Study on the chemical stability of β-lactam antibiotics in concomitant simple suspensions with magnesium oxide.

Background: A simple suspension method, where solid formulations are disintegrated and suspended by being soaked in warm water followed by tube administration, is widely used, especially for elderly patients with dysphagia in Japanese clinical settings. However, there is insufficient information on drug stability in the simple co-suspension of multiple formulations especially including acidic or alkaline ones. The influence of occasional prolonged soakage on drug stability is also of concern.

Synthesis of Biosynthetic Intermediates of Vibrioferrin and Enzyme Reactions Using Them as Substrates.

Biosynthetic intermediates of siderophore vibrioferrin (VF), O-citryl-L-serine, 2-aminoethyl citrate, and alanine-2-amidoethyl citrate were respectively synthesized as a mixture of stereoisomers. These compounds were used as substrates for enzyme reactions using recombinant PvsA, PvsB, and PvsE proteins as corresponding enzyme equivalents. The results of our study show that each enzyme reacts with a respective substrate and produces VF along the proposed biosynthetic pathway.

Preparation of [1'- C]citric acid as a probe in a breath test to evaluate tricarboxylic acid cycle flux.

[1'- C]Citric acid (1) was efficiently prepared from dimethyl 1,3-acetonedicarboxylate in two steps as a probe for a breath test. The synthetic method was selected because of the yield and reproducibility. Compound 1 was orally administrated to rats, and the time course of the increase of CO / CO ratios (Δ CO ) in their breath was successfully followed, indicating the metabolism of 1.

Analysis of the vibrioferrin biosynthetic pathway of Vibrio parahaemolyticus.

Siderophores are small-molecule iron chelators produced by many microorganisms that capture and uptake iron from the natural environment and host. Their biosynthesis in microorganisms is generally performed using non-ribosomal peptide synthetase (NRPS) or NRPS-independent siderophore (NIS) enzymes. Vibrio parahaemolyticus secretes its cognate siderophore vibrioferrin under iron-starvation conditions.

A study on the chemical stability of cholesterol-lowering drugs in concomitant simple suspensions with magnesium oxide.

Background: Difficulty in taking solid medicines is a common issue particularly for the elderly because of a decline in swallowing function, also known as dysphagia. For patients with such a dysfunction, a simple suspension method, in which solid medicines are disintegrated and suspended using warm water, has been developed and widely used in Japanese clinical settings. However, there is little information on drug stability in the simple co-suspension of multiple formulations especially including acidic or alkaline ones.

Study on the Use of Ozone Water as a Chemical Decontamination Agent for Antineoplastic Drugs in Clinical Settings.

The exposure of healthcare workers to antineoplastic drugs in hospitals has been recognized to be harmful. To minimize the risk of exposure, the removal of these drugs from work environments, such as compounding facilities, has been recommended. In our previous paper, the degradation and inactivation efficacy of ozone water, which is being introduced into Japanese hospitals as a chemical decontamination agent, was reported for its effects on typical antineoplastic drugs (gemcitabine, irinotecan, paclitaxel).

Degradation and inactivation efficacy of ozone water for antineoplastic drugs in hospital settings.

Purpose: Occupational exposure to antineoplastic drugs in hospital settings is recognized to be hazardous, and as such environmental decontamination including degradation and inactivation of such drugs is recommended. To data, although various agents such as oxidants have been reported to be useful for decontamination, simpler, safer, and more convenient methods are required. In this study, the degradation and inactivation efficacy of ozone water, which has newly been introduced for decontamination of antineoplastic drugs in spills, was investigated for formulations of gemcitabine, irinotecan, and paclitaxel.

Application of Quantitative NMR Spectroscopy to the Quality Evaluation of Diclofenac Gargles as Hospital Preparations.

Hospital preparations are frequently prepared in Japanese hospitals when ready-made formulations to meet patients' needs are unavailable. Although the quality of hospital preparations have to be ensured for efficacy and safety, such quality evaluation tends to be insufficient mainly due to lack of manpower and experimental environments in hospitals. In this paper, we investigated the applicability of quantitative (q)NMR spectroscopy to the quality control of diclofenac gargles as examples of hospital preparations, as it has various merits for the quantitative analysis of mixtures in solutions.

Synthesis of ¹³C-lidocaine as a probe of breath test for the evaluation of cytochrome P450 activity.

