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苄基异喹啉类化合物具有较强的拮抗钙调素的活性,测定这类化合物HPLC参数LogK'作为疏水参数与抑制钙调素的活性进行相关分析,结果表明活性随化合物亲脂性的增大而升高,二者较符合抛物线关系。  相似文献   

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苄基异喹啉化合物是一类钙调素拮抗剂.对新合成的双苄基异喹啉化合物 D20对钙调素依赖的磷酸二酯酶的抑制作用进行了研究,IC50=5μmol/L,表明其拮抗作用大于三氟啦嗪,是强的拮抗剂.荧光分析表明,钙调素与化合物 D20的结合常数为2.64(μmol/L)-1,一个化合物 D20分子与两个钙调素分子结合,并显示了结合方向性及空间位阻影响.  相似文献   

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本文对双苄基异喹啉生物碱的化学反应作了总结.  相似文献   

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苄基异喹啉生物碱在木兰亚纲等植物类群中的分布   总被引:2,自引:0,他引:2  
  相似文献   

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 双苄基异喹啉类化合物拮抗钙调素(CaM),抑制CaM激活的环核苷酸磷酸二酯酶(PDE),研究表明:蝙蝠葛碱和小檗胺分子中12位羟墓被芳香基团酯化或醚化时,芳香基团的电子云分布状态变化能增加或降低分子的拮抗活性;取代基中的次甲基数增加可以增强分子的拮抗活性。分子非极性端引入含氮基团,化合物的拮抗活性较低。测试的化合物中,E_6D_(12)和D_(14)的拮抗CaM活性较强,IC_(50)分别为0.58μmol/L0.58μmol/L和0.53μmol/L。实验结果表明,分子的拮抗活性与分子非极性端的疏水性、电子云分布状态以及分子空间结构等多种结构性质相关。  相似文献   

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本文就1982年至1994年来双苄基异喹啉类生物碱(BBI)在植物资源,化学成分,生理活性等方面的研究作一简要概述。  相似文献   

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全球紫堇属Corydalis约400余种,广泛分布于北温带和非洲南部地区。在我国,该属多种物种作为民间用药具有上千年历史。紫堇属植物富含异喹啉生物碱,对该类成分通常以回流、超声加热、湿法超微粉碎法和酶解辅助技术等方法提取,并使用溶剂分离法、硅胶柱色谱法、反向填料柱色谱法、HPLC法、离子交换树脂法、高效逆流色谱法和活性引导技术等方法进行分离纯化法。紫堇属生物碱有效部位或单体成分都具有较强药理活性,现代药理学表明,该属所含生物碱类成分对心脑血管、抗肿瘤、镇痛、消炎、保肝和抗血小板凝集等均具有显著的药理作用。本文对已报道的紫堇属植物生物碱类成分的结构类型、特征、药理作用以及提取分离方法研究进行综述,为植物药用化学成分富集和安全用药提供借鉴。  相似文献   

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苄基异喹啉类化合物具有较强的拮抗钙调素(Calmodulin,Cam)的活性,测定这类化合物HPLC参数LogK′作为疏水参数与抑制钙调素的活性进行相关分析,结果表明活性随化合物亲脂性的增大而升高,二者较符合抛物线关系。  相似文献   

11.
本文研究了铝与钙调蛋白相互作用的荧光光谱。实验证明,Al~3与CaM的结合所引起的构象变化与Ca~(2+)与CaM结合所引起的构象变化既有相同之处,也有不同之处。Al~(3+)在CaM分子上的结合有特异性结合与非特异性结合两种情况。其特异性结合位点可能为2—3个。钙调蛋白的非竞争性拮抗剂酸枣仁皂甙A(JuA)可以继续抑制已被Al~(3+)部分抑制的PDE-CaM的活力。  相似文献   

