狼毒二萜类化学成分及其药理作用研究进展

狼毒Euphorbiae Ebracteolatae Radix为大戟科(Euphorbiaceae)植物狼毒大戟Euphorbia fischeriana或月腺大戟E.ebracteolata的干燥根,是一种广泛应用,具有广阔开发前景的中药材。狼毒含有多种生物活性成分,其中二萜类化合物是最为重要的一个部分,主要包括松香烷型、巴豆烷型、海松烷型、玫瑰烷型、西松烷型、巨大戟烷型、贝壳杉烷型、阿替斯烷型8种类型,此外还有少量二萜二聚体及其他类型的二萜类化合物。狼毒二萜类化学成分具有显著的抗肿瘤、抗炎、抗菌、抗病毒等药理作用。对狼毒二萜类化学成分及其药理作用进行综述,以期为更好地开发狼毒资源及其临床应用提供参考。     

中药紫株的化学成分研究

目的：研究紫株Callicarpa pedunculata R.Brown的化学成分。方法：利用各种色谱技术进行分离纯化,通过各种理化方法及光谱（IR,MS,^1HNMR,^13CNMR)分析鉴定其化学结构。结果：从紫株全草的氯仿提取物中分离得到10种化合物,分别鉴定为：4个二萜类化合物：14α－羟基－7,15－异松烷二烯－18烷酸（14α－hydroxy-7,15-isopimaradien-18-oic acid,Ⅰ）;16α,17-二羟基－3－氧－扁枝杉烷（16α,17-dihydroxy-3-oxo-phyllocladane,Ⅱ）;8,11,13,15-四烯松香烷－18－烷酸（8,11,13,15-abietatraen-18-oic acid,Ⅲ）;6α-羟基尼刀瑞尔醇（6α-hydroxy nidorellol,Ⅳ）;2个黄酮类化合物5－羟基－3,4‘,7-三甲氧基黄酮（5－hydroxy-3,4‘,7-trimethoxyflavone,Ⅴ）;3,5-二甲基莰非醇（3,5－dimethylkaempherol,Ⅵ）;其余的分别为：熊果酸（ursolic acid,Ⅶ）,肌醇（myoinositol, Ⅷ）,β-谷甾醇（β-sitosterol,Ⅸ）,β-香树素（β－amyrin, Ⅹ）。结论：化合物Ⅰ-Ⅵ为首次从该种植物中分离得到,且化合物Ⅰ-Ⅳ分别为4种不同类型的二萜。熊果酸的含量高达1％,本植物可作为其资源植物。     

Efficacy of phytol-derived diterpenoid immunoadjuvants over alum in shaping the murine host's immune response to Staphylococcus aureus

The ubiquitous gram-positive bacterium Staphylococcus aureus occupies a unique niche in humans for its ability to survive both as a commensal and a life-threatening pathogen. Its complex relationship with the host and its ability to engender a throng of virulence factors, have hindered the development of a successful vaccine against it. The use of immunoadjuvants to enhance host immunity and prevent the shift from commensalism to pathogenicity is a rational approach for containing infection. The objective of this study was to understand the mechanisms by which alum and two phytol-derived immunoadjuvants, phytanol (PHIS-01) ¹ and phytanyl chloride (PCl) ² shape the interaction between S. aureus and its murine host. We studied the effects of the phytol derivatives, relative to alum, on the induction of inflammatory cytokines and chemokines, recruitment of CD11b⁺ cells, generation of specific anti-S. aureus antibodies and in vitro clearance of S. aureus. Our results showed that both PHIS-01 and PCl were stronger inducers of protective cytokines IL-17 and IL-1β than alum, and far exceeded alum in enhancing anti-S. aureus antibody response. However, both alum and the phytol derivatives (particularly PCl) promoted efficient recruitment of CD11b⁺ cells. Furthermore, PHIS-01, alum and to a lesser extent, PCl were able to up-regulate the expression of key inflammation-related genes that were highly down-regulated by S. aureus alone. In vitro killing assays showed that both PHIS-01 and PCl were far more potent than alum in promoting S. aureus clearance; this indicated their efficiency in shaping an effective anti-S. aureus immune microenvironment. In summary, our study provides evidence for the better effectiveness of phytol-derived immunoadjuvants over alum in enhancing anti-S. aureus immunity.     

