Synthesis and Anthelmintic Activity of 7-Hydroxy- 5-oxo-5H-thieno[3,2-b]pyran-6-carboxanilides and -6-thiocarboxanilides

7-Hydroxy-5-oxo-5H-thieno[3,2-b]pyran-6-carboxanilides and -6-thio-carboxanilides represent a novel series of anthelmintic compounds, with broad-spectrum activity against important parasitic nematodes in sheep and dogs. In particular, an improved efficacy against Trichostrongylus colubriformis in sheep over the related 3-carbamoyl-4-hydroxycoumarins has been noted. New synthetic routes to the key intermediate, 7-hydroxythieno[3,2-b]pyran-5-one, have been developed.     

Binding Sites for Ca2+-Channel Effectors and Ryanodine in Periplaneta americana—Possible Targets for New Insecticides

The calcium channel and the ‘calcium release channel’ of muscle membrane of the cockroach Periplaneta americana have been characterized. Biological assays with calcium channel blockers and ryanodine on different insects and acari revealed pronounced insecticidal effects with ryanodine, but not with calcium channel blockers, at concentrations between 0·1 and 300 μg ml⁻¹. Skeletal muscle membranes derived either from the tubular network or from the sarcoplasmatic reticulum of P. americana were characterized with respect to the binding of the dihydropyridine (DHP) [³H]isradipine (PN 200-110), the phenyl-alkylamine [³H]verapamil and the alkaloid [³H]ryanodine. Preliminary binding studies with the benzothiazepine [³H]diltiazem suggest a low-affinity binding site with a IC₅₀ value of 3·3 μM . All binding sites tested were sensitive to treatment with proteinase K. Optimal conditions for binding of the radioligand ryanodine revealed the highest specific binding at pH 8 and at calcium chloride concentrations between 100 and 500 μM . EGTA at 10 μM abolished 95% of the ryanodine binding. Binding studies with calcium channel binding sites revealed a pronounced effect of low Ca²⁺ concentrations on specific isradipine binding, whereas verapamil and diltiazem binding were only reduced by the presence of 200 μM EGTA. With respect to high Ca²⁺ concentrations, specific binding of diltiazem, isradipine and verapamil was reduced by 73, 40 and 20%, respectively, at 5 mM Ca²⁺. Radioligand binding experiments showed high-affinity binding sites for ryanodine and isradipine. K_D values of 0·95 nM (B_max=550 fmol mg⁻¹ protein) and 0·75 nM (B_max=213 fmol mg⁻¹ protein) were determined respectively. A lower-affinity binding site was identified in binding studies with verapamil (K_D=7·4 nM and B_max=27 fmol mg⁻¹ protein). [³H]isradipine displacement studies with several dihydropyridines revealed the following ranking of affinity: nitrendipine>isradipine>Bay K8664≪nicardipine. Displacement of [³H]verapamil binding by effectors of the phenylalkylamine binding site showed that bepridil and S(-)verapamil had the highest affinities of the compounds tested followed by (±)verapamil, nor-methylverapamil and R(+)verapamil.     

基于IPV6协议重构校园网的研究

为适应我国对第二代教育与科研网的建设,对互联网的IPV6协议进行了深入探讨,并在分析校园网的实际需求基础上提出了相应的解决方案,为校园网的重构提出了指导性的方法。     

黄芪多糖对大肠埃希菌侵入肠上皮细胞的保护研究

采用CaCo2细胞单层肠上皮系统感染模型,将5×10-5mmol/L,1×10-4mmol/L和2×10-4mmol/L 3种不同浓度的黄芪多糖及不含黄芪多糖DMEM细胞培养液分别加入已平铺于培养板的CaCo2细胞单层系统中与定量的大肠埃希菌混合培养,观察侵入细胞的大肠埃希菌量。结果黄芪多糖浓度为5×10-5,1×10-4mmol/L和2×10-4mmol/L,处理的CaCo2细胞液的细菌培养数量分别为252.5个±54.5个,240.8个±44.2个和292.7个±71.3个,而对照组为598.8个±114.8个,显示黄芪多糖能显著减少大肠埃希菌进入上皮细胞的数量,增强肠黏膜的屏障功能。     

Caco-2细胞模型及其在营养素小肠吸收机理研究中的应用

Caco-2细胞源自人结肠癌细胞,体外培养时能自发地进行类似肠道细胞的形态学和生化学上的分化,获得许多小肠吸收细胞的特性,如形成微绒毛结构;在细胞表面形成良好的刷状缘;在细胞间形成紧密连接;分泌水解酶以及合成转运糖、氨基酸和药物等的载体转运系统。由培养在微孔滤膜上的Caco-2细胞构建的模型为研究营养素在小肠的吸收机理提供了一个有效且易于操作的实验手段。本文主要综述了Caco-2细胞模型的建立、特征、检测及其在氨基酸、维生素、核苷和微量元素等营养素小肠吸收机理研究中的应用。     

