某些二茂铁烷基杂环化合物的合成与表征

以BF3·OEt2为催化剂,以CH2Cl2作溶剂,用α-二茂铁基醇与吗啉及六氢吡啶反应,得到二茂铁烷基杂环化合物.对所合成的6个二茂铁烷基杂环化合物进行了元素分析及质子核磁共振谱表征.     

Cloning and expression of apolipophorin-III from the common cutworm, Spodoptera litura

Infections of the eye and genital tract with the bacterium Chlamydia trachomatis are a major cause of morbidity worldwide and are costly to treat. Development of a vaccine capable of protecting against infection or severe disease presents special challenges but would be the most effective long-term option for control of chlamydial disease. Progress has been made in understanding protective and pathological immune mechanisms in these infections, and a number of potential vaccine candidates have been developed.     

Residual activity of three slow-release temephos formulations against Aedes aegypti larvae

Residual effectiveness of plaster matrix formulations of temephos and temephos plus an emulsifier (Atlox 3409F) were evaluated against Aedes aegypti larvae during an 8-wk period. Formulations of 2% and 5% (AI) Atlox with 5% (AI) temephos yielded 100% larval mortality for 8 wk. A 5% temephos formulation without the addition of the emulsifier produced 100% larval mortality through only 1 wk.     

Modulation of the Rev-RRE interaction by aromatic heterocyclic compounds

The HIV-1 Rev protein regulates the nucleocytoplasmic distribution of viral precursor RNAs that encode HIV-1 structural proteins. Rev-mediated viral RNA expression requires a sequence-specific interaction between Rev and a viral RNA sequence, the Rev responsive element (RRE). Because the Rev-RRE interaction is essential for HIV-1 replication, anti-viral agents that selectively block this interaction may be effective anti-HIV-1 therapeutics. Here, we show that certain aromatic heterocyclic compounds, in particular, a tetracationic diphenylfuran, AK.A, can block binding of Rev to its high-affinity viral RNA binding site. AK.A abolishes Rev-RRE interactions at concentrations as low as 0.1 microM. Inhibition appears to be selective and results from competitive binding of the drug to a discrete region within the Rev binding site. Interestingly, the molecular basis for the AK.A-RNA interaction, as well as the mode of RNA binding differs from previously described aminoglycoside Rev inhibitors. Analysis of a variety of aromatic heterocyclic compounds and their derivatives reveals stereo-specific features required for the inhibition. Our results further demonstrate the feasibility of identifying and designing small molecules that selectively block viral RNA-protein interactions.     

Glutathione peroxidase-like activity of simple selenium compounds. Peroxides and the heterocyclic N-oxide resazurin acting as O-atom donors

Selenite and selenocystamine [(CyaSe)2] efficiently activate the decomposition of H2O2 by GSH and by other thiols, as demonstrated using a leuco crystal violet POD-based H2O2 assay which is applicable (unlike other assays) also in presence of thiols. The GPx-like activities were estimated to be 3.6 and 2.7 mumol H2O2/min per mumol SeO3(2-) and (CyaSe)2, respectively. Both selenium compounds also activate reduction of the heterocyclic N-oxide resazurin (RN-->O) to resorufin (RN) by GSH; H2O2 competes with reduction of this dye. GSSeH and CyaSeH, formed by interaction of GSH with SeO3(2-) and (CyaSe)2, respectively, are likely to be the active reductants. CyaSeH, generated gamma-radiolytically from (CyaSe)2, exhibits an absorption peak at 243 nm and is removed by H2O2 with a rate constant of 9.7 x 10(2) M-1 s-1, and slightly slower by hydroperoxides. We have no evidence for one-electron interactions between GSSeH or CyaSeH and H2O2, with formation of free radical intermediates, as previously proposed in the case of selenium-activated reduction of cytochrome c by GSH (Levander et al., Biochemistry 23, 4591-4595 (1973)). Our results can be explained by O-atom transfer from the substrate to the active selenol group, RSeH + H2O2 (RN-->O)-->RSeOH + H2O (RN), and recycling of RSeOH to RSeH (+ H2O) by GSH, analogous to the selenenic acid pathway of GPx. The substrate specificity appears to be different, however, in that GPx is unable to catalyse RN-->O reduction, and GSSeH hardly catalyses the decomposition of cumene- or t-butyl-hydroperoxide; CyaSeH, on the other hand, is active also with the hydroperoxides. RN-->O is reduced to RN also by certain oxidizing free radicals, e.g. by the thiyl CyaS.., O-atom transfer may in this case lead to the generation of reactive oxyl radicals.     

