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Volume 30, Issue 7
Displaying 1-50 of 60 articles from this issue
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YOSHINORI HARADA, MASARU SAITO, KUGAKO MATSUMURA, HIDEO KATO, YOICHI I ...1982 Volume 30 Issue 7 Pages 2301-2312
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe crystal structures of the three forms (I, II, III) and the hydrate of tulobuterol hydrochloride (C-78) have been determined by X-ray analysis by using direct methods and refined by the block-diagonal least-squares method including anisotropic thermal parameters to final R values of 0.048, 0.057, 0.066 and 0.060 for forms, I, II, III and the hydrate, respectively. The molecular conformations in the four different crystalline forms are almost identical, though slight conformational differences are observed at the tertiary butyl terminal. The molecular packings however, are very different. Hydrogen bonds connecting the tulobuterol cations and the chloride anions form either a closed dimer-like unit in I and III or an open chain in II. In the hydrated crystal, a ribbon-like system of hydrogen bonds is formed by intervention of water molecules. Comparison of the crystal structures among these four forms of C-78 suggests a mechanism for the phase transition in the solid state and explains their thermodynamic properties previously reported.View full abstractDownload PDF (842K) -
HIDEKI MIKI, JUNJI YAMADA1982 Volume 30 Issue 7 Pages 2313-2318
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of 4-alkylthio-2-chloroquinazolines with alkylamines in dimethylformamide afforded 2, 4-bis (alkylthio)-, 2-alkylamino-4-alkylthio-, 4-alkylamino-2-chloro-, 4-alkylamino-2-alkylthio-, and 2, 4-bis (alkylamino) quinazolines. The relative easines of displacement of the chlorine and/or the alkylthio group in 4-alkylthio-2-chloroquinazolines depended on the bulkiness rather than the basicity of the alkylamine. A possible reaction mechanism is discussed.View full abstractDownload PDF (669K) -
TETSUSHI SAINO, TETSUYA SOMENO, HIROSHI MIYAZAKI, SHINICHI ISHII1982 Volume 30 Issue 7 Pages 2319-2325
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS^<14>C-Labelled leupeptin, Ac-L-[U-14C]-leucyl-L-leucyl-L-argininal, with a specific radioactivity of 20.9 mCi/mmol was prepared by a semisynthetic procedure in which L-leucyl-L-argininal dibutylacetal obtained by an enzymatic cleavage of leupeptin dibutyl-acetal with thermolysin was employed as a key compound. The chemical and radiochemical purities of the labelled leupeptin were found to be over 99% by high performance liquid chromatography using radioisotope and ultraviolet detectors.View full abstractDownload PDF (657K) -
MOHAMMED MOHAMMED YOUSIF, SEITARO SAEKI, MASATOMO HAMANA1982 Volume 30 Issue 7 Pages 2326-2332
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSQuinoline 1-oxides (1a-c) readily reacted with dimedone (2) and 1, 3-cyclohexanedione (10) in acetic anhydride or in dimethylformamide (DMF)-containing 1.2 eq of acetic anhydride to afford the corresponding 2-substituted quinolines (3a-c and 11a-c). The reaction of 3-bromoquinoline 1-oxide (1d) with 2 in DMF-acetic anhydride gave the 2-substituted quinoline (3d), whereas that in acetic anhydride alone afforded the enol acetate of 3d (3d'). The reactions of isoquinoline 2-oxide (5) with 2 and 10 similarly gave the 1-substituted isoquinolines (6 and 12). While pyridine 1-oxide (7) reacted with 2 to give the 2-substituted pyridine (8), the reaction with 10 produced 3-(2, 6-dioxocyclohexylidene)-2-(4-pyridyl) cyclohexanone (13).View full abstractDownload PDF (674K) -
OSAMU MIYASHITA, TOSHIHIKO KASAHARA, KOICHI MATSUMURA, HIROSHI SHIMADZ ...1982 Volume 30 Issue 7 Pages 2333-2341
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBoth cis (6) and trans (7) isomers of 6-alkoxy-5-fluoro-5, 6-dihydrouracils were prepared by catalytic hydrogenolysis of t-6-alkoxy-r-5-halogeno-5-fluoro-5, 6-dihydrouracils (4 and 5). The structures were estimated by comparing coupling constants (JH6F) in the proton magnetic resonance (PMR) spectra and confirmed by a single-crystal X-ray analysis of cis-6-ethoxy-5-fluoro-5, 6-dihydrouracil (6a). The stereochemistry of 6-alkoxy-5-alkoxycarbonyl-5-fluoro-5, 6-dihydrouracils (11-13) was clarified similarly on the basis of the PMR data. The chemical behavior of these compounds in acidic and basic media was examined.View full abstractDownload PDF (944K) -
MASAO FUJITA, TAKAO INOUE1982 Volume 30 Issue 7 Pages 2342-2348
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour C-glucosylxanthones [Mangiferin (3), isomangiferin (2), 4 and 5] and three C-glucosylflavones [swertisin (6), isoswertisin (7) and isoswertiajaponin (8)] were isolated from the fresh leaves of Iris florentina L. (Iridaceae). The structures of 4 and 5 were shown to be 7-O-methylmangiferin and 7-O-methylisomangiferin, respectively, by chemical and spectroscopic methods. In addition, the 13C nuclear magnetic resonance chemical shifts of aryl carbons in these C-glucosylxanthones (2-5) were assigned. On the basis of the co-occurrence of several types of xanthone and flavone C-glucosides, the biosynthetic relationship between both C-glucosides is briefly discussed.View full abstractDownload PDF (891K) -
TOHRU HINO, YASUHIRO TORISAWA, MASAKO NAKAGAWA1982 Volume 30 Issue 7 Pages 2349-2356
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAcetylation of 3-acetylindole (9) with acetyl chloride-aluminum chloride in nitrobenzene or methylene chloride gave 3, 5-diacetylindole (10) as the major product, together with 3, 6- and 3, 7-diacetylindole (11, 12) as minor products. The similar acetylation of ethyl 3-indolecarboxylate (16) also gave the 5-acetyl derivative (17a) as the major product, together with the 6-and 7-acetyl derivatives (18a, 19) as minor products. Oxidation of 1, 3-diacetylindole (15) with lead tetratrifluoroacetate gave 3-indolinones (22, 23) and a dimeric product (24).View full abstractDownload PDF (851K) -
