Search PubMed⌕ Search

Biomedical subjects

H Fujimura

Publications and source records attributed to H Fujimura.

At least 235 records · Page 13Linked to original sources
PubMed1981

[Topical anti-inflammatory activity of dexamethasone 17-valerate (author's transl)].

The anti-inflammatory activity of dexamethasone 17-valerate ointment (DV-17, 0.12%) was investigated by topical application in mice and rats, and the effects compared with those of dexamethasone (DX, 0.12%), betamethasone 17-valerate (BV-17, 0.12%), beclomethasone 17,21-dipropionate (BE, 0.025%) and hydrocortisone 17-butyrate (HC, 0.1%) which were prepared with the same ointment base. DV-17 inhibited markedly the superficial inflammation such as increased vascular permeability induced by intradermal injection of histamine or bradykinin in rats and edema induced by a drop of croton oil into the mouse ear. DV-17 also inhibited significantly rat paw edema induced by carrageenin, yeast, nystatin and mustard. The inhibitory activity of DV-17 on those acute inflammatory responses was similar to that of DX and BV-17. In the inhibitory activity on carrageenin induced paw edema, DV-17 was less potent than that of DX when given orally, however was similar to DX in topical application. DV-17 also inhibited granulation tissue proliferation by subcutaneous paper disk implantation and nontreated foot swelling in adjuvant arthritic rats, but the inhibitory activity of DV-17 on the inflammation of these distant areas was lower than that of DX. On the other hand, systemic effects such as decrease in weight of adrenal or thymus and body weight loss were most evident in the case of DX and lower with DV-17. DV-17 prolonged wound healing and inhibited the delayed-type hypersensitivity induced by picryl chloride. The activity was equivalent to that of DX and BV-17. From the above results, it may be considered that DV-17 possesses potent anti-inflammatory activity, whereas it has fewer side effects and is a useful glucocorticoid for external application.

Administration, Topical↗
PubMed1980

Antiinflammatory principles of Aconitum roots.

The methanol extracts of Aconitum roots have shown inhibition of increased vascular permeability induced by acetic acid and of hind paw edema produced by carrageenin in mice. The extract of A. carmichaeli has been fractionated, monitored by the capillary permeability test, to yield the aconitines as active principles. The aconitines have inhibited the increased vascular permeability induced by acetic acid in mice peritoneal cavity and that induced by histamine in rat intradermal sites, and the hind paw edema formation induced by carrageenin n rats and mice at low doses. The benzoylaconines have exhibited inhibitory effects of the aforementioned acute inflammations but at higher doses. The aconitines have reduced the granulation tissue formation of the chorio-allantoic membrane of the chick embryo. On the other hand, the Aconitum alkaloids have elicited no effects on the ultraviolet erythema formation in guinea pigs at lower doses than the lethal ones and failed to show positive responses on the vascular permeability in the granuloma pouch and on adjuvant arthritis in rats at the doses employed.

Acetates↗
PubMed1980

Interaction of indomethacin and aspirin or mepirizole in rats as shown by gastrointestinal ulcerogenic and anti-inflammatory activities.

The interaction of indomethacin and aspirin or mepirizole was studied in rats. Concomitant oral administration of aspirin and indomethacin had no significant influence on the gastro-ulcerogenicity of indomethacin alone, but caused significantly less intestinal damage than an identical dose of indomethacin alone. In proportion to the inhibitory activity of intestinal lesions, aspirin also showed the activity that antagonized significantly the shortening of small intestinal length, loss of body weight and delay of charcoal transport in the intestine induced by indomethacin alone. Aspirin tended to reduce also the anti-inflammatory and analgesic effects of indomethacin in combined administration. On the other hand, mepirizole significantly reduced both gastric and intestinal ulcerogenicities by indomethacin alone in concomitant oral administration and inhibited dose-dependently the incidence and severity of those lesions. The inhibitory activity of gastrointestinal lesions by mepirizole was in proportion to the activities that antagonized the shortening of the small intestine, loss of body weight and delay of charcoal transport by indomethacin. Moreover, in contrast to aspirin, mepirizole exerted more potent anti-inflammatory and analgesic effects in combined administration than in the single administration of indomethacin. Therefore, aspirin reduced both the intestinal side effect and the anti-inflammatory effect induced by indomethacin in combination, while the combination of mepirizole reduced the gastrointestinal side effects by indomethacin alone, but seemed to be additive in the anti-inflammatory effect.

Animals↗
PubMed1980

[Pharmacological studies of new sulfhydryl compounds 2-mercapto-2-methylpropanoyl-L-cysteine (SA96). I. Evaluation of anti-rheumatic action (author's transl)].

