Abstract：
:Characteristics of transport of an oral aminocephalosporin, cefroxadine, in rabbit small intestinal brush border membrane vesicles were examined. Uptake rate of cefroxadine was saturable in the presence of an inward H+ gradient, and kinetic parameters were similar to those of cephradine. However, the uptake rate was almost linear with the concentration in the absence of an inward H+ gradient up to 5 mM. Overshoot phenomenon was observed in the presence of an inward H+ gradient at 37 degrees C, but it disappeared with decrease of temperature. The Arrhenius plot of uptake rate constant showed a break point at approximately 30 degrees C. Cefroxadine uptake was optimum in the vicinity of pH 5.5 at 37 degrees C, but the dependence on extravesicular pH disappeared at 15 degrees C. The uptake of cefroxadine in the presence of an inward H+ gradient was markedly inhibited by other aminocephalosporins such as cephalexin, but the inhibition was only slight in the absence of an inward H+ gradient. Alkyl alcohols such as n-hexyl alcohol also inhibited H(+)-coupled uptake of cefroxadine at the concentration range at which the alcohols increased the membrane fluidity, and overshoot phenomenon diminished, suggesting that H(+)-coupled transport of cefroxadine is sensitive to the alcohol-induced increase in membrane fluidity. On the other hand, the alcohols rather stimulated its uptake in the absence of an H+ gradient.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Kitagawa S,Sugaya Ydoi
10.1248/bpb.19.268subject
Has Abstractpub_date
1996-02-01 00:00:00pages
268-73issue
2eissn
0918-6158issn
1347-5215journal_volume
19pub_type
杂志文章abstract：:Permeation enhancement of ketoprofen (KP) from supersaturated systems and the effects of antinucleant polymers on both stability and permeation of supersaturated KP were investigated using silicone membrane as a skin model. The supersaturation was prepared by the cosolvent technique with water and propylene glycol (PG...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.28.1684
更新日期：2005-09-01 00:00:00
abstract：:The convulsant interaction between enoxacin (ENX), a new quinolone antibacterial agent (NQ), and felbinac (FLB), a non-steroidal anti-inflammatory drug (NSAID), in vivo was reproduced as the change of GABA-induced current response in Xenopus oocytes injected with mouse brain mRNA. GABA (10 microM) response was inhibit...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.16.726
更新日期：1993-07-01 00:00:00
abstract：:The predictability of serum vancomycin (VCM) concentrations by means of the Bayesian method was evaluated to establish whether the method can be used to select safe and effective VCM treatment regimens for individual patients. Serum VCM concentrations at the trough and 2 h after the end of infusion (peak) were measure...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.25.1333
更新日期：2002-10-01 00:00:00
abstract：:Cisplatin-induced nephrotoxicity is related to an increase in lipid peroxidation and oxygen free radicals in a kidney. In the present study, we investigated the effect of the dietary antioxidants, capsaicin (Cap), against cisplatin-induced lipid peroxidation and nephrotoxicity in rats. Nephrotoxicity induced by treatm...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.28.1635
更新日期：2005-09-01 00:00:00
abstract：:A novel constituent, shamimicin, 1"', 1"'-bis-2-(3,4-dihydroxyphenyl)-3,4-dihydro-3,7-dihydroxy-5-O-xylopyranosyloxy-2H-1-benzopyran along with lupeol, which possesses potent hypotensive activity, has been isolated from Bombax ceiba stem bark. BCBMM--one of the most active hypotensive fractions has revealed its advers...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.26.41
更新日期：2003-01-01 00:00:00
abstract：:To ascertain if there is stereoselectivity in peroxisomal proliferation induced by chiral peroxisome proliferators, induction by stereoisomers of 2-methyl-4'-chlorophenoxyacetic acid and 2-methyl-2-(2'-4'-dichlorophenoxy)acetic acid were studied in rat in vivo and in vitro with isolated rat hepatocytes. No significant...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.16.39
更新日期：1993-01-01 00:00:00
abstract：:Regorafenib is a small molecule inhibitor of tyrosine kinases, and has been shown to improve the outcomes of patients with advanced colorectal cancer and advanced gastrointestinal stromal tumors. The transport profiles of regorafenib by various transporters were evaluated. HEK293/organic anion transporting polypeptide...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b14-00740
更新日期：2015-01-01 00:00:00