(13)C-Labeled lidocaine, 2-di[1-(13)C]ethylamino-N-(2,6-dimethylphenyl)acetamide (1), was synthesized from [1-(13)C]acetic acid in six steps, as a probe for a breath test to evaluate in vivo cytochrome P450 activity. The measurement of (13)CO2 in breath was successfully performed following oral administration of (13)C-lidocaine 1 to mice.

A rare case of Parkinson's disease with severe neck pain owing to crowned dens syndrome.

Background: Pain is regarded as one of the most common nonmotor symptoms in Parkinson's disease (PD). In particular, musculoskeletal pain has been reported as the most common type of PD-associated pain. Crowned dens syndrome (CDS), related to microcrystalline deposition in the periodontoid process, is the main cause of acute or chronic cervical pain.

An efficient laboratory-scale preparative method for [1-(13)C]glycocholic acid.

A breath test using [1-(13)C]glycocholic acid as a substrate is a potential diagnostic method for small intestinal bacterial overgrowth syndrome. [1-(13)C]Glycocholic acid has been thus synthesized in an excellent yield from ethyl [1-(13)C]glycinate hydrochloride in a one-pot reaction. This method is suitable for the preparation of the labeled compound on a laboratory scale, which helps to perform extensive clinical studies of the breath test.

Metabonomic study on the biochemical response of spontaneously hypertensive rats to chronic taurine supplementation using (1)H NMR spectroscopic urinalysis.

There is a wealth of experimental information and some clinical evidence available in the literature suggesting that taurine exerts preventive effects on cardiovascular diseases. In particular, taurine has been shown to reduce blood pressure in not only hypertensive patients but also in a number of hypertensive rodent models such as spontaneously hypertensive rats (SHR). However, the molecular basis of the efficacy and toxicity of the compound has not been fully characterized.

Sample preparation method to minimize chemical shift variability for NMR-based urinary metabonomics of genetically hypertensive rats.

Urinary metabonomics based on proton nuclear magnetic resonance ((1)H NMR) has been widely employed to study metabolic differences associated with gene function and pathophysiological and toxicological stimuli. However, the chemical shift variability of (1)H NMR signals, which is due to differences in pH and ionic strength among urine samples, remains an outstanding problem for efficient data mining. Thus, we have proposed an improved sample preparation method where urine samples are lyophilized and reconstituted in a buffer solution (pH 7.

A metabonomic study of biochemical changes characteristic of genetically hypertensive rats based on (1)H NMR spectroscopic urinalysis.

Spontaneously hypertensive rats (SHR) provide a simple model for studying essential hypertension. Their genetic and metabolic features are of great interest because they may provide insights into the pathophysiological processes underlying essential hypertension. We have thus investigated the metabolic characteristics of SHR at various ages, covering the prehypertensive stage and the developmental phase of hypertension, using a (1)H nuclear magnetic resonance (NMR)-based metabonomic approach.

LC-NMR identification of a novel taurine-related metabolite observed in (1)H NMR-based metabonomics of genetically hypertensive rats.

This paper describes the LC-NMR spectroscopic identification of a novel urinary endogenous metabolite responsible for the signals, which were found as major contributors to the separation between genetically hypertensive rats (SHRSP) and normotensive control rats (WKY) in previous NMR-based metabonomic studies. Urine samples from 26-week-old normotensive rats were analyzed by an LC-NMR system equipped with a reversed-phase column having high retention ability for polar compounds. (1)H NMR spectra were continuously obtained in the on-flow mode, and the retention times of the unassigned signals in question were determined.

Fog simulation using a mesoscale model in and around the Yodo River Basin, Japan.

In this study, fog simulations were conducted using the Fifth-Generation NCAR/Penn State Mesoscale Model (MM5) in and around the Yodo River Basin, Japan. The purpose is to investigate the MM5 performance of fog simulation for long-term periods. The simulations were performed for January, February, March, and July, 2005 with a coarse 3-km and a nested fine 1-km grid domains.

1H NMR-based metabonomic analysis of urine from young spontaneously hypertensive rats.

Spontaneously hypertensive rats (SHR) and their substrains are a useful model for studying essential hypertension which is a complex, polygenic, and multifactorial disorder. Their genetic and metabolic features are of great interest because they may provide insights into the mechanism of blood pressure regulation. We have compared urinary metabolic profiles of young SHR with those of their age-matched normotensive controls, Wistar Kyoto rats, using (1)H NMR-based metabonomics.

Systemic peripheral vascular resistance as a determinant of functional cardiac reserve in response to exercise in patients with heart disease.

