7 resultados para tanshinone IIB

em Chinese Academy of Sciences Institutional Repositories Grid Portal


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Stejnulxin, a novel snake C-type lectin-like protein with potent platelet activating activity, was purified and characterized from Trimeresurus stejnegeri venom. Under non-reducing conditions, it migrated on a SDS-polyacrylamide gel with an apparent molecular mass of 120 kDa. On reduction, it separated into three polypeptide subunits with apparent molecular masses of 16 kDa (alpha), 20 kDa (beta(1)) and 22 kDa (beta(2)), respectively. The complete amino acid sequences of its subunits were deduced from cloned cDNAs. The N-terminal sequencing and cDNA cloning indicated that beta(1) and beta(2) subunits of stejnulxin have identical amino acid sequences and each contains two N-glycosylation sites. Accordingly, the molecular mass difference between 1 and 2 is caused by glycosylation heterogenity. The subunit amino acid sequences of stejnulxin are similar to those of convulxin, with sequence identities of 52.6% and 66.4% for the U. and beta, respectively. Stejnulxin induced human platelet aggregation in a dose-dependent manner. Antibodies against UNA inhibited the aggregation response to stejnulxin, indicating that activation of alpha(IIb)beta(3) and binding of fibrinogen are involved in stejnulxin-induced platelet aggregation. Antibodies against GPIbalpha or alpha(2)beta(1) as well as echicetin or rhodocetin had no significant effect on stejnulxin-induced platelet aggregation. However, platelet activation induced by stejnulxin was blocked by anti-GPVI antibodies. In addition, stejnulxin induced a tyrosine phosphorylation profile in platelets that resembled that produced by convulxin. Biotinylated stejnulxin bound specifically to platelet membrane GPVI.

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Scutellarin was purified from the plant Erigeron breuiscapus (Vant.) Hand.-Mazz. The activity against 3 strains of human immunodeficiency virus (HIV) was determined in vitro in this study. These were laboratory-derived virus (HIV-I-IIIB), drug-resistant virus (HIV-I-74V), and low-passage clinical isolated virus (HIV-1(KM018)). From syncytia inhibition study, the EC50 of scutellarin against HIV-I-IIB direct infection in C8166 cells was 26 mu M with a therapeutic index of 36. When the mode of infection changed from acute infection to cell-to-cell infection, this compound became even more potent and the EC50 reduced to 15 mu M. This suggested that cell fusion might be affected by this compound. By comparing the inhibitory effects on p24 antigen, scutellarin was also found to be active against HIV-1(74V) (EC50 253 mu M) and HIV-1(KM018) (EC50 136 mu M) infection with significant difference in potency. The mechanism of its action was also explored in this study. At a concentration of 433 mu M, scutellarin inhibited 48% of the cell free recombinant HIV-1 RT activity. It also caused 82% inhibition of HIV-1 particle attachment and 45% inhibition of fusion at the concentrations of 54 mu M. In summary, scutellarin was found to inhibit several strains of HIV-1 replication with different potencies. It appeared to inhibit HIV-1 RT activity, HIV-1 particle attachment and cell fusion. These are essential activities for viral transmission and replication. (c) 2005 Elsevier Inc. All rights reserved.

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拓扑异构酶(topoisomerase)是一类控制和修改双螺旋DNA复制和转录过程中的拓扑结构的酶,是生命活动中最重要的酶。以IA类和II类拓扑异构酶中共存的toprim以及CAP-like结构域为研究对象,对拓扑异构酶中的三大类酶的分子进化情况进行了分析。结果显示在IA类和II类酶之间序列保守性很低,但是具有两个保守的结构域,在IIB类拓扑异构酶中toprim结构域中存在着和其他toprim结构域相同的四个保守位点,而在CAP-like结构域中IA类和II类中存在较大差异,没有明显的序列保守性,IIB类和IIA类的CAP-like结构域在二级结构上非常相似。从toprim结构域系统进化研究中我们发现IIA类和皿类中toprim结构域的进化关系很近,两类酶的toprim结构域在亲缘关系上和primase较远,而以上三者和IA类的进化关系最远。CAP-like结构域的系统进化研究发现IIA类以及IA类的domain4的CAP-like结构域进化关系比较近,IIB类和他们之间关系稍微远一些,IA类的domain3和以上几个结构域的关系较远,这也与他们的二级结构上的一致性是相同的。通过分析,IIA、IIB类起源于类似IA类的古老的拓扑异构酶,'在IA类进化中经过基因复制产生了两个不同的CAP-like结构域。然后祖先拓扑异构酶发生了变化,N'端加入了ATPase结构域和DNAgyrase/Mutlsecond结构域,形成了严格依赖ATP供能的真核生物IIA类,在细菌中断开成为两个亚基的细菌中IIA类。IIB类是祖先细胞的IIA类的一个或者是两个亚单位在古细菌以及真核生物中通过复制、重组和缺失造成的,IIB类中的toprim结构域很接近IIA类,可以认为,llB类中的toPrim结构域直接由IIA类转移而来,而IIB类中的cAP一1汰e结构域较IIA类中产生更早一些,应该是由拓扑异构酶祖先中产生的二级结构为aβaaββ的CAP-like结构域直接进化而来。然而,两个结构域的基因在连接到一起时候发生了不同于一般顺序的拼接,于是nB类中两个结构域形成了不同于现在的IA类和IIA类的顺序。

