Analysis of intestinal bacterial carboxylesterase-mediated metabolites and the potential antitumour molecular mechanism of angoroside C.

Angoroside C (AgrC) is a compound with many pharmacological properties. However, its antitumour potential has not been well studied. The low bioavailability of AgrC suggests a strong link to gut bacteria.

GLP-1 receptor agonists for the treatment of obesity: Role as a promising approach.

Obesity is a complex disease characterized by excessive fat accumulation which is caused by genetic, environmental and other factors. In recent years, there has been an increase in the morbidity, disability rate,and mortality due to obesity, making it great threat to people's health and lives, and increasing public health care expenses. Evidence from previous studies show that weight loss can significantly reduce the risk of obesity-related complications and chronic diseases.

Hydroxyurea ameliorates atherosclerosis in ApoE mice by potentially modulating Niemann-Pick C1-like 1 protein through the gut microbiota.

The efficacy and mechanism of hydroxyurea in the treatment of atherosclerosis have rarely been reported. The goal of this study was to investigate the efficacy of hydroxyurea in high-fat diet-fed ApoE mice against atherosclerosis and examine the possible mechanism underlying treatment outcomes. ApoE mice were fed a high-fat diet for 1 month and then administered hydroxyurea by gavage continuously for 2 months.

Rationale and methods of the Antioxidant and NMDA receptor blocker Weans Anoxic brain damage of KorEa OHCA patients (AWAKE) trial.

Background: Ischemic brain injury is a major hurdle that limits the survival of resuscitated out-of-hospital cardiac arrest (OHCA).

Methods: The aim of this study is to assess the feasibility and potential for reduction of ischemic brain injury in adult OHCA patients treated with high- or low-dose Neu2000K, a selective blocker of N-methyl-D-aspartate (NMDA) type 2B receptor and also a free radical scavenger, or given placebo. This study is a phase II, multicenter, randomized, double-blinded, prospective, intention-to-treat, placebo-controlled, three-armed, safety and efficacy clinical trial.

Low molecular mass chondroitin sulfate suppresses chronic unpredictable mild stress-induced depression-like behavior in mice.

The present study is aimed at testing the antidepressant--like effects and probable mechanisms of action of low molecular mass chondroitin sulfate (LMMCS) on depression induced by chronic unpredictable mild stress (CUMS) in mice. Four weeks of CUMS exposure resulted in depressive-like behavior, expressed by a significant decrease in the locomotor activity and sucrose consumption and increased immobility time in the forced swim test. Further, there was a significant reduction of 5-HT level in the hippocampus region of depressed mice.

Isoflurane produces antidepressant effects inducing BDNF-TrkB signaling in CUMS mice.

Rationale: The volatile anesthetic isoflurane is suggested to produce a rapid and robust antidepressive effect in preliminary clinical trials. Recently, isoflurane was found to activate the tropomyosin receptor kinase B (TrkB) signaling which is the underlying mechanism of the rapid antidepressant ketamine.

Objective: Our study investigated the effect of isoflurane anesthesia on chronic unpredictable mild stressed (CUMS) model in mice and verified the role of brain-derived neurotrophic factor (BDNF)/TrkB/ the mammalian target of rapamycin (mTOR) signaling in the antidepressant effect of isoflurane.

Full dose, half dose, or discontinuation of etanercept biosimilar in early axial spondyloarthritis patients: a real-world study in China.

Introduction: To investigate the effect of dose maintenance, reduction, or discontinuation of the etanercept biosimilar Yisaipu (YSP) on early axial spondyloarthritis (axSpA) patients in remission with YSP 50 mg once weekly (QW).

Material And Methods: Patients were enrolled in three groups: full dose (YSP50), half dose (YSP25), and discontinuation (YSP0). Patients were assessed by the same rheumatologist every 8 weeks for 48 weeks.

A convenient method for the enantiomeric separation of α-amino acid esters as benzophenone imine Schiff base derivatives.

A convenient liquid chromatographic method for the separation of α-amino acid esters as benzophenone Schiff base derivatives on coated chiral stationary phases (CSPs) (Chiralcel OD-H, Chiralcel OD, Chiralpak AD-H, Chiralpak AD, and Chiralpak AS) or covalently immobilized CSPs (Chiralpak IA, Chiralpak IB, and Chiralpak IC) derived from polysaccharide derivatives is described. Benzophenone imine derivatives of α-amino acid esters were readily prepared by stirring benzophenone imine and the hydrochloride salts of α-amino acid esters in 2-propanol. The chromatographic separations were conducted at a flow rate 1.

Beta1-adrenergic receptor activation decreases ANP release via cAMP-Ca2+ signaling in perfused beating rabbit atria.

Aims: Although a beta-adrenoceptor (beta-AR) blockade-induced increase in plasma atrial natriuretic peptide (ANP) levels is implicated in the therapeutic significance of beta-AR antagonists, the role of beta-AR in the regulation of ANP release is not clearly defined. The purpose of the present study was to define the role of beta-AR subtypes and the mechanisms responsible for regulation of atrial ANP release.

Main Methods: Experiments were performed in isolated perfused beating rabbit atria, including measurement of atrial contractile response, cAMP efflux, and atrial myocyte ANP release.

[The clinical characters of 30 patients with enteropathic arthritis and literature review].

Objective: To better understand the clinical characters of enteropathic arthritis patients.

Methods: The clinical, laboratory and X-rays data of 30 enteropathic arthritis in-patients were analyzed.