MIKI SONODA, NOBUTAKA KURIYAMA, YUKIHIKO TOMIOKA, MOTOYOSHI YAMAZAKI1982 Volume 30 Issue 7 Pages 2357-2363
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of 1-ethoxycarbonylaziridine with malononitrile in the presence of sodium hydride gave 2-amino-3-cyano-1-ethoxycarbonyl-4, 5-dihydropyrrole (IIa) in 47% yield. Similarly, 1-ethoxycarbonyl-2-methyl (or phenyl) aziridine reacted with malononitrile to give 2-amino-3-cyano-5-methyl (or 4-phenyl)-4, 5-dihydropyrrole (IIb or c). Compounds IIa-c were dehydrogenated to the corresponding pyrroles (IVa-c) when heated with chloranil in benzene. 2-Amino-3-cyano-1-ethoxycarbonyl-4-phenylpyrrole (IVc) was also synthesized from ethyl N-phenacylcarbamate and malononitrile. The 2-benzamido derivatives of IIa-c reacted with N-bromosuccinimide in the presence of 2, 2'-azobisisobutyronitrile to produce the corresponding 2-benzamido-3-cyano-1-ethoxycarbonylpyrroles (Va-c) as major products.View full abstractDownload PDF (694K) -
MITSUHIRO WAKIMASU, CHIEKO KITADA, MASAHIKO FUJINO1982 Volume 30 Issue 7 Pages 2364-2368
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis of a heptadecapeptide corresponding to the amino acid sequence of dynorphin, H-Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Trp-Asp-Asn-Gln-OH, using the 4-methoxy-2, 6-dimethylbenzenesulfonyl (Mds) group for the protection of the guanidino function of arginine, is described. To synthesize dynorphin, three peptide fragments corresponding to residues, 1-3, 4-10, 11-17, were prepared and used as building blocks for the final construction of the full sequence of this opioid peptide. Final deprotection of the fully protected peptide was achieved by treatment with 0.15M methanesulfonic acid in trifluoroacetic acid-thioanisole at room temperature for 1 h and the purification was effected by column chromatography on carboxymethyl (CM)-cellulose and by preparative high performance liquid chromatography (HPLC). The synthetic heptadecapeptide was compared with purified natural dynorphin by means of reverse-phase HPLC and found to be identical with natural dynorphin.View full abstractDownload PDF (607K) -
EIICHI IBUKI, SHIGERU OZASA, YASUHIRO FUJIOKA, MOTOFUMI OKADA, YOSHIHI ...1982 Volume 30 Issue 7 Pages 2369-2379
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of twenty-seven polyphenyls, including quater-to sexiphenyls, was synthesized by the cross-coupling reaction of aryl Grignard reagents with arylene diiodides in the presence of bis (acetylacetonato) nickel (II). Twenty of them were obtained in fairly good yields (50-95%) under mild conditions at temperatures below ca. 60°C in ether-benzene solution within a few hours. In the cases of the remaining seven polyphenyls, however, lower yields (1-34%) were inevitable owing to the sterically crowded geometry of the reactant (s). Thus, the Kharash-type Grignard cross-coupling reaction was proved to be an efficient and convenient method for synthesizing a variety of polyphenyls, except in the cases of reactants with remarkably crowded geometry. The infrared, ultraviolet, and proton magnetic resonance spectral properties of several polyphenyls including three new compounds, 3-(2-biphenylyl)-o-quaterphenyl, 6'-(3-biphenylyl)-m-quaterphenyl, and 3, 4'-di (2-biphenylyl) biphenyl, are presented and discussed.View full abstractDownload PDF (1011K) -
HIROMICHI BESSO, RYOJI KASAI, YUHICHIRO SARUWATARI, TOHRU FUWA, OSAMU ...1982 Volume 30 Issue 7 Pages 2380-2385
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new dammarane-saponins, named ginsenoside-Ra1 (1) and ginsenoside-Ra2 (2) were isolated from the root of Panax ginseng C.A. MEYER by means of chromatography on silica gel and reversed phase chromatography on highly porous polymer. The structures of saponins 1 and 2 were established to be 20 (S)-protopanaxadiol 3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranoside-20-O-β-D-xylopyranosyl (1→4)-α-L-arabinopyranosyl (1→6)-β-D-glucopyranoside and 20 (S)-protopanaxadiol 3-O-β-D-glucopyranosyl (1→2)-β-D-glucopyranoside-20-O-β-D-xylopyranosyl (1→2)-α-L-arabinofuranosyl (1→6)-β-D-glucopyranoside, respectively.View full abstractDownload PDF (583K) -
TAMIO MORIKAWA, MIKIO TAKEDA, YOSHIHISA ARAI, KENJI TSUJIHARA1982 Volume 30 Issue 7 Pages 2386-2392
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of five 3-substituted-1-(2-chloroethyl)-3-(methyl-α-D-glucopyranosid-2-yl)-1-nitrosoureas (5a-e) was prepared and tested for antitumor activities. The compounds were obtained by the reaction of N-substituted methyl-α-D-glucosaminides (3a-e) with isocyanate followed by nitrosation with dinitrogen tetroxide. All the nitrosoureas obtained were remarkably active against leukemia L1210 and Ehrlich ascites carcinoma and showed greater therapeutic ratios than the positive controls ; 1-(2-chloroethyl)-3-(β-D-glucopyranosyl)-1-nitrosourea (GANU) and 1-(2-chloroethyl)-3-(D-glucopyranos-2-yl)-1-nitrosourea (DCNU).View full abstractDownload PDF (674K) -
Studies on the Saponins of Ginseng. IV. On the Structure and Enzymatic Hydrolysis of Ginsenoside-Ra1HARUYO KOIZUMI, SHUICHI SANADA, YOSHITERU IDA, JUNZO SHOJI1982 Volume 30 Issue 7 Pages 2393-2398
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe presence of ginsenoside-Ra in Ginseng Radix has been demonstrated by thin-layer chromatography. Recently, ginsenoside-Ra was shown to be a mixture of more than two saponins. Among them, ginsenoside-Ra1 was isolated and its structure was determined on the basis of spectral, chemical and enzymatic hydrolysis evidence as 20 (S)-protopanaxadiol 3-O-β-D-glucopyranosyl (1→2)-β-D-glucopyranosido-20-O-β-D-xylopyranosyl (1→4)-α-L-arabinopyranosyl (1→6)-β-D-glucopyranoside (1). Besides compound K (8), three prosapogenins, 20 (S)-protopanaxadiol 3-O-β-D-glucopyranosido-20-O-β-D-glucopyranoside (7), 20 (S)-protopanaxadiol 3-O-β-D-glucopyranosido-20-O-β-D-xylopyranosyl (1→4)-α-L-arabinopyranosyl (1→6)-β-D-glucopyranoside (9), and 20 (S)-protopanaxadiol 20-O-β-D-xylopyranosyl (1→4)-α-L-arabinopyranosyl (1→6)-β-D-glucopyranoside (10) were obtained in the course of enzymatic hydrolysis of ginsenoside-Ra1. Further, 20 (S)-protopanaxadiol 3-O-β-D-glucopyranosido-20-O-α-L-arabinopyranosyl (1→6)-β-D-glucopyranoside (6), 7 and 8 were obtained by enzymatic hydrolysis of ginsenoside-Rb2 (4). The course of enzymatic hydrolysis of ginsenosides with naringinase is also discussed.View full abstractDownload PDF (759K) -
