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Volume 33, Issue 4
Displaying 1-50 of 67 articles from this issue
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KATSUO HATAYAMA, SADAKAZU YOKOMORI, YUTAKA KAWASHIMA, RYUICHI SAZIKI, ...1985 Volume 33 Issue 4 Pages 1327-1333
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFive dihydrochalcone derivatives, 2'-carboxymethoxy-4, 4'-bis (3-methyl-2-butenyloxy) dihydrochalcone (M-6-b), 2', 4-bis (carboxymethoxy)-4'-(3-methyl-2-butenyloxy) dihydrochalcone (M-2), 2', 4-bis (carboxymethoxy)-4'-(3-carboxy-2-butenyloxy) dihydrochalcone (M-1-a), 2', 4-bis (carboxymethoxy)-4'-(3-hydroxymethyl-2-butenyloxy) dihydrochalcone (M-1-b), and 2'-carboxymethoxy-4-hydroxy-4'-(3-methyl-2-butenyloxy) dihydrochalcone (M-4-b), which are the main metabolites in rats of a new anti-ulcer drug "sofalcone"(2'-carboxymethoxy-4, 4'-bis (3-methyl-2-butenyloxy) chalcone) were synthesized and the anti-ulcer activities of the major metabolites in humans, M-6-b, M-2, and M-1-a, were examined by Shay's and Takagi's methods and also by the use of rats with histamine-induced ulcer. The most active compound was M-6-b, which showed activity equal to or slightly weaker than that of sofalcone.View full abstractDownload PDF (752K) -
KENKICHI TAKAUCHI, AKIRA TOKUMURA, JUNICHI YOSHIDA, TAKEHISA IWAMA, YA ...1985 Volume 33 Issue 4 Pages 1334-1341
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe alkaline hydrolysate of "Depressor-I", an antihypertensive phospholipid occurring in the acetone-soluble fraction of bovine brain, was [3H] acetylated and applied to an alumina column. Various [3H] acetylated compounds were eluted. Among the major fractions, the eluates with hexane and hexane-benzene (9 : 1, 7 : 3 and 5 : 5, v/v) mixtures contained labile compounds which decomposed on standing for one month. Gas chromatography-mass spectrometry was carried out with the corresponding sample obtained in a "cold"experiment, and diosgenin acetate, a sapogenin, was detected besides cholesteryl acetate. A new class of phospholipid containing steroidal components is proposed.View full abstractDownload PDF (831K) -
KUNIO SAITO, SHIGEYOSHI SAIJO, KEISHI KOTERA, TADAMASA DATE1985 Volume 33 Issue 4 Pages 1342-1350
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new chiral bisphosphine, (2R, 3S)-1, 2-bis (diphenylphosphino)-3-tBoc-aminobutane (RS-5), was prepared from L-threonine. Mesylation of tBoc-L-threonine methyl ester (2) and subsequent reduction with sodium borohydride gave the alcohol (10), which was treated with potassium carbonate to afford a key intermediate, (2S, 3S)-1-tBoc-3-methyl-2-aziridinemethanol (SS-7b). Mesylation of SS-7b, followed by treatment with sodium diphenylphosphide afforded the new chiral bisphosphine (RS-5). The structure of RS-5 was confirmed by the X-ray analysis of its crystalline CuCl complex (RS-12). The cationic rhodium (I) complexes prepared from RS-5 and RS-12 are efficient asymmetric hydrogenation catalysts for N-acyldehydroamino acids, giving (S)-N-acylamino acids in high optical yields (83-94% ee).View full abstractDownload PDF (872K) -
TAKEO HIGASHINO, MASUMI TAKEMOTO, EISAKU HAYASHI1985 Volume 33 Issue 4 Pages 1351-1359
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Aroylquinazolines (3) were prepared in good yields by alkaline hydrolysis of α-aryl-4-quinazolinylmethyl benzoates (15), followed by oxidation. The reaction of 3 with sodium hydroxide in dimethyl sulfoxide (DMSO) was found to proceed in two ways. One path is the aryl migration to lead to 4-aryl-3, 4-dihydro-4-quinazolinecarboxylic acids (4), and the other is the fission of the C4-CO bond to yield quinazoline (5) and aroic acids (6). Potassium ferricyanide oxidized the carboxylic acids 4 to the corresponding 4-arylquinazolines (14) with elimination of carbon dioxide. Reaction of 4-benzoylquinazoline (3a) with methylmagnesium iodide did not result in the migration, but instead yielded of α-methyl-α-phenyl-4-quinazolinemethanol (18) and 3, 4-dihydro-α, 4-dimethyl-α-phenyl-4-quinazolinemethanol (19).View full abstractDownload PDF (798K) -
YUKIHIKO TOMIOKA, KIMIKO OHKUBO, MOTOYOSHI YAMAZAKI1985 Volume 33 Issue 4 Pages 1360-1366
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reactions of 3-, 5-, 6-, 7- and 8-nitroquinolines, 1-or 2-nitronaphthalene and m-substituted (CF3, COCH3 and COC6H5) nitrobenzenes with ethyl cyanoacetate and potassium hydroxide in dimethylformamide, followed by hydrolysis of the reaction mixture with hydrochloric acid or sodium hydroxide, gave the corresponding o-aminoaroylnitriles.View full abstractDownload PDF (649K) -
HIROSHI KOHDA, WAKAKO TOKUMOTO, KIYOE SAKAMOTO, MICHIKO FUJII, YUKO HI ...1985 Volume 33 Issue 4 Pages 1367-1374
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe MeOH extract of Ganoderma lucidum has an inhibitory action on histamine release from rat mast cells. From the physiologically active fraction of the extract, along with the known triterpenes ganoderic acids A and B, two new triterpenes were isolated and named ganoderic acids C and D. The structures of ganoderic acids C and D were determined to be 3β, 7β, 15α-trihydroxy-11, 23-dioxo-5α-lanost-8-en-26-oic acid and 7β-hydroxy-3, 11, 15, 23-tetraoxo-5α-lanost-8-en-26-oic acid respectively. Ganoderic acids C and D were shown to inhibit histamine release from rat mast cells. Quantitative analysis of these triterpenes was performed for the purpose of crude drug quality control.View full abstractDownload PDF (807K) -
TSUNEO ITOH, TOSHIHIKO IMINI, HARUO OGURA, NORIO KAWAHARA, TAKAKO NAKA ...1985 Volume 33 Issue 4 Pages 1375-1379
