bluuebunny/crossref_metadata_2025_split huggingface dataset:
Effects of Ascorbic Acid on Interactions between Ciprofloxacin and Ferrous Sulphate, Sodium Ferrous Citrate or Ferric Pyrophosphate, in Mice
Authors: Motoya Toshiro , Miyashita Masahide , Kawachi Akio , Yamada Katsushi 
Published: July 2003

Abstract
The absorption of ciprofloxacin has been reported to be impaired by concomitant administration of ferrous sulphate. The effects of sodium ferrous citrate and ferric pyrophosphate, which have been used as extensively as ferrous sulphate, on the absorption of ciprofloxacin were compared with that of ferrous sulphate. The effects of ascorbic acid on the interactions between ciprofloxacin and each iron compound were studied in mice. Mice were treated orally with ciprofloxacin (50 mg kg−1) alone, the iron compound (ferrous sulphate, sodium ferrous citrate or ferric pyrophosphate; 50 mg elemental iron kg−1) alone, ciprofloxacin with each iron compound or ciprofloxacin in combination with each iron compound and ascorbic acid (250 mg kg−1).
The maximum serum concentration of ciprofloxacin was significantly (P &lt; 0.01) reduced from 1.15 ± 0.11 μg mL−1 (ciprofloxacin alone) to 0.17 ± 0.01, 0.27 ± 0.01 or 0.28 ± 0.02 μg mL−1, respectively, when ferrous sulphate, sodium ferrous citrate or ferric pyrophosphate was administered along with ciprofloxacin. The addition of ascorbic acid did not affect the inhibitory effects of each iron compound on the absorption of ciprofloxacin. Ciprofloxacin did not affect the variation of serum iron levels after administration of each iron compound. The addition of ascorbic acid significantly (P &lt; 0.01) enhanced the increase in serum iron concentration after administration of sodium ferrous citrate, showing an increase from 270 ± 6 μg dL−1 to 463 ± 11 μg dL−1 compared with an increase from 248 ± 8 μg dL−1 to 394 ± 18 μg dL−1 after administration of sodium ferrous citrate alone. Ascorbic acid also caused a significant (P &lt; 0.01) increase in serum iron concentration from 261 ± 16 μg dL−1 to 360 ± 12 μg dL−1 after administration of ferric pyrophosphate, although it did not affect the levels after ferrous sulphate administration.
The results suggest that sodium ferrous citrate and ferric pyrophosphate should not be administered with ciprofloxacin (as for ferrous sulphate) and that sodium ferrous citrate is converted to the ferric form more easily than ferrous sulphate. This difference in convertibility might contribute to a clinical difference between sodium ferrous citrate and ferrous sulphate.
Effects of Trimebutine Maleate on Delayed Rectifier K+ Currents in Guinea-pig Ventricular Myocytes
Authors: Morisawa Tsuyoshi , Hasegawa Junichi , Tanabe Katsuyuki , Watanabe Ayako , Kitano Masayuki , Kishimoto Yosuke 
Published: July 2003

Abstract
The effects of trimebutine maleate, a drug commonly used to regulate motility in the gastrointestinal tract, on the delayed rectifier K+ current (IK) were evaluated in guinea-pig ventricular myocytes to determine whether the drug has a proarrhythmic effect through blockade of IK.
Trimebutine decreased IK in a concentration-dependent manner. To investigate the effects of trimebutine on two components of IK (IKr and IKs; rapidly activated and slowly activated components, respectively), we performed the envelope-of-tails test. Trimebutine-sensitive IK was determined by digital subtraction of IK during exposure to trimebutine from control IK for each duration of the test pulse over the range 50 ms-2 s. The ratio of ΔIK, tail/ΔIK plotted against pulse duration for trimebutine-sensitive IK gradually decreased to a steady-state value as the duration of the test pulse was lengthened. This finding suggested a weak inhibitory effect of trimebutine on both IKr and IKs. The effects of trimebutine on the inward rectifier K+ current (IKl) responsible for the resting potential and final repolarization phase of the action potential were investigated by applying voltage clamp ramps over a broad range of potentials. No significant effects were observed at 10 or 100 μm. We next investigated the effects of the drug on the L-type Ca2+ current (ICa). Significant inhibition of ICa was observed at trimebutine concentrations greater than 10 μm.
These results suggested that trimebutine maleate has weak inhibitory effects on IKr, IKs and ICa at concentrations much higher than those in clinical use.
Endothelium-dependent Sensory Non-adrenergic Non-cholinergic Vasodilatation in Rat Thoracic Aorta: Involvement of ATP and a Role for NO
Authors: Park Jong Il , Shin Chang Yell , Lee Young Wook , Huh In Hoi , Sohn Uy Dong 
Published: July 2003

