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Volume 39, Issue 12
Displaying 51-64 of 64 articles from this issue
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Yoshiro OHMOMO, Masahiko HIRATA, Katsuhiko MURAKAMI, Yasuhiro MAGATA, ...1991 Volume 39 Issue 12 Pages 3343-3345
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new radioiodinated monoamine oxidase A (MAO-A) specific inhibitor, [125I]iodoclorgyline, was synthesized from its tin precursor by iododestannylation reaction using sodium [125I]iodide and hydrogen peroxide with high yield and site specificity. The product possessed a high radiochemical purity as well as high specific activity. The method can be readily applicable for labeling with 123I, a very suitable radioisotope for in vivo imaging with single photon emission computer tomography (SPECT). Biodistribution studies of the [125I]iodoclorgyline in mice showed high initial uptake in the brain, and brain radioactivity reached a constant level at 60 min after intravenous injection. The results suggested that [125I]iodoclorgyline might have potential as a radiopharmaceutical for MAO-A studies in the brain with SPECT.View full abstractDownload PDF (639K) -
Satoshi TERASHIMA, Mineo SHIMIZU, Syunji HORIE, Naokata MORITA1991 Volume 39 Issue 12 Pages 3346-3347
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe hot water extracts of Chrysanthemum morifolium, Bixa orellana and Ipomoea batatas, were found to have potent inhibitory activity towards lens aldose reductase (AR). Ellagic acid (4) was isolated from C. morifolium and I. batatas, isoscutellarein (7) from B. orellana and 3, 5-dicaffeoylquinic acid (10) from I. batatas, respectively, as potent inhibitors.View full abstractDownload PDF (505K) -
Masaru KOBAYASHI, Keisuke ISHIDA, Susumu TERABAYASHI, Hiroshi MITSUHAS ...1991 Volume 39 Issue 12 Pages 3348-3349
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe leaves of Cupressus funebris (Cupressaceae) were shown to contain four chlorophyll-derived pigments (2-5a), together with a new natural norlabdane-type diterpene 1a. Compounds 1a and 5a were isolated as methyl esters 1b and 5b. The pigments were identified as pheophytin a (2), 10S- and 10R-hydroxypheophytin a (3 and 4), and methyl pheophorbide a (5b), from spectroscopic analyses.View full abstractDownload PDF (511K) -
Yasuo ODA, Yoshiyuki TATSUMI, Shigeru AONUMA1991 Volume 39 Issue 12 Pages 3350-3352
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTulipa gesneriana lectin-erythrocyte (TGL-E) which agglutinates mouse erythrocytes showed a potent mitogenic activity on mouse spleen cells and human peripheral blood lymphocytes, however, TGL-E had only slight mitogenic activity on mouse thymus cells. Its subunit α with a molecular weight (MW) of about 26000 showed a potent mitogenic activity as did that of native lectin, but subunit β with a MW of about 14000 showed no activity, indicating that the mitogenic activity of TGL-E originates from subunit α. TGL-E stimulated T cell enriched spleen cells which passed through a nylon column, but not spleen cells from a nude mouse or spleen cells treated with anti-Thy 1·2 antibody and complement. Thus, TGL-E stimulates only mouse T cells but not B cells. the other lectin in tulip bulbs, Tulipa gesneriana lectin-yeast showed no mitogenic activity on mouse spleen, thymus cells or human paripheral blood lymphocytes.View full abstractDownload PDF (468K) -
Yoshihiko INAMORI, Masafumi OGAWA, Hiroshi TSUJIBO, Kimiye BABA, Mitsu ...1991 Volume 39 Issue 12 Pages 3353-3354
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3, 3', 4, 5'-Tetrahydroxystilbene (I) and 3, 3', 4, 5'-tetrahydroxybibenzyl (II), isolated from the heartwood of Cassia garrettiana CRAIB (Leguminosae), showed inhibitory effects on antigen-induced histamine release from rat peritoneal mast cells in vitro. The inhibitory effect of I (IC50=30.2 μM) was much stronger than that of II (>100 μM). Compound II, as well as I (IC50=7.3 μM) reported previously, also inhibited the histamine release from human peripheral basophils induced by anti-immunoglobulin E (IgE) in vitro, and its IC50-value was 68.0 μM. These results suggest that the trans-olefin structure in the molecule may be necessary for I to have an inhibitory effect on histamine release. Considering that disodium cromoglycate did not show any significant inhibitory effect on anti-IgE-induced histamine release from human basophils, the strong inhibitory effects of I in both tests are of considerable interest.View full abstractDownload PDF (457K) -
