Pogostone Enhances the Antibacterial Activity of Colistin against MCR-1-Positive Bacteria by Inhibiting the Biological Function of MCR-1

The emergence of the plasmid-mediated colistin resistance gene mcr-1 has resulted in the loss of available treatments for certain severe infections. Here we identified a potential inhibitor of MCR-1 for the treatment of infections caused by MCR-1-positive drug-resistant bacteria, especially MCR-1-positive carbapenem-resistant Enterobacteriaceae (CRE). A checkerboard minimum inhibitory concentration (MIC) test, a killing curve test, a growth curve test, bacterial live/dead assays, scanning electron microscope (SEM) analysis, cytotoxicity tests, molecular dynamics simulation analysis, and animal studies were used to confirm the in vivo/in vitro synergistic effects of pogostone and colistin. The results showed that pogostone could restore the bactericidal activity of colistin against all tested MCR-1-positive bacterial strains or MCR-1 mutant–positive bacterial strains (FIC < 0.5). Pogostone does not inhibit the expression of MCR-1. Rather, it inhibits the binding of MCR-1 to substrates by binding to amino acids in the active region of MCR-1, thus inhibiting the biological activity of MCR-1 and its mutants (such as MCR-3). An in vivo mouse systemic infection model, pogostone in combination with colistin resulted in 80.0% (the survival rates after monotherapy with colistin or pogostone alone were 33.3% and 40.0%) survival at 72 h after infection of MCR-1-positve Escherichia coli (E. coli) ZJ487 (blaNDM-1-carrying), and pogostone in combination with colistin led to one or more order of magnitude decreases in the bacterial burdens in the liver, spleen and kidney compared with pogostone or colistin alone. Our results confirm that pogostone is a potential inhibitor of MCR-1 for use in combination with polymyxin for the treatment of severe infections caused by MCR-1-positive Enterobacteriaceae.     

β-cyclodextrin Sensitized Spectrofluorimetry for the Determination of Abiraterone Acetate and Abiraterone

A novel spectrofluorimetric method to determine abiraterone acetate and its active metabolite, abiraterone was developed, based on the fact that fluorescence intensity of abiraterone acetate and abiraterone could be enhanced in β-cyclodextrin (β-CD) due to the formation of the inclusion complex. The inclusion interaction of β-CD and abiraterone acetate and the β-cyclodextrin sensitized spectrofluorimetry was examined. The various factors influencing fluorescence were discussed in details. The results showed that under the optimized conditions, the linear range of calibration curve for the determination of biraterone acetate and abiraterone was 0.20?~?6.0 μg/mL, and the detection limit (LOD) was 6.8 (r?=?0.997) or 6.6 ng/mL (r?=?0.996), respectively. No interference was observed from common co-existing substances or pharmaceutical excipient. The method was successfully applied to the analysis of abiraterone acetate in pharmaceutical formulation and abiraterone in human serum/urine.     

Anionic surfactant selective electrode for the titrimetric determination of anionic surfactant

The construction and characteristic performance of a PVC membrane electrode responsive for sodium dodecylsulfate (SDS) are described in this paper. The electrode based on CTA⁺DS^? ion pair as ionophore in PVC membrane displays a Nernstian slope of ?58.8 ± 0.7 mV/decade in a 1.32 × 10^?6 to 3.75 × 10^?3 mol L^?1 concentration range and a limit of detection of 1.13 × 10^?6 mol L^?1. The electrode can be used for 3 months without showing significant changes in the value of slope or working range. The electrode has been utilized as an end point indicator electrode for potentiometric titration involving Hyamine as titrant. More than 100 titrations were carried out for the evaluation of the electrode parameters: the standard deviations of the equivalent volume and the equivalent potential, the height of the potential jump and the number of faulty titrations. The behavior of the electrode was assessed with regard to their usefulness in routine analysis.     

UPLC-ELSD Determination of 1-Octacosanol in Raw Material and Health Products

Determination of the levels of 1-octacosanol is important in food stuff for the study of its pharmacological activities and health benefits. In this study, a novel, simple and fast internal standard method for the non-derivatization ultra-performance liquid chromatographic determination of 1-octacosanol in raw materials and health products was developed and validated based on evaporative light scattering detection. The linearity (r ² > 0.998), recovery (99.1–100.2%, RSD <2.7%), intra- and inter-day precision (RSD <3.8%), limit of detection (1.0 mg/L), limit of quantification (2.2 mg/L) of the 1-octacosanol were determined. The method was successfully applied to nine real 1-octacosanol products. The results of analyses had close agreement with the labeled claims of 1-octacosanol content in these products. Compared with the classical gas chromatography method, the developed method was simpler, faster and more environmentally friendly due to avoiding any derivatization step. This protocol represents a rapid and feasible method for quality control of 1-octacosanol products.

     

准弹性激光光散射在血细胞检测中的应用

本文利用准弹性激光散射法和细胞电泳法对不同哺乳动物的红细胞,淋巴细胞、粒细胞进行检测,结果表明在一定条件下,不同类型的血细胞平均电泳速度有明显差别。这一结果为光散射法应用于血细胞检测提供了可能性。     

Hulthen势与谱生成代数

本文将Hulthen势场中的S波径向方程作适当的变量变换、使其可用so(2.1)李代数求解;进而通过倾斜变换引入附加参数ω以改善解的收敛性,并给出了迭代求解的全部计算公式。