Results: Among the 30 patients, 14 were male, 16 were female.

Increase of atrial ANP release by 2,3-butanedione monoxime in beating rabbit atria.

2,3-Butanedione monoxime (BDM) is a chemical phosphatase and has been known to dissociate mechanical contraction in the excitation-contraction coupling via inhibition of myofibrillar ATPase. BDM has also been found to decrease sarcolemmal L-type Ca(2+) channel activity and intracellular Ca(2+) in cardiac myocytes. It has been shown that Ca(2+) entry via L-type Ca(2+) channels decreased atrial myocyte atrial natriuretic peptide (ANP) release.

Cardiac mast cells regulate myocyte ANP release via histamine H2 receptor in beating rabbit atria.

It has been shown that histamine inhibits atrial natriuretic peptide (ANP) release. Because cardiac mast cells are the principal source of histamine in the heart, we hypothesized that cardiac mast cells are involved in the regulation of atrial ANP release. To test the hypothesis, experiments were performed in perfused beating rabbit atria allowing atrial pacing and measurements of changes in atrial stroke volume, intraatrial pulse pressure and myocyte ANP release.

Comparative studies between covalently immobilized and coated chiral stationary phases based on polysaccharide derivatives for enantiomer separation of N-protected alpha-amino acids and their ester derivatives.

Liquid chromatographic enantiomer separation of several N-benzyloxycarbonyl (CBZ) and N-tert-butoxycarbonyl (BOC) alpha-amino acids and their corresponding ethyl esters was performed on covalently immobilized chiral stationary phases (CSPs) (Chiralpak IA and Chiralpak IB) and coated-type CSPs (Chiralpak AD and Chiralcel OD) based on polysaccharide derivatives. The solvent versatility of the covalently immobilized CSPs in enantiomer separation of N-CBZ and BOC-alpha-amino acids and their ester derivatives was shown and the chromatographic parameters of their enantioselectivities and resolution factors were greatly influenced by the nature of the mobile phase. In general, standard mobile phases using 2-propanol and hexane on Chiralpak IA showed fairly good enantioselectivities for resolution of N-CBZ and BOC-alpha-amino acids and their esters.

Comparison of several polysaccharide-derived chiral stationary phases for the enantiomer separation of N-fluorenylmethoxycarbonyl alpha-amino acids by HPLC.

The liquid chromatographic enantiomer separation of N-fluorenylmethoxycarbonyl (FMOC) protected alpha-amino acids was performed on nine polysaccharide-derived chiral stationary phases (CSPs). The cellulose derived coated CSPs, Chiralcel OD-H (separation factor = 1.09-2.

Liquid chromatographic enantiomer resolution of N-hydrazide derivatives of 2-aryloxypropionic acids on a crown ether derived chiral stationary phase.

The liquid chromatographic separation of the enantiomers of several N-hydrazide derivatives of 2-aryloxypropionic acids was performed on a crown ether type chiral stationary phase derived from (18-crown-6)-2,3,11,12-tetracarboxylic acid. The behavior of chromatographic parameters by the change of mobile phases and additives for the resolution of these analytes was investigated. The enantiomers of all analytes were base-line resolved with a mobile phase of 100% methanol containing 20 mM H2SO4.

Osmoregulation of atrial myocytic ANP release: osmotransduction via cross-talk between L-type Ca2+ channel and SR Ca2+ release.

Hyperosmolality has been known to increase ANP release. However, its physiological role in the regulation of atrial myocytic ANP release and the mechanism by which hyperosmolality increases ANP release are to be defined. The purpose of the present study was to define these questions.

High and low gain switches for regulation of cAMP efflux concentration: distinct roles for particulate GC- and soluble GC-cGMP-PDE3 signaling in rabbit atria.

This study tests the hypothesis that particulate (p) guanylyl cyclase (GC) and soluble (s) GC are involved in the distinct roles for the regulation of cGMP-PDE-cAMP signaling and of mechanical and secretory functions in the heart. Experiments were performed in perfused beating rabbit atria. C-type natriuretic peptide (CNP) and SIN-1, an NO donor, or BAY 41-2272 (BAY), a direct activator for sGC, were used to activate pGC and sGC, respectively.

Histamine inhibits atrial myocytic ANP release via H2 receptor-cAMP-protein kinase signaling.

Changes in cyclic nucleotide production and atrial dynamics have been known to modulate atrial natriuretic peptide (ANP) release. Although cardiac atrium expresses histamine receptors and contains histamine, the role of histamine in the regulation of ANP release has to be defined. The purpose of the present study was to define the effect of histamine on the regulation of ANP release in perfused beating rabbit atria.

Subtype-specific roles of cAMP phosphodiesterases in regulation of atrial natriuretic peptide release.

cAMP is known to control the release of atrial natriuretic peptide. To define the roles of cyclic nucleotide phosphodiesterase subtypes in the regulation of atrial natriuretic peptide (ANP) release, experiments were done with perfused beating rabbit atria. Phosphodiesterase 3 subtype-specific inhibitors, milrinone and cilostamide, inhibited myocytic ANP release with a concomitant increase in cAMP efflux.

Protein kinase-dependent and Ca(2+)-independent cAMP inhibition of ANP release in beating rabbit atria.

Regulation of atrial release of atrial natriuretic peptide (ANP) is coupled to changes in atrial dynamics. However, the mechanism by which mechanical stretch controls myocytic ANP release must be defined. The purpose of this study was to define the mechanism by which cAMP controls myocytic ANP release in perfused, beating rabbit atria.