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Volume 30, Issue 5
Displaying 1-50 of 63 articles from this issue
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TOYOHISA TSUKAMOTO, SHUSHI MORITA, JUTARO OKADA1982 Volume 30 Issue 5 Pages 1539-1549
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOxidation of glucose to gluconic acid using a catalyst consisting of glucose oxidase and catalase both immobilized on activated carbon was employed to study the liquid-solid contacting efficiency (f) in a trickle-bed reactor. The global rates of reaction were measured at 25°C and at atmospheric pressure, as a function of catalyst loading (1.0 to 9.0 g), catalyst partiole size (0.055 and 0.110 cm), superficial liquid velocity (0.044 to 0.337 cm/s), and superficial gas velocity (1.63 to 7.35 cm/s). The measured rate was considered to be the sum of the rates at the liquid-covered and gas-covered outer surfaces of catalyst particles. The value of f was determined by integrating numerically the mass balance equations for oxygen and the equation for the intrinsic rate of reaction simultaneously. The estimated value of f did not vary with catalyst loading. While f was independent of gas flow rates, it was influenced by both liquid flow rates and particle sizes. The effects of these operating parameters on f are discussed on the basis of the static and/or dynamic holdup.View full abstractDownload PDF (1122K) -
HITOSHI TANAKA, REIKO MURATA, AKIYOSHI YOSHIDA, SHINICHI HAYASHI1982 Volume 30 Issue 5 Pages 1550-1556
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new glucoside, sennoside G, was isolated from the leaves of Cassia angustifolia (Senna) in crystalline form and shown by chemical and physical means to be the optical antipode of sennoside A with respect to the sennidin moiety. The optical rotatory dispersion spectrum of sennidin G showed a pattern exactly opposite to that of sennidin A. Sennosides A, B and G were isomerized to each other reversibly, and were oxidized to give 8-glucosylrhein.View full abstractDownload PDF (652K) -
KAZUE SATOH, TADASHI MIYASAKA, KIICHI ARAKAWA1982 Volume 30 Issue 5 Pages 1557-1566
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn treatment with hydrazine hydrate (80%) and methylhydrazine, oxazolo [3, 2-b] pyridazinium perchlorates (I) furnish hemi-perchlorates of 4H-pyridazino [6, 1-c] [1, 2, 4] triazines (VI) and 1-methyl-4H-pyridazino [6, 1-c] [1, 2, 4] triazinium perchlorates (VIII), respectively. On reaction with phenylhydrazine by refluxing in acetonitrile, I affords an osazone (XII), a phenylazopyridazine (XIII) and its hydrazo derivative (XIV), which are also formed from N-phenylamino-6-chloro-2-phenacyl-2, 3-dihydropyridazin-3-ylideneimine phenylhydrazone (XV) by refluxing with phenylhydrazine in acetonitrile. In the reaction of I with hydrazines, it has been shown that the initial attack of the reagent always occurs at the C8a-position to furnish various condensed pyridazine derivatives.View full abstractDownload PDF (1042K) -
SHIGERU KOBAYASHI, KAZUTO OKIMOTO, YASUHIRO IMAKURA1982 Volume 30 Issue 5 Pages 1567-1573
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCleavage of the methylenedioxy ring in aromatic formyl (1-3), nitro (4 and 5), and acetyl (30) compounds with N-sodium benzyloxide-benzyl alcohol in dimethyl sulfoxide gave 3-hydroxybenzene derivatives (19, 22-24, 26, 27, and 33). In the case of the acetyl compound 30, the 4-hydroxybenzene derivative (34) was also obtained as a minor product. Regioselective cleavage of the ring in aromatic compounds having electron-withdrawing groups with nucleophilic oxide anions is discussed. Cleavage of the ring in 1-5 and 30 with 2N sodium methoxide in dimethyl sulfoxide-dimethylformamide was found to be useful for the praotical preparation of 3-hydroxybenzene derivatives (6-10 and 31).View full abstractDownload PDF (796K) -
TADASHI OKAWARA, TAKASHI MATSUDA, YOSHIHIDE NOGUCHI, MITSURU FURUKAWA1982 Volume 30 Issue 5 Pages 1574-1578
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA one-pot synthesis of β-lactams (4) was successfully achieved by the reaction of β-haloacyl chlorides (1) with α-amino acids (2) in aqueous 5% sodium hydroxide solution in the absence of phase transfer catalyst in yields of 43-91%.View full abstractDownload PDF (559K) -
MINORU MACHIDA, HARUKO TAKECHI, YUICHI KANAOKA1982 Volume 30 Issue 5 Pages 1579-1587
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSUpon irradiation, a homologous series of N-[ω-(methylanilino) alkyl] phthalimides 5, having a nonconjugated bichromopholic system, undergoes regioselective remote photooyclization to give medium- to large-sized (up to twenty-two-membered) diazacyclols 6.View full abstractDownload PDF (910K) -
KOICHIRO YAMADA, MIKIO TAKEDA, NOBUO ITOH, NORIHIDE UMINO, KATSUO IKEZ ...1982 Volume 30 Issue 5 Pages 1588-1593
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRacemic 5, 7-dihydroxy-1-(3, 4, 5-trimethoxybenzyl)-1, 2, 3, 4-tetrahydroisoquinoline [(±) -1], a positional isomer of trimetoquinol (TMQ) with respect to its dihydroxy moiety, has been optically resolved. The bronchodilating activity in anesthetized cats (i.v. administration) was found to reside in the levorotatory enantiomer [(-) -1]. The absolute stereochemistry of the active enantiomer [(-) -1] was determined to be S by X-ray crystallographic analysis.View full abstractDownload PDF (667K) -
