Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Volume 35, Issue 4
Displaying 1-50 of 55 articles from this issue
  • KIYOKO TAKAMURA, KUNIO ITO, FUMIYO KUSU
    1987 Volume 35 Issue 4 Pages 1327-1333
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    The adsorption of catecholamines including norepinephrine, epinephrine, isoproterenol, dopamine, dopa and homocatechol on a gold electrode surface was studied in phosphate buffer of pH 6.9 by specular reflection measurement. Norepinephrine is oxidized at potentials more positive than +0.1 V vs. saturated calomel electrode (SCE) and adsorbed at the potential range from-0.7 to-0.05 V. Its antagonists, phenoxybenzamine, tolazoline, ergotamine, oxprenolol and propranolol, are also adsorbed on the electrode, more strongly than norepinephrine. The adsorption behavior of catecholamines on the electrode surface may reflect electrostatic interactions between adrenergic transmitter substances and their receptors.
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  • TSUTOMU KAMIYAMA, SABURO ENOMOTO, MASAMI INOUE
    1987 Volume 35 Issue 4 Pages 1334-1338
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The mechanism of the hydroalkylation of benzene and methylbenzenes to cyclohexylbenzenes was studied in the presence of a palladium-fused salt (NaCl-AlCl3) catalyst under hydrogen pressure. The activities of the hydrogenation catalyst and the alkylation catalyst were each estimated kinetically. The activity of the fused salt was compared with that of anhydrous aluminum chloride for the alkylation of aromatic compounds. The rate constants and Arrhenius parameters of the hydrogenation on palladium and the alkylation on the fused salt supported the presence of the cyclohexyl cation as an intermediate species in the hydroalkylation.
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  • TOMOMI KAWASAKI, HIROAKI OHTSUKA, CHUN-SHENG CHIEN, MITSUGU OMATA, MAS ...
    1987 Volume 35 Issue 4 Pages 1339-1346
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The spectral (proton and carbon-13 nuclear magnetic resonance) and chemical properties of the 1-acetyl-2-hydroxyindolines 1-5, which can exist in the ring (A) and chain (B) tautomers, have been investigated. The methylation and acetylation of the 2-hydroxy-3-indolinones 1-3 gave the ring tautomeric methyl ether and acetyl esters of 1-3, while the reaction with ο-phenylenediamine (9) gave the quinoxalines 10 and 11 as the chain tautomeric products. The reactions of 1-3 with the phosphonium ylide 12 gave the 2-methoxycarbonylmethyl-3-indolinones 14 (R = Ph) and 16 (R = Me) and/or the 2-hydroxy-3-methoxycarbonylmethyleneindolines 15 (R =Ph) and 18 (R = H), respectively, depending on the nature of the substituent (R) at the 2-position in 1-3. The acetylation and reaction of the 2, 3-dihydroxyindoline 4 with 12 are also described.
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  • REIJI KOBAYASHI, YUJI SAMEJIMA, SHOICHI NAKAJIMA, KEN-ICHI KAWAI, SHUN ...
    1987 Volume 35 Issue 4 Pages 1347-1352
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Three new compounds designated as cycloaspeptides A (1), B (2), and C (3) were isolated along with ergosterol from the mycelial chloroform extract of Aspergillus sp. NE-45. The structures of cycloaspeptides A. B, and C were established on the basis of chemical and spectroscopic evidence as 1, 2, and 3, respectively. Cycloaspeptides are new cyclic pentapeptides containing an anthranilic acid residue and two N-methyl amino acid residues.
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  • MASAYUKI TANNO, SHOKO SUEYOSHI
    1987 Volume 35 Issue 4 Pages 1353-1359
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The carbon-13 nuclear magnetic resonance spectra of l-aryl-3, 3-dialkyl-l-nitrosoureas and related compounds were measured at about-40°C, and their chemical shifts were assigned. The conformations of the N-nitroso compounds having the l-aryl-l-nitrosoureido group were established through comparisons with N-alkyl-N-nitrosoanilines, and the decomposition mechanism of 1-aryl-3, 3-dialkyl-l-nitrosoureas is discussed on the basis of the results.
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  • MASAYUKI TANNO, SHOKO SUEYOSHI
    1987 Volume 35 Issue 4 Pages 1360-1371
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Nitrosation of 3-alkyl-1-arylureas was investigated with sodium nitrite in 99% formic acid or with isoamyl nitrite in chloroform. The preparation of 3-alkyl-1-aryl-1-nitrosoureas was effectively performed by using isoamyl nitrite in the absence of acids, since the 1-nitrosoureas were isomerized to the 3-nitroso isomers by acids. The carbon-13 nuclear magnetic resonance and infrared spectral properties of the products were examined and their structural features are discussed.
    It was found that 3-alkyl-1-aryl-1-nitrosoureas decomposed to form alkyl isocyanates and 3-alkyl-1- (2-nitroaryl) ureas in carbon tetrachloride. 1, 3-Rearrangement and transnitrosation also took place in this solvent.
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  • CHIHIRO UEDA, MASAHITO NOYAMA, HIDENOBU OHMORI, MASAICHIRO MASUI
    1987 Volume 35 Issue 4 Pages 1372-1377
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The reactivity of phthalimide-N-oxyl radical (2), which is produced by an electrochemical one-electron oxidation of N-hydroxyphthalimide (1), was investigated. The self-decomposition of 2 obeyed second-order kinetics with respect to itself and the rate was little affected by changing the temperature or the concentration of dissolved oxygen, water or added base. In the reaction between 2 and benzhydrol or its α-deuterated derivative, the decay of the radical was first-order with respect to each component. The observed large deuterium isotope effect (kH/kD= 10.6 at 25 °C) is attributed to the rate-limiting hydrogen abstraction. Rate measurements were performed on the reaction with 24 other substrates which have one or more hydrogen atoms on a benzylic or allylic position or on a carbon adjacent to a hetero atom.
