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Biomedical subjects

H Fujimura

Publications and source records attributed to H Fujimura.

At least 55 records · Page 3Linked to original sources

Gastrointestinal motility enhancing effect of ginger and its active constituents.

The effect of ginger root (Zingiberis Rhizoma) on gastrointestinal motility was examined based on its ability to enhance charcoal meal transport in mice. Oral administrations of the acetone extract of ginger (which contains volatile oils and bitter substances) at 75 mg/kg, [6]-shogaol at 2.5 mg/kg, or a [6]-, [8]- or [10]-gingerol at 5 mg/kg enhanced the transport of a charcoal meal. The effects of these substances were similar to or slightly weaker than those of metoclopramide and donperidone.

Animals

Vascular dilatory action of Artemisia capillaris bud extracts and their active constituent.

In perfusion experiments, the acetone extract of Artemisia capillaris buds significantly inhibited the response to norepinephrine of helical strips of rabbit thoracic aorta. The acetone extract was fractionated by column chromatography to identify the active constituent. Kinetic experiments using rabbit thoracic aorta showed that 6,7-dimethoxycoumarin (scoparone) has a marked inhibitory effect on the contractions induced by norepinephrine, 5-hydroxytryptamine, histamine and angiotensin II. Like nitroglycerin, scoparone appeared to be a competitive antagonist of norepinephrine.

Animals

Antianoxic action of evodiamine, an alkaloid in Evodia rutaecarpa fruit.

In order to determine the antianoxic potential of evodiamine, its effects were compared to those of vinpocetine (VPT), using a series of animal models of anoxia. In mice, evodiamine was equivalent to VPT in the KCN-induced anoxia model but was greater than VPT in the low-pressure-induced anoxia model. Its effectiveness was increased by combined treatment with physostigmine, suggesting the involvement of a cholinergic mechanism in the antianoxic action of evodiamine.

Alkaloids

Synthesis and analgetic activity of sulfur-containing morphinans and related compounds.

3-Acylthiomorphinans, 3-carbamoylthio-3-deoxydihydromorphine and 3-benzoylthio-9-aza-17-carbamorphinan were synthesized by Newman-Kwart rearrangement of the corresponding O-thiocarbamates. The analgetic activities were lower than that of pentazocine, and the opioid receptor binding affinities were very weak. These acylthiomorphinans showed low antinociceptive activity compared with corresponding sulfur-containing benzomorphans. 3-Carbamoylthio-deoxydihydromorphine had no significant analgetic activity.

Analgesics

The effect of scoparone, a coumarin derivative isolated from the Chinese crude drug Artemisiae capillaris flos, on the heart.

In the present study, scoparone isolated from Artemisia Capillaris Flos has been investigated to determine its pharmacological properties on the heart. Scoparone was found to cause the increase in coronary flow and heart rate, but did not affect cardiac output, left ventricular pressure or left ventricular work in the isolated perfused heart. Scoparone at 25 mg/kg and 50 mg/kg, p.o. had a marked inhibitory effect on the ST wave depression. Consequently it is suggested that scoparone has antianginal action.

Animals

Antianoxic action and active constituents of evodiae fructus.

In order to develop new drugs from natural products, constituents of natural medicines were examined for their effectiveness in the KCN-induced anoxia model in mice. Methanol extract from a Chinese medicine, evodia (fruits of Evodia rutaecarpa Benth. or E. officinalis Dode), had a significant effect in the KCN-induced anoxia model in mice and therefore the active constituents were further examined. The results indicated that the antianoxic action of evodia was found in the fraction containing evodiamine. Further analysis of the active constituent indicated that evodiamine and rutaecarpine, indole-alkaloids found in large amounts in the Chinese medicine evodia, were mainly responsible for the antianoxic action.

Animals

Vascular dilatory action of the Chinese crude drug. II. Effects of scoparone on calcium mobilization.

