A series of novel balofloxacin ethylene isatin derivatives with remarkable improvement in lipophilicity, as compared to the parent compound balofloxacin, were designed, synthesized and characterized by 1H NMR, MS and HRMS. These derivatives were initially evaluated for their in vitro antimycobac...

Increasingly isolated frequency of antibiotic-resistant V. alginolyticus strains in clinic and aquaculture has been reported, but the mechanisms of V. alginolyticus antibiotic resistance are largely absent. In the present study, native/SDS-PAGE based proteomics, which may provide information on ...

Fluoroquinolone antibiotics (FQs) are ubiquitous and ionisable in surface waters. Here we investigate gatifloxacin (GAT) and balofloxacin (BAL), two widely used FQs, and determine the photochemical reactivity of their respective dissociation species that arise at different pH to understand the r...

Balofloxacin is a fluroquinolone antibiotic drug which has been used for the treatment of urinary tract infections (UTIs). Identification and structural characterization of metabolites is a critical component of both drug discovery and drug development research. In vivo metabolites of balofloxac...

The overuse of antibiotics to control bacterial pathogens leads to the generation of their antibiotic-resistant strains including Edwardsiella tarda. Understanding of mechanisms of the antibiotic resistance is crucial to develop novel methods to manage the infection. Here, two-dimensional electr...

Effects of noncompetitive and competitive NMDA receptor antagonists have been repeatedly characterized using place conditioning models. The present study aimed to characterize the effects in mice of another NMDA receptor antagonist acting at polyamine binding site, eliprodil. Five-day conditioni...

The nephritogenostde peptide fragment could be successfully synthesized using the Fmoc/Bzl strategy, coupling the fully protected Asp(OBzl) fragment 3–10, produced in high purity on a 2-chlorotrityl support, to the N-terminal glycine residue of the resin-bound C-terminal segment 11–21 and ther...

The barks of Aegiphila lhotzkyana and A. obducta contain several 24-ethyl- and 24-methylsterols. Among these, stigmasterol, clerosterol, 22-dehydroclerosterol, and the respective β-glucosides were the dominant sterols. The glucoside of 22-dehydroclerosterol is described for the first time. The ...

Background/Aims: Gastric motor disturbances, associated with a delay in gastric emptying, occur in patients with the irritable bowel syndrome. The influence of fedotozine and κ agonists on the cologastric reflex produced by nonpainful colonic distention was evaluated in conscious dogs. Methods:...

Background: Fedotozine is a peripheral opioid agonist. Its effects were assessed in experimental ileus in rats. Methods: Ileus was induced by abdominal surgery (laparotomy and cecum palpation) or peritonitis (acetic acid, intraperitoneally). Digestive motility was recorded by electromyography an...

The effect of fedotozine was evaluated in a model of colonic hypersensibility to balloon distension in anesthetized rats. Acetic acid (0.6%, intracolonically) significantly enhanced the hypotension reflex response to colonic distension (P

Background & Aims: Visceral hypersensitivity plays a major role in the pathophysiology of inflammatory bowel syndrome (IBS). Opioid κ receptors on afferent nerves may modulate it and may be the target of new IBS treatments. The aim of this study was to evaluate the effects of fedotozine, a pote...

The effect of fedotozine on visceral hypersensitivity was evaluated in conscious rats. One hour after colonic irritation (0.6% acetic acid intracolonically), a 30 mmHg colonic distension was applied for 10 min. Irritation increased the number of abdominal contractions induced by colonic distensi...

Fedotozine is a kappa opioid receptor agonist having antinociceptive properties but devoid of diuretic effects. The aim of the study was to evaluate the discriminative stimulus effects of fedotozine at doses previously reported to produce maximal effects in in vivo assays measuring kappa-mediate...

Ginsenosides have been reported to possess pharmacological effects, such as antioxidative, anti-inflammatory and antitumor effects. Nevertheless, little has been reported about the anti-breast cancer effects of ginsenoside Rk1 (Rk1). In this work, we explored the anti-breast cancer effects of Rk...

BackgroundGinsenoside Rh2 (Rh2), an important ingredient from Panax ginseng, has received much attention due to a range of pharmacological actions.

BackgroundGinsenosides have been reported to have many health benefits, including anti-inflammatory effects, and the resolution of inflammation is now considered to be an active process driven by M2-type macrophages. In order to determine whether ginsenosides modulate macrophage phenotypes to re...

Given the limited studies and conflicting findings, the transport character of ginsenosides crossing the blood–brain barrier (BBB) remains unclear. The present study was designed to qualitatively determine the distribution of ginsenosides in brain tissues after oral administration of ginseng to...

BackgroundPanax ginseng is a physiologically active plant widely used in traditional medicine that is characterized by the presence of ginsenosides. Rb1, a major ginsenoside, is used as the starting material for producing ginsenoside derivatives with enhanced pharmaceutical potentials through ch...

Sepsis-induced acute lung injury (ALI) is a life-threatening medical condition with high mortality and morbidity in the critical care units. Though, it was commonly accepted that inflammation and apoptosis of lung epithelial cells played an essential role in the pathogenesis of ALI, the underlyi...