TADATAKA ISHIKAWA, MASATOSHI YAMATO1982 Volume 30 Issue 5 Pages 1594-1601
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSActive methylene compounds, diethyl malonate, α-tetralone, dimedone, acetyl-acetone, malononitrile, and diketene, were reacted with 1-ethoxyisochroman (1) to give the corresponding 1-substituted isochroman derivatives, 4, 5, 6, 7, 8, 9, 10, and 11, respectively. When 4 was treated with sodium ethoxide or potassium tert-butoxide, ethyl 1, 4-dihydro-2-naphthoate (14a), ethyl 1, 2-dihydro-2-naphthoate (14b), and ethyl 2-naphthoate (13) were obtained. On the other hand, the reaction of 2-(1-isochromanyl) cyclohexanone (3) with potassium tert-butoxide afforded 9-formyl-1, 2, 3, 4-tetrahydroanthracene (20) and 1, 2, 3, 4, 9, 10-hexahydroanthracene (21). The conversion mechanisms of 1-substituted isochromans (2, 3, 4, and 7) into naphthalenes (13, 14a, b, and 18) and 1, 2, 3, 4-tetrahydroanthracenes (20 and 21) are proposed.View full abstractDownload PDF (880K) -
MASANORI KUROYANAGI, YOOKO YAMAMOTO, SEIGO FUKUSHIMA, AKIRA UENO, TADA ...1982 Volume 30 Issue 5 Pages 1602-1608
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new cyclobutane derivative, which may be formed from dehydrokawain by [2+2] cycloaddition, named compound B (8a), mp 226-227°C, C28H24O6, and a new flavanonol, named compound C (10a), mp 142-143°C, C17H14O6, together with pinobanksin (1a), taxifolin (2a), quercetin-3β-D-glucopyranoside 2"-gallate (3), pinosylvin (4a), methyl gallate (5a), dehydrokawain (6) and compound A (7a) were isolated from Polygonum nodosum (Polygonaceae). The structures of the new compounds, 8a and 10a, were established to be rel-1, trans-3-bis-(4-methoxy-2-oxopyran-6-yl)-cis-2, trans-4-diphenyl cyclobutane and (2R, 3R)-3-hydroxy-5-methoxy-6, 7-methylenedioxy-flavanone, respectively, on the basis of physicochemical evidence. The structure of 7a was also established to be rel-(1R, 6S, 7S, 8S)-5-methoxy-7-phenyl-8-(4-methoxy-2-oxopyran-6-yl)-1-(E) styryl-2-oxabicyclo-[4, 2, 0]-oct-4-en-3-one and this compound was found to be identical with aniba-dimer-A.View full abstractDownload PDF (807K) -
SETSUKO SEKITA, KUNITOSHI YOSHIHIRA, SHINSAKU NATORI, SHUNICHI UDAGAWA ...1982 Volume 30 Issue 5 Pages 1609-1617
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBioproduction of chaetoglobosins, novel type cytochalasans, by Chaetomium spp. was examined. Details of the culture conditions and methods for separation of the metabolites of Chaetomium globosum are presented. Some cytological effects of chaetoglobosins were also mentioned.View full abstractDownload PDF (1332K) -
SETSUKO SEKITA, KUNITOSHI YOSHIHIRA, SHINSAKU NATORI, HARUMITSU KUWANO1982 Volume 30 Issue 5 Pages 1618-1628
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structures (Chart 7) of chaetoglobosins A, B, and D, 10-(indol-3-yl)-[13] cytochalasans, were elucidated by isomerization reactions and physical method including precise 1H-NMR decoupling experiments.View full abstractDownload PDF (982K) -
SETSUKO SEKITA, KUNITOSHI YOSHIHIRA, SHINSAKU NATORI, HARUMITSU KUWANO1982 Volume 30 Issue 5 Pages 1629-1638
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structures (Chart 1) of chaetoglobosins C, E, F, G, and J, 10-(indol-3-yl)-[13] cytochalasans, were established on the basis of physical data, especially 1H-NMR, and chemical correlations. The stereo-structural features of chaetoglobosins are discussed.View full abstractDownload PDF (1027K) -
YASUHIKO SATO, HIDEO NAKAI, MASAO WADA, HIROSHI OGIWARA, TOMISHIGE MIZ ...1982 Volume 30 Issue 5 Pages 1639-1645
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhotolysis of N-ω-alkoxyalkylphthalimides 1 gave the intramolecularly cyclized compounds, oxazolo [4, 3-a] isoindoles 2a-g, pyrrolo [2, 1-a] isoindoles 6i-j, oxazolo [4, 3-a]-isoindole-1-spiro-1'-cycloalkanes 2k-n and 3, 4-dihydro-2-benzazepine-1, 5 (2H)-dione 3, via δ-hydrogen abstraction and/or two-fold Norrish type II processes.View full abstractDownload PDF (896K) -
YOSHIHIDE NOGUCHI, MASANOBU ISODA, KENKICHI KUROKI, MITSURU FURUKAWA1982 Volume 30 Issue 5 Pages 1646-1652
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOne-pot syntheses of sulfinates, sulfinamides, and thiosulfinates by O-, N-, and S-sulfinylations of alcohols, amines, and thiols with p-toluenesulfinic acid in the presence of various activating reagents, phenyl phosphorodichloridate (1), diphenyl phosphoro-chloridate (2), triphenylphosphine N-chlorosuccinimide (NCS) (3), and 3-(phthalimidoxy)-1, 2-benzoisothiazole 1, 1-dioxide (4), were investigated. All of these reagents were reasonably effective for O-and S-sulfinylation, but ineffective for N-sulfinylation. Among them, the reagents 1 and 2 were slightly more efficient than the others.View full abstractDownload PDF (770K) -
MICHIO NAMIKOSHI, KEIZO SASAKI, YUKIKO KOISO, KAZUTAKA FUKUSHIMA, SHIG ...1982 Volume 30 Issue 5 Pages 1653-1657