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  • SHOETSU KONNO, SETSUYA OHBA, MATAICHI SAGI, HIROSHI YAMANAKA
    1987 Volume 35 Issue 4 Pages 1378-1382
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The addition reactions of various nucleophiles to 6-methyl-3-phenyl-1, 2, 4-triazine (1) were investigated and a practical preparation of 1 was developed. The reactions showed many similarities to those of quinazoline (at the 4-position) and acridine (at the 9-position). The hitherto unknown compounds 5-cyano- (3), 5-carbamoyl- (5) and 5-phenacyl-6-methyl-3-phenyl-1, 2, 4-triazines (11c) were synthesized.
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  • KIYOSHI IKEDA, TOSHIO TAKAHASHI, CHIKAKO SHIMIZU, SHINICHI NAKAMOTO, K ...
    1987 Volume 35 Issue 4 Pages 1383-1387
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    A new methodology for chemical differentiation of one amino and four hydroxyl groups of glucosamine derivatives and its application for the synthesis of lipid X are described.
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  • KAZUNOBU HARANO, HIDEO KIYONAGA, TAKUZO HISANO
    1987 Volume 35 Issue 4 Pages 1388-1396
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    Ο- (1-Cyclopropylethyl) S-methyl dithiocarbonate (Ib) was solvolyzed in various solvents to give S- (1-cyclopropylethyl) S-methyl dithiocarbonate (IIb) quantitatively. The reaction obeyed the first-order rate law and the rates were considerably affected by the polarity of the solvent used. Phenolysis of Ib with p-chlorophenol gave IIb and a small amount of the phenol ether. Plots of the logarithm of the reaction rates against Y values gave a linear relationship. The reaction was found to be markedly accelerated by phenolic solvents. The rate in p-chlorophenol is 509 times faster than that in ethanol. The role of hydrogen-bonding to the thione sulfur in the rearrangement reaction is discussed.
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  • KIYOSHI TANAKA, TEIJI KIMURA, TOMOYA OKADA, XING CHEN, FUMIO YONEDA
    1987 Volume 35 Issue 4 Pages 1397-1404
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Some 1, 5-dihydro-5-deazaflavin (1, 5-dihydropyrimido [4, 5-b] quinoline-2, 4 (3H, 10H) -dione) derivatives possessing chiral substituents at the N-3 position were synthesized. Asymmetric reduction of ethyl benzoylformate in the presence of magnesium perchlorate was carried out with these chiral 1, 5-dihydro-5-deazaflavin derivatives to give ethyl mandelate in moderate optical and chemical yield. The influence of metal additives other than magnesium upon the asymmetric induction and yield of the reduction was investigated, and it was suggested that intermediate ternary complexation is probably involved in the reaction. No improvement of chiral induction was obtained by changing the metal catalyst.
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  • YASUMITSU TAMURA, MANABU SASHO, SHUJI AKAI, HISAKAZU KISHIMOTO, JUN-IC ...
    1987 Volume 35 Issue 4 Pages 1405-1412
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    4-Methoxy and 4-acetoxyhomophthalic anhydrides were prepared by convenient oxidations of homophthalic acid derivatives followed by hydrolysis and dehydrative cyclization. Strong base-induced cycloaddition of these anhydrides to 2-ehloro-6, 6-ethylenedioxy-5, 6, 7, 8-tetrahydro-1, 4-naphthoquinone gave the tetracyclic adducts, which were efficiently converted into 4-demethoxydaunomycinone and daunomycinone.
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  • KUNIO HIROI, HIROYASU SATO, LIH-MING CHEN, KUMIKO KOTSUJI
    1987 Volume 35 Issue 4 Pages 1413-1426
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Introduction of a silyl group at the a-position of allylic sulfides, followed by the aluminum chloride-catalyzed reaction of the resulting α-silylallylic sulfides with acid chlorides resulted in regioselective acylation at the γ-position of the allylic system to give γ-acylated vinylic sulfides, chemically equivalent to 1, 4-dicarbonyl compounds. Heating of the products in refluxing benzene with an equimolar amount of p-toluenesulfonic acid produced 2-cyclopentenone derivatives. Treatment of the acylated products with an equimolar amount of concentrated sulfuric acid gave α-phenylthiofuran derivatives. These procedures provide a novel method for cyclopentannelation and furan annelation.
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  • MASARU KOBAYASHI, MIYUKI FUJITA, HIROSHI MITSUHASHI
    1987 Volume 35 Issue 4 Pages 1427-1433
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    Pregnenolone (1), coniferylferulate (2) and nine mono-and dihydroxyphthalide derivatives (5-13) were isolated from the commercial C. officinale rhizome. Their structures were determined from the spectroscopic data and the dihydroxyphthalides senkyunolide-H (11) and-I (12) and senkyunolide-J (13) were synthesized from the major components ligustilide (14) and senkyunolide-A (16), respectively. These oxygenated phthalides were absent in the fresh C. officinale rhizome and they were shown to be derived from the major volatile phthalides during storage of the crude drug. Coniferylferulate (2) also decomposes partly during storage, giving ferulic acid.
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  • TAKASHI HARAYAMA, KEIKO SAKURAI, KEIKO TANAKA, YUKIYA HASHIMOTO, HIDET ...