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new and convenient synthesis of 1, 3-dialkylpyrido [2, 3-d] pyrimidine-2, 4 (1H, 3H)-diones from 6-allylamino-and 6-(substituted allyl) aminouracils by PdCl2-CuCl-O2-catalyzed oxidative cyclization is described. Further, 1, 3-dimethylpyrido [2, 3-d] pyrimidine 2, 4 (1H, 3H)-dione (4a) was prepared by the reaction of 6-allylamino-1, 3-dimethyluracils (3a) with (AcO)2 Pd and by the thermal cyclization of 3a.View full abstractDownload PDF (583K) -
YOSHIHIRO NITTA, YASUSHI ARAKAWA1985 Volume 33 Issue 4 Pages 1380-1386
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of carboxylic acid esters with an excess of p-toluenesulfonic acid gave the corresponding p-toluenesulfonates. The mechanism of the transesterification is discussed.View full abstractDownload PDF (742K) -
YINGJIE CHEN, TADAHIRO TAKEDA, YUKIO OGIHARA1985 Volume 33 Issue 4 Pages 1387-1394
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new saponins were isolated from the fruits of Xanthoceras sorbifolia BUNGE. The structures of these saponins were deduced on the basis of chemical and spectral evidence as 22-O-acetyl-21-O-(4-O-acetyl-3-O-angeloyl)-β-D-fucopyranosyl-3-O-[β-D-glucopyranosyl- (1→2)-β-D-glucuronopyranosyl] protoaescigenin (7), 22-O-acetyl-21-O- (3, 4-di-O-angeloyl) -β-D-fucopyranosyl-3-O- [β-D-glucopyranosyl- (1→2)-β-D-glucuronopyranosyl] protoaescigenin (8), 28-O-acetyl21-O- (4-O-acetyl-3-O-angeloyl) -β-D-fucopyranosyl-3-O- [β-D-glucopyranosyl- (1→2) -β-D-glucuronopyranosyl] protoaescigenin (9) and 28-O-acetyl-21-O-(3, 4-di-O-angeloyl) -D-fucopyranosyl-3-O- [β-D-glucopyranosyl-(1→2)-β-D-glucuronopyranosyl] protoaescigenin (10). The names "bunkankasaponins A, B, C and D"are proposed for 7, 8, 9 and 10, respectively.View full abstractDownload PDF (860K) -
TAKEO HIGASHINO, MASUMI TAKEMOTO, AKIRA MIYASHITA, EISAKU HAYASHI1985 Volume 33 Issue 4 Pages 1395-1399
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWhen mixtures of 7-chloro-3-phenyl-3H-1, 2, 3-triazolo [4, 5-d] pyrimidine (4), aromatic aldehydes (5), and a catalytic amount of 1, 3-dimethylbenzimidazolium iodide were refluxed in tetrahydrofuran (THF) in the presence of sodium hydride, 7-aroyl-3-phenyl-3H-1, 2, 3-triazolo [4, 5-d]-pyrimidines (1) were obtained in moderate yields. Although the yield was unsatisfactory, the reaction of 1 with sodium hydroxide in dimethyl sulfoxide (DMSO) resulted in aryl migration, followed by ready oxidative decarboxylation, giving 7-aryl-3-phenyl-3H-1, 2, 3-triazolo [4, 5-d]-pyrimidines (3) by way of 7-aryl-6, 7-dihydro-3-phenyl-3H-1, 2, 3-triazolo [4, 5-d] pyrimidine-7-carboxylic acids (2). When the reaction mixture of 1 with sodium hydroxide was directly subjected to potassium ferricyanide oxidation, 1 was easily convertible to 3 in good yield.View full abstractDownload PDF (505K) -
HARUHISA KIZU, MICHIYO KOSHIJIMA, MASATOMI HAYASHI, TSUYOSHI TOMIMORI1985 Volume 33 Issue 4 Pages 1400-1406
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour triterpene glycosides, named Kizuta saponins K4 (I), K5 (II), K7 (III) and K7C (IV), were isolated from the stem and bark of Hedera rhombea BEAN (Araliaceae). On the basis of chemical and physicochemical evidence, they were characterized as follows : I, 3-O-acetyl-20 (S)-dammar-24-ene-3β, 6α, 20, 26-tetraol 26-O-β-D-glucopyranoside ; II, 3-oxo-20 (S) -dammar-24-ene-6α, 20, 26-triol 26-O-β-D-glucopyranoside ; III, 20 (S) -dammar-24-ene-3β, 6α, 20, 26-tetrol 26-O-β-D-glucopyranoside ; IV, 20 (S) -dammar-24-ene-3β, 20, 26-triol 3, 26-di-O-β-D-glucopyranoside.View full abstractDownload PDF (832K) -
CHIHIRO UEDA, HIDENOBU OHMORI, KYOJI UENO, YUKA HAMADA, SHINJI TATSUMI ...1985 Volume 33 Issue 4 Pages 1407-1413
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAnodic oxidation of several 4-and 4'-substituted benzanilides in the presence of a strong base, 1, 8-diazabicyclo [5. 4. 0] undecene-7 (DBU), was investigated by cyclic voltammetry and controlled potential electrolysis at a glassy carbon electrode in acetonitrile. The original voltammetric peak of the anilides shifted to less positive potentials on addition of DBU. The magnitude of the cathodic shift was linearly correlated with the Hammett σ values of the 4'-substituents, and the oxidation process could be explained in terms of a one-electron abstraction from the anilide which exists as a hydrogen-bonded complex with the base. Controlled potential electrolysis of the anilides under basic conditions gave three different types of dimers depending on the nature of the 4'-substituent, X. When X=alkyl group, the 4- (N-benzoyl-N-phenyl) amino-2, 5-cyclohexadienone derivative (2) was obtained. Diphenylamine derivatives (3) and (4) produced through N-2' and N-4' dimerization were the main products when X=hetero atom and X=H, respectively. A sandwich-type approach of the radicals formed by the initial one-electron transfer can account for these results.View full abstractDownload PDF (700K) -
TAKUO KOSUGE, HITOSHI ISHIDA, ATSUHIRO INABA, HARUO NUKAYA1985 Volume 33 Issue 4 Pages 1414-1418
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn efficient synthesis of 4-and 6-bromooxindoles, previously unknown compounds, from 6-and 4-amino-2-nitrotoluenes and the transformation of 6-bromooxindole to 3-acylated derivatives are described.View full abstractDownload PDF (646K) -
HITOSHI TANAKA, MASAYOSHI SHIBATA, KAZUO OHIRA, KAZUO ITO1985 Volume 33 Issue 4 Pages 1419-1423
