495 resultados para R1


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Interferons (IFNs), consisting of three major subfamilies, type I, type II (gamma) and type III (lambda) IFN, activate vertebrate antiviral defences once bound to their receptors. The three IFN subfamilies bind to different receptors, IFNAR1 and IFNAR2 for type I IFNs, IFN gamma R1 and IFN gamma R2 for type II IFN, and IL-28R1 and IL-10R2 for type III IFNs. In fish, although many types I and II IFN genes have been cloned, little is known about their receptors. In this report, two putative IFN-gamma receptor chains were identified and sequenced in rainbow trout (Oncorhynchus mykiss), and found to have many common characteristics with mammalian type II IFN receptor family members. The presented gene synteny analysis, phylogenetic tree analysis and ligand binding analysis all suggest that these molecules are the authentic IFN gamma Rs in fish. They are widely expressed in tissues, with IFN gamma R1 typically more highly expressed than IFN gamma R2. Using the trout RTG-2 cell line it was possible to show that the individual chains could be differentially modulated, with rIFN-gamma and rIL-1 beta down regulating IFN gamma R1 expression but up regulating IFN gamma R2 expression. Overexpression of the two receptor chains in RTG-2 cells revealed that the level of IFN gamma R2 transcript was crucial for responsiveness to rIFN-gamma, in terms of inducing gamma IP expression. Transfection experiments showed that the two putative receptors specifically bound to rIFN-gamma. These findings are discussed in the context of how the IFN gamma R may bind IFN-gamma in fish and the importance of the individual receptor chains to signal transduction. (c) 2009 Elsevier Ltd. All rights reserved.

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The toxic effect of Pb2+ has been studied in eukaryotic cells by using Tetrahymena as a target. The maximum power (P (m)) and the growth rate constant (k) were determined, which showed that values of P (m) and k were linked to the concentration (C) of Pb2+. The addition of Pb2+ caused a decrease of the maximum heat production and growth rate constant, indicating that Tetrahymena growth was inhibited in the presence of Pb2+, and Pb2+ took part in the metabolism of cells. From micrographs, morphological changes of Tetrahymena were observed with addition of Pb2+, indicating that the toxic effect of Pb2+ derived from destroying the membrane of surface of Tetrahymena. According to the thermogenic curves and photos of Tetrahymena under different conditions, it is clear that metabolic mechanism of Halobacterium halobium R1 growth has been changed with the addition of Pb2+.

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基于春玉米生长季土壤温度动态观测资料,研究黄土高原南部旱作区不同水分管理模式对春玉米(Zeamays)农田土壤温度动态变化和玉米生育期土壤积温(>10℃)的影响,其结果对理解不同水分管理模式对玉米生长影响具有一定参考价值。【方法】以沈单10为供试作物品种,水分管理模式2007年采用补充灌溉、雨养和地膜覆盖3种处理。在2007年基础上,2008年增加秸秆覆盖,试验采用完全方案,于2007年和2008年连续进行2年田间试验。【结果】地膜覆盖具有明显的增温效应,而秸秆覆盖具有明显降温效应;玉米不同生育阶段>10℃土壤积温,以出苗阶段(PT-VE)最低,生殖生长阶段(R1-R6)次之,营养生长阶段(VE-R1)最高。不同水分管理模式对不同生育期的土壤积温影响不同:地膜覆盖在PT-VE阶段较低,补充灌溉在VE-R1阶段较低,雨养处理在R1-R6阶段较低。地膜覆盖条件下土壤温度对大气温度变化的响应更为敏感,与大气温度变化最为紧密;而秸秆覆盖土壤温度对大气温度变化的反应最迟钝。补充灌溉和地膜覆盖处理籽粒产量显著高于雨养处理(P<0.05),与雨养相比,2007和2008年补充灌溉分别增产30.0%和25.7%,地膜...

