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PubMed1987

Inhibitory effect of prolonged oral administration of cetraxate hydrochloride on experimentally-induced intestinal metaplasia in Wistar rats.

The effect of cetraxate hydrochloride (Neuer) on the induction of intestinal metaplasia by intragastric instillation of 5% NaOH solution was investigated in Wistar rats. Oral administration of cetraxate, beginning 2 days after NaOH treatment, resulted in a significant increase in antral mucosal blood flow and a significant reduction in the incidence and amount of intestinal metaplasia in experimental week 25, but no significant changes in basal acid secretion or antral mucosal pH. On histological examination, goblet cell metaplasia were frequently seen. These results show that the increased gastric blood flow produced by cetraxate hydrochloride may be associated with the suppression of induction of intestinal metaplasias.

Administration, Oral↗
PubMed1994

Anti-ulcer effect of 1,6-dihydro-2-[2-(2-methylpropoxy) anilino]-6-oxo-5-pyrimidinecarboxylic acid on experimental gastric ulcers in rats.

The effects of 1,6-dihydro-2-[2-(2-methylpropoxy) anilino]-6-oxo-5-pyrimidinecarboxylic acid (MAR-99, CAS 98772-05-5) on various experimental gastric ulcers were studied in rats. MAR-99 (3-100 mg/kg, p.o. or i.d.) showed the anti-ulcer effect in Shay-, stress, acetylsalicylic acid (ASA)- and compound 48/80-ulcer models and significantly accelerated healing of acetic acid-induced gastric ulcer in rats. In addition, MAR-99 (1-10 mg/kg p.o.) decreased dose-dependently the gastric mucosal damage induced by necrotizing agents such as 99.5% ethanol, 0.6N HCl and 0.2 N NaOH. These results indicate that MAR-99 may be useful for the treatment of gastric ulcer in human.

Acetates↗
PubMed1996

Dipeptide uptake: a novel marker for testicular and ovarian macrophages.

BACKGROUND: Testicular and ovarian macrophages seem to be involved in paracrine regulation of steroidogenesis. Markers suitable for the identification of these cells under viable conditions would allow new experimental approaches in the study of biological interactions between hormone-producing cells and tissue macrophages. METHODS AND RESULTS: Dipeptide uptake was studied in primary cultures from rat testis and ovaries with the fluorescent dipeptide derivative beta-Ala-Lys-N epsilon-aminomethylcoumarin acetic acid (AMCA). Fluorescence microscopic studies revealed that the reporter peptide accumulated specifically in testicular macrophages, which were identified by subsequent immunostaining with the OX-42 antibody. In the ovarian cultures, however, transport of the fluorescence-labeled dipeptide was observed in cells that exhibited the morphological characteristics of macrophages but did not show positive immunoreactivity against the antibody employed. In both cases, dipeptide accumulation was blocked by the addition of Tyr-Gly, thus indicating that transport was not due to endocytosis. Competition studies performed with primary cultures from testis have shown that di-and tripeptides effectively reduce uptake of the tracer peptide, whereas compounds without an alpha- or beta-amino group, such as captopril and benzylpenicillin, do not. CONCLUSIONS: These results indicate that the testicular and ovarian macrophages are equipped with a dipeptide transport system. The selective accumulation of the fluorescent dipeptide derivative beta-Ala-Lys-N epsilon-AMCA in testicular and ovarian macrophages permits the identification of these cell types under viable conditions.

Amino Acids↗
PubMed1993

Development of active center-directed plasmin and plasma kallikrein inhibitors and studies on the structure-inhibitory activity relationship.

The molecule of trans-4-aminomethylcyclohexanecarbonylphenylalanine 4-carboxymethylanilide (8), which is a potent and selective inhibitor of plasma kallikrein, can be divided into three parts (P1, P1' and P2'), each of which contains one of the rings. In order to study the role of each part in the manifestation of potent and selective inhibitory activity and the relationship between the structure and inhibitory activities toward plasmin, plasma kallikrein, urokinase and thrombin, each part was substituted with various other moieties to give many kinds of analogs and their inhibitory activities against the above enzymes were examined. Among them, trans-4-aminomethylcyclohexanecarbonyl-O-2-bromobenzyloxycarbon yltyrosine 4-acetylanilide (12) inhibited plasmin and plasma kallikrein with IC50 values of 2.3 x 10(-7) M and 3.7 x 10(-7) M, and K(i) values of 1.2 x 10(-7) M and 1.3 x 10(-7) M, respectively.

