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Biomedical subjects

K Tsurumi

Publications and source records attributed to K Tsurumi.

At least 55 records · Page 3Linked to original sources
PubMed1986

Study of drug interaction between the new antiallergic drug 11-oxo-11H-pyrido[2,1-b]quinazoline-2-carboxylic acid and theophylline.

A new chemical compound, 11-oxo-11H-pyrido[2,1-b]quinazoline-2-carboxylic acid (Sm 857), known to inhibit the second stage type I allergy and endowed with antiasthmatic action, was investigated with regard to its effects on theophylline (TP) blood level in comparison with ketotifen and tranilast, antiasthmatics of the same therapeutic category as Sm 857, and tiaramide, an antiinflammatory agent. Sm 857 was administered orally to rats at 50 mg/kg, followed by oral administration of TP at 10 mg/kg or intravenous administration of aminophylline 13 mg/kg 10 min later. The concomitant use of Sm 857 apparently lowered the development of TP blood level during 1-5 h after administration when compared with the control. A similar lowering effect on TP blood level was observed at both single and 3-day prior administration of Sm 857. Ketotifen also reduced TP blood level at a dose of 50 mg/kg, while tranilast proved to have almost no such influence on TP blood level. Unlike the mentioned antiasthmatics, tiaramide tended to delay TP clearance. The determination of TP free fraction produced by addition of testing drugs to TP-containing rat serum in vitro after incubation for a certain period of time revealed a 30% increase in free fraction percent in case of Sm 857 addition, 7% increase in case of tranilast addition and no change at all in case of ketotifen and tiaramide addition. Above results suggest that the concomitant use of Sm 857 and TP might cause drug interaction. Sm 857 is thought to increase the blood free fraction of concomitantly used TP and to accelerate elimination of TP from blood.

Aminophylline↗
PubMed1985

Interaction of BW755C, a potent inhibitor of lipoxygenase and cyclo-oxygenase, with mitochondrial cytochrome oxidase.

The interaction between BW755C (3-amino-1-[m-(trifluoromethyl)phenyl]-2-pyrazoline), a potent inhibitor of both lipoxygenase and cyclo-oxygenase, and respiratory chain in mitochondria and electron transport particles (ETP) from rat livers was examined. BW755C accelerated the oxygen uptake by mitochondria without the addition of substrate for the respiratory chain. Spectrophotometric study revealed that BW755C was quickly oxidized by cytochrome oxidase in mitochondria to a compound possessing an absorption maximum at 524 nm. p-Phenylenediamine (p-diaminobenzene, PPDA), which, like BW755C, serves as an electron donor to cytochrome oxidase, was shown to inhibit the generation of active oxygen in macrophages; the inhibition was stronger than that of BW755C. These results strongly suggest that the oxidative conversion of BW755C by mitochondrial cytochrome oxidase is associated with its potentially inhibitory action on the active oxygen-generating system in phagocytes.

4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyraz↗
PubMed1985

Effects of butorphanol and its metabolites on the levels of monoamines and their metabolites in the rat brain.

The effects of butorphanol and its main metabolites, norbutorphanol and hydroxybutorphanol, on the contents of monoamines and their metabolites in various regions of the rat brain were compared with those of morphine and pentazocine using the HPLC-ECD method. The administrations of morphine and pentazocine increased dopamine turnover in the striatum and hypothalamus in a drug dose-dependent manner. The stimulative effects of butorphanol on the dopamine system were weaker than those of morphine and pentazocine, and there were no dose-dependencies in these effects of butorphanol. Butorphanol, morphine and pentazocine increased 5-HT turnover, but there was no drug dose-dependent effect in the case of butorphanol. These differences for the effects of butorphanol from those of morphine and pentazocine seemed to result from the antagonist-agonist property of butorphanol and from a different manner of interaction with the opioid receptor. The effects of butorphanol on the levels of the norepinephrine system were weak. It was considered that the effects of butorphanol on monoamine turnover were produced by the action of butorphanol itself, because norbutorphanol and hydroxybutorphanol showed little change on the level of monoamines and their metabolites.

3,4-Dihydroxyphenylacetic Acid↗
PubMed1985

Cephem antibiotics and alcohol metabolism.