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe flavonolignan (±)-silybin (1), having an antihepatotoxic activity, has been synthesized via a key intermediate (9), which was prepared from readily available starting materials (2) and (3). The aldehyde (9) was transformed to the methoxymethyl ether (10), which was condensed with an acetophenone derivative (11) to yield the chalcone (12). Oxidation of the chalcone (12) with alkaline hydrogen peroxide, followed by treatment of the resulting epoxide (13) with hydrochloric acid afforded (±)-1.View full abstractDownload PDF (669K) -
TAKUO OKUDA, KAZUKO MORI, TSUTOMU HATANO1985 Volume 33 Issue 4 Pages 1424-1433
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe determination of relative astringency (RA) and relative affinity to methylene blue (RMB), based on those of geraniin (RAG and RMBG), shows good reproducibility with small amounts of samples for the estimation of the tannin content of plant extracts, and has been applied to the evaluation of the basal activity of 84 tannins and related compounds. The values obtained for polyphenols of lower molecular weight, which are not regarded as tannins, were zero or almost zero. An increase of these two values of up to about 1.3-1.4 times with increase of molecular weight of polyphenols (particularly such increase due to galloylation) was observed for each type of tannin tested. The RMBG determination gives values somewhat larger than the RAG values for hydrolyzable tannins, and rather smaller than the RAG values for condensed tannins.View full abstractDownload PDF (887K) -
MIYOJI HANAOKA, SINKYU KIM, MITSURU INOUE, KAZUYOSHI NAGAMI, YASUJI SH ...1985 Volume 33 Issue 4 Pages 1434-1443
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA simple and convenient transformation of berberine (1) into trans-, cis-, and unsaturated benzindenoazepines through regioselective C14-N bond cleavage of 8, 14-cycloberbines is described. Acidic treatment of the 8, 14-cycloberbine (2) effected regioselective ring opening to afford the trans-and cis-benzindenoazepines (7a and 7b) as the kinetically and thermodynamically controlled products, respectively. Dehydration of their N-methyl derivatives (11a and 11b) gave the unsaturated benzindenoazepine (20), which was obtained more efficiently from the 8, 14-cycloberbine (2) by treatment with p-toluenesulfonic acid in benzene followed by N-methylation. Similarly, the ring D-inverted 8, 14-cycloberbine (23) was converted to the corresponding trans-, cis-, and unsaturated benzindenoazepines (24a, 24b, and 27, respectively).View full abstractDownload PDF (1100K) -
TOHRU KIKUCHI, SATOKO MATSUDA, SHIGETOSHI KADOTA, TAKAAKI TAI1985 Volume 33 Issue 4 Pages 1444-1451
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new sesquilignans, named hedyotol-A, -B, -C, and -D, were isolated from the leaves of Hedyotis lawsoniae, along with four known lignans. The structures of these novel lignans were determined on the basis of spectroscopic and chemical evidence.View full abstractDownload PDF (826K) -
HIROMI KOBAYASHI, HIROKO KARASAWA, TOSHIO MIYASE, SEIGO FUKUSHIMA1985 Volume 33 Issue 4 Pages 1452-1457
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new phenylpropanoid glycosides, named cistanosides E (III) and F (IV), were isolated from Cistanchis Herba, the whole plant of Cistanche salsa (C. A. MEY.) G. BECK (Orobanchaceae), together with two known lignan glycosides, liriodendrin (I) and (+)-syringaresinol O-β-D-glucopyranoside (II). The structures of III and IV were determined to be 2-(4-hydroxy-3-methoxyphenyl) ethyl O-α-L-rhamnopyranosyl-(1→3)-O-β-D-glucopyranoside and α-L-rhamnopyranosyl (1→3)-O-(4-O-caffeoyl)-D-glucopyranose, respectively, on the basis of chemical and spectral data.View full abstractDownload PDF (656K) -
TAKUO AOYAMA, TOSHIYUKI OKUTOME, TOYOO NAKAYAMA, TAKASHI YAEGASHI, RYO ...1985 Volume 33 Issue 4 Pages 1458-1471
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSVarious amidinonaphthols and their acyl derivatives were synthesized and evaluated for inhibitory activities against trypsin, plasmin, kallikrein, thrombin, Clr and Cls, as well as against in vitro complement-mediated hemolysis. 6-Amidino-2-naphthyl 4-guanidinobenzoate (74, FUT-175) was found to have potent inhibitory activities, particularly against trypsin (IC50 : 0.02 μM), Clr (IC50 : 0.1 μM) and Cls (IC50 : 0.02 μM), and to be highly effective in inhibiting the complement-mediated hemolysis (IC50 : 0.03μM). FUT-175, furthermore, showed considerable effectiveness in the systemic Forssman shock reaction, in which involvement of the complement system as the pathogenetic factor is well established.View full abstractDownload PDF (1048K) -
HIROSHI WADA, SHINICHI KODATO, MASATOSHI KAWAMORI, TAMIO MORIKAWA, HID ...1985 Volume 33 Issue 4 Pages 1472-1487
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDerivatives of dehydroabietic acid (1) having a hydrophilic moiety (such as amino, carbamoyl, carbamoyloxy, ureido, sulfamoyl, or sulfo) at positions 12 and/or 18 of the dehydroabietane nucleus were prepared and tested for antiulcer activity by means of antisecretory and antipepsin assays in rats. Among these compounds, the salts of 12-sulfodehydroabietic acid (62, 63, and 64) were found to exhibit remarkably high antipepsin activity without aldosterone-like activity.View full abstractDownload PDF (1201K) -
TANEKAZU KUBOTA, JIRO HANAMURA, KENJI KANO, BUNJI UNO1985 Volume 33 Issue 4 Pages 1488-1495