Condensed heterocyclic compounds: synthesis and antiinflammatory activity of novel thiazolo[3,2-alpha] pyrimidines

In this study, thirty six new 2-benzylidene-7-methyl-3-oxo-5- phenyl-2,3-dihydro-5H-thiazolo[3,2-alpha]pyrimidine-6-carboxylic acid methyl esters were synthesized and characterized by spectral, crystallographic, and elemental analysis. The antiinflammatory activity of the compounds was tested by the carrageenan hind paw edema test. It was found that compound 6a having a 2-meth-oxyphenyl group at position 5 and a benzylidene group at position 2 was the most potent compound in this series. All the compounds that were tested for ulcer activity gave positive results.     

Cytostatic activity of some essential oils against HEp-2 cells

Samples of different essential oils have been tested for their cytostatic activity. The samples of cinnamon and clove essential oils showed a strong in vitro activity against HEp-2 cells.     

Novel bismuth compounds have in vitro activity against Helicobacter pylori

We examined the in vivo effects of ONO-5046xNa, a specific neutrophil elastase (NE) inhibitor, on the growth of 2 non-small cell lung cancer cell lines, EBC-1 and PC-3, transplanted into severe combined immunodeficiency (scid) mice. The daily intraperitoneal injection of ONO-5046xNa (50 mg/kg/day) completely suppressed the tumor growth in EBC-1, a human squamous carcinoma cell line which produces immunoreactive NE. By contrast, in PC-3, a human adenocarcinoma cell line which is unable to produce immunoreactive NE, the ONO-5046xNa treatment caused delayed growth of the tumor. These findings suggest that ONO-5046xNa may have a clinical role in preventing the growth of human non-small cell lung cancer.     

Synthesis and antimycobacterial activity of some new 3-heterocyclic substituted chromones

The aldol synthesis of benzimidazole, benzothiazole and benzothiazolium salt derivatives of chromones is described. The structures of the compounds have been proved by elemental analysis and 1H NMR spectra. The antimycobacterial activity of some of the prepared compounds have been tested in vitro against Mycobacterium tuberculosis (H37Rv) and Mycobacterium fortuitum (1021).     

The larvicidal activity of solvent extracts of three medicinal plants against third instar larvae of Chrysomyia albiceps

Four solvent extracts of each of Lemongrass (Symbopogon citratus), Santonica (Artemisia cinae) and Pomegranate (Punica granatum) were tested against the 3rd instar larvae of Chrysomyia albiceps. The pomegranate extracts showed the larvicidal activity with LC50 ranging between 25 ppm (acetone extract) and 280 ppm (chloroform extract). The Santonica showed larvicidal activity with LC50 ranging between 48 ppm (ethanol extract) and 380 ppm (acetone extract). The Lemongrass showed activity with LC50 ranging between 135 ppm (ethanol extract) and 570 ppm (chloroform extract). So, the most effective action in accordance to LC50 were the acetone extract of pomegranate, followed by ethanol extract of Santonica and lastly ethanol extract of Lemongrass. The slope functions of these three extracts were 4.6, 2.8 and 8.22 respectively. The shift to insect control by plant extracts pave the way to a somewhat healthy environment.     

