Decomposition Characteristics of the TTIP (Tetraisopropyl Orthotitanate) Precursor for Atomic Layer Deposition.

The decomposition of tetraisopropyl orthotitanate (TTIP), a representative precursor used in the atomic layer deposition (ALD) of titanium dioxide (TiO) film, and the resulting changes in the thin film properties of the TiO film were investigated. TTIP was evaluated after exposure to thermal stress in an enclosed container. The vapor pressure results provide reasonable evidence that impurities are generated by the decomposition of TTIP under thermal stress.

Immunomodulatory and anti-inflammatory efficacy of hederagenin-coated maghemite (γ-FeO) nanoparticles in an atopic dermatitis model.

We investigated the immunomodulatory and anti-inflammatory efficacy of hederagenin coating on maghemite (γ-FeO) nanoparticles (HM) in atopic dermatitis (AD), as well as the physical and optical properties of maghemite nanoparticles (MP) using SEM, XRD spectroscopy, UV-vis spectra, Raman spectra, and FTIR spectroscopy. Dose-dependent treatment with HM (10, 50, 100, 200 μg/mL) inhibited the expression of Interleukin-2 (IL-2) and Tumor necrosis factor- α (TNF-α) in inflammatory induced HaCaT and Jurkat cells with inflammation caused by TNF/IFN-γ and PMA/A23187. AD model was induced by performing topical application of 2,4-dinitrochlorobenzene (DNCB) and dermatophagoides farinae extract (DFE) for a 31-day period on 8-week-old BALB/c mice.

Glycosylation generates an efficacious and immunogenic vaccine against H7N9 influenza virus.

Zoonotic avian influenza viruses pose severe health threats to humans. Of several viral subtypes reported, the low pathogenic avian influenza H7N9 virus has since February 2013 caused more than 1,500 cases of human infection with an almost 40% case-fatality rate. Vaccination of poultry appears to reduce human infections.

Surface-Modified Industrial Acrylonitrile Butadiene Styrene 3D Scaffold Fabrication by Gold Nanoparticle for Drug Screening.

Biocompatibility is very important for cell growth using 3D printers, but biocompatibility materials are very expensive. In this study, we investigated the possibility of cell culture by the surface modification of relatively low-cost industrial materials and an efficient three-dimensional (3D) scaffold made with an industrial ABS filament for cell proliferation, spheroid formation, and drug screening applications. We evaluated the adequate structure among two-layer square shape 3D scaffolds printed by fused deposition modeling with variable infill densities (10-50%).

Novel Small Molecule Targeting the Hemagglutinin Stalk of Influenza Viruses.

Combating influenza is one of the perennial global public health issues to be managed. Antiviral drugs are useful for the treatment of influenza in the absence of an appropriate vaccine. However, the appearance of resistant strains necessitates a constant search for new drugs.

Highly sensitive two-dimensional MoS gas sensor decorated with Pt nanoparticles.

A two-dimensional molybdenum disulfide (MoS)-based gas sensor was decorated with Pt nanoparticles (NPs) for high sensitivity and low limit of detection (LOD) for specific gases (NH and HS). The two-dimensional MoS film was grown at 400°C using metal organic gas vapour deposition. To fabricate the MoS gas sensor, an interdigitated Au/Ti electrode was deposited using the electron beam (e-beam) evaporation method with a stencil mask.

Mitigation Effects of a Novel Herbal Medicine, Hepad, on Neuroinflammation, Neuroapoptosis, and Neuro-Oxidation.

Parkinson's disease (PD), a common adult-onset neurodegenerative disorder with complex pathological mechanisms, is characterized by the degeneration of dopaminergic nigrostriatal neurons. The present study demonstrated that the herbal medicines Hepad 1 and 2 protected against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced dopaminergic neurotoxicity in C57BL/6 mice and SH-SY5Y cells. Hepad 1 and 2 remarkably alleviated the enhanced expression of pro-inflammatory cytokines (tumor necrosis factor-α, interleukin-6, inducible nitric oxide synthase, cyclooxygenase-2, macrophage-1, and phosphorylated iκB-α) and apoptotic signals (Bcl-2-associated X protein, caspase-3, and poly [ADP-ribose] polymerase-1).