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome important problems in the application of multiple regression analysis (MRA) to the study of quantitative structure-activity relationships (QSAR) are the effect of so-called collinearity among the explaining variables on MRA and the chance correlation. In order to reduce these effects on MRA we have here employed a combination of principal component analysis (PCA) and MRA. Firstly all the explaining variables (xi) are normalized to the zero mean and one variance (x'i), then converted to zero correlation coefficient by using the technique of PCA. Principal component scores pertinent to each principal component (Zm) were next calculated, and MRA was carried out with a linear combination of Zm's. Important Zm's can easily be identified by applying the character of zero correlation coefficient among the variables. The above multiple regression equation is rewritten as a linear combination of x'i or xi by using the transformation matrix between Zm and x'i. This type of equation also seems to be useful for the purpose of predicting new drug structures. Actual calculation results are presented for some drug series. Finally, classification of the explaining variables was done by focusing on the factor loading values of the variables.View full abstractDownload PDF (856K) -
TAKUO KOSUGE, HITOSHI ISHIDA, MICHIYO ISHII1985 Volume 33 Issue 4 Pages 1496-1498
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe anticoagulative principle in Persicae Semen was investigated. In the isolation process, plasma recalcification time in mice was used for the pharmacological measurement of anticoagulative activity of the material. The active principle was isolated by a combination of partition and column chromatography on silica gel, and identified as triolein.View full abstractDownload PDF (416K) -
TAKUO KOSUGE, HITOSHI ISHIDA, HIDEHIRO YAMAZAKI1985 Volume 33 Issue 4 Pages 1499-1502
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe anticoagulative principles were isolated from Curcumae Rhizoma by a combination of partition and column chromatographies on silica gel, and identified as 1, 7-bis (4-hydroxy-3-methoxyphenyl)-1, 6-heptadiene-3, 5-dione (curcumin), p, p'-dihydroxydicinnamoylmethane and p-hydroxycinnamoylferuloylmethane. During the isolation process plasma recalcification time in mice was used to follow the anticoagulative activity of the material.View full abstractDownload PDF (516K) -
TAKUO KOSUGE, HITOSHI ISHIDA1985 Volume 33 Issue 4 Pages 1503-1506
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRhei Rhizoma is an important herb in antiphlogistic, cathartic, antipyretic, anticoagulant and hemostatic prescriptions in Chinese medicine. The anticoagulative principle in the herb was isolated by a combination of partition, fractional precipitation and column chromatography on silica gel. In the isolation process, plasma recalcification time in mice was found to be useful for following the anticoagulative activity of the material. The anticoagulative principle was identified as d-catechin by direct comparison with an authentic sample.View full abstractDownload PDF (480K) -
ZHUANGXIN ZHANG, JUN ZHOU, KOJI HAYASHI, HIROSHI MITSUHASHI1985 Volume 33 Issue 4 Pages 1507-1514
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe chemical components of the Chinese crude drug "Pai-Wei, " dried root of Cynanchum atratum BUNGE (Asclepiadaceae), have been studied. Five new oligoglycosides named cynatratoside-A (3), -B (4), -C (6), -D (8), and -E (9) were isolated by column chromatography and their structures were determined on the basis of chemical and spectral evidence.View full abstractDownload PDF (930K) -
KENICHIRO NAKASHIMA, KAHORU SHIMADA, SHUZO AKIYAMA1985 Volume 33 Issue 4 Pages 1515-1521
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe hydrazones of hydralazine hydrochloride with various aromatic aldehydes were prepared and their spectral properties were examined. On the basis of the above examination, a colorimetric determination of hydralazine hydrochloride with p-dimethylaminocinnamaldehyde based on solvent extraction (CHCl3) was developed. The calibration curve obtained was linear up to 9.8 μg/ml of hydralazine hydrochloride. The method was successfully applied for the analysis of commercial pharmaceutical preparations (tablet and injection). The contents found were 106±2% (tablet) and 100±1% (injection) of the labeled values.View full abstractDownload PDF (594K) -
AKIRA TAKADATE, YOSHIKO OHKUBO, MITSURU IRIKURA, SHUJIRO GOYA, MASAKI ...1985 Volume 33 Issue 4 Pages 1522-1527
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe fluorescence characteristics of 7-anilino-4-methylcoumarin-3-acetic acid (AMCA), which may be useful as a fluorescent probe in protein binding investigations, were examined in various solvents and α-globulin solution. The fluorescence of AMCA was significantly enhanced in lesspolar solvents and in the presence of α-globulin with a shift of the emission maximum to shorter wavelength. Scatchard plots and continuous variation plots indicated that one molecule of AMCA binds to α-globulin. AMCA was applied as a probe in binding studies of some estrogens and corticoids with α-globulin. The spectral changes of the AMCA-α-globulin system in the presence of steroids indicated that estrogens (α- and β-estradiol, estriol) competitively displace AMCA bound to α-globulin but corticoids (cortisone, hydrocortisone) do not. The binding parameters of estrogens for α-globulin were also estimated. The present data suggest that AMCA is useful as a fluorescent probe for assessing the binding of steroids, including estrogens, to α-globulin.View full abstractDownload PDF (568K) -
YUSUKE SASAKI, MICHIKO MATSUI, HIROKI FUJITA, MASAHIRO HOSONO, MASUMI ...1985 Volume 33 Issue 4 Pages 1528-1536
