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H Ikuta

Publications and source records attributed to H Ikuta.

At least 55 records · Page 3Linked to original sources
PubMed1987

Pharmacological properties of N-methoxy-3-(3,5-ditert-butyl-4-hydroxybenzylidene)-2-pyrrolidone (E-5110), a novel nonsteroidal antiinflammatory agent.

The antiinflammatory activity of a novel pyrrolidone derivative E-5110 was investigated using anti-inflammatory, analgesic and antipyretic animal models in comparison to indomethacin (IND) and piroxicam (PIR). The acute antiinflammatory activity of E-5110 on carrageenin paw edema was similar to IND, and half of PIR. E-5110 inhibited the pleural exudate volume and leucocyte infiltration in a reversed passive Arthus reaction more potent than IND. The chronic inflammatory responses in the established adjuvant- and type II collagen-induced arthritis were suppressed by E-5110 similar to IND and PIR. The analgesic potency of E-5110 was similar to IND and PIR, but the antipyretic activity of E-5110 was more potent than that of IND, and slightly more potent than that of PIR. The ulcerogenic effect of E-5110 on rat gastric mucosa was less than that of the reference drugs.

Animals↗
PubMed1987

In vitro effect of N-methoxy-3-(3,5-ditert-butyl-4-hydroxybenzylidene)-2-pyrrolidon e (E-5110), a novel nonsteroidal antiinflammatory agent, on generation of some inflammatory mediators.

Cultured rat synovial cells generate PGE2 upon stimulation with a factor derived from rate polymorphonuclear cells (Prostaglandins 27, 697, 1984). E-5110 inhibited PGE2 generation by the synovial cells. The IC50 values (microM) for inhibition of PGE2 generation were 0.026 for E-5110, 0.008 for indomethacin, 0.112 for piroxicam, 0.003 for R-830, 0.667 for BW-755C and 2.05 for benoxaprofen. Calcium ionophore A-23187-stimulated LTB4 generation by human neutrophils was inhibited by E-5110 with an IC50 value of 0.20 microM, which was similar to NDGA. The inhibition of LTB4 by E-5110 was more potent than that of R-830, BW-755C or benoxaprofen. E-5110 also inhibited superoxide generation by human neutrophils stimulated with opsonized zymosan, f-Met-Leu-Phe and phorbol myristate acetate. These results indicate that E-5110 is a potent dual inhibitor that suppresses superoxide generation.

Animals↗
PubMed1987

Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.

A series of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones was synthesized and evaluated as candidate antiinflammatory/analgesic agents as well as dual inhibitors of prostaglandin and leukotriene synthesis. Some compounds that showed dual inhibitory activity were found to possess equipotent antiinflammatory activities to indomethacin, with reduced ulcerogenic effects. One of the compounds, N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-o ne, was found to have a wider safety margin than indomethacin or piroxicam, and was selected for detailed evaluation as a candidate drug for clinical application.

Animals↗
PubMed1987

Identification of Warthin's tumor with technetium-99m pertechnetate.

Salivary gland imaging with Tc-99m pertechnetate is a useful procedure for evaluating the functional status of salivary glands. The only neoplasms of salivary glands known to consistently concentrate Tc-99m pertechnetate are Warthin's tumor and oncocytoma. In the five cases presented, increased concentration of Tc-99m pertechnetate was seen in these tumors of the parotid glands. This finding was useful for preoperative identification of Warthin's tumor. During this investigation, the concentration of Tc-99m pertechnetate in Warthin's tumor varied by histologic type. Thus, a dynamic study may be helpful in evaluating the accumulation rate of Tc-99m pertechnetate into this tumor type. Because the retention of Tc-99m pertechnetate in tumor following stimulation is useful for the diagnosis of Warthin's tumor, a washout image is of importance in establishing this diagnosis.

Adenolymphoma↗
PubMed1987

[The difference between the mechanism of 67Ga accumulation and 59Fe accumulation in cultured tumor cells].

It is well known that the mechanism of 67Ga accumulation into tumor cells is mediated with transferrin receptor as well as iron. The present study was designed to explore the difference between the mechanism of gallium accumulation and that of iron by using mouse leukemic cell line L5178Y. When monensin which inhibits the recycle of transferrin receptor was added to the incubated system, accumulation of 59Fe and 67Ga was clearly diminished compared with that of control. However, inhibition of 59Fe accumulation was more remarkable than that of 67Ga. Furthermore, monensin has a action of Na+ ionophore which decreases Na+ gradient between the inside and the outside of the plasma membrane. Following administration of monensin, 67Ga accumulation was diminished according to the loss of the Na+ gradient. On the other hand, following administration of valinomycin, 67Ga accumulation was not affected by the loss of the K+ gradient. From these results, it was suggested that the mechanism of 67Ga accumulation into tumor cells differed from that of 59Fe and transferrin receptor and Na+ gradient of tumor cells played an important role on 67Ga accumulation into tumor cells.

Animals↗
PubMed1987

Effect of the novel non-steroidal antiinflammatory agent N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-one on in vitro generation of some inflammatory mediators.

