Research Progress of Ketolide Antibiotics

Macrolide antibiotics have been widely used in clinic due to their good antibacterial effects and high safety, but the drug-resistant bacteria appear constantly. To solve the problem of drug resistance in pathogens, scholars obtain the third generation of macrolide antibiotics, ketolide antibiotics, which are developed by modifying the structure of macrolide antibiotics, thereby efficiently solving the problem. Ketolide antibiotics are a type of erythromycin derivatives with macrolide structure, and the typical drugs mainly include telithromycin, cethromycin and solithromycin, etc . This paper briefly introduced the recent progress of ketolide antibiotics, with an attempt to provide help to the research and development of new macrolide antibiotics.

Neutral Complex Extraction and Synergistic Extraction of Macrolide Antibiotics

Based on the theory of reactive extraction, new solvent systems were developed to replace butylacetate for extraction of macrolide antibiotics (erythromycin, kitasamycin, spiramycin meleumycin etc.). A new neutral complex solvent extraction system, fatty alcohol-kerosene (marked by El), was used for extraction of erythromycin, one of the macrolide antibiotics. The extraction equilibrium equation is obtained, and the extraction distribution is as followsD = exp (-36.33×103/RT + 18.77)[B](o)1.1/(1 + 108.07-PH)The effects of several parameters on extraction equilibrium were investigated. Furthermore, a new synergistic extraction system (marked by E2) was developed, in which another solvent was used as synergistic agent to replace the diluent kerosene in the neutral complex extraction system. Based on these new extraction systems, an improved process for extraction of erythromycin was developed, showing remarkable advantages in technology and economics owing to its low solvent consumption of 3kg per billion unit compared with 9—10 for butylacetate. The recovery process of solvent from raffinate may be eliminated.

Investigation on the Veterinary Antibiotics Contamination in Groundwater with SPE-LC/MS/MS

[Objective]The aim is to provide data support for the prevention and control of pollution of exogenous chemical in pig breeding industry.[Methods]Solid-phase extraction（SPE）and tandem mass（LC-MS/MS）were used for determining four classes（tetracyclines,quinolones,macrolides and sulfonamides）of 10 common veterinary antibiotics in groundwater of an important pig breeding base in the Yangtze River Delta region of China.[Results]Results revealed the total concentration of the ten antibiotics in urban rivers ranged from 20.1 ng /L to 61.2 ng /L.The highest proportion was taken by tetracyclines,account for 95%,the concentration was up to 44.0 ng /L.Quinolones shared the second largest proportion of total concentration,about 29%,the concentration was up to 21.6 ng /L,while concentration of sulfonamides and macrolides were respectively below 2.7 ng /L and 6.3 ng /L.The highest total concentration of the ten antibiotics in rural rivers was up to 467 ng /L,60% of which was shared by tetracyclines,the highest concentration of tetracyclines was 253 ng /L.Sulfonamides share 20% of the total concentration,the highest concentration of it was 165 ng /L.The highest concentration of macrolides and quinolones was 14.6 ng /L and 14.5 ng /L,respectively.[Conclusion] Antibiotics＇ pollution in town rivers is more serious than urban rivers＇ pollution caused by antibiotics.

Advances in Medical Treatment of Primary Aldosteronism

Primary aldosteronism(PA)is the most common form of secondary hypertension,with its main manifestations including hypertension and hypokalemia.Early identification of PA is extremely important as PA patients can easily develop cardiovascular complications such as atrial fibrillation,stroke,and myocardial infarction.The past decade has witnessed the rapid advances in the genetics of PA,which has shed new light on PA treatment.While surgery is the first choice for unilateral diseases,bilateral lesions can be treated with mineralocorticoid receptor antagonists(MRAs).The next-generation non-steroidal MRAs are under investigations.New medications including calcium channel blockers,macrophage antibiotics,and aldosterone synthase inhibitors have provided a new perspective for the medical treatment of PA.

Pathogenicity and Antimicrobial Resistance in Coagulase-Negative Staphylococci

The coagulase-negative staphylococci (CoNS) group was considered saprophytic or rarely pathogenic for many years. Since the first case of septicemia caused by CoNS, there has been a progressive increase in the prevalence of healthcare-associated infections caused by CoNS. The CoNS group has emerged as one of the main causes of nosocomial infections related to vascular catheters and prostheses, especially among immunocompromised patients. This gradual increase in infections is due to the change in the relationship between patients and procedures since CoNS are closely related to devices implanted in the human body. CoNS are successful in colonizing the host because they have several virulence mechanisms, such as biofilm formation and production of enzymes and toxins, in addition to several mechanisms of resistance to antimicrobials. Despite their great clinical relevance, few studies have focused on CoNS’s pathogenicity and resistance to antimicrobials, which reveals the current need to better understand the factors by which this group became pathogenic to humans and other animals. This review aims to synthesize the aspects related to the pathogenicity and antimicrobial resistance in CoNS.

液相色谱-质谱法同时检测畜禽肉中五种大环内酯类抗生素

大环内酯类抗生素(macrolide antibiotics,MALS)对革兰氏阳性菌和支原体有较强的抑制能力,支原体在畜禽中是感染面较广的多发病,因此这类抗生素在动物药品和饲料添加物中占有重要位置.然而,人们在获得经济利益的同时对抗生素的副作用也有了进一步的认识.……

Combined Action of Lysozymes of Fresh-Water Bivalve Mollusks and Antibacterial Preparations against Some Clinical Strains of Microorganisms

The aim of the present study was to determine the MICs using broth microdilution method and their combination effect by （minimum inhibitory concentrations） of selected antibiotic agents determination of FICindex （fractional inhibitory concentrations）. Lysozyme Anodonta cygnea was more active than Lysozyme Uniopictorum, especially against Gram-negative bacterias. Combination of Macropen and Lysozyme Unio pictorum has a synergistic effect, while a separation of these antibacterial agents was not active against some of the strains of microorganisms.

Metabolomic profiles in a green alga (Raphidocelis subcapitata) following erythromycin treatment: ABC transporters and energy metabolism

A recent study showed that erythromycin(ERY)exposure caused hormesis in a model alga(Raphidocelis subcapitata)where the growth was promoted at an environmentally realistic concentration(4μg/L)but inhibited at two higher concentrations(80 and 120μg/L),associated with opposite actions of certain signaling pathways(e.g.,xenobiotic metabolism,DNA replication).However,these transcriptional alterations remain to be investigated and verified at the metabolomic level.This study uncovered metabolomic profiles and detailed toxic mechanisms of ERY in R.subcapitata using untargetedmetabolomics.Themetabolomic analysis showed that metabolomic pathways including ABC transporters,fatty acid biosynthesis and purine metabolism were associated with growth promotion in algae treated with 4μg/L ERY.An overcompensation was possibly activated by the low level of ERY in algae where more resources were reallocated to efficiently restore the temporary impairments,ultimately leading to the outperformance of growth.By contrast,algal growth inhibition in the 80 and 120μg/L ERY treatments was likely attributed to the dysfunction of metabolomic pathways related to ABC transporters,energy metabolism and metabolism of nucleosides.Apart from binding of ERY to the 50S subunit of ribosomes to inhibit protein translation as in bacteria,the data presented here indicate that inhibition of protein translation and growth performance of algae by ERY may also result from the suppression of amino acid biosynthesis and aminoacyl-tRNA biosynthesis.This study provides novel insights into the dose-dependent toxicity of ERY on R.subcapitata.