Further experiments were conducted to examine the effect of scoparone (6,7-dimethoxycoumarin), a coumarin derivative found in the Chinese crude drug "Capillaris Flos," on calcium mobilization. Scoparone does not affect Ca2+ influx through the voltage-dependent channel due to membrane depolarization. Its inhibitory action may be dependent not only on the inhibition of Ca2+ release from sarcoplasmic reticulum but also on the inhibition of extracellular Ca2+ influx through the receptor-operated channel.

Animals

Dermal penetration enhancement by crude drugs: in vitro skin permeation of prednisolone enhanced by active constituents in cardamon seed.

Several extracts of crude drugs were prepared and tested as penetration enhancers for the diffusion of prednisolone through mouse skin in vitro. The acetone extract of cardamon seed (Eelettaria cardamomum) was selected for further study to identify the active principles. The result showed that terpineol and acetyl terpineol are the active components in cardamon seed.

Animals

[Kappa-type opioid receptor in human placental membrane].

Since many opioid receptor preparations are heterogeneous systems containing multiple types of receptor, characterization of each type of the receptor is influenced by contamination with other types of receptor. Demonstrating kappa receptor proved more difficult owing to the ability of kappa ligands to interact with a number of receptor classes and to the lack of the homogeneous preparation. It has been reported that kappa ligands selectively bind to human placental membrane. To establish homogeneous kappa receptor preparation, the kappa binding to human placenta was characterized. The portion which was predominantly villus tissue was removed from freshly collected placenta, and the P3-membrane fraction was prepared. Kappa opioid agonist, such as 3H-Dynorphin A, 3H-ethylketocyclazocine and 3H-U-69593, bound to the human placental membrane fraction in a manner of single class of binding site (Bmax: approximately 40 fmol.mg-1 protein). In contrast, 3H-dihydromorphine, 3H-DAGO (mu agonist), 3H-DADLE (delta agonist) or 3H-SKF-10047 (sigma agonist) showed no binding activity. The specific binding of 3H-diprenorphine was displaced only by kappa-selective ligand (U-50488H, dynorphin, butorphanol). These results suggest that opioid binding in human placental membrane is specific for kappa opioid.

Humans

[A case of facioscapulohumeral muscular dystrophy with sensorineural hearing loss and retinal angioma].

We report a sporadic case of 12 years old boy with facioscapulohumeral dystrophy (FSHD), sensorineural hearing loss and exudative angioma of bilateral retina. His hearing loss was noted at 9 years, followed by muscle weakness of his right upper extremity at 11 years. Complete neurological examination at 12 years revealed FSH type distribution of muscle weakness with high serum CK level (330 U/L), moderate sensorineural hearing loss and exudative angiomas of bilateral retina. The biopsy from biceps brachii muscle showed advanced dystrophic changes with a dense inflammatory cell infiltration predominating on perivascular distribution and type II fiber predominance. The features of infiltrating lymphocytic surface antigen seen in this case were compatible with those of FSHD rather than those of polymyositis. In the literature, the association of FSHD with hearing loss and retinal vessel abnormalities has been documented on 15 cases as an unusual form of FSHD. However, it has otherwise been noted that the associations of FSHD and hearing loss or retinal vessel abnormalities are unequivocally frequent, Whenever special attention has been made. Morphological examination with light and electron microscopies on the muscle specimen in this patient did not demonstrate any recognizable abnormality such as arterio-venous shunt or thickening of vessel wall basal lamina. However, it cannot be completely excluded that exudation around the abnormal vessel wall in the muscle may play an initial role in the pathogenesis of FSHD. Further morphological survey on vessel abnormalities may be necessary in the FSHD muscle.

Child

The vasorelaxant effect of evocarpine in isolated aortic strips: mode of action.