abstract：:Two conjugates of marine polysaccharide (MPS) and bovine serum albumin (BSA) were prepared using two methods, periodate oxidation and reductive amination, with the intent of enhancing its immunogenicity. Sera samples from Balb/c mice immunized with the products named MPS-BSAp and MPS-BSAr respectively were evaluated b...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.1532
更新日期：2004-10-01 00:00:00
abstract：:Meiosis activating sterol (MAS), the intermediate of cholesterol biosynthesis, is an important substance to stimulate oocytes maturation in FSH-induced signal transduction pathway. Lanosterol 14alpha-demethylase (CYP51) converts lanosterol to MAS. Although MAS is firstly isolated from bovine testis, the information ab...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.29.430
更新日期：2006-03-01 00:00:00
abstract：:Potent ligands of peroxisome proliferator-activated receptor γ (PPARγ) such as thiazolidinediones (pioglitazone, troglitazone, etc.) improve insulin sensitivity by increasing the levels of adiponectin, an important adipocytokine associated with insulin sensitivity in adipose tissue. Several constituents from medicinal...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章,评审
doi：10.1248/bpb.b14-00037
更新日期：2014-01-01 00:00:00
abstract：:In our previous paper, mixed polyetheleneglycol (PEG) modification of liposomes by a mixture of 1-monomethoxypolyethyleneglycol-2,3-distearoylglycerol (PEG-DSG) with short polyoxyethylene chain and PEG-DSG with long one was shown to increase fixed aqueous layer thickness (FALT) around the liposomal membrane, and this ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.30.208
更新日期：2007-01-01 00:00:00
abstract：:We aimed to identify a novel flavonoid from the in-house natural products to suppress matrix metalloproteases (MMPs), which is responsible for degradation of collagen and other extracellular matrix proteins. Total eight natural products were screened for identification of a novel MMP-9 suppressor using MMP-9 reporter ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b13-00534
更新日期：2014-01-01 00:00:00
abstract：:D-Aspartate (D-Asp), a free D-amino acid found in mammals, plays crucial roles in the neuroendocrine, endocrine, and central nervous systems. Recent studies have implicated D-Asp in the pathophysiology of infertility and N-methyl-D-Asp receptor-related diseases. D-Asp oxidase (DDO), a degradative enzyme that is stereo...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b14-00690
更新日期：2015-01-01 00:00:00
abstract：:Darexaban maleate is a novel oral direct factor Xa inhibitor. Darexaban glucuronide (YM-222714) was the major component in plasma after oral administration of darexaban to humans and is the pharmacologically active metabolite. Additionally, YM-222714 N-oxides were detected as minor metabolites in human plasma and urin...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.35.413
更新日期：2012-01-01 00:00:00
abstract：:Sixteen cardenolides, two hemiterpenoids, two phenylpropanoids and a phenylethanoid isolated from the roots of Streptocaulon juventas (LOUR.) MERR. were examined for their antiproliferative activity toward three human-derived (HT-1080 fibrosarcoma, lung A549 adenocarcinoma, cervix HeLa adenocarcinoma) and three murine...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.26.1431
更新日期：2003-10-01 00:00:00
abstract：:Endogenously produced reactive oxygen species reportedly stimulate insulin secretion from islet β-cells. However, the molecular machinery that governs the oxidant-induced insulin secretion has yet to be determined. The present study demonstrates, using rat islet β-cell-derived RINm5F cells, the involvement of the tran...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.35.346
更新日期：2012-01-01 00:00:00
abstract：:Oxidative stress is recognized as an important mediator of brain disorders. Nevertheless, there are few antioxidants approved for brain diseases. There are two types of mechanisms as antioxidant systems in vivo, antioxidants and antioxidant enzymes. Antioxidants are consumed by the reaction with reactive oxygen specie...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章,评审
doi：10.1248/bpb.b17-00091
更新日期：2017-01-01 00:00:00
abstract：:The total alkaloid fractions of the methanolic extracts of the leaves, ripe fruits, roots, seeds and stem of Solanum pseudocapsicum were subjected to in-vitro cytotoxicity, short-term toxicity and long-term survival studies. All the five fractions exhibited potent activity. The total alkaloid fraction of leaves was fo...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.528
更新日期：2004-04-01 00:00:00
abstract：:The effect of gel-forming (1-->3)-beta-D-glucan on the immunological activities of murine kupffer cells was examined. A branched type gel-forming (1-->3)-beta-D-glucan, GRN, was administered intravenously to mice. GRN associating to kupffer cells was detected by an immunohistochemical technique using anti-GRN antibody...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.21.278