Inhibitory activity of cigarette-smoke condensate on the mutagenicity of heterocyclic amines

Cigarette-smoke condensate (CSC) is a complex mixture containing over 3800 identified chemicals including nicotine, water, mutagens, antimutagens, cytotoxins and inert chemicals. Although CSC is mutagenic in the Ames test, its effect on the activity of other mutagens has not been characterized. Using the Ames Salmonella bacterial mutagenesis assay, we found CSC exerts a significant inhibitory effect on mutagens requiring bioactivation. Those studied included heterocyclic amines (Glu-P-1, Glu-P-2, IQ, MeIQ, Trp-P-1 and Trp-P-2), benzo[a]pyrene (B[a]P) and aflatoxin B1. However, CSC had no effect on the activity of direct-acting mutagens (2-nitrofluorene, sodium azide, 4-nitro-1,2-phenylenediamine, 4-nitroquinoline N-oxide and methyl methanesulfonate). With indirect-acting mutagens, the reduced number of revertants observed in the presence of CSC was not attributable to cytotoxicity. CSC exhibited a potent inhibitory effect on the cytochrome P-450 dependent monooxygenases, ethoxyresorufin O-deethylase and B[a]P hydroxylase. This suggests inhibition of the cytochrome P-450 isozymes as one possible mechanism for the antimutagenicity of CSC. Fractionation studies of CSC revealed that the neutral, weakly acidic (phenolic) and basic fractions are all effective as antimutagens against Glu-P-1, a representative heterocyclic amine. This indicates that several classes of chemicals contribute to the inhibitory effect of CSC on the mutagenicity of the heterocyclic amines.     

The influence of some compounds commonly used in biochemical studies of mitochondria on the activity of monoamine oxidases

It was previously described that low concentrations of sodium azide monoamine oxidase (MAO) B assayed by spectrophotometric measurement of benzaldehyde or by hydrogen peroxide accumulation. We failed to confirm this effect using radiometric determination of MAO activity. Tris or dinitrophenol inhibit MAO. The data suggest that some "regulatory effects" depend on the assay of MAO activity.     

Lupus anticoagulant activity of some antiphospholipid antibodies against phospholipid bound beta 2 glycoprotein I

AIMS: To determine whether beta 2 glycoprotein I (beta 2GPI) dependent anticardiolipin (aCL) antibodies detected in solid phase enzyme linked immunosorbent assays can also have lupus anticoagulant activity. METHODS: Six anticardiolipin antibodies were affinity purified from patients with these antibodies and lupus anticoagulant activity in their plasma. RESULTS: The anticardiolipin antibodies bound only to anionic phospholipids in the presence of beta 2GPI and bound to beta 2GPI in the absence of phospholipids. Four out of six had lupus anticoagulant activity in the dilute Russell viper venom time test. CONCLUSIONS: The results show that some beta 2GPI dependent aCL are lupus anticoagulants. It is unclear why only some should have lupus anticoagulant activity while others do not.     

Study of the antiviral activity of some new classes of AS-triazine derivatives (preliminary note)

Monoclonal antibodies were raised to a synthetic peptide corresponding to amino acids 1-29 of the human gonadotropin-releasing hormone (GnRH) receptor. One of the two antibodies was found to recognise GnRH receptors on human pituitary gonadotrophs as determined by immunohistochemistry and supported by Western blotting. The antibody also bound to T47D human breast carcinoma cell line as determined by flow cytometric analysis.     

Modulus of elasticity of some refractory compounds

Conclusions Measurements were made of the moduli of elasticity of nonporous refractory compounds prepared by the method of diffusion impregnation. The following values were obtained: 49,300±2000 kg/mm² for NbN, 58,700±2000 kg/mm² for TaN, 58,000±2000 kg/mm² for NbC, 65,000±2000 kg/mm² for NbB₂, 70,000±2000 kg/mm² for TaB₂, 68,500±2000 kg/mm² for Mo₂B₅, and 79,000±2000 kg/mm² for W₂B₅.Translated from Poroshkovaya Metallurgiya, No. 3 (63), pp. 32–33, March, 1968.