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Bryophytes are the transitional forms from water habitants to terrestrials, however, there have been only a few works on their photosynthesis. It was the first time to study on photosynthetic fluorescence spectra and fluorescence kinetics of primitive and advanced species comparatively. Both the primitive and advanced ones had the same fluorescence spectra at room temperature, which contained two maximum emissions: F686-690 from the Photosystem II and F736-740 from the Photosystem I. And then, there were three maximum emissions in the fluorescence spectra at 77K :F687-689 and F697-699 from Photosystem II, and F723-734 from Photosystem I. The first two maximum emissions were the same for both the primitive and advanced species. According to the third maximum emission the bryophytes under study fell into two categories: The first one possessing the maximum emission around 725 nm, including Ditrichum flexicaule , Didymodon icmadophyllum , Didymodon rigidicaulis, Aloina obliquifolia, Plagiomnium confertidens and Marchantia polymorpha, which were primitive mosses and advanced liverwort. The second one possessing the maximum emission around 732nm, including Thuidium delicatulum , Pylaisia brotheri , Myuroclada maximowiczii , Taxiphyllum taxirameum, Gollania neckerella, Eurohypnum leptothallum, which were advanced mosses, and the primitive one Plagiomnium rostratum. The characteristics of fluorescence spectra implied that the Photosystem II was conservative and Photosystem I was changeable during bryophyte evolution. The primitive mosses possess mainly the PSI core complex (CPI) and then the advanced species contain both CPI and LHC-I. In analysis of photosynthetic fluorescence kinetics, Fv/(Fc+Fv) is a measure of the activity of the Photosystem II; Fv/Fm is dependent on efficiency of primary photoconversion in the Photosystem II; Fm/(Fo+Fv) is related to photosynthetic carbon assimilation; and Fd/Fs is a measure of the potential photosynthetic quantum conversion. The fluorescence kinetics of the bryophyte photosynthesis showed that the Photosystem II activity, the efficieiency of primary photoconversion in Photosystem II, the photosynthetic carbon assimilation and the efficiency of the potential photosynthetic quantum conversion in primitive species, such as Ditrichum flexicaule, Didymodon icmadophyllus, D. rigidicaulis, Plagiomnium rostratum and the liverwort Marchantia polymorpha, were lower than those in the advanced species, Myuroclada maximowiczii, Pylaisia brotheri , Gollania neckerella Taxiphyllum taxirameum , Thuidium delicatulum. However, the primitive Plagiomnium confertidens was of the high activities and efficiencies and the advanced Eurohypnum leptothallum was of low ones. It seemed that P. confertidens and E. leptothallum were an intermediatefrom the primitive to the advanced.  相似文献   

13.
By measuring the derivative absorption spectra of chloroplasts of different populations of Pinus armandi Franch., it was found that southern populations maintained higher absorption at 680 nm than at 670 nm, but some of the northern populations deviated the maximum absorption from 680 nm to 670 nm, which indicated that the activity of PS Ⅱ in some of the northern populations declined. Clear geographical differences also have been found in the positions of emission peaks of PS Ⅰ and PS Ⅱ in the fluorescence emission spectra at 77 K. Analysis of the fluorescence excitation spectra at 77 K revealed geographical changes in the absorption.status of Chl a. Besides, the experimental results indicated that the intact needles of Pinus armandi are not ideal materials to be used in detecting the geographical variation in photochemical reaction process because the presence of thicker coat, resin etc. can conceal the spectral differences in different populations.  相似文献   

14.
70年代就有报道从蛇毒中提纯NAD糖苷水解酶(NADase,E.C.3.2.2.5)和一些生物性质方面的研究.Huang等[1]从皖南尖吻蝮蛇毒中分离得到的NADase是由两个相同亚基组成,含糖33%,等电点为7.6.刘清亮等[2]研究了NADase的ESR谱,推知Cu2+离子至少与三个氮原子配位.本文主要研究多种?..  相似文献   

