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Osamu TAKEDA, Seiji TANAKA, Kazuo YAMASAKI, Hiroshi KOHDA, Yuzuru IWAN ...
1989 Volume 37 Issue 4 Pages
1090-1091
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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Thirty-four extracts of crude drugs and medicinal plants have been screened for activity against Oncomelania nosophora, the intermediate host of the Japanese strain of Schistosoma japonicum. Strong molluscicidal activity was found in the MeOH extract of Anemarrhenae Rhizoma. Although timosaponin A-III, one of the main saponins of Anemarrhenae Rhizoma, showed very strong killing activity, markogenin-3-O-β-D-glucopyranosyl (1-2)-O-β-D-galactopyranoside having the same glycosidic linkage was found to be inactive.
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Koichi MACHIDA, Keisuke OSAWA
1989 Volume 37 Issue 4 Pages
1092-1094
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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From the peels of Citrus hassaku HORT. ex TANAKA (Rutaceae), eight flavonoid aglycones were isolated and characterized as 4', 5, 6, 7, 8-pentamethoxyflavone (I), 3', 4', 5, 6, 7, 8-hexamethoxyflavone (II), 3, 3', 4', 5, 6, 7, 8-heptamethoxyflavone (III), 3', 4', 5, 6, 7-pentamethoxyflavone (IV), 4', 5, 7-trimethoxyflavone (V), 3, 3', 4, ', 5, 7, 8-hexamethoxyflavone (VI), 4', 5, 7, 8-tetramethoxyflavone (VII) and 3', 4', 5, 7, 8-pentamethoxyflavone (VIII), based on spectral and chemical data.
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Kenji SHIMADA, Masaharu NAKAJIMA, Hiroyuki WAKABAYASHI, Susumu YAMATO
1989 Volume 37 Issue 4 Pages
1095-1096
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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A rapid and simple flow injection analysis for the determination of germanium (Ge) is described. Ge is reacted with phenylfluorone in a mixing coil (0.5 mm i.d.×300 cm) at 40°C, and the developed color is measured at 508 nm. The calibration graph is linear over the concentration range of 0.04-10 μg ml
-1 (2-500 ng). Interference by various foreign substances, amino acids and vitamins, was investigated. Satisfactory results were obtained by the proposed method. The method was applied to a commercially available Ge-containing health beverage.
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Hideo KUREBAYASHI, Masamichi FUKUOKA, Akira TANAKA
1989 Volume 37 Issue 4 Pages
1097-1099
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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In order to investigate the isotope effect on the microsomal oxidative deamination of cyclohexylamine, α-deuterium(D)-labelled cyclohexylamine was synthesized. The deuterium labelling was found exclusively at the α-position with a purity of greater than 99 atom percent. Metabolic studies in vitro indicate that a significant deuterium isotope effect operates in the oxidative deamination of α-D-labelled cyclohexylamine. On incubation with rabbit liver microsomes in the presence of reduced nicotinamide adenine dinucleotide phosphate (NADPH) and oxygen, the ratio of apparent deamination rate constants (k
H/k
D) was 2.0±0.2 (mean±S.D.).
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Toshiyuki FUJIOKA, Fumiko INOUE, Masayuki KURIYAMA
1989 Volume 37 Issue 4 Pages
1100-1102
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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Two new affinity resins for the purification of opioid-binding materials were prepared. On was AH-Sepharose coupled with [D-Ala
2, D-Leu
5]enkephalin and the other was AF-Amino Toyopearl with [D-Ala
2, Leu
5]enkephalin. Solubilized-opioid receptors from rat brain were treated with these affinity resins and the materials with opioid-binding activities were purified. On sodium dodecyl sulfate (SDS)-polycrylamide gel electrophoresis, the purified materials showed one major band with a molecular weight of 62000-64000. The results suggested that the prepared resins are useful tools for the purification of opioid receptors.
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Satoshi KOIKEDA, Masahiro TAMARU, Masuo GOTO, Nozomu MORI, Shinji TAKA ...
