Chemical Constituents from the Leaves of Zanthoxylum Schinifolium

cis‐Fagaramide ( 1 ), a new amide, together with fifty known compounds, have been isolated from the leaves of Zanthoxylum schinifolium. These known compounds include twenty‐one coumarins, eleven alkaloids, one furan, four benzenoids, three chlorophylls, four triterpenoids, one diterpenoid, one sesquiterpenoid, and four steroids. The structures of these compounds were determined by means of spectral analyses.     

2-氨基-4,5-二取代烃嘧啶类衍生物的新合成方法

研究了2-氨基-4,5-二烃基取代嘧啶类衍生物的一个新的简易合成方法,该方法以简单且廉价的4个芳香醛和3个脂肪醛为原料,经过四步反应得到12个2-氨基-4,5-二烃基取代嘧啶类化合物,总收率在40%～70%,经氢核磁共振(1H NMR)、碳核磁共振(13C NMR)和高效液质联用(LC-MS)对其目标产物进行表征.     

[2+2]型Schiff碱大环化合物及其配合物的合成

利用Mn2 ,Ba2 作为模板离子,合成了一类新型的Schiff碱型大环化合物,Mn2 用于L1和L2的合成,并在洗涤时自动解络,L3和L4的合成以Ba2 为模板.L3和L4的Ba2 配合物经与Na2SO水溶液反应解络,得到自由配体L3和L4.上述大环配体和各种配合物均经元素分析,IR,1H NMR,MS等证实了它们的结构和组成.     

The crystal structures of 10-oxa-1,4,7-trithiacyclododecane, 7,10,13-trioxa-1,4-dithiacyclopentadecane, 7,10,13,16-tetraoxa-1,4-dithiacyclooctadecane and 4,7,13,16-tetraoxa-1,10-dithiacyclooctadecane

The structures of four macrocyclic polyether sulfides have been determined by single crystal x-ray diffraction methods. The compounds studied were 1,4,7-trithia-12-crown-4, 1,4-dithia-15-crown-5, 1,4-dithia-18-crown-6 and 1,10-dithia-18-crown-6. In all four compounds the potential donor sulfur atoms point out of the ring. This causes the rings to be irregularly shaped.     

Synthesis,Characterization and Biological Activities of Novel Acrylamide Compounds

With dimethomorph and flumorph as the leading compounds, four novel acrylamide compounds with two types of structure were designed and synthesized by means of the method of ＂me too chemistry＂. The target compounds were characterized by 1H NMR, IR, MS, and elemental analysis. The influences of solvent and raw material on the yield were investigated and optimum processing conditions were determined. The results of preliminary biological tests show that all those compounds exhibit certain antifungal activities.     

Lipid constituents of Trifolium resupinatum var. microcephalum

The two new compounds (3-methyl-1-nonene-3-ol and 2',3'-dihydroxy propyl pentadecanoate) and four known compounds were isolated from Trifolium resupinatum L. var. microcephalum Zoh. (Leguminosae). All the compounds were reported for the first time from this plant. The stuructures of the isolates were determined by 1D, 2D NMR techniques and MS spectroscopy.     

Determination of Four Volatile Compounds with Anti-Inflammatory Biological Activity in Houttuynia chordata Thunb. by Gas Chromatography and Gas Chromatography–Mass Spectrometry

An analytical procedure was developed for the determination of four volatile components with anti-inflammatory biological activity in Houttuynia cordata Thunb. by gas chromatography and gas chromatography–mass spectrometry. Four compounds (α-pinene, β-myrcene, 1-decanol and 2-undecanone) were selected as analytes because they are common major constituents in volatile compositions of Houttuynia cordata Thunb Anti-inflammatory efficacy in vivo suggested that the four compounds provided inhibitory effects on xylene-induced ear edema formation in a dose-dependent manner. The four compounds were determined by gas chromatography in mouse serum after oral administration of volatile oil and water distillate liquid of Houttuynia cordata Thunb Related chromatographic conditions were investigated and selected. A good separation of the four compounds and internal standard was achieved. The method reflected the quality of Houttuynia cordata Thunb. and its preparations.     