Abstract
The involvement of non-adrenergic non-cholinergic (NANC) transmitters, such as adenosine 5′-triphosphate (ATP) and nitric oxide (NO), in the neurogenic relaxation of rat thoracic aorta was investigated in vessel segments suspended for isometric tension recording by polygraph.
Responses to electrical field stimulation (EFS) and exogenous vasodilator were investigated in vessels precontracted with 5-hydroxytryptamine. EFS (100 V, 2–16 Hz, for 10 s at 3-min intervals), in the presence of guanethidine (10 μm) and atropine (10 μm) produced frequency-dependent relaxations. Pretreatment with tetrodotoxin (1 μm) markedly reduced the relaxation and desensitization with capsaicin (10 μm) significantly inhibited the relaxation. Exogenously added ATP caused concentration-dependent relaxations. Mechanical removal of the endothelium significantly inhibited EFS- and ATP-induced relaxation by 30 ± 3% and 37 ± 2%, respectively. Pretreatment with a P1-purinoceptor antagonist, 8-phenyltheophylline (10 μm) or P2X-purinoceptor antagonist, Evans blue (10 μm) did not influence the relaxations to EFS and exogenously added ATP. In contrast, the P2Y-purinoceptor antagonist, basilen blue (100 μm) markedly reduced the relaxations to EFS by 52 ± 4% in the endothelium-intact preparations. However, in the endothelium-denuded preparations and capsaicin-pretreated preparations, basilen blue did not change relaxations elicited by EFS. The NO synthase inhibitor, NG-nitro-l-arginine methyl ester (l-NAME, 100 μm) also significantly inhibited the relaxations to EFS and ATP by 40 ± 6% and 30 ± 2%, respectively, in the endothelium-intact preparations but had no effect on the relaxations in the endothelium-denuded preparations or capsaicin-pretreated preparations. In addition, the EFS-induced relaxations were also inhibited 43 ± 7% by pretreatment with 1H-[1,2,4]-oxadiazolo[4,3-α]quinoxalin-1-one (ODQ; 1 μm), soluble guanylate cyclase inhibitor.
This study suggests that the NANC nerve system is present in the thoracic aorta of rat, mediating vasodilatation by sensory nerves. ATP, as a neurotransmitter released from sensory nerves, activates P2Y-purinoceptors located on the endothelium and stimulates the NO/cyclic GMP pathway, resulting in vasodilatation.
Differential Potency of Beclomethasone Esters In-vitro on Human T-lymphocyte Cytokine Production and Osteoblast Activity
Authors: Seeto Celina , Namkung-Matthai Heeja , Jayram Shalini , Foe Kuncoro , Brown Ken F , Hughes J Margaret , Mason Rebecca S , Armour Carol L , Seale J Paul 
Published: July 2003

