Search PubMed⌕ Search

Biomedical subjects

T Horie

Publications and source records attributed to T Horie.

At least 505 records · Page 28Linked to original sources
PubMed1983

Flavonoids: potent inhibitors of arachidonate 5-lipoxygenase.

Various flavonoids were found to be relatively selective inhibitors of arachidonate 5-lipoxygenase which initiates the biosynthesis of leukotrienes with the activity of slow reacting substance of anaphylaxis. Cirsiliol (3',4',5-trihydroxy-6,7-dimethoxyflavone) was most potent, and the enzyme partially purified from rat basophilic leukemia cells was inhibited by 97% at a concentration of 10 microM (IC50, about 0.1 microM). 12-Lipoxygenases from bovine platelets and porcine leukocytes were also inhibited but at higher concentrations (IC50, about 1 microM), and fatty acid cyclooxygenase purified from bovine vesicular gland was scarcely affected. The compound at 10 microM suppressed by 99% the immunological release of slow reacting substance of anaphylaxis from passively sensitized guinea pig lung (IC50, about 0.4 microM).

Animals↗
PubMed1983

Epidemiology of an outbreak of erythema infectiosum in Tokyo.

Endemic outbreaks of erythema infectiosum were observed in various areas of Japan from 1977 to 1981. Even in a limited district of Tokyo, we recorded 395 cases until June 1981, so this might be the largest epidemic in Japan. Most cases occurred from January to June. The peak incidence was at the age of 7 years and the average age was 8.9 years. The outbreak also occurred among our hospital nurses, but no severe case was observed in hospitalized patients. Furthermore, the symptoms in adults were as mild as in children, suggesting the little participation of immunity in this disease. By epidemiologic survey, erythema infectiosum was distinct from rubella.

Adolescent↗
PubMed1983

Comparison of airway responsiveness to exercise and histamine inhalation in asthmatics.

In order to investigate the differences between EIA positive and negative subjects, pulmonary function data at rest, atopic tendency and bronchial sensitivity and reactivity were compared. Pulmonary function data revealed no significant difference between two groups except closing volume which was higher in EIA positive patients (p less than 0.01) and also Rrs which was higher in EIA positive patients only in female (p less than 0.05). Incidence of positive skin tests and higher levels of IgE were more frequent in EIA positive, however, IgE was not significantly different. Relationship between % fall of FEV1 after exercise and bronchial sensitivity was examined, however, no correlation was found in two parameters. Bronchial reactivity was not different in two groups. This suggests that EIA positive patients cannot be distinguished from EIA negative by pulmonary function data at rest or by atopic tendency, and also that different mechanisms play a role to produce airway constriction following exercise and inhalation challenge.

Adolescent↗
PubMed1983

[CT scan in severe head injury with special reference to Glasgow coma scale].

CT scan demonstrates the invaluable information about the parenchymal lesions of head injuries. The parenchymal lesions were classified into 6 categories; 1) isodensity without mass effect: I(-), 2) isodensity with mass effect: I(+), 3)high density: H, 4) high-low density complex: H-L, 5) low density: L, 6) diffuse cerebral swelling: DCS. Glasgow coma scale (GCS) and outcome scale (GOS) were international practical scales for the evaluation of severity and prognosis of severe head injuries. One hundred and seventy-four cases with severe head injury were analysed. I(+), H and H-L were common findings in the group of GCS 3-6, and I(-) was in GCS 7-12 and GCS 13-15. H and H-L were not related with GCS. DCS was most common in GCS 7-12. Acute epidural hematoma was frequent in the group of GCS 13-15, and acute subdural hematoma was in GCS 3-6. The prognosis was significantly poor in the group of GCS 3-6, with the mortality of 72 percents. On the other hand, the prognosis was quite good in GCS 7-12 and GCS 13-15. There were few reports about the traumatic subarachnoid hemorrhage (SAH). SAH was one of the important risk factors in severe head injuries and it was frequently associated with I(+), H and H-L. The prognosis of the patients with SAH was most unfavorable in the presence of I(+). Number of analyses were reported about the traumatic intraventricular hemorrhage (IVH). IVH was also one of the powerful risk factors and this was commonly associated with H and H-L. The prognosis of the patients with IVH was very poor. Finally, the groups of the patients, whose prognoses turned out to be unexpected results from GCS on admission, were analysed. First, the age was an important factor. In the patients, whose prognoses were good in spite of low GCS, I(-) was a mostly common finding, while SAH, IVH and obscured cisterns, esp. basal and quadrigeminal, were less common. In the patients, whose prognoses were poor despite of favorable GCS, H and H-L were common findings. SAH and IVH were also common. The poor prognosis was induced by secondary systemic complications, such as pneumonia and meningitis, etc.

Adolescent↗
PubMed1982

Inhibition of aldose reductases from rat and bovine lenses by flavonoids.

