More than 140 modified ribonucleosides have been identified in RNA. Determination of endogenous modified ribonucleosides in biological fluids may serve as non-invasive disease diagnostic strategy. However, detection of the modified ribonucleosides in biological fluids is challenging, especially ...

Ribonucleosides are the end products of RNA metabolism. These metabolites, especially the modified ribonucleosides, have been extensively evaluated as cancer-related biomarkers. However, the determination of urinary ribonucleosides is still a challenge due to their low abundance, high polarity a...

Two polymorphic crystals (α and β) of 4-hydroxy-1-methylpiperidine betaine hydrochloride, HO-MPBH+·Cl−, have been synthesized and their structures solved by the X-ray diffraction methods. The piperidine ring adopts the chair conformation and the hydroxy group at C(4) in the α-polymorph is in...

A 1:1 complex between N-methylpiperidine betaine and hydrochloric acid, MPBH·Cl, has been characterized by single crystal X-ray analysis, FTIR spectroscopy, and DFT calculations. The crystals are monoclinic, space group P21/n, with a=6.0644(3), b=13.0220(6), c=12.7653(7)Å, β=101.925(5)°. The...

Introduction: The beneficial effects of tiotropium bromide, a long acting anticholinergic bronchodilator, in the management of chronic obstructive pulmonary disease have been shown in previous studies. The present study aimed to compare the efficacy and safety of generic (Tiova®) and brand-name ...

BackgroundRecent evidence suggests that acetylcholine acting through muscarinic receptors may play an inhibitory role in the mechanisms that drive the structural changes in the airways called airway remodeling. The novel anticholinergic drug tiotropium bromide, which selectively antagonizes musc...

ObjectiveTiotropium is a long-acting muscarinic antagonist approved for maintenance treatment of asthma in children, adolescents, and adults in the United States, and recommended as add-on treatment for uncontrolled asthma despite treatment with inhaled corticosteroids and/or long-acting beta-2 ...

Tiotropium bromide is a novel, inhaled, once-daily anticholinergic bronchodilator that has recently been approved in the United States for use in patients with COPD. Its unique feature is the persistence of bronchodilation for > 24 h due to prolonged M3 muscarinic receptor blockade. Tiotropium p...

Recurrent relapses of allergic lung inflammation in asthmatics may lead to airway remodeling and lung damage. We tested the efficacy of tiotropium bromide, a selective long-acting, muscarinic receptor antagonist as an adjunct therapy in relapses of allergic asthma in mice. We compared the effect...

BackgroundThis study aimed to compare rapid improvements in respiratory function and symptoms following single inhalation of formoterol (FOM) dry power inhaler (DPI) or tiotropium bromide (TIO) DPI in patients with chronic obstructive pulmonary disease (COPD).

IntroductionAcute exposure to organic dust (OD) in pig barns induces intense airway inflammation with neutrophilia and hyperresponsiveness. This reaction is likely associated with increased cholinergic activity. Therefore, the involvement of cholinergic mechanisms in the reaction to acute exposu...

BackgroundOral inhalation is the main drug delivery route for treating obstructive lung conditions. Thus, many inhaler devices with various design and pharmaceutical formulation have been introduced. The fine particle dose (FPD) and mass median aerodynamic diameter (MMAD ≤ 5 μm) of the aerosol...

Combining a long-acting β2-agonist (LABA) with a long-acting muscarinic antagonist (LAMA) is the cornerstone to treat patients with chronic obstructive pulmonary disease (COPD). In this study we have characterized the interaction between the LAMA tiotropium bromide, and the LABA olodaterol, on ...

The consumption of plant sterols is reported to have a beneficial effects on human health, i.e. phytosterols are known for their cholesterol-lowering properties. Whereas, they are prone to oxidation and currently there is ongoing worldwide research aimed at the biological effect of phytosterol o...

Excited state intramolecular charge transfer (ICT) process in a donor–chromophore–acceptor system 5-(4-dimethylamino-phenyl)-penta-2,4-dienoic acid ethyl ester (DMAPPDE) has been investigated spectroscopically in combination with quantum chemical calculations. The molecule DMAPPDE shows dual f...

In this paper, we described the preparation of fused (Het)Aryltetrahydroindolizinones via N-acyl iminium intermediates. Two different routes were also explored to achieve the synthesis. The first one consists in the intramolecular reaction of β-hydroxylactams whereas the second route one is an ...

Several series of novel non-thiourea-containing aminopyrazine derivatives were designed based on the MK-2 inhibitors 1-(2-aminopyrazin-3-yl)methyl-2-thioureas. These compounds were synthesized and evaluated for their inhibitory activity against MK-2 enzyme in vitro. Compounds with low micromolar...

This study presents the synthesis and characterization of novel metal-free (H2Pc) and metallo porphyrazines (magnesium(II) (MgPz), copper(II) (CuPz), iron(II) (FePz), manganese(II) (MnPz) and nickel(II) (NiPz)) substituted with four 2-methylpyrazine groups on the peripheral positions. The spectr...

In the present study, Azilsartan (AZL) was subjected to ICH recommended forced degradation conditions of hydrolysis, oxidation, dry heat and photolysis. The drug degraded to four degradation products (I–IV) under acidic, alkaline and water hydrolysis and photolysis. All the four degradation pro...

Azilsartan is the eighth approved member of angiotensin II receptor blockers for hypertension treatment. Considering that some drugs have additional effects when administered, we studied its effects and mechanisms of action on a human lung cancer cell line A549. We have also modified the structu...