Abstract
Beclomethasone dipropionate is an inhaled corticosteroid, used for the treatment of asthma. It is metabolised to 17-beclomethasone monopropionate, which has greater affinity for corticosteroid receptors than the parent compound, and to beclomethasone. We investigated the potency of beclomethasone dipropionate, 17-beclomethasone monopropionate and beclomethasone (compared with dexamethasone as a reference steroid) in two different human cell types, peripheral blood mononuclear cells and osteoblasts.
We found that beclomethasone dipropionate, 17-beclomethasone monopropionate (EC50 10−14 m) and beclomethasone (EC50 approx. 10−12 m) were much more potent than dexamethasone (EC50 10−8 m) in inhibiting interleukin-5 production by peripheral blood mononuclear cells. In contrast, beclomethasone dipropionate, 17-beclomethasone monopropionate and beclomethasone were equipotent with dexamethasone (EC50 range 0.3–1.2 times 10−9 m) in affecting several functional assays of osteoblasts (e.g. alkaline phosphatase activity and osteocalcin synthesis).
These results show that the relative bioactivities of corticosteroids vary between different human cell types, and that affinities observed in receptor binding assays are not necessarily predictive of the bioactivity in cell populations, such as peripheral blood mononuclear cells and osteoblasts, which are putatively relevant to efficacy and side effects respectively.
Structure-Activity Relationships of Anthraquinones in the Decrease of Intestinal Motility
Authors: Kuo Daih-Huang , Kuo Sheng-Chu , Cheng Juei-Tang 
Published: July 2003

Abstract
The effects of substituted anthraquinones on intestinal motility were evaluated in-vitro using rabbit small intestinal strips.
This structure-activity relationship study revealed the critical requirement of a hydroxy group at R2 position. The intestinal motility was inhibited 50% (IC50) by emodine (8 μM), 2-hydroxy anthraquinone (20 μM), 2,6-dihydroxy anthraquinone (25 μM), 2,7-dihydroxy anthraquinone (10 μM), 1,2,4-trihydroxy anthraquinone (80 μM) and 1,2,5,8-tetra-hydroxy-anthraquinone (9 μM). The presence of other polar groups at R2 position such as an amino, aldehyde and carboxylic acid group significantly reduced the activity (IC50 360–400 μM). The presence of a methyl group and esterification of the carboxylic acid at R2 position was found to abolish the activity.
These data are useful for the future development of anthraquinones as laxative agents.
The Effect of Progesterone on Spontaneous and Agonist-Evoked Contractions of the Rat Aorta and Portal Vein
Authors: Mukerji Mark S , Leathard Helen L , Huddart Henry 
Published: July 2003

Abstract
The mechanisms underlying the suppression of vasocontractility caused by progesterone were investigated by studying changes in the contractile force of rat isolated aorta and portal vein, induced by altering extracellular concentrations of noradrenaline (NA) potassium ions (K+) and calcium ions (Ca2+).
In the aorta, progesterone (10 μM) had a general suppressive effect on NA-, Ca2+- and K+-induced contractions. In contrast, in the portal vein a more selective suppression of contractions was observed. Both tonic and phasic components of contractions induced by cumulative addition of Ca2+ to tissues equilibrated in Ca2+-free saline were suppressed. The phasic but not tonic components of contractions induced by NA addition were suppressed. There was no significant effect on tonic contractions induced by elevated (40–120 mM) K+, but a concentration-dependent suppression of the phasic component of contractions was observed during depolarisation with smaller elevations of K+ concentrations (5–20 mM).
These results suggest that on the portal vein the suppressive effect of progesterone is due to a potassium channel opening action, whilst on the aorta a different or additional mechanism of suppression exists.
Effects of the Oral Administration of a β3-Adrenergic Agonist on Lipid Metabolism in Alloxan-Diabetic Rats
Authors: Milagro Fermín I , Martínez J Alfredo 
Published: July 2003

