Alkylated/aminated nitroimidazoles and nitroimidazole-7-chloroquinoline conjugates: Synthesis and anti-mycobacterial evaluation

The success in exploring anti-tubercular potency of nitroimidazole and quinoline, the core moieties of recently approved anti-tubercular drugs instigated us to synthesize a series of alkylated/aminated 2-methyl-5-nitroimidazoles and nitroimidazole-7-chloroquinoline conjugates and to evaluate them for their activities against Mycobacterium tuberculosis as well as for their cytotoxicity towards the J774 murine macrophage cell line. Although the synthesized compounds did not surpass the activity of the standard drug Isoniazid, they have appreciable activities with minimal cytotoxicity. The synthesized nitroimidazole-7-chloroquinoline conjugate, 11c, having butyl chain as linker, proved to be the most potent among the series with an MIC₅₀ value of 2.2?μg/mL.     

An Integrated Proteomic Approach Uncovers Novel Substrates and Functions of the Lon Protease in Escherichia coli

Controlling the cellular abundance and proper function of proteins by proteolysis is a universal process in all living organisms. In Escherichia coli, the ATP‐dependent Lon protease is crucial for protein quality control and regulatory processes. To understand how diverse substrates are selected and degraded, unbiased global approaches are needed. We employed a quantitative Super‐SILAC (stable isotope labeling with amino acids in cell culture) mass spectrometry approach and compared the proteomes of a lon mutant and a strain producing the protease to discover Lon‐dependent physiological functions. To identify Lon substrates, we took advantage of a Lon trapping variant, which is able to translocate substrates but unable to degrade them. Lon‐associated proteins were identified by label‐free LC‐MS/MS. The combination of both approaches revealed a total of 14 novel Lon substrates. Besides the identification of known pathways affected by Lon, for example, the superoxide stress response, our cumulative data suggests previously unrecognized fundamental functions of Lon in sulfur assimilation, nucleotide biosynthesis, amino acid and central energy metabolism.     

Five New Alkaloids from the Roots of Sophora flavescens

Five new quinolizidine alkaloids, including three sparteine‐type alkaloids ( 1  –  3 ) and two cytisine‐type alkaloids ( 4 and 5 ), along with four known ones, were isolated from the roots of Sophora flavescens. Their structures were determined by extensive spectroscopic techniques including IR, UV, NMR, and HR‐ESI‐MS. All the compounds were evaluated for their antibacterial activities against Staphylococcus aureus and Escherichia coli.     

Phytochemical Composition and Biological Activities of Dyssodia tagetiflora Lag.

While plants of the genus Dyssodia are used by man to a certain extent, few phytochemical and pharmacological studies have been performed with species of this genus. D. tagetiflora is an endemic plant of Mexico and has been used as fodder. The aim of this research was to isolate and identify the main bioactive components and evaluate the insecticidal, antioxidant, genotoxic and cytoprotective activities of D. tagetiflora. The isolated substances included an essential oil composed of six monoterpenes, and extracts containing two flavonols, three flavonol‐glycosides and four thiophenes. The compounds were characterized using spectroscopic and spectrometric methods, including GC/MS, MS and NMR. The essential oil showed insecticidal activity against Drosophila melanogaster larvae. The methanolic extract of D. tagetiflora (DTME) had strong antioxidant activity against DPPH and ABTS radicals; DTME showed no evidence of genotoxic or cytotoxic effects. In contrast, DTME showed a cytoprotective effect attenuating the formation of H₂O₂‐induced micronuclei in Vicia faba roots. This report is the first to describe the phytochemical and biological activity of D. tagetiflora.     

杂交水稻及其亲本光合特性的研究 Ⅲ.功能叶片碳代谢中一些酶活性

对杂交水稻青优159（母本青A,父本R159）和广优四号（母本广A,父本青六矮）及其亲本功能叶片光合碳代谢中一些酶活性进行了研究。实验结果表明了两组杂交水稻的RuBPCase活性、RuBPCase/RuBPOase活性比值超过其各自的亲本;而杂交水稻青化159和广优四号的RuBPOase活性、乙醇酸氧化酶活性、光呼吸速率、光呼吸速率与光合速率的比值明显的低于其各自双亲．对RuBPCase活性和乙醇酸氧化酶活性与光合速率进行相关分析,结果表明RuBPCase活性与光合速率有正相关关系,相关系数为0．768;而乙醇酸氧化酶活性与光合速率负相关,相关系数为-0．834;两者均达到α＝0．05显著水平。     

Modulator effect of DL-α-difluoromethylarginine treatments on differentiation processes of young maize calluses

The effect of pretreatments with 0.5, 1, 3, 5 and 10 mM of DL--difluoromethylarginine (DFMA), an irreversible suicide inhibitor of the arginine decarboxylase (ADC) activity, on the differentiation process of young maize calluses was studied. Callus protein, total polyamine content and ADC activity decreased versus control in all the assayed treatments. Furthermore, ornithine decarboxylase (ODC) activity was significantly lower in the treated calluses, which was probably due to the arginase activity detected in them. Short tratments at high doses of DFMA significantly increased the number of regenerated buds versus the control (four times more in 10 mM and almost two times more in 5 mM). By contrast, long treatments at low doses (0.5, 1 and 3 mM) reduced the number of plantlets. Conjugated putrescine seems to be implicated in the regeneration response of control and high DFMA-treated calluses.     