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS[D-Arg2] dermorphin and nineteen N-terminal tetrapeptide analogs were synthesized by a conventional solution method and their analgesic activities after subcutaneous administration to mice were examined. The analgesic effect was assessed by means of the tail pressure test. [D-Arg2] dermorphin was found to have analgesic potency equal to or slightly greater than that of dermorphin. The N-terminal tetrapeptide, H-Tyr-D-Arg-Phe-Gly-OH (I), showed a potency 4.8 times that of morphine and comparable with that of dermorphin on a molar basis. Among the tetrapeptide analogs, several analogs in which Gly4 was replaced by sarcosine or D-Ala exhibited very potent activity more than that of I. On the other hand, replacement of Gly4 by Pro, Leu or D-Leu resulted in a marked decrease in potency. Replacement of either Phe3 by other aromatic amino acid or D-Arg2 by other basic D-amino acid gave analogs with greatly decreased activities. However, one analog whose guanidino functionality on D-Arg2 was blocked by a nitro group, showed activity one-third that of the parent peptide (I). On the basis of these results, the structure-activity relationship for the tetrapeptide is discussed.View full abstractDownload PDF (960K) -
TOSHIHIRO FUJII, YASUHIRO AKABANE, MICHIYO FUJII, YOSHIYUKI KONDO, KOS ...1985 Volume 33 Issue 4 Pages 1537-1543
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the presence of 5 mM Ca2+ or 2mM Mg2+, a protein-bound polysaccharide (PS-K) isolated from Basidiomycetes inhibited the tubulin-dependent adenosine triphosphatase (ATPase) activity of microtubule-associated proteins (MAPs) in a concentration-dependent manner, though it had little effect on the activity in the absence of tubulin. The extent of inhibition decreased at lower concentrations of Ca2+ or Mg2+ and an excess amount of tubulin largely restored the inhibitory effect. When Mn2+ was added to the reaction mixture instead of these divalent cations, the presence of PS-K conversely stimulated the tubulin-dependent ATPase activity of MAPs at lower Mn2+ concentrations (<1-2 mM) under the conditions tested, though PS-K inhibited the ATPase activity at high Mn2+ concentrations. Maximal stimulation and inhibition were about 160% and 70% of the original level (i.e., in the absence of PS-K), respectively. PS-K could also enhance MAPs ATPase activity under conditions where it enhanced the activity in the presence of tubulin, indicating that PS-K itself interacts with MAPs ATPase as tubulin does. The addition of a large amount of ATP under experimental conditions where PS-K inhibited tubulin-dependent Mn2+-ATPase activity of MAPs, on the other hand, led to stimulation by PS-K. Thus, the influence of PS-K on the ATPase activity was dependent on the molar ratio of metal ions to adenosine triphosphate (ATP).View full abstractDownload PDF (727K) -
YOSHIO INOUYE, YUKIE KAWAGUCHI, SHOSHIRO NAKAMURA1985 Volume 33 Issue 4 Pages 1544-1551
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA neutral metalloendopeptidase, produced by Streptomyces, which has anti-inflammatory activity against carrageenan-induced edema in rats was purified by affinity chromatography on N-benzyloxycarbonylglycyl-D-leucylaminohexyl-Sepharose (Z-Gly-D-Leu-AH-Sepharose) to electrophoretic homogeneity. The enzyme was adsorbed on a Z-Gly-D-Leu-AH-Sepharose column equilibrated with phosphate buffer (pH 7.0). The column was washed with phosphate buffer (pH 5.6) containing 2 M urea and eluted with acetate buffer (pH 4.1) supplemented with 2 M urea. The caseinolytic activity of the enzyme, which was lost on treatment with ethylenediaminetetraacetate, was recovered by the addition of ZnCl2 to the reaction mixture. The enzyme showed the maximum caseinolytic activity at pH between 7.0 and 8.0, and was stable in the pH range of 5.0-10.0. The molecular weight was estimated to be 59000. The enzyme preferentially hydrolyzed N-benzyloxycarbonylglycyl-L-leucine amide, N-benzyloxycarbonylglycyl-L-phenylalanine amide and N-benzyloxycarbonylglycyl-L-leucyl-L-tyrosine among the synthetic substrates tested in this work. The producing microbe was identified as Streptomyces mauvecolor based on the results of taxonomic studies.View full abstractDownload PDF (819K) -
SUSUMU ISHIMITSU, SADAKI FUJIMOTO, AKIRA OHARA1985 Volume 33 Issue 4 Pages 1552-1556
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWhen phenylalanine was illuminated in the presence of riboflavin in 0.1 M citrate buffer (pH 5.0), loss of phenylalanine was observed. The photochemical reaction in the riboflavin system was found to reduce phenylalanine, giving hydroxyphenylalanines (p-tyrosine, m-tyrosine and o-tyrosine). The hydroxylation of phenylalanine was inhibited by radical scavengers, e. g., 1, 2-dihydroxybenzene-3, 5-disulfonic acid, catalase, potassium iodide, potassium bromide, sodium thiocyanate and mannose. On the other hand, 1, 4-diazabicyclo [2. 2. 2] octane and guanosine, which are known to react with singlet oxygen, had no significant effect. The findings suggest that superoxide radical and hydrogen peroxide are essential intermediate species in the hydroxylation reaction and that the active species responsible for the photochemical hydroxylation of phenylalanine in the riboflavin system is the hydroxyl radical.View full abstractDownload PDF (543K) -
NAOHITO OHNO, KAZUYOSHI IINO, IWAO SUZUKI, KICHIRO SATO, SHOZO OIKAWA, ...1985 Volume 33 Issue 4 Pages 1557-1562
