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Biomedical subjects

T Mimura

Publications and source records attributed to T Mimura.

At least 55 records · Page 3Linked to original sources
PubMed1989

Comparative platelet anti-aggregant activity of D-cysteinolic acid analogues.

D-Cysteinolic acid (1) analogues with an S-C-C-N skeleton showed increased platelet anti-aggregant activity in the following order: 2-aminoethanesulfonic acids, thiazolidines, 2-aminoethanethiols and 2-aminoethyl disulfides. Methyl substitutions at the 2-position potentiated the activity. Of these analogues, bis [(R)-2-aminopropyl] disulfide was the most potent inhibitor of platelet aggregation, with about 600-fold the activity of (1).

Animals↗
PubMed1989

Induction of angiotensin-converting enzyme inhibitory activity by acid-limited proteolysis of glyceraldehyde 3-phosphate dehydrogenase.

Angiotensin-converting enzyme (ACE) inhibitors were excised from glyceraldehyde 3-phosphate dehydrogenase (GAPDH) preparations of tuna and porcine muscles by heating at 120 degrees C for 5 min in 1 M AcOH-20 mM HCl. The inhibitors were then purified by successive chromatographies. The final product from tuna was identified as Pro-Thr-His-Ile-Lys-Trp-Gly-Asp, which was the ACE inhibitor obtained from tuna muscle [Kohama et al. (1988) Biochem. Biophys. Res. Commun. 155, 332-337]. The porcine ACE inhibitor was found to be Pro-Ala-Asn-Ile-Lys-Trp-Gly-Asp, which was identical to the porcine muscle GAPDH peptide 79-86. These results strongly suggested that the ACE inhibitory octapeptides derived from GAPDH proteins by acid-limited proteolysis at Asp-Pro and Asp-Ala peptide bonds.

Amino Acid Sequence↗
PubMed1989

Glucosamine enhanced sperm-egg binding but inhibited sperm-egg fusion in mouse.

In order to study the sperm-egg recognition mechanism on the surface of the plasma membrane, zonae were removed from mouse eggs by exposure to acidic conditions. Sperm binding to denuded eggs was then observed in the presence of various sugars. Among several carbohydrates tested, only glucosamine (GlcN) was found to increase the number of sperm bound to eggs while inhibiting sperm-egg fusion. The inhibition was reversible; when denuded eggs were transferred to a GlcN free medium, a high rate of polyspermy was observed.

Animals↗
PubMed1989

Flow cytometric analysis of mouse sperm using monoclonal anti-sperm antibody OBF13.

The variable reactivity of OBF13 monoclonal antibody to mouse sperm was studied using a fluorescein activated cell sorter. Sperm from cauda epididymis were incubated with ionophore A23187, subjected to indirect immunostaining and analyzed by a cell sorter. Three peaks showing different fluorescence intensities were observed. These peaks contained (i) not stained (N), (ii) acrosomal cap or anterior region stained (A) and (iii) head stained (H) sperm, respectively. H type sperm showed more intense integral fluorescence than A type sperm. It was also noted that the H type were observed when cauda epididymal sperm were incubated with A23187, but not among non-incubated, or A23187 treated caput epididymal sperm. When sperm were pre-categorized as "dead" or "alive" by propidium iodide staining, no A type were observed in the "live" population. These results suggest that the sperm exhibiting the OBF13 antigen in the acrosome region lost their viability before they accomplished a "true" acrosome reaction.

Acrosome↗
PubMed1989

Synthesis of an inhibitor of human immunodeficiency virus infection.

Anti-HIV effects of lentinan sulfate were investigated by using an HTLV-I-carrying cell line, MT-4, in vitro. Lentinan, a fungal branched (1----3)-beta-D-glucan, was sulfated to various degrees by means of two kinds of procedures using piperidine N-sulfonic acid in dimethyl sulfoxide or chlorosulfonic acid in pyridine. Lentinan sulfate with a sulfur content of more than 13.9% effectively prevented HIV-induced cytopathic effects (CPE) at concentrations of more than 3.3 micrograms/ml. However, low-substituted lentinan sulfate did not prevent HIV-induced CPE at any concentration tested. When the countercation was 50% Na+ and 50% pyridinium ion, the inhibitory capacity was low. Anticoagulant activity of the lentinan sulfate was also assessed.

Anticoagulants↗
PubMed1989

Studies on pharmacological activation of human serum immunoglobulin G by chemical modification and active subfragments. VIII. Effect of carboxamide-methylated light chain (Fr.I-L) on leukocyte functions.