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中药化学成分,尤其是活性成分,是中药发挥药效作用的物质基础,它的深入研究是中药现代化的关键和核心。而中药成分的复杂性和药效的整体性,一般的分析及研究方法无法简捷快速地解决中药有效成分鉴定的难题,直接影响到中药研究开发的进程。质谱技术,尤其是软电离质谱及其联用技术,由于其具有灵敏、快速、分辨率高的优点,使得质谱日益成为研究复杂生物分子和中药体系中的应用问题的强有力手段。本论文以刺五加新药的开发为背景,采用有效部分的研究方法,运用先进的质谱技术,以药理活性筛选为指导,全面地研究了刺五加的活性成分。首先,采用电喷雾多极串联质谱技术,研究了正负离子条件下传统中药刺五加中的有效成分刺五加营B和刺五加营E的特征质谱行为,并提出了质谱碎裂机理,可以此鉴定传统刺五加有效成分,对传统刺五加药材及相关药品的快速鉴别和质量控制具有重要意义。以人参皂营R1为例,定量地研究四种碱金属离子浓度对皂普结构分析的影响,为合理添加碱金属离子以提高皂着分析的灵敏度提供了依据。在此基础上,用电喷雾多极串联质谱技术简便而又快捷地区分了两对生理活性差别较大的人参皂营的同分异构体:Rg1和PF11,Rg2和Rg3,为深入研究人参皂普的药效成分和作用机制奠定了一定的基础。系统地研究了β-香树”脂醇型的三种五环三菇皂营在不同模式下的多级串联质谱特征,为从多角度阐明皂昔类化合物的结构提供了新的思路。结构相近的皂普类化合物在电喷雾多级串联质谱中都表现出了与其自身结构相符的特征质谱行为,为不同皂营混合物的快速鉴定提供了一种快速有效的分析方法。在此基础上,研究了两种典型的刺五加仆卜皂营的质谱特征,并用多种质谱手段从刺五加叶总皂普中检测到18种皂普成分,其中有8种皂营成分在刺五加中而未见有文献报道,并用质谱首次发现了刺五加叶皂营的结构和其在植物体内代谢的相关性,这一结果对研究刺五加皂营的体内代谢有着十分重要的意义。以药理目标活性成分为指标,采用对比实验和一系列正交实验,对刺五加活性成分的提取方法,提取工艺和纯化工艺进行了优化,首次采用联合树脂法一次性分离纯化刺五加中两类有效成分总皂昔和总黄酮,经工艺优化最终得到总有效成分达85%以上的刺五加制剂,为刺五加新药的开发提供了大量的工艺参数。基于环糊精包合物(CDs)在中药剂型改造及提高某些药物稳定性和生物利用度方面广阔的应用前景和刺五加新药开发中的实际需要,系统到研究了三种环糊精(a-CD,β-CD和γ-CD)与刺五加皂昔元齐墩果酸(OA)形成的复合物。纬果表明,三种环糊精都能与OA形成稳定的l:1复合物,而β-CD和γ-CD还能与以形成2:1“三明治”状的复合物。复合物气液两相性质具有良好的相关性,为质谱快速筛选和表征这类非共价复合物提供了必要的条件。采用同样的方法对三种环糊精与刺五加中黄酮类化合物(芦丁和懈皮素)的复合物进行了系统研究,结果发观,三种环糊精都与芦丁(R)和棚皮素(Q)形成1:1复合物。但复合物稳定性有差异,对环糊精与芦丁的1:1复合物,以β-CD复合物最稳定,而对于环糊精与槲皮素1:1复合物则以α-CD复合物最稳定,这与芦丁含有糖链有关。刺五加活性成分黄酮类化合物生物利用度和活性的另一有效途径是制备黄酮-金属络合物。黄酮-金属络合物作为潜在的药物开发正日益受到重视,本文利用电喷雾质谱系统地研究了第四周期五种二价金属离子与棚皮素形成的络合物,并采用多级串联质谱部分表征了这些络合物的结构和稳定性之间的关系,为建立黄酮金属络合物筛选体系和表征提供了一种较好的方法,为这类新药的研制开发提供了一定的理论基础。