Mechanisms of the disulfiram-like reaction of cephem antibiotics were studied. Changes in ethanol (EtOH) and acetaldehyde (AcH) levels in the blood with EtOH loading following daily intravenous administration of cephem antibiotics were determined in rats and the following were found: The daily intravenous injection of cefazolin, cefotiam (CTM), cefsulodin, cefoxitin or ceftizoxime in no way varied the changes in the EtOH and AcH levels in the blood with EtOH loading. The daily intravenous injection of cefmetazole, cefoperazone, cefamandole, latamoxef, cefmenoxime or cefotetan caused the AcH level in the blood to be elevated significantly until at least 8 hours after the EtOH loading, but was inert on the EtOH level on the blood. The daily administration of 1-methyl-2-tetrazoline-5-thione (TZ), a compound having a partial structure similar to those of the cephem antibiotics elevating the AcH level in the blood on EtOH loading, was inert on the EtOH level in the blood but elevated the AcH level in the blood. The daily administration of 1-(2-dimethylaminoethyl)-2-tetrazoline-5-thione (MTZ), a compound having a partial structure similar to that of CTM, was inert either on the EtOH or AcH level in the blood. The cephem antibiotics elevating the AcH level in the blood all had a (1-methyl-1H-tetrazol-5-yl) thiomethyl group in the 3 position of the aminocephalosporanic acid nucleus. It was though that the disulfiram-like reaction caused by the cephem antibiotics was derived from the elevation of AcH level in the blood.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetaldehyde↗
PubMed1984

Fractionation and characterization of urinary heparan sulfate excreted by patients with Sanfilippo syndrome.

Urinary heparan sulfates (HS) from two siblings with mucopolysaccharidosis (MPS) III-B were fractionated by chromatography with Dowex 1 and Sephadex G-50. Their Mr ranged from 1600 to 8000, and 95% of them were included in the region less than 5000. Fractions with lower Mr contained larger amounts of O-and N-sulfates. The chemical analysis and deaminative cleavage of HS suggested that an intact HS molecule was composed of some blocks rich in GlcNAc and GlcUA and other blocks rich in GlcNS, IdUA and O-sulfate. GlcNAc-UA-GlcNS-UA-GlcNAc-UA-GlcNAc was found to be a major oligosaccharide of HS with Mr less than 1800. Trisaccharides, GlcNAc-GlcUA-aMan and GlcNAc-IdUA-aMan, were released from the nonreducing end of HS-oligosaccharides by deaminative cleavage. They carried 0-3 moles of ester sulfate. GlcNAc-IdUA-aMan was more sulfated than the other. The release of significant amounts of nonsulfated trisaccharide conform to the enzyme defect in this disease. Urinary HS obtained from another patient with MPS III were examined by the same way. Although the patient was not examined enzymatically, the structure of urinary GAG suggested a defect of alpha-N-acetylglucosaminidase in the patient.

Adolescent↗
PubMed1984

The effect of clidanac, a potent anti-inflammatory drug, on mitochondrial respiration: a consideration on the uncoupling activity of optical enantiomers.

The uncoupling activities of clidanac and its dechlorinated derivative on oxidative phosphorylation were examined using isolated rat liver mitochondria. Clidanac was found to uncouple the oxidative phosphorylation and no difference was detected in the uncoupling potency of the two enantiomorphs. Dechlorclidanac was significantly less effective in the uncoupling activity than clidanac.

Animals↗
PubMed1984

[Active oxygen and anti-inflammatory drug: measurement by luminol dependent chemiluminescence].