    1987 Volume 35 Issue 4 Pages 1434-1442
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    Total synthesis of dl-aspterric acid (1) has been accomplished. Robinson annulation of the keto ester (2) with methyl vinyl ketone, followed by reduction with LiAlH4 and oxidation with MnO2, afforded the enone alcohol (4), which was converted to the hydroxy-ether (6) via three steps (I2-Ag2O, AgOAc, and alkaline hydrolysis). Successive treatment of 6 with tert-butyldimethylsilyl chloride, tert-BuOK-MeI, NaBH4, Ac2O-pyridine and 5% HCl afforded the hydroxy acetate (18). The hydroxy acetate (18) was converted to the hydroxy ketone (20) via catalytic hydrogenation under medium pressure, Jones oxidation, and alkaline hydrolysis. Treatment of 20 with PCl5 gave the norketone (21), which is the degradation product of 1. The dimethylacetal (25) of 20 was treated with Me3SiCN-SnCl2 to give the methoxy cyanides A (26) and B (27). The major methoxy cyanide B (27) was successively treated with KOH, Me3SiCl-NaI, Ac2O, and 5% HCl to give the monoacetate (31), which was finally converted to 1 via ring contraction with PCl5 and alkaline hydrolysis.
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  • SHUICHI MIYAMOTO, MASAFUMI YOSHIMOTO, KOICHI KOJIMA
    1987 Volume 35 Issue 4 Pages 1443-1451
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    A diene analog (2) of isocarbacyclin has been found to be a potent inhibitor of platelet aggregation. A molecular mechanics calculation study on model compounds of both prostacyclin (1) and 2 was undertaken in an attempt to elucidate the stereochemical properties and to find the active conformers. At first the ring structures were investigated, then the directions of the a-chain and finally the entire model compounds were studied. A working hypothesis that four functional groups, consisting of a carboxyl group of the a-chain, a hydroxyl group at position 11, another hydroxyl group of the ω-chain and a π-electron system at the 5, 6 and 6a positions, play an important role in binding with a receptor to elicit activities is presented. Three-dimensional arrangements of these essential functional groups in stable conformations were examined by superimposing the coordinates of the four groups of 2 on those of 1, because these moieties in the receptor-bound conformations should be identically located in both molecules. Three candidates for the active conformers are presented as a basis for a rational approach to the design of prostacyclin agonists.
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  • HIDETOSHI WATANABE, SHUICHI MIYAMOTO, MASAFUMI YOSHIMOTO, TOSHIHARU KA ...
    1987 Volume 35 Issue 4 Pages 1452-1459
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    A quantitative structure-activity relationship formulated for 59 4-anilinopyrimidines inhibiting reserpine-induced ptosis was applied to the design of new, more active, antidepressant compounds. The utility of correlation equations in designing new congeners is discussed and the designed compounds synthesized show the most active group of the anilinopyrimidines.
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  • HIDEJI ITOKAWA, HIROSHI MORITA, KINZO WATANABE
    1987 Volume 35 Issue 4 Pages 1460-1463
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Three novel eudesmane-type sesquiterpenes, 10-epi-5β-hydroperoxy-β-eudesmol (I), 10-epi-5α-hydroperoxy-β-eudesmol (II) and 4, 10-epi-5β-hydroxydihydroeudesmol (III), have been isolated from the rhizomes of Alpinia japonica. Their structures were determined by spectroscopic methods and chemical conversions.
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  • AYA NITTA
    1987 Volume 35 Issue 4 Pages 1464-1478
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Japanese cinnamon on the market was investigated histologically using specimens collected in Japan. Sixteen lots of material were inspected. They were found to be diverse in internal structure with respect to the amount and combination of mechanical tissue in the bark.
    In addition, the difference between the Nikkei root bark and stem bark was clarified. Neither fiber bundles nor a cutinized cell layer was observed in the root bark, which had tangentially elongated cork cells, large oil cells in the primary cortex, and less mechanical tissue than the stem bark. Marketed samples exhibiting a cutinized cell layer probably contain bark from exposed roots or are adulterated with stem bark.
    Botanical specimens of the following Cinnamomum species were also examined histologically : Nikkei, C. sieboldii syn. C. loureirii; Yabu-nikkei, C. insularimontanum syn. C. japonicum; Kusunoki, C. camphora; Maruba-nikkei, C. daphnoides; and Shiba-nikkei, C. daphnoides subsp. Doederleinii. The root bark structures of these species were compared at five growth stages and are described in detail. At maturity, three types of structure could be distinguished. One type is shown by Nikkei and Yabu-nikkei. The second is Kusunoki, which has anatomical features not found in other species. Maruba-nikkei and Shiba-nikkei, which differ noticeably only in the amount of mechanical tissue, exhibit the third type of structure.
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  • SHIGERU ADEGAWA, TOSHIO MIYASE, AKIRA UENO
    1987 Volume 35 Issue 4 Pages 1479-1485
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    Five new guaiane-type sesquiterpene lactones, diaspanolides A (V) and B (VI) and diaspanosides A (VIII), B (IX) and C (X), have been isolated from Diaspananthus uniflorus (SCH. BIP.) KITAM. (Compositae), together with five known compounds, costunolide (I), reynosin (II), dehydrocostuslactone (III), 11, 13α-dihydrozaluzanin C (IV) and glucozaluzanin C (VII). The structures were determined on the basis of spectral data and some chemical transformations.
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  • RYOJI KASAI, TOSHIHIKO OINAKA, CHONG-REN YANG, JUN ZHOU, OSAMU TANAKA
    1987 Volume 35 Issue 4 Pages 1486-1490
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    From the Chinese folk medicine “Liang Wang Cha” (leaves and leafstalks of Nothopanax delavayi, Araliaceae), two new oleanane type triterpene glycosides, named liangwanosides I (1) and II (2), were isolated. The structures of 1 and 2 were determined as the 28-β-D-glucopyranosyl and 28-α-L-rhamnopyranosyl (1→4) -β-D-glucopyranosyl (1→6) -, β-D-glucopyranosyl esters of 3-O-α-L-arabinopyranosyl-3β-hydroxyolean-12-ene-28, 29-dioic acid, respectively.