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天花粉蛋白(Trichosanthin,TCS)是从葫芦科植物括楼(TrichosanthesKiriloii)球根中提取的一种由247个氨基酸组成的I型核糖体失活蛋白(RibosomeInactivatingProtein,RIP)。TCS具有广谱的生物学和药学活性,包括抗肿瘤、免疫抑制、中期引产以及抗病毒活性,TCS还具有抗白血病和淋巴瘤的作用。TCS能够抑制HI卜1在急性感染的T淋巴细胞和慢性感染的巨噬细胞中的复制。TCS抗HIV的机制还不清楚,一般认为与R1(RibosolneInactivating)活性有关。TCS的毒副作用限制了它在抗HIV/AIDS临床上的进一步应用。人们期望通过改造或修饰,在保留TCS抗HIV活性的同时,降低其神经毒副作用及所引起的变态反应。因此,研究TCS的抗HIV-1作用机制及构效关系,有利于拓宽TCS的临床应用适应症,也对RIP类化合物基础研究和应用研究具有重要的指导作用。本论文在实验室己有研究工作的基础上,对TCS抗HIV-1作用、机制及构效关系进一步研究。首先,采用MTT比色法检侧TcS对人T淋巴细胞系C8166、HIV-1慢性感染细胞系H9/HIV-1IIIB细胞毒性作用以及采用台盼蓝染色法检测了TCs对刺激转化的人外周血单个核细胞(PeriphejralBloodMononuclearCen,PBMC)的细胞毒性作用;以合胞体形成抑制实验检测了TCS对实验株HIV-1ms诱导C8166细胞致细胞病变的抑制作用;以捕捉HIV-1p24抗原ELISA方法检测TCS对实验.株HIV-1IIIB在急性感染C8166,细胞和慢性感染Hg细胞中复制的抑制作用、临床分离株HIV-1KMO18在PBMC中复制的抑制作用、耐药株HIV-174v在C8166细胞中复制的抑制作用。其次,利用荧光实时定量RT-PCR检测了TCS对HIV-IIIB吸附和融合宿主细胞的抑制作用;采用高效液相色谱(HighPerformanceLiquidChromatograPhy,HPLC)检测了TCS脱HIV-IRNA腺嘿呤作用;另外还检测了TCS对病毒颗粒的直接杀伤作用、TCS对HIV感染和未感染细胞融合的抑制以及对HIV重组逆转录酶活性的抑制作用。最后,利用以蛋白工程技术构建的14个TCD突变体研究其抗HIV的构效关系,其中活性中心突变体:结果表明,TCS不仅能够有效抑制实验株HIV-1mB在C8166细胞中的复制和HIV-1ms诱导宿主细胞的病变作用,还能抑制临床分离株HIV-1KM018在PMBC中的复制和耐药株HIV-174v在C8166细胞中的复制,但TCS对HIV-1在慢性感染H9细胞中的复制无直接抑制作用。TCS不能抑制HIV-1进入宿主细胞;对感染细胞和未感染细胞的融合没有抑制作用;TCS也不能抑制HIV-1重组逆转录酶活性;TCS对病毒颗粒的直接杀伤作用不大;但TCS能够使裸露的HIV-1RNA脱腺漂呤,可能TCS的脱缥岭活性或其它酶活性直接损伤病毒或者病毒感染细胞的核酸,而胞质腺嗦岭含量的增高则可以导致线粒体膜电位的降低、细胞色素C的释放、活性氧的增加和抗凋亡因子表达的下降,结果使感染细胞更多的凋亡,这可能是TCS抗HIV的一个机制。结果也表明,活性中心突变体TCSM(120-123)与TCSE160A/E189A,在失去绝大部分R工活"性的同时,也几乎完全失去抗HIV活性。、而另一个活性中心突变体TCSR122G,RI活性下降1的倍,却仍保留一定的抗HIV活性。TcSC末端删除突变体(TCSC2,TCSC4和TCSC14)抗HIV活性的下降(1.4-4.8倍)与其R1活性呈平行下降(1.2-3.3倍)。这些结果表明TCS抗HIV-1活性与其R1活性显著相关,但似乎又不是唯一的决定因素,因为我们发现二个分别在C末端加上末端19个氨基酸延伸肤或KDEL信号肤的突变体TCS饥触与TCSKDEL,虽然保留全部的RI活性,但却几乎完全失去抗HIV活性,表明有其它机制介入了TCS的抗HIV-1活性。TCS抗原决定簇位点突变后对TCS抗HIV-1活性没有显著影响,但当在抗原决定簇突变体所引入的Cys残基上加上PEG漱后,这些突变体则显著降低了抗HIV-1的活性。