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCarbon-13 nuclear magnetic resonance (13C-NMR) spectral analyses of the cultured fruit body of Grifola frondosa and the extracted glucan fractions were performed. NMR spectra of the fruit body were measured by suspending the powdered material in D2O. The spectrum of the lyophilized fruit body showed signals of mono-, oligo-, and polysaccharides and fatty acids. The spectrum of the fruit body defatted with 80% ethanol showed signals attributable to poly-saccharides. By comparison with the spectra of extracts from the fruit body, these signals were assigned to α- and β-glucans. Well-resolved signals were also obtained in the spectra of residues extracted with hot water, and cold and hot alkali. These results suggest that (1) the majority of glucans presented in the fruit body has high motional freedom, (2) this method is suitable for studies of the assembly of biopolymers and the ultrastructure of fungal fruit bodies, (3) this method could be applicable for the standardization of commercially grown mushrooms.View full abstractDownload PDF (593K) -
MASAO HIRAIWA, YUTAKA UDA1985 Volume 33 Issue 4 Pages 1563-1570
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn α-L-fucosidase [EC 3.2.1.51] was isolated from liver of the marine gastropod, Aplysia kurodai. The enzyme was purified by procedures involving extraction, ammonium sulfate precipitation, and chromatographies on diethylaminoethyl (DEAE)-Sephadex, hydroxylapatite and Sepharose 6B. The final preparation was sufficiently free from other glycosidase activities and gave a single protein band on disc gel electrophoresis. The molecular weight of the enzyme was estimated to be 330000 by Sephadex G-200 column chromatography. The enzyme has two optimal pH values, one at pH 3.0 and the other at pH 6.4, but it was stable only in the pH range from 4.5 to 6.0. The enzyme released fucose not only from p-nitrophenyl α-L-fucoside but also from human milk oligosaccharides.View full abstractDownload PDF (875K) -
HIROSHI HAMADA, NORIKO TOSHIMITSU, MISAO KOJIMA, TAMOTSU MORITA1985 Volume 33 Issue 4 Pages 1571-1575
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of methanol and magnesium chloride on the induction of cytoplasmic respirationdeficient (RD or petite) mutants of yeast, Saccharomyces cerevisiae, by metal compounds were investigated. ZnCl2, HgCl2, NiCl2, CdCl2 and MnCl2 induced 1.8-2.2% RD mutants at concentrations where almost no growth inhibition was observed. Induction of RD mutants by these metal compounds decreased to the spontaneous level (1.4%) in 4% methanol. The effect of methanol was weaker on RD mutant induction by PbCl2 and CuCl2. The induction of RD mutants by CoCl2 was not affected by methanol. NiCl2 and CdCl2 were strongly mutagenic at higher concentrations, and the mutagenicity of these metal compounds was also repressed by 4% methanol. The frequency of RD mutants induced in the presence of 1×10-2M MnCl2 was increased from 13.5 to 60.7% by the addition of methanol. This increase of the induction of RD mutants in the presence of MnCl2 and methanol was antagonized almost completely by the addition of MgCl2 to the culture medium. The same effect of MgCl2 was observed in the absence of methanol. The effects of methanol and MgCl2 on the induction of RD mutants in yeast are discussed.View full abstractDownload PDF (541K) -
TAMOTSU MORITA, YASUTAKE YANAGIHARA1985 Volume 33 Issue 4 Pages 1576-1582
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn attempt to improve the response of yeast cells to promutagens and procarcinogens in mutagenicity assay was made by using osmotic-sensitive mutants of a yeast, Saccharomyces cerevisiae. Four osmotic-sensitive mutants of yeast which showed increased sensitivity to 1.5 M KCl were induced by ethylmethanesulfonate treatment. One of the mutants, strain C658-K42, was highly sensitive to antibiotics such as mitomycin C, novobiocin, nalidixic acid, chloroquine and rifampicin at concentrations showing no growth-inhibitory effect on the original strain, S. cerevisiae C658. Strain C658-K42 was considered to have a defect in the cell membrane. These osmotic-sensitive mutants were tested for suitability for screening by using well-known procarcinogens (promutagens), dimethylnitrosamine, 3, 4-benzpyrene and 2-acetylaminofluorene. The response of these mutants in a mutagenicity assay (Trp+ reversion) was apparently increased compared with that of the original strain. The yeast cells which were harvested from a late logarithmic phase culture could activate procarcinogens to genetically active forms without any exogeneously added metabolic activation system.View full abstractDownload PDF (750K) -
TAKASHI ABIKO, HIROSHI SEKINO1985 Volume 33 Issue 4 Pages 1583-1591
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe nonatetracontapeptide corresponding to the entire amino acid sequence of thymopoietin I was synthesized by successive azide condensation of seven fragments : Boc-(36-41)-NHNH2, Boc-(30-35)-NHNH2, Boc-(25-29)-NHNH2, Boc-(20-24)-NHNH2, Boc-(16-19)-NHNH2, Boc-(8-15)-NHNH2 and Boc-(1-7)-NHNH2 with H-(42-49)-OBzl. The deprotection of the protected nonatetracontapeptide was achieved by treatment with hydrogen fluoride in the presence of anisole-thioanisole-m-cresol. An increase of E-rosette-forming cells was obtained after incubation of peripheral blood from a uremic patient with the synthetic nonatetracontapeptide at the dose of 1 μg/ml.View full abstractDownload PDF (966K) -
NDU D. IFUDU, AZUBUIKE C. DIKE1985 Volume 33 Issue 4 Pages 1592-1598