Amino Acid Sequence↗
PubMed1993

Syntheses and inhibitory effects on gastric lesions of trans-guanidinomethylcyclohexane carboxylic acid arylamides.

A novel series of trans-guanidinomethylcyclohexanecarboxylic acid (trans-GMCHA) arylamides was synthesized. The several trans-GMCHA arylamide derivatives showed more potent inhibitory effects on the stress- and HCl-ethanol-induced gastric ulcers than cetraxate in rats. In acute toxicity studies in mice, most amides showed such severe toxicity that all mice injected with these compounds (50 mg/kg, i.p.) died. However, mice injected with the trans-GMCHA (2'-,3'- and 4'-ethoxycarboxy)phenylamide (7, 8 and 9) which bear an alkyloxycarbonyl group at benzene ring survived. From these results, trans-GMCHA (2'-ethoxycarbonyl)phenylamide (7) was selected as a promising anti-ulcer agent.

Animals↗
PubMed1991

Ligand specificity of human plasminogen kringle 4.

The ligand specificity of the human plasminogen kringle 4 was characterized in terms of ligand size, aromatic/aliphatic character, and ionic charge distribution. The binding of the following ligands was investigated via 1H NMR spectroscopy, and their equilibrium association constants (Ka) were determined: (1) p-aminomethylbenzoic acid (Ka approximately 4.8 mM-1), (2) benzylamine (Ka approximately 0.2 mM-1), (3) l-aminohexane (Ka approximately 0.07 mM-1), (4) 7-aminoheptanoic acid (Ka approximately 6.6 mM-1), (5) 5-aminopentanoic acid (Ka approximately 16 mM-1), (6) N alpha-acetyl-L-arginine (Ka approximately 0.3 mM-1), and (7) N alpha-acetyl-L-arginine methyl ester (Ka approximately 0.08 mM-1). Benzamidine and L-arginine do not bind measurably to kringle 4. We have also established that 1-hexanoic acid and 4-methylbenzoic acid do not interact significantly with kringle 4 (Ka less than 0.05 mM-1). The Trp62 resonances were found to be quite sensitive to aromatic ligands as well as to aliphatic ligand length. Phe64 is similarly sensitive to the ligand aromatic/aliphatic character and chain length and to the identity of the ligand anionic group. His31 and His33 do not respond significantly to variations in ligand structure, although they are perturbed by aromatic and aliphatic effectors. The perturbations induced by the arginine derivatives on these residues show that these compounds interact with the lysine-binding site (LBS) of kringle 4. The LBS was further characterized using 2D NMR studies of a kringle 4/trans-(aminomethyl)cyclohexanecarboxylic acid (AMCHA) complex. A complete assignment of the AMCHA spectrum in the bound state was achieved. This enabled the unambiguous identification of intermolecular contact points between the central AMCHA protons and Trp62 and Trp72. A model based on the X-ray crystallographic structure of kringle 4, incorporating these constraints, has been derived.

4-Aminobenzoic Acid↗
PubMed1990

Effects of 12-sulfodehydroabietic acid monosodium salt (TA-2711), a new anti-ulcer agent, on gastric mucosal lesions induced by necrotizing agents and gastric mucosal defensive factors in rats.

Effects of TA-2711 on gastric mucosal lesions induced by various necrotizing agents and several defensive factors of gastric mucosa were investigated in rats. Oral administration of TA-2711 at 12.5 to 200 mg/kg prevented the formation of gastric mucosal lesions induced by 99.5% ethanol, 0.6 N HCl, 0.2 N NaOH and boiling water with ED50 values of 24, 58, 16 and 101 mg/kg, respectively. Oral TA-2711 at 100 mg/kg increased the gastric mucosal prostaglandin E2 (PGE2) level without any change in transmucosal potential difference. A sustained decrease in gastric mucosal blood flow produced by intragastric administration of 99.5% ethanol was inhibited by oral TA-2711 (50, 100 mg/kg) and 16,16-dimethyl PGE2 (10 micrograms/kg). The effect of TA-2711 on ethanol-induced decrease in blood flow was suppressed by indomethacin (10 mg/kg, s.c.). Oral TA-2711 (25-100 mg/kg) dose-dependently increased the amount of mucus adherent to the gastric mucosa. In addition, gastric HCO3- secretion was increased by intragastric TA-2711 at 2.5 and 5.0 mg/ml. These results suggest that TA-2711 enhances gastric mucosal resistance by increasing mucus and HCO3- secretion and by maintaining mucosal blood flow, and protects the gastric mucosa against various irritants. The effects of TA-2711 appear to be mediated by mucosal prostaglandins such as PGE2.

