Synthesis and Biological Activities of Phosphonylalkylpurine Derivatives

Abstract

Syntheses and biological activities of 2-phosphonylmethoxy-ethyl (PME) purine analogs are described.     

Industrial production of soy sauce

Summary Soy sauce is a seasoning agent with a salty taste and a distinct aroma suggestive of meat extracts. The sauce is made by fermentation of a combination of soy beans and wheat in water and salt. This paper covers the method for production of fermented soy sauce, and that for acid-hydrolysis of defatted soy bean proteins. The microorganisms involved in soy sauce production, and biochemical and chemical changes in soy bean and wheat during fermentation influence greatly the sensory attributes and quality of soy sauce. Recent progress in industrialization of soy sauce manufacture is discussed.This paper is dedicated to Professor Herman Jan Phaff in honor of his 50 years of active research which still continues.     

Isolation and characterization of polyphenol oxidase isozymes of clingstone peach

The polyphenol oxidase system in clingstone peach (Prunus persica) was investigated. Polyacrylamide disc-gel electrophoresis indicated four bands with polyphenol oxidase activity in extracts from acetone powder of clingstone peach. These four isozymes were then isolated from a buffer extract of peach acetone powder by cold acetone precipitation, followed by diethylaminoethyl cellulose column chromatography. All isozymes had different heat stabilities. At 55 C, polyphenol oxidases A, B, and D had half-lives of 5.4, 14.6, and 14.1 minutes, respectively. Polyphenol oxidase C was stable over a period of 50 minutes of incubation at 55 C, but had a half-life of 2.2 minutes at 76 C. None of the isozymes had monophenolase activity, and they varied in their specificity for several diphenols. The following values were found for polyphenol oxidases A, B, C, and D, respectively, with catechol as substrate: optimal pH: 6.8, 6.5, 7.2, and 7.0; Michaelis constant: 6.6, 4.2, 7.0, and 36 mm; V(max)/(E(0)): 4.95, 39.4, 2.16, and 80.0 (DeltaA min(-1) mg(-1)). Each isozyme showed a different amount of inhibition by NaHSO(3), NaCl, NaCN, l-ascorbic acid, glutathione, ethylenediaminetetraacetate, and sodium diethyldithiocarbamate.     

以家蚕Bombyx mori L.讨论鳞翅目幼虫头部的形态

鳞翅目幼虫(通称蠋)头部的构造比较特殊,到现在还有各种不同的见解。我们试用家蚕来解释和统一这些不同的见解。     

非洲蝼蛄, Gryllotalpa africana de Beauvois, (直翅目:蝼蛄科)的外部形态.Ⅰ.头部和取食机械

蝼蛄为华北主要农作物害虫之一,对於此类大害虫,作各方面的研究,直接或间接都有助於了解和防治。蝼蛄形态方面的工作很少,和同目的蝗科(Acridiidae)昆虫比较,虽然同具经济重要性,但相去很远;并且已发表的工作(Chiu,1933;Furukawa,1936),既未述及和骨片(sclerites)密切相关的肌肉系统,且其中部份事实和观点,有重新考虑的必要。为了弥补这些缺陷,蝼蛄的形态,有作详细研究的     

Carboxyfullerene prevents iron-induced oxidative stress in rat brain

Carboxyfullerene, a water-soluble carboxylic acid derivative of a fullerene, was investigated as a protective agent against iron-induced oxidative stress in the nigrostriatal dopaminergic system of anesthetized rats. Intranigral infusion of exclusive carboxyfullerene did not increase lipid peroxidation in substantia nigra or deplete dopamine content in striatum. Infusion of ferrous citrate (iron II) induced degeneration of the nigrostriatal dopaminergic system. An increase in lipid peroxidation in substantia nigra as well as decreases in K+-evoked dopamine overflow and dopamine content in striatum were observed 7 days after the infusion. Co-infusion of carboxyfullerene prevented iron-induced oxidative injury. Furthermore, tyrosine hydroxylase-immunoreactive staining showed that carboxyfullerene inhibited the iron-induced loss of the dopaminergic nerve terminals in striatum. The antioxidative action of carboxyfullerene was verified by in vitro studies. Incubation of brain homogenates increased the formation of the Schiff base fluorescent products of malonaldehyde, an indicator of lipid peroxidation. Both autooxidation (without exogenous iron) and iron-induced elevation of lipid peroxidation of brain homogenates were suppressed by carboxyfullerene in a dose-dependent manner. Our results suggest that intranigral infusion of carboxyfullerene appears to be nontoxic to the nigrostriatal dopaminergic system. Furthermore, the potent antioxidative action of carboxyfullerene protects the nigrostriatal dopaminergic system from iron-induced oxidative injury.     

