PubMed Health⌕ Search

Biomedical subjects

Y Seto

Publications and source records attributed to Y Seto.

At least 181 records · Page 10Linked to original sources
PubMed1982

[Anti-inflammatory, analgesic and anti-pyretic activities of a non-steroidal anti-inflammatory drug, etofenamate, in experimental animals].

Anti-inflammatory, analgesic, and anti-pyretic activities of orally administered etofenamate, the diethylene glycol ester of flufenamic acid, were investigated in experimental animals. Against acetic acid-induced vascular permeability in mice and ultra-violet light-induced erythema in guinea pigs, etofenamate produced a dose related inhibition at doses of 40--320 mg/kg and 5--20 mg/kg, respectively. In rats, felt-pellet-induced granuloma formation and adjuvant-induced arthritis were significantly inhibited by repeated administration of etofenamate at doses of 20 mg/kg/day for 5 days and 40 mg/kg/day for 21 days, respectively. Etofenamate showed an inhibitory activity on the squeak response caused by flexing and extending the silver nitrate-induced arthritic joint in rats; and it produced a dose related anti-writhing activity at doses of 50--300 mg/kg and 10--80 mg/kg in mice and rats, respectively, in the acetic acid-induced writhing test. Etofenamate showed a significant anti-pyretic activity at doses of 0.2 mg/kg or more. These potencies of etofenamate were 0.5 to 1.6 times those of flufenamic acid. In particular, the anti-erythema, anti-arthritis, and anti-pyretic activities of etofenamate were approximately equivalent to or superior to those of flufenamic acid. From these results, it was suggested that etofenamate given orally, like other non-steroidal anti-inflammatory drugs, showed anti-inflammatory, analgesic, and anti-pyretic activities in experimental animals.

Analgesics↗
PubMed1982

[Anti-inflammatory activity of a non-steroidal anti-inflammatory agent, zomepirac sodium, in experimental animals].

Anti-inflammatory and gastrointestinal ulcerogenic activities of zomepirac sodium were investigated in experimental animals. The inhibitory activity of zomepirac sodium against carrageenin hind paw edema in rats, acetic acid-induced increase in vascular permeability in mice, and UV-erythema in guinea pigs was more potent than that of indomethacin. Anti-edema activity of zomepirac sodium was seen in adrenalectomized rats. Zomepirac sodium, like indomethacin, inhibited the delayed phase of hind paw edema produced by mixed phlogistics, but not the early phase mediated by histamine and serotonin in rats. Zomepirac sodium produced a dose-dependent inhibition against granuloma formation, established adjuvant arthritis, and development of adjuvant arthritis in rats; and its activity was slightly less potent than that of indomethacin. The inhibitory activity of zomepirac sodium on PGE2 biosynthesis in vitro was about one-third that of indomethacin. The ulcerogenic activity of zomepirac sodium was about 5 times weaker than that of indomethacin. From these results, it was suggested that zomepirac sodium was effective on various types of inflammation and showed particularly potent inhibitory activity against acute inflammation. These findings suggest that the mode of action of zomepirac sodium is similar to that of other acidic non-steroidal anti-inflammatory drugs.

Adrenalectomy↗
PubMed1982

[Anti-inflammatory and analgesic activities of a trans-cutaneous non-steroidal anti-inflammatory agent, etofenamate gel].

Anti-inflammatory and analgesic activities of topically applied etofenamate gel (5% etofenamate) were investigated in experimental animals. Etofenamate gel showed a dose related inhibition against vascular permeability caused by histamine in mice and ultra violet light-induced erythema in guinea pigs at doses of 10--100 mg/site and 25--200 (ED50 = 26.6) mg/site, respectively. The erythema was not inhibited with its topical application of 100 mg/site to the skin distant from the erythema. Granuloma formation, caused by felt-pellet implantation, was inhibited in a dose dependent manner by repeated application of etofenamate gel (10--100 mg/site/day). Etofenamate gel inhibited the pain-like responses in both the arthritic joint and the edematous hind paw of rats with 50--200 mg/joint and 100 mg/paw, respectively. In these tests, the vehicle gel did not show any significant activity. The potency of etofenamate gel was stronger than that of adrenal-extracts ointment (Mobilat) and approximately comparable to indomethacin ointment (1% indomethacin) in a weight basis of formulations. Topical application of etofenamate (0.5--2 mg/ear) resulted in a dose related decrease of contact hypersensitivity to oxazolone in mice, and its activity was nearly equipotent to flufenamic acid and about one-fourth that of indomethacin. From these results, it was suggested that etofenamate gel, applied topically to the inflamed tissue, showed a certain inhibitory activity against acute and subacute-chronic inflammation and inflammatory pain-like responses.