TOHRU HIROSE, SHINSAKU MISHIO, JUNICHI MATSUMOTO, SHINSAKU MINAMI1982 Volume 30 Issue 7 Pages 2399-2409
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCondensation of 2-amino-6-chloropyridine (1) with diethyl ethoxymethylenemalonate gave the aminomethylenemalonate 2, which upon thermal cyclization (Gould-Jacobs reaction) afforded ethyl 7-chloro-1, 4-dihydro-4-oxo-1, 8-naphthyridine-3-carboxylate (3). Alkylation of 3 produced the 1-alkyl derivative 4. Substitution of 4 with a cyclic amine gave ethyl 7-substituted 1-alkyl-1, 4-dihydro-4-oxo-1, 8-naphthyridine-3-carboxylate (5). The ester 5 was hydrolyzed to the corresponding carboxylic acid 6. 7-Substituted 1-alkyl-1, 4-dihydro-4-oxo-1, 6-naphthyridine-3-carboxylic acids (20) were also synthesized from 4-amino-2-chloropyridine (13) in a similar manner. The in vitro antibacterial activity was enhanced by the presence of a cyclic amine at position 7 on 6 and 20. In general, the 1, 8-naphthyridine 6 was more active than the 1, 6-naphthyrdine counterpart 20. 1-Ethyl-1, 4-dihydro-4-oxo-7-(1-piperazinyl)-1, 8-naphthyridine-3-carboxylic acid (6e) (an analog of both pipemidic acid and nalidixic acid) was comparable to pipemidic acid but superior to nalidixic acid in terms of activity in vitro against Pseudomonas aeruginosa.View full abstractDownload PDF (967K) -
TAKAO SAKAMOTO, YOSHINORI KONDO, HIROSHI YAMANAKA1982 Volume 30 Issue 7 Pages 2410-2416
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree kinds of pyridopyrimidines were synthesized from appropriate pyrimidine derivatives. Cross-coupling of 4-amino-5-iodopyrimidines with α, β-unsaturated carboxylic esters followed by ring-closure afforded pyrido [2, 3-d] pyrimidines. Ammonolysis of 4-ethoxycarbonyl-5-phenylethynyl-and 5-ethoxycarbonyl-4-phenyl-ethynyl-pyrimidines which were obtained by cross-coupling of the corresponding halopyrimidines with phenylacetylene, gave pyrido [3, 4-d]-and pyrido [4, 3-d]-pyrimidines, respectively.View full abstractDownload PDF (679K) -
TAKAO SAKAMOTO, YOSHINORI KONDO, HIROSHI YAMANAKA1982 Volume 30 Issue 7 Pages 2417-2420
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2, 4-Dimethyl-6-phenyl-furo-and-thieno-[2, 3-d]-pyrimidine were synthesized by cross-coup ing of 2, 6-dimethyl-5-iodopyrimidines with phenylacetylene in the presence of palladium catalyst, followed by cyclization of the resulting phenylethynylpyrimidines. 2, 4-Dimethyl-6-phenyl [2, 3-d] pyrimidine was also synthesized by the thermal decomposition of 4-azido-2, 6-dimethyl-5-styrylpyrimidine, which was obtained from the 4-chloro derivative.View full abstractDownload PDF (512K) -
TAKASHI TANAKA, KEIKO KAWAMURA, HIROSHI KOHDA, KAZUO YAMASAKI, OSAMU T ...1982 Volume 30 Issue 7 Pages 2421-2423
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new dihydrochalcone-glucoside named confusoside (3) was isolated from the leaves of Symplocos confusa. This compound (3) was elucidated to be the 4'-O-β-D-glucoside of davidigenin (4) (2', 4, 4'-trihydroxyldihydrochalcone) by 1H and 13C nuclear magnetic resonance spectroscopy. No dihydrochalcone-glycoside could be isolated from the leaves of the following plants of Symplocaceae : S. glauca, S. lucida, S. myrtacea, S. liukiuensis, S. prunifolia, S. theophrastaefolia, S. cochinchinensis and S. chinensis var. leucocarpa. However, verbenalin (6) was isolated from the leaves of S. glauca.View full abstractDownload PDF (412K) -
YOSHIAKI FURUYA, YOSHIO KOSUGI, KAZUO ITOHO, KAZUKI YAMAGUCHI, TOSHIHI ...1982 Volume 30 Issue 7 Pages 2424-2428
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWhen mixed with methanol containing a catalytic amount of sulfuric acid and kept at 10°C for 10 h, benzoylacetone (BA) gave two products methoxylated on the side of the acetyl group (viz., 3, 3-dimethoxy-1-phenyl-1-butanone (AK) and 3-methoxy-1-phenyl-2-buten-1-one (A'E)) but no products methoxylated on the side of the benzoyl group (4, 4-dimethoxy-4-phenyl-2-butanone (BK) and 4-methoxy-4-phenyl-3-buten-2-one (B'E)) or products methoxylated on both carbonyls. Furthermore, BA did not undergo acid-catalyzed methanolysis under our conditions. The reason why acetal formation of the acetyl carbonyl occurs more easily than that of the benzoyl carbonyl, and the relationship of AK and A'E, which is not an intermediate in the formation of AK from BA even though AK can be formed from it, are discussed.View full abstractDownload PDF (495K) -
MUNEAKI TAKASE, SUMIO TERADA, HAJIME YAMAMOTO, TOSHIHARU NARITA, MASAH ...1982 Volume 30 Issue 7 Pages 2429-2432
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to confirm the structure of condurangogenin B, which is the aglycone of antitumor-active condurango glycoside (CG) B0, the hypoiodite reaction of condurangogenin C 3-acetate, was carried out. A mixture of condurangogenin C 3-acetate, Pb (OAc)4, I2, CaCO3, and diethyl ether was irradiated under nitrogen using a tungsten lamp. HPLC separation of the reaction products gave three compounds, P-1, P-2, and P-3. The structures of these compounds were determined from the spectroscopic data. The PMR and mass spectra of P-1 were essentially identical with those of condurangogenin B 3-acetate. Thus, the ester linkage positions (11-cinnamoyl, 12-acetyl) and the ketal structure of conduragogenin B were confirmed. As CGD0, 20-O-methyl-CGD0, and 20-iso-O-methyl-CGD0 could be converted chemically to CGB0, these glycosides have the same positions of ester linkages as CGB0.View full abstractDownload PDF (474K) -