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of a cationic surfactant, cetyltrimethyl ammonium bromide (CTAB), on the rate of alkaline hydrolysis of four p-substituted benzene sulfonyl fluoride derivatives was investigated. The p-substituents were classified into clectron-withdrawing (p-NO2) and electron-donating (p-NH2, p-CH3CONH and p-CH3) groups. These different groups produced opposite effects on the rate of alkaline hydrolysis of the corresponding esters in the presence of CTAB. Our investigation on the alkaline hydrolysis of various p-substituted benzene sulfonyl fluorides indicated an inhibitory effect of CTAB in all cases irrespective of the nature of the p-substituent. Solubility studies and multiplot analysis of the kinetic data clearly indicated that the various substituents were appreciably partitioned into the micellar phase. The solubility studies further indicated complexation between the substrate and surfactant. It may be concluded that in sulfonyl fluoride-CTAB systems, the extent of interaction between the substrate and surfactant may be the primary factor determining the type of effects observed instead of the electron activity of the p-substituent. The substrate solubilization in the submicellar region may also play a secondary role.View full abstractDownload PDF (635K) -
ATSUSHI WATANABE, YUMIKO YAMAOKA, EIICHI AKAHO, KOJI KURODA, TERUYOSHI ...1985 Volume 33 Issue 4 Pages 1599-1608
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwenty-six drugs acting on the nervous system and 30 drugs acting on the individual organs, all listed in the JPX, were investigated by polarizing microscopy using the improved immersion method. For 30 drugs having the form of plates, lamellar or scales, two key refractive indices were measured ; these drugs were classified as group A. For 8 drugs having the form of elongated prisms, needles or rods showing always parallel extinction, one key refractive index along the direction of elongation was measured (classified as group B). For 18 other anisotropic crystalline drugs, two refractive indices were measured approximately at the most frequently observable positions ; these drugs were classified as group C. It was found that drugs of groups A and B could be conveniently identified or analyzed by polarizing microscopy by measuring their key refractive indices, and these drugs accounted for 68% of the 56 drugs tested. The correlation between refractive index and birefringence was plotted on rectangular coordinates ; such a plot was also useful for the analysis of drugs by polarizing microscopy. Furthermore, the thicknesses of crystal sections might be easily estimated from the birefringence and interference colors, so polarizing microscopy could be useful for the quality control of slightly soluble drugs by estimating their specific surface areas.View full abstractDownload PDF (1912K) -
KAZUHIKO JUNI, JUNKO OGATA, NORIKO MATSUI, MIHO KUBOTA, MASAHIRO NAKAN ...1985 Volume 33 Issue 4 Pages 1609-1614
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPolylactic acid (PLA) microspheres containing bleomycin were prepared by a solventevaporation process. The release rate of bleomycin from PLA microspheres was very small. The release profiles of the drug from microspheres prepared by using L-and DL-isomers and PLA of different molecular weights did not differ significantly for up to 120 h. The release rate of the drug could be greatly enhanced by incorporating fatty acid esters as additives in the microspheres. It was found that the release rate of the drug could be controlled by using different additives and by adjusting the amount of the additive. Scanning electron microscopic observations suggested that the additive was uniformly distributed in the microspheres as small droplets. The enhanced release rate of the drug in the presence of the additives can be attributed to the highly porous structure of the PLA matrix through which the drug is released by diffusion.View full abstractDownload PDF (776K) -
AKIHIKO HASEGAWA, HIROSHI NAKAGAWA, ISAO SUGIMOTO1985 Volume 33 Issue 4 Pages 1615-1619
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPre-formulation studies were carried out to develop a sustained-release dosage form of nifedipine with good bioavailability. Granules were prepared by spray-coating nifedipine-enteric coating agent solid dispersions on an inert core material. Typical enteric coating agents, hydroxypropylmethylcellulose phthalate and methacrylic acid-methacrylic acid methyl ester copolymer, were used as carriers of the solid dispersions. Dissolution of nifedipine from granules coated with solid dispersions was practically nil in JPX 1st fluid, but a supersaturation phenomenon was observed in JPX 2nd fluid. These granules resulted in prolonged absorption of the drug with good bioavailability in beagle dogs and human volunteers. This absorption characteristic arises from the pH dependency of the dissolution behavior of these solid dispersions. That is, dissolution of nifedipine was suppressed in acidic medium and showed supersaturation in comparatively neutral medium. It was confirmed that the granules were transported through the gastrointestinal tract and showed prolonged drug release behavior with good bioavailability.View full abstractDownload PDF (617K) -
EIJI MIZUTA, ATSUKO TSUBOTANI1985 Volume 33 Issue 4 Pages 1620-1632
