槐花提取化合物K3体外抗HIV-1活性的研究

目的:研究槐花提取化合物K3的体外抗HIV-1活性,并对其抗HIV-1机制进行初步探讨.方法:采用MTT比色法检测化合物对各种细胞的毒性.用合胞体形成计数法,p24抗原捕获ELISA法及RT-PCR等多种方法研究化合物体外抗HIV-1活性.结论:槐花提取化合物K3体外有较好的抗HIV-1活性,能够抑制病毒实验株(HIV-1ⅢB,耐药株(HIV-1 74v)和临床分离株(HIV-1KM018)等多种病毒株的复制,且其作用机制是多靶点的,不仅可以抑制病毒的进入,还可以抑制HIV-1逆转录酶活性.

灯盏花乙素和槐花化合物K3 体外抗HIV-1 活性研究

由于目前抗HIV 药物价格昂贵且有较强的毒副作用，传统药物将成为未来 HIV 治疗的主流药物。许多植物来源的天然化合物体外具有较好的抗HIV 活性， 有些化合物甚至可以作用在病毒复制周期的不同阶段。HIV 侵入抑制剂目前成 为抗HIV 药物研发的热点。HIV 侵入抑制剂靶定在病毒复制周期的结合或融合 位点，对临床中已产生耐药性突变的病毒株也有较好的抑制作用。该类抑制剂 的出现将为HARRT 疗法提供更多新的药物组合。开发新一代的HIV-1 侵入抑制 剂，与逆转录酶或蛋白酶抑制剂联合使用将增加治疗的有效性并减少毒副作用 的产生。 灯盏花乙素（Scutellarin）与槐花化合物K3 均从天然植物资源中提取，且 前者在我国临床上一直有着广泛应用。我们对这两种化合物的抗HIV-1 活性进 行了研究，检测了其对实验室适应病毒株（HIV-1ⅢB）、耐药株（HIV-174V）和临 床分离病毒株（HIV-1KM018）的抑制活性。灯盏花乙素是从植物滇黄芩中分离出 来的具有多种生物活性的黄酮类化合物，该化合物抑制HIV-1ⅢB 诱导C8166 细 胞合胞体形成的EC50 为26μM，选择指数为36。灯盏花乙素对耐药病毒株和临 床分离株也表现出良好的抑制作用。从槐花中提取的硫酸酯类化合物K3 体外研 究证实也有很好的抗HIV-1 活性，它不仅可以抑制HIV-1 致细胞病变效应，也 可以抑制感染细胞中的HIV-1 特异性抗原表达，该化合物的半数有效抑制浓度 EC50 为5～54μM。 灯盏花乙素与槐花化合物K3 的抗HIV-1 机制研究结果表明：两种化合物均 能有效抑制病毒进入细胞。灯盏花乙素在54μM 时抑制45%的病毒粒子进入细 胞，槐花化合物K3 在40μM 时能够有效抑制56％的HIV-1 进入细胞；灯盏花乙 素与槐花化合物K3 也可以抑制C8166 细胞与慢性感染的H9/HIV-1ⅢB 细胞间的融合，灯盏花乙素的EC50 为15μM，而槐花化合物K3 的EC50 为5μM；两种化 合物对体外重组的HIV-1 逆转录酶有微弱的抑制作用，在433μM 时，灯盏花乙 素可以抑制48％的逆转录酶活性，槐花化合物K3 在300μM 时能够抑制80％的 HIV-1 逆转录酶活性；这两种化合物体外对HIV-1 均无直接杀伤作用，也不能抑 制慢性感染细胞中的病毒复制和HIV-1 蛋白酶活性。因此，灯盏花乙素与槐花 化合物K3 的体外抗HIV-1 作用机制主要源于其能够抑制HIV-1 RT 活性和阻止 HIV-1 进入细胞。 灯盏花乙素和槐花化合物K3的有效抗病毒活性和多种作用途径使其成为具 有发展潜力的抗病毒先导化合物。

Higher-order analysis of crack-tip fields in power-law hardening materials

In this paper, we present an exact higher-order asymptotic analysis on the near-crack-tip fields in elastic-plastic materials under plane strain, Mode I. A four- or five-term asymptotic series of the solutions is derived. It is found that when 1.6 < n less-than-or-equal-to 2.8 (here, n is the hardening exponent), the elastic effect enters the third-order stress field; but when 2.8< n less-than-or-equal-to 3.7 this effect turns to enter the fourth-order field, with the fifth-order field independent. Moreover, if n>3.7, the elasticity only affects the fields whose order is higher than 4. In this case, the fourth-order field remains independent. Our investigation also shows that as long as n is larger than 1.6, the third-order field is always not independent, whose amplitude coefficient K3 depends either on K1 or on both K1 and K2 (K1 and K2 arc the amplitude coefficients of the first- and second-order fields, respectively). Firmly, good agreement is found between our results and O'Dowd and Shih's numerical ones[8] by comparison.