SHINICHI SHIMAMURA, KOICHI YASUMURA, KENJI OKAMOTO, KENJI MIYATA, AKIR ...1982 Volume 30 Issue 7 Pages 2433-2439
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA heptacosapeptide (known as γ3-MSH) which is located within the amino acid sequence of bovine corticotropin-β-lipotropin precursor protein was synthesized by fragment condensation of Z-(1-12)-OSu and H-(13-27)-OBzl followed by deprotection with trifluoromethanesulfonic acid-thioanisole in TFA. The synthetic peptide exhibited weak melanocyte-stimulating activity (1.5×106 U/g, in vitro).View full abstractDownload PDF (818K) -
Studies on Ketene and Its Derivatives. CIX. Synthesis of naturally Occurring Anthracene-9, 10-dionesNOBUYA KATAGIRI, TETSUZO KATO, JUN NAKANO1982 Volume 30 Issue 7 Pages 2440-2446
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis of naturally occurring anthracene-9, 10-diones (12a-c) from ethyl 2-benzyl-4, 6-dihydroxybenzoates (7a-d), prepared by the reaction of diketene with ethyl 4-aryl-3-oxobutanoates (6a-d), is described. Reaction of diketene with 6a-d in the presence of sodium hydride in tetrahydrofuran gave 7a-d. Treatment of 7a-d with methyl iodide in the presence of potassium carbonate, followed by ethanolic sodium hydroxide, gave 2-benzyl-4, 6-dimethoxybenzoic acids (9a-d). Cyclization of 9a-d with trifluoroacetic acid-trifluoroacetic anhydride gave anthrone derivatives (10a-d) which, without purification, were oxidized with chromium trioxide to give the anthracene-9, 10-diones (11a-d). Selective demethylation of 11a-c with boron tribromide gave 12a-c.View full abstractDownload PDF (674K) -
MINORU KUBOTA, HIROSHI KOJIMA, OSAMU NAGASE, HIRO AMANO, HIROSHI TAKAG ...1982 Volume 30 Issue 7 Pages 2447-2452
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to obtain enkephalin derivatives with high analgesic activity, four enkephalinol analogs having the Tyr-D-Arg unit in the N-terminal position were synthesized. Of these, H-Tyr-D-Arg-Gly-MePhe-Met (O)-ol exhibited analgesic activity comparable to that of morphine after intravenous administration to mice.View full abstractDownload PDF (750K) -
SHIGEHIRO OKUYAMA, SHIGETOSHI MIYAMOTO, KATSUICHI SHIMOJI, YOSHITAKA K ...1982 Volume 30 Issue 7 Pages 2453-2462
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThirteen structural analogs of leukotrienes C and D were prepared and tested for contractile activities on guinea pig pulmonary parenchymal strips. The analogs differed from the native structures in the peptide moiety, the 5-hydroxyl group, the carboxyl group and in the number and geometry of ethylenic bonds. Deamino analogs of leukotriene C4 (LTC4) and leukotriene D4 (LTD4) retained substantial contractile activities. Amide analogs of LTD4 and 5-O-methyl-LTC4 showed some activity. Modification of the peptide moiety caused a 1-3 orders of magnitude decrement. Analogs in which the various ethylenic bonds were saturated retained substantial contractile activity. However, perhydro LTD had no contractile activity.View full abstractDownload PDF (918K) -
JONG CHOL CYONG, MAKOTO TAKAHASHI1982 Volume 30 Issue 7 Pages 2463-2466
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA cyclic guanosine monophosphate (GMP)-like substance which can be quantitated both by competitive binding assay and by radioimmunoassay has been found in Evodiae Fructus, an oriental herb. This substance has been extracted and extensively purified by Bio-Rad AG 1×4 and aluminum oxide column chromatographies and thin-layer chromatography (TLC). The purified substance was identified as cyclic GMP, since it showed the same physicochemical properties as authentic cyclic GMP on TLC with various solvents, ultraviolet spectroscopy, and high pressure-liquid chromatography and it was found to be decomposable by cyclic nucleotide specific phosphodiesterase. The existence of cyclic GMP was also demonstrated in several species of Rutaceae. The pharmacological significance of cyclic GMP in this medicinal herb is discussed here.View full abstractDownload PDF (504K) -
SHINICHI NAKATSUJI, RIE NAKANO, MIE KAWANO, KENICHIRO NAKASHIMA, SHUZO ...1982 Volume 30 Issue 7 Pages 2467-2473
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS5-(p-Dimethylaminophenyl)-2, 4-pentadienal (DAPDA) was conveniently prepared from p-dimethylaminobenzaldehyde by using readily available 4-(tert-butylthio)-3-buten-2-one as the chain lengthening agent. It has been shown that DAPDA is a useful reagent for detection and colorimetric determination of many pharmaceuticals (e.g., ethyl p-aminobenzoate (EAB), procaine hydrochloride, sulfisoxazole, sulfamethoxazole, sodium p-aminosalicylate, etc.) containing primary aromatic amino groups. This method is based on the reaction of these amines with DAPDA in the presence of trichloroacetic acid in methanol to form protonated Schiff bases which can be determined spectrophotometrically in the neighborhood of 630 nm. The limit of detection of these aromatic amines was in the range of 0.05-1.0μg/ml in each case. Lambert-Beer's law holds over 0.2-10μg/ml. The results were comparable to those obtained by hitherto reported methods. The method was successfully applied to commercial preparations of primary aromatic amines.View full abstractDownload PDF (675K) -
ITSUO YOSHIZAWA, RYOKO OHUCHI, KYOKO NAGATA, SHINJI ITOH, NORIO KAWAHA ...1982 Volume 30 Issue 7 Pages 2474-2486