The active oxygen produced from stimulated phagocytic cells emits luminol-dependent chemiluminescence (CL) upon reaction with luminol. So the active oxygen was measured by using the CL and the results of this were compared with those by the LDH-NADH method. Moreover, effects of nonsteroidal anti-inflammatory drugs (NSAID) on the generation of active oxygen were studied by both methods. Rat peritoneal and pleural exudated cells (PEEC and PLEC) emitted strong CL on incubation with zymosan, but that from rat whole blood cells was very weak. The effects of superoxide dismutase, catalase, NaN3 and L-ascorbic acid on the generation of active oxygen from rat phagocytic cells were different between CL and LDH-NADH methods. These discrepancies seem to be due to the different kinds of active oxygen that can be measured by both methods. Except for BW-755C, most of the NSAID had only a slight inhibitory effect on the generation of active oxygen measured by both methods, and the ex vivo effect was the same as that observed in vitro. It may be considered that NSAID decrease the phagocytic function of cells by non-specifically stabilizing the biological membrane and inhibit slightly the generation of active oxygen from phagocytes. On the other hand, the CL method could be performed not only in PEEC and PLEC, but also in whole blood cells. From these results, it was suggested that CL measurement can be used as a simple and valuable method for the detection of all types of active oxygen including superoxide anion radical and its metabolites and for testing cellular functions and drug actions on them.

Animals↗
PubMed1983

Adrenergic and cholinergic innervation of the common bile duct in men and cats.

To clarify whether or not the common bile duct (CBD) has peristaltic movement, the muscular structure and intrinsic innervation were investigated for the full length of the CBD in 50 fresh human autopsy specimens and 50 cats. Nearly the same results were obtained in control groups of humans and cats. 1) Abundant sympathetic noradrenergic innervation, mainly composed of two plexuses, was demonstrated in each layer of the common bile duct tissue. 2) Parasympathetic nervous innervation was also abundant in each layer of the common bile duct and was composed of two ganglionated cholinergic plexuses. 3) Human and cat ganglia were composed of several nerve cells, which were mostly of Dogiel type II. 4) No other biogenic monoamines than adrenaline (A) and noradrenaline (NA) were detected. 5) Digestive tract hormones were undetectable. 6) The presence of smooth muscle was confirmed all along the common bile duct in all cases. The muscular tissue of the CBD was more abundant in humans than in cats. 7) The results of quantitation of catecholamine and acetylcholine esterase in the common bile duct tissue demonstrated a good correlation between biochemical and histochemical activities.

Adrenergic Fibers↗
PubMed1983

Anti-inflammatory effect of diclofenac-sodium ointment (cream) in topical application.

This study was performed to develop a topical ointment of diclofenac-Na which has a potent anti-inflammatory activity by oral administration. At first, research was carried out on the ointment base which influences the external anti-inflammatory effect of the drug. Ointments of diclofenac-Na were prepared with three kinds of bases: lipophilic, emulsion (cream) and gel bases; and their anti-inflammatory effects were compared. The cream was found to have the most potent effect. Therefore, in the next experiment, an optimum concentration of diclofenac-Na in cream was determined comparing the anti-inflammatory effect among the cream preparations containing 0.5, 0.75, 1.0 and 1.5% of the drug. Obvious effects were observed with the cream containing 1.0% and 1.5% of the drug concentration, and there was no significant difference in the anti-inflammatory activities of these two concentrations. Based on these results, the cream preparation containing 1.0% of diclofenac-Na (DF cream) was adopted as the external ointment of the drug. The anti-inflammatory effect of this cream was compared with that of existing anti-inflammatory ointments, i.e., indomethacin gel (IM gel), bufexamac cream (BM cream) and mobilat ointment (ML ointment). DF cream produced obvious inhibition on increased vascular permeability and on acute edema and remarkable suppression of ultraviolet erythema. These activities of DF cream were similar to those of IM gel and more potent than those of BM cream and ML ointment. The inhibitory effect of DF cream on the proliferation of granulation tissue was almost equal to that of ML ointment and more distinguishable than that of IM gel and BM cream. In adjuvant arthritis, DF cream reduced the swelling remarkably in the treated paw and slightly in the untreated paw. The anti-adjuvant activity of DF cream was equal to that of IM gel and more potent than that of BM cream and ML ointment. In pain to pressure stimulation, an analgesic effect was observed in the early stage of DF cream application, and its activity was slightly stronger than that of the other ointments. These results show that DF cream has an obvious anti-inflammatory effect as an external preparation, and the activity is comparable or superior to that of similar existing anti-inflammatory ointments. This cream may be considered as useful in the clinical field as a topical anti-inflammatory preparation.

Administration, Topical↗
PubMed1983

Effect of anti-inflammatory drugs on endotoxin-induced diarrhea in mice.