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAzalomycin F4a (C56H95N3O17), an antibiotic produced by Streptomyces hygroscopicus var. azalomyceticus, was purified and its physicochemical properties were determined. Partial strutures of this compound were elucidated from its spectral data.View full abstractDownload PDF (596K) -
MICHIO NAMIKOSHI, SHIGEO IWASAKI, KEIZO SASAKI, MITSURU YANO, KAZUTAKA ...1982 Volume 30 Issue 5 Pages 1658-1668
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDegradations of azalomycin F4a were carried out, and the structures of the products were determined.View full abstractDownload PDF (1283K) -
SHIGEO IWASAKI, MICHIO NAMIKOSHI, KEIZO SASAKI, MITSURU YANO, KAZUTAKA ...1982 Volume 30 Issue 5 Pages 1669-1673
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe skeletal structure of azalomycin F4a (1) was determined on the basis of available data about the physicochemical properties of F4a and about the structures of the degradation products of this compound and of its derivatives. The structure was found to consist of a 36-membered lactone ring bearing multiple hydroxy functions, a diene and a dienoic ester group, as well as a side chain with an N-methylguanidine moiety as its terminal. One of the hydroxyl groups on the lactone ring forms a hemiketal ring with the keto group on a ring carbon, and another hydroxyl group forms a hemiester with a malonic acid moiety.View full abstractDownload PDF (548K) -
JEAN-CHARLES LANCELOT, JEAN-MARIE GAZENGEL, SYLVAIN RAULT, MAX ROBBA1982 Volume 30 Issue 5 Pages 1674-1679
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSynthesis of pyrrolo [1', 2' : 1, 2] pyrazino [6, 5-c] carbazole derivatives is described starting from 3-amino-4, 6-dinitro-9-ethylcarbazole (1). The pyrrole ring is obtained by reaction with 2, 5-dimethoxytetrahydrofuran. Cyclization of the pyrazine ring is achieved after reduction of the nitro grouping by intramolecular cyclization of 4, 6-diamino-9-ethyl-3-(1-pyrrolyl) carbazole derivatives. 1H nuclear magnetic resonance spectra are studied.View full abstractDownload PDF (796K) -
MOHAMMED MOHAMMED, YOUSIF, SEITARO SAEKI, MASATOMO HAMANA1982 Volume 30 Issue 5 Pages 1680-1691
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReactions of quinoline, lepidine, 4-chloro-, 4-methoxy- and 4-morpholino-quinoline 1-oxides (1a-e) with Meldrum's acid (2) in acetic anhydride smoothly occurred at room temperature to afford the corresponding 5-(2-quinolyl)-Meldrum's aoids (3a-e) in good yields. On the other hand, when the reactions were carried out in dimethylformamide containing 1.2 eq acetic anhydride the N-ylides (4a-e) were produced ; while the reactions of 1a, d, e yielded only N-ylides 4a, d, e, 4b, c were formed along with smaller amounts of 3b, c in the reactions of 1b, c. 3-Bromoquinoline 1-oxide (1f) gave only the N-ylide (4f) and isoquinoline 2-oxide (6) gave the 1-substituted isoquinoline (7) independently of the reaction conditions. Further, 5-alkyl-Meldrum's acids (8a-c) also reacted readily with 1a in acetic anhydride to give the corresponding 2-substituted quinolines (9a-c) in good yields. Heating of 3a, b with conc. hydrochloric acid, 10% hydrochloric acid or methanol containing 10% hydrogen chloride gave 2-methylquinolines (10a, b), 2-quinolineacetic acids (11a, b) or their methyl esters (12a, b), respectively. Similarly, 9a-c afforded 2-alkylquinolines (14a-c) in good yields upon being refluxed with conc. hydrochloric acid.View full abstractDownload PDF (983K) -
YASUMITSU TAMURA, SATOSHI FUKUMORI, AKIMORI WADA, SHIGEHIRO OKUYAMA, J ...1982 Volume 30 Issue 5 Pages 1692-1696
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe photochemical behavior of a number of 2-acyl-3-alkylamino-5, 5-dimethyl-2-cyclohexen-1-ones has been investigated. Irradiation of these systems resulted in δ-hydrogen abstraction by the excited carbonyl oxygen to form a biradical intermediate, which produces the dealkylation product.View full abstractDownload PDF (648K) -
SUSUMU FUNAKOSHI, HARUAKI YAJIMA1982 Volume 30 Issue 5 Pages 1697-1705
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs a starting material for the synthesis of human parathyroid hormone (1-38), a C-terminal-protected eicosapeptide ester (positions 19-38) was synthesized by successive condensation of four peptide fragments; (positions 29-38), (25-28), (22-24) and (19-21).View full abstractDownload PDF (1211K) -
SUSUMU FUNAKOSHI, NOBUTAKA FUJII, HARUAKI YAJIMA, CHOHEI SHIGENO, ITSU ...1982 Volume 30 Issue 5 Pages 1706-1717
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe octatriacontapeptide corresponding to positions 1 to 38 of human parathyroid hormone (hPTH), a half of the whole molecule, was synthesized by assembling 9 peptide fragments in a conventional manner. Arg (mesitylene-2-sulfonyl), a new arginine derivative bearing an acid-labile protecting group, was employed in combination with a new deprotecting procedure with 1 M trifluoromethanesulfonic acid-thioanisole in TFA. The synthetic peptide exhibited an activity of 1400 IU/mg when assayed by the mouse bone adenyl cyclase activity assay.View full abstractDownload PDF (1493K) -
KATSUHIDE MATOBA, MIHOKO SHIBATA, TAKAO YAMAZAKI1982 Volume 30 Issue 5 Pages 1718-1721
