Tetrahymena 14-nm filament-forming protein (49K protein) is a structural protein which is involved in activity of the pronuclei during conjugation (O. Numata, T. Sugai, and Y. Watanabe (1985)Nature (London) 314, 192–194). Using monoclonal and polyclonal antibodies, we here demonstrate the prese...

The Tetrahymena 14-nm filament-forming protein (49K protein) is a structural protein involved in oral morphogenesis and in pronuclear behavior during conjugation. Cloning the 49K protein gene from a Tetrahymena thermophila cDNA library, we found that its primary structure exhibits a high sequenc...

Diltiazem hydrochloride, topically applied at 2% concentration, is considered effective for the treatment of chronic anal fissures, although it involves several side effects among which anal pruritus and postural hypotension. To test the hypothesis that a sustained delivery system of diltiazem h...

The hydrodynamic behavior of chitosan hydrochloride macromolecules in aqueous solutions of D- and l-ascorbic acid in a temperature range 25–45 °C was studied by capillary viscometry. The intrinsic viscosity, the Huggins constant, and the temperature coefficient of viscosity were estimated. The...

Highly efficient poly functionalized pyrrolo[3,2-a]carbazoles via ring contraction through rearrangement and intramolecular Michael addition reaction using one pot multicomponent reaction (MCR) is reported for the first time. Free radical scavenging and anticancer activities were determined by D...

An initial study of the side-chain unsubstituted 2'-hydroxyacrylophenone system shows it to have a considerably greater propensity for intermolecular addition than the comparable 2'-hydroxychalcone system, readily undergoing base-catalysed addition of, for example, alcohol and thereby ...

Pancreatic cancer is one of the most deadly neoplasm with a 5-year survival rate of less than 6% owing to its remarkable tolerance to nutrient starvation, and new drugs and treatment strategies are urgently needed. During a project aiming at discovery of anticancer agents, we performed a structu...

A new 1,4-dihydropyridine photoaffinity ligand, [3H]diazipine, has been assessed by binding and photolabeling, and compared with a currently used [3H]Diazipine reversibly binds to skeletal muscle Ca2+ channels with a similar affinity of [3H]azidopine, but [3H]diazipine labels the channels two ti...

In the course of a program aimed at designing antitumor agents containing an indolocarbazole framework, an efficient synthetic scheme based on the use of 3,4-dibromo-N-methylmaleimide and 7-azaindole has been developed to elaborate a series of mono- and di-aza derivatives of arcyriaflavin. The p...

Background: Empiric therapy for community-acquired pneumonia (CAP) requires the use of antibiotics with activity against a broad spectrum of respiratory pathogens and suitable pharmacokinetic properties to simplify IV-to-oral step-down therapy switches.Objective: The aim of this study was to com...

The chemical stability of a less-painful ready-to-use o/w emulsion for intravenous (i.v.) delivery of clarithromycin was investigated. The formulation contained 0.5% w/v drug, 2% w/v soybean oil, 5% w/v egg phosphatide, 0.6% w/v oleic acid, 0.3% hexanoic acid and 2.5% w/v glycerin in water. The ...

A clinical study was conducted to assess the ability of a microdose (100 μg) to predict the human pharmacokinetics (PK) following a therapeutic dose of clarithromycin, sumatriptan, propafenone, paracetamol (acetaminophen) and phenobarbital, both within the study and by reference to the existing...

In the present study, novel less-painful tocol emulsions for the intravenous delivery of clarithromycin were prepared and optimized. The therapeutically effective concentration of clarithromycin, 5 mg/ml, was achieved using tocopherol succinate (TS) combined with oleic acid as lipophilic counter...

The purpose of this paper is to prepare a new formulation of clarithromycin emulsion (ClaE) with the clarithromycin–phospholipid complex which was analyzed by DSC. High-pressure homogenization, Nicomp™ 380 Particle Sizing system, and HPLC were used to prepare and investigate ClaE, while UPLC/MS...

The aim of this study was to develop an efficient method of preparing less irritant clarithromycin-loaded liposomes (CLA-Lip) for injection with a high drug loading and to evaluate their physicochemical characteristics before and after lyophilization. CLA-Lip were prepared using the film-dispers...

Several emulsion formulations (e.g., mixtures of drug with a nutritional emulsion, e.g., Liposyn®, ready-to-use w/o/w emulsion, and ready-to-use o/w emulsions) were developed and tested for potential use as a less-painful i.v. formulation of clarithromycin. The formulations contained 5 mgml drug...

The bioproduction of lactobionic acid and its salts can be performed by enzymatic complex glucose-fructose oxidoreductase (GFOR) and glucono-δ-lactonase (GL) of Zymomonas mobilis. Considering the applicability of these compounds in pharmaceutical area, the aim of this study was to assess the ac...

Introduction. Gadoxetate-disodium is a liver-specific MR contrast agent absorbed by hepatocytes via organic anion transporting polypeptide 1B3 and is excreted into the biliary system by multidrug resistance-associated protein 2. It has been suggested that relative parenchymal enhancement on hepa...

AimTo investigate the feasibility of gadoxetate disodium-enhanced magnetic resonance (MR) cholangiography in chronic obstructive cholestatic biliary disease in the clinical setting.

Background & AimsAlthough gadoxetate disodium-enhanced magnetic resonance imaging (MRI) shows higher sensitivity for diagnosing hepatocellular carcinoma (HCC), its arterial-phase images may be unsatisfactory because of weak arterial enhancement. We investigated the clinical effectiveness of arte...