[Synthesis and biological activity of sulfur containing derivatives of chalcone. IV. A novel method for the synthesis of thioaurones (author's transl)].
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Chalcone↗
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[Reactions concerned in tertiary amine n-oxides. VI. Reactions of 2'-hydroxychalcone derivatives with amine N-oxides (author's transl)].
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Catalysis↗
[Reaction of guanidines with alpha-diketones. II. Relation between the structure of reaction products of 1,1-pentamethyleneguanidine and benzamidine with 1-phenylpropane-1,2-dione and benzil and the coloration of Voges-Proskauer reaction (author's transl)].
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Amidines↗
[Chemical components of the roots of Angelica keiskei Koidzumi. II. The structure of the chalcone derivatives (author's transl)].
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Chalcone↗
The usefulness of electrophysiological-pharmacologic studies in the long-term therapy of paroxysmal tachycardias.
In 96 cases of paroxysmal tachycardia, results of chronic pharmacological assessment (CPA) were compared with acute electrophysiological-pharmacologic assessments (EPA) to evaluate the usefulness of EPA. I. Patients with sustained VT (31 cases): Sustained VT and repetitive ventricular response (RVR) could be induced in 61% and 23% respectively. More than one effective drug was found by EPA for 23 of 24 subjects. Of the 22 followed by CPA, the effectiveness of medication was excellent for 14 (64%), moderate for 1, slight for 4, and ineffective for 3 (14%). II. Patients with non-sustained VT (23 cases): RVR could be induced in 52%. Effective medication was identified by EPA for 8 of 10 patients. Of the 7 followed by CPA, the effectiveness of medication was excellent for 2(28.5%) moderate for 2, and ineffective for 3. III. Patients with PSVT (42 cases): PSVT could be induced in 90% of cases. Effective medication was found for all 31 cases which underwent EPA. Of the 23 cases followed by CPA, the chronic efficacy of drugs was excellent for 7 (30%), moderate for 5 (22%), slight for 7 (30%), and noneffective for 4 (18%). Therefore, we conclude that the usefulness of EPA differs according to the type of tachycardia. EPA is most useful in predicting chronic results for patients with sustained VT, especially when the sustained VT is readily reproducible by electrical stimulation. It is less useful for nonsustained VT and PSVT. With nonsustained VT, EPA is limited by difficulty in repeatedly inducing RVR, and by difficulty in predicting the appropriate medication for chronic oral therapy. With PSVT, even though the PSVT can be induced with greater success, EPA is limited by variations in pharmacologic effects over time, which create discrepancies between EPA and CPA.
Administration, Oral↗
Role of ONO-3144, a new cardioplegic agent, in the reoxygenation injury in the anoxic myocardium.
We have investigated the effect of ONO-3144 (2-aminomethyl-4-tert-butyl-6-propionylphenol), which facilitates the conversion of prostaglandin G2 to H2 and acts as a scavenger of free radicals, on the reoxygenation injury in the anoxic heart. Rat hearts were perfused retrogradely with Krebs-Henseleit (KH) medium for 30 min (n = 8) in Group I. In Group II, the hearts which were perfused with anoxic KH medium for 40 min were reoxygenated for 30 min (n = 8). Group III hearts were similar to those in Group II except that 4 mg ONO-3144/liter was added to both anoxic and reoxygenation media (n = 8). Coronary effluent was collected for creatine kinase (CK) loss. Four rats hearts in each group were fixed for electron microscopic study and the remaining hearts were frozen in liquid nitrogen for measurement of adenosine triphosphate (ATP). A six-fold increase in CK leakage, observed after reoxygenation of anoxic heart, was prevented by ONO-3144. Tissue ATP was reduced from 22.2 +/- 0.9 mumol/g dry weight (Group I) to 5.5 +/- 1.1 mumol/g dry weight (Group II). A significant amount of ATP (9.05 +/- 1.22 mumol/g dry weight) was preserved in the treated Group III. The number of normal cells obtained by morphometrical analysis increased significantly from 56.7 +/- 7.8% (Group II) to 86.2 +/- 1.0% (Group III) and moderately injured cells were reduced to 3% in Group III as compared to 16% in the untreated Group I. Injury to the severely injured cells was not prevented by the drug treatment. At electron microscopic level, the cellular membranes, mitochondria and glycogen deposits were well preserved in Group III. Thus, ONO-3144 treatment provides a protection against reoxygenation injury in the anoxic myocardium by scavenging. .OH or other closely related species of free radicals. Therefore, free radicals generated through the conversion of prostaglandin G2 to H2 might play an important role in the reoxygenation injury of the anoxic myocardium.
