Mechanism of bombesin-induced tonic contraction of the porcine lower esophageal sphincter.

Gastroesophageal reflux disease (GERD) is a disorder that is related to an incompetent lower esophageal sphincter (LES). Previous studies showed that bombesin could increase LES pressure in humans and opossums. The aim of the present study was to characterize the effects of bombesin on porcine LES contraction.

Salvia miltiorrhiza Induces Tonic Contraction of the Lower Esophageal Sphincter in Rats via Activation of Extracellular Ca2+ Influx.

Up to 40% of patients with gastroesophageal reflux disease (GERD) suffer from proton pump inhibitor refractory GERD but clinically the medications to strengthen the lower esophageal sphincter (LES) to avoid irritating reflux are few in number. This study aimed to examine whether Salvia miltiorrhiza (SM) extracts induce tonic contraction of rat LES ex vivo and elucidate the underlying mechanisms. To investigate the mechanism underlying the SM extract-induced contractile effects, rats were pretreated with atropine (a muscarinic receptor antagonist), tetrodotoxin (a sodium channel blocker), nifedipine (a calcium channel blocker), and Ca(2+)-free Krebs-Henseleit solution with ethylene glycol tetraacetic acid (EGTA), followed by administration of cumulative dosages of SM extracts.

Preparation and characterization of gelatin-based mucoadhesive nanocomposites as intravesical gene delivery scaffolds.

This study aimed to develop optimal gelatin-based mucoadhesive nanocomposites as scaffolds for intravesical gene delivery to the urothelium. Hydrogels were prepared by chemically crosslinking gelatin A or B with glutaraldehyde. Physicochemical and delivery properties including hydration ratio, viscosity, size, yield, thermosensitivity, and enzymatic degradation were studied, and scanning electron microscopy (SEM) was carried out.

The association between circulating endothelial progenitor cells and outcome in different subtypes of acute ischemic stroke.

Objectives: This study evaluated the relationship between serial changes in circulating endothelial progenitor cells (EPCs) and outcomes in patients with different subtypes of acute ischemic stroke (AIS).

Methods: This prospective cohort study evaluated 65 patients with AIS, including 45 with small-vessel and 20 with large-vessel diseases. The circulating level of EPCs (CD133(+)/CD34(+) and KDR(+)/CD34(+) cells) was determined at different time points (within 48h and on Days 7 and 30 post-stroke).

Elevating bioavailability of curcumin via encapsulation with a novel formulation of artificial oil bodies.

Utilization of curcumin has been limited due to its poor oral bioavailability. Oral bioavailability of hydrophobic compounds might be elevated via encapsulation in artificial seed oil bodies. This study aimed to improve oral bioavailability of curcumin via this encapsulation.

Optimization of rate-controlled 17beta-estradiol nanoparticles for cerebral ischemia therapy.

The objective of this study was to prepare and evaluate rate-controlled 17beta-estradiol nanoparticles (E2-NPs), and then optimize them by central composite design (CCD) using a response surface methodology (RSM). The E2-NPs were designed for cerebral ischemia therapy and prepared by oil-in-water (o/w) emulsion by mixing E2 and phosphatidylcholine, cross-linking of the bovine serum albumin (BSA) wall material with glutaraldehyde, and subsequently creating a biodegradable coating shell with L-arginine. In two-factor, five-level CCD, the independent variables were the pH value of the aqueous phase (X1) and the amount of glutaraldehyde (X2).

Discovery, synthetic methodology, and biological evaluation for antiphotoaging activity of bicyclic[1,2,3]triazoles: in vitro and in vivo studies.

Novel bicyclic[1,2,3]triazoles (4, 7, 11, 15) have been synthesized using a one-pot metal free strategy with high structural diversity as photoprotective agents, and their effect on UVA-induced senescence in human dermal fibroblast cells (FB) and the associated mechanism are delineated. 11d plus UVA can induce a decrease in reactive oxygen species (ROS) production and senescence-associated β-galactosidase (SA-β-gal) activity but an increase in adenosine triphosphate (ATP) synthesis and mitochondrial membrane potential (ΔΨmt). The mRNA levels of six senescence-associated genes, matrix metalloproteinase-1 (MMP-1), was decreased, while elastin, procollagen I type I, fibronectin, COL1α1, and tissue inhibitor of metalloproteinase-1 (TIMP-1) were increased.