Abstract
Previous studies have reported that β3-adrenergic agonists regulate plasma glucose, triglycerides and free fatty acids in situations of hyperglycaemia and dyslipidaemia in rodents. In this study Trecadrine, a novel compound with affinity for β3-adrenergic receptors, has been tested in an alloxan-induced model of hyperglycaemia in rats.
Alloxan-induced hyperglycaemic rats were orally treated with Trecadrine (1 mg/kg/day for 4 days), resulting in an improvement of hyperglycaemia (from 16.6 to 8.3 mmol L−1, P &lt; 0.001). This effect was not associated with statistical differences in plasma insulin levels, which may be explained by changes in insulin resistance and carbohydrate oxidation in peripheral tissues. Furthermore, a reduction in internal white fat weight (-39%), which was not statistically significant, as well as in plasma triglycerides (from 1.89 to 0.33 mmol L−1, P &lt; 0.001) and free fatty acids (from 0.70 to 0.39 mmol L−1, P &lt; 0.001), was found after Trecadrine administration. Trecadrine apparently induced lipolytic activity in adipocytes, as suggested by the increase of oxygen consumption in white adipose tissue (+282%, P &lt; 0.001), while free fatty acids decreased apparently through their utilisation in other tissues. Furthermore, the increase in brown adipose tissue oxygen consumption (+50%, P &lt; 0.01) and in rectal temperature (P &lt; 0.05) suggests that both glucose and fatty acid oxidation may be enhanced in this tissue.
These results give support to the possible therapeutic use of β3-adrenergic compounds in situations of hyperglycaemia, particularly when this is accompanied by hypertriglyceridaemia.
Inhibition of Vascular Smooth Muscle Tone by the H+, K+-ATPase Inhibitor SCH 28080
Authors: Rhoden Kerry J 
Published: July 2003

Abstract
Vascular smooth muscle is thought to possess an H+-K+ ATPase that contributes to the regulation of intracellular K+ concentration and pH. We have examined the effect of the H+, K+-ATPase inhibitor SCH 28080 on vascular smooth muscle tone in guinea-pig and human isolated arteries, and on 86Rb+ uptake in cultured guinea-pig aortic smooth muscle cells.
SCH 28080 (0.1–300 μM) produced relaxation of isolated guinea-pig aorta, guinea-pig pulmonary artery and human pulmonary artery. Relaxation occurred in tissues pre-contracted with phenylephrine, histamine or the thromboxane mimetic U44069. Relaxation was reversible, and was not affected by tetrodotoxin, indomethacin, nordihydroguiaretic acid (NDGA), 1-aminobenzotriazole (1-ABT), NG-nitro-L-arginine methyl ester (L-NAME), removal of the endothelium or removal of extracellular K+. SCH 28080 had no effect on 86Rb+ uptake in cultured guinea-pig aortic smooth muscle cells.
In conclusion, SCH 28080 relaxes vascular smooth muscle at concentrations known to inhibit the H+-K+ ATPase. The persistence of relaxation in a K+-free medium and the failure of SCH 28080 to inhibit 86Rb+ uptake suggest that relaxation may be unrelated to H+, K+-ATPase inhibition, and indicate that this agent may not be considered as a selective H+, K+-ATPase inhibitor in vascular preparations.
Effect of Iron(III) Chitosan Intake on the Reduction of Serum Phosphorus in Rats
Authors: Baxter Joseph , Shimizu Fuki , Takiguchi Yasuyuki , Wada Masahiro , Yamaguchi Tatsuaki 
Published: July 2003

