Modified Fluoroquinolones as Antimicrobial Compounds Targeting Chlamydia trachomatis

Chlamydia trachomatis causes the most common sexually transmitted bacterial infection and trachoma, an eye infection. Untreated infections can lead to sequelae, such as infertility and ectopic pregnancy in women and blindness. We previously enhanced the antichlamydial activity of the fluoroquinolone ciprofloxacin by grafting a metal chelating moiety onto it. In the present study, we pursued this pharmacomodulation and obtained nanomolar active molecules (EC₅₀) against this pathogen. This gain in activity prompted us to evaluate the antibacterial activity of this family of molecules against other pathogenic bacteria, such as Neisseria gonorrhoeae and bacteria from the ESKAPE group. The results show that the novel molecules have selectively improved activity against C. trachomatis and demonstrate how the antichlamydial effect of fluoroquinolones can be enhanced.     

Antidiabetic Drugs in the Treatment of Alzheimer’s Disease

The public health burden of type 2 diabetes mellitus and Alzheimer’s disease is steadily increasing worldwide, especially in the population of older adults. Epidemiological and clinical studies suggest a possible shared pathophysiology between the two diseases and an increased risk of AD in patients with type 2 diabetes mellitus. Therefore, in recent years, there has been a substantial interest in identifying the mechanisms of action of antidiabetic drugs and their potential use in Alzheimer’s disease. Human studies in patients with mild cognitive impairment and Alzheimer’s disease have shown that administration of some antidiabetic medications, such as intranasal insulin, metformin, incretins, and thiazolidinediones, can improve cognition and memory. This review aims to examine the latest evidence on antidiabetic medications as a potential candidate for the treatment of Alzheimer’s disease.     

Neurochemical Alterations in Social Anxiety Disorder (SAD): A Systematic Review of Proton Magnetic Resonance Spectroscopic Studies

(1) Objective: Considering that current knowledge of mechanisms involved in the molecular pathogenesis of Social Anxiety Disorder (SAD) is limited, we conducted a systematic review to evaluate cumulative data obtained by Proton Magnetic Resonance Spectroscopic (¹H MRS) studies. (2) Methods: A computer-based literature search of Medline, EMBASE, PsycInfo, and ProQuest was performed. Only cross-sectional studies using ¹H MRS techniques in participants with SAD and healthy controls (HCs) were selected. (3) Results: The search generated eight studies. The results indicated regional abnormalities in the ‘fear neurocircuitry’ in patients with SAD. The implicated regions included the anterior cingulate cortex (ACC), dorsomedial prefrontal cortex (dmPFC), dorsolateral prefrontal cortex (dlPFC), insula, occipital cortex (OC), as well as the subcortical regions, including the thalamus, caudate, and the putamen. (4) Conclusions: The evidence derived from eight studies suggests that possible pathophysiological mechanisms of SAD include impairments in the integrity and function of neurons and glial cells, including disturbances in energy metabolism, maintenance of phospholipid membranes, dysregulations of second messenger systems, and excitatory/inhibitory neurocircuitry. Conducting more cross-sectional studies with larger sample sizes is warranted given the limited evidence in this area of research.     

Nonresponse analysis and adjustment in a mail survey on car accidents

Statistical accident data plays an important role for traffic safety development involving the road system, vehicle design, and driver education. Vehicle manufacturers use data from accident mail surveys as an integral part of the product development process. Low response rates has, however, lead to concerns on whether estimates from a mail survey can be trusted as a source for making strategic decisions.     

Do Drug-likeness Rules Apply to Oral Prodrugs?

This paper describes a comparative analysis of the physicochemical and structural properties of prodrugs and their corresponding drugs with regard to drug-likeness rules. The dataset used in this work was obtained from the DrugBank. Sixty-five pairs of prodrugs/drugs were retrieved and divided into the following categories: carrier-linked to increase hydrophilic character, carrier-linked to increase absorption, and bioprecursors. We compared the physicochemical properties related to drug-likeness between prodrugs and drugs. Our results show that prodrugs do not always follow Lipinski's Rule of 5, especially as we observed 15 prodrugs with more than 10 hydrogen bond acceptors and 18 with a molecular weight greater than 500 Da. This fact highlights the importance of extending Lipinski's rules to encompass other parameters as both strategies (filtering of drug-like chemical libraries and prodrug design) aim to improve the bioavailability of compounds. Therefore, critical reasoning is fundamental to determine whether a structure has drug-like properties or could be considered a potential orally active compound in the drug-design pipeline.     