治疗艾滋病的药物组合物,其制备方法及其用途

本发明提供一种治疗艾滋病的药物组合物，其中含有治疗艾滋病有效量的式(I)化合物联苯环辛二烯类木脂素(+)-戈米辛 K3[(+)-gomisin K3]及可药用载体和/或赋形剂。该药物组合物通过抑制逆转录酶和蛋白酶活性的作用机制，从而达到抑制HIV-1病毒的增殖。本发明同时给出了该药物组合物的制备方法，及其在制备逆转录酶抑制剂药物和在制备抗艾滋病药物中的应用。

Anti2HIV Lignans from Schisandra micrantha

　目的:从小花五味子中发现具有抗HIV 活性的化学成分。方法:采用多种柱层析分离进行化合物的分离 和纯化,通过波谱分析鉴定化合物的结构,化合物的抗HIV21 活性通过对HIV21 感染C8166 细胞致细胞病变的抑制试验得 到。结果:从小花五味子的茎藤部分分离得到了4 个木脂素,分别鉴定为micrantherin A (1) , gomisin K3 (2) , gomisin G (3) 和 vladinol F (4) 。化合物4 具有显著的抗HIV21 活性,IC50 = 3151μg/ mL ,选择指数为27145。结论:化合物1 为新的木脂素, 化合物4 的抗HIV21 活性值得进一步研究。

农杆菌介导的单子叶植物早熟禾的转化(英文)

利用种子和胚分别在两种培养基K3和K5诱导产生了早熟禾(Poa pratensis L.)一个品种Mado的胚性愈伤组织。K3培养基含有10.0μmol/L的二氯苯氧乙酸(2,4-D)、0.5μmol/L的苄氨基嘌呤(BAP)。K5培养基是K3另加0.5μmol/L的硫酸铜。光照条件为20～30μmol·m~(-2)·s~(-1)、16h光照、8h黑暗。温度保持在24℃。用携有bar基因和gus基因的pDM805质粒转化的农杆菌AGL1对胚性愈伤组织进行转化。共得到4个转基因株系。影响转基因效率的主要因素

Agrobacterium-mediated transformation of Kentucky bluegrass

Embryogenic calli of Kentucky bluegrass, named Md, were induced from mature seeds and embryos, and proliferated on medium K3 containing 2,4-dichlorophenoxyacetic acid (2,4-D, 10.0 mumol/L), 6-benzylaminopurine (BAR, 0.5 mumol/L) and K5 which was the K3 medium supplemented with cupric sulfa (0.5 mumol/L) under dim-light condition (20-30 mumol.m(-2).s-1, 16 h light) at 24 degreesC. Embryogenic calli were transformed with plasmids pDM805 Carring bar and gus genes, Which was mediated by an Agrobacterium strain AGL1, four transgenic lines were obtained. The important factors that affect the transformation efficiency and obtain desirable number of transgenic plants included: (1) the quality of embryogenic calli; (2) light condition and time of co-cultivation; (3) concentration of antibiotics used for suppressing the overgrowth of Agrobacterium in the course of transformed plant regeneration; (4) selection pressure, etc. The micro nutrient of cupric had significant influence on the quality of embryogenic calli. This presentation is the first successful protocol of Kentucky bluegrass transformation mediated by Agrobacterium.

黄土高原南瓜高糖低硝酸盐施肥模式研究

采用N、P、K3因素最优设计,在陕北黄土高原进行了南瓜氮、磷、钾用量及其肥效反应模式田间试验,研究不同施肥量对南瓜硝态氮、可溶性糖两项营养品质的影响,旨在探讨南瓜品质高糖低硝酸盐的N、P、K肥效反应模式,提出优化的施肥方案。结果表明,N肥单因素对南瓜硝态氮和可溶性糖含量影响最大,K肥单因素对南瓜硝态氮和可溶性糖含量影响不显著,N与P交互作用对南瓜高糖低硝酸盐影响显著,K肥施用量一定时,氮肥与磷肥的施用量不易过大。根据南瓜N、P、K肥效反应模式,筛选出南瓜品质硝态氮含量在200mg·kg-1以下、可溶性糖含量在7%以上的较佳施肥量为施氮95～120 kg·hm-2,施磷40～70 kg·hm-2,施钾35～80 kg·hm-2,N∶P2O5∶K2O=1∶0.42∶0.37。