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  • MAGOHEI YAMADA, YOJI MARUI, CHOZO HAYASHI, SHOJI TAKEMURA
    1987 Volume 35 Issue 4 Pages 1491-1496
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Substituted benzoylthiocholines were synthesized and their application as reagents for clinical measurement of pseudocholinesterase was investigated. Among 21 compounds, 2, 3-dimethoxybenzoylthiocholine (19b) was found to be an excellent substrate for the measurement of the enzyme. The procedure was simple and self-hydrolysis of the substrate at the optimum pH of the enzyme was minimal.
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  • HIROSHI HOSODA, SAKIKO TAMURA, REIKO TSUKAMOTO, NORIHIRO KOBAYASHI, JU ...
    1987 Volume 35 Issue 4 Pages 1497-1502
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    An enzyme immunoassay method using a monoclonal antibody for the determination of 11-deoxycortisol is described. The anti-11-deoxycortisol antibody was produced in ascites by inoculating antibody-secreting hybridoma cells into BALB/c mice. The enzyme labeling of 11-deoxycortisol was carried out by the N-succinimidyl ester method. The activated esters of three carboxylated steroids were treated with β-galactosidase to give enzyme-labeled antigens. A protein A-double antibody method was employed for separation of the bound and free fractions in the immunoassay. It.was found that the monoclonal antibody had a high affinity for a homologous enzyme-labeled antigen prepared from 4- (2-carboxyethylthio) -11-deoxycortisol and the binding was inhibited by the analyte, 11-deoxycortisol. In the heterologous systems using labels prepared from 11-deoxycortisol 3- (O-carboxymethyl) oxime and 11-deoxycortisol 21-hemisuccinate, a lower and no significant immunoreactivities were observed, respectively. These results indicate that the antigen-binding site of the monoclonal antibody is complementary to and covers the 11-deoxycortisol portion remote from the position used for attachment to, the carrier in the preparation of the immunogen. The homologous assay system showed high sensitivity and specificity comparable to those of the radioimmunoassay using tritium as a tracer. These findings should be helpful in the development of various immunoassay systems with the monoclonal antibody.
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  • EIJI SHIMADA, NAOKO KUDOH, MITSUGU TOMIOKA, GO MATSUMURA
    1987 Volume 35 Issue 4 Pages 1503-1508
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    A simple and rapid method has been developed to determine the relative amounts of 4-and 6-sulfate in chondroitin sulfate or proteoglycan preparations. Unsaturated disaccharide products derived from the samples by chondroitinase ABC digestion in 0.01 M Tri-HCl buffer (pH 8.0) were applied to a silica gel-coated thin-layer chromatographic plate and separated in a solvent system of n-propanol-isopropanol-n-butanol-water (55 : 20 : 5 : 20, v/v) containing 0.04M NaCl and 0.01 M ammonia without a desalting step, which was necessary in paper chromatography or thin-layer chromatography on cellulose. The developing time was as short as 2-2.5 h at room temperature. After staining of the separated products with a carbazole reagent followed by immersing the plate in liquid paraffin, the ratio of monosulfated disaccharides, generally found as major components in chondroitin sulfate chains, was estimated by densitometry.
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  • YOSHIHIKO INAMORI, MAYURI KUBO, HIROSHI TSUJIBO
    1987 Volume 35 Issue 4 Pages 1509-1514
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Racemomycin-A (RM-A) showed delayed insecticidal activity against female adults (3d after adult emergence) of Musca domestica and Blattella germanica treated by the topical application method;the LD50 values were 3.76 μg/insect (3 d) and 32.5 μg/insect (7d), respectively. RM-A also showed delayed insecticidal activity against the 3rd instar larva of Culex pipiens pallens and M. domestica treated by the immersion method;the LC50 value for the former was 2.46 ppm (3d), but the insecticidal effect against the latter was weak. RM-A applied by the immersion method also inhibited the adult emergence of C. pipiens pallens and M. domestica, with IC50 values of 1.41 and 199.5 ppm, respectively. Furthermore, RM-A exhibited insecticidal activity against female adults of B. germanica and larvae of Periplaneta fuliginosa treated by the bait method. The insecticidal activity of RM-A on adults of B. germanica was almost equal to that of boric acid bait agent (15%) at the concentration of 2.0%.
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  • SATORU TANI, AKIRA ISHIKAWA, HIROSHI YAMAZAKI, YUHKOH KUDO
    1987 Volume 35 Issue 4 Pages 1515-1522
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Antiserum to the rat pepsinogen (PG) purified by us was raised in the rabbit. We established a radioimmunoassay system for PG and measured the content of it in the digestive and urinary organs. Immunoreactive PG in serum was confirmed to be PG by high-performance liquid chromatography using an ion exchange column. Serum PG levels in pregnant or lactating rats were higher than normal. The maximum level during lactation was 6 or 7 times the normal value, and began to decrease from about the 16th day after delivery. Serum PG in infant rats was elevated along with the content of mucosal PG. In the measurement of serum PG levels in experimental peptic ulcer rats, no significant change was observed in Shay and cysteamine ulcers produced in the forestomach or/and the duodenum. However, serum PG levels rose significantly in rats with indomethacin, stress and ethanol ulcers, which represent injuries on the glandular portion.
