purpose. To investigate the pharmacokinetics of bevacizumab in rabbits for three different routes administrations: intravitreal injection, subconjunctival and eye drops. methods. Pigmented received one by topical drops (1.25 mg/0.05 mL six times daily first 7 days), single injection mL), or mL). Bevacizumab concentrations plasma ocular tissues treated fellow eyes were determined sandwich enzyme-linked immunosorbent assay at 1, 2, 4, 12 weeks after administration. results. After eye, mean...

Transport of drugs applied by traditional dosage forms is restricted to the eye, and therapeutic drug concentrations in target tissues are not maintained for a long duration since eyes protected unique anatomy physiology. For treatment anterior segment various droppable products prolong retention time on ocular surface have been introduced market. On other hand, direct intravitreal implants, using biodegradable or non-biodegradable polymer technology, widely investigated chronic...

Recent epidemiological studies have shown that patients with age-related macular degeneration (AMD) a considerably higher risk of developing Parkinson's disease (PD) later in life, suggesting possible link between these diseases. However, the common mechanisms two diseases remain obscure, although pathophysiology each has been well investigated. In this study, we sought to explore shared pathological features AMD and PD by focusing on leucine-rich repeat kinase 2 (LRRK2) α-synuclein, both...

Purpose.: The purpose of this study was to clarify the impact P-glycoprotein (P-gp) on blood–retinal barrier (BRB) and blood–aqueous humor (BAB) permeability, in contrast blood–brain (BBB) permeability. Methods.: Permeabilities six compounds, including P-gp substrates (quinidine, digoxin, verapamil), were investigated wild-type mdr1a knockout rats using retinal, aqueous humor, brain uptake index (RUI, AHUI, BUI, respectively) methods integration plot analysis. Results.: In both rat strains,...

The Asahi River Dam reservoir is one of the important freshwater resources for Okayama City, Japan. eutrophication has been warned since 1980s. In this study, we discuss relationship between hydraulic retention time and increase phytoplankton, influence wind-driven currents on spatial distribution phytoplankton based observations numerical simulations. Observations were carried out from 1993 to 1995. simulation hydraulics in was by applying an orthogonal curvilinear finite difference method....

The highly efficient and stereocontrolled syntheses of sphingomyelin carbon analogues 1 2 were achieved by effectively utilizing Hofmann rearrangement enantiomerically pure β-hydroxyamide 7, which was prepared an asymmetric hydrogenation α-acyl-γ-butyrolactone 9 ring opening with NH3. Intermediary isocyanate 6 selectively trapped the vicinal hydroxy group in intramolecular fashion to produce oxazolidinone derivative, 5. In synthesis a quite polar compound such as 1, convenient one-pot...

We designed a simple and sensitive method to assay the activity of factor VIIa-tissue complex, using as substrate N alpha-benzyloxycarbonyl-L-arginine p-nitrobenzyl ester (Z-Arg-ONb) (Zur, M., Nemerson, Y. (1978) J. Biol. Chem. 253, 2203-2209). The principle was measure amount alcohol released during hydrolysis reversed-phase high performance liquid chromatography. Z-Arg-ONb had broad specificity for plasma serine proteases IXa. Using this method, we examined effect tissue on esterase VIIa...

The Asahi River Dam reservoir is one of the important freshwater resources for Okayama City, Japan. eutrophication has been warned since 1980s. In this study, we discuss relationship between hydraulic retention time and increase phytoplankton, influence wind-driven currents on spatial distribution phytoplankton based observations numerical simulations. Observations were carried out from 1993 to 1995. simulation hydraulics in was by applying an orthogonal curvilinear finite difference method....

1,3-Diacetyl-2-ketoprofen glyceride (DAKG), a prodrug of ketoprofen, was synthesized as model compound in our attempt to develop central nervous system (CNS) drug delivery treat Alzheimer's disease. The primary purpose the present study is test whether DAKG improves ketoprofen brain and quantitatively evaluate several factors that influence distribution this prodrug. ddY mice were injected with either or at dose 40 μmol/kg then plasma pharmacokinetics these agents assessed. uptake clearance...

Three sesterterpenoids, aplysinoplides A−C (1−3), were isolated from the marine sponge Aplysinopsis digitata. Their structures determined on basis of spectroscopic data. They exhibited cytotoxic activity against P388 mouse leukemia cells.

Abstract Objective We evaluated the impact of chronic kidney disease (CKD) on presence and severity aortic stenosis (AS) in patients at high risk for coronary artery (CAD). Methods One hundred twenty consecutive who underwent invasive angiography were enrolled. Aortic valve area (AVA) was calculated by continuity equation using transthoracic echocardiography, normalized body surface (AVA index). Results Among all 120 patients, 78% had CAD, 55% CKD (stage 3: 81%; stage 4: 19%), 34% AS <...

A 63‐year‐old man with hepatocellular carcinoma consequent to chronic viral hepatitis C presented severe dermatitis on the lower right side of back after transcatheter arterial chemoembolization (TACE) via 10th intercostal artery, because his hepatic artery had already collapsed due repeated usage for TACE. The regional skin showed redness and hardness pustules. Histologically, there was epidermal appendage necrosis, as well exocytosis red blood cells. With a diagnosis injury leakage...

Systemically administered pravastatin effectively treats diabetic retinopathy without central nervous system side effects. The efflux transport mechanism of from the brain has already been clarified. In this study, influx across blood-retinal and blood-brain barriers (BRB BBB) retina were investigated using rats. Pravastatin (blood-to-tissues) was assessed retinal uptake index (RUI BUI) methods, microdialysis performed to investigate (retina-to-blood) pravastatin. RUI BUI values for...

Purpose To investigated whether a new drug delivery system (DDS) could enable the controlled release of tafluprost and suppress retinal ganglion cell (RGC) death in rats after optic nerve transection (ONT).Methods A DDS containing 0.04%, 0.20% or 1.00% tafluprost, vehicle, was injected intravitreally 8-12-week-old male Sprague-Dawley 7 days before ONT, retinas were extracted ONT. For comparison, eye drops 0.0015% vehicle used once day. The analyzed with liquid chromatography–tandem mass...

Journal Article Role of Ca2+ in the Substrate Binding and Catalytic Functions Snake Venom Phospholipases A2 Get access Keizo Teshima, Teshima *Department Hygienic Chemistry, Faculty Pharmacy, Hoshi UniversityShinagawa-ku, Tokyo 142 Search for other works by this author on: Oxford Academic PubMed Google Scholar Yutaka Kitagawa, Kitagawa Yuji Samejima, Samejima 2 2To whom correspondence should be addressed. Saju Kawauchi, Kawauchi Shinobu Fujii, Fujii **Department Biochemistry, Osaka...

Bacillus cereus sphingomyelinase belongs to the Mg2+-dependent neutral sphingomyelinase, which hydrolyses sphingomyelin phosphocholine and ceramide, acts as an extracellular hemolysin. The triplet residues, His151–Asp195–His296, of enzyme are highly conserved among bacterial mammalian sphingomyelinases. residues converge on active-site pocket 3D model enzyme. To investigate function these in acid-base catalysis, we introduced several mutations for each residue by site-directed mutagenesis....