Abstract
Because of the widespread use of aluminium- and calcium-containing phosphate binders for the control of hyperphosphataemia in patients with end-stage renal failure, an iron(III) chitosan complex was synthesised and fed to rats to measure its effect on serum phosphorus and calcium, intestinal phosphate binding and phosphate absorption.
Thirty-six Wistar rats were randomly selected and distributed into a baseline group (n = 6), a control group (n = 8 (days 0–15), n = 8 (days 16–30)) and a treatment group (n = 8 (days 0–15), n = 8 (days 16–30)). The control groups ingested AIN-76 diet mix with a 1% w/w fibre content; however, the treatment groups had the fibre content completely substituted with iron(III) chitosan. The mean weights of the treated rats were slightly lower from 15 days (not significant); but overall, rat growth was not stunted in the treatment groups. The serum phosphorus levels of the treated group (n = 8) were significantly reduced after 15 days (P = 0.004; control: 5.7 ± 0.9 mg dL−1; treatment: 4.4±0.5 mg dL−1; 95% CI of difference: 0.5–2.2) and 30 days (P = 0.002; control: 5.5 ± 0.9 mg dL−1; treatment = 4.1 ± 0.6 mg dL−1; 95% CI of difference: 0.6–2.3) as compared with the respective control group. The serum calcium-phosphorus product was 62.0 ± 12.1 mg2 dL−2 for the control and 45.1 ± 6.6 mg2 dL−2 for the treatment group after 30 days (P = 0.004). The serum iron concentration of the treatment group did not differ from the baseline value after 15 and 30 days, but the treatment group was significantly higher than the control group (P &lt; 0.05) after 30 days. The faeces phosphorus levels (mg day−1) were higher (P &lt; 0.01) and its iron content was much higher (P &lt; 0.01) for the treated group. The urine phosphorus (mg kg−1) was not significantly reduced for the treated group, but the mean was consistently less. The kidney and liver weights of both groups were similar, but the phosphorus content of the kidney (mg (g kidney)−1) was higher for the treated group after 30 days (P = 0.041; control, 4.2 ± 1.2 mg g−1 vs treatment, 5.6 ± 1.4 mg g−1. Because iron(III) chitosan had a high phosphorus-binding capacity of 308 (mg P) per gram of Fe3+ for both the in-vitro (pH 7.5) and in-vivo studies, which is greater than nearly all commonly used phosphate binders, and a small net phosphorus absorption difference of 3.7 mg day−1, it is an efficient phosphate binder for lowering serum phosphate levels without increasing serum calcium levels.
The Ethanol-soluble Part of a Hot-water Extract from Artemisia iwayomogi Inhibits Liver Fibrosis Induced by Carbon Tetrachloride in Rats
Authors: Park Eun-Jeon , Nan Ji-Xing , Kim Ji-Young , Kang Hee-Chul , Choi Jung Hwan , Lee So Jung , Lee Bo Hye , Kim Sun Jin , Lee Jae Hyun , Kim Yoon Chul , Sohn Dong Hwan 
Published: July 2003

Abstract
This study was carried out to investigate the protective effects of the hot-water extract from Artemisia iwayomogi (Compositae) on carbon tetrachloride-induced liver fibrosis in rats.
Liver injury was induced by oral administration of carbon tetrachloride (1 mL kg−1) twice a week during 4 weeks of A. iwayomogi treatment. Extracts from A. iwayomogi were prepared and administered to rats orally (2 g kg−1 as A. iwayomogi for 4 weeks) as follows: group 1, hot-water extract; group 2, ethanol-soluble part of hot-water extract; group 3, ethanol-insoluble part of hot-water extract; and group 4, methanol extract.
In rats treated with the ethanol-soluble part of the hot-water extract, liver hydroxyproline content was reduced to 74% that of carbon tetrachloride control rats (P &lt; 0.05). Protein expression of alpha smooth muscle cell like actin was also decreased in rats treated with the ethanol-soluble part of the hot-water extract, which indicates inhibition of hepatic stellate cell activation. Liver malondialdehyde levels were significantly lowered in rats treated with the ethanol-soluble part of hot-water extract (P &lt; 0.05). Serum cholesterol levels in rats treated with hot-water extract, ethanol-soluble or -insoluble parts of hot-water extract or methanol extract were significantly reduced when compared with those of carbon tetrachloride control rats (P &lt; 0.05).
The ethanol-soluble part of the hot-water extract from A. iwayomogi inhibited fibrosis and lipid peroxidation in rats with liver fibrosis induced by carbon tetrachloride. Both hot-water extract (either ethanol-soluble or -insoluble) and methanol extract of A. iwayomogi also lowered serum cholesterol levels in fibrotic rats.
Antitumour Activity and Side Effects of Combined Treatment with Chitosan and Cisplatin in Sarcoma 180-Bearing Mice
Authors: Kimura Yoshiyuki , Onoyama Mitsuko , Sera Toshiki , Okuda Hiromichi 
Published: July 2003