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBesides the main products, 17α-ethyl-17β-methyl-18-nor-5β-androst-13-en-3α-ol (7a), 17α-methyl-D-homo-5β-androstane-3α, 17aβ-diol (8), and 17α-methyl-17aβ-chloro-D-homo-5β-androstan-3α-ol (9), other minor degradation products of pregnanediol 3, 20-disulfate (2) were obtained under reflux in 3 N hydrochloric acid, and were structurally identified by comparison with synthetic specimens. The steroidal mono olefins isolated were 5β-pregn-3-en-20α-ol (10a), 5β-pregn-2-en-20α-ol (11a), 5β-pregn-20-en-3α-ol (12a), and 5β-pregn-17 (20)-en-3α-ol (13a). The Z-isomer of 13a, 5β-pregn-17 (20)-en-3α-ol (14a), was detected by gas chromatography and identified by gas chromatography-mass spectrometric comparison with synthetic compound. Steroidal dienes were obtained as a mixture of Δ2-and Δ3-compounds having partial D-ring structures corresponding to 7a, 12a, and 13a. Although it was a minor product, 5β-pregnane-3α, 20β-diol (16) was also obtained, and its isolation suggests the formation of a C20-carbonium ion in the course of the hydrolysis. The yield of intact steroid, pregnanediol (1), was only 18.4% of the total products obtained.View full abstractDownload PDF (1269K) -
TSUNEHIRO KITAGAWA, HIDEAKI TANIMORI, KENSEI YOSHIDA, HISATSUGU ASADA, ...1982 Volume 30 Issue 7 Pages 2487-2491
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new viomycin-bovine serum albumin conjugate was characterized, and 19 viomycin molecules were found to be coupled with one molecule of the carrier protein. Enzyme labelling of viomycin with β-D-galactosidase was performed by a continuous two-step process using a maleimide succinimidyl ester type cross-linker. The optical conditions for enzyme immunoassay of viomycin using the new anti-viomycin antiserum and the enzyme labelled viomycin (double antibody method) were studied and a procedure with satisfactory accuracy and precision was developed. The specificities of two anti-viomycin antisera were compared by the enzyme immunoassay technique. Evidence that the enzyme immunoassay procedure is preferable to radioimmunoassay for a comparative study is also presented.View full abstractDownload PDF (631K) -
KATSUMI TAMAOKU, KEIYU UENO, KAYOKO AKIURA, YOSUKE OHKURA1982 Volume 30 Issue 7 Pages 2492-2497
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFive N-ethyl-N-(2-hydroxy-3-sulfopropyl) aniline derivatives have been synthesized and assessed as water-soluble hydrogen donors for the photometric determination of hydrogen peroxide in the presence of peroxidase. These compounds, sodium salts of N-ethyl-N-(2-hydroxy-3-sulfopropyl) aniline, N-ethyl-N-(2-hydroxy-3-sulfopropyl)-m-toluidine, N-ethyl-N-(2-hydroxy-3-sulfopropyl)-m-anisidine, 3, 5-dimethyl-N-ethyl-N-(2-hydroxy-3-sulfopropyl) aniline and 3, 5-dimethoxy-N-ethyl-N-(2-hydroxy-3-sulfopropyl)-aniline, gave high absorbances at visible wavelengths in media in the weakly alkaline to fairly acidic pH range. Further, the urea adduct of hydrogen peroxide could be conveniently used as a standard material.View full abstractDownload PDF (622K) -
HIROYUKI AKAGI, TOMOJIRO HAYASHI, TAEKO NAKAYAMA, TERUMI NAKAJIMA, TAK ...1982 Volume 30 Issue 7 Pages 2498-2502
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNative angiotensins of dog, guinea pig, rabbit, horse, pig and ox were isolated from plasma using homologous kidney extract as the renin source, and their sequences were analyzed by means of amino acid analysis and fluorescent peptide mapping. Angiotensins of dog, guinea pig and rabbit were identical with Ile5-angiotensin I, and the sequences of native angiotensins of the other species were in accord with the results reported previously.View full abstractDownload PDF (593K) -
MICHINAO MIZUGAKI, TOMOKO NISHIMAKI, TAKAYUKI SHIRAISHI, HIROSHI YAMAN ...1982 Volume 30 Issue 7 Pages 2503-2511
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn enzyme fraction which catalyzes the reduction of trans-2-enoyl-coenzyme A (trans-2-enoyl-CoA) to the corresponding saturated acyl-CoA derivative was separated from Escherichia coli (E. coli) extracts. The enzyme utilized reduced nicotinamide adenine dinucleotide phosphate (NADPH) as a sole electron donor for the reduction of substrates, and it acted on acyl-CoA substrates, but not on acyl-carrier protein esters. Therefore, the name NADPH-dependent trans-2-enoyl-CoA reductase was proposed for this enzyme. The reductase was stable at around pH 7-8, and was active over a wide pH range between 6 and 9. It had a functional thiol group and was readily inhibited by thiol reagents such as p-hydroxymercuribenzoic acid, and by cupric and some other metal ions. The enzyme was induced when E. coli cells were cultured in a medium containing oleic acid. These results suggest that this reductase does not participate in the de novo synthesis of fatty acids but is a new enzyme, although its physiological role is uncertain at the present stage.View full abstractDownload PDF (854K) -
YOSHIFUMI MATSUDA, KYOSUKE MIYAZAKI, YUKIO FUJIMOTO, YOSHIO HOJIMA, HI ...1982 Volume 30 Issue 7 Pages 2512-2520
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo forms of N-α-tosyl-L-arginine methyl ester (TAME) hydrolyzing activities were found in dog urine and one of them was confirmed to be dog urinary kallikrein (DUK, E.C. 3. 4. 21. 8). Mainly by chromatographic techniques, the kallikrein was purified about 1390-fold from the dialyzed dog urine with the overall yield of 36% of vasodilator activity. The specific activities of the finally purified preparation of DUK were 1250 kallikrein units (KU)/A280 of vasodilator activity and 11.3μmol/min/A280 of TAME esterolytic activity, and the preparation was homogeneous on disc gel electrophoresis and ultracentrifugal analysis. The molecular weight of DUK was estimated to be approximately 2.6 to 2.9×104 by vertical plate polyacrylamide gel electrophoresis, gel filtration on a Sephadex G-100 column and ultracentrifugation, and the isoelectric point of this enzyme was also determined as pI 4.2. Various properties such as pH stability, optimum pH for esterolytic activity and heat stability were similar to those of dog renal kallikrein.View full abstractDownload PDF (911K) -
OSAMU TAMEMASA, GEORGE A. GIGENIS, MASAKATSU TEZUKA, ATSUSHI TAKEDA, J ...1982 Volume 30 Issue 7 Pages 2521-2528
