The Evidence for Effective Inhibition of INa Produced by Mirogabalin ((1R,5S,6S)-6-(aminomethyl)-3-ethyl-bicyclo [3.2.0] hept-3-ene-6-acetic acid), a Known Blocker of CaV Channels

Mirogabalin (MGB, Tarlige^®), an inhibitor of the α₂δ-1 subunit of voltage-gated Ca²⁺ (Ca_V) channels, is used as a way to alleviate peripheral neuropathic pain and diabetic neuropathy. However, to what extent MGB modifies the magnitude, gating, and/or hysteresis of various types of plasmalemmal ionic currents remains largely unexplored. In pituitary tumor (GH₃) cells, we found that MGB was effective at suppressing the peak (transient, I_Na(T)) and sustained (late, I_Na(L)) components of the voltage-gated Na⁺ current (I_Na) in a concentration-dependent manner, with an effective IC₅₀ of 19.5 and 7.3 μM, respectively, while the K_D value calculated on the basis of minimum reaction scheme was 8.2 μM. The recovery of I_Na(T) inactivation slowed in the presence of MGB, although the overall current–voltage relation of I_Na(T) was unaltered; however, there was a leftward shift in the inactivation curve of the current. The magnitude of the window (I_Na(W)) or resurgent I_Na (I_Na(R)) evoked by the respective ascending or descending ramp pulse (V_ramp) was reduced during cell exposure to MGB. MGB-induced attenuation in I_Na(W) or I_Na(R) was reversed by the further addition of tefluthrin, a pyrethroid insecticide known to stimulate I_Na. MGB also effectively lessened the strength of voltage-dependent hysteresis of persistent I_Na in response to the isosceles triangular V_ramp. The cumulative inhibition of I_Na(T), evoked by pulse train stimulation, was enhanced in its presence. Taken together, in addition to the inhibition of Ca_V channels, the Na_V channel attenuation produced by MGB might have an impact in its analgesic effects occurring in vivo.     

分子生物学技术在土壤生物修复中的应用及展望

综述了分子生物学技术包括环境微生物群落降解基因分析、16S rRNA序列分析技术以及荧光原位杂交技术在生物修复技术中跟踪污染土壤中降解微生物行为、监测降解基因和微生物群落变化,揭示了其中的分子机制的应用现状,对各项技术应用中需要注意的问题进行了讨论并对其发展前景进行了展望。     

一种磁控管用扼流线圈仿真设计

采用电路仿真软件仿真滤波组件S参数曲线,观察曲线随器件参数的变化;介绍利用三维全波电磁仿真软件HFSS简化设计流程的方法,并与测试结果对比.结果 表明:利用3D仿真软件在满足器件设计精度的同时可以简化线圈的设计流程.     

3-(S)-(-)-(1-氨甲酰基-1,1-二苯基甲基)吡咯烷的制备

3-(S)-(-)-1-氨甲酰基-1,1-二苯基甲基)吡咯烷是合成抗尿失禁药物达非那新的重要中间体。它由3-(S)-( )-3-羟基吡咯烷盐酸盐经磺酰化和烷基化反应得到3-(S)-( )-(1-氰基-1,1-二苯基甲基)-1-甲苯磺酰基吡咯烷,再经过去磺酰化和水解4步反应制得,总产率为5.1%。     

Role of the Ubiquitin System in Stress Granule Metabolism

Eukaryotic cells react to various stress conditions with the rapid formation of membrane-less organelles called stress granules (SGs). SGs form by multivalent interactions between RNAs and RNA-binding proteins and are believed to protect stalled translation initiation complexes from stress-induced degradation. SGs contain hundreds of different mRNAs and proteins, and their assembly and disassembly are tightly controlled by post-translational modifications. The ubiquitin system, which mediates the covalent modification of target proteins with the small protein ubiquitin (‘ubiquitylation’), has been implicated in different aspects of SG metabolism, but specific functions in SG turnover have only recently emerged. Here, we summarize the evidence for the presence of ubiquitylated proteins at SGs, review the functions of different components of the ubiquitin system in SG formation and clearance, and discuss the link between perturbed SG clearance and the pathogenesis of neurodegenerative disorders. We conclude that the ubiquitin system plays an important, medically relevant role in SG biology.     