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Reaction of [Ph(4)P]2WS4 With NiCl2 in methanol solution in the presence of NaOCH3 leads to the formation of [Ph(4)P](2) [S2W(mu-S)(2)Ni(S-2)] (I) A Similar reaction between (NH4)(2)WS4 and NiCl2 under O-2 atmosphere in the presence of Ph(4)PCl or (n)Bu(4)NCl affords [Ph(4)P](2)([(S-2)W(O)(mu-S)(2)]Ni-2] (IIa) and [(n)Bu(4)N](2)([(S-2)W(O)(mu-S)(2)]Ni-2} (IIb) Under argon the same reaction gives [Ph(4)P](2)[Ni(WS4)(2)] (IIIa) and [(n)Bu(4)N](2)[Ni(WS4)(2)] (IIIb). [Ph(4)P](2)[Ni(WOS3)(2)] (IV) and [Ph(4)P](2)[Ni(WO2S2)(2)] (V) can be prepared from the reaction of [Ph(4)P]2WOS3 and [Ph(4)P]2WO2S2 with NiCl2. Treatment of (NH4)(2)WS4 with CuCl in the presence of PPh(3) in boiling pyridine produces W(mu-S)(4)Cu-2(PPh(3))(3) (VI), which can further react with excess PPh(3) to give W(mu-S)(4)Cu-2(PPh(3))(4) . py (VII). Complex I crystallizes in the space group P2(1)/n with the cell parameters: a = 20.049(4), b = 17.010(4), c = 14.311(7) Angstrom; beta = 110.24(3)degrees and Z = 4; R = 0.058 for 4267 independent reflections. The structural study confirms that complex I contains two terminal sulfide ligands, two bridging sulfide ligands, a side-on disulfide ligand, and a planar central W(mu-S)(2)Ni four membered ring. Complex VII crystallizes in the space group C2/c with the cell parameters: a = 26.436(8), b = 20.542(6), c = 19.095(8) Angstrom; beta = 125.00(3)degrees and Z = 4; R = 0.080 for 3802 independent reflections. The structural study reveals a perfect linear arrangement of the three metal atoms Cu-W-Cu.

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纳米材料的合成、结构功能特性及其应用的研究成为人们共同关注的前沿课题.CeO_2是一种廉价而用途极广的材料,如用于发光材料、催化剂、电子陶瓷等.细胞色素c是一种含血红素的金属蛋白质分子,通过对其电化学行为的研究,为认识生物体内的电子传递反应机理和能量转换提供有用信息,对于揭示生命现象的本质具有重大意义.细胞色素c在裸金电极上是极不可逆的,现已发现了加速其可逆反应的多种促进剂,对其电化学反应机理也进行了深入的讨论.本文用溶胶-凝胶法合成了CeO_2纳米晶;将CeO_2纳米晶修饰在金电极上研究了细胞色素c的电子传递反应,发现CeO_2纳米晶是一种良好的促进剂.1 样品的制备与测试称取一定量草酸铈(GR),用蒸馏水调成浆状,滴加浓HNO_3(GR)和H_2O_2(AR),完全溶解后加入柠檬酸(GR),于50~70℃时缓慢蒸发形成溶胶,继续加热有大量气泡产生,并有白色凝胶形成,体积膨胀,有大量棕色烟放出.将凝胶于120℃干燥12h,得到淡黄色干凝胶,将其在不同温度下进行热处理,即得到CeO_2纳米晶.用日本理学D/MAX-IIB型X射线衍射仪进行结构分析;用H-600型透射电子显微镜进行粒子形貌分析和大小测定;...

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本文以生烃性能、排烃量、排烃效率以及运移过程中石油的变化作为研究方向,以辽河油田大民屯凹陷下第三系生油岩为研究对象,探讨有关石油(天然气)生成和初次运移的一些重要理论问题,同时解决油田生产中遇到的一些实际问题。本文分为两个部分,第一部分着重研究生油岩的特征及生烃性能,第二部分重点研究了生油岩的非烃性能,所获得的主要成果概括如下。1.提出了大民屯凹陷下第三系III型生油岩无阶段连续生烃演化模式,根据此模式对大民屯凹陷“小而肥”的问题可以作出较一些合理的解释。2.建立了大民屯凹陷下第三系生油岩的排烃模式,此模式表明大民屯凹陷下第三系生油岩中液态烃的排出不是间歇式而是连续进行的。3.大民屯凹陷下第三系生油岩中IIb型生油岩的全油排烃效率为13.8-92.3%,III型生油岩的全油排烃效率为18.9-86.8%。研究表明生油岩的有机质丰度制约其排烃量,但并不制约其排烃效率,排烃量大的其排烃效率不一定大。对大民屯凹陷下第三系生油岩而言,多数情况下III型生油岩的排烃效率大于IIb型生油岩的排烃效率。4.在国内首次对烷烃单个化合物的热模拟排烃效率、围岩粒度及受热时间等因素对排出烃和残留烃组成的影响的进行了研究。根据烷烃单个化合物的排烃效率推断,原油可能是以富油流体的形式从油岩中运移出来的,即使如此排出油仍将发生组分分馏。围岩粒度对排出烃的组成有一定的影响。受热时间对于不同类型生油岩残留烃和排出烃烷烃组成的影响也有差异。由于影响残留烃和排出烃组成的因素较多,因此很难用一个模式来概括其变化规律,对具体的盆地和生油岩要做具体分析才能得出正确的认识。6.对比了残留烃和排出烃的五环三萜烷参数和甾烷参数,发现排烃作用对生物标志物的组成有相当大的影响,使目前所用的一些指示有机质来源和成熟度的甾、萜参数的适用范围受到了限制。这些分子有机地球化学参数在用作生油岩中有机质来源和成熟度指标时必须以生油岩未发生过排烃前提,而在用作运移研究指标时则必须以所研究的原油和生油岩处在相同的成熟度水平为前提,否则其地质意义就可能解释不清。