Yorinobu YONEZAWA, kenji SHIRAKURA, Akinobu OTSUKA, Hisakazu SUNADA1991 Volume 39 Issue 12 Pages 3355-3358
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs equation was derived for the dissolution from the whole surface of a nondisintegrating single component tablet under a nonsink condition where the initial weight of a tablet is equal to the weight needed to saturate the solution. also, equations for several dissolution manners of the tablet under the nonsink condition were derived in the postulation of a dominant dissolution rate constant which determines the dissolution manner. The aplicability of these equations was examined by dissolution measurements with nondisintegrating single component tablets. Dissolution measurements of tablets prepared using the amount required to saturate the solution were conducted by masking their flat or side surface with adhesive tape in accordance with the conditions for the derivation of equations. These dissolution behaviors were treated by the use of derived equations to confirm the validity.Among the derived equations, dissolution from the whole surface of a tablet was expressed in the same form as the negative two-thirds law equation for particles, and a nondisintegrating single component tablet compressed by the use of stuitable amount was thought to behave like a single crystal. Also, equations, i.e., the negative two-thirds law and the negative square root law, thus derived were thought to be applicable for the dissolution of a nonspherical particle and crystal concerning the crystal's habit and its dissolution property.View full abstractDownload PDF (572K) -
Kazuhiko ARIMORI, Yoshiko HASHIMOTO, Masahiro NAKANO1991 Volume 39 Issue 12 Pages 3359-3361
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTransfer of aprindine from the blood into the intestinal lumen or into the peritoneal cavity was examined after intravenous administration of the drug at a dose of 5 mg/kg in rats. The amount of the drug transferred from the blood into the intestinal lumen was much greater than into the peritoneal cavity. The average amounts of aprindine transported into the intestinal lumen and the peritoneal cavity were 0.12 and 0.03% of the dose (5 mg/kg) in 120 min, respectively. Thus, a notable difference in the clearance values of the drug was obtained between the intestinal lumen (14.8 ml/h) and the peritoneal cavity (4.94 ml/h). The net water flux showed that secretion predominated in the peritoneal transport while absorption overbalanced secretion in the intestinal transport. It seems likely that a solvent drag effect by water movement did not contribute much to the transport of aprindine from the blood to the intestinal lumen or the peritoneal cavity. The differences in transport across the two membranes could be due to differences in the surface area and other geometrical factors. Differences could also be due to a difference in the pharmacologic effects of the drug which causes a decrease in tissue splanchnic perfusion.View full abstractDownload PDF (560K) -
Hirofumi TAKEUCHI, Hideto SASAKI, Toshiyuki NIWA, Tomoaki HINO, Yoshia ...1991 Volume 39 Issue 12 Pages 3362-3364
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe absorption characteristics of vitamin E acetate (VEA) formulated into a dry emulsion system after its oral administration to beagle dogs were determined and compared to those of two different dosage forms (an oily mixture of the drug with cottonseed oil and an oil (drug)-in-water emulsion). The three dosage forms were administered in a crossover fashion to six nonfasting subjects, and the drug absorption was assessed from the plasma concentration of the major metabolite (free vitamin E). VEA formulated in the dry emulsion was rapidly absorbed, which suggested that a considerable amount was released as reformed emulsion droplets in the gastrointestinal tract as well as in water in vitro. Based on the analysis of variance, no significant differences in bioavailability parameters (AUC, Cmax or Tmax) were observed among the three dosage forms.View full abstractDownload PDF (476K) -