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  • HIROAKI NANBA, HISATORA KURODA
    1987 Volume 35 Issue 4 Pages 1523-1530
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    A polysaccharide (6-branched β-1, 3-glucan, As-I) extracted from mycelia of Cochliobolus miyabeanus (Ascomycetes) inhibited the growth of against mouse syngeneic tumors (80% inhibition of MM-46 carcinoma and 30% inhibition of IMC carcinoma) when injected i.p. (0.1 mg/kg/d). As-I enhanced the phagocytosis of syngeneic tumor cells by macrophages about 1.5 times, and the production of superoxide anion about 1.2 times. As-I also activated natural killer cells and increased the activity of killer T cells about 1.3 times.
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  • KIYOSHI KONISHI, HIROKAZU ADACHI, ISAMU HORIKOSHI
    1987 Volume 35 Issue 4 Pages 1531-1537
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Quinones contained in the membrane of Photobacterium phosphoreum grown aerobically were studied. Ubiquinone-8 (Q-8), menaquinone-8 (MK-8), and demethylmenaquinone-8 (DMK-8) were identified by mass spectroscopy. To establish the function of the quinones in the aerobic respiratory chain, depletion and reincorporation experiments were performed. Quinones were removed efficiently by n-pentane-acetone (9 ;1, v/v) extraction. The depleted membrane showed no reduced nicotinamide adenine dinucleotide (NADH) oxidase activity and yet retained NADH dehydrogenase activity and ubiquinol-1 (Q1H2) oxidase activity.
    When Q-8 was reincorporated into quinone-depleted membrane vesicles by a freeze-thaw-sonication method, the NADH oxidase activity was restored completely. However, the other quinones contained in P. phosphoreum (MK-8 and DMK-8) did not have the ability to restore the activity of NADH oxidase. The Q1 H2 oxidase or NADH dehydrogenase activity did not alter with the addition of the three kinds of quinones. These results suggest that Q-8 is a component of the aerobic respiratory chain of P. phosphoreum.
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  • YOSHIYUKI KOIDA, HIDEO TAKAHATA, MASAO KOBAYASHI, MASAYOSHI SAMEJIMA
    1987 Volume 35 Issue 4 Pages 1538-1545
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The dissolution behavior of 4 drugs from ethylcellulose (EC) microcapsules (MC) was examined at various temperatures. From the early dissolution curves, the apparent dissolution rate constants and permeability constants (Pm) were estimated. The permeation across a Millipore filter and an EC cast membrane were also examined for comparison. The values of activation energy of Pm of MC ranged from 4.0 to 7.6 kcal/mol, independently of the drug solubility, and were close to those obtained for permeation through the Millipore filter and EC cast membrane. Pm values of the EC cast membrane (thickness : 10 μm) were small and decreased greatly with increase in the thickness. These results suggested that the drugs were not transported through the polymer phase but through the water channels existing in the MC membrane. Superposition analysis was applied to the dissolution curves measured at various temperatures and it was found that the extent of the superposition was better for less water-soluble drugs. The dependency of drug permeation through MC on wall thickness (from 5 to 20 μm) was examined using isoniazid. Pm values decreased linearly up to about 12 μm and were constant for a thicker wall at all dissolution temperatures. The activation energy of the dissolution rate constants increased with increasing wall thickness. The water.channels were classified into two types, one with fairly large pores or cracks and which was predominant in thinner films, and another with fine and uniformly distributed channels and which was predominant in thicker films.
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  • TERUTAKA TAKAHASHI, YUKO UEZONO, YUTAKA NAKANISHI
    1987 Volume 35 Issue 4 Pages 1546-1554
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    A method for controlling the gastric pH of rabbits to low acidity (pH > 4) by using different antacids was investigated, and the physiological state of rabbits during gastric-acidity control and repeated bioavailability tests was also examined in terms of hemocytological and clinico-biochemical parameters. Neither dried aluminum hydroxide gel (DAH) nor synthetic aluminum silicate (SAS) could elevate the gastric pH to more than 4. In the case of sodium bicarbonate (SBB), the gastric pH increased transiently to around 6 immediately after ingestion of the diet containing SBB and then decreased rapidly to the region of high acidity (pH < 3). On the other hand, magnesium aluminosilicate (MAS) could maintain the gastric pH in the range from 4 to 6 over a period of 3 h after ingestion of the diet containing MAS. Thus, we conclude that MAS is the preferred antacid for maintaining the gastric pH at low acidity over a long period. Analysis of hemocytological and clinico-biochemical data suggested that the physiological state of rabbits is hardly affected by gastric-acidity control and repeated bioavailability tests.
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  • TOSHIHISA YOTSUYANAGI, TSUNEO OHKUBO, TAKAFUMI OHHASHI, KEN IKEDA
    1987 Volume 35 Issue 4 Pages 1555-1563
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Calcium-induced alginate gelation was examined in terms of water content changes. The gelation was accompanied with considerable water loss, which reached about 50-60% (w/w) reduction in the fully-cured state. The calcium association with the polymer was strong enough to maintain the shape of fully-cured beads in distilled water and the amount of the ions associated with the alginate used in the present study was 1.6 × 10 -3mol/g of polymer. The diffusion coefficients of several model compounds having molecular weights ranging from 122 to 1050 were estimated as a function of the polymer concentration in the fully-cured beads.
    The swelling property of dried gel particles prepared from fully-cured hydrogels was of interest : the particles remained unchanged in distilled water or acidic medium (pH 1.5 KCl-HCl) but swelled rather rapidly in pH 7.0 phosphate buffer to a size greater than their original size before being dried. Such a pH-sensitive swelling property could be advantageous for orally-administered drug vehicles, especially when an acid-sensitive drug is incorporated in the gel.
