Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors

In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells.     

河南省平舆县农业环境污染现状及防治对策

分析河南省平舆县农业环境污染的主导因素:土壤受废水、农药、化肥、地膜、畜禽粪便对环境污染现状,探讨防治对策.     

Discovery and directed evolution of a glyphosate tolerance gene

The herbicide glyphosate is effectively detoxified by N-acetylation. We screened a collection of microbial isolates and discovered enzymes exhibiting glyphosate N-acetyltransferase (GAT) activity. Kinetic properties of the discovered enzymes were insufficient to confer glyphosate tolerance to transgenic organisms. Eleven iterations of DNA shuffling improved enzyme efficiency by nearly four orders of magnitude from 0.87 mM-1 min-1 to 8320 mM-1 min-1. From the fifth iteration and beyond, GAT enzymes conferred increasing glyphosate tolerance to Escherichia coli, Arabidopsis, tobacco, and maize. Glyphosate acetylation provides an alternative strategy for supporting glyphosate use on crops.     

黑龙江省东部山区养渔业与森林生态环境的关系

为充分利用林区的自然资源,1986—1987年先后在帽儿山实验林场和依兰县先锋林场进行了养鱼试验,经过120天的饲养期,鱼产量在帽儿山为3094.5kg/ha,在先锋为1882.5kg/ha。 林区水资源丰富,水质稳定;水的pH值偏低,多为软水,水中营养盐类贫乏。用石灰清塘可使pH值由6.5升至8.3。施肥可促进浮游生物的增殖,藻类的优势种为隐藻,浮游动物为近邻剑水蚤。灯光诱虫既能使鲤鱼生长明显加快,又能除去部分森林害虫。林区水体污染较轻,故家养鱼类病害也较少。 在帽儿山、鱼的增重倍数为5.33,饵料系数为2.14;在先锋则分别为7.68和1.35。由于鲤鱼适应低温环境,所以长势较鲢鳙鱼为好。在帽儿山鲤鱼平均重0.31kg,在先锋则为0.40kg。 林区宜主养鲤鱼,也应放养草食和腐食性的鱼类,以充分利用水体中的生态位。     

Cloning of a novel phytase from an anaerobic rumen bacterium,Mitsuokella jalaludinii,and its expression in Escherichia coli

The full length phytase gene of Mitsuokella jalaludinii was successfully cloned and was found to be 1 047 bp in length, with 348 amino acids, and was designated as PHY7 phytase gene. A comparison of the sequence of PHY7 phytase gene of M. jalaludinii with various microbial phytase gene sequences showed that it was not similar to those from other bacteria except Selenomonas ruminatium, thus suggesting that they may both express a new class of phytase. The PHY7 phytase gene was subsequently subcloned into bacterial expression vector, p ET32 a, for expression in Escherichia coli strain Rosetta-gami. Expression of the recombinant phytase gene was optimised and characterised. The recombinant phytase was estimated to be approximately 55 k Da by SDS-PAGE analysis. The recombinant phytase exhibited optimum activity at 55°C, p H 4.5 and showed good p H stability from p H 3.5 to 5.5(78% relative activity). Metal ions such as Ca2+, Mg2+, and K+ were found to exert significant stimulatory effect on the recombinant phytase activity while Cu2+, Fe3+, and Zn2+ greatly inhibited the enzyme activity. The recombinant phytase showed moderate resistance to trypsin proteolysis, but susceptible to pepsin proteolysis. The results of the study showed that several characteristics of recombinant phytase were slightly different from the native enzyme. Unfavourable characteristics such as reduced p H stability and metal ion effects should be taken into consideration during feed enzyme formulation.     

带V型减震器的框架——核心筒体结构动力计算方法

高层框架－核心筒体结构中，在框架与核心简体连接处设置Ｖ型减震器，使框架与核心筒体之间的刚性连接变成了弹性阻尼连接，从而减小了地震作用下结构的动力反应。本文通过对带Ｖ型减震器的高度框架－核心筒体结构动力特点的分析，建立了这种减震结构的动力计算模型，提出了这种减震结构的动力计算方法，并对计算公式进行了推导。     

Induction of Tolerance to Fusarium Wilt and Defense-Related Mechanisms in the Plantlets of Susceptible Berangan Banana Pre-lnoculated with Pseudomonas sp. （UPMP3） and Burkholderia sp. （UPMB3）

This study is aimed at assessing the ability of two endophytic bacteria originally isolated from healthy oil palm roots, Pseudomonas sp. （UPMP3） and Burkholderia sp. （UPMB3） to induce resistance in susceptible Berangan banana against Fusarium oxysporum race 4 （FocR4）. Increased accumulation of resistance-related enzymes such as peroxidase （PO）, phenylalanine ammonia lyase （PAL）, lignithioglycolic acid （LTGA）, and pathogenesis-related （PR） proteins （ehitinase and β-1,3-glucanase） has been observed in plantlets treated with endophytic bacteria UPMP3 and UPMB3 singly or as mixture under glasshouse conditions. Pre-inoculation of banana plantlets with UPMP3 showed a significant reduction in Fusarium wilt incidence 72 d after challenged inoculation with FocR4. UPMB3 was less effective in suppressing Fusarium wilt compared to UPMP3, whereas, the mixture of both endophytes showed an intermediate effect. Based on these results, it is concluded that UPMP3 could be a promising biological control agent that can trigger resistance against Fusarium wilt in susceptible Berangan banana.     

The composite genome of the legume symbiont Sinorhizobium meliloti

The scarcity of usable nitrogen frequently limits plant growth. A tight metabolic association with rhizobial bacteria allows legumes to obtain nitrogen compounds by bacterial reduction of dinitrogen (N2) to ammonium (NH4+). We present here the annotated DNA sequence of the alpha-proteobacterium Sinorhizobium meliloti, the symbiont of alfalfa. The tripartite 6.7-megabase (Mb) genome comprises a 3.65-Mb chromosome, and 1.35-Mb pSymA and 1.68-Mb pSymB megaplasmids. Genome sequence analysis indicates that all three elements contribute, in varying degrees, to symbiosis and reveals how this genome may have emerged during evolution. The genome sequence will be useful in understanding the dynamics of interkingdom associations and of life in soil environments.     

Observation of covalent intermediates in an enzyme mechanism at atomic resolution

In classical enzymology, intermediates and transition states in a catalytic mechanism are usually inferred from a series of biochemical experiments. Here, we derive an enzyme mechanism from true atomic-resolution x-ray structures of reaction intermediates. Two ultra-high resolution structures of wild-type and mutant d-2-deoxyribose-5-phosphate (DRP) aldolase complexes with DRP at 1.05 and 1.10 angstroms unambiguously identify the postulated covalent carbinolamine and Schiff base intermediates in the aldolase mechanism. In combination with site-directed mutagenesis and (1)H nuclear magnetic resonance, we can now propose how the heretofore elusive C-2 proton abstraction step and the overall stereochemical course are accomplished. A proton relay system appears to activate a conserved active-site water that functions as the critical mediator for proton transfer.