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选择青海湖地区的次生芨芨草草地为研究对象,以围栏内封育和围栏外自由放牧的草地做对照,研究了围栏内外土壤种子库的萌发状况、密度和数量、物种多样性,以及土壤种子库与地上植被的关系。结果表明,围栏内外土壤种子库的萌发趋势非常相似,但是萌发种子累计数量不同;围栏内外土壤种子库中萌发种子的平均密度分别为3660和2460粒·m-2,围栏内萌发种子数比围栏外提高了48.8%;围栏内外土壤种子库的物种多样性指数差异较大,围栏内外丰富度指数R1分别为17和13,R2为3.693和2.832,丰富度围栏内大于围栏外,多样性指数和丰富度指数具有相同的规律,均匀度指数围栏内外分别为0.812和0.857,则是围栏外大于围栏内。围栏内外地上植被群落组成存在显著差异,围栏内的封育草地的物种丰富度和多样性指数均大于围栏外的放牧草地,而均匀度指数则呈相反趋势。

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由Bi(Hcydta).5H2O和Nd(NO3).6H2O按1︰1的物质的量比,在水溶液中合成了含Bi(III)-Nd(III)的异核配位聚合物{[(NO3)Nd(H2O)4(μ3-cydta)Bi(μ-ONO2)].2.5H2O}n.用元素分析、红外光谱、热重-差热和X射线单晶衍射等手段对标题配合物的组成和结构进行了表征.该配合物属三斜晶系,空间群P1,晶胞参数:a=0.9235(3)nm,b=1.0902(4)nm,c=1.4253(5)nm,α=71.840(4)°,β=86.877(4)°,γ=76.991(4)°,Z=2,Mr=936.65,V=1.3284(8)nm3,Dc=2.342g.cm-3,μ=8.646mm-1,F(000)=900,最终偏离因子R1=0.0406,wR2=0.1124.在该配合物中,铋(III)与配体cydta4-的4O2N和1个硝酸根中1个O原子以及邻位分子的硝酸根形成8配位的畸变双帽三棱柱.钕(III)与4个水分子的O,1个硝酸根中2个O以及来自3个不同配体cydta4-的桥联羧基O结合,形成9配位的三帽三棱柱构型.羧酸根在Bi—Nd和硝酸根在Bi—Bi间的桥联作用...

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A new compound, (CH5N2)(3)(PMo12O40CH4N23H2O)-C-.-H-. (1), was synthesized and structurally characterized by elemental analyses, IR spectra, UV spectra, NMR spectra and ESR spectra. This is, to our knowledge, the first example of an imidazole-polyoxometalate species. The compound was recrystallized from N,N-dimethylformamide (DMF), and then black block-like crystals of (C3H5N2)(4)((PMoMo11O40)-Mo-V-O-VI)(.)4C(3)H(7)NO(.) 2H(2)O (2), were obtained. It crystallizes in a triclinic space group P (1) over bar with n=12.423(3) Angstrom, b=12.666(3) Angstrom, c=13.341(3) Angstrom, alpha=70.56(3)degrees, beta=71.16(3)degrees, gamma=64.18(3)degrees, V= 1742.3(6) Angstrom(3), Z=1, R1 = 0.0585, wR2 = 0.1885. An X-ray crystallographic study showed that the crystal structure is constructed by electrostatic attractions and hydrogen bonds between a dodecamolybdophosphoric anion and an imidazole. The imidazole and DMF molecules occupy cavities in a polyoxometalate lattice ordered along a c-axis. The structure of (2) is similar to that of (1) from a comparison of both IR spectra and TGA Curves.

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A novel compound [Ni(phen)(3)](2)[(SiMo10V1/2O40)-O-V((VO)-O-IV)(2)] . 2H(2)O has been hydrothermally synthesized and structurally characterized by single-crystal X-ray diffraction. The compound crystallizes in the triclinic, system, space group P-1, a = 12.378(4) Angstrom, b = 14.148(5) Angstrom, c = 14.316(2) Angstrom, alpha = 105.91(2)degrees, beta = 95.31(2)degrees, gamma = 96.89(3)degrees, V = 2373.0(12) Angstrom(3), Z = 1, (lambdaMo(Kalpha)) = 0.71073 Angstrom, R1 (wR2) = 0.0869(0.2174). Data were collected on a Siemens P4 four-circle diffractometer at 293 K in the range of 1.51 < theta < 22.50degrees using the omega-scan technique. Empirical absorption correction (psi scan) was applied. The structure was solved by the direct method and refined by the Full-matrix least-squares on F-2 using the SHELXL-97 software. X-ray crystallographic study showed that the title compound contained a bi-capped alpha-Kegin-type [(SiMo10V2O40)-O-IV((VO)-O-IV)(2)](4-) polyoxoanion.