贵金属（Au, Ag, Pt, Pd）纳米材料的可控合成及性能研究

功能化的贵金属纳米材料的设计和可控制备在材料科学研究领域引起了人们广泛的关注。贵金属纳米材料的光学、电学、磁学和催化等物理和化学性质不但与其大小有关，而且还与其形貌息息相关。因此寻求简单而有效的低温溶液合成途径以实现对贵金属纳米材料的尺寸和形貌控制尤为重要。本论文的主要研究内容可以归纳如下： (1)在水溶液中利用种子生长方法分别制备了核壳Au-Pd/Pt三金属复合纳米粒子和三层的核壳AuAg复合纳米粒子。这些纳米粒子的尺寸和组成可以通过改变金种子的加入量来加以调控。 (2)通过种子生长和取代沉积相结合的方法制备了具有金核铂/银双金属壳的铃铛状纳米粒子。通过扫描电子显微镜、透射电子显微镜和X-射线光电子能谱对所得纳米粒子的尺寸、结构和组成进行了表征。 (3)以二肽甘氨酰甘氨酸作为模板合成了具有[111]取向的单晶银纳米片。通过改变实验条件探讨了片状银纳米结构的形成机理。片状银纳米结构的产率可达到80%，反应物之间的摩尔比对产物的尺寸和形貌有至关重要的作用。 (4)将K3[Fe(CN)6]和Na2S2O3的混合溶液进行水热处理，得到了具有立方体形貌的FeIIIFeIII(CN)6（柏林绿）微晶。实验结果显示K3[Fe(CN)6]和Na2S2O3的摩尔比及其浓度对所得产物的尺寸、形貌和组成有决定性的作用。 (5)在室温下通过混合3, 3', 5, 5'-四甲基联苯胺和氯铂酸，成功合成了有机-无机杂化的纳米纤维。纳米纤维的尺寸和形状可以通过改变反应物的比和浓度加以控制。基于不同的实验结果，提出了纳米纤维的可能形成机理。

Voltammetric study of vitamin K-3 at interdigitated array microelectrodes

Cyclic voltammetry of Vitamin K-3 (V-K3) was measured with Pt disk electrode, platinum interdigitated array (Pt-IDA) and Au-IDA microelectrodes in single and dual modes. The effects of pH, scan rate and collector potential on the current of generator and collector were studied. The collection efficiency of V-K3 at IDA electrodes was measured. The linear ranges for current response as a function of V-K3 concentration were found to he 10 mu M-1 mM (i(g)) and 1 mu M - 1 mM (i(c)) for the generator and collector of the Pt-IDA electrode, respectively. The effects of waiting time, potential difference and pulse electrolysis time in differential pulse voltammetry (DPV) on the peak current of V-K3 were studied to get the optimal condition at 0.1 M Na2HPO4, pH 11.50 and 11.0 for Au-IDA and Pt-IDA, respectively.

去甲肾上腺素电极过程的圆二色谱电化学研究

现场圆二色薄层光谱电化学研究去甲肾上腺素的电化学氧化还原过程 .研究表明去甲肾上腺素 ( pH =7.0磷酸缓冲溶液中 )在玻碳电极上经历了不可逆的电化学氧化 ,且遵从后行化学反应 (EC)机理 ,去甲肾上腺素醌和去甲肾上腺素红的再还原遵从简单电子转移 (E)机理 .由双对数法获得去甲肾上腺素电化学氧化的式电位为E10’=0 .2 0V ,电子转移系数和电子转移数之积为αn =0 .38,标准复相电极反应常数k10 =1 .2× 1 0 -4 cm·s-1.去甲肾上腺素醌和去甲肾上腺素红的电化学还原反应参数分别为E2 0’=0 .2 5V ,αn =0 .37,k2 0 =4.4× 1 0 -5 cm·s-1和E3 0’=- 0 .2 5V ,αn =0 .33,k3 0 =1 .1× 1 0 -4 cm·s-1.

中国黄土的磁组构特征及其古风向指示意义

The transportation and deposition of eolian materials of Chinese loess is correlated and effected by the monsoon from the mid-high latitude. Therefore study of the winter monsoon evolution can help us to understand the dynamic mechanism to climate changes in the east-Asian areas. The anisotropy of magnetic susceptibility (AMS) measurements have been carried out on the samples from the last 250ka wind -blown loess-paleosol sequences at Baicaoyuan and Luochuan. And the main conclusions are following:The magnetic foliation is almost horizontal of the two sections. AMS canthus be represented by an oblate ellipsoid with average K3 perpendicular to thebedding plane and Ki within the bedding plane. It has also shown that the ^-factor isless than 0.5 of the majority of samples. So the two sections are normal magneticfabric for sediments.The degree of anisotropy always shows a strong correlation with the foliationrather than with lineation, therefore the anisotropy is controlled by the foliation.Furthermore the foliation is nearly less than 1.02 and shows the typical wind-blownsediments anisotropy.The intensity of winter monsoon, grain size of the eolian inputs, the foliationand the degree of anisotropy are somewhat inter-related. Generally, the higherintensity of the winter monsoon will carry coarser-grained eolian material, therebyresulting in a larger foliation during deposition. Also the post-depositional compactioncontributes to the anisotropy.The AMS features between loess and paleosol are somewhat different. Wefound that the F, P values of paleosol are lower than that of its parent loess respectively. Moreover, the difference does also exists between the two sections. The anisotropy of Baicaoyuan is more significant than Luochuan section, which maybe related with the location and the intensity of the post-deposition reworks.5. We note that the declination of the long axis is NWW in Baicaoyuan section and the observed NWW direction of the winter monsoon winds based on AMS is consistent with the view that the winter monsoons prevail along the NW-SE direction. But at the Luochuan section, because of the strong affection of the post-deposition reworks, the direction of the long axis is nearly random in the foliation and hardly recognizes the paleowind direction since the last two interglacials.Correlation between the two loess-paleosol sequences implies that it is available in arid or semi-arid areas to take AMS to recognize the paleowind directions on the Loess Plateau.