贵州优良草种苇状羊茅规范化栽培施肥试验

2003~2004年采用二次通用旋转组合设计研究了氮、磷、钾不同施用水平对苇状羊茅鲜草产量的影响,获得优化回归模型为y=3426．86 623．07x1 220．75x3;主效应分析表明,增施氮、钾肥的增产效果十分明显,而增施磷肥的作用很小。经模拟寻优,获得年产鲜草4 864kg／667m2的施肥方案为每667m2施纯N 50kg、纯K2O 55kg。     

水稻不育系培矮64S的空间诱变效应及后代的SSR分析

对经过卫星搭载的培矮64S种子及后代进行了有关性状研究和SSR标记分析,结果表明:培矮64S空间诱变后代SP1代发芽率、存苗率、株高、抽穗期、株叶型的性状与对照相比没有明显变化;但SP2代在株高、粒型和育性等性状上发生了变异;从SP3代中获得柱头比培矮64S明显增大的变异株系,这对于改良培矮64S的异交结实率和提高制种产量具有重要意义。此外,对10个SP3变异株进行SSR分析结果表明,扩增片段数目变化约占55.21%,扩增片段分子量变化约占44.79%,空间诱变引起的变异可能是以DNA缺失-重复为主。SSR座位的变异频率平均为23.33%,变异座位在水稻基因组中是随机分布的。     

Effects of tris(1,3-dichloro-2-propyl) phosphate on epididymal sperm parameters in adult male rats

Tris(1,3-dichloro-2-propyl) phosphate (TDCIPP) is widely used as a flame retardant and is known to exhibit anti-androgenic effects in vitro and in vivo. To assess the reproductive toxicity potency of TDCIPP, we investigated the effects of 7 days of TDCIPP oral administration on epididymal sperm motion and concentration in adult male Wistar–Imamichi rats. Thirty-five days after the final administration, sperm parameters were evaluated by computer-assisted sperm analysis. Results showed that sperm swimming progression and vigor and sperm concentration in TDCIPP-treated rats were unexpectedly higher than those in control rats. TDCIPP did not significantly affect the percentage of motile sperms or sperm swimming pattern. These results contribute to the understanding of the biological effects of TDCIPP.     

典型旱作农田土壤氧化亚氮排放的氨氧化微生物相对贡献

氨氧化过程对氧化亚氮（N2O）排放具有重要贡献。在不同土壤类型和农田管理下,氨氧化微生物类群对N2O排放的相对贡献组成规律还缺乏系统的研究。本研究选取典型农田耕层土壤（潮土、黑土、砖红壤）,以及有机肥改良的砖红壤剖面土壤,采用选择性抑制法（乙炔和辛炔）研究氨氧化细菌（AOB）、氨氧化古菌和全程硝化菌（AOA+comammox）以及异养硝化菌对土壤硝化潜势、净硝化速率及N2O排放的相对贡献。结果表明,在耕层土壤中,潮土、黑土和砖红壤的pH分别是8.0、6.7和5.7,硝化潜势分别是N 32.5、6.6和4.8 mg?kg-1?d-1,净硝化速率分别是N 7.1、3.0和0.5 mg?kg-1?d-1,7天N2O累积排放量分别是N 38.0、35.4和8.7 μg?kg-1。AOB主导耕层土壤的硝化潜势,对硝化潜势的贡献分别是82%、58%和100%。对于净硝化速率,在潮土和砖红壤中,AOB和AOA+comammox贡献相当（均在30%~40%）,而黑土中由AOB主导（72%）。AOB主导耕层土壤的N2O排放,对N2O排放的贡献分别是72%、92%和58%。在改良的砖红壤剖面土壤中,在0~20 cm、20~40 cm和40~60 cm,pH分别是7.0、5.5和4.9,硝化潜势分别是N 6.6、2.0和1.1 mg?kg-1?d-1,净硝化速率分别是N 4.1、0.9和0.2 mg?kg-1?d-1,N2O排放分别是N 16.3、6.5和2.8 mg?kg-1?d-1。随土壤由深层至表层,硝化潜势、净硝化速率及N2O排放显著提高。AOA+comammox主导表层硝化潜势及净硝化速率的提高（分别贡献63%和54%）,AOB主导N2O排放的增加（贡献54%）。本研究为制定与土壤氨氧化特性及土壤性质相匹配的N2O减排措施提供了新的科学依据。