荚蒾属植物化学成分的研究进展

荚蒾属植物化学成分种类丰富,以vibsane型二萜、环烯醚萜等萜类成分为主,还有黄酮、木脂素、酚类和植物甾醇等成分,药用价值很高,有较大的开发潜力。本文通过查阅和分析相关文献,对荚蒾属植物的化学成分进行全面整理,旨在为该属植物的进一步研究和开发利用提供参考。     

固相萃取-高效液相色谱法测定拟缺香茶菜中3个二萜类成分的含量

目的建立测定拟缺香茶菜药材中二萜类成分Kamebacetal-A、Kamebacetal-B、肾形香茶菜丙素的方法。方法采用固相萃取-高效液相色谱法(SPE-HPLC)测定3个二萜类成分的含量。使用Venusil C18(4.6 mm×250 mm,5μm)反相色谱柱;流动相:乙腈(A)-水(B)梯度洗脱;流速:1 m L/min;柱温:30℃;检测波长230 nm。结果拟缺香茶菜中Kamebacetal-A、Kamebacetal-B、肾形香茶菜丙素分别在0.056~0.448 g/L(r=0.999 2),0.002 6~0.020 8 g/L(r=0.999 4),0.016~0.128 g/L(r=0.999 7)内与峰面积成良好的线性关系;平均回收率分别为97.53%(RSD=2.16%),96.02%(RSD=2.01%),98.23%(RSD=2.10%)。结论所建立的方法灵敏、准确、稳定,可用于拟缺香茶菜中Kamebacetal-A、Kamebacetal-B、肾形香茶菜丙素的含量测定,为拟缺香茶菜抗肿瘤谱效关系的研究奠定基础。     

南方红豆杉枝叶二萜类化学成分的研究

采用硅胶柱色谱以及制备HPLC等柱色谱方法,从南方红豆杉（Taxus wallichiana var. mairei）枝叶氯仿萃取部位分离鉴定了12个紫杉烷类二萜化合物,分别为： 2-deacetoxytaxinine E （1）,2-deacetoxytaxinine J （2）,7-deacetoxytaxinine J （3）,taxinine J （4）,7,2′-didesacetoxyaustrospicatine （5）,N-methyltaxol C （6）,2-deacetoxydecinnamoyl taxinine J （7）,taxol （8）, 7-epi-taxol （9）,7-epi-10-deacetoxytaxol （10）,cephalomannine（11）,7-epi-cephalomannine（12）。其中,化合物1,3为首次从该植物枝叶中分离得到。     

A new labdane-type diterpenoid from Leonurus japonicus

Five fractions prepared from the crude extract of Leonurus japonicus were examined in order to determine their cytotoxic potential. Under the bioassay guidance, a new labdane-type diterpenoid (1), and nine known ones (2–10) along with a seco-labdane (11) were isolated from the aerial parts of Leonurus japonicus. The structure elucidation was primarily based on comprehensive spectroscopic analyses, including HRESIMS, IR, and 1D and 2D NMR methods. Compound 4 (6β-hydroxy-15,16-epoxylabda-8,13(16),14-trien-7-one) exhibited potential cytotoxicity against HeLa cell line (IC₅₀ = 23.75 μM).     

南蛇藤茎的化学成分研究

目的研究南蛇藤Celastrus orbiculatus茎的化学成分。方法采用石油醚、醋酸乙酯、正丁醇分别对南蛇藤茎的乙醇提取物进行萃取;对萃取物运用硅胶、凝胶等分离手段进行反复分离纯化,经理化常数测定,结合UV、IR、1H-NMR、13C-NMR、MS方法鉴定结构。结果分离得到10个化合物,分别鉴定为山海棠二萜内酯A(Ⅰ)、(5β,8α,9β,10α,16β)-16-hydroxykaurane-18-oic acid(Ⅱ)、水杨酸(Ⅲ)、2,4,6-三甲氧基苯酚-1-O-β-D-葡萄糖苷(Ⅳ)、异槲皮苷(Ⅴ)、槲皮素-7-O-β-D-葡萄糖苷(Ⅵ)、( )-儿茶素(Ⅶ)、香草酸(Ⅷ)、β-胡萝卜苷(Ⅸ)、β-谷甾醇(Ⅹ)。结论以上化合物均为首次从该植物的藤茎中分离得到,化合物Ⅰ~Ⅲ为本属植物中首次分离得到,化合物Ⅳ~Ⅷ为本植物中首次分离得到。     

Chemical constituents of Isodon melissoides

Four new diterpenoids, melissoidesin E (1), F (2), G (4) and H (5), together with one known diterpenoid and two lignan glycosides, were isolated from aerial parts of Isodon melissoides. Their structures were established by spectral analysis and comparison with related compounds. The lignan glycosides (compounds 7 and 8) were the first examples to be isolated from the genus Isodon plants.     

香茶菜属植物的研究概况及药用前景展望

本文综述截止到1986年上半年国内外发表的有关香茶菜属植物研究的资料。对本属植物研究的大概趋势进行了概括;进而又在此基础上,对大家所关心的本属植物的药用前景作了一些探讨,并就这个问题提出笔者的几点看法。