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSQuinoline N-oxide was treated with 1H-pyrrole in the presence of acetic anhydride to give 2-(2 [1H] pyrrolyl) quinoline (Ib) in 37.4% yield. In the reaction of Ib and 2-chloroethyl tosylate (V) in acetone catalyzed by potassium hydroxide, 2-(1-(2-tosyloxyethyl)-2 [1H]-pyrrolyl) quinoline (Ic) was obtained. Ic was unstable and cyclized gradually to a quaternary tosylate (VIa), which was reduced with sodium borohydride in methanol to 9, 13-diazagona-1, 3, 5 (10), 14, 16-pentaene (VII), which was identified as its picrolonate.View full abstractDownload PDF (640K) -
NORIKO HONJO, TOKIHIRO NIIYA, YOSHINOBU GOTO1982 Volume 30 Issue 5 Pages 1722-1730
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reactions of 2, 4- (Ia-d) and 2, 5-disubstituted thiazole 3-oxides (Ie-f) with aryl isocyanates (II) were studied. While the reactions of Ia-d with II proceeded smoothly to give bis (5-imidazolyl) disulfides (IV), those of Ie-f with II did not take place. The structures of IV were deduced from their chemical behavior and spectral data. The reaction mechanism of Ia-d with II is discussed.View full abstractDownload PDF (846K) -
YUTAKA YAMAMOTO, AKIHIKO YANAGI1982 Volume 30 Issue 5 Pages 1731-1737
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTrimethylstannyl and bis (trimethylstannyl) derivatives of pyridine, quinoline, and isoquinoline were prepared from the corresponding halo and dihalo (chloro or bromo) derivatives and trimethylstannyl sodium, which was generated in situ from chlorotrimethyl-stannane and sodium. These stannyl derivatives readily underwent iododestannation on treatment with iodine to produce the corresponding iodo and diiodo derivatives of pyridine, quinoline, and isoquinoline, respectively, in good yields.View full abstractDownload PDF (688K) -
SUSUMU FUNAKOSHI, HARUAKI YAJIMA, CHOHEI SHIGENO, ITSUO YAMAMOTO, RIKU ...1982 Volume 30 Issue 5 Pages 1738-1746
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe tetratriacontapeptide amide corresponding to positions 1 to 34 of human parathyroid hormone, H-(hPTH 1-34)-NH2, was synthesized by the solution method. As a deprotecting reagent, 1M trifluoromethanesulfonic acid-thioanisole in trifluoroacetic acid was employed. When mouse bone adenyl cyclase activity was measured, our synthetic active fragment of human PTH exhibited an activity of 3380-4400 IU/mg.View full abstractDownload PDF (1118K) -
KOJI KASUYA, SHOICHI KANDA, TETSUO MISAKI1982 Volume 30 Issue 5 Pages 1747-1752
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA study on the determination of sodium liothyronine in tablets by colorimetry is described. The method is based on the iodine-starch (potato) reaction after ignition of the sample with potassium carbonate. For the ignition procedure, effeotive mixing of the sample and potassium carbonate, each previously pulverized, in an agate mortar was essential if reproducible results were to be obtained. The conditions of the iodine-starch reaction were optimized for application to a dosage level as low as 5 μg of sodium liothyronine in a tablet. The accuracy and recovery of the proposed method are satisfactory for practical pharmaceutical analysis.View full abstractDownload PDF (710K) -
HIROYUKI KANEKI, MITSUYA TANAKA1982 Volume 30 Issue 5 Pages 1753-1759
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAdsorption of β-galactosidase (EC 3. 2. 1. 23), β-glucosidase (EC 3. 2. 1. 21) and β-acetyl-glucosaminidase (EC 3. 2. 1. 30) on agarose substituted with N-(ε-aminohexanoyl)-β-D-galactosylamine, -β-D-glucosylamine, -2-acetamido-2-deoxy-β-D-glucosylamine and -β-D-mannosylamine was studied. All the glycosidases were adsorbed only at low buffer concentration. Although the adsorptions of Taka-diastase and Sanactase glycosidases were non-biospecific, the adsorption required the presence of the glycone as a ligand and the elution patterns in column chromatography were affected by variation of the glycone moiety of the adsorbent. The adsorptions of the enzymes on galactosylamine-agarose were prevented by low concentrations of hexoses and pentoses. The adsorption and desorption of emulsin glycosidase were apparently biospecific considering that the enzyme protein has one binding site for glucoside and one for galactoside, although the biospecificity was inexplicable in view of the large K1 values of the spacerligand compounds.View full abstractDownload PDF (864K) -
HIROKO KAWANO, MIEKO OTANI, KEIKO TAKEYAMA, YUICHI KAWAI, TADANORI MAY ...1982 Volume 30 Issue 5 Pages 1760-1765
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(1) Ergothioneine is contained as a component of the organella membranes in the rat liver, and is liberated by heat treatment or dithiothreitol treatment. The amount of bound form increases with aging up to 11 weeks of age, and then decreases. All of the ergothioneine measured by the normal determination procedures can be considered to be free form. (2) Ergothioneine is bound to proteins in the blood plasma, but is present in free form in erythrocytes. (3) Biosynthesis of ergothioneine from amino acids in rats was not detectable. Ergothioneine is ingested from the diet and accumulated in the body. (4) When dietary ergothioneine is restricted for 18 weeks, the amount in the liver falls to a threshold value but apparently does not fall further, and no deficiency symptoms are observed. (5) Experimental ergothioneine-free rats were successfully produced in the second generation (born to parent rats fed on ergothioneine-free diet).View full abstractDownload PDF (682K) -