Oral administration of 2-mercapto-2-methylpropanoyl-L-cysteine (SA 96), a newly synthesized sulfhydryl compound, showed protective and curative effects on adjuvant-induced arthritis in rats similarly to those seen with D-penicillamine (D-PA). However, the effects of these compounds were not dose-dependent, and the maximum effects of SA96 were observed at 10 mg/kg/day. On the contrary, SA96 and D-PA had little effect on the various acute and subacute inflammatory responses induced in rat and mice. Formation of hemolytic plaque forming cells in the spleen of mice immunized with 5 X 10(8) sheep red blood cells was potentiated by the oral administration of both compounds. These stimulatory effects of SA96 and D-PA on the humoral immune responses were also not dose-dependent, and the maximum effects of SA96 were observed with 10 mg/kg/day, as in the case of adjuvant-induced arthritis in rats. In in vitro experiments, the inactivation of rheumatoid factor and the inhibition of collagenase and bone alkaline phosphatase activities were observed with both compounds, but these effects of SA96 were more potent than those of D-PA. As there is a similarity in the pharmacological profiles of SA96 and D-PA, SA96 may prove to be clinically effective for rheumatoid arthritis.

Acute Disease↗
PubMed1980

[Comparative study on the pharmacological activities of protizinic acid and various non-steroidal anti-inflammatory agents (author's transl)].

The potency of anti-inflammatory and ulcerogenic activities of a new anti-inflammatory agent, (10-methyl-7-methoxy-2-phenothiazinyl)-2-propionic acid (protizinic acid, PRT), was compared with those of various known non-steroidal anti-inflammatory agents in 5 experimental models. The ED30 of PRT in carrageenin edema with oral administration was 18.0 mg/kg and its potency was third following indomethacin (IM) and diclofenac sodium (DF), among the 15 agents tested. The ED50 of PRT in ultraviolet erythema with oral administration and the IC50 in protein denaturation were 1.07 mg/kg and 0.89 X 10(-5)M, respectively and the activities were the most potent among all agents. The IC50 of PRT in platelet aggregation induced by arachidonic acid was 5.55 X 10(-5)M and the rank of potency was sixth following to IM, DF, flufenamic acid, aluminium and ranked fifth following azapropazone, MF, alclofenac, metiazinic acid (MA), except for basic agents, mepirizole, benzydamine hydrochloride and tiaramide hydrochloride. Thus, PRT seemed to have a relatively weak ulcerogenic activity in contrast to potent anti-inflammatory activity. Also, PRT was superior to MA, an analogue of PRT, in potency of anti-inflammatory activity, in all experimental models.

Animals↗
PubMed1979

[Anti-inflammatory actions of proteases, bromelain, trypsin and their mixed preparation (author's transl)].

Anti-inflammatory actions of proteases, bromelain (BR), trypsin (TR) and their mixed preparation (KT) were studied mainly in rabbits using various experimental test methods. Inhibitory action of edema formation induced by carrageenin was observed to be dose dependent with oral administrations of KT. This inhibitory action of KT was more remarkable than actions of BR and TR, suggesting a possible synergism between the latter two. Such action was also observed with non-steroidal anti-rheumatic drugs, phenylbutazone (PB), indomethacin and acetylsalicylic acid. Oral administration of KT exerted definite inhibition or a tendency toward inhibition against paw edema induced by dextran, histamine or egg albumin or skin edema induced by anti-rabbit serum and thermal stimulation. Furthermore, inhibition of vascular permeability increase induced by histamine and bradykinin as well as a tendency toward inhibition against protein exudation in CMC-pouch method were observed. On the other hand, contrary to PB, potent inhibitory action was not manifested in the persistent proliferative inflammation models, the granuloma formation induced formalin soaked filter paper and cotton pellet and the mustard edema. Therefore, it can be deduced that the inhibitory action of KT against edema formation may be dependent mainly on the inhibitory action of vascular permeability increase and the anti-inflammatory action may be specific for acute exudative inflammation.

Animals↗
PubMed1979

[Cathartic activity of spasmogens in mice, rats and guinea pigs (author's transl)].

To examine the effect of spasmogens on propulsive motility in the intestine, cathartic activity of drugs was investigated. Mice, rats and guinea pigs were individually observed in cages with 20 separate small rooms in which a sheet of filter paper covered the botton of case for observation of feces. The effect was evaluated 1 hr after drug administration. Cathartic activity of spasmogens was the most marked in mice followed by rats, but was rarely observed in guinea pigs. Cholinergic drugs and cholinesterase inhibitors had a cathartic effect in mice and rats, but the activity differed. Drugs such as acetylcholine and physostigmine produced a low cathartic activity even at sublethal and lethal doses. Other drugs as bethanechol, pilocarpine and neostigmine had a dose dependent cathartic effect at doses below lethal ones and were found to be clinically useful for intestinal relaxation after laparotomy. Among autacoids which contract the intestine by direct action on smooth muscles, histamine and bradykinin had no cathartic effect in mice and rats. 5-HT and prostaglandin E2 were dose dependent with a marked cathartic effect in both species. 5-HTP produced the same cathartic activity as that seen with 5-HT in mice, but had no cathartic effect in rats. The cathartic effect of BaCl2 was low, but dose dependent in both species. We recommend this method for the study of the effect of various compounds on the propulsive motility of the intestine.

