coordinated movement (P < 0.05). Both compounds prolonged the suprathreshold barbiturate induced sleeping time (P < 0.05). The number of sleeping animals increased by 30% and 20% for compounds I and II, respectively, under the subthreshold dose of sodium barbital.     

New cytotoxic sulfated saponins from the starfishCertonardoa semiregularis

Two new sulfated saponins designated as certonardosides P2 and I3 (1 and 2) were isolated from the brine shrimp active fraction of the MeOH extract of the starfish Certonardoa semiregularis. The structures were determined on the basis of spectral analysis. Compounds 1 and 2 were tested for cytotoxicity against five human tumor cell lines (A549, SK-OV-3, SK-MEL-2, XF498, and HCT15), and compound 1 displayed significant cytotoxicity against the SK-MEL-2 skin cancer cell.