Thirty flavones, four isoflavones and thirteen coumarins were tested as inhibitors of lens aldose reductase, which is believed to participate in the initiation of cataract formation in diabetes. Many were found to be potent inhibitors, and the two most potent ones were axillarin (5,7,3',4'-tetrahydroxy-3,6-dimethoxyflavone) and 6,3',4'-trihydroxy-5,7,8-trimethoxyflavone (LARI 1). These two flavones inhibited aldose reductase purified from rat lens with IC50 values of 2.6 X 10(8) and 3.6 X 10(8) M respectively. They also inhibited aldose reductase purified from bovine lens with IC50 values of 1.8 X 10(7) M. The potencies of the two compounds were superior to those of all the previously reported inhibitors of aldose reductase. Inhibition of rat and bovine lens aldose reductases by the two compounds was of a non-competitive type with DL-glyceraldehyde as the variable substrate. Some flavones including axillarin and LARI 1 were found to be poorly or scarcely inhibitory against several adeninenucleotide-requiring enzymes, which are involved in glycolysis and other metabolic reactions. These results obtained show that the two flavones have some features which may be required in clinically useful drugs for diabetic patients. All the potent inhibitors of the compounds tested had a flavone skeleton, one (or two free) hydroxyl(s) in ring C, and more than three hydroxyls (free or methylated) in ring A. The possible relationships of structures to inhibitory potencies of the compounds tested are discussed.

Aldehyde Reductase↗
PubMed1982

Determination of tripamide and its metabolites in plasma, red blood cells and urine by high-performance liquid chromatography.

A procedure for the determination of tripamide and its hydroxylated metabolites in plasma, red blood cells and urine by reversed-phase high-performance liquid chromatography is described. The concentrations in red blood cells showed a monophasic decline and the half-life was 9.5 h. The concentration in red blood cells was markedly higher than that in plasma, showing that 95-98% of the drug is present in whole blood, after a dose of tripamide (90 mg) in man. The specificity and sensitivity of this procedure appear to be satisfactory for pharmacokinetic studies.

Adult↗
PubMed1982

Antimicrobial characteristic of insoluble alkylpyridinium iodide.

Insoluble and soluble alkylpyridinium iodides (C8 to C18) were synthesized. The insoluble agents were quaternized 4-vinylpyridine-divinylbenzene copolymers. The insoluble agent [C12(50)] that contained 50% divinylbenzene and had a C12 alkyl chain was selected as the most suitable insoluble agent. C12(50) showed poor durability of the antibacterial activity, but C12(50), which had lost the activity, was refreshed by washing with ethanol. This washing became ineffective after a few cycles of antibacterial treatment and refreshment. Such C12(50) recovered the activity upon 1.0 N NaOH treatment. The antibacterial activity of C12(50) depended on its surface area. It showed high antimicrobial activity against gram-positive bacteria and also showed activity against gram-negative bacteria and yeasts. But the activities of C12(50) and laurylpyridinium iodide solution were different against some microbes. The antibacterial activities of the agents were investigated against Escherichia coli and Micrococcus luteus under various conditions. The activity of C12(50) was higher at a higher temperature or at a lower cell concentration. The activity of C12(50) decreased on addition of NaCl, glucose, or bovine albumin to the cell suspension or in 0.01 M sodium-potassium phosphate buffer. C12(50) showed less activity when cells were mixed with dead cells or the supernatant of dead cells killed in an autoclave. The mode of action of the laurylpyridinium iodide solution against E. coli and M. luteus was similar to that of C12(50) except for the influence of E. coli cell concentration.

Alkanes↗
PubMed1982

Solvent drag effect in drug intestinal absorption. I. Studies on drug and D2O absorption clearances.

It was shown that the intestinal absorption clearance of D2O (CLD2O) could be a more appropriate index to study the solvent drag effect than water volume flow which was the difference between water influx and outflux in the intestinal lumen. Then, the correlation between the intestinal absorption clearances of drugs (CLdrug) and CLD2O were studied using the in situ recirculating method in the rat small intestine. The drugs used were low molecular drugs, that is, benzoic acid, salicylic acid, p-hydroxybenzoic acid and antipyrine, and comparably high molecular drugs, that is, cephalexin (CEX), cefroxadine (CXD) and cephalothin (CET). CLdrug and CLD2O were obtained in hypertonic, isotonic and hypotonic perfused solution adjusted with sodium chloride. Consequently, the correlations for all drugs except CET were significant and high solvent drag effects were observed. CLdrug of benzoic acid, salicylic acid and antipyrine were approximately equal to CLD2O, suggesting that the intestinal mucosa could not distinguish these lower molecular drugs from water. For the high molecular drugs such as cephalosporins, however, some extent of reflection from the membrane was certainly found in CEX and CXD, and the extent in CET was assumed much larger than CEX and CXD, resulting that the contribution of solvent drag in CET could not be found. Consequently, it was suggested that the solvent drag had some important role in the intestinal absorption of cephalosporins.

Animals↗
PubMed1982

1-Anilino-8-naphthalene sulfonate binding site on human erythrocyte membrane using fluorescence lifetime and polarization.