Amines↗
PubMed1979

[Effect of spasmolytics on cathartic activity of pilocarpine, 5-HT and prostaglandlin E2 in mice (author's transl)].

Effects of autonomic, anti-histaminic, anti-5HT drugs, papaverine and morphine on cathartic activity of spasmogens such as pilocarpine, 5-HT and prostaglandin E2 (PGE2) were tested by giving these drugs to mice subcutaneously. Mice used were male dd strain weighing 20 +/- 2 g and the catharatic effect was evaluated by the all or none method. The cathartic effect by pilocarpine was inhibited markedly by anti-cholinergic drugs such as atropine and diphenhydramine, but not by hexamethonium and methysergide. Therefore, the action of pilocarpine was found to be direct on the acetylcholine receptors. The catharatic effect by 5-HT was inhibited significantly by hexamethonium and methysergide. Atropine inhibited the cathartic effect of 5-HT, but the inhibitory activity was lower by about one hundredth than that on pilocarpine-induced diarrhea. It is suggested that 5-HT has dual sites of actions and there are less cholinergic and specific serotonergic actions. The cathartic effect by PGE2 was inhibited by anticholinergic, anti-5HT and ganglion blocking agents. PGE2 appears to possess the same mode of action as both pilocarpine and 5-HT. Papaverine inhibited little the cathartic effect of all three spasmogens, while morphine had a potent and nonspecific inhibitory effect on the cathartic action of all three spasmogens.

Animals↗
PubMed1978

Anti-convulsant effect of phthalazino-2,3b-phthalazine-5(14H),12(7h)-dione (L-5418). I. Behavioral effect.

Since it had been demonstrated that L5418 has an anti-convulsant effect with no relation to its anti-inflammatory properties, comparative studies were carried out with the use of currently available anti-convulsant agents as controls. L-5418 inhibited tonic convulsions induced by maximal electroshock and strychinine in mice and prevented animals from the death sequence. L-5418 had an inhibitory effect on tonic convulsions induced by pentetrazol and N-sulfamoyl-hexahydroazepine (SaH 41-178), but not on clonic convulsions by those compounds at even a high dosage or on clonic convulsions induced by picrotoxin and bemegride. Trimethadione produced an inhibitory effect on both tonic and clonic convulsions. The hypnotic agents, phenobarbital and glutethimide inhibited both convulsions, but a higher dose was required in the case of clonic convulsions. Anti-convulsant agents are classified into three different groups according to their mode of action. L-5418 had the same mode of action as seen with diphenylhydantoin and carbamazepine. As L-5418 did not inhibit tremor induced by tremorine, an anti-Parkinson effect was ruled out. When L-5418 was administered alone, the animals did not lose the righting reflex nor show muscle relaxation observed in inclined screen and rotarod tests. Moreover, the compound had no influence on the aggressive behavior induced by electrical stimulation or olfactory bulb ablation. L-5418 possesses a selective anti-convulsant effect, yet has no sedative, tranquilizing or disturbing effects on movement such as equilibrium disturbance or muscle relaxation. L-5418 may prove useful for grand mal epilepsy as it is less toxic than diphenylhydantoin and carbamazepine.

Aggression↗
PubMed1978

Anti-convulsant effect of phthalazino-[2,3b]-phthalazine-5(14H), 12(7H)-dione (L-5418). II. Electroencephalographic study.

L-5418 has an anti-convulsant effect which is similar to that of diphenylhydantoin. The effects of L-5418 on EEG activity in rabbits with acute and chronic implantation of electrodes were studied in comparison with those of currently available anti-convulsants. Intravenous administration of L-5418 increased a slow-wave sleep pattern in the spontaneous EEG, which was also induced by diphenylhydantoin. With respect to the focal seizure in the cerebral cortex induced by local application of penicillin, L-5418 showed suppressive effects on the frequency and duration of seizure discharge, and on the spread of seizure discharge to other parts of the brain. The efficacy was about twice that of diphenylhydantoin. L-5418 and dephenylhydantoin did not increase the threshold of seizures induced by bemegride while trimethadione raised the threshold. L-5418 also showed suppressive effects twice as active as diphenylhydantoin on after-discharge induced by electrical stimulation of the hippocampus and amygdala. This suppressive effect on after-discharge of the limbic system may be parallel with the suppressive effect on psychomotor seizure. From these results of L-5418 on an experimental model of epilepsy, it is suggested that L-5418 has suppressive effects similar to that of diphenylhydantoin on convulsion and the efficacy proved to be twice that of diphenylhydantoin in the EEG study.

Animals↗