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was demonstrated by in vivo and in vitro radioactivity determinations and autoradiographic studies that the pancreas of animals pretreated with carbon tetrachloride or ethionine exhibited a reduced radioactivity uptake upon 14C-labeled L-leucine administration, whereas no significant decrease was observed in uptake of D-leucine. This uptake decrease from radioactive L-leucine in the pancreas of the treated animals is suggested to be due to inhibitions of protein synthesis and active membrane transport in the pancreas. The present investigations suggest that comparative studies of amino acid uptake by the pancreas using 11C-labeled D-and L-amino acids such as leucine might be more useful in the detection and assessment of pancreatitis by nuclear imaging of the pancreas than the use of L-amino acids alone or DL-amino acid racemates.View full abstractDownload PDF (1157K) -
YOSHIHARU KARUBE, TATSUO MAEDA, TAKESHI IMOTO, MASATO OHYA, SETSURO SU ...1982 Volume 30 Issue 7 Pages 2529-2533
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeventeen 99mTc-labeled ligands were evaluated as tumor scanning agents by preparing sequential scintigrams of mice bearing intramuscularly transplanted Ehrlich tumor. The ligands were labeled by the SnCl2 method and were administered intravenously to the mice. The ligands studied were ethylenediamine-N, N-diacetic acid (u-EDDA) and structurally related compounds. 99mTc complexes of u-EDDA, ethylenediamine-N, N'-diacetic acid, N-hydroxyethyliminodiacetic acid, and propylene-1, 3-diamine-N, N-diacetic acid achieved clear visualization of Ehrlich tumors. The image of the tumor was less clearly visualized with the complexes of iminodiacetic acid, N-methyliminodiacetic acid, nitrilotriacetic acid, ethylenediamine-N, N, N, ', N'-tetraacetic acid, N-hydroxyethylethylenediamine-N, N, ', N'-triacetic acid, hydrazine-N, N-diacetic acid, and 3-oxopiperazine-1-acetic acid.View full abstractDownload PDF (1137K) -
AKIRA KUSAI, SEIJI TANAKA, SEIGO UEDA1982 Volume 30 Issue 7 Pages 2534-2543
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe kinetics and mechanisms of the degradation of 2, 5-bis (1-aziridinyl)-3, 6-dimethyl-1, 4-benzoquinone (MEB) and 2, 5-bis (1-aziridinyl)-3, 6-diisopropyl-1, 4-benzoquinone (IPEB) were investigated and compared with those of 2, 5-bis (1-aziridinyl)-1, 4-benzoquinone (EB) investigated previously. The degradation of MEB and IPEB follows pseudo first-order kinetics in the same way as that of EB. The pH-rate profiles showed slopes of -1 on the acidic side and +1 on the basic side, as did that of EB. Thus, the degradation of MEB and IPEB is subject to specific acid-base catalysis. The apparent activation energies for MEB degradation at pH 4 and pH 11 were 16 and 24 kcal/mol, and those for IPEB degradation were 17 and 23 kcal/mol, respectively. In basic aqueous solution, MEB and IPEB are degraded to dihydroxybenzoquinones with monohydroxy-mono (1-aziridinyl) benzoquinones as intermediates in the same way as EB. On the other hand, in acidic aqueous solution, (2-hydroxyethylamino) benzoquinones are produced from MEB and IPEB, as in the case of EB, but they are further degraded to hydroxybenzoquinones. This was not practically observed in the case of EB. This phenomenon can be explained as follows : the alkyl groups at the 3 and 6 positions of benzoquinone increase the relative hydrolysis rate of 2-hydroxyethylamino groups derived from the hydrolytic cleavage of aziridine rings at the 2 and 5 positions of benzoquinone, making it comparable to the ring cleavage rate of aziridinyl groups.View full abstractDownload PDF (807K) -
MIKIO ARISAWA, JUNKO OHSHIMA, EMI OHSAWA, HIROMI B. MARUYAMA, YUZURU S ...1982 Volume 30 Issue 7 Pages 2544-2554
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn vitro antibacterial activities of a new cephalosporin, ceftriaxone, were bacteriologically characterized in comparison with those of cefotaxime and ceftizoxime. Minimal inhibitory concentrations (MIC) of cefriaxone determined on 680 fresh clinical isolates in Japan showed extraordinarily high activity against all gram-negative bacteria. Especially notable was its high activity against Proteeae species and Haemophilus influenzae ; in this respect it was greatly superior to both cefotaxime and ceftizoxime. It also showed high activity against Pseudomonas aeruginosa and some anaerobic pathogens. Against other strains, in general ceftriaxone exhibited activity comparable to those of 2 structurally related cephalosporins, except for Klebsiella sp. and Pseudomonas maltophilia, against which it showed lower activity. Its activity is bactericidal and, in contrast to cefotaxime and ceftizoxime, its minimal bactericidal concentration (MBC) value was less than 3 times the MIC except for Ps. aeruginosa. Its mode of action was morphologically assessed. Ceftriaxone showed an unusually high stability to most bacterial β-lactamases except to so-called cefuroximases from Bacteroides fragilis, Pseudomonas cepacia and Proteus vulgaris. In addition, ceftriaxone was found to be a very potent inhibitor of cephaloridine hydrolysis by various β-lactamases.View full abstractDownload PDF (985K) -
SEIKI TANADA, KEITO BOKI, TATSUMI TOUMIYA, HIROYOSHI KINUGASA, TAKEO N ...1982 Volume 30 Issue 7 Pages 2555-2560
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structures of micropores and supermicropores of activated carbon are discussed on the basis of the results of application of the two-term equation, a=W01/ν*exp[-(A/βE01)2]+W02/ν*exp[-(A/βE02)2)] to the adsorption isotherms of hydrogen sulfide. The fact that the Dubinin-Radushkevich plots of the adsorption isotherms showed deviation from linearity whereas the two-term equation described them well seems to indicate that the activated carbon used possesses heterogeneous pores, that is, micropores and supermicropores with a flat slit shape. The distribution of radii of supermicropores seems to favor micropores rather than mesopores. It was suggested that the net differential heat of adsorption was more affected by the heterogeneity of pores than by the changes of lateral interactions of adsorbed hydrogen sulfide in relation to the increasing amount adsorbed.View full abstractDownload PDF (634K) -