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  • EIHEI FUKUOKA, MIDORI MAKITA, SHIGEO YAMAMURA
    1987 Volume 35 Issue 4 Pages 1564-1570
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The crystallite orientation in intact tablets was investigated by X-ray diffraction methods. XRay diffraction patterns were obtained by the symmetrical-reflection method and the symmetrical-transmission method. Crystallite orientation was evaluated by comparing the diffraction intensities obtained experimentally with those calculated theoretically from the structure factors for the respective planes of the crystal. The (100) planes of aspirin crystallites and the (110) and the (120); (210) planes of salicylic acid crystallites were found to align parallel to the upper surface of the tablet during compression. The crystallite orientation varied with applied pressure for salicylic acid tablet. The flat film technique (pinhole technique) was also used and the results obtained agreed well with those obtained by the diffractometric methods.
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  • SHUU MATSUMOTO, MAKIKO TAKEI, MASAMI MORIYAMA, HIDEYO IMANISHI
    1987 Volume 35 Issue 4 Pages 1571-1578
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The effect of recombinant human interferon (IFN) -gamma (Met-Gln form), having the same amino acid sequence as that of natural human IFN-gamma except for the N-terminal Met residue, on antibody-dependent cellular cytotoxic (ADCC) activity of human peripheral polymorphonuclear leukocytes (PMNs) against anti-chicken red blood cell (CRBC) immunoglobulin G (IgG) -coated CRBC was investigated comparatively with those of natural human IFN-alpha and -beta in vitro. IFN-gamma dramatically induced the ADCC activity at all doses tested when examined at a 1/104 dilution rate of the IgG, while no significant induction was observed with IFN-alpha or-beta. The Fc receptor (FcR) analysis by flow cytometry using fluorescein isothiocyanate-labelled (FITC) -anti-CRBC IgG revealed that IFN-gamma but not IFN-alpha or-beta remarkably increased the number of PMNs bearing FcR. By applying an in vitro measurement system for activated oxygen species using luminol solution, it was demonstrated that activated oxygen species were actually released from PMNs in the ADCC reaction. Further, inhibition experiments using three oxygen scavengers (superoxide dismutase, catalase and dimethyl sulfoxide) demonstrated the involvement of superoxide anion and hydroxy radical as cytolytic mediators in the PMN-ADCC activity induced by IFN-gamma.
    These results indicate a much more potent PMN-activating ability of IFN-gamma than IFN-alpha or-beta and involvement of a mechanism dependent on the enhancement of FcR expression on the PMN surface and the increased release of superoxide anions and hydroxy radicals in the PMN-ADCC augmentation by IFN-gamma.
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  • MIKI SHOJI, MASA-AKI MORI, TADASHI KAWAJIRI, MICHIO SAYAMA, YOSHIHIRO ...
    1987 Volume 35 Issue 4 Pages 1579-1586
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The metabolism of 2, 4-dinitrotoluene (2, 4-DNT), 2, 4-dinitrobenzyl alcohol (2, 4-DNB) and 2, 4-dinitrobenzaldehyde (2, 4-DNAl) in rat liver microsomal and cytosol fractions was investigated. The objectives of these studies were to determine whether 2, 4-DNAI, a potent mutagen, is produced in the oxidation of 2, 4-DNB to 2, 4-DNBA and to clarify the nature of the enzymes responsible for the oxidation of 2, 4-DNT to 2, 4-DNB, 2, 4-DNAl and 2, 4-dinitrobenzoic acid (2, 4-DNBA). Data obtained from high-performance liquid chromatography indicated that the major products of 2, 4- DNT, 2, 4-DNB and 2, 4-DNAl in the microsomal and cytosol preparations were 2, 4-DNB, 2, 4- DNAl, and 2, 4-DNBA and 2, 4-DNB, respectively. The results indicate that 2, 4-DNAl is an intermediate in the oxidation of 2, 4-DNB to 2, 4-DNBA. In addition, data obtained by incubating 2, 4-DNT, 2, 4-DNB or 2, 4-DNAl with microsomal or cytosol fraction under air, nitrogen and various concentrations of CO in oxygen, using cofactors nicotinamide adenine dinucleotide phosphate and reduced nicotinamide adenine dinucleotide phosphate [NAD (P) and NAD (P) H] and inhibitors (SKF-525A, dimethyl sulfoxide, chloral hydrate, allopurinol, pyrazole and ο- phenanthroline) suggest that : (a) oxidation of 2, 4-DNT to 2, 4-DNB is mediated by microsomal P-450; (b) oxidation of 2, 4-DNB to 2, 4-DNAl is mediated mainly by cytochrome P-450 and NAD-dependent alcohol dehydrogenase; (c) oxidation of 2, 4-DNAl to 2, 4-DNBA and reduction of 2, 4-DNAl to 2, 4-DNB may be mediated by NAD (P) -dependent aldehyde dehydrogenases and NAD (P) H-dependent aldehyde reductases, respectively. These results indicate that 2, 4-DNT is metabolized stepwise to 2, 4-DNB, 2, 4-DNAl and 2, 4-DNBA in the rat liver and suggest that the oxidation of 2, 4-DNB to 2, 4-DNAl is a metabolic activation of 2, 4-DNT and that the microsomal cytochrome P-450 and alcohol dehydrogenase may play an important role in the metabolic activation of 2, 4-DNT.