Adenosine Triphosphate↗
[Studies on the anti-ulcer effects of isoprenyl flavonoids (1). The anti-ulcer effects of isoprenyl chalcone extracted from Sophora subprostrata (author's transl)].
A series of extracted fractions from sophora subprostrata was screened by determining anti-ulcer effects in pylorus ligated and stressed rats. Fr. [C-2] had the most potent anti-ulcer effects of all fractions extracted. Sophoradin and sophoranone which were isolated from Fr. [C-2] were also found to have inhibitory effects on ulcer formation in pylorus ligated and stressed rats. The anti-ulcer effect of sophoradin was relatively potent in comparison with that of sophoranone and/or Fr. [C-2]. The anti-ulcer effect of sophoranone was approximately the same as that of Fr. [C-2]. The authors examined the effects of sophoradin and sophoranone on gastric secretion in pylorus ligated rats. Sophoradin and sophoranone significantly reduced the volume of gastric juice. Sophoradin but not sophoranone inhibited the free and total acid output of gastric juice. The effect of sophoradin was examined on various secretagogues which induced gastric secretions in rats with acute fistula. Sophoradin showed a tendency to inhibit tetragastrin- and insulin-induced gastric acid secretion, but there were no effects on methacholine- and histamine-induced secretions. These results suggest that sophoradin may have marked anti-ulcer and inhibitory effects on gastric secretion.
Animals↗
Studies on increased bile formation produced by polyoxybenzenes in rats.
Mechanism of hypercholeretic effect of three polyoxybenzenes, 2,4,6-trihydroxypropiophenone (THPP), 4-methylumbelliferone (4-MU) and 3-(2',4',5'-triethoxybenzoyl)propionic acid (AA-149), was studied in rats. Biliary clearance of 14C-labeled erythritol indicated that all the choleretics increased canalicular bile production. AA-149 excreted in the bile chiefly as the glucuronide provided no significant osmotic drive for bile formation. Both the biliary bile acid concentration and total biliary excretion of bile acids were lower in the rats treated with THPP, 4-MU or AA-149 than in control rats. These choleretics were also effective in the isolated rat liver perfusion system, in which concentration and output of biliary bile acids were low. Thus, it was unlikely that bile acids were involved in the hypercholeresis induced by the choleretics. THPP, 4-MU and AA-149 increased biliary excretion of sodium both in the biliary-cannulated rats and in the isolated rat liver perfusion system. It was concluded that the hypercholeresis induced by THPP, 4-MU and AA-149 was due to an enhanced formation of the bile acid-independent fraction of canalicular origin, probably mediated by the active transfer of sodium into the canaliculi.
Animals↗
Effect of an anti-ulcer agent, 2'-carboxymethoxy-4, 4'-bis (3-methyl-2-butenyloxy) chalcone (SU-88), on the biosynthesis of gastric sulfated mucosubstances in restrained and water-immersed rats.
2'-Carboxymethoxy-4,4'-bis(3-methyl-2-butenyloxy) chalcone (SU-88) has an anti-ulcer effect which is considered to increase the resistant factors of the gastric mucosa. In order to clarify the mechanism of the action of SU-88, the biosynthesis of gastric sulfated mucosubstances (SMS) in vivo and in vitro was investigated in rats with gastric erosion induced by restraint and water-immersion. The incorporation of 35S-sulfate into gastric SMS was significantly reduced 18 hr after the onset of stress. Pretreatment with SU-88 (500 mg/kg, p.o., X 10 days) prevented a reduction in the incorporation of 35S-sulfate due to stress when 35S-sulfate was administered in vivo. On the contrary, the incorporating activity of 35S-sulfate into the SMS in the isolated rat gastric mucosa with erosion was significantly increased 12 hr after the onset of stress, as compared with that of the control group in vitro. The incorporation of 35S-sulfate into the SMS was still further increased by the oral administration of SU-88. The mode of action of SU-88 on the biosynthesis of SMS was discussed.
Animals↗
Effects of etafenone on myocardial energy metabolism as studied by an organ redoximeter and biochemical analyses.