The c-Abl inhibitor, Radotinib HCl, is neuroprotective in a preclinical Parkinson's disease mouse model.

Accumulating evidence suggests that the non-receptor tyrosine kinase c-Abl plays an important role in the progression of Parkinson's disease (PD) and c-Abl inhibition could be neuroprotective in PD and related α-synucleinopathies. Nilotinib, a c-Abl inhibitor, has shown improved motor and cognitive symptoms in PD patients. However, issues concerning blood-brain barrier (BBB) penetration, lack of selectivity and safety still remain.

Pharmacokinetic drug interaction and safety after coadministration of clarithromycin, amoxicillin, and ilaprazole: a randomised, open-label, one-way crossover, two parallel sequences study.

Purpose: Ilaprazole, the latest proton pump inhibitor, can be used with clarithromycin and amoxicillin as a triple therapy regimen for eradicating Helicobacter pylori. The aim of this study was to evaluate pharmacokinetic drug interactions and safety profiles after coadministration of clarithromycin, amoxicillin, and ilaprazole.

Methods: A randomised, open-label, one-way crossover, two parallel sequences study was conducted in 32 healthy subjects.

Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors.

Radotinib (IY5511HCL), a novel and selective BCR-ABL1 tyrosine kinase inhibitor, has shown pre-clinical and phase I activity and safety in chronic myeloid leukemia. This phase II study investigated the efficacy and safety of radotinib in Philadelphia chromosome-positive chronic phase-chronic myeloid leukemia patients with resistance and/or intolerance to BCR-ABL1 tyrosine kinase inhibitors. Patients received radotinib 400 mg twice daily for 12 cycles based on results from the phase I trial.

In vitro analysis of the anti-cancer activity of mitoxantrone loaded on magnetic nanoparticles.

In this study, the anti-tumor activity of mitoxantrone loaded on magnetic nanoparticles (MTMP) was examined using DU145 prostate cancer cells. Composite nanoparticles with an average size of 20 nm were prepared using a chemical co-precipitation technique. The MTMP nanoparticles were cytotoxic to DU145 cells and inhibited cell proliferation.

Synthesis and characterization of bicalutamide-loaded magnetic nanoparticles as anti-tumor drug carriers.

This study examined the optical characteristics of bicalutamide-loaded magnetic/ethylene glycol composite nanoparticles (BMP), as well as their anti-cancer activity against cancer cells. The gamma-Fe2O3 magnetic nanoparticles (MNPs), approximately 20 nm in diameter, were prepared via a chemical co-precipitation method and coated with two surfactants to yield a water-based product. The characteristics of the particles were determined via X-ray diffraction (XRD), field emission scanning electron microscopy, and Raman spectrophotometry.

Effect of CYP2C19 genetic polymorphism on pharmacokinetics and pharmacodynamics of a new proton pump inhibitor, ilaprazole.

It is well known that the CYP2C19 genetic polymorphism influences the pharmacokinetics and pharmacodynamics of proton pump inhibitors (PPIs), but no report has addressed the effects on ilaprazole, a newly developed PPI. To investigate the effects of the CYP2C19 genetic polymorphism on the disposition and pharmacodynamics of ilaprazole, multiple doses of once-daily 10 mg ilaprazole were repeatedly administered for 7 days to 27 healthy Korean participants, comprising 9 homozygous CYP2C19 extensive metabolizers (homo EMs), 10 heterozygous EMs (hetero EMs), and 8 homozygous poor metabolizers (PMs). The plasma concentration and pharmacodynamic response were measured in the last dose interval.

Synthesis and in vitro anti-cancer evaluation of ethylene glycol-saponin loaded on magnetic nanoparticles.

Prostate cancer is one of the most preventable cancers, yet effective therapeutics, especially targeted therapy, are still lacking. Saponin has been reported to possess various biological properties such as anti-cancer and anti-inflammatory activity. In this study, the anti-tumor activity of magnetic nanoparticles loaded with ethylene glycol and a saponin complex (ESMP) against DU145 prostate cancer cells was examined.

HO-1 and JAK-2/STAT-1 signals are involved in preferential inhibition of iNOS over COX-2 gene expression by newly synthesized tetrahydroisoquinoline alkaloid, CKD712, in cells activated with lipopolysacchride.