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  • YOSHIMASA NISHIHARA, LARRY W. ROBERTSON, KOZO UTSUMI
    1987 Volume 35 Issue 4 Pages 1587-1595
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Treatment of isolated rat liver mitochondria with certain tetrachlorobiphenyls (TCBs) resulted in uncoupling of oxidative phosphorylation. In the present study, we examined the effects of chloro-substituent sites in TCB on the uncoupling action. Furthermore, the mechanism by which effective TCBs induce uncoupling action was explored. 2, 3, 2, 3'- (23-), 2, 4, 2, 4'- (24-), 2, 5, 2, 5'- (25-), and 2, 6, 2, 6'- (26-) TCBs caused uncoupling of oxidative phosphorylation, whereas 3, 4, 3, 4'- (34-) TCB did not. TCBs which were effective in causing uncoupling action contained chlorine atoms at the 2, 2'-positions in the biphenyl ring. 2, 2'-Chloro substitutions give the molecule a highly angular (non-planar) conformation. On the other hand, 34-TCB, which was ineffective, possesses chlorine atoms at lateral adjacent positions in the biphenyl ring. This substitution pattern allows a coplanar conformation of the molecule. Thus, the conformation of effective TCBs was non-planar, whereas that of ineffective isomers was coplanar. The permeability of mitochondrial membranes to ions was increased by the effective TCBs (23-, 24-, 25-, and 26-TCBs) as evidenced by K+-and Ca2+-release from mitochondria, which was followed by the dissipation of membrane potential. However, the ineffective TCB (34-TCB) neither increased the ion-permeability nor dissipated the membrane potential. These facts led us to propose to the following uncoupling mechanism; the effective TCBs, when intercalated into the mitochondrial membranes, produce non-specific increases in membrane permeability to ions, which leads to the dissipation of membrane potential. These effects of non-planar TCBs appear to be different from the mechanism of protonophoric uncouplers in which the dissipation of membrane potential is performed by only H+ transfer across the mitochondrial membranes.
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  • YOSHIYASU TERAO, NOBUYUKI IMAI, KAZUO ACHIWA
    1987 Volume 35 Issue 4 Pages 1596-1598
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Evidence for an ambivalent azomethine ylide intermediate was provided by the 1, 3-cycloaddition of deuterated N-benzyl-N- (methoxymethyl) trimethylsilylmethylamine to dimethyl benzylidene malonate and related reactions.
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  • YOSHIHISA SHIBANUMA, TOSHIHIKO OKAMOTO
    1987 Volume 35 Issue 4 Pages 1599-1603
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The 7-methoxyhydrophenanthrone (8) was synthesized from the 4a-nitromethylhydrophenanthrone (3) via nitration, reduction, and conversion of the resulting amino group to a methoxy group. On methylation of the intermediary phenol (7) with diazomethane, two products (9 and 10) were obtained along with the desired 8. The structures of these compounds having an aldoxime moiety were determined by physico-chemical methods. The mechanism of this unusual aldoxime formation from a nitromethyl group is discussed.
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  • HIROSHI TAKAHASHI, AKIHIRO KAWABATA, KIMIO HIGASHIYAMA
    1987 Volume 35 Issue 4 Pages 1604-1607
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    New chiral compounds, (S) -N-acylpyrrolidinylmethanols (1b-f and 1h), were synthesized and chiral methyltitanium diisopropoxides (2a-h) were prepared from 1a-h. Enantioselective carbon-carbon bond formation between aromatic carbaldehydes and 2a-h was achieved in yields of 90-97% and 10.5-54.1%ee. The chiral auxiliaries (1a-h) were recovered in almost quantitative yields without any loss of optical purity.
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  • TATSUYA MASUMIZU, KOOHEI NOZAWA, KEN-ICHI KAWAI, SHOICHI NAKAJIMA
    1987 Volume 35 Issue 4 Pages 1608-1609
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    A new electrochemical method of acetylation, using methyl acetate at room temperature, was developed. The current efficiency in all the reactions with primary alcohols exceeded 100%, ranging from 126 to 166%, indicating that this method of acetylation is advantageous for the preparation of acetates from the viewpoint of energy economy.
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  • TAKEHIKO FUKUNAGA, KOICHI NISHIYA, KOICHI TAKEYA, HIDEJI ITOKAWA
    1987 Volume 35 Issue 4 Pages 1610-1614
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    A new saponin, 3-Ο- [β-D-glucopyranosyl (1-02) β-D- glucuronopyranosyl] soyasapogenol B (XII) has been isolated from the herb of goat's rue (Galega officinalis L.), together with phytosterol (I), medicagol methyl ether (IV), medicagol (VI), phytosterol-β-D- glucoside (VIII), and allantoin (XI). The structures of the compounds were derermined on the basis of chemical and spectral evidence. This is the first time that I, IV, VI, VIII and XI have been isolated from this plant.
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  • LUCY SAI CHEONG WAN, PAUL WAN SIA HENG
    1987 Volume 35 Issue 4 Pages 1615-1618
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    An accurate method for measuring the fast uptake of water into tablets was established. The method involved the use of a video camera to monitor the flow of liquid in the capillary tube of the water penetration apparatus. Measurements of water uptake could be made in as short an interval as 0.04 s from 0 s. The liquid penetration profiles show that there are three linear portions of the double logarithmic plot of volume penetrated vs. time, with a different slope for each linear portion.
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  • TAKUMI SUZUKA, ATSUSHI FURUYA, AKIRA KAMADA, MASARU YAMAZAKI, TOSHIAKI ...
    1987 Volume 35 Issue 4 Pages 1619-1623
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    InCa2+-containing media, 1 mm diethyl maleate (DEM) increased the in vitro cefmetazole transport in rat everted colonic sac rapidly after a significant nonprotein thiol loss, but the increase in the ileal sac occurred only slowly after a significant nonprotein thiol loss. However, Ca2+-free media promoted the adjuvant effect of DEM rapidly even in the ileal sac. Since vanadate in the Ca2+-containing media also promoted the adjuvant effect of DEM, it is suggested that a perturbation of Ca2+ homeostasis as a secondary effect after nonprotein thiol loss is related to the increase of the intestinal mucosal permeability and that the ileal mucosa has stronger resistance to the secondary effect than the colonic mucosa does. The adjuvant effect of 300 mm salicylate (SA) was also promoted in Ca2+-free media. Since the effect of SA was stronger than that of DEM even though SA caused less nonprotein thiol loss, it is considered that the effect of SA involves at least two mechanisms.