Human serum immunoglobulin G light chain (Fr.I-L), which was reduced and carboxamide-methylated, showed no effect on formyl-methionyl-leucyl-phenylalanine (FMLP)-induced chemotaxis nor on phagocytosis of yeasts when directly added to guinea pig polymorphonuclear leukocytes (PMNs). However, intravenously administered Fr.I-L inhibited emigration of leukocytes into the peritoneal cavity and promoted phagocytosis of yeasts in a yeast-induced peritonitis model in mice. Moreover, Fr.I-L reduced FMLP-induced chemiluminescence (CL) from PMNs. These facts indicated that the anti-inflammatory action of Fr.I-L was caused by inhibiting emigration of leukocytes into the injured site and scavenging superoxide radicals from the cells.

Animals↗
PubMed1989

Biological properties of angiotensin-converting enzyme inhibitor derived from tuna muscle.

A novel inhibitor of angiotensin-converting enzyme (ACE) derived from tuna muscle, Pro-Thr-His-Ile-Lys-Trp-Gly-Asp (tuna AI), was chemically synthesized, and its biological properties were investigated. Synthetic tuna AI was found to be chemically and biologically indistinguishable from the native one. Tuna AI inhibited rabbit lung ACE non-competitively with Ki values of 1.7 and 5.7 microM with substrates, hippuryl-L-histidyl-L-leucine and angiotensin I, respectively. This peptide (5.3 microM) also doubled the effect of bradykinin in the contraction of isolated guinea pig ileum. The peptide did not show zinc chelating activity and carboxypeptidase A inhibitory activity. Thus, tuna AI was found to be a unique ACE inhibitory peptide with non-competitive manner, differing from many naturally occurring peptide ACE-inhibitors.

Amino Acid Sequence↗
PubMed1989

Enhancement of heparin-binding ability of fibronectin by S-carboxamide-methylation.

Human plasma fibronectin (FN) was reduced and carboxamidemethylated, and its binding ability to several matrices was analyzed in vitro. The binding of S-carboxamidemethyl (Cam)-FN to heparin-Sepharose was not influenced by either 4 M urea, 0.5 M NaCl or 0.5% heparin, but was disrupted by the coexistence of urea and NaCl or heparin. S-Cam-FN, compared with intact FN, obviously had a more potent ability to bind heparin, while it had little or no binding ability to gelatin, fibrin and thrombin-stimulated platelets. A conformational change of S-Cam-FN by heparin-binding has been proposed as a possible mechanism from the result of circular dichroic spectrum measurement.

Binding Sites↗
PubMed1989

Further studies on the pharmacological effect of the anti-inflammatory compound, bis[2-(E-2-octenoylamino)ethyl] disulfide.

Further studies on the pharmacological effect of orally administered bis[2-(E-2-octenoyl-amino)ethyl] disulfide (compd. I-3) was examined by using several experimental models in vivo. Compound I-3 showed analgesic activity, inhibiting both acetic acid- and acetylcholine-induced writhings in mice. This compound also showed antipyretic activity against yeast-induced fever in rats, and significantly inhibited arachidonic acid-induced mortality in mice. However, it had no effect on serotonin-induced paw edema formation or platelet activating factor-acether-induced mortality in mice. The effects of compd. I-3 are suggested to be due to inhibition of prostaglandin biosynthesis.

Amides↗
PubMed1989

The effect of a cystamine derivative, bis[2-(E-2-hexenoylamino)ethyl] disulfide, on rat platelet aggregation.

Bis[2-(E-2-alkenoylamino)ethyl] disulfides (compds. I), synthesized from cystamine and 2-trans fatty acids, inhibited collagen-induced rat and rabbit platelet aggregation. The most potent compound was bis[2-(E-2-hexenoylamino)ethyl] disulfide (compd. I-1), and this compound suppressed thromboxane B2 formation from arachidonic acid in rat platelets. The results suggested that compd. I-1 has an inhibitory effect on cyclooxygenase.

Alkenes↗
PubMed1989

The inhibitory effect of bis[2-[(E)-2-octenoylamino]ethyl] disulfide on the cyclooxygenase pathway.

Bis[2-[(E)-2-octenoylamino]ethyl] disulfide (compd. I-3) inhibited collagen- and arachidonic acid-induced rat platelet aggregation, although not adenosine 5'-diphosphate (ADP)-induced rat platelet aggregation. Based on these results, we then investigated the inhibitory effect of compd. I-3 on thromboxane B2 formation from arachidonic acid in rat platelets, and prostaglandin I2 formation in rat aortae. Compound I-3 inhibited both thromboxane B2 and prostaglandin I2 formation, suggesting that it has an inhibitory effect on cyclooxygenase. The inhibitory effect of compd. I-3 was confirmed in experiments using a crude preparation of sheep seminal vesicle microsomal prostaglandin synthetase. These findings suggested that compd. I-3 has an inhibitory effect on cyclooxygenase activity, like nonsteroidal anti-inflammatory drugs.