Abstract
We examined the possible modulation by chitosan of the antitumour effects and side effects of cisplatin (cis-diaminedichloroplatinum, CDDP). The study showed that CDDP had potent antitumour activity when administered orally as well as intraperitoneally. We also compared the antitumour activity and side effects of orally administered CDDP plus orally administered chitosan versus intraperitoneally administered CDDP plus orally administered chitosan in sarcoma 180-bearing mice.
When CDDP (1.25 mg kg−1 × 2 day−1) was intraperitoneally administered to sarcoma 180-bearing mice, myelotoxicity (the reduction of leucocyte and platelet numbers), nephrotoxicity (the increase of blood nitrogen urea level), immunotoxicity (the reduction of spleen and thymus weight) and a reduction in body weight resulted. These intraperitoneally administered CDDP-induced side effects were not prevented by oral administration of chitosan (150 mg kg−1 × 2 day−1 and 750 mg kg−1 × 2 day−1) for 14 consecutive days. On the other hand, the side effects such as the reductions of body and spleen weights induced by orally administered CDDP (1.25 mg kg−1 × 2 day−1) were prevented by the oral administration of chitosan (150 mg kg−1 × 2 day−1 and 750 mg kg−1 × 2 day−1).
From these results, we conclude that the orally administered chitosan plus CDDP might be useful for the prevention of body weight reduction and immunotoxicity (the reduction of spleen weight) induced by the orally administered CDDP without diminishing antitumour activity.
Effect of Luffa echinata on Lipid Peroxidation and Free Radical Scavenging Activity
Authors: Kumar V Prashanth , Shashidhara S , Kumar M M , Sridhara B Y 
Published: July 2003

Abstract
The dried alcoholic (50%) extract of the plant Luffa echinata was investigated for inhibition of lipid peroxidation, for hydroxyl radical scavenging activity and interaction with 1,1-diphenyl-2-picrylhydrazyl stable free radical (DPPH).
It was found that the test extract exhibited a considerable inhibition of lipid peroxidation and possessed hydroxyl radical scavenging activity. Evaluation of antiradical scavenging activity showed significant interaction with DPPH.
These properties could be considered as a useful and exploitable combination for justifying the reported activity.
In-vitro Inhibition of Human Erythrocyte Acetylcholinesterase by Salvia lavandulaefolia Essential Oil and Constituent Terpenes
Authors: Perry Nicolette S L , Houghton Peter J , Theobald Anthony , Jenner Peter , Perry Elaine K 
Published: July 2003

Abstract
Sage (Salvia spp) is reputed in European herbal encyclopaedias to enhance memory, and current memory-enhancing/anti-dementia drugs are based on enhancing cholinergic activity by inhibiting cholinesterase. In this study the effects of Salvia lavandulaefolia Vahl. (Spanish sage) essential oil and some of its constituent terpenes on human erythrocyte acetylcholinesterase were examined in-vitro. The main constituents in the essential oil batch used for analysis of cholinesterase inhibition were camphor (27%), 1,8-cineole (13%), α- and β-pinene (10–15%) and bornyl acetate (10%) with other minor constituents (1% or less) including geraniol, limonene, linalool, terpineol and γ-terpinene.
Using the Ellman spectrophotometric method, kinetic analysis was conducted on the interaction of the essential oil and the main monoterpenoids, camphor, 1,8-cineole and α-pinene. IC50 values were obtained for the essential oil, 1,8-cineole and α-pinene and were 0.03 μg mL−1, 0.67 mM and 0.63 mM, respectively. Camphor and other compounds tested (geraniol, linalool and γ-terpinene) were less potent (camphor IC50: &gt;10 mM). The essential oil, α-pinene, 1,8-cineole and camphor were found to be uncompetitive reversible inhibitors.
These findings suggest that if the inhibitory activity of the essential oil is primarily due to the main inhibitory terpenoid constituents identified, there is a major synergistic effect among the constituents. Since no single constituent tested was particularly potent, it remains to be determined whether these in-vitro cholinesterase inhibitory activities are relevant to in-vivo effects of the ingestion of S. lavandulaefolia essential oil on brain acetylcholinesterase activity.