Direct recording of reduced nicotinamide adenine dinucleotide (NADH) fluorescence was conducted with an organ redoximeter in isolated perfused guinea pig heart. Cross-clamping of the aortic inflow line resulted in an increase in NADH fluorescence. After etafenone (10(-6) M), there was a significant prolongation of the time to the detectable or the maximum increase in NADH fluorescence. The magnitude of the increase in NADH fluorescence tended to be reduced (135% as compared with 145% in the control group). Supplemental chemical analyses revealed a significant increase in creatine phosphate, adenosine triphosphate (ATP) and total adenine nucleotide in the etafenone-pretreated group 15 min after postischemic reperfusion, although the ischemia-induced changes were not improved by this compound. It was suggested that the better recovery of myocardial high energy phosphate levels produced by etafenone was brought about by a decrease in oxygen consumption due to a decrease in mechanical performance of the heart and possibly by a better resynthesis of ATP.
Animals↗
Effect of 2'-carboxymethoxy-4,4'-bis(3-methyl-2-butenyloxy) chalcone (sofalcone) on chronic gastric ulcers in rats.
The anti-ulcer effect of sofalcone, an isoprenyl chalcone derivative, on acetic acid-induced gastric ulcers in rats was studied histologically and histochemically. After administrations of sofalcone at 50 and 200 mg/kg twice daily for 10 days, contraction of the ulcer, mucosal regeneration, accelerated development of the collagen fibers in the granulation tissue at the base of the ulcer, and increase of acid mucopolysaccharides, an alcian blue stain-positive substance covering the regenerated mucosa, were noted. The healing effect of sofalcone was balanced in mucosal regeneration and connective tissue proliferation (formation of the collagen fibers). Sofalcone of 50 mg/kg showed a greater healing effect than gefarnate at the same dose and had a similar healing effect as L-glutamine at 200 mg/kg.
Acetates↗
Cytoprotective effect of SU-88, an anti-ulcer agent, in the rat.
The gastric cytoprotective action of SU-88, an anti-ulcer agent, was studied in rats. SU-88 dose-dependently prevented the formation of gastric lesions induced by absolute ethanol as observed by PGE2. The efficacy of SU-88 when given i.p. was more potent than the p.o. administration. Indomethacin (5mg/kg, p.o.) given 30 min prior to SU-88 dosing blocked this protective effect, whereas it was not affected when indomethacin was given 30 min after the SU-88 dosing. Cimetidine, on the other hand, failed to exert a protective effect against the ethanol-induced lesions and caused a significant increase in the lesions induced by 0.6N HCI. Pretreatment with SU-88 prior to cimetidine resulted in a marked reduction in the lesions. SU-88 was found to increase the synthesis of gastric glycoproteins and to prevent the reduction of glycoprotein synthesis caused by the administration of absolute ethanol. However, no increase in the synthesis was observed 5 min after the SU-88 dosing, although the lesion was significantly suppressed at that time. These findings indicate that SU-88 possesses a cytoprotective effect and that this effect seems to be mediated by the increase in endogenous PG.
Animals↗
Effects of eperisone applied by microiontophoresis on neurons in the medial and lateral vestibular nuclei.
Electrophysiological studies were performed to elucidate the mechanism underlying the antivertigo action of eperisone, an antispastic drug, using cats anesthetized with alpha-chloralose. Iontophoretic application of eperisone up to 100 nA produced a dose-dependent inhibition of spike generation upon vestibular nerve stimulation in monosynaptic and polysynaptic neurons of the medial vestibular nucleus (MVN). The inhibition of neurons in the MVN was more prominent than that in the lateral vestibular nucleus. In addition, iontophoretically applied eperisone in doses of 50-100 nA inhibited the orthodromic spike elicited by vestibular nerve stimulation in the MVN monosynaptic neurons projecting to the abducens nucleus (ascending neuron), without affecting that in the MVN neurons projecting to the spinal cord (descending neuron). An inhibition of antidromic spike elicited by abducens nucleus stimulation in the MVN monosynaptic ascending neurons was observed in some cases during application of eperisone. These results suggest that eperisone predominantly inhibits synaptic transmission of the MVN ascending neurons.
Animals↗
Effect of sofalcone on the gastric cell proliferation in the experimental gastritis of rats.