The effect of evocarpine (EVO), a quinolone alkaloid isolated from Evodiae fructus, on Ca2+-blocking activity has been examined. In the isolated rat thoracic aorta evocarpine significantly inhibited the contraction induced by 60 mM K+ with an IC50 of 9.8 microM, and that induced by external Ca2+ in the depolarized muscle in concentrations of 10-100 microM. The relaxant effect of evocarpine and verapamil was antagonized by Bay K8644. The increase of 45Ca2+-influx induced by 60 mM K+ was significantly inhibited by 100 microM evocarpine. In the isolated rabbit thoracic aorta 100 microM evocarpine had no effect on the norepinephrine-induced contraction in normal medium or on the phasic contraction in Ca2+-free medium or on the transient relaxation induced by activation of the Na+ pump. The content of cyclic AMP or cyclic GMP was unchanged. These results suggest that evocarpine inhibits Ca2+ influx through voltage-dependent calcium channels.

Alkaloids

The peripheral neuropathy of necrotizing arteritis: a clinicopathological study.

We have reviewed the clinical and morphological data from 100 patients with necrotizing arteritis in muscle and/or in nerve samples taken by biopsy. The neuropathy occurred in the context of a multisystem disorder (Group 1) or in apparent isolation (Group 2). The average age of patients was 59 in Group 1 and 61 in Group 2. Females were more commonly affected than males, especially in the first group. Necrotizing arteritis complicated the course of rheumatoid arthritis in 25 patients. In 3 patients necrotizing arteritis was associated with infection with the human immunodeficiency virus, the agent of AIDS. Tests for hepatitis B surface antigen were positive in 19 patients. Mononeuritis was present in 13, mononeuritis multiplex in 62, and distal symmetrical sensory or sensorimotor neuropathy in 19 patients. In both groups of patients, the muscle biopsy was more frequently diagnostic for arteritis than was the nerve biopsy (80% versus 55%). The average incidence of isolated fibers undergoing axonal degeneration was 64.8%; that of demyelinated/remyelinated fibers was 1.9%. We conclude that the combination of nerve and muscle sampling increases the chance of visualizing characteristic arterial lesions in vasculitic neuropathy.

Adult

Effect of alismol on adrenergic mechanism in isolated rabbit ear artery.

Effects of alismol, a sesquiterpenoid isolated from the rhyzome of Alisma orientale, on adrenergic mechanisms were examined in the isolated rabbit ear artery. Alismol (10(-6) to 10(-4) M) inhibited the contraction of isolated rabbit ear artery by electrical stimulation of the perivascular nerves. The inhibition was concentration-dependent; at a concentration of 10(-4) M, the inhibition was 90% (n = 8). Treatment with 10(-4) M alismol inhibited the increase in 3H-noradrenaline (3H-NAd) release induced by electrical stimulation by 63 +/- 6%. Alismol at 10(-4) M did not affect the neuronal uptake of 3H-NAd in the artery. Alismol at 10(-4) M slightly inhibited contractions induced by exogenously administered NAd. These results demonstrate that alismol inhibits the adrenergic neuro-effector mechanisms in rabbit ear artery, and they suggest that alismol acts primarily on nerve terminals and inhibits their responses to electrical stimulation by interfering with NAd release.

Animals

Effectiveness of continuous arteriovenous hemofiltration for patients with refractory heart failure.

Continuous arteriovenous hemofiltration (CAVH) was carried out in 8 patients with refractory congestive heart failure. All these patients had heart failure and oliguria for over 24 hours and intensive treatment with digitalis, diuretics, catecholamines and vasodilators was prescribed. Hemodynamics were followed closely during CAVH. During CAVH, pulmonary arterial pressure and pulmonary capillary wedge pressure were significantly reduced in all patients, the right atrial pressure decreased in 6 with right cardiac failure, the heart rate decreased in 3 with tachycardia and the blood pressure and cardiac index were elevated in 3 with hypotension. These observations show that CAVH can be performed safely and effectively in patients with congestive heart failure, oliguria and hypotension.

Adult