更新日期：1998-03-01 00:00:00
abstract：:Propiverine hydrochloride, oxybutynin hydrochloride and terodiline hydrochloride have both anticholinergic and antispasmodic effects, and are used for the management of urinary frequency and incontinence. The average standard therapeutic doses of these drugs differ greatly. We retrospectively analyzed their pharmacolo...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.30.1297
更新日期：2007-07-01 00:00:00
abstract：:The purpose of this research is improvement of therapeutic treatment for periodontitis by using lipophilic and/or hydrophilic zinc materials. The sample suspension injections were prepared from zinc octanate (C8Zn), zinc stearate (C18Zn), zinc sulfate hepta-hydrate (ZnSO4) and tricalcium phosphate (ZnTCP) containing 6...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b12-00218
更新日期：2012-01-01 00:00:00
abstract：:Madecassoside (MA), one of the principle terpenoids in Centella asiatica, has shown protect effect on isolated rat hearts and isolated cardiomyocytes against reperfusion injury in our previous studies. The aim of this study is to investigate if MA also protected against myocardial ischemia-reperfusion injury in vivo. ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.458
更新日期：2008-03-01 00:00:00
abstract：:The effect of insulin administration on bone formation was investigated in the femoral diaphysis of rats with skeletal unloading. When the femoral-diaphyseal tissues from normal rats were cultured in the presence of insulin (10(-9) and 10(-8) M) for 48 h, the hormone produced a significant increase of alkaline phospha...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.16.1179
更新日期：1993-11-01 00:00:00
abstract：:The gastric H+, K+-ATPase is a proton pump that is responsible for gastric acid secretion and that actively transports protons and K+ ions in opposite directions to generate in excess of a million-fold gradient across the membrane under physiological conditions. This pump is also a target molecule of proton pump inhib...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章,评审
doi：10.1248/bpb.27.1
更新日期：2004-01-01 00:00:00
abstract：:The interaction of human leukocyte antigen (HLA) with specific drugs is associated with delayed-type hypersensitivity reactions, which cause severe cutaneous toxicity. Such interactions induce structural alterations in HLA complexes via several different mechanisms such as the hapten theory, p-i concept, and altered p...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b20-00102
更新日期：2020-01-01 00:00:00
abstract：:The ICR/f rat is a recessive-type hereditary cataractous strain, and opacity in the lens usually becomes evident at around 75 d of age. We previously found that the instillation of eye drops containing a disulfiram and hydroxypropyl-beta-cyclodextrin inclusion complex (DSF eye drops) delays lens opacification in ICR/f...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.981
更新日期：2008-05-01 00:00:00
abstract：:It has been identified that skeletal muscle is an endocrine tissue. Since skeletal muscle aging affects not only to muscle strength and function but to systemic aging and lifespan, myokines secreted from skeletal muscle may be crucial factors for intertissue communication during aging. In the present study, we investi...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b17-00969
更新日期：2018-01-01 00:00:00
abstract：:Lutein is a carotenoid and it has antioxidant effects. Lutein may have a protective effect on ischemia reperfusion (I/R) injury induced by free radical species. However, little is known about the protective effect of lutein on I/R injury in vivo. The present study was undertaken to clarify the protective effects of lu...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.29.1764
更新日期：2006-08-01 00:00:00
abstract：:The pulmonary vein contains a myocardial layer extending from the left atrium, which is receiving attention as the source of ectopic electrical activity underlying atrial fibrillation. Electrophysiological and pharmacological analysis of the pulmonary vein myocardium performed in various experimental animal species ha...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章,评审
doi：10.1248/bpb.b212020
更新日期：2013-01-01 00:00:00
abstract：:Five rabbit aldo-keto reductases (AKRs) that participate in the reduction of drug ketones and endogenous ketosteroids have recently been cloned and characterized. Among them, AKR1C30 and AKR1C31 show the highest amino acid sequence identity of 91%, but markedly differ in their substrate specificity and inhibitor sensi...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b14-00555
更新日期：2014-01-01 00:00:00