It was shown that the human erythrocyte ghost membrane had two kinds of binding site for 1-anilino-8-naphthalene sulfonate (ANS) from binding kinetics. In measuring the fluorescence lifetime of ANS in the human erythrocyte ghost membrane suspension, two kinds of fluorescence lifetime were obtained: tau 1 = 15 ns at low ANS concentration and tau 2 = 8.4 ns at high ANS concentration. Comparing the results obtained from binding kinetics with those from fluorescence lifetime, it was considered that more hydrophobic binding site with fluorescence lifetime tau 1 contained the binding site with high and low binding constant and less hydrophobic binding site with fluorescence lifetime tau 2 corresponded to the binding site with low binding constant. From the results of binding kinetics of ANS to the erythrocyte membrane and the extracted membrane components (proteins and lipids), and those of the rotational relaxation time obtained from the ANS polarization in the erythrocyte membrane suspension, it was shown that the binding sites of ANS in the human erythrocyte ghost membrane were mainly composed of proteins at low ANS concentrations and lipids at high ANS concentrations.

Anilino Naphthalenesulfonates↗
PubMed1982

Studies on metabolism of tripamide. III. Metabolic fate of 14C-tripamide in rats and rabbits.

The metabolic fate of a new antihypertensive agent, tripamide (N-(4-aza-endo-tricyclo[5.2.1.0(2,6))]-decan-4-yl)-4-chloro-3-sulfamoylbenzamide), in rats and rabbits was studied using its 14C-labeled compound. The blood level of radioactivity in both species reached the maximum at 1 hr after oral administration, indicating the rapid absorption of the drug from the gastrointestinal tract. Following either oral or intravenous administration, a high concentration was observed in the liver of rats, but it was found in the kidney of rabbits. The major metabolite was 4-chloro-3-sulfamoylbenzoic acid in tissues, urine and feces; and in both species, the unchanged drug was only detected in the kidney. The pathway of excretion of radioactivity was via urine and feces in case of rats; but in rabbits, it was predominantly excreted via urine, although significant quantities of radioactivity were excreted with feces. The radioactivity excreted in feces was attributable to that which was excreted in bile, indicating the absorption of almost all the tripamide administered in both species. During the period of repeated dosing, though blood levels increased gradually and became about 1.5 times as high as that in the single dosing, radioactivity did not accumulate in most tissues and organs.

Animals↗
PubMed1981

Phosphorescence of alkaline phosphatase of E. coli in vitro and in situ.

Escherichia coli K-12, which is rich in alkaline phosphatase, exhibits phosphorescence characteristic of tryptophan at room temperature. E coli mutants which do not have alkaline phosphatase do not show long-lived phosphorescence. The phosphorescence spectrum and lifetime of E. coli K-12 was similar to that of purified alkaline phosphatase from E. coli. These results indicate that the long-lived tryptophan phosphorescence in E. coli is likely to be derived from alkaline phosphatase in situ. The temperature dependence of tryptophan phosphorescence life-time of purified alkaline phosphatase and E. coli K-12 differ; this may imply that alkaline phosphatase in E. coli may be associated with the cell envelope and is therefore protected against structural changes in the protein which result in increased phosphorescence decay rates.

Alkaline Phosphatase↗
PubMed1981

The prognosis of corticosteroid-responsive individuals.

Response of intraocular pressure to topical corticosteroid administration is determined genetically, and the genes that determine corticosteroid responsiveness of IOP and primary open angle glaucoma are considered closely related. To elucidate the relationship between corticosteroid responsiveness and primary open angle glaucoma, 35 patients with high corticosteroid responsiveness were followed up without therapy for at least ten years. During the follow-up period, a sustained rises in IOP greater than 21 mm Hg developed in five of 22 originally normotensive subjects. In two cases, glaucomatous field changes were demonstrated along with pressure elevation. Of 13 originally ocular hypertensives, further rise of IOP associated with glaucomatous field changes developed in seven. Results strongly indicate that pressure elevation is more likely to develop in corticosteroid-responsive individuals and the glaucomatous field defects are more likely to develop in responsive are compared with nonresponsive subjects.

Adrenal Cortex Hormones↗
PubMed1981

The correlation between drug binding to the human erythrocyte and its hemolytic activity.

Cationic phenothiazine derivatives, anionic anthranilic acid derivatives and fluorescent probe 1-anilino-8-naphthalene sulfonate (ANS) which had hemolytic activities were used to investigate hemolysis of human erythrocyte. The observed hemolytic activities of drugs could divided into two categories: (1) the difference of the binding activity of drugs to the erythrocyte and (2) the difference of the membrane perturbation activity of drugs bound to the erythrocyte. The human erythrocyte had two kinds of binding sites for any drug used. The first site of them was already saturated before hemolysis occurred and the second site of them may play an important role in hemolysis by these drugs.

Anilino Naphthalenesulfonates↗