Abietanes↗
PubMed1980

A simple rapid method for isolating soluble fibrin complexes from fibrinogen by treatment with thrombin and t-AMCHA.

Using treatment with thrombin associated with trans-aminomethylcyclohexane carboxylic acid (t-AMCHA), a simple and rapid method for isolating soluble fibrin complexes (SFC) from fibrinogen in the plasma was developed. By this procedure, the recovery rates of SFC and early FDP (mainly X) increased according to the concentration of t-AMCHA, reaching a maximum at 286 mM t-AMCHA. On the other hand, the recovery rate of fibrinogen remained below 1.5% and that of late FDP was almost 100% at all concentrations of t-AMCHA. These results suggested that SFC and FDP could be isolated from fibrinogen by thrombin and t-AMCHA (286 MM) treatment. Moreover, it was possible to isolate SFC from FDP using gel filtration after treatment with thrombin and t-AMCHA. The SFC could be quantified by assay of the eluted fractions containing SFC by the staphylococcal clumping test.

Aprotinin↗
PubMed1984

Effect of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) on gastric mucosal damage induced by various necrotizing agents in rats.

The effect of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) on the gastric mucosal damage induced in rats by various necrotizing agents was compared with those of cimetidine, cetraxate and prostaglandin (PG) E2. MN-1695 at doses of 0.37 mg (1 mumol) to 3.72 mg (10 mumol)/kg, significantly decreased in a dose-dependent manner the damage indices after the application of ethanol, HCl, NaOH, 25% NaCl or boiling water. Cimetidine in doses of 12.6 mg (50 mumol) to 126 mg (500 mumol)/kg was effective only against HCl-induced damage. Cetraxate in doses of 34.2 mg (100 mumol) to 342 mg (1 mmol)/kg was effective against damage due to ethanol, HCl, 25% NaCl or boiling water. However, cetraxate increased the damage index of NaOH-induced injury. PGE2 in a dose of 25 micrograms (70 nmol)/kg was effective against ethanol and 25% NaCl. The histological changes of gastric mucosal cells produced by ethanol were significantly decreased by MN-1695 and PGE2. These results suggest that MN-1695 has a cytoprotective action like that of PGE2 and that this cytoprotection inhibits the development of various kinds of experimental gastric ulcers.

Animals↗
PubMed1980

Cerebral complication of antifibrinolytic therapy in the treatment of ruptured intracranial aneurysm. Animal experiment and a review of literature.

Among the reported complications of the antifibrinolytic therapy in the treatment of ruptured intracranial aneurysms, nausea and vomiting, cerebral arteriopathy and secondary hydrocephalus would be a matter of concern in its possible CNS involvement. However, little is known about the possibility of direct cerebral effect in synthetic antifibrinolytics. A simply designed animal experiment disclosed remarkable effects on electroencephalography, blood flow of the cerebral cortex and intracranial pressure. Such antifibrinolytics should not be given intrathecally in any situation even if the accumulation of the agents in cerebrospinal fluid is essential to prevent recurrent hemorrhage.

Aminocaproates↗
PubMedDate not supplied

[Effect of imizin and transamine on the bioelectrical activity of the ventrolateral columns of the spinal cord].

It was established in experiments on spinal rats that imizine (2.5-10 mg/kg) decreased spontaneous activity and that evoked by stimulation of the sciatic nerve and intraarterial injection of bradykinin in the dorsal horns and ventrolateral columns of the spinal cord. Transamine (1-5 mg/kg) reduced the evoked activity in the dorsal horns and ventrolateral columns but potentiated spontaneous activity in these structures. Naloxone (1 mg/kg) reduced the effect of imizine (5 mg/kg) on the bradykinin-induced nociceptive activity in the ventrolateral columns of the spinal cord.

Animals↗