15.
大黄蒽醌衍生物是中药大黄的主要成份。该类衍生物与钙调素(calmo-dulin,CaM)依赖的磷酸二酯酶(PDE)的相互作用表明:它们可作用子钙调素。其中,大黄酸结合CaM并抑制CaM依赖的磷酸二酯酶(CaM-PDE);而大黄素、大黄酚和芦荟大黄素既刺激CaM-PDE的活力,又刺激PDE的基础活力,其作用机制尚待阐明;当有Ca~(2+)或无Ca~(2+)条件下测定时,大黄酸对PDE基础活力均无影响。表明:象其它的CaM拮抗剂一样,大黄酸能抑制钙调素依赖的PDE的活力。  相似文献   

16.
胰蛋白酶与ANS的相互作用   总被引:7,自引:0,他引:7  
利用荧光光谱法研究了在不同pH、压力及不同浓度的脲作用时荧光探针1,8-ANS(1-anilionnaphthalene-8-sulfonicacid)与胰蛋白酶的相互作用.发现在低pH时ANS可以结合到胰蛋白酶上,其中以pH2.0、3.0时结合最强.进一步的研究发现脲变性对胰蛋白酶结合ANS的能力有很大的影响:1.5mol/L的脲即可使得胰蛋白酶结合ANS的能力大大降低,但有趣的是即使高达4mol/L的脲对胰蛋白酶色氨酸残基荧光也无明显影响.另外,在pH猝变、脲变性、及逐渐改变压力时,胰蛋白酶色氨酸残基荧光和结合到胰蛋白酶分子上的ANS的荧光的变化大不相同.上述结果暗示胰蛋白酶的色氨酸残基所在的区域和其结合ANS的区域是两个不相同的区域.  相似文献   

17.
荧光法研究血清白蛋白与药物的结合作用   总被引:3,自引:0,他引:3  
本文应用荧光光谱法,观测了药物分子头孢菌素Ⅳ、异烟肼、维生素B_6和氟哌酸对白蛋白荧光的猝灭。由Lineweaver-Burk双倒数作图法,确定了药物与白蛋白作用的离解常数。并通过Forster偶极-偶极无辐射能量转移机理确定了药物分子氟哌酸在人血清白蛋白中与色氨酸残基之间的距离R为2.55nm,由这一距离确定了药物分子可能进入的区域和位置。  相似文献   

18.
鱼类染色体的荧光显带研究   总被引:9,自引:1,他引:9  
应用GC碱基特异性荧光染料色霉素A,辅以AT减基特异性荧光染料Hoechst33258,DAPI或喹吖因对鲤鱼,鲫鱼,大鳞副泥鳅和的有丝分裂染色体及黄鳝的有丝分裂和减数分裂染色体进行了荧光显带研究,结果发现,色霉素A3可以特异性地显示鱼类有丝分裂及减数分裂各个时期核仁组织区NORS的存在,Hoechst33258,DAPI或喹吖因则使这些区域(NORs)淡染,大鳞副泥鳞的染色体NORs 分布位置具有性别,根据实验结果,对有关鱼类染色体的荧光染色研究及其应用进行了讨论。  相似文献   

19.
The conformational change of hen egg-white lysozyme (EC 3.2.1.17) induced by the interaction with tri-N-acetyl-D-glucosamine were investigated by steady state and time-resolved fluorescence spectroscopy. To identify more clearly the conformation of hen egg-white lysozyme interacting with the ligand, the fluorescence decay kinetics of the lysozyme and its complex with the ligand were precisely measured at their full spectral regions. The spectral analysis based on the time-resolved studies showed that the binding of the ligand affected not only the Trp62 directly linked to the ligand but its influence was extended to the vicinity of Trp108 and further to the hydrophobic matrix box region. Near the binding site, the intramolecular distance between Trp108 and Glu35 was expanded or contracted depending on the pH of the buffer solution. On the other hand, the interaction of Trp28 and/or Trp111 with their surroundings was reduced by restriction of fluctuational motions at the hydrophobic matrix box region.  相似文献   

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