Prostaglandins (PGs) increase the intestinal fluid to result in diarrhea. Some laxatives are known to exert their actions partially by stimulating the PGs biosynthesis. On the other hand, it is well documented that nonsteroidal anti-inflammatory drugs (NSAID) inhibit markedly the PGs biosynthesis. Since endotoxin (ETX) also produces diarrhea similarly in all species of experimental animals, we investigated the effect of various NSAID and steroidal anti-inflammatory drugs (SAID) on ETX-induced diarrhea in mice. ETX given p.o. did not produce diarrhea, but it could induce it after parenteral administration, especially intravenous injection. ALL NSAID and SAID tested inhibited ETX-induced diarrhea at dose levels similar to or lower than those commonly producing an acute anti-inflammatory effect. The anti-diarrheal effects were found in not only acidic NSAID, but also in basic NSAID and SAID which did not inhibited ultraviolet erythema, acute death induced by arachidonic acid injection and PGs biosynthesis. Therefore, this test using ETX-induced diarrhea in mice may be used as a new and desirable method for screening or evaluating anti-inflammatory drugs. The mechanism of diarrheogenic action of ETX is poorly understood, but may be attributed to inhibition of PGs biosynthesis besides other unknown actions.

Animals↗
PubMed1983

The effect of two body positions on head righting in severely disabled individuals with cerebral palsy.

This study examines the association between head righting and two commonly used therapeutic positions: semiprone on an inclined prone positioner and upright short-sitting in an adapted wheelchair. The subjects were 26 individuals with cerebral palsy and multiple handicaps who had difficulty maintaining active head control in a vertical orientation. Such head control is necessary for attending to learning tasks in the classroom and activities of daily living in the clinic. The frequency and duration of head righting during a feeding task was measured by means of a mercury switch system mounted on a headband and attached to an electromechanical digit counter and a clock. Measurements of duration and frequency beyond the predetermined range of functional head righting plus measurements on five control variables were analyzed by four statistical methods: t-test on the means, simple correlation, cannonical correlation, and regression analysis. The control variables were age, mobility level, degree of hypertonicity, level of seizure activity, and level of reflex maturity. Results indicate that, in this severely handicapped population, head righting while in the adapted wheelchair is no different from head righting while in the semiprone position. One control variable, level of independent mobility, was positively correlated with the length of time that subjects were able to maintain head righting in the semiprone position.

Adolescent↗
PubMed1983

[Influence of indomethacin and clidanac on the blood pressure lowering effect of beta-blockers].

In conscious rabbits, the intravenous administration of pindolol (1.25 mg/kg), propranolol (1 mg/kg) and alprenolol (2 mg/kg) induced a highly significant decrease of mean arterial blood pressure and significant bradycardia. In the same model, the intravenous administration of saline, indomethacin, and clidanac did not affect the mean arterial blood pressure and heart rate. Pretreatment with indomethacin and clidanac reduced the effect of these beta-blockers on the mean arterial blood pressure and had no effect on the heart rate. Treating of the guinea pig heart homogenate with 1 microM indomethacin or clidanac decreased the number of beta-adrenoceptors without changing their affinity. These results suggest that indomethacin and clidanac interfere with beta-adrenoceptor-mediated effects.

Adrenergic beta-Antagonists↗
PubMed1983

[Ossification arising in the atypical epithelium in primary stomach cancer--report of a case].

We report a case of primary stomach carcinoma arising in the atypical epithelium, which was accompanied with ossification. The patient was a 73-year-old man, who was operated because of the possibility of advanced Type IIa carcinoma. Grossly, a large papillary polypoid lesion was recognized in the anterior wall of the antrum near the pylorus ring. Histological study revealed well differentiated tubular adenocarcinoma arising in the atypical epithelium; ossification was found in the stroma without necrosis, calcification or chondrification. Ossification arising in primary stomach carcinoma is very rare. Only five cases of ossification in primary stomach carcinoma have been reported in the world literature; two of these were Japanese patients. Probably ours is the first reported case with both stomach carcinoma and ossification arising in the atypical epithelium.

Adenocarcinoma↗