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  • LUCY SAI CHEONG WAN, THANGARAJAH JEYABALAN
    1987 Volume 35 Issue 4 Pages 1624-1628
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    The effect of polyvinylpyrrolidone (PVP) powder on the formation of pellets of lactose, paracetamol and phenacetin was studied. The high water-solubility and affinity of lactose for water affect pellet growth and properties. Lactose pelletised with PVP powder resulted in some non-wetting of the PVP powder and hence pellet growth was restricted. In the case of phenacetin, a hydrophobic material, pellet growth increased markedly with PVP concentration. This is also attributed to the large viscosity build-up in some regions of the feed material in the pelletiser dish, giving rise to large pellets being formed. Balling of the feed material occurs resulting in an increase in pellet growth. Pelletisation of mixtures of varying proportions of the feed materials showed that the properties of pellets assumed those of the major component.
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  • TAKAFUMI NAGATOMO, AKIRA TAJIRI, TAKASHI NAKAMURA, REI HOKIBARA, YUKO ...
    1987 Volume 35 Issue 4 Pages 1629-1632
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    To assess the antihypertensive effect of terazosin, 2 [4- (tetrahydro-2-furanyl) carbonyl-l-piperazinyl] -6, 7-dimethoxy-4-quinazolinamine hydrochloride dihydrate, the inhibitory potency of terazosin on 3H-prazosin, 3H-p-aminoclonidine, 3H-dihydroalprenolol (3H-DHA), 3H-serotonin and 3H-ketanserin bindings to α1-, α2-and β-adrenergic receptors and 5HT1 and 5HT2 (serotonergic) receptors was examined by using the radioligand binding method. The results were compared with those for prazosin and bunazosin. Dog brain and aorta were used in the present study. A high inhibition of 3H-prazosin binding to α1-adrenoceptors in dog aorta by terazosin was observed, but the inhibitions of 3H-DHA, 3H-p-aminoclonidine, 3H-serotonin and 3H-ketanserin bindings by this drug were very weak. l-Terazosin showed the greatest inhibitory effect on 3H-prazosin binding to α1-adrenoceptors in dog aorta and brain. These results suggest that an inhibitory effect of terazosin at α1-aradrenoceptor binding sites may contribute to the hypotensive effect; the α2-and β-adrenoceptors and the serotonergic binding sites do not appear to be involved.
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  • Yuji Hanzawa, Kei-ichi Kawagoe, Masayuki Ito, Yoshiro Kobayashi
    1987 Volume 35 Issue 4 Pages 1633-1636
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    Racemic fluoroalkyl (E) -vinyl carbinols (1a-d) were kinetically resolved by Sharpless epoxidation. The optical purity of the resolved alcohols was excellent (98% ee) in mono-and difluoromethyl derivatives (1b and 1c) and moderate (60% ee) in a trifluoromethyl compound (1a).
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  • Yoshiaki Shirataki, Yayoi Tagaya, Ichiro Yokoe, Manki Komatsu
    1987 Volume 35 Issue 4 Pages 1637-1640
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    A new aromatic glycoside, named sophoraside A (1), was isolated from the roots of Sophora japonica, together with puerol A (2) and puerol B (3). The structure of 1 was characterized as puerol B 5-O-β-D-glucopyranoside by its chemical and spectral data. These compounds have new frameworks among the naturally occurring compounds.
    2 greatly inhibits 3H-ethylketocycloazocine on the receptor-binding assay test.
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  • Sayoko Hiranuma, Takeshi Shimizu, Hirosuke Yoshioka, Katsuhiko Ono, Hi ...
    1987 Volume 35 Issue 4 Pages 1641-1644
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    Various derivatives of aphidicolin (1) were prepared and their inhibitory effects on purified DNA polymerase α in vitro were assayed. Among these derivatives, the new 3α-, 17, 18-trihydroxyaphidicol-15-ene (24) was as inhibitory as the known 3-deoxy-and 3-oxoaphidicolins, (20) and (14). All the other derivatives with modification of any of the hydroxyl groups of 1 had no effect on the enzyme in vitro. The structure-activity relationships are discussed concerning functionalization on the aphidicolane ring.
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  • Kenji Yoshida, Shoji Yahara, Reiko Saijo, Kohtaro Murakami, Toshiaki T ...
    1987 Volume 35 Issue 4 Pages 1645-1648
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
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    The uncrushed berries of Solanum nigrum L. were immersed in cold MeOH for two years. From these berries, four new steroidal alkaloids, enzymatically derived from the original constituents, were obtained.
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  • Shozo Shoji, Fumiaki Haraguchi, Akira Okayama, Takayuki Funakoshi, Yuk ...
    1987 Volume 35 Issue 4 Pages 1649-1652
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    A peptic fragment from elastase was separated by affinity chromatography on an immobilized trialanine-agarose column. The fragment lost the enzymatic activity but retained the affinity for trialanyl peptide. It also stimulated pyruvate dehydrogenase activity in rat fat pads and protein kinase activity in the plasma membrane fraction of guinea-pig adipocytes.
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  • Yingjie Chen, Mitsuhiko Nose, Yukio Ogihara
    1987 Volume 35 Issue 4 Pages 1653-1655
    Published: April 25, 1987
    Released on J-STAGE: October 19, 2009
    JOURNAL FREE ACCESS
    The genuine sapogenin 20 (S) -protopanaxatriol (1) and its corresponding prosapogenin 20 (S) -ginsenoside-Rh1 (3) were prepared by direct treatment of the peracetate of 20 (S) -ginsenoside-Rg2 in an alcoholic alkaline solution. Two kinds of alkaline conditions were compared.
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