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Two novel dibenzo-18-crown-6 sodium isopolytungstates, [(DB18C6)(CH3OH)Na](2)W(6)O(19)(.)DB18C6(.)H(2)O 1 and [(DB18C6)(DMF)(2)Na](4)W(10)O(32)(.)2DMF(.)2H(2)O 2, have been synthesized in mixed methanol and acetonitrile solvents and characterized by elemental analysis, TGA, IR and single crystal X-ray diffraction. The compound 1 crystallizes in the monoclinic space group C2/c with a = 23.182(8), b = 19.527(2), c = 18.737(3) Angstrom, beta = 115.15(2)degrees, V = 7678(3) Angstrom(3), Z = 4, and R1(wR2) = 0.0611(0.1504). The compound 2 crystallizes in the monoclinic space group P21/n with a = 16.516(2), b = 22.325(6), c = 20.425(7) Angstrom, beta = 91.78(2)degrees, V = 7528(3) Angstrom(3), Z = 2, and R1(wR2) = 0.0397(0.0773). The compound 1 exhibits a novel organic-inorganic sandwich-type structure, in which the crown ether-sodium complexes are coordinated to the terminal oxygen atoms of W6O192-. In compound 2, all Na+ ions are thoroughly enveloped into the organic moieties of crown ether and DMF molecules and are connected with the 'naked' polyanions W10O324- via the electrostatic attraction.

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The title compound, [C12H24O6][H3PMo12O40]. 22H(2)O, was synthesized by the self-assembly of 18-crown-6 (abbreviated as C12H24O6 or 18C6) and H3PMo12O40 in the mixed solvent of CH3OH and CH3CN, and was characterized by IR, H-1 NMR and Xray diffraction for the first time. Crystal data: Triclinic, P (1) over bar, a = 13.428(3) Angstrom, b = 13.557(3)A, c = 14.642(3) Angstrom, a = 105.39(3)degrees, beta = 90.06(3)degrees, gamma = 119.56(5)degrees, V = 2207.5(8) Angstrom(3), Z = 1, R1 = 0.0719, wR2 = 0.1990. It has a disordered alpha-Keggin PMo12O403- anion, which contains the strong alternating short (mean 1.844 Angstrom) and long (mean 1.958 Angstrom) Mo-O-Mo bonds. In the unit cell, crown ethers and molybdophosphates are alternatively arranged in good order along c-axis. An oxonium ion is located at the center of a crown ether molecule., Oxonium ion interacts with 18C6 by the means of hydrogen bonds (mean 2.7771 Angstrom), which are electrostatic or resonant. The observations show the existence of [H3O(C12H24O6)](+) (C) 2000 Elsevier Science B.V. All rights reserved.

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长链烷氧基取代苯基卟啉化合物是一类性能良好的充电膜材料及照相感光材料.本文对合成一系列四-(对-烷氧基笨基)卟啉(取代基如式(1)R1=R2=R3=R4=H;(2)R1=C16H33,R2=R3=R4=H;(3)R1=R2=C16H33,R3=R4=H;(4)R1=R2=R3=C16H33,R4=H;(5)R1=R2=R3=R4=C16H33)进行质谱分进,结果表明,当用DEI电离方式时,不仅能给出较大丰度的分子离子峰,而且其EDIMS谱还清楚地反映出卟啉苯环羟基氢取代基团的丢失规律.然而其他电离方式却难以达到这样的效果.2 样品与仪器 部分所用样品承吉林大学王永祥博士赠送.质谱实验在 VG公司生产的 Quattro三级四极串联质谱仪上进行,采用DCI方式进样,但不通反应气故称DEI,离子源温度为100℃,发射电流260μA,用IBM386数据系统采集数据.

