THE LINKAGE OF ELECTRON TRANSPORT CHAINS IN FUSED MEMBRANE PROVED BY MONITORING THE REDUCTION OF CYTOCHROME C

The redox states of cytochrome c (cyt. c) of the respiratory electron transport carriers, in the deficient thylakoid of spinach chloroplast, crista vesicles of liver mitochondria and their combined system were monitored. The reconstituted system prepared by combining deficient thylakoid with crista vesicles showed a higher reductive effects of cyt. c than the system prepared by combining chloroplast and mitochondria. The less inhibition effects of photosynthetic chain and respiratory chain on light-induced reduction of cyt. c in combined system had been observed. Further, with cooperation between photosynthetic chain inhibitor and respiratory inhibitor, the combined system still showed the light-induced cyt, c reductive effects.These results indicated that the deficient thylakoid can combine with crista vesicles in the hypotonic solution to form a fused membrane in which the electron carriers of both energy transfer membranes can link together, and that the linkage of electron carriers may be in multipl     

Synthesis and antibacterial activity of 4“-O-carbamoyl analogs of clarithromycin

<正>A series of novel 4"-O-carbamoyl analogs of clarithromycin were synthesized and evaluated for their in vitro antibacterial activity. All of the desired compounds showed excellent activity against erythromycin-susceptible S.pneumoniae.Particularly,4-fluorobenzyl carbamate 7a demonstrated potent activity against erythromycin-resistant S.pneumoniae encoded by the mef gene,and remarkably improved activity against erythromycin-resistant S.pneumoniae encoded by the erm gene,and the erm and mef genes.     

EFFECT OF nifA PRODUCT ON SUPPRESSION OF Nif~- PHENOTYPE OF gin MUTATION AND CONSTITUTIVE SYNTHESIS OF NITROGENASE IN Klebsiella pneumoniae

This paper describes the role of nifA product on the ammonia regulation of nitrogen fixation in K. pneumoniae. A plasmid carrying nifA gene under the promoter of tetracycline resistance gene was constructed. When this nifA carrying plasmid was introduced into a glnAG mutant, the Nif~-phenotype of this gln mutant was suppressed. Furthermore, when the plasmid was introduced into the wild type and glnAG mutant, derepression of nitrogenase synthesis in ammonia occurred in both strains and the products of nif genes can be detected by two-dimensional gel electrophoresis in the extracts of these ammonia-grown bacterial cells.The constitutive synthesis of nitrogenase in NH_4~ was also demonstrated in free living nitrogen-fixing bacteria, Enterobacter cloacae, when the bacteria received the plasmid carrying nifA gent from K. pneumoniae.     

A Study on the Interaction of the DAS-K with Bovine Serum Albumin by On-line Ultrafiltration and Chemiluminescence

Potassium dehydroandrographolide succinate （DAS-K） has antibacterial and antiviral effects. It has been used widely for the treatment of virus pneumonia, malaria and respiratory infections. In this work, a novel flow-injection chemiluminescence （CL） method for the determination of DAS-K was proposed. The method is based on the reaction between DAS-K and hexacyanoferrate（III） in alkaline solution to give weak CL signal, which is enhanced by rhodamine B. The experimental conditions for the CL reaction were optimized and the possible reaction mechanism was discussed. Under the optimum conditions, the concentration of DAS-K is proportional to the CL intensity in the range of 0.1-80 μmol·L^-1 with a detection limit of 0.05 μmol·L^-1. The interaction of the DAS-K with bovine serum albumin by on-line ultrafiltration and flow-injection chemiluminescence was studied. The concentrations of unbound DAS-K from ultra filter tube were determined by the flow-injection CL method. The binding parameters were estimated by the Scatchard plot and Klotz plot. The proposed system proved that FIA-CL coupled with on-line ultrafiltration sampling was a fast and simple technique for the study of drug-protein interaction.     

Quantification of Erdosteine in the Low-volume of Dog Plasma by Liquid Chromatography Tandem Mass Spectrometry

Introduction Erdosteine[N-(carboxymethylthioacetyl)-homocysteine thiolactone](Fig.1)is a synthetic derivative of natural amino acid methionine[1].It has been commonly used in clinical practice as a mucolytic drug and as an enhancer of respiratory ventilation in the treatment of patients with chronic obstructive respiratory disease.     