KAZUYUKI KIZUKI, MASAHIKO IKEKITA, YUUJI SHIMAMOTO, HIROSHI MORIYA1982 Volume 30 Issue 7 Pages 2561-2569
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSProkallikrein was partially purified from porcine pancreas by water extraction in the presence of soybean trypsin inhibitor, ethylenediaminetetraacetic acid (EDTA), N-ethylmaleimide and benzamidine, followed by a combination of ammonium sulfate fractionation, ion-exchange chromatographies, gel filtration and chromatofocusing in the presence of various protease inhibitors. The prokallikrein preparation obtained was stable on storage at -25°C ; after 1.5 months only 2% of prokallikrein was activated. It was also fairly stable when it was lyophilized and stored at room temperature. The prokallikrein was rapidly activated by trypsin. Chymotrypsin also activated prokallikrein, but an extremely large amount of chymotrypsin was necessary. Urokinase, cathepsins C and D, plasmin, thrombin, Factor Xa, collagenase, elastase, prolidase and leucine aminopeptidase caused no detectable activation of prokallikrein. Several components of prokallikrein were detected by isoelectric focusing. The pI values of the two main components were 4.47 and 4.68. Slight spontaneous activation of prokallikrein occurred during the chromatographies even when the greatest care was taken.View full abstractDownload PDF (966K) -
MATAO KANAOKA, MASAO YOSHIZAKI, HIROHARU FUJINO1982 Volume 30 Issue 7 Pages 2570-2574
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe ether-soluble neutral constituents of the dried roots of Trichosanthes japonica REGEL, Trichosanthes kirilowii MAXIM. and Trichosanthes cucumeroides MAXIM. were examined. Mixed glycerides, Δ7-stigmastenol (IV), α-spinasterol (V), steryl (mixture of Δ7-stigmastenol and α-spinasterol)-β-D-glucopyranoside (VI, VII) and steryl (mixture of Δ7-stigmastenol and α-spinasterol)-6'-fatty acyl (mixture of palmitic acid and (Z, Z)-9, 12-octadecadienoic acid)-β-D-glucopyranoside (VIII, IX, X, XI) were identified.View full abstractDownload PDF (660K) -
HIROSHI KASHIWAGI, YUJI FUJIKI, SABURO ENOMOTO1982 Volume 30 Issue 7 Pages 2575-2578
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe heterogeneous vapor-phase alkylation of pyridine with methanol was examined over metal cation-exchanged X-and Y-type zeolites in an atmosphere of nitrogen. β-Methylation was observed over H+-or Li+-exchanged zeolites, whereas α-and γ-methylation (the former occurred in preference) were observed over alkaline earth cation-exchanged zeolites. For example, at 400°C, the yields of α-, β-, and γ-picolines over the HY catalyst were 2.6, 12.2, and 2.6%, whereas those over the BaY catalyst were 22.7, 3.8, and 7.6%, respectively. This catalytic ring alkylation over metal cation-exchanged zeolites was also examined by the use of pyridine with ethanol and picolines with either methanol or ethanol.View full abstractDownload PDF (521K) -
TAIICHIRO WATANABE, SHINICHI SUGAWARA, TETSUO MIYADERA1982 Volume 30 Issue 7 Pages 2579-2582
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESStert-Butyl α-amino-2, 4, 6-cycloheptatriene-1-acetate (6) was prepared by treatment of tert-butyl N-benzylideneglycinate (5) with n-butyllithium followed by reaction with tropylium tetrafluoroborate. Heating 6 in xylene resulted in isomerization to tert-butyl α-amino-1, 3, 6-cycloheptatriene-1-acetate (7). Both the glycine derivatives were utilized for the acylation of a 7-amino-3-deacetoxycephalosporanic acid (7-ADCA) derivative (10) to obtain the orally active acyl derivative (14).View full abstractDownload PDF (481K) -
SHINJI SAKATA, SEISHIRO YONEI, HIROSHI YOSHINO1982 Volume 30 Issue 7 Pages 2583-2585
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new method for the synthesis of 2-substituted 6-methylpurine ribosides from guanosine is described. Reaction of N (2), O (2'), O (3'), O (5')-tetraacetyl-O (6)-p-toluenesulfonylguanosine with carbanion from ethylacetoacetate gave the 6-ethoxycarbonylmethyl derivative, which was further converted to 2-amino-6-methylpurine riboside by deacetylation and decarboxylation. Replacement of the amino group of the compound by the fluoro group was achieved by the Schiemann reaction. The fluoro group could easily be replaced by several nucleophiles. As a result, 2-methylthio-, and 2-dimethylamino-6-methyl-9-β-D-ribofuranosylpurines could be effectively prepared.View full abstractDownload PDF (468K) -
KATSUHIDE MATOBA, TAKAO YAMAZAKI1982 Volume 30 Issue 7 Pages 2586-2589
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS[1H] Pyrrole (IIa) was reacted with 2-chloroethyl tosylate (III) in acetone in the presence of potassium hydroxide (condition A) to give 1-(4-oxo-2-methyl-2-pentyl) [1H]-pyrrole (IV) instead of 1-(2-tosyloxyethyl) [1H] pyrrole (IIb). IV was obtained from the reaction of IIa and mesityl oxide (V) in acetonitrile in the presence of potassium hydroxide (condition B). With IIa under condition B, crotononitrile, ethyl crotonate, and 4, 4-dimethyl-2-cyclohexenone (IX) gave 3-(1-[1H] pyrrolyl) butyronitrile (VIIa), 3-(1-[1H] pyrrolyl) butyric acid (VIIIa), and a mixture of 4, 4-dimethyl-3-(1-[1H] pyrrolyl) cyclohexanone (X) and 1-cyanomethyl-4, 4-dimethyl-3-(1-[1H] pyrrolyl) cyclohexanol (XI), respectively.View full abstractDownload PDF (546K) -
JUN NAKANO, NOBUYA KATAGIRI, TETSUZO KATO1982 Volume 30 Issue 7 Pages 2590-2594
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis of 1, 3-dimethoxyfluoren-9-ones (7a-f) from ethyl 2-aryl-4, 6-dihydroxybenzoates (4a-d), prepared by the reaction of diketene with ethyl 3-aryl-3-oxopropionates (3a-d), is described. Reaction of diketene with 3a-d in the presence of sodium hydride in tetrahydrofuran gave 4a-d. Methylation of 4a-d with methyl iodide, followed by treatment with alcoholic sodium hydroxide, gave 2-aryl-4, 6-dimethoxybenzoic acids (6a-d). Cyclization of 6a-d with trifluoroacetic anhydride gave 7a-f.View full abstractDownload PDF (538K) -