Administration, Topical↗
PubMed1981

Virus-induced alterations in insulin release in hamster islets of Langerhans.

After the inoculation of Golden Syrian hamsters with the TC-83 vaccine strain of Venezuelan encephalitis (VE) virus, a sustained diminution in glucose-stimulated insulin release and glucose intolerance of shorter duration develops. To understand better the mechanism of this defect in insulin release, we examined insulin secretion in response to several test agents in isolated perifused islets from control and 24-d post-VE virus-infected hamsters. 50 islets were used in all perifusion experiments, and data were expressed as total insulin released as well as peak response for each test agent during a 30-min perifusion period from control and VE-infected islets. After perifusion with 20 mM glucose, a 45% diminution of insulin release was noted in VE-infected islets in comparison with control islets, which in turn was similar to in vivo findings. However, following 1-mM tolbutamide stimulation, insulin release was similar in control and VE-infected islets. In separate studies, 1 mM tolbutamide, 10 mM theophilline, 1 mM dibutyryl cyclic (c)AMP, and 1 mM 8-bromo-cAMP resulted in statistically similar insulin-release curves in control and VE-infected islets. Additional experiments assessing [5-3H]glucose use in control and infected islets after 20 min of perifusion with 20 mM glucose revealed virtually identical values (239 +/- 30-control; and 222 +/- 27-VE-infected islets). Morphological and morphometric evaluation of VE-infected islets (21 d following virus inoculation) showed no changes in islet volume density, beta cell density, and beta cell granulation. Thus, VE virus induces a defect in glucose-stimulated insulin release from hamster beta cells that can be corrected by cAMP analogues and does not alter islet glucose use.

8-Bromo Cyclic Adenosine Monophosphate↗
PubMed1981

In vivo distribution of 14C-labeled N4-behenoyl-1-beta-D-arabinofuranosylcytosine in mice.

In order to clarify the pharmacological characteristics of N4-behenoyl-1-beta-d-arabinofuranosylcytosine (BHAC) and 1-beta-D-arabinofuranosylcytosine (AraC) with regard to their distribution in vivo, 14C-labeled BHAC and 13C-labeled AraC were injected intravenously into mice. Their in vivo distribution was determined by whole-body macroautoradiography and by an oxidation method. The disappearance rates of BHAC[cytosine-2-14C] and BHAC[behenoyl-l-14C] from the blood were slower than that of AraC[cytosine-2-14C], and the elimination rates of BHAC[cytosine-2-14C] and BHAC[behenoyl-14C] into the urine and feces were also slower than that of AraC[cytosine-2-14C]. The total amounts of BHAC[cytosine-2-14C] and BHAC[behenoyl-1-14C] eliminated within 48 hr after the injection were small. AraC[cytosine-2-14C] was equally distributed in each organ, while large amounts of BHAC[cytosine-2-14C] were found in and the placentae. The BHAC[behenoyl-1-14C]level in the thymus was lower than that of BHAC[cytosine-2-14C]. A very low level of radioactivity was found in most of the organs 6 hr after the injection of Arac[cytosine-2-14C], but BHAC[cytosine-2-14C] was observed even 24 hr after the injection. Radioactivity was still found in the liver, spleen, kidneys and adrenal glands of mice injected with BHAC[behenoyl-1-14C] even after 72 hr. In pregnant mice, AraC]cytosine-2-14C] was transmitted to the fetuses, but only a very small amount of 14C-BHAC was transmitted to the fetuses.