1989 Volume 37 Issue 4 Pages
1103-1105
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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The effect of a change in the concentration of c-myc protein on the expression of genes for two phosphoglycerate kinase isozymes was investigated. The steady state levels of messenger ribonucleic acids (mRNAs) for sperm-type and non-sperm-type proteins were determined by blot hybridization using the RNA of the mouse cell line 38-2 containing the inducible rat c-myc gene cultured under various conditions. Without inducing the c-myc gene, mRNA for non-sperm-type protein was detected at a level that remained essentially constant during both activation and inactivation of the c-myc gene. mRNA for sperm-type protein was not detected in 38-2 cells cultured under any conditions used. Change in the amount of c-myc protein alone does not appear to bring about a switch of the expression of the two phosphoglycerate kinase genes during spermatogenesis in mouse testis.
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Gaetano GIAMMONA, Libero Italo GIANNOLA, Bianca CARLISI
1989 Volume 37 Issue 4 Pages
1106-1108
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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Coupling of isoniazid with polysuccinimide afforded a water-insoluble polymeric pro-drug; by reaction with ethanolamine it was chemically transformed in a water-soluble adduct. The in vitro release of isoniazid from the drug-polymer adduct was studied by using an artificial stomach wall lipid membrane. The transfer rate constant from simulated gastric juice to simulated plasma was defined and compared with that of an equivalent dose of pure drug.
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Katsuhiko OKUMURA, Hisahiro YOSHIDA, Akira KAMIYA, Ryohei HORI
1989 Volume 37 Issue 4 Pages
1109-1111
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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To clarify the mechanism by which basic drugs accumulate in the lung mitochondria, the binding selectivity of drugs to different submitochondrial components of the perfused rat lung was examined. The accumulation of basic drugs was the highest in the mitochondrial outer membrane fraction. The drug accumulation in this fraction increased with lipid solubility and was dose-dependent. It appears then that selective binding sites for basic drugs are present in the mitochondrial outer membrane.
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Toshio NISHIYAMA, Takao HAMA
1989 Volume 37 Issue 4 Pages
1112-1113
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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Drug effects are described in terms of fuzzy sets; practical application to simple cases gave reasonable results.
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Fusao KAIHO, Reiko KOIKE, Hideaki NOMURA, Hiromi HARA, Kimiko MARUOKA, ...
1989 Volume 37 Issue 4 Pages
1114-1116
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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The enhancing effect of cetyl lactate (CL) on the percutaneous absorption of indomethacin (ID) from test solutions in propylene glycol (PG) was investigated by using the abdominal skin of rats in vivo.The percutaneous absorption rate of ID from 1 or 3% CL-PG test solution through the intact skin of rats was observed to be faster than that from the control solution (without CL). The bioavailability of ID was about 0.04% for the control solution, 2.2% for 1% CL-PG and 6.8% for 3% CL-PG test solutions. These results suggest that CL functions as an enhancer for the percutaneous absorption of ID. Furthermore, marked enhancing effects on percutaneous absorption of ID were obtained at a concentration greater than 1% CL in PG.In order to elucidate the mode of action of CL as an absorption enhancer, the percutaneous absorption of ID from the control solution and 3% CL-PG test solution through damaged skin from which the stratum corneum had been stripped was additionally investigated. It was confirmed that CL acts on the stratum corneum to produce its effect.
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Sakae AMAGAYA, Kazumichi HARADA, Akira MIYAKE, Hiroko IWAMA, Yukio OGI ...
1989 Volume 37 Issue 4 Pages
1117-1119
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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The direct addition of levamisole to murine splenic lymphocytes had no effect on the mitogenic activity of lipopolysaccharide. However, the addition of serum of mice orally treated with levamisole increased the mitogenic activity, and this increased activity using serum was similar to the result obtained in an in vivo experiment. These results suggest that the new in vitro experimental method using serum may be able to reproduce the in vivo effect of drugs.
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Kiyoshi TOMIOKA, Mitsuru SHINDO, Kenji KOGA
1989 Volume 37 Issue 4 Pages
1120-1122
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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By the mediation of a chiral amino ether (4), the asymmetric α-benzylation of cyclohexanone (1) was effected via an achiral lithioenamine (6) to give α-benzylcyclohexanone (3) in up to 52% ee. A dramatic leaving-group effect of electrophiles on enantioselectivity was also observed.
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Tsutomu MASUJIMA, Yumi MUNEKANE, Juing-Yi LEE, Yukio SATO, Hisanobu YO ...