Hydrogen treated TiO2 nanoparticles onto FTO glass as photoanode for dye-sensitized solar cells with remarkably enhanced performance

Hydrogen treatment is a facile and efficient approach for the enhancement in the functioning of TiO₂ nanoparticles for dye-sensitized solar cells (DSSC). In this work, TiO₂ nanoparticles have been synthesized in the hydrogen environment followed by the deposition onto FTO glass substrates with various film thickness as photoanodes for DSSC. The synthesized hydrogen treated TiO₂ nanoparticles based photoanodes have showed significantly improved photocurrent in the resulting fabricated devices. SEM and TEM analyses have confirmed the particle size and morphology of TiO₂ nanoparticles at various magnifications. The crystalline structure and phase identification were studied by XRD analysis and Raman spectroscopic measurements. The UV–Vis spectroscopy analysis was carried out to find the response of samples for ultraviolet and visible light. The current-voltage measurements have confirmed the improvement of photocurrent that is principally due to improved photo-activity of hydrogen treated TiO₂ nanoparticles. Moreover, hydrogen treated TiO₂ nanoparticles-based photoanode with the film thickness of 11.65 μm has remarkably enhanced power conversion efficiency of 6.05% in DSSCs. The ability of highly photoactive hydrogen treated TiO₂ nanoparticles will provide the new openings in different fields that include photo-electrochemical water splitting and in many other applications.     

UHPLC-DAD Multi-Method for Determination of Phenolics in Aromatic Plants

The aim of this paper was to develop and validate a method of ultra high-performance liquid chromatography coupled with diode array detector (UHPLC-DAD), which allows quantifying simultaneously 19 phenolic compounds in aromatic plants. Twenty-one fresh and dried aromatic plants were extracted with methanol before their UHPLC-DAD analysis. The method was validated regarding specificity, working range, linearity, limit of detection (LOD) and quantification (LOQ), precision, and accuracy. The developed method allows detecting and quantifying the phenolic compounds at low concentrations (LOD < 0.15 μg/mL, except for carnosol and carnosic acid). The relative standard deviation obtained was lower than 5.73 and 8.75%, for repeatability and intermediate precision, respectively. The proposed method is straightforward and sensitive, with good precision and accuracy. Dried thyme presented the highest diversity of phenolic compounds and rosmarinic acid was present in most of the samples. This analytical tool is a valid alternative to conventional methods to quantify phenolic compounds in aromatic plants or in their extracts.     

Influence of B-site cations ordering on magnetization and dielectric relaxations in Li–Ni spinel ferrites

Ho-substituted Li–Ni ferrites with composition L i_1.2Ni_0.4Ho_xFe_2-xO₄; 0≤ x ≤ 0.15 were synthesized by a self-ignited sol-gel process. An annealing temperature of 950 °C is estimated via thermal-gravimetric (TGA) analysis. X-ray diffraction (XRD) scans have confirmed the formation of the ferrite phase with a spinel structure in all samples. Substitution of Ho ions on the B-site significantly reduced the porosity from 38 -to 23% and the crystallite size from 23.4 -to 21.7 nm. Microstructural analysis revealed a denser structure with an increase in Ho content. Dielectric results showed that both the dielectric loss and dielectric constant depict a nonlinear variation with the addition of Ho. Complex impedance behavior with a single semicircle for all samples suggests the predominant effect of the grain boundary mechanism. The substitution of Ho ions in place of Fe ions significantly decreased the electrical conductivity. The anisotropic Ho³⁺ ions reinforce the L-S coupling which consequently enhanced the coercive force from 145 -to 389 Oe, and thus the anisotropy constant.     

Quality assurance and authentication of herbal drug (Argyrolobium roseum and Viola stocksii) through comparative light and scanning electron microscopy

The quality assurance and authentication of crude herbal drugs play important role in the effective therapeutic effect of herbal drug and their products. There are many reported problems in quality assurance of herbal crude drugs concerning to their correct identification. The present study was designed with the aim to document the authentication and quality assurance of the herbal crude drugs (Argyrolobium roseum and Viola stocksii) thorough light microscopy (LM) and scanning electron microscopy (SEM). The detailed foliar anatomical studies showed polygonal epidermal cells having anticlinal walls in Argyrolobium roseum while rounded epidermal cells were observed in Viola stocksii. The anomocytic stomata type was observed in Argrolobium roseum while actinocytic was noticed in Viola stocksii. The pollen of studied species appeared as tricolporate showing reticulate exine sculpturing in Argrolobium roseum while fine perforations were recorded in Viola stocksii. Furthermore, quantitative analysis of phenols, flavonoids, and antioxidant activity showed high flavonoid and phenol content in Argyrolobium roseum as compared with Viola stocksii. It was observed that Argyrolobium roseum was discriminated from the Viola stocksii based on the leaf and pollen micromorphological traits by using LM and SEM techniques. It was concluded that LM and SEM techniques were found useful for the quality assurance of botanicals and their authentication.