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Reaction of 1,3-cyclohexadiene(tricarbonyl)iron (1) with ortho-substituted aryllithium reagents ArLi (Ar=o-CH3C6H4, o-CH3OC6H4, o-CF3C6H4) in ether at low temperature, and subsequent alkylation of the acylmetalates formed with Et3OBF4 in aqueous solution at 0-degrees-C or in CH2Cl2 at -60-degrees-C gave the 1,3-cyclohexadiene(dicarbonyl)[ethoxy(aryl)carbene]iron complexes (eta4-C6H8)(CO)2FeC(OC2H5)Ar (3, Ar = o-CH3C6H4; 4, Ar = o-CH3OC6H4), and the isomerized product (eta3-C6H8)(CO)2FeC(OC2H5)C6H4CF3-o (5), respectively, among which the structure of 3 has been established by an X-ray diffraction study. Complex 3 is monoclinic, space group P2(1) with a = 8.118(4), b = 7.367(4), c = 14.002(6) angstrom, beta = 104.09(3)-degrees, V = 812.2(6) angstrom3, Z = 2, D(c) = 1.39 g cm-3, R = 0.056, and R(w) = 0.062 for 976 observed reflections. Complexes 3 and 5 were converted into the chelated allyliron phosphine adducts(eta3-C6H8)(CO)2(PR31)FeC(OC2H5)Ar (6, Ar = o-CH3C6H4, R1 = Ph; 7, Ar = o-CH3C6H4, R1 = OPh; 9, Ar = o-CF3C6H4, R1 = Ph), by reaction with phosphines in petroleum ether at low temperatures.

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海洋生物具有产生丰富多样的次生代谢产物的能力,其中红藻门松节藻科海藻卤代次生代谢产物以其结构新颖、生物活性独特引起了天然产物化学家的重视。 本论文对海洋红藻多管藻和松节藻进行了化学成分研究,综合利用各种色谱学方法 (硅胶柱层析、反相硅胶柱层析、凝胶Sephadex LH-20柱层析、半制备高效液相色谱以及重结晶等) 和现代波谱学技术 (IR、UV、EI-MS、FAB-MS、HR-ESI-MS、CD、1H-NMR、13C-NMR、DEPT、1H-1H COSY、HSQC、HMBC等),共分离鉴定了100个化合物,发现25个新化合物。 从多管藻中分离鉴定38个化合物 (24个溴酚化合物),其中7个新化合物 (均为溴酚化合物),包括1个菲并呋喃结构溴酚 (P1), 2个二氢菲结构溴酚 (P2, P3),1个含 5,7-dihydrodibenzo[c,e]oxepine 结构溴酚 (P4)和3个简单溴酚 (P5, P6, P7)。P1 (urceolatin) 属首例报道的具有菲并呋喃结构的天然产物,从该种中分离的化合物P12 和 P13 可能是其生源合成的前体。P2和P3为第二例报道的具有二氢菲结构的溴酚化合物。 从松节藻中分离并鉴定了62 个化合物,其中18 个为溴酚类新化合物,44 个为已知化合物。化合物具有多变的取代基团,包括2 个脲基吡咯烷酮溴酚化合物 (R1, R2), 4 个γ-脲基丁酸溴酚化合物 (R3-R6),5 个酰胺溴酚化合物 (R7, R8, R9, R13, R14),1 个溴酚砜化合物 (R12), 1 个Xanthene 溴酚化合物 (R10)和5 个简单溴酚化合物 (R11, R15, R16, R17, R18)。R1、R2 是首例报道的含有脲基吡咯烷酮片段的天然产物,R10 为首次报道的溴代Xanthene 类天然产物。 对分离到的化合物进行了清除DPPH 和ABTS两种自由基活性的筛选。结果发现溴酚类天然产物具有显著的DPPH自由基清除活性,其中R3 的IC50 仅为3.3 μM, 其活性强度约为阳性对照BHT (IC50 为82.1 μM) 的24倍。另外,溴酚类天然产物对ABTS自由基有较强的清除活性,R2 的TEAC(Trolox efficency activity capacity)值为5.2 mM,约为阳性对照 (ascorbic acid, 1.02 mM) 的 5 倍。初步的构效关系研究发现,稠环分子、多羟基和邻位甲氧基等结构特点能有效增强DPPH 自由基清除活性;特殊取代基如脲基、吡咯烷酮等含有氮原子的基团,能有效增强ABTS 自由基清除活性,多羟基、溴代等结构特点也使其活性有所增强。 本研究结果丰富了海藻卤代化合物的结构类型,为多管藻和松节藻的合理利用提供了一定的科学依据。