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Volume 92 (1988)
- Issue 6 Pages 337-
- Issue 5 Pages 271-
- Issue 4 Pages 201-
- Issue 3 Pages 167-
- Issue 2 Pages 61-
- Issue 1 Pages 1-
Volume 92, Issue 4
Displaying 1-6 of 6 articles from this issue
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Takashi MATSUBARA, Katsumi HIROSE, Hisao HATAKEYAMA, Hirokuni JYOYAMA, ...1988 Volume 92 Issue 4 Pages 201-213
Published: 1988
Released on J-STAGE: February 23, 2007
JOURNAL FREE ACCESSEffect of the nonsteroidal anti-inflammatory drug 480156-S on liver drug-metabolizing activity was studied in rats, and its effect was compared with that of cimetidine. Cytochrome P-450-dependent 7-alkoxycoumarin O-dealkylase activity was not affected by a single administration of 480156-S, but the activity, especially the O-demethylase but not the O-depropylase, was suppressed dose-dependently by multiple administrations. Pretreatment of rats with phenobarbital caused a diminution of the inhibitory action of 480156-S. Treatment of rats with cimetidine resulted in a marked decrease in the activity, although it recovered 24 hr later. After the pretreatment of animals with 480156-S or reference drugs, the pharmacological action of diazepam was determined using muscle relaxation and inhibitions of electroshock-induced convulsion and pentetrazole-induced clonic convulsion as the indicators. Prolonged pharmacological activity of diazepam was observed when liver drug-metabolizing activity was lowered by the pretreatment. On the other hand, pentobarbital-induced anesthesia was prolonged by the pretreatment of rats with cimetidine, but the anesthesia was not modified by the administration of 480156-S. These results suggest the inhibitory action of 480156-S on a specific form(s) of P-450 isozyme.View full abstractDownload PDF (10382K) -
Katsuyuki NISHIKI, Kozue NISHINAGA, Daigo KUDOH, Katsumi IWAI1988 Volume 92 Issue 4 Pages 215-225
Published: 1988
Released on J-STAGE: February 23, 2007
JOURNAL FREE ACCESSA hemorrhoid model was prepared by means of application of croton oil onto the recto-anus of rats. Cotton swab soaked with the inducer, which consisted of water, pyridine, diethylether and 6% croton oil in diethylether, was inserted into the anus. The following conditions were found to be optimal for preparing the model: cotton swab containing 0.16 ml of the inducer solution was applied to the anus of a 6 week-old rat (body wt. about 140 g) for 10 sec. The edema developed linearly until 7-8 hr after application, and the severity of the edema was sustained almost constantly for more than 24 hr. Macroscopic observations at 6 hr p. a. revealed homogeneous and consistent inflammation in the recto-anus applied region. Histological observation showed appearance of edema, infiltration of fibrin, inflammatory cells, vasodilatation, blood congestion and medium to high degrees of necrosis in the mucosal epithelium. Thus this model was useful for evaluating the effect of anti-hemorrhoidal drugs on intumescence and vasodilatation. The efficacy of diflucortolone valerate, hydrocortisone caproate and hydrocortisone was evaluated in this model. Wet weight and vasopermeability increased by the inducer was suppressed strongly by simultaneous application of the corticoids, and the degree of suppression was parallel with the potency of the glucocorticoid activity. Compared to Scheriproct®, Posterisan forte®, Posterisan® and Borraginol N®, Neriproct® showed the strongest effects in the protection against and treatment of the experimental hemorrhoid. Scheriproct®, which was less active than Neriproct®, was also found to have higher efficacy than the others.View full abstractDownload PDF (11398K) -
Katsuyuki NISHIKI, Daigo KUDOH, Kozue NISHINAGA, Katsumi IWAI, Hidehik ...1988 Volume 92 Issue 4 Pages 227-240
Published: 1988
Released on J-STAGE: February 23, 2007
JOURNAL FREE ACCESSSeveral glucocorticoids as a cream formulation were applied to the recto-anus of the crotonoil-induced hemorrhoid rat. Among the steroids tested, i.e. diflucortolone valerate (DFV), prednisolone (PS), hydrocortisone caproate (HC), and hydrocortisone (H), DFV was found to suppress inflammation most effectively. The effect of DFV was not affected by combination with lidocaine. In this model, the analgesic effect of lidocaine was apparently prolonged by an increase of the threshold for pain by the anti-inflammatory effect of DFV. This additive effect is regarded as a merit of the combination in Neriproct®. Therapeutic effects of Neriproct® and several anti-hemorrhoid drugs were also examined by using a hemorrhoid model with abrasive irritation compared to those obtained by the croton-oil model. In both models, efficacy of Neriproct® was superior to that of the other drugs such as Scheriproct®, Proctosedyl®, Posterisan forte®, Borraginol N®, Posterisan® and Borraza G®. Microscopic observation showed that destruction of the mucus epithelium, necrosis of the mucus layer, infiltration of inflammatory cells and vasodilatation in the croton-oil model were also suppressed markedly by Neriproct® application. No difference was observed in the efficacy between the cream and suppository formulation of Neriproct®. Suppression of wound healing was found with a dosage of DFV lower than those of PS, HC and H. However, the efficacy ratio of the wound-healing suppression and anti-inflammation of DFV was the largest among the steroids tested.View full abstractDownload PDF (14961K) -