High-performance liquid chromatography on dynamically modified silica : III. Modification of silica with long-chain and symmetrical quarternary ammonium compounds

The influence of the nature of quaternary ammonium compounds on retention in high-performance liquid chromatography on dynamically modified silica was investigated. Adsorption isotherms were determined on bare silica (LiChrosorb Si 60) for four alkyltrimethylammonium bromides and two symmetrical tetraalkylammonium bromides, each containing 15–21 carbon atoms. It was found that only the long-chain quaternary ammonium ions are adsorbed on to the silica surface in appreciable amounts and that the affinity increasing number of carbon atoms in the alkyl chain. The maximum amount that can be adsorbed per gram of silica is of the same order of magnitude for each of the four long-chain quaternary ammonium compounds. This amount, however, is reached at lower concentrations in the eluent the longer is the alkyl chain.The retention of five test compounds was determined over the whole concentration range investigated for each of the modiflying agents. The surfactant concentration that causes maximum retention for four of five test compounds coincides with its critical micellar concentration. The retention mechanisms and the influence of the type of the modifying agent on selectivity are discussed, and compared with published results on related experiments on chemically bonded stationary phases.     

新型手性单胺氧化酶选择性抑制剂的设计、合成与生物活性研究

本文以取代的手性苯乙胺为原料,设计合成了4种新型叔胺盐酸盐化合物.通过NMR,IR和MS等表征方法对所合成目标产物的结构进行确定.在生物活性方面,首先通过CCK-8法测定4种化合物对正常细胞增殖的影响,实验结果表明:部分化合物对小鼠成纤维细胞L929表现出一定的细胞毒性.酶的选择性实验说明R构型影响小分子对单胺氧化酶(MAO)的选择性抑制活性,另一方面取代基的给电子能力也会对酶的活性有影响.     

Chemical constituents of Taraxacum formosanum

Three new compounds, taraxacine-A (1), taraxacine-B (2) and taraxafolin (3) together with twenty-five known compounds, which include two beta-carboline alkaloids, two indole alkaloids, two chlorophylls, two flavonoids, one coumarin, two triterpenoids, one monoterpenoid, one ionone, four steroids and eight benzenoids, were isolated and characterized from the fresh aerial parts of Taraxacum formosanum. Structures of new compounds were determined by spectral analysis.     

Flavonoids isolated from Draconis Resina

One new chalcone, 4,6-dihydroxy-2-methoxy-3-methyldihydrochalcone (4), together with four known compounds, dammaradienol (1), (-)-5-methoxyflavan-7-ol (2), 5-methoxy-6-methyl-2-phenyl-7H-chromen-7-one (3), and dracorhodin (5), were isolated from Draconis Resina. The structures of these compounds were determined by spectral methods. Among these five compounds, compounds 1, 2, and 3 exhibited cytotoxicity against KB and HepG2 cells.     

Cytotoxic Constituents from the Stem Bark of Zanthoxylum Pistaciiflorum

Two new esters, methyl 4‐(prenyloxy)dihydrocinnamate and methyl 4‐(geranyloxy)dihydrocinnamate, together with fourteen known compounds have been isolated from the stem bark of Zanthoxylum pistaciiflorum. The structures of two new compounds were determined through spectral analyses. Among the isolates, four compounds exhibited effective cytotoxicities against P‐388 and HT‐29 cell lines in vitro.     

1,3-双(氯硅基)丙烷与硫化氢的反应

用氯铂酸为催化剂,由有机硅氢化物对烯丙基硅化合物加成,合成了四个新的1,3-双(氯硅基)丙烷(A)。以九个不同的(A)在吡啶的存在下,分别与硫化氢反应,得到了十一个新的六元杂环(1-硫-2,6-二硅环己烷)化合物。测定了它们的物理常数,用物理和化学方法确证了结构。     

Studies on Fragrance Raw Materials of α-Terpineol Analogues

Thirty four α-substituted or α, α-disubstituted-( 1-methylcyclohexen-4-yl )methanols and α-substituted or α,α-disubstituted-(4-methylcyclohexyl) methanols weresynthesized. Thirty two of them are new compounds. 1H NMR and IR spectra of allthe compounds were determined, MS spectra of some of them were obtained as well.The characteristic odors were evaluated.Keywords Fragrance raw materials,α-Terpineol analogues, Synthesis, Structuredetermination     

海洋放线菌S592次级代谢产物及其体外抑菌活性研究

对海洋放线菌S592的次级代谢产物以及体外抑菌活性进行研究.将菌株S592进行大量发酵,采用色谱方法对菌株发酵产物进行分离纯化,通过波谱技术对所获单体化合物进行结构鉴定,并测定化合物的体外抑菌活性.从海洋放线菌S592中分离得到6个化合物,含2个螺环抗生素lobophorin类化合物,1个环肽类化合物,2个苯甲酰胺类化...     