一株产胞外多糖植物内生菌EJS-3菌株的分离和鉴定

从中药植物-百部的组织中分离到一株高产胞外多糖的植物内生菌EJS-3菌株,该菌株在产糖培养基中可以得到23.6g/L的胞外多糖,转化率为47.2%(gEPS/g蔗糖)。通过16SrRNA基因序列分析对该菌株进行了鉴定。通过PCR扩增,得到1450bp的16SrRNA序列。PCR产物序列通过BLAST软件在NCBI网站中进行同源性比较。通过Bioedit7.0和Treedrawing软件绘制系统发育树。结果显示,EJS-3的16SrRNA序列和数据库中的类多粘芽孢杆菌KCTC1663菌株的序列的同源性为99.31%。在细菌系统发育分类学上,EJS-3菌株归属多粘类芽孢杆菌(Paenibacilluspolymyxa)。     

酶法合成阿托伐他汀侧链中间体（S）-4-氯-3-羟基丁酸乙酯的研究进展

第三代羟甲戊二酰辅酶A （HMG-CoA）还原酶抑制剂——阿托伐他汀是年销售额超过百亿的重磅降血脂药物,因其疗效显著而广受医生患者好评.阿托伐他汀主要通过疏水性母核及手性侧链进行合成,而手性侧链的制备是合成关键.目前,生物催化技术在手性药物合成中的应用备受关注,而阿托伐他汀手性侧链中间体（S）-4-氯-3-羟基丁酸乙酯的酶法合成也成为研究热点.本文主要介绍近年酶法合成在（S）-4-氯-3-羟基丁酸乙酯中的研究进展.     

SSR标记辅助回交转育大豆7S球蛋白α-亚基致敏蛋白缺失新品系

为快速培育7S球蛋白致敏蛋白α-亚基缺失的优质大豆新品系,以（α＇＋α）-亚基双缺失型材料日B为供体亲本,东农47为受体亲本,以杂交一回交转育方法为基础,结合SSR标记辅助遗传背景选择与主要农艺性状鉴定及品质分析,在BC2F4选育到7S球蛋白α-亚基缺失新品系Cb80。Cb80综合农艺性状优良,遗传背景回复率大于90％,其蛋白质及氨基酸总量为44．1％、41．95％,分别比轮回亲本东农47提高3．5和3．76个百分点。     

草鸡煲中腐败菌的分离鉴定

为了采取针对性措施控制草鸡煲中的微生物污染,采用平板划线分离方法对草鸡煲中的主要微生物菌群进行分离,再根据菌落形态、菌体形态、生理生化实验以及16S rDNA序列分析对菌株进行鉴定。结果表明,引起草鸡煲腐败变质的主要菌群有产气肠杆菌、成团泛生菌、假单胞菌、荧光假单胞菌、蜡状芽孢杆菌、类芽孢杆菌。     

Detection of cauliflower mosaic virus by the polymerase chain reaction: testing of food components for false-positive 35S-promoter screening results

 Today DNA-based techniques are very common for the detection of genetically modified organisms (GMOs) in food products. For fast and easy detection of GMOs, polymerase chain reaction (PCR) screening methods, which amplify common transgenic elements, are applied in routine analysis. These techniques do not allow differentiation between GMOs and the natural occurrence of transgenic elements, such as the 35S-promoter of cauliflower mosaic virus (CaMV) or the NOS-terminator of Agrobacterium tumefaciens, and thus may result in false-positive detection of GMOs. In this study we evaluated three different existing 35S screening systems and report the development of two new CaMV-specific PCR systems. These PCR systems based on CaMV-specific genes allow the identification of positively screened 35S food samples as naturally virus-infected products or plants. Seven food samples tested positive in routine 35S screening analysis and negative in GMO specific systems were investigated using the new virus-specific PCR systems. In all seven samples CaMV was detected. Received: 26 April 1999 / Revised version: 28 June 1999