Animals↗
PubMed1989

Serum parathyroid hormone concentration measured by highly sensitive assay in post-thyroidectomy hypocalcemia of patients with Graves' disease.

To investigate the role of parathyroid function in transient hypocalcemia after subtotal thyroidectomy for Graves' disease, the serum parathyroid hormone (PTH) concentration and nephrogenous (N) cAMP were measured in 16 patients before and after surgery. Serum PTH was measured with two commercially available kits (PTH-M, PTH-C), PTH-M is a recently developed highly sensitive assay using an antibody recognizing the mid-portion of human PTH and a synthetic 125I-tyr45-human PTH (43-68) as a radioligand. One of the 16 patients had severe clinical tetany and had a markedly lower PTH-M concentration and NcAMP after thyroidectomy. However, no significant change in serum PTH-M, PTH-C and NcAMP were observed in the other patients, although their serum calcium (Ca) concentrations decreased significantly. The Data were analyzed by dividing the patients according to the change in serum Ca or PTH. Serum PTH-M and PTH-C significantly decreased in 4 patients whose serum Ca clearly decreased after surgery. Serum Ca on the first postoperative day was significantly lower in patients whose serum PTH decreased after thyroidectomy than in patients whose serum PTH did not. Furthermore, the serum Ca concentration was significantly correlated with PTH-M, and with NcAMP on the third postoperative day. These data proved that hypofunction of the parathyroid gland is important in transient hypocalcemia after subtotal thyroidectomy for Graves' disease. The pathogenetic mechanism of transient hypocalcemia was discussed in comparison with the data from a patient who had overt parathyroid injury.

Calcium↗
PubMed1989

Arterial-venous concentration gradient as a potential source of error in pharmacokinetic studies. Plasma concentration differences of 6-chloro-2-pyridylmethyl nitrate on constant infusion to rats.

1. Plasma concentrations of 6-chloro-2-pyridylmethyl nitrate (CPMN) at different sampling sites in the circulation were determined during and after constant infusion in the rat. 2. An arterial-venous CPMN concentration gradient was found and characterized by the following trends. During CPMN infusion into the right atrium, plasma concentrations were higher in arterial (aortic arch) than venous (inferior vena cava) plasma. After cessation of infusion the venous plasma concentrations were significantly higher (P less than 0.05) than those in arterial samples. There was a low concentration gradient between the right atrium and the peripheral artery, but substantial difference between the peripheral artery and the vein. There was a 1.8-2.4 extraction ratio of CPMN across the arterial-venous bed.

Animals↗
PubMed1989

[Ga-67 scintigram in evaluation of malignant lymphoma of the thyroid originating from chronic thyroiditis].

At the Itoh Hospital, 27 patients with primary malignant lymphoma of the thyroid gland have been diagnosed from April 1985 to April 1988. Within the 27 patients, 8 patients were treated with a diagnosis of chronic thyroiditis during 1 year to 7 years at Itoh Hospital. Ga-67 scintigraphy was performed in the 8 patients as suspected malignant lymphoma. Of the 8 patients, 6 were very strong positive, 1 was strong positive and 1 was weak positive. All patients with Ga-67 strong positive scans should have a biopsy and the scans are helpful to direct the biopsy. Ga-67 scintigraphy is useful in the diagnosis of malignant lymphoma of the thyroid gland.

Aged↗
PubMed1988

Isolation of angiotensin-converting enzyme inhibitor from tuna muscle.

A novel inhibitor of angiotensin-converting enzyme (ACE) has been discovered and isolated in a pure form from acid extract of tuna muscle by successive column chromatographies and HPLC. The final preparation showed IC50 values of 1 microM and 2 microM for ACEs from bovine and rabbit lungs, respectively. The amino acid sequence of the inhibitor has been established as Pro-Thr-His-Ile-Lys-Trp-Gly-Asp by the Edman procedure and carboxypeptidase digestion.

Amino Acid Sequence↗
PubMed1988

Suppression of gastric ulcer induced by stress and HCL-ethanol by intravenously administered metallothionein-II.

A metallothionein isoform metallothionein-II was isolated from the livers of zinc acetate-treated rats. Metallothionein-II, which showed a single band on polyacrylamide gel electrophoresis, was subjected to two kinds of anti-ulcer screening systems. It was shown that intravenously administered metallothionein-II suppressed the formation of rat water-immersion stress- and HCl-ethanol-induced gastric ulcer significantly. The effect may partly be derived from the zinc contained in the metallothionein-II. However, the effect of metallothionein-II was much stronger than that of an equivalent mole of zinc. Apparently, metallothionein-II had an anti-ulcerogenic activity not based on the effect of intrinsic zinc.

Acetates↗