Animals↗
PubMed1980

Clinical experiences with left gastric vena caval shunt in patients with esophageal varices.

Left gastric vena caval shunt (Inokuchi) was performed in four patients with liver cirrhosis; electively in two and prophylactically in two cases. The overall results have been satisfactory in terms of the effect on esophageal varices and postoperative complications. This procedure appeared to be superior to distal splenorenal shunt or other direct surgical procedures in several aspects. Since left gastric vena caval shunt does not require particularly elaborate surgical techniques and can be performed safely even in patients with considerably impaired hepatic function, it can be recommended as an ideal surgical procedure to be performed in elective and prophylactic surgical candidates.

Adult↗
PubMed1980

[Anti-inflammatory activity of a topical glucocorticoid, fludroxycortide tape in experimental animals (author's transl)].

Fludroxycortide tape is a thin plastic tape which contains a synthetic glucocorticoid, fludroxycortide of 4 microgram/cm2. fludroxycortide tape with a topical application of 1 cm2 inhibited significantly contact hypersensitivities to oxazolone and picryl chloride in the ear skin of mice and PCA caused by IgE-like antibodies in the depilated abdominal skin of rats. Topical application of 1 to 4 cm2 of fludroxycortide tape produced a significant inhibition against histamine-induced vascular permeability, skin edema induced by intradermal injection of carrageenin into the depilated back and ear edema induced by topical application of croton oil in rats. Topical to oxazolone in dose-dependent manner, and had no thymolytic action, while in a dose of 100 microgram/ear, thymus atrophy occurred. Ear edema induced by croton oil was markedly inhibited by topical application of fludroxycortide (0.4 microgram/ear). Thus, fludorxycortide tape has topical anti-inflammatory activity against both allergic and non-allergic inflammation in mice and rats, and the topical anti-inflammatory activity of fludroxycortide appears to be favourably dissociated from its thymolytic action.

Administration, Topical↗
PubMed1978

(Lysyl-Glycyl-Glycyl)5 and (Lysyl-Glycyl-Glycyl)10 as models of histone. Interaction with DNA and acetylation by calf thymus enzyme.

Sequential polypeptides (Lys-Gly-Gly)5 and (Lys-Gly-Gly)10 were synthesized as models for the N-terminal region of H4 histone and their interactions with DNA were studied. The ability of (Lys-Gly-Gly)10 to precipitate DNA was found to be much higher than that of (Lys-Gly-Gly)5. For example, at the physiological salt concentration, (Lys-Gly-Gly)10 precipitates DNA but (Lys-Gly-Gly)5 does not. Both peptides could be acetylated by a partially purified histone acetyltransferase preparation derived from calf thymus. epsilon-Amino groups of lysyl residues were the sites of the acetylation. DNA-cellulose chromatography of the products indicated that acetylation weakened the interaction of the peptides with DNA.

Acetylation↗
PubMed1978

Antitumor activity of a new amino acid derivative, N6,N9-bis-(butyloxycarbonylaminomethyl)-L-citrulline.

Approximately 800 amino acid derivatives have been synthesized and screened in order to evaluate their antitumor activity against various transplantable rat ascites hepatomas. Among them, N6,N9-bis(butyloxycarbonylaminomethyl)-L-citrulline (A-924) was found to be highly effective against various rat ascites hepatomas. A-924, when given orally, exhibited prolongation of survival of rats implanted intravenously with ascites hepatoma cells such as AH-44, AH-66, AH-130, AH-66F, or AH-41C.

Administration, Oral↗
PubMed1975

Mechanism of action of anti-influenza benzamidine derivatives.

Benzamidine derivatives exhibited a high antiviral effect in vivo against influenza virus strains A2/Adachi and B/Lee. The inhibiting properties of anti-influenza benzamidine derivatives on the virus-induced inflammation undoubtedly plays an important role in the clarification of the mechanism of action of these drugs.

Amidines↗