Masayoshi YAMAGUCHI, Noriaki SHIMOKAWA, Takeshi HOSHI1991 Volume 39 Issue 12 Pages 3365-3367
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe preventive effect of calcium hydroxide on the disorder of bone metabolism caused by skeletal unloading was investigated. Skeletal unloading was designed using the model of hindlimb hang in rats. Skeletal unloading for 7d caused a significant decrease of inorganic phosphorus concentration in the serum and of alkaline phosphatase activity and deoxyribonucleic acid (DNA) content in the femoral diaphysis of rats. Oral administration of calcium hydroxide (16 and 24 mg Ca/kg) caused a significant increase in serum inorganic phosphorus concentration and femoral-diaphyseal calcium content and alkaline phosphatase activity of rats with skeletal unloading. Bone DNA content was significantly increased by the dose of 24 mg Ca/kg. These results clearly indicate that skeletal unloading-induced disorder of bone metabolism is partly prevented by oral administration of calcium hydroxide. Calcium ingestion may be useful as a therapeutic tool in the disorder of bone metabolism caused by skeletal unloading.View full abstractDownload PDF (591K) -
Toshiyuki KAJI, Chika YAMAMOTO, Michiko SAKAMOTO1991 Volume 39 Issue 12 Pages 3368-3369
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSConfluent cultures of vascular endothelial cells derived from the human umbilical vein were incubated in a serum-free medium in the presence of low molecular weight heparin (LMWH) with molecular weights of 4000-6000 dalton (Da), or of unfractionated heparin (UFH) with average molecular weight 12000 Da, and prostacyclin production was determined by radioimmunoassay for 6-keto-prostaglandin F1 α, the state metabolite of prostacyclin. LMWH at 1 U/ml as anti-factor Xa activity significantly increased prostacyclin production after 6 h or longer; however, UFH at 1 USP U/ml did not induce such a significant change. The LMWH-induced increase in prostacyclin production occurred at 0.1 U/ml and above after 6 h of treatment. Since prostacyclin is both a potent inhibitor of platelet aggregation and a vasodilator, it was suggested that the increased endothelial cell prostacyclin production induced by LMWH may be a component of the anticoagulant activity of the drugView full abstractDownload PDF (429K) -
Tsuguo IKEBE, Shu MURAKAMI, Shuzo TAKEHARA, Masamitsu SAKAMORI1991 Volume 39 Issue 12 Pages 3370-3372
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of N-(2-pyrrolidinylmethyl)-2-methoxy-5-sulfamoylbenzamide derivatives bearing a long alkyl chain at the 1-position of the pyrrolidine ring was synthesized and found to possess high affinities for serotonin 5-HT1A receptors.View full abstractDownload PDF (436K) -
Koichi KAWASAKI, Machiko NAMIKAWA, Yuko YAMASHIRO, Takao HAMA, Tadanor ...1991 Volume 39 Issue 12 Pages 3373-3375
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHybrids of a fibronectin-related tripeptide (Arg-Gly-Asp) and amino-poly(ethylene glycol) were prepared and their inhibitory effect on experimental metastasis in mice was examined. The hybrids exhibited a potent inhibitory effect on the metastasis of B16 melanoma BL6.View full abstractDownload PDF (395K) -
Fumio IKEGAMI, Satoshi ITAKAGI, Tsutomu ISHIKAWA, Godelieve ONGENA, Yu ...1991 Volume 39 Issue 12 Pages 3376-3377
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSβ-(Isoxazolin-5-on-2-yl)alanine (BlA), a biosynthetic precursor of the neurotoxic amino acid β-N-oxalyl-L-α, β-diaminopropionic acid (ODAP), was confirmed to be derived from O-acetyl-L-serine (OAS) and isoxazolin-5-one by cysteine synthase in higher plants. Some properties of this enzyme in the biosynthesis of BlA are described.View full abstractDownload PDF (396K) -
Yasuhiro KOHAMA, Norihito MURAYAMA, Keishi TANAKA, Akira INADA, Tsutom ...1991 Volume 39 Issue 12 Pages 3378-3380
Published: December 25, 1991
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel immunosuppressant, Fr.5-B, has been isolated from the debris of Bacillus stearothermophilus UK563 autolysate. Fr.5-B suppressed mouse mixed leukocyte reaction at doses ranging from 10-4 to 1 μg/ml, but not proliferation stimulated by concanavalin A and lipopolysaccharide.View full abstractDownload PDF (422K)