Highly potent germination inhibitors in aqueous eluate of fruits of Bishop's weed (Ammi majus L.) and avoidance of autoinhibition

The aqueous eluate from fruits ofAmmi majus (Bishop's weed, Umbelliferae) remarkably inhibited germination of adjacent seeds ofAnastatica hierochuntica, lettuce, or tomato but had no effect on intact fruits ofAmmi. Similar inhibition was found in dark or in light, except that seeds ofA. hierochuntica were significantly more inhibited in the dark than in the light. Xanthotoxin was isolated, identified, and found to account for about a sixth of the inhibitory activity of the eluate. After fruits ofAmmi were submerged in a large volume of water for 4 days, the fruits still exuded enough inhibitors to prevent germination ofA. hierochuntica, lettuce, or tomato. Data support also the proposal that the phytotoxins are compartmentalized between the inner and the outer fruit envelopes. The inner layer excludes inhibitors from the embryo and autotoxicity is thus avoided, whereas the outer one ensures a gradual liberation of the phytotoxic compounds. This, as well as the high reactivity of the eluate, the high densities ofAmmi fruits in nature, and their relatively limited annual germination, suggest chemical inhibition of neighboring plant species other thanAmmi. Hence, in addition to their chemical protection against predators of either lower or higher organisms, furanocoumarins in fruits ofAmmi majus may contribute to its success as a weed.     

两类昆虫生长调节剂作用机制的比较

两种昆虫生长调节剂——几丁质合成抑制剂和非舀类蜕皮激素类似物虽然都是作用于蜕皮过程，但有着截然不同的作用机制，本文对这两种杀虫剂作用机制的研究进展进行了总结和比较。     

Access of the substrate to the active site of yeast oxidosqualene cyclase: an inhibition and site-directed mutagenesis approach

A structural model of Saccharomyces cerevisiae oxidosqualene cyclase (SceOSC) suggests that some residues of the conserved sequence Pro-Ala-Glu-Val-Phe-Gly (residues 524-529) belong to a channel constriction that gives access to the active-site cavity. Starting from the SceOSC C457D mutant, which lacks the cysteine residue next to the catalytic Asp456 residue Cys457 has been replaced but Asp456 is still there, we prepared two further mutants where the wild-type residues Ala525 and Glu526 were individually replaced by cysteine. These mutants, especially E526C, were very sensitive to the thiol-reacting agent dodecyl-maleimide. Moreover, both the specific activity and the thermal stability of E526C were severely reduced. A similar decrease of the enzyme functionality was obtained by replacing Glu526 with alanine, while substitution with the conservative residues aspartate or glutamine did not alter catalytic activity. Molecular modeling of the yeast wild-type OSC and mutants on the template structure of human OSC confirms that the channel constriction is an important aspect of the protein structure and suggests a critical structural role for Glu526.     

Effects of amino acid replacements around the reactive site of chicken ovomucoid domain 3 on the inhibitory activity toward chymotrypsin and trypsin

We have previously shown that replacing the P1-site residue(Ala) of chicken ovomucoid domain 3 (OMCHI3) with a Met or Lysresults in the acquisition of inhibitory activity toward chymotrypsinor trypsin, respectively. However, the inhibitory activitiesthus induced are not strong. In the present study, we introducedadditional amino acid replacements around the reactive siteto try to make the P1-site mutants more effective inhibitorsof chymotrypsin or trypsin. The amino acid replacement AspTyrat the P2' site of OMCHI3(P1Met) resulted in conversion to a35000-fold more effective inhibitor of chymotrypsin with aninhibitor constant (K_i) of 1.17x10^–11 M. The K_i valueof OMCHI3(P1Met, P2'Ala) indicated that the effect on the interactionwith chymotrypsin of removing a negative charge from the P2'site was greater than that of introducing an aromatic ring.Similarly, enhanced inhibition of trypsin was observed whenthe AspTyr replacement was introduced into the P2' site of OMCHI3(P1Lys).Two additional replacements, AspAla at the P4 site and ArgAlaat the P3' site, made the mutant a more effective inhibitorof trypsin with a K_i value of 1.44x10^–9 M. By contrast,ArgAla replacement at the P3' site of OMCHI3(P1Met, P2'Tyr)resulted in a greatly reduced inhibition of chymotrypsin, andAspAla replacement at the P4 site produced only a small changewhen compared with a natural variant of OMCHI3. These resultsclearly indicate that not only the P1-site residue but alsothe characteristics, particularly the electrostatic properties,of the amino acid residues around the reactive site of the proteaseinhibitor determine the strength of its interactions with proteases.Furthermore, amino acids with different characteristics arerequired around the reactive site for strong inhibition of chymotrypsinand trypsin.     