Effects of sofalcone on the morphometrical glandular structure and the generative cell proliferation in the gastric mucosa of gastritis, induced in rats by the treatment of sodium taurocholate (TCA) for 3 and 6 months, were examined by means of 3H-thymidine autoradiography. Morphometrical observation revealed that the ratios of the length of the glandular portion/the total length of the gastric gland were generally decreased in both fundic and pyloric glands with TCA treatments, which may indicate mucosal atrophy. These atrophic changes were improved to the normal levels by the administration of sofalcone for 3 weeks after the treatment of TCA. On the other hand, cell proliferative activity, indicated by the labeling indexes in the generative cell zone of gastric mucosa, was increased in TCA induced gastritis rat, which seems to be the response to replace the increased cell loss. The administration of sofalcone to the gastritis rats further increased the labeling indexes, especially in pyloric gland with statistical significance in both TCA treated rats for 3 and 6 months. From these results, it is suggested that sofalcone stimulates the compensatory increase of proliferative activity of generative cells, which would be available to repair the gastric mucosa with gastritis.
Animals↗
Mechanisms of action of eperisone on isolated dog saphenous arteries and veins.
Effects of eperisone, an antispasmodic in skeletal muscle, were investigated in helical strips of dog saphenous artery and vein. Eperisone relaxed saphenous arteries and veins previously contracted with norepinephrine, serotonin, acetylcholine, K+, or Ba2+; but in contrast, it produced contractions in the blood vessels contracted with prostaglandin (PG) F2 alpha. Treatment with eperisone attenuated the contractions induced by norepinephrine and serotonin in the arteries and those by clonidine and phenylephrine in the veins. Eperisone inhibited angiotensin II-induced relaxations, mediated possibly by endogenous PGI2, but did not alter relaxations caused by exogenous PGI2. Treatment with eperisone (10(-5) M) potentiated the contractile response to electrical stimulation of adrenergic nerves; the potentiating effect was suppressed by yohimbine. The eperisone-induced contraction in PGF2 alpha-contracted arteries was inhibited by treatment with indomethacin or aspirin, although cyclooxygenase activity was not inhibited by eperisone. These results may indicate that eperisone blocks postjunctional alpha 1- and alpha 2-adrenergic, muscarinic, serotonergic receptors and prejunctional alpha 2 adrenoceptors and reduces PGI2 synthesis via a mechanism other than cyclooxygenase inhibition.
Animals↗
Effects of afloqualone on vestibular nystagmus and the lateral vestibular nucleus.
To clarify the antivertiginous effect of afloqualone, an antispastic drug, we examined its action on the vestibular nervous system in cats. The results suggest that afloqualone inhibits vestibular nystagmus probably due to both inhibition of selective polysynaptic transmission and enhancement of the effects of GABA and glycine in the lateral vestibular nucleus (LVN), and its GABA-enhancing effect is thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site.
Acetylcholine↗
Effects of eperisone-HCl on the stretch reflex in anesthetized cats.
The effect of eperisone-HCl on the spinal stretch reflex was investigated in cats anesthetized with urethane-chloralose. The reflex activity, elicited by muscle stretches, was recorded from the split ventral root and analyzed using a cross-correlation histogram between the motoneuronal spikes and muscle stretches. Eperisone-HCl was intravenously applied at a dose of 5 mg/kg. It was found that eperisone weakly inhibited the reflex activity of tonic motoneurons (approximately 30%), and that of the phasic ones was either moderately (approximately 70%) or completely (100%) inhibited by eperisone. The cross-correlation analysis suggested that the membrane potentials of both tonic and phasic motoneurons are equally lowered by eperisone or that monosynaptic transmission from primary afferents of muscle spindles to motoneurons is inhibited by eperisone.
Anesthesia↗
Anti-nicotinic and anti-muscarinic actions of eperisone in the isolated canine atrium.
The effects of eperisone, an antispastic agent, on the chronotropic and inotropic responses to acetylcholine, nicotine or stimulation of intracardiac autonomic nerves were evaluated in isolated, blood-perfused canine atrium. Eperisone (10-300 micrograms) injected into the sinus node artery of the isolated atrium produced dose-related negative chronotropic and inotropic effects, which were not affected by atropine. In the same doses, eperisone inhibited the negative chronotropic and inotropic responses to an injection of acetylcholine and intracardiac parasympathetic stimulation. Eperisone also suppressed the negative followed by positive cardiac responses to nicotine, but did not modify the positive responses to intracardiac sympathetic stimulation or norepinephrine. The inhibitory effect persisted much longer for the responses to nicotine or parasympathetic stimulation than for those to acetylcholine. These results suggest that eperisone at doses that induce direct cardiac depressant effects exerts its blocking action on nicotinic receptors at parasympathetic ganglia and sympathetic nerve terminals and on muscarinic receptors at the effector cells in the dog heart.
Acetylcholine↗