HIDEKO ARICHI, YOSHIYUKI KIMURA, HIROMICHI OKUDA, KIMIYE BABA, MITSUGI ...1982 Volume 30 Issue 5 Pages 1766-1770
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of the roots of Polygonum cuspidatum SIEB. et ZUCC. ("Kojo-kon" or "Itadori-kon" in Japanese) and its stilbene components (resveratrol and piceid) on lipid metabolism in rats and mice (higher animals) were investigated. Resveratrol and piceid inhibited the deposition of triglyceride and cholesterol in the liver of rats fed corn oil-cholesterol-cholic acid mixture. Piceid reduced the serum triglyceride and low density lipoprotein-cholesterol (LDL-ch) levels, and atherogenic index [total cholesterolhigh density lipoprotein-cholesterol (HDL-ch)/HDL-ch] in the oil mixture-fed rats. It was found that intraperitoneal or oral administration of resveratrol or piceid reduced triglyceride synthesis from 14C-palmitate in the liver of mice. In contrast, these stilbene components did not affect hormone-induced lipolysis in fat cells from rat eqididymal adipose tissue.View full abstractDownload PDF (626K) -
YOSHIFUMI MATSUDA, KYOSUKE MIYAZAKI, YUKIO FUJIMOTO, YOSHIO HOJIMA, HI ...1982 Volume 30 Issue 5 Pages 1771-1775
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe substrate specifioities of some glandular and plasma kallikreins, bovine trypsin and plasmin, and boar acrosin were investigated using five tripeptidyl-p-nitroanilides and ten arginine and lysine ester derivatives as substrates. Of the substrates examined, N-α-benzoyl-L-arginine methyl and ethyl esters (Bz-Arg-Me and Bz-Arg-Et) and N-α-acetyl-L-arginine methyl ester (Ac-Arg-Me) were the most effective for the pancreatic and intestinal kallikreins, while N-α-tosyl-L-arginine methyl ester (Tos-Arg-Me) and Bz-Arg-Me were effectives as substrates for the human salivary and guinea-pig coagulating gland kallikreins, respectively. Ac-Arg-Me and N-α-acetyl-glycyl-L-lysine methyl ester (Ac-Gly-Lys-Me) were also good substrates for the boar acrosin. All of the tripeptidyl-p-nitroanilide substrates examined were hydrolyzed relatively ineffeotively by glandular kallikreins and boar acrosin. However, D-valyl-L-leucyl-L-arginine-p-nitroanilide (Val-Leu-Arg-pNA) and D-prolyl-L-phenylalanyl-L-arginine-p-nitroanilide (Pro-Phe-Arg-pNA) were found to be moderately useful substrates for various kallikreins and related enzymes.View full abstractDownload PDF (653K) -
TAKASHI ABIKO, HIROSHI SEKINO1982 Volume 30 Issue 5 Pages 1776-1783
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWe have replaced the Ac-Ser residue of bovine thymosin α1 (position 1) with Ser in order to examine the resulting change in immunological effect on the low resette-forming capacity with sheep erythrocytes of cells from a lipoid nephrosis patient. The deacetyl-thymosin α1 was synthesized by the solution method. For the synthesis of the protected octaeicosapeptide, five peptide fragments were prepared by the stepwise elongation method with N-ethoxycarbonyl-2-ethoxy-1, 2-dihydroquinoline as a coupling reagent. The condensations of the fragments were achieved by Rudinger's azide procedure. Finally, all protecting groups were removed by HF treatment followed by catalytic hydrogenation. The in vitro addition of the synthetic deacetyl-thymosin α1 at a dose of 100 μg/ml was able to restore the rosette-forming capaoity with sheep erythrocytes of lipoid nephrosis cells to normal levels. Our preparations of deacetyl-thymosin α1 and thymosin α1 were found to be equally active in cases of lipoid nephrosis.View full abstractDownload PDF (1116K) -
HARUKI YAMADA, YUKIO OHSHIMA, TOSHIO MIYAZAKI1982 Volume 30 Issue 5 Pages 1784-1791
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe extracellular polysaccharide fraction of Absidia cylindrospora (ACE), which has been used as an immunogen in immunochemical studies of Mucorales polysaccharide, showed marked heterogeneity of its mannoheteroglycans. ACE was classified into mannantype and fucomannan-type fraotions of sequential separation using affinity chromatography on concanavalin-A (con-A) Sepharose, ion exchange chromatography on diethylaminoethyl Sephadex, zone electrophoresis and gel filtration on Sephadex G-100. Serological reactivity to anti-ACE appeared in the con-A bound and high-mannose content fraction. By methylation analysis and proton magnetic resonanoe studies of each polysaccharide, it was confirmed that the fucomannan-type fraction mainly consisted of α (1→6) linked mannopyranosyl residues and fucopyranosyl non-reducing ends, whereas the mannan-type fraction consisted of (1→2) linked mannopyranosyl residues and mannopyranosyl non-reducing ends. These results were similar to those for mannoheteroglycans from A. cylindrospora mycelium. These results indicated that ACE of the immunogen contained serologically active mannan and fucomannan.View full abstractDownload PDF (920K) -
