Toward the synthesis and biological screening of a cyclotetrapeptide from marine bacteria

The first synthesis of a naturally occurring tetrapeptide cyclo-(isoleucyl-prolyl-leucyl-alanyl) has been achieved using a solution-phase technique via coupling of dipeptide segments Boc-L-Pro-L-Leu-OH and L-Ala-L-Ile-OMe. Deprotection of the linear tetrapeptide unit and its subsequent cyclization gave a cyclopeptide, identical in all aspects to the naturally occurring compound. Bioactivity results indicated the antifungal and antihelmintic potential of the synthesized peptide against pathogenic dermatophytes and earthworms.     

温室番茄循环曝气地下滴灌土壤水分动态及耗水特性

为探求循环曝气地下滴灌对温室番茄土壤水分及耗水特性的影响规律,采用正交试验,研究了不同滴灌带埋深、曝气水平及灌水量对温室番茄土壤含水率、耗水量、产量及水分利用效率的影响.整个生育期内番茄耗水量呈先增大后减小的趋势,曝气处理番茄耗水量显著高于不曝气处理.相比于不曝气处理,曝气滴灌处理番茄产量提高10%,水分利用效率提升0.4%.15 cm滴灌带埋深、溶氧值30 mg/L以及75%ET₀灌水量处理的番茄产量和水分利用效率达到最大值,分别为64 951.3 kg/hm²和23.26 kg/(hm²·mm).结果表明,曝气处理对番茄产量、水分利用效率的影响具有统计学意义(P<0.05).曝气对于土壤含水率有一定影响,且曝气处理有助于番茄对水分的吸收.滴灌带埋深和灌水量交互作用对番茄产量的影响具有统计学意义(P<0.05),滴灌带埋深和曝气量交互作用对番茄产量的影响具有统计学意义(P<0.01),灌水量与滴灌带埋深、灌水量与曝气水平交互作用分别对番茄水分利用效率的影响具有统计学意义(P<0.01).     

土壤微生物产电信号评价芘污染毒性的研究

通过向土壤中加入葡萄糖促进微生物产电过程,研究了芘污染条件下土壤产电变化规律。利用双室微生物燃料电池(Microbial fuel cells,MFCs),实时、连续记录芘污染土壤产电电压。产电110 h后结束MFCs运行,采用循环伏安法检测芘对土壤微生物电化学活性的影响;结合PCR-DGGE及测序技术,分析芘对MFCs阳极表面细菌群落结构的影响。结果显示,MFCs产电电量随芘浓度增加显著降低。循环伏安检测显示芘降低了土壤微生物的电化学活性。DNA序列分析表明,阳极细菌与已报道的产电细菌高度相似,包括Sporolactobacillus、Clostridium、Enterobacter、Bacillus及Ethanoligenens。芘降低了Bacillus丰度。     

小型生物质燃气发动机燃烧稳定性试验

为探明生物质燃气各组分相对含量对发动机工作稳定性的影响,在一台小型火花点火发动机上进行了生物质燃气发动机循环变动试验研究,着重分析了理论空燃比与实际空燃比的比值理论空燃比与实际空燃比的比值、H2含量(H2在CH4-H2中的体积分数)及CO2含量(CO2在CH4-H2-CO2中的体积分数)的变化对燃烧稳定性的影响。试验结果表明,燃料组分对燃烧稳定性有较大影响。在本试验中,当理论空燃比与实际空燃比的比值较小、燃料组分中H2含量较低时(如理论空燃比与实际空燃比的比值为0.4、H2的体积分数为25%及理论空燃比与实际空燃比的比值为0.6、H2的体积分数为17%),CO2含量对燃烧稳定性起支配作用,CO2含量的增加导致循环变动增加(上述工况的平均指示压力循环变动系数均超过了10%),在个别条件下导致部分燃烧。随着理论空燃比与实际空燃比的比值及H2含量的增加,CO2含量对燃烧的影响作用逐渐减弱,当理论空燃比与实际空燃比的比值及H2含量达到一定程度时(理论空燃比与实际空燃比的比值为0.6、H2的体积分数为33%及50%,以及理论空燃比与实际空燃比的比值为0.8所对应的所有H2含量条件)CO2含量对燃烧的影响作用已不明显。通过改变燃料组分条件的方法,能够提高生物质燃气发动机的工作稳定性。该研究的成果对生物质燃气发动机燃烧稳定性、经济性及排放特性改善,以及生物质燃气发动机技术应用、推广均有重要指导意义。     

Characterizing the Anti-HIV Activity of Papuamide A

Papuamide A is representative of a class of marine derived cyclic depsipeptides, reported to have cytoprotective activity against HIV-1 in vitro. We show here that papuamide A acts as an entry inhibitor, preventing human immunodeficiency virus infection of host cells and that this inhibition is not specific to R5 or X4 tropic virus. This inhibition of viral entry was determined to not be due to papuamide A binding to CD4 or HIV gp120, the two proteins involved in the cell-virus recognition and binding. Furthermore, papuamide A was able to inhibit HIV pseudotype viruses expressing envelope glycoproteins from vesicular stomatitis virus or amphotropic murine leukemia virus indicating the mechanism of viral entry inhibition is not HIV-1 envelope glycoprotein specific. Time delayed addition studies with the pseudotyped viruses show that papuamide A inhibits viral infection only at the initial stage of the viral life cycle. Additionally, pretreatment studies revealed that the virus, and not the cell, is the target of papuamide A’s action. Together, these results suggest a direct virucidal mechanism of HIV-1 inhibition by papuamide A. We also demonstrate here that the other papuamides (B-D) are able to inhibit viral entry indicating that the free amino moiety of 2,3-diaminobutanoic acid residue is not required for the virucidal activity.     