Salvia miltiorrhiza causes tonic contraction in rat ileum through Ca²⁺-calmodulin pathway.

Ethnopharmacological Relevance: Danshen, root of Salvia miltiorrhiza (SM), has been traditionally used in Chinese medicine for the treatment of heart, abdomen, gurgling in the intestines, and relieving fullness. However, the effects of SM on intestine have rarely been done to date.

Aim Of The Study: To investigate the contraction effect of SM on isolated rat ileum and its mechanisms involved.

Preparation, characterization and cytotoxicity evaluation of tanshinone IIA nanoemulsions.

Tanshinone IIA (TA) is a major active component of Danshen (Salvia miltiorrhiza bunge), a well-known traditional Chinese medicine. In this paper, we describe an optimal method for preparing TA nanoemulsions (TA-NEs) to solve the problems of TA's poor solubility in water and insufficient dissolution rate. Optimization of the method for preparing nanoemulsions of lipid soluble TA by emulsification/high pressure homogenization was carried out with a 2(3) factorial design, using Tween 80, lecithin and water content as independent variables.

Preliminary study of a traditional Chinese medicine formula in systemic lupus erythematosus patients to taper steroid dose and prevent disease flare-up.

Systemic lupus erythematosus (SLE) is a chronic systemic autoimmune disease. Prolonged complete remission is rare. Most patients with SLE need long-term treatment with glucocorticoid and immunomodulators.

Optimization of epirubicin nanoparticles using experimental design for enhanced intravesical drug delivery.

The aim of this study was to develop poly(ethyl-2-cyanoacrylate) (PECA) epirubicin-loaded nanoparticles (EPI-NP). A 2(3) factorial design was adopted with the type of surfactant, surfactant concentration and the pH of the polymerization medium as independent variables. The particle size, entrapment efficacy and polydispersity index of eight formulations were then evaluated.

Formulation design of an HPMC-based sustained release tablet for pyridostigmine bromide as a highly hygroscopic model drug and its in vivo/in vitro dissolution properties.

Pyridostigmine bromide (PB), a highly hygroscopic drug was selected as the model drug. A sustained-release (SR) tablet prepared by direct compression of wet-extruded and spheronized core pellets with HPMC excipients and exhibited a zero-order sustained release (SR) profile. The 2(3) full factorial design was utilized to search an optimal SR tablet formulation.

Significant correlations between severe fatty liver and risk factors for metabolic syndrome.

Background And Aim: It is known that ultrasonography (US) cannot differentiate between non-alcoholic fatty liver disease (NAFLD) and steatohepatitis. However, US can accurately estimate the severity of the steatosis. The clinical significance of severe hepatic fatty change by US has not been explored.

Preparation, physicochemical characterization, and antioxidant effects of quercetin nanoparticles.

The purpose of this study was to develop quercetin-loaded nanoparticles (QUEN) by a nanoprecipitation technique with Eudragit E (EE) and polyvinyl alcohol (PVA) as carriers, and to evaluate the antioxidant effects of quercetin (QU) and of its nanoparticles. The novel QUEN systems were characterized by particle size and morphology, yield and encapsulation efficiency, differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), (1)H nuclear magnetic resonance ((1)H NMR), and dissolution study. It was observed that the weight ratio of QU:EE:PVA at 1:10:10 carried a particle size of <85 nm, a particle distribution with polydispersity index <0.

Microencapsulation of extract containing shikonin using gelatin-acacia coacervation method: a formaldehyde-free approach.