Studies on Scutellariae Radix. VI. Effects of Flavanone Compounds on Lipid Peroxidation in Rat LiverYOSHIYUKI KIMURA, HIROMICHI OKUDA, TADATO TANI, SHIGERU ARICHI1982 Volume 30 Issue 5 Pages 1792-1795
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCompounds (I and II) which inhibited lipid peroxides formation (in in vitro experiments) were isolated together with various flavonoids from the roots of Scutellaria baicalensis GEORGI. From the analytical and physical data, compounds I and II were identified as (2S)-2', 5, 6', 7-tetrahydroxy-flavanone and (2R, 3R)-2', 3, 5, 6', 7-pentahydroxy-flavanone, respectively. Compound II inhibited the lipid peroxide formation by Fe2+ and ascorbic acid. Compounds I and II inhibited the lipid peroxide formation induced by adenosine diphosphate and reduced nicotinamide adenine dinucleotide phosphate in rat liver homogenate.View full abstractDownload PDF (523K) -
YOSHINOBU NAKAI, KEIJI YAMAMOTO, KATSUHIDE TERADA, HIDETOSHI HORIBE1982 Volume 30 Issue 5 Pages 1796-1802
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe partition coefficients of p-nitrophenol between 0.05N HCl and CHCl3 were measured with or without tri-O-methyl-β-cyclodextrin (methyl-β-CD) at 15.5, 20.0, and 25.0°C. The partition coefficients increased linearly with methyl-β-CD concentration. In the presence of 3.00×10-2M methyl-β-CD, the value was about 2.5 times larger than that measured in the absence of methyl-β-CD. Methyl-β-CD was not detected in the aqueous phase by polarimetry, and most of the methyl-β-CD molecules were present in the CHCl3 phase. The increase of the partition coefficients can be interpreted in terms of 1 : 1 complex formation between methyl-β-CD and p-nitrophenol. The complexes of methyl-β-CD and p-nitrophenol in the aqueous solution and the CHCl3 solution were studied quantitatively by ultraviolet absorption measurements. The formation of inclusion complex in D2O was also investigated by proton magnetic resonance spectroscopy.View full abstractDownload PDF (731K) -
YUKIO SATO, MICHIKO YOKOO, SHUICHI TAKAHASHI, TAKEO TAKAHASHI1982 Volume 30 Issue 5 Pages 1803-1810
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe photolysis of riboflavine with a low-intensity light source was investigated. Biphasic rate curves were obtained ; that is, an induction period was observed before the reaction rate reached its maximum value. The duration of the initial phase depended on the temperature and the concentration of riboflavine. The molecular associations of isoalloxazine nuclei may be responsible for such biphasic photolysis. The addition of xanthine derivatives to an aqueous solution of riboflavine reduced the rate of photolysis. Although the rate was reduced most effectively by theophylline, it appears that the interaction between riboflavine and theophylline differs considerably from that in other systems, i.e., caffeine, theobromine, and hypoxanthine systems.View full abstractDownload PDF (843K) -
YOSHINOBU NAKAI, EIHEI FUKUOKA, SHINICHIRO NAKAJIMA, MASAMI MORITA1982 Volume 30 Issue 5 Pages 1811-1818
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA computer program for the determination of the degree of crystallinity and the disorder parameter in lactose based on Ruland's method, one of the X-ray diffraction methods, was written. The correctness of the program was confirmed by comparing the computed results with those caloulated by the usual Ruland's method and Herman's method using several samples of lactose with different crystallinities. A series of integral upper limits was determined by rearranging the equation presented by Ruland. The degree of crystallinity and the disorder parameter in crystalline lactose which was used as the 100% crystalline standard in the other methods were estimated as ca. 70% and ca. 3.5 A2, respectively. The effects of the normalization constant on the calculated results were rather small. However, the effects of integral upper limits on those results were large. A series of integral upper limits seems to be a very important factor for crystallinity determination by Ruland's method.View full abstractDownload PDF (791K) -
YORISHIGE IMAMURA, KAZUHIKO ARIMORI, MASANOBU SONODA, HISASHI ICHIBAGA ...1982 Volume 30 Issue 5 Pages 1819-1823
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of salicylic acid on the hypoglycemic activity and blood carbutamide concentration after oral administration of carbutamide was investigated in rabbits. Salicylic acid was found to enhance the hypoglycemic activity, while on the other hand, it was found to deorease the blood carbutamide concentration. Salicylic acid markedly decreased the in vivo binding of carbutamide to rabbit plasma proteins, and caused a significant increase in the plasma concentration of unbound carbutamide, despite a significant decrease in the plasma concentration of total carbutamide. These results lead us to conclude that the displacement of carbutamide from its plasma protein binding sites by salicylic acid produces both the enhanced hypoglycemic activity and the decreased blood carbutamide concentration.View full abstractDownload PDF (572K) -
HIROYUKI KOJIMA, HIROSHI KIWADA, YURIKO KATO1982 Volume 30 Issue 5 Pages 1824-1830