Resting cardiac function is a poor indicator of functional cardiac reserve that is invoked during exercise. The objective of this study was to investigate the relationship between functional cardiac reserve and systemic vascular resistance (SVR) using an ambulatory radionuclide monitoring system (the Vest system) in patients with heart disease. The study population consisted of 29 patients (all male [mean +/- SD age, 63 +/- 10 years]), 23 with coronary artery disease, 3 with dilated cardiomyopathy, and 3 with hypertensive heart disease.

Inhibitory effects of amlodipine and fluvastatin on the deposition of advanced glycation end products in aortic wall of cholesterol and fructose-fed rabbits.

Recent studies suggest that advanced glycation end products (AGEs) can promote the development of atherosclerotic lesions in a similar manner to oxidatively modified low density lipoproteins. As oxidative stress accelerates the formation of AGEs, antioxidant drugs may exert atheroprotective effects via suppression of AGE formation. Although amlodipine, a calcium channel blocker, and fluvastatin, a 3-hydroxy-3-methylglutaryl CoA reductase inhibitor, show antioxidant and atheroprotective effects, the relation of AGEs to their effects is unknown.

Investigations into biochemical changes of genetic hypertensive rats using 1H nuclear magnetic resonance-based metabonomics.

Genetically hypertensive rats provide a simple and accessible model for studying essential hypertension, which is a polygenic, heterogenous and multifactorial disease. Their genetic and metabolic features are of great interest because they may provide insight into the pathophysiological processes underlying essential hypertension. We have investigated the genetic influence on metabolic balance and metabolite excretion patterns in stroke-prone spontaneously hypertensive rats (SHRSP) with established hypertension using 1H NMR-based metabonomics.

An autopsy case of infectious endocarditis in a methamphetamine abuser usefulness of microbiological examination.

We present here a case of sepsis due to infectious endocarditis in a methamphetamine abuser. A 32 year-old male presented high fever and abdominal pain last two weeks. He was admitted to the hospital on the diagnosis of infectious endocarditis.

Use of 13C labeling and NMR spectroscopy for the investigation of degradation pathways of Amadori compounds.

The degradation pathways of Amadori compounds in vivo have not been fully understood because of the lack of suitable techniques although the compounds are considered to be key intermediates in glycation, which contributes to the development of pathologies associated with various chronic and age-related diseases. A new approach using 13C labeling and NMR spectroscopy has thus been described to obtain more insight into the degradation pathways. A 13C-labeled model Amadori compound, [1-13C]Nepsilon-(1-deoxy-D-fructos-1-yl)hippuryl-lysine, was synthesized to investigate the degradation pathways of the sugar moiety.

Determination of urinary glyoxal and methylglyoxal by high-performance liquid chromatography.

Carbonyl stress compounds such as glyoxal and methylglyoxal have been recently attracting much attention because of their possible clinical significance in chronic and age-related diseases. A high-performance liquid chromatographic procedure has been developed for the simultaneous quantitation of glyoxal and methylglyoxal in human urine. The assay is based on the reaction of these compounds with 1,2-diamino-4,5-dimethoxybenzene to form fluorescent adducts, which are separated by reversed-phase high-performance liquid chromatography in a total run time of 45 minutes and quantitated fluorometrically using 2,3-pentanedione as an internal standard.

Distal shower embolization during directional coronary atherectomy and stenting for diffuse stenosis of right coronary artery: current limitations of intravascular ultrasonography for evaluating fragile plaque.

A 74 year-old male with old anterior and inferior myocardial infarctions was treated with staged percutaneous coronary intervention. A chronic total occlusion of the middle segment of the left anterior descending branch was successfully stented during the first stage, and during the second stage, preprocedural intravascular ultrasonography (IVUS) revealed that the proximal segment of the right coronary artery was diffusely stenosed by mixed plaque. Directional coronary atherectomy under IVUS guidance was performed, but coronary slow flow appeared during the procedure.

Rapid internal acyl migration and protein binding of synthetic probenecid glucuronides.

Internal acyl migration reactions of drug 1-O-acyl-beta-D-glucopyranuronates (1beta-acyl glucuronides) are of interest because of their possible role in covalent binding to proteins and consequent adverse effects. The reactivity of the synthetic probenecid 1beta-acyl glucuronide (PRG), the principal metabolite of probenecid (PR) in humans, has been investigated in terms of acyl migration, hydrolysis, and covalent binding to proteins in phosphate buffer (pH 7.4) and human plasma at 37 degrees C.