Three new phenanthrenes from Monomeria barbata Lindl

<正>Three new monophenanthrene compounds were isolated from an acetone extract of the tubers of Monomeria barbata Lindl. (Orchidaceae).Using spectroscopic methods,the structures of compounds 1-3 were determined as 1,4,7-trihydroxy-2-methoxy- 9,10-dihydrophenanthrene(1),1-(p-hydroxybenzoyl)-2-methoxy-4,7-dihydroxy-9,10-dihydrophenanthrene(2),1,3,8-tri(p-hydroxybenzyl) -4-methoxy-phenanthrene-4,7-diol(3).These compounds showed cytotoxicities on four tumor cell lines(HepG2, HL-60,Skov-3,A431).     

A new phenolic amide from the roots of Paris verticillata

A new phenolic amide 8, together with the nine known phenolic compounds 1-7, 9 and 10 were isolated from the MeOH extract of the roots of Paris verticillata. The structure of the new compound 8 was determined to be 1-N-feruloylaminobutyl-4-rho-hydroxybenzamide by spectroscopic methods. The isolated compounds were tested for cytotoxicity against four human tumor cell lines using the SRB assay.     

Phomosines H-J, novel highly substituted biaryl ethers, isolated from the endophytic fungus Phomopsis sp. from Ligustrum vulgare

From the endophytic fungus Phomosis sp., four known phomosines A-D (1-4) and three new phomosines H-J (5-7) have been isolated. The structures of the new compounds were determined on the basis of their spectroscopic data analysis (1H, 13C, 1H-1H COSY, HMQC, and HMBC NMR, as well as mass spectrometry). The structures of phomosine H (5) and J (7) were also confirmed by semisynthesis from phomosine A (1). The remaining four known compounds [phomosines A-D (1-4)] were identified by comparing their spectroscopic data with those reported in the literature. The four known metabolites were biologically active. Of the novel metabolites, only 6 was antifungal and antibacterial.     

HPLC法测定不同施肥模式栽培的金线莲中黄酮类成分

HPLC法测定不同施肥模式栽培的金线莲中3种黄酮类成分:槲皮素、山奈酚和异鼠李素.超声-微波协同提取法提取4种不同施肥模式下金线莲中的黄酮类成分.HPLC-电喷雾离子化法/质谱(HPLC-ESI-MS)对黄酮类化合物进行定性分析.HPLC分析得槲皮素在0.25~20.0μg/m L(r=0.999 2)、山奈酚在0.25~20.0μg/m L(r=0.999 5)、异鼠李素在1.0~80.0μg/m L(r=0.999 0)范围内峰面积与浓度呈良好的线性关系,不同栽培方法的金线莲药材中槲皮素、山奈酚、异鼠李素的质量分数分别在151.8~240.0、47.2~88.2、16.8~29.8μg/g之间.方法简单、精确,快速,可为科学评价不同培养模式金线莲质量提供依据.栽培过程施加氮、磷、钾(NPK)复合肥及添加腐植素和微量元素,能提高金线莲中3种黄酮类成分的含量.栽培过程施加硫、磷(SP)复合肥,槲皮素、山奈酚和异鼠李素的质量分数分别下降了2.3%、17.2%和18.8%.结果表明采用不同施肥模式直接影响到药材中的药效物质的含量.     

Design,synthesis, cytotoxicity and 3D-QSAR analysis of new 3,6-disubstituted-1,2,4,5-tetrazine derivatives as potential antitumor agents

We synthesized two new series of 3-substituted-6-(2,5-dimethylpyrazol-1-yl)-1,2,4,5-tetrazines and analysed them for a potential role as antitumor agents. Twenty-two compounds were obtained, and four molecular structures were determined by X-ray diffraction analysis. Using flow cytometry and MTT assay, potential action on cell toxicity was determined for each of the compounds for four cancer cell lines. The potency and selectivity demonstrated by these compounds are dependent on the cancer cell line, where the following compounds were found the most promising agents against certain cell lines: compounds 1i and 1j for HL-60 cells, 1a and 1b on HCT116 cells, 1f on Hela cells and 2h on H1975 cells. The action exerted by these compounds is comparable to the well-known cancer treatment drug etoposide and higher than vatalanib. To arrive at the structural requirements for activity on each cell line, a SAR and 3D-QSAR analysis was carried out. From the 3D-QSAR models, steric and electronic features were identified in the aromatic centres, and were key components for cytotoxic activity on HL-60 cell lines. The cytometry results suggest that some tetrazine derivatives induce apoptosis on HCT116 cells.