Tsutomu KAMEYAMA, Toshitaka NABESHIMA, Akira KATOH, Shin-ichi OGAWA1988 Volume 92 Issue 4 Pages 241-250
Published: 1988
Released on J-STAGE: February 23, 2007
JOURNAL FREE ACCESSEffects of naftidrofuryl oxalate (LS-121) on experimental amnesia models, which were induced by cycloheximide (CXM), scopolamine (SLOP) and basal-forebrain (BF) lesion, were investigated using the step-through passive avoidance response in rats. In the retention test, a cut-off time of 600 sec was employed for the measurement of step-through latency (STL). The animals, that showed over 300 sec of STL was regarded as having the criterion of memory retention (% of retention). Increase in both parameters of STL and % of retention was regarded to indicate that the drug was able to improve the amnesia. If only one of the two parameters was increased, we considered that the drug had a tendency to improve the amnesia. Pretraining, post-training and pre-retention treatment of LS-121 (25 mg/kg) improved CXM-and SLOP-induced amnesia. Post-training treatment of LS-121 (25 mg/kg) showed a tendency to improve the BF lesion-induced amnesia. These results suggest that the antiamnesic action of LS-121 may be produced through an activation of the acetylcholinergic neuronal system. Since it improved the amnesia when administered in the pre-retention test, there is a possibility that LS-121 has not only a protective effect, but also a therapeutic effect. Furthermore, it is suggested that LS-121 may also have a therapeutic effect on Alzheimer's disease, since it showed a tendency to improve the BF lesion-induced amnesia.View full abstractDownload PDF (7626K) -
Kazuhiko SUDO, Kazuhiro HONDA, Masayuki TAKI, Masanao KANITANI, Yuichi ...1988 Volume 92 Issue 4 Pages 251-261
Published: 1988
Released on J-STAGE: February 23, 2007
JOURNAL FREE ACCESSExperiments were performed to investigate the effects of TJ-41 on spermatogenic disorders under current treatment with adriamycin (ADR). Male ICR mice were intraperitoneally injected with ADR at the dose of 0.15 mg/kg, twice a week for 5 weeks. Simultaneously, these mice were orally administered TJ-41 at the dose of 1, 2 or 4 g/kg for 12 weeks. The effects of TJ-41 were evaluated by histological analysis of germ cells in the testis at 7 weeks after the last injection of ADR. TJ-41 at a dose of 4 g/kg significantly inhibited the decrease of testis weight in mice treated with ADR. TJ-41 at doses of 1 and 4 g/kg significantly decreased the proportion of seminiferous tubules without germ cells as compared with the ADR-treated group. On the other hand, TJ-41 at doses of 1 and 4 g/kg significantly increased the proportion of normal seminiferous tubules and the Sertoli cell ratio of spermatocytes as compared with the ADR-treated group. These results indicate that TJ-41 may qualitatively and quantitatively protect against the decrease of germ cells in the testis of mice treated with ADR.View full abstractDownload PDF (11590K) -
Miwa MISAWA, Naoto IMAMURA1988 Volume 92 Issue 4 Pages 263-270
Published: 1988
Released on J-STAGE: February 23, 2007
JOURNAL FREE ACCESSThe measurement of viscoelasticity of airway secretions (sputum) has been very difficult, because the secretions, mainly consisting of high molecular weight glycoproteins, are heterogeneous and non-Newtonian viscous fluid. In the present study, a new in vitro method was devised for evaluating the effects of mucolytic expectorants, using porcine gastric mucin as a mucous fluid. Twenty percent porcine gastric mucin solution was prepared by dissolving it in tris-HCl buffer solution. The mucolytics tested were incubated with the mucin solution at pH 7.0 and 37°C for 30 min. The viscoelasticity of mucous fluid was determined by the glass plate method and rheometer method. The two cysteine-mucolytics, acetylcysteine (10-3 ?? 10-1M) and ethylcysteine (10-3 ?? 10-1 M) showed a marked viscoelasticity-lowering effect with either method. On the other hand, another cysteine-mucolytic, carbocysteine had no mucolytic effect at pH 7.0, but showed its effect at pH 6.0. A protease-mucolytic, α-chymotrypsin (0.1 ?? 10 mg/ml), remarkably lowered the viscoelasticity of mucin fluid with either method. Bromhexine (3×10-4 ?? 3×10-3 M) had no mucolytic effect even at the range of pH 6 ?? 8. From the above findings, it is indicated that distinct evaluation of the mucolytic actions of expectorants is feasible using porcine gastric mucin. The glass plate method has many advantages over the rheometer method in terms of required sample volume, measurement time, inexpensiveness, and so on.View full abstractDownload PDF (5816K)
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