A new class of corrosion inhibitors for waterborne coatings: 4-methyl-γ-oxo-benzene-butanoic acid complexes

Amine and transition metal based complexes with 4-methyl-γ-oxo-benzene-butanoic acid represent a new class of corrosion inhibitors specifically designed for long-term corrosion protection in waterborne coatings. Today, corrosion protection in waterborne technology is typically achieved using traditional anticorrosive pigments initially developed for use in solventborne coatings. Regulations concerning heavy metals and limitations regarding the compatibility and performance of such materials in waterborne coatings have created a need for novel approaches. Mechanistic aspects are discussed for the 4-methyl-γ-oxo-benzene-butanoic complexes based on electrochemical solution experiments (electrochemical impedance spectroscopy (EIS), linear sweep voltammetry (LSV)) and investigations performed on coated substrates. Exposure results underline the high efficiency of such complexes for both long-term corrosion protection and weld seam rust control in waterborne coatings.     

含杂环甲胺基的氰基丙烯酸酯类光合作用抑制剂的合成和活性研究进展

氰基丙烯酸酯是一类PSII电子传递抑制剂,笔者发现在抑制剂分子疏水性基团苯环被吡啶替代能大大提高其抑制活性,对此先导结构进一步优化,设计合成以下系列新化合物:含2-氯(或烷氧基)-5-吡啶甲胺基的氰基丙烯酸酯、含2-氟-5-吡啶甲胺基的氰基丙烯酸酯、含2-氯-5-噻唑甲胺基的氰基丙烯酸酯、氮在吡啶环不同位置的吡啶甲胺基氰基丙烯酸酯、含烷硫基取代的吡啶甲胺基的氰基丙烯酸酯、含二茂铁甲胺基的氰基丙烯酸酯。生测结果表明:这些含杂环甲胺基的氰基丙烯酸酯类化合物对油菜等十字花科类杂草表现出很好的除草活性,且茎叶处理优于土壤处理。     

Transformations and losses of fertilizer nitrogen on no-till and conventional till soils

A field study was conducted in 1982 to measure the effect of no-till (NT) and conventional till (CT) systems on N transformation after surface and subsurface applications of N fertilizers. Urea, urea-ammonium nitrate (UAN) solution, (NH₄)₂SO₄ (AS), and CA(NO₃)₂ were applied to NT and CT plots (5.95 m²) at a rate of 448 kg N ha^–1. A comparison of fertilizer N recovered in soils receiving incorporated or surface applied N was used to estimate NH₃ volatilization while denitrification was estimated from fertilizer N recovered in the presence and absence of nitrapyrin with incorporated N. Immobilization was assessed in microplots (0.37 m²) after surface application of (¹⁵NH₄)₂SO₄ to NT and CT systems at a rate of 220 kg N ha^–1.The results indicate little difference between NT and CT systems on urea hydrolysis rates and immobilization of surface applied fertilizer N. Approximately 50% and 10% of the surface applied N was recovered in the inorganic and organic fractions, respectively, on both tillage systems. The N not recovered was likely lost from plot areas through soil runoff. Incorporation of UAN, urea and AS resulted in 20 to 40% greater inorganic N recovery than from surface application. Nitrification rates were greater under the NT than the CT system. The similarities in concentration in the various N pools observed between the two tillage systems may be partially due to the short length of time that NT was imposed in this field study (<1 year) since other researchers using established tillage systems (>5 y) indicate that NT tends to promote decreased efficiency of fertilizer N.     

Free energy perturbation studies on binding of A-74704 and its diester analog to HIV-1 protease

Free energy simulations have been employed to rationalize thebinding differences between A-74704, a pseudo C₂- symmetricinhibitor of HIV-1 protease and its diester analog. The diesteranalog inhibitor, which misses two hydrogen bonds with the enzymeactive site, is surprisingly only 10-fold weaker. The calculatedfree energy difference of 1.7 ± 0.6 kcal/mol is in agreementwith the experimental result. Further, the simulations showthat such a small difference in binding free energies is dueto (1) weaker hydrogen bond interactions between the two (P₁and P₁) NH groups of A-74704 with Gly27/Gly27' carbonyls ofthe enzyme and (2) the higher desolvation free energy of A-74704compared with its ester analog. The results of these calculationsand their implications for design of HIV-1 protease inhibitorsare discussed.     

气相防锈技术在热力设备防腐蚀中的应用

归纳总结了近年来气相缓蚀剂的研究开发情况,介绍和探讨了气相防锈技术的特点及其在热力设备防腐蚀中的应用,包括气相缓蚀剂的气化装置设计、应用工艺、监测方法等,指出了气相防锈技术的发展趋势.     

产高温碱性蛋白酶菌株筛选及酶学性质研究

从高温堆肥土样中筛选到一株高产蛋白酶的菌株,经鉴定为Bacillus subtilis,命名为I15.对最适产酶发酵条件进行了优化,并研究了发酵产蛋白酶的酶学性质.结果表明,玉米淀粉和豆饼粉是该菌发酵产蛋白酶的最适经济碳氮源;该蛋白酶属高温碱性蛋白酶,具有很强的热稳定性和酸碱稳定性.另外,突出的性质是该蛋白酶对表面活性剂和温和型去垢剂具有超强的耐受性,将具有广阔的市场前景.