The role of apoptosis signal-regulating kinase 1 in lymphotoxin-beta receptor-mediated cell death

LIGHT (homologous to lymphotoxins, shows inducible expression, and competes with herpes simplex virus glycoprotein D for herpesvirus entry mediator, a receptor expressed by T lymphocytes) is a member of the tumor necrosis factor superfamily that can interact with lymphotoxin-beta receptor (LTbetaR), herpes virus entry mediator, and decoy receptor (DcR3). In our previous study, we showed that LIGHT is able to induce cell death via the non-death domain containing receptor LTbetaR to activate both caspase-dependent and caspase-independent pathway. In this study, a LIGHT mutein, LIGHT-R228E, was shown to exhibit similar binding specificity as wild type LIGHT to LTbetaR, but lose the ability to interact with herpes virus entry mediator. By using both LIGHT-R228E and agonistic anti-LTbetaR monoclonal antibody, we found that signaling triggered by LTbetaR alone is sufficient to activate both caspase-dependent and caspase-independent pathways. Cross-linking of LTbetaR is able to recruit TRAF3 and TRAF5 to activate ASK1, whereas its activity is inhibited by free radical scavenger carboxyfullerenes. The activation of ASK1 is independent of caspase-3 activation, and kinase-inactive ASK1-KE mutant can inhibit LTbetaR-mediated cell death. This suggests that ASK1 is one of the factors involved in the caspase-independent pathway of LTbetaR-induced cell death.     

Single molecule imaging of supported planar lipid bilayer--reconstituted human insulin receptors by in situ scanning probe microscopy

A 480-kDa disulfide-linked heterodimer single-pass transmembrane protein, the insulin receptor, is autophosphorylated upon insulin binding to its extracellular domain. Remarkably, the structural basis for this activation process remained largely unknown until the recent cryoelectron microscopy studies of the insulin-insulin receptor complex by Luo et al. [Science 285 (1999) 1077]. We report here the results of an in situ study by high-resolution scanning probe microscopy of the full-length insulin receptor reconstituted within supported planar lipid bilayers. Our preliminary studies confirm that (1) the intact receptor can be reconstituted constitutively within a lipid vesicle and (2) fusion of the receptor-containing vesicles to mica resulted in the formation of molecular flat 5.5-nm-thick supported planar bilayers populated by two populations of protrusions, the shape and size of which are consistent with those of the insulin receptor's intra- and extracellular domains as modeled by the cryo-EM data of Ottensmeyer et al. [Biochemistry 39 (2000) 12103]. These results establish a framework for real-time studies of insulin-insulin receptor binding by in situ SPM and single molecule force spectroscopy.     

The LuxR family protein SpnR functions as a negative regulator of N-acylhomoserine lactone-dependent quorum sensing in Serratia marcescens

Serratia marcescens SS-1 produces at least four N-acylhomoserine lactones (AHLs) which were identified using high-resolution mass spectrometry and chemical synthesis, as N-(3-oxohexanoyl) homo-serine lactone (3-oxo-C6-HSL), N-hexanoyl- (C6-HSL), N-heptanoyl (C7-HSL) and N-octanoyl- (C8-HSL) homoserine lactone. These AHLs are synthesized via the LuxI homologue SpnI, and regulate via the LuxR homologue SpnR, the production of the red pigment, prodigiosin, the nuclease, NucA, and a biosurfactant which facilitates surface translocation. spnR overexpression and spnR gene deletion show that SpnR, in contrast to most LuxR homologues, acts as a negative regulator. spnI overexpression, the provision of exogenous AHLs and spnI gene deletion suggest that SpnR is de-repressed by 3-oxo-C6-HSL. In addition, long chain AHLs antagonize the biosurfactant-mediated surface translocation of S. marcescens SS-1. Upstream of spnI there is a gene which we have termed spnT. spnI and spnT form an operon and although database searches failed to reveal any spnT homologues, overexpression of this novel gene negatively affected both sliding motility and prodigiosin production.     

The genome of B. subtilis phage SSP1: the topology of DNA molecules.

DNA molecules of B. subtilis phage SPP1 exhibit terminal redundancy and are partially circularly permuted. This was established by the hybridization of selected EcoRI restriction fragments to single strands of SPP1 DNA and by an analysis of the distribution of denaturation loops in partially denatured SPP1 DNA molecules. Deletions in SSP1 DNA are not compensated by an increase in terminally repetitious DNA. This finding, which is unique to SPP1, is discussed in terms of a modification of the Streisinger/Botstein model of phage maturation.