1989 Volume 37 Issue 4 Pages
1123-1125
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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Computerized laser photoacoustic microscopy was developed and applied to the immuno-selective imaging of the microdistribution of a biological component. Human lambda-type light-chain was chosen as a model target protein and its peroxidase conjugated antibody was used for selective binding to the target protein and its staining. Using a microscopic calibration curve which was obtained from the images of homogeneously dispersed standard samples, the total quantities of randomly dispersed artificial standard samples were estimated to evaluate the reliability of this method. Finally, the method was applied to a tissue section sample, a human fetal pacrease section, to get the local and total quantitative images of the lambda-type light-chain.
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Hiroyuki SETOI, Hiroshi KAYAKIRI, Masashi HASHIMOTO
1989 Volume 37 Issue 4 Pages
1126-1127
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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A practical synthesis of FR900490 (1__-), a peptidyl immunomodulator of microbial origin, has been achieved through diastereoselective preparation of α, β-diaminobutyric acid 2__-.
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Motomichi KONO, Yutaka SAITOH, Masaji KASAI, Akira SATO, Kunikatsu SHI ...
1989 Volume 37 Issue 4 Pages
1128-1130
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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Introducing the mercaptoethyl group at the 7-N position of mitomycin C 1 has led to the isolation of 7-N, 7'-N'-dithiodiethylenedimitomycin C 2. The compound 2 showed excellent antitumor activity against sarcoma 180 (sc-ip) and leukemia P388 (ip-ip) in mice. As an extension of this study, we synthesized mitomycin dimers with symmetrical disulfide and mitomycin derivatives with unsymmetrical disulfide at the 7-N side chain. Among these compounds, the water soluble conjugate 3 with ethyl γ-L-glyuamyl-L-cysteinylglycinate was far more effective against sarcoma 180 and leukemia P388 than 1. During the subsequent stage of inquiry for the potent congeners of 3, the compound 4 (water solubility : >500 mg/ml), designated as KW2149, with the γ-L-glutamylcystamino group at the 7th position was finally selected for further evaluation.
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Isao KITAGAWA, Nam In BAEK, Kazuyoshi OHASHI, Masahiro SAKAGAMI, Masay ...
1989 Volume 37 Issue 4 Pages
1131-1133
Published: April 25, 1989
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Four new ionophoric resin-glycosides have been isolated from the tuber of Merremia mammosa (Convolvulaceae), an Indonesian folk medicine ("Bidara upas"). The structures of two major resin-glycosides, named mammosides B (1__∼) and H1 (2__∼), have been determined on the basis of chemical and physicochemical evidence including a synthesis of the glycosidic acid designated as mammoside I (3__∼).
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Tsunehiro KITAGAWA, Hideaki TANIMORI, Yohko KOHNO, Akira AKAHORI, Shin ...
1989 Volume 37 Issue 4 Pages
1134-1136
Published: April 25, 1989
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Antiserum specific to Pinellia tuber was elicited in a rabbit. The extract of the tuber was converted to solid-phase antigen using microtiter plates. A new method for enzyme immunoassay of the tuber extract was developed with an antiserum to the tuber and a solid-phase antigen as immunological reagents, and β-D-galactosidase-labeled anti-rabbit IgG as the tracer. The method was successfully applied to the quantitative analysis of the extracts of Pinellia tuber contained in various chinese tradiational medicines. The specificity of the assay to the extracts was also demonstrated.
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Atsuko ITOH, Takao TANAHASHI, Naotaka NAGAKURA
1989 Volume 37 Issue 4 Pages
1137-1139
Published: April 25, 1989
Released on J-STAGE: March 31, 2008
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Two new monoterpene glucosides with unusually 7, 8-disubstituted tetrahydroisoquinoline nucleus, neoipecoside and 7-methylneoipecoside, have been isolated from Cephaelis ipecacuanha A. Richard. Their structures were elucidated as 1 and 2 by spectroscopic and chemical means.
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Kazuo MASUDA, Kenji SHIOJIMA, Hiroyuki AGETA
1989 Volume 37 Issue 4 Pages
1140-1142
Published: April 25, 1989
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From the fresh whole plants of Lemmaphyllum microphyllum var. obovatum (Polypodiaceae), we isolated two new oily tricyclic triterpenoid hydrocarbons, 13βH-malabraicatriene (1) and 13αH-malabaricatriene (2), having the malabaricane skeleton. Their structures were established by physicochemical methods. This is first example of the isolation of tricyclic triterpenoid hydrocarbons from a natural source.
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