生物絮凝剂的研究与开发

总结了生物絮凝剂的研究与开发状况。叙述了研究生物絮凝剂的背景，概括了产絮凝剂生物的筛选，鉴定及培养条件，分析了生物絮凝剂的结构，性能，作用机理，列举了生物絮凝剂的应用；最后，谈了目前对其开发的情况和新的研究方法。     

Alkylation of Staurosporine to Derive a Kinase Probe for Fluorescence Applications

The natural product staurosporine is a high‐affinity inhibitor of nearly all mammalian protein kinases. The labelling of staurosporine has proven effective as a means of generating protein kinase research tools. Most tools have been generated by acylation of the 4′‐methylamine of the sugar moiety of staurosporine. Herein we describe the alkylation of this group as a first step to generate a fluorescently labelled staurosporine. Following alkylation, a polyethylene glycol linker was installed, allowing subsequent attachment of fluorescein. We report that this fluorescein–staurosporine conjugate binds to cAMP‐dependent protein kinase in the nanomolar range. Furthermore, its binding can be antagonised with unmodified staurosporine as well as ATP, indicating it targets the ATP binding site in a similar fashion to native staurosporine. This reagent has potential application as a screening tool for protein kinases of interest.     

有机化工废水COD高效降解菌的分离筛选及应用

利用有机化工废水培养基从新疆高海拔盐湖样品中分离筛选到COD降解菌18株,对COD降解率高的8株菌株混合后处理废水,与其他普通活性污泥相比,COD去除率更高(86.3%)。经16S r DNA初步鉴定,该8株菌分别属于拟杆菌门Bacteroidetes、厚壁菌门Firmicutes和变形菌门Proteobacteria。将该混合菌群用于生物曝气池试验,添加尿素0.75 g/L作为氮源,其COD降解率可达82.5%;添加金枪鱼蛋白胨0.5 g/L可使COD降解率提高到92.2%。     

REPLACE: a strategy for iterative design of cyclin-binding groove inhibitors

We describe a drug-design strategy termed REPLACE (REplacement with Partial Ligand Alternatives through Computational Enrichment) in which nonpeptidic surrogates for specific determinants of known peptide ligands are identified in silico by using a core peptide-bound protein structure as a design anchor. In the REPLACE application example, we present the effective replacement of two critical binding motifs in a lead protein-protein interaction inhibitor pentapeptide with more druglike phenyltriazole and diphenyl ether groups. These were identified through docking of fragment libraries into the volume of the cyclin-binding groove of CDK2/cyclin A vacated through truncation of the inhibitor peptide-binding determinants. Proof of concept for this strategy was obtained through the generation of potent peptide-small-molecule hybrids and by the confirmation of inhibitor-binding modes in X-ray crystal structures. This method therefore allows nonpeptide fragments to be identified without the requirement for a high-sensitivity binding assay and should be generally applicable in replacing amino acids as individual residues or groups in peptide inhibitors to generate pharmaceutically acceptable lead molecules.     

小麦白粉病离体叶段筛选方法初探

本研究用小麦离体叶段法测定8种药剂各4个浓度对小麦白粉病的防效,结果表明,离体叶段法可用于新化合物对小麦白粉病菌的活性筛选.     

竹叶黄酮护肤霜功效的研究

将竹叶黄酮添加到护肤霜基质中制得竹叶黄酮护肤霜,按有关标准对产品进行了性能测试和评价.护肤功效检测表明,含质量分数为1.5％的竹叶黄酮护肤霜在UVB区的平均吸光度为1.273,在UVA区的防晒效果达到三星级,具有较好的防晒功效;有优良的保湿功效;能显著降低皮肤黑色素含量而美白皮肤;可改善皮肤纹理度,降低皮肤粗糙度;增加皮肤弹性;且人体试验安全、无刺激性,是一种天然的化妆品功能性成分添加剂.     

生物絮凝剂产生菌的筛选及絮凝处理靛蓝印染废水的研究

从活性污泥中分离出22株菌株,筛选得到具有絮凝活性的菌株14株,其中FJ-7、FJ-15絮凝活性较高。将两株絮凝剂产生菌分别纯培养及以体积比1∶1比例混合培养,发现混合培养发酵液对高岭土悬浊液的絮凝效果优于各菌株的纯培养发酵液。利用此混合发酵液对靛蓝印染废水进行絮凝处理,考察了生物絮凝剂和助凝剂CaC l2的用量、废水pH对脱色效果的影响。在混合菌发酵液和助凝剂CaC l2的体积分数分别为5%和4%、废水pH=8.0的最适脱色条件下,混合发酵液对靛蓝废水的脱色率可达87.2%。     

Designed amyloid beta peptide fibril - a tool for high-throughput screening of fibril inhibitors

Amyloid beta peptide (Abeta) fibril formation is widely believed to be the causative event of Alzheimer's disease pathogenesis. Therapeutic approaches are therefore in development that target various sites in the production and aggregation of Abeta. Herein we present a high-throughput screening tool to generate novel hit compounds that block Abeta fibril formation. This tool is an application for our fibril model (Abeta(16-37)Y(20)K(22)K(24))(4), which is a covalent assembly of four Abeta fragments. With this tool, screening studies are complete within one hour, as opposed to days with native Abeta(1-40). A Z' factor of 0.84+/-0.03 was determined for fibril formation and inhibition, followed by the reporter molecule thioflavin T. Herein we also describe the analysis of a broad range of reported inhibitors and non-inhibitors of Abeta fibril formation to test the validity of the system.     

发现天然活性物质的潜在途径--生物胺转运体的靶标筛选

生物胺转运体(BAT)是生物膜上的一种蛋白质,它通过将底物从细胞外转运到神经末端来终止多巴胺(DA)、5-羟色胺(5-HT)和去甲肾上腺素(NE)的作用.大量药物和给药方法以BAT为靶点,以底物或抑制剂的形式发挥作用.本文总结了作用于BAT上的药物活性的几种测量方法,并以麻黄碱及其立体异构体为例来讨论这些方法用来发现天然活性物质的潜在应用.