We found that CKD712, an S enantiomer of YS49, strongly inhibited inducible nitric oxide synthase (iNOS) and NO induction but showed a weak inhibitory effect on cyclooxygenase-2 (COX-2) and PGE(2) induction in LPS-stimulated RAW 264.7 cells. We, therefore, investigated the molecular mechanism(s) responsible for this by using CKD712 in LPS-activated RAW264.

Protective effect of maghemite nanoparticles on ultraviolet-induced photo-damage in human skin fibroblasts.

This study examined the optical properties of an oxidized form of maghemite (γ-Fe(2)O(3)) nanoparticles and their protective effects against the photoaging of human skin fibroblasts irradiated with ultraviolet (UV) light. Nanoparticles with diameters ranging from 8.7 to 12 nm were prepared using a chemical co-precipitation method.

Design, synthesis, and antiangiogenic effects of a series of potent novel fumagillin analogues.

A series of fumagillin analogues containing the C6-substituted cinnamoyl moiety were designed, synthesized, and evaluated for antiangiogenic activity. Among them, 4-hydroxyethoxy-cinnamoyl fumagillol (4a) and 4-hydroxyethoxy-3,5-dimethoxycinnamoyl fumagillol (4d) exhibited more potent anti-proliferation activity in CPAE and HUVEC cells with low cytotoxicity in vitro. These compounds are presently under further pharmacological evaluation studies.

Enantiomers of higenamine inhibit LPS-induced iNOS in a macrophage cell line and improve the survival of mice with experimental endotoxemia.

The importance of development of single enantiomers (optically pure isomers) of chiral molecules has been recognized and manifested in countless pharmaceutical and biological advancement. (RS)-(+/-)-Higenamine (racemic mixture), an active ingredient of Aconite tuber, has been shown to have antioxidant activity along with inhibitory action of iNOS expression in various cells. In the present study, the effects of each enantiomer of higenamine [(S)-(-)-higenamine and (R)-(+)-higenamine] were investigated in comparison with the effects of racemic mixture [(RS)-(+/-)-higenamine] on iNOS expression and NO production in RAW 264.

Molecular design, synthesis, and hypoglycemic and hypolipidemic activities of novel pyrimidine derivatives having thiazolidinedione.

We previously reported the synthesis and biological activity of novel substituted pyridines and purines having thiazolidinedione with hypoglycemic and hypolipidemic activities. We now report the synthesis and antidiabetic activity of novel substituted pyrimidines having thiazolidinedione moiety. These compounds (entry No.

Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione.

A series of substituted pyridines and purines containing 2,4-thiazolidinedione were designed and synthesized from their corresponding pyridines and purines. These synthesized compounds (entry no. 6a-d, 12a-e, 18a-d, 23a-c) were evaluated for their effect on triglyceride accumulation in 3T3-L1 cells in vitro and their hypoglycemic and hypolipidemic activity in the genetically diabetic KKA(y) mice in vivo.

Phosphorylation of vanilloid receptor 1 by Ca2+/calmodulin-dependent kinase II regulates its vanilloid binding.

Vanilloid receptor 1 (VR1), a capsaicin receptor, is known to play a major role in mediating inflammatory thermal nociception. Although the physiological role and biophysical properties of VR1 are known, the mechanism of its activation by ligands is poorly understood. Here we show that VR1 must be phosphorylated by Ca2+-calmodulin dependent kinase II (CaMKII) before its activation by capsaicin.

Synthesis and antihyperglycemic activity of erythrose, ribose and substituted pyrrolidine containing thiazolidinedione derivatives.

A series of erythrose, ribose, and substituted pyrrolidine containing 2,4-thiazolidinediones were synthesized. Among them, thirteen unsaturated thiazolidinediones, six saturated thiazolidinediones and two unsaturated malonates were evaluated for their ability to enhance glucose utilization in cultured L6 myocytes. On the basis of the in vitro activity, 5-[4-[2-(1-benzyl-3,4-bis-benzyloxypyrrolidin-2-yl)ethoxy]benzylidene]thiazolidine-2,4-dione 24b was selected as the candidate for further pharmacological studies.