A newly synthesized compound, the non-steroidal antiinflammatory agent N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-o ne (E-5110) was investigated. E-5110 inhibited prostaglandin E2 (PGE2) generation by cultured rat synovial cells upon stimulation with interleukin-1-like factor of rat polymorphonuclear leucocytes (PMN). The IC50 values (mumol/l) for PGE2 generation were 0.026 for E-5110, 0.008 for indometacin, 0.112 for piroxicam and 0.667 for the compound B (3-amino-1-(M-trifluoromethyl-phenyl-2-pyrazoline). Calcium ionophore A23187-stimulated leukotriene B4 generation by human PMN was inhibited by E-5110 with an IC50 value of 0.20 mumol/l; E-5110 was as inhibitory as nordihydroguaiaretic acid and was more potent than the compound B (IC50 of 2.58 mumol/l). E-5110 suppressed superoxide generation by human PMN stimulated with opsonized zymosan, f-Met-Leu-Phe and phorbol myristate acetate. E-5110 also inhibited the generation of leucocytic pyrogen and leucocyte factor(s) which stimulated collagenase production by cultured synovial cells.

Animals↗
PubMed1987

[A new method of vascular anastomosis by CO2 laser: experimental and clinical study].

It is difficult to maintain the long-term patency after conventional anastomosis especially for the small caliber vessels. Since 15 years we have performed aortocoronary bypass with suture materials for the patients with ischemic heart disease. There are some problems in maintaining the long-term patency of the bypass grafts. Low energy CO2 laser was utilized to make vascular anastomosis with a few stay sutures. Vascular anastomoses (side-to-side, end-to-end, end-to-side) were carefully made by CO2 laser in the regions of the femoral arteries and veins, the carotid arteries and jugular veins in dog. A-C bypass was also successfully carried out between the internal mammary artery and the left anterior descending artery under the beating heart in experiment. Outputs of 20-40 mW and irradiation times of 6-12 sec/mm were optimal conditions for anastomosis of the small caliber vessels. There were no problems in the intensity and the healing of the anastomotic sites in comparison with the conventional suture method. On the basis of these excellent experimental results a low energy CO2 laser was employed clinically for vascular anastomosis of the peripheral vessels in 28 patients with angina pectoris or chronic renal failure and cardiac failure. There were no complications such as bleeding and suture line aneurysm after surgery. In conclusion, vascular anastomosis by laser might be recommended in performing with safety and rapidity for small caliber vessels.

Adult↗
PubMed1987

Pharmacological properties of the novel non-steroidal antiinflammatory agent N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2 -one.

The antiinflammatory activity of the novel pyrrolidin-2-one derivative N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-o ne (E-5110) was investigated and compared with those of indomethacin and piroxicam in various antiinflammatory, analgesic and antipyretic animal models. The acute antiinflammatory activity of E-5110 on the carrageenin paw edema was similar to that of indomethacin, and half that of piroxicam. The chronic inflammatory responses in established adjuvant- and type II collagen-induced arthritis, which are widely used models of rheumatoid arthritis, were suppressed as effectively by E-5110 as by indomethacin and piroxicam. E-5110 decreased the pleural exudate volume and inhibited leucocyte infiltration in a reversed passive Arthus reaction more potently than indomethacin, suggesting that mediators other than prostaglandin E2 may play an important role in this inflammatory process. The analgesic potency of E-5110 against inflammatory pain was similar to that of indomethacin or piroxicam, but the antipyretic activity of E-5110 was more potent than that of the reference drugs. The ulcerogenic effect of E-5110 on rat gastric mucosa was less than those of indomethacin and piroxicam. In conclusion, E-5110 is a very potent antiinflammatory compound acting against various types of inflammation, and has a favorable therapeutic index.

Animals↗
PubMed1986

Prognostic factors in giant cell tumor of bone. A modified histological grading system useful as a guide to prognosis.

An analysis of 26 patients with giant cell tumor of bone was carried out to determine the clinical and pathological factors affecting the prognosis of the tumor, with a follow-up program of more than 3 years. The physical characteristics of the pathological features were measured objectively using an image analyzer. A significant correlation between the therapeutic procedures and recurrence of the tumor was found, but no pathological variables were significantly correlated. Excision or resection en bloc should be performed for the initial treatment of the tumor. Local recurrence could not be predicted on the basis of histological grading. Stromal cell atypia was significantly correlated with metastasis, but multinucleated giant cells bore no correlation to either recurrence or metastasis. The use of a modified histological grading system based not on variations of the stroma and giant cells but only on the atypia of mononuclear stromal cells, either malignant or classical, is recommended for the clinical assessment of the tumor.

Adolescent↗
PubMed1985

A study on the osseous elements in malignant fibrous histiocytoma of bone.

By studying histochemically and ultrastructurally a case of malignant fibrous histiocytoma (MFH) of bone with neoplastic osteoid elements, the distinction of the tumor from osteosarcoma was discussed. MFH was likely to originate from undifferentiated mesenchymal cells that induced a histiocytic line of differentiation, and some histiocytes seemed to be transformed into well differentiated fibroblastic cells which accordingly differentiated into fibroblasts and osteoblasts. This may explain the existence of the osseous elements in MFH. Sarcoma showing the bimodal--histiocytic and fibroblastic--differentiation should be diagnosed as malignant fibrous histiocytoma, even if it contains tumorous osteoid; it must be clearly distinguished from osteosarcoma, in which the various cells only on a fibroblastic line of differentiation can be identified and the osteoblasts are the predominant cells.

Acid Phosphatase↗