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dissolution properties and physico-chemical properties of three polymorphic forms of (α-bromoisovaleryl) urea are reported. Form II transformed to form I repidly in water at 37°C, but this transition was delayed by 0.25% gelatin. The solubility of form II was 50% higher than that form I. The transition temperatures of form II to form I, and form III to form I were 70.2°C and 11.4°C, respectively, as determined by measurements of dissolution rates and solubilities. The enthalpy values, ΔHsol and ΔHdiss, of the polymorphs were calculated. The thermodynamic values of form II and form III for the conversion to form I were calculated from these values, i.e. heats of transition (ΔHtrans), differences of free energy at 37°C (ΔGT), differences of entropy at 37°C (ΔST), and entropy changes at transition temperatures (ΔStrans). The differences of free energy, which may affect the bioavaliabilities of polymorphs, and the ΔStrans values were found to be fairly small.View full abstractDownload PDF (664K) -
HIROYUKI KOJIMA, HITOSHI NIIMURA, HIROSHI KIWADA, YURIKO KATO1982 Volume 30 Issue 5 Pages 1831-1836
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA simple and sensitive determination method for (α-bromoisovaleryl) urea in plasma was developed by using gas-liquid chromatography with an electron capture detector, (α-Bromoisovaleryl) urea was extracted from plasma with ethyl ether and ethanol in a ratio of 5 : 1 (volume); the recovery was 97.5%. The plasma concentrations were determined by the internal standard GLC-ECD method without further clean-up by column chromatography. The detection limit was about 0.5 μg/ml in 0.1 ml plasma. In order to determine the effect of polymorphism (form I, form II, and form III) of (α-bromoisovaleryl)-urea on the bioavailiabilities, plasma levels in rats after intraduodenal administration were investigated. The areas under the blood concentration curves (AUC) and the mean dissolution times (MDT) were calculated to determine the extent of bioavailability and the rate of bioavailability, respectively. The results indicated that the polymorphic states of (α-bromoisovaleryl) urea did not show significantly different bioavailabilities.View full abstractDownload PDF (614K) -
YOSHIAKI KAWASHIMA, SHAN YANG LIN, MASAFUMI NAITO, HIDEO TAKENAKA1982 Volume 30 Issue 5 Pages 1837-1843
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSodium theophylline monohydrate was precipitated from ethylene diamine solution of theophylline by adding aqueous sodium chloride solution to the system with or without ethanol. The dried precipitates were redispersed in the filtrate without ethanol and were agglomerated with water liberated from the system by adding chloroform and ethanol to the filtrate with agitation. The sedimentation velocity of the agglomerated precipitates and their sedimentation volume at equilibrium were investigated to identify a suitable composition of the medium for agglomeration by gradually increasing the chloroform fraction in the medium. The sedimentation volume slightly increased before dropping drastically at 41% chloroform fraction, at which the precipitates were microagglomerated after passing through a flock stage of high bulk volume. At 56% chloroform fraction, the sedimentation volume sharply decreased again because of secondary agglomeration of the microagglomerates. The sedimentation velocity of the agglomerated precipitates increased with increasing chloroform fraction of the medium in the range above 41%. The agglomerate size increased drastically when the secondary agglomeration occurred. No changes in the sizes and shapes of the elemental crystals were found even after agglomeration. A triangular phase diagram was obtained to described a suitable composition of the medium for agglomeration. It was also proved that simultaneous agglomeration with crystallization was possible in a mixture of four liquids, i.e. ethylenediamine solution of theophylline, aqueous solution of sodium chloride, ethanol and chloroform, with a suitable composition.View full abstractDownload PDF (1169K) -
HIROSHI SAITO, TAKASHI UEYAMA, NOBUKO NAKA, JUN YAGI, TOSHIHIKO OKAMOT ...1982 Volume 30 Issue 5 Pages 1844-1850
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPharmacological properties, especially, analgesic, antipyretio, antiinflammatory, sedative and antidiuretic activities, of ignavine, one of the main alkaloids in Aconite root, are discussed on the basis of the results of blind screening. Ignavine showed antiinflammatory activity in the acetic acid-induced writhing and carrageenin paw edema tests at doses of 50 and 100 mg/kg p.o., which did not produce undesirable effects such as sedation, motor incoordination, muscle relaxation, hypothermia, ulceration or antidiuresis. Pharmacological properties of mesaconitine are also discussed; mesaconitine showed antiinflammatory, antipyretic and weak sedative activities.View full abstractDownload PDF (753K) -
TOSHIHIRO NOHARA, YOSHIKO ITO, HARUKO SEIKE, TETSUYA KOMORI, MINEHIRO ...1982 Volume 30 Issue 5 Pages 1851-1856