KENJI OKAMOTO, KOICHI YASUMURA, NOBUHIRO YAMAMURA, SHINICHI SHIMAMURA, ...1982 Volume 30 Issue 7 Pages 2595-2598
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe pentadecapeptide corresponding to the entire amino acid sequence of α-MSH II, isolated from salmon pituitary gland, was synthesized by a conventional procedure. The synthetic peptide exhibited in vitro melanocyte-stimulating activity of 1.66×1010 MSH U/g.View full abstractDownload PDF (648K) -
ITSUO MORI, YOSHIKAZU FUJITA, KIMIKO SAKAGUCHI1982 Volume 30 Issue 7 Pages 2599-2603
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new sensitive, rapid and simple spectrophotometric method for the determination of cephalexin (CEX) and ampicillin (AB-PC) was established using o-hydroxyhydroquinonephthalein (Qn. Ph.) and palladium (II) [Pd (II)] at a low concentration of cetyltrimethylammonium chloride (CTAC) in weak acidic media. This method is based on the fact that the intensity of the absorption peak of Qn. Ph. -Pd (II) complex at 630 nm is decreased significantly by the addition of CEX or AB-PC, and the decrease in the absorbance is proportional to the concentration of CEX or AB-PC. The method could be used in the concentration range up to -17μg/10 ml of CEX and -14μg/10 ml of AB-PC, where the spectrophotometric sensitivities were estimated to be 0.0015μg/cm2 for CEX and 0.0012μg/cm2 for AB-PC for an absorbance unit of 0.001 at 630 nm, and was applied to the determination of CEX or AB-PC in pharmaceutical preparations.View full abstractDownload PDF (520K) -
TAKASHI ABIKO, IKUKO ONODERA, HIROSHI SEKINO1982 Volume 30 Issue 7 Pages 2604-2610
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA heptadecapeptide amide, H-Pyr-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2, corresponding to the entire amino acid sequence of human gastric I, was synthesized by the solution method. This peptide inhibited lactate dehydrogenase activity by 87.6% at a concentration of 300 pg/ml. This peptide was tested for suppression of PHA-induced lymphocyte proliferation, but showed no significant activity.View full abstractDownload PDF (882K) -
HIROKO KAWANO, FUMIKO HIGUCHI, TADANORI MAYUMI, TAKAO HAMA1982 Volume 30 Issue 7 Pages 2611-2613
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe lactate level in red blood cells from rats administered ergothioneine by i.p. injection for 7 d (1.6 mg/kg/d) then starved for 24 h was maintained at the normal level, whereas that of the control group (no ergothioneine) decreased to 60%. No effect of ergothioneine administration was observed on the lactate level in red blood cells when rats were fed ad libitum. Addition of 10-3 M ergothioneine to either a suspension or a hemolysate of red blood cells from intact rats accelerated lactate formation. Moreover, the amounts of glucose-6-phosphate (G-6-P) and fructose-6-phosphate (F-6-P) in red blood cells decreased to 74% and 51% of the control level respectively. The amount of pyruvate in red blood cells did not change. It is suggested that ergothioneine had the effect of accelerating the glycolytic metabolism in red blood cells, or effected an increase in the permeability of red blood cells to glucose.View full abstractDownload PDF (444K) -
KANJI TAKADA, SHOZO ASADA, SHOZO MURANISHI1982 Volume 30 Issue 7 Pages 2614-2617
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe applicability of the model-independent method to pharmacokinetic analysis was statistically studied. For this purpose, two kinds of data were used, i.e., plasma disappearance data for warfarin (a typical example of a triple-exponential decay) and for amoxicillin (double-exponential decay). By using statistical analysis with least-squares fitting (SALS), a nonlinear regression analysis program, curve fittings were carried out with respect to those data sets. In the case of the warfarin data, the triple-exponential equation was superior to the model-independent one in terms of both the residual sum of squares and an information criterion (AIC). However, very little difference between the two could be seen by eye when the results were drawn on graph paper. In the case of the amoxicillin data, the model-independent equation was statistically superior to the double-exponential one. The applicability of this model-independent method to pharmacokinetic analysis was thus confirmed.View full abstractDownload PDF (471K) -
HARUHISA UEDA, NAOKI NAMBU, TSUNEJI NAGAI1982 Volume 30 Issue 7 Pages 2618-2620
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThermodynamic values for two polymorphic forms of tolbutamide (form A and form B) were calculated on the basis of solubility determination and differential scanning calorimetry. The transition temperature and the heat of transition were estimated to be 93.3°C, and 230 cal/mol by the former method, and 98.5°C, and 255 cal/mol by the latter method. The dissolution rate was only slightly affected by the polymorphic form.View full abstractDownload PDF (400K) -
NAOKI WAKIYAMA, KAZUHIKO JUNI, MASAHIRO NAKANO1982 Volume 30 Issue 7 Pages 2621-2628
Published: July 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDL-Polylactic acid (PLA) microspheres were prepared from three lots of PLA by a solvent-evaporation process and release patterns of butamben, tetracaine and dibucaine from these microspheres were examined. As a first step, the physicochemical characteristics of three lots of PLA were examined. The release mechanism was examined by scanning electron microscopy. Microsphere characteristics and release patterns from the microspheres were dependent on both PLA characteristics and the local anesthetics used for the preparation.View full abstractDownload PDF (2307K)