Indirect Flow Injection Chemiluminescence Method for the Determination of Tetracyclines Using Cu(Ⅱ) as a Probe Ion

Tetracycline antibiotics (TCs) are active against a wide range of gram-positive and gram-negative bacteria, being extensively used in human and veterinary medicine to treat and prevent bacterial infections1. Among the TCs, TC, OTC and CTC are commercially available and permitted for human administration. However, the degradation products occurring in storage conditions might induce potential adverse effects. Thus, many studies have focused on the development of a rapid, sensitive and reli…     

Comprehensive profiling of lysine acetylome in Staphylococcus aureus

The Gram-positive bacterium Staphylococcus aureus(S.aureus)is a wide spread common opportunistic pathogen that causes a wide variety of infectious diseases,from benign skin infections to life-threatening diseases such as the methicillin-resistant Staphylococcus aureus(MRSA)infection.Although emerging evidence suggests that lysine acetylation may play critical roles in bacterial physiology,the atlas of acetylome in S.aureus has not been studied.To comprehensively profile protein lysine acetylation in S.aureus,we used an integrated approach that combined immune affinity peptide enrichment using anti-lysine acetylation antibody,high-pH HPLC fractionation,and HPLC/mass spectrometry analysis.This study led to the identification of 1361 non-redundant acetylation sites on 412 proteins found in a search of S.aureus protein database extracted from the Swiss-Prot database.We further performed bioinformatic analysis to characterize this modification,including gene ontology annotation,protein-protein interaction,and domain analysis of the acetylation sites.We found that the acetylated proteins were enriched in multiple biological pathways,such as ribosomal function and energy metabolism.Our data provides a rich source for functional studies of lysine acetylation in S.aureus.     

Synthesis of Clarithromycin Using Protective Technique of Total Silylation

Clarithromycin, 6- O-methylerythromycin A (CAM), is a semisynthetic macrolide antibiotic of 6 which exhibits strong antibacterial activity toward a wide range of bacteria inclusive of gram positive bacteria, some gram negative bacteria, anaerobic bacteria, Mycoplasma, Chlamidia and Helicobacter pylori, and because of its high stability in the acidic environment of the stomach, it can be orally administered to treat respiratory organ diseases, and also to prevent recurrence of ulcer when used in a combination with other medicines.     

MULTISTAGE EVALUATION SCALE, DIFFER ENTIAL THRESHOLD STEPS AND EQUIVALENT SENSATION CON TOURS OF RESPIRATORY FLOW-RESISTIVE LOAD SENSATION

This paper presents and discusses the methodology and results of studies on respiratory sensation byusing a fuzzy set category judgement model and applying the concept of just noticeable difference (JND)step and equivalent sensation. A new kind of category scale, the multistage evaluation scale (MES), based on a fuzzy set categoryjudgement model for quantifying respiratory sensory magnitude has been put forward and verified in 37subjects. The perceived magnitude of added resistance estimated using MES could reflect properly thedifference in sensory perception caused by added loads with equal intensity but applied to different phasesof the breathing cycle. In addition, the psychophysical function obtained conforms to the Stevens' powerlaw. On the contrary, the classical category scale does not possess some of these attributes. In 9 subjects, we determined that the sensory continuum corresponding to either inspiratory or ex-piratory added resistive load, ranging 10-500 mm H_2O· 1~(-1)·s, consisted of 6     

An eco-friendly water mediated synthesis of 1,2,3-triazolyl-2- aminopyrimidine hybrids as highly potent anti-bacterial agents

An elegant and efficient synthesis of novel 1,2,3-triazole fused 2-aminopyrimidine hybrids has been accomplished for the first time in the green solvent viz. water. The hybrid molecules exhibit significant anti-bacterial activity when screened against three human pathogens viz. Staphylococcus aureus, Pseudomonas aeruginosa and Klebsiella pneumoniae. In comparison to the commercially marketed drug tetracycline, some of them are equally potent and a few are more potent.     

Structure-Activity Relationship of Fluoroquinolones Against K:pneumoniae

The structure-activity relationship of °uoroquinolones, which show anti-K. pneumoniae activity, was studied by using principal component analysis (PCA) and hierarchical cluster analysis (HCA). The PCA results showed that the lowest unoccupied molecular orbital energy, energy difference between the highest occupied and the lowest unoccupied molecular orbital, dipole moment, net atomic charge on atom I, molecular polarizability, partition coe±cient and molecular refractivity of these compounds are responsible for the separation between high-activity and low-activity groups. The HCA results were similar to those obtained with PCA. By using the chemometric results, four synthetic compounds were analyzed through PCA and HCA, and three of them are proposed as active molecules against K. pneumoniae which is consistent with the results of clinical experiments. The methodologies of PCA and HCA provide a reliable rule for classifying new °uoroquinolones with anti-K. pneumoniae activity.     

Application of PCA and HCA to the Structure-activity Relationship （SAR） Study of Fluoroquinolones

1 INTRODUCTION The earliest antibacterial agents used as chemo- therapeutic drugs in the 1920s were synthetic agents, such as sulponamides. Since the discovery of peni- cillin and its entry into clinical use in the 1940s, the field has been dominated over the past 50 years by natural products or their semi-synthetic derivatives. The fluoroquinolones are the only synthetic anti- bacterial agents to rival β-lactams for impact in clinical usage in the antibacterial field. In recent years, …