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeven compounds have been isolated from whole plants of Paris quadriforia L. and their chemical structures characterized as follows ; pennogenin (1), pennogenin 3-O-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→4)]-β-D-glucopyranoside (2), pennogenin 3-O-α-L-rhamnopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→4)-[α-L-rhamno-pyranosyl-(1→2)]-β-D-glucopyranoside (3), 22-hydroxyfurostanol 3, 26-O-bisglycoside corresponding to 3 (4), 1-dehydrotrillenogenin (5), ecdysterone (10) and kaempferol 3-O-β-D-glucopyranosyl-(1→4)-β-D-glucopyranoside (11). In addition, a stimulative effect of 3, one of the major components, on isolated bull frog heart was observed.View full abstractDownload PDF (709K) -
CHING-SHING LEE, YUICHI HASHIMOTO, KOICHI SHUDO, TOSHIHIKO OKAMOTO1982 Volume 30 Issue 5 Pages 1857-1859
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo potent mutagens, 2-amino-3-methylimidazo [4, 5-f] quinoline and 2-amino-3, 4-dimethylimidazo [4, 5-f] quinoline, were synthesized.View full abstractDownload PDF (474K) -
OSAMU MIYASHITA, KOICHI MATSUMURA, HIROSHI SHIMADZU, NAOTO HASHIMOTO1982 Volume 30 Issue 5 Pages 1860-1864
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1-Acyl- and 1, 3-diacyl-5-alkoxycarbonyl-5-fluoro-6-substituted-5, 6-dihydrouracils were synthesized for study as a class of pro-drugs of 5-fluorouracil (5-FU).View full abstractDownload PDF (559K) -
KENICHI TANJI, TAKAO SAKAMOTO, HIROSHI YAMANAKA1982 Volume 30 Issue 5 Pages 1865-1867
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the palladium-catalyzed cross-coupling reaction of halopyrimidines with terminal acetylenes, 2- and 4-chloropyrimidines can be used as starting compounds, though their reactivity is inferior to that of 2- and 4-iodopyrimidines. The conversion of the 2- and 4-alkynylpyrimidines thus obtained into the corresponding pyrimidinylmethyl ketones was successfully achieved by consecutive treatment with piperidine and oxalic acid dihydrate.View full abstractDownload PDF (466K) -
TERUYOSHI MARUNAKA, YUKIHIKO UMENO1982 Volume 30 Issue 5 Pages 1868-1871
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS5-Fluoro-5'-deoxyuridine and ethyl (±)-6-n-butoxy-5-fluoro-5, 6-dihydrouracil-γ-5-carboxylate are new pro-drug forms of 5-fluorouracil that have been developed as antitumor agents. A gas chromatographic-mass fragmentographic determination of the active substance 5-fluorouracil in biological materials following administration of each compound was established. The detection limit for 5-fluorouracil was 1 ng/ml of plasma and 1-5 ng/g of wet weight of visceral tissues.View full abstractDownload PDF (513K) -
RIICHI TAWA, SHINGO HIROSE, KENZO ADACHI1982 Volume 30 Issue 5 Pages 1872-1875
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA method has been developed for the determination of the fraction of a single species in a binary mixture of tertiary amines, by measurement of the pseudo first-order reaction rates for decomposition of the π-complexes with tetracyanoethylene. The initial absorbances at three wavelengths (u, v and w) and their sum in a simplified complementary tristimulus colorimetry were calculated by a numerical method. The color points of the reaction solution at the initial time were calculated, so that the fraction of as single species in a mixture of tertiary amines could be evaluated.View full abstractDownload PDF (465K) -
TOYOZO UNO, KAZUO OKUMURA, YOSHIHIRO KURODA1982 Volume 30 Issue 5 Pages 1876-1879
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structure of the red product of the Fujiwara reaction was investigated by using chloroform as a gem-polyhalogen compound. Isolation of the product followed by nuclear magnetic resonance and mass spectroscopic analysis revealed the red chromophore to be the sodium salt of N1, N2-bis [(1E, 3E)-4-formyl-1, 3-butadien-1-yl] formamidine. The structure of the red products formed from trichloroacetic acid and chloral hydrate were also investigated. High-performance liquid chromatography analysis and mass spectra showed that both products have the same structure as that from chloroform. Since the red product from benzotrichloride has an analogous spectrum, it is concluded that the structure of the red produots formed from the series of trichloroalkyl compounds (RCCl3) is the nitrogenated polyene produced by the ring cleavage of two pyridine rings.View full abstractDownload PDF (471K) -
TAKAHARU MIZUTANI, HITOMI KIMURA, KAORUKO WAGI, TAMAMI OKAYAMA1982 Volume 30 Issue 5 Pages 1880-1883
Published: May 25, 1982
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe primary immune response in young adult mice to sheep red blood cells was studied by following the effects of anti-IgM or anti-Fc sera on the number of plaqueforming cells for IgM (dPFC) and IgG (iPFC) in the spleen. The number of dPFC in the case of administration of anti-IgM serum at 1 h before antigen injection was significantly decreased to 3.7±0.9/106 spleen cells in comparison with the value of control serum (69.0±15.7/106 spleen cells). However, the numbers of iPFC in the cases of both anti-IgM or control sera were similar. From these results, we suppose that progenitors of IgM-producing cells are different from progenitors of IgG-producing cells in adult mice.View full abstractDownload PDF (524K)