The application of microcapsule for pharmaceutical dosage form for various drugs has received considerable attention in recent years due to its multiple advantages. The most frequently used crosslinking agent formaldehyde in the gelatin-acacia microencapsulation process was altered by glycerol in this study. The effect of various parameters such as the concentration of surfactant, concentration of gelatin and continuous phase pH condition on the microcapsule particle size distribution was experimentally investigated.

Formulation design of a highly hygroscopic drug (pyridostigmine bromide) for its hygroscopic character improvement and investigation of in vitro/in vivo dissolution properties.

Pyridostigmine bromide (PB) sustained-release (SR) pellets were developed by extrusion-spheronization and fluid-bed methods using Taguchi experimental and 2(3) full factorial design. In vitro studies, the 2(3) full factorial design was utilized to search for the optimal SR pellets with specific release rate at different time intervals (release percent of 2, 6, 12, and 24 hr were 6.24, 33.

Comparison of the solubility and dissolution rate between gliclazide solid complex and its nanospheres.

The solid complex of gliclazide and beta-cyclodextrin was prepared by neutralization method and the precipitation solvent evaporation method was used to prepare gliclazide nanospheres. Fourier-transform infrared spectroscopy and differential scanning calorimetry were used to examine whether gliclazide solid complex and gliclazide nanospheres were successfully formed in this study. The dissolution rate of gliclazide from its nanospheres was faster than its solid complex and pure drug.

Analysis of brain distribution and biliary excretion of a nutrient supplement, gastrodin, in rat.

Gastrodin is a bioactive constituent of rhizome in Gastrodia elata Blume (Orchidaceae) The aim of this study is to develop a rapid and sensitive liquid chromatographic method coupled to microdialysis sampling system to measure the unbound of gastrodin in rat blood, brain and bile. Microdialysis probes were simultaneously inserted into the jugular vein, brain striatum and bile duct of each anesthetized rat for sampling after the administration of gastrodin (100 or 300 mg kg(-1)) through the femoral vein. Separation of unbound gastrodin from various biological fluids was applied to an RP-select B column (250 mm x 4.

Liquid chromatographic method with amperometric detection to determine acteoside in rat blood and brain microdialysates and its application to pharmacokinetic study.

A simple and sensitive liquid chromatography with amperometric detection was developed for the first time to monitor the protein-unbound acteoside in the rat blood and brain microdialysate by microdialysis technique. Microdialysis samples without further cleanup procedures were directly injected into the HPLC and separated using a reversed-phase C18 column (150 mmx2 mm, i.d.

An investigation of acetylcholine released in skeletal muscle and protein unbound drug released in blood based on the pyridostigmine bromide (pretreatment drug) sustained-release pellets by microdialysis technique in the rabbit model.

Pyridostigmine bromide (PB) is a reversible acetylcholinesterase inhibitor that has been used as a pretreatment drug for "Soman" nerve gas poisoning in combat to increase survival. The once-daily PB-sustained-release (SR) pellets were developed by extrusion-spheronization and fluid-bed methods in our laboratory, which was followed by zero-order release mechanism. The results showed that the released concentration of acetylcholine (ACh) in skeletal muscle and the released concentration of protein unbound drug in blood were determined by microdialysis technique to have significant differences (P<0.

Measurement of unbound ranitidine in blood and bile of anesthetized rats using microdialysis coupled to liquid chromatography and its pharmacokinetic application.

To investigate the pharmacokinetics of unbound ranitidine in rat blood and bile, multiple microdialysis probes coupled to a liquid chromatographic system were developed. This study design was parallel in the following groups: the control-group of six rats received ranitidine alone (10 and 30 mg/kg, i.v.

Identification and determination of geniposide contained in Gardenia jasminoides and in two preparations of mixed traditional Chinese medicines.

A high-performance liquid chromatographic method was applied to the determination of the geniposide concentration in Gardenia fruit and preparations of traditional Chinese medicine using a mobile phase of acetonitrile-methanol-5 mM monosodium phosphate (pH 4.6) (5:15:80, v/v/v). Intra-assay and inter-assay accuracy and precision of the analyses were < or = 10% in the range of 0.