浙北平原创新发展农业循环经济模式选择和对策

嘉兴地处浙北水网平原,其农耕历史悠久,传统农业发达,农业废弃物资源十分丰富,开发利用潜力巨大。在当前建设现代都市型农业发展中,面对资源环境的制约,如何利用农业废弃物资源和治理农业面源污染任务艰巨。为此,应创新农业废弃物资源化利用方式,构建多种循环农业新模式,建设生态高效农业,形成低能耗、低排放、能循环、高效率的多元化循环农业发展模式,不断开发农业循环经济新产业。本文提出了创新发展农业循环经济的几种主要典型模式,并对如何发展农业循环经济新产业提出了自己的见解。     

Lyngbyastatins 8–10, Elastase Inhibitors with Cyclic Depsipeptide Scaffolds Isolated from the Marine Cyanobacterium Lyngbya semiplena

Investigation of an extract from the marine cyanobacterium Lyngbya semiplena, collected in Tumon Bay, Guam, led to the identification of three new cyclodepsipeptides, lyngbyastatins 8–10 (1–3). The structures of 1–3 were determined by NMR, MS, ESIMS fragmentation and chemical degradation. Compounds 1–3 are closely related to lyngbyastatins 4–7. Like the latter compounds, we found 1–3 to inhibit porcine pancreatic elastase, with IC₅₀ values of 123 nM, 210 nM and 120 nM, respectively.     

湖北省循环农业发展状况评价与政策建议

本文运用层次分析法,从经济与社会发展、资源减量投入、资源循环利用、资源环境安全4个方面,构建出评价湖北循环农业发展的评价指标体系.在此基础上,采用加权函数法及聚类分析法,对2005年湖北13个主要地级市的循环农业发展状况进行了综合评价,并按照各地级市的循环农业发水平,将其分别归类到中下等水平、中等水平、良好水平3个等级中;继而通过计算各指标制约度Bi,分析了13个主要地级市循环农业发展的限制因素,发现不同地区限制循环农业发展的因素存在较大差异,并据此提出了相应的政策建议.     

利尿剂乙酰唑胺在玻碳电极上的伏安行为

在Britton-Robinson(B-R)缓冲液中,用循环伏安法(CV)、线性扫描伏安法(LSV)和微分脉冲伏安法(DPV)研究了利尿剂乙酰唑胺在玻碳电极(GCE)上的伏安行为.结果表明,在pH6.0的B-R缓冲液中,乙酰唑胺在+1.32 V(vs.SCE)电位处产生一个DPV阳极氧化峰,氧化峰电流与乙酰唑胺浓度在3.00-54.0μmol.L-1范围内呈良好的线性关系,最低检测限为0.450μmol.L-1,从而建立了DPV法定量测定乙酰唑胺的新方法.并初步研究了乙酰唑胺的电化学反应机理.     

Anthelmintic Actions of the Cyclic Depsipeptide PF1022A and its Electrophysiological Effects on Muscle Cells of Ascaris suum

The cyclic depsipeptide PF1022A, given orally to mice, showed very good anthelmintic activity against Heligmosomoides polygyrus and Heterakis spumosa at 50 mg kg⁻¹. In vitro, PF1022A was very active against Trichinella spiralis and had good activity against Nippostrongylus brasiliensis at 1 μg ml⁻¹. An 18-membered enniatin analogue, JES 1798, showed good activity only against N. brasiliensis at 10 μg ml⁻¹. The optical antipode of PF1022A had poor activity even at 100 μg ml⁻¹. The effects of PF1022A on the membrane potential and input conductance of somatic muscle of Ascaris suum were examined using a two-microelectrode current-clamp technique. PF1022A did not antagonize the effects of the selective nicotinic agonist levamisole. PF1022A and an analogue, JES 1798, but not the PF1022A antipode, produced a small time-dependent increase in input conductance associated with no potential change. The increase in input conductance did not occur in the Cl⁻-free bathing solution, suggesting that the increase in input conductance was mediated by Cl⁻ ions. The addition of high concentrations of Ca²⁺ to the preparation after the addition of PF1022A did not lead to production of Ca²⁺-activated Cl⁻ channels, suggesting that its mode of action was not that of a Ca²⁺ ionophore. The mechanism by which the cyclic depsipeptide might increase the Cl⁻ conductance is discussed.