Glutamine synthetase and glutamate synthase from Sclerotinia sclerotiorum

Glutamine synthetase (GS, EC 6.3.1.2) and glutamate synthase (GOGAT, EC 1.4.1.13) were purified from Sclerotinia sclerotiorum and some of their properties studied. The GS transferase and biosynthetic activities, as well as GOGAT activity, were sensitive to feedback inhibition by amino acids and other metabolites. GS showed a marked dependence on ADP in the transferase reaction and on ATP in the Mg²⁺-dependent biosynthetic reaction. Regulation of GS activity by adenylylation/deadenylylation was demonstrated by snake venom phosphodiesterase treatment of the purified enzyme. GOGAT required NADPH as an electron donor; NADH was inactive. GOGAT was strongly inhibited by p-chloromercuribenzoate and the inhibition was reversed by cysteine. The enzyme was also markedly inhibited by o-phenanthroline, 2,2′-bipyridyl and azaserine. l-Methionine-dl-sulphoximine (MSX) and azaserine inhibited the incorporation of ¹⁵N-labelled ammonium sulphate into washed cells of S. sclerotiorum. MSX and azaserine respectively also inhibited purified GS and GOGAT activities. GDH activity was not detected in cell-extracts. Thus the GS/GOGAT pathway is the main route for the assimilation of ammonium compounds in this fungus.     

THE BIOLOGICAL ACT'IVITIES OF YELLOW AZALEA,RHODODENDRON MOLLE G. DON AGAINST THE VEGETABLE LEAFMINER,LIRIOMYZA SATIVAE (DIPTERA: AGROMYZIDAE) *

Abstract The results of laboratory and greenhouse bioassays indicated that Rhodojaponin‐ III (Abbr. R‐ 1) and extracts of flowers from Rhododendron molle G. Don possessed signficant feeding inhibition and insectcidal properties against the larvae and adults of Liromyzia sativae. Treated with 500 mg/L R‐ III 1 000 mg/L molosul‐tap, and 10 000 mg/L methanol(MeOH) ethyl acetate (EtOAc), CH₂Cl₂, methanol‐water (MeOH‐H₂O) extracts the rates of feeding inhibition were 77. 34 % 74.30 % 82.15 % 77.50 % 67. 33 % 62.85 % against the 2nd instar larvae, and were 67.66% 55.21 % 49.72% 54.26% 46.81 % 38.53% against the 3rd instar larvae, respectively;LC₅₀ values against the 2nd instar larvae were 208.65, 166.05, 2.74 ± 10³,766.72, 5.95 ± 10³, 1.85 ± 10³mg/L, and against 3rd larvae were 300.62, 256.00, 4.33 ±10³, 1.03 ± 10³,9.79 ± 10³, and 2.62± 10³mg/L, respectively. Against the adults, LC₅₀ values of R‐III EtOAc extract and molosultap were 159.07.723.87 and 134.55mgL respectively after treatment for 24 h.     

Modified monoclonal antibody production kinetics kappa/gamma mRNA levels, and metabolic activities in a murine hybridoma selected by continuous Culture

During long-term continuous culture of the hybridoma cell line 11317, a better-producing subclone (I1317-SF11), giving improved productivity, has been selected. The comparison of the original cell line (I1317-DC) with this subclone revealed that although the growth patterns of both clones were similar, both in continuous and in batch cultures, considerable differences could be seen between the clones with respect to monoclonal antibody (MAB) accumulation, MAB production rate, the levels of mRNA coding for heavy and light chains of IgG, and some metabolic activities. In continuous culture as well as in batch culture, I1317-SF11 showed increased levels of mRNA coding for kappa and gamma chains compared with I1317-DC and/or a modified ratio of the mRNA species when compared to that in I1317-DC. Using pulse experiments, it could be established that the biosynthesis of both chains was augmented in I1317-SF11. Although the kappa and gamma mRNA levels were modified or inversed for I1317-SF11, the cells always synthesized more kappa than gamma chains. The overall increase in the synthetic activity of I1317-SF11 is suggested as one reason for the considerable increase of IgG productivity and product accumulation in continuous culture as well as in repeated batch cultures. Tests concerning metabolic activity revealed that I1317-SF11 had a predominantly glycolytic metabolism independent of growth requirements, whereas for I1317-DC the metabolism became increasingly glycolytic with increased growth. The antibody yield coefficient of I1317-SF11 on glutamine was significantly higher than that of I1317-DC for the continuous culture, whereas the antibody coefficients on glucose were almost similar for both clones under the different culture conditions used. Both antibody coefficients were considerablly influenced by the specific growth rate.All these facts together lead to the conclusion that subclone I1317-SF11 uses more of the energy available, or it was the energy and/or precursors available for the synthesis and production of MAB more efficiently than the thesis and production of MAB more efficiently than the original cell line. Although the levels of mRNA coding for heavy and light chains of IgG were modified, it could be confirmed that the overall regulation of MAB-synthesis and -production occurs post-translationally and that at higher growth rates, more biosynthetic activity is diverted to biomass production. (c) 1994 John Wiley & Sons, Inc.     

一种修正的动态神经元网络模型的类脑电活动及其应用

在作者以前所提出的一种简化现实性神经网络模型－动态神经元网络模型的基础上,进一步考虑了发放神经脉冲引起的兴奋性变化以及每个神经元和其它神经元之间都只有有限联结的性质。使修正后的模型具有更强的生物学真实性。计算机仿真表明由这样的网络产生的类脑电活动对初值极端敏感,具有明显的混沌动力学性质,利用这一点作者们成功地对电脑文档进行了加密和解密,参数和初值的微小改变都使解密失败,从而可望由此得出高度可靠的保