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA study on the frequency distribution of various pharmacokinetic parameters was conducted using pharmacokinetic data based on human blood samples obtained after administration of three cephalosporin derivatives. The results indicated that pharmacokinetic parameters ka, ke, V, α, β, k12, k21, V1, Vd and Cl followed lognormal distribution curves rather than normal distribution curves. Thus, in the case of a one-compartment open model, it was demonstrated that mean plasma concentration-time curves could be prepared more precisely by use of the geometrical mean values of V, ke and ka. In the case of a two-compartment open model, the use of the geometrical mean values of V1, α, β and ke rather than those of V1, k12, k21 and ke was considered to be preferable in view of the reliability of the rate constants α, β, k12 and k21.View full abstractDownload PDF (1049K) -
YUKIHISA KURONO, TOMONARI KUWAYAMA, KINYA KAMIYA, TAMOTSU YASHIRO, KEN ...1985 Volume 33 Issue 4 Pages 1633-1640
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe oxazolidine ring-opening and ring-closing reactions (acid-base equilibrium reactions) of oxazolam were investigated by using a stopped-flow spectrophotometer. The cis and trans isomers of oxazolam were found to have distinct ring-opening rate constants and the constant of the cis isomer was 10 to 20 times larger than that of the trans isomer. The ring-opening is hydrogen ioncatalyzed at low pH region. The ring-closing occurs in a hydroxide ion-catalyzed reaction in the alkaline region and is affected by the deprotonation of the diazepinone ring. The individual intrinsic rate constants for the ring-opening and ring-closing reactions were determined from the rate-pH profile. These rate measurements are of value to distinguish between cis and trans isomers of oxazolam.View full abstractDownload PDF (763K) -
SHOZO KOUCHIWA, MASAMI NEMOTO, SHIGERU ITAI, HIROSHI MURAYAMA, TSUNEJI ...1985 Volume 33 Issue 4 Pages 1641-1651
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA theoretical method was developed to describe the time course of the available surface area (S (t)) in the dissolution process of solid dosage forms. In general, dissolution of solid dosage forms includes disintegration and deaggregation (dispersion of disintegrated granules and powders), and since the mechanism is very complex, S (t) in the dissolution medium cannot be determined by numerical calculation. However, the integrated value of S (t), which can be considered to be the available surface area generated during the dissolution time course, can be calculated from the dissolved amount and the dissolution parameters. In addition, the ratio of the available surface area generated by time t to the total available surface generated can be regarded as a cumulative probability distribution. By the regression of this ratio (F(t)) to the probability distribution, the time course of S (t) was able to be determined numerically. The application of this theory to the dissolution of flufenamic acid in tablets is described.View full abstractDownload PDF (780K) -
TAKEO KAWAGUCHI, MASAHIKO SAITO, YOSHIKI SUZUKI, NAOKI NAMBU, TSUNEJI ...1985 Volume 33 Issue 4 Pages 1652-1659
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe bioactivation characteristics of 3', 5'-diesters of 5-fluoro-2'-deoxyuridine (FUdR) esterified with saturated aliphatic acids, including acetic, propionic, butyric, hexanoic, octanoic, decanoic, dodecanoic and trimethylacetic acids, were studied by using rat tissue homogenates and plasma. The susceptibility of the esters to hydrolysis by the biological media increased as the acyl promoiety was lengthened up to octanoyl. Further elongation resulted in decreasing susceptibility. Antitumor activity against L1210 of the esters with a longer chain or branched acyl group administered intraperitoneally and orally to tumor-bearing mice was also examined. Both the antitumor activity and the therapeutic index (ILSmax/ILS30) of the esters improved as the acyl promoiety was lengthened from octanoyl to dodecanoyl. These results suggested that the higher antitumor activities of longer alkyl chain diesters of FUdR are due to their slow rates of FUdR regeneration with esterases.View full abstractDownload PDF (764K) -
NOBUYOSHI KANENIWA, MAKOTO OTSUKA1985 Volume 33 Issue 4 Pages 1660-1668
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of grinding in an agate centrifugal ball mill on the transformations of polymorphs of chloramphenicol palmitate (CPP) were studied by means of X-ray diffraction analysis, infrared (IR) spectroscopy and differential scanning calorimetry (DSC). Three kinds of the polymorphs of CPP were reported, that is, forms A, B and C. There was no change in the X-ray diffraction profile of form A (stable form) on grinding for 600 min, but its profile became broader than that of intact form A. There was no change in the X-ray diffraction profile of form B (meta-stable form) on grinding for 130 min, but form B was transformed into form A by grinding for more than 140 min. Form B ground for 140 min contained about 35% form A ; when ground for 150 min, it contained about 80% form A, and when ground for more than 150 min, it contained a constant level of about 80% form A. The X-ray diffraction profile of form C (meta-stable form) suggested that form C was transformed into form B by grinding for 20 min ; thereafter the product was transformed into form A by grinding for 160 min. Form C ground for 4 min contained about 60% form B ; when ground for 20 min, it contained about 100% form B, and ground for 160 min, it contained about 80% form A. These results suggest that the transformations of polymorphs of CPP by grinding are form C→form B→form A. The melting point (mp) and the heat of fusion (H) were measured by DSC. The mp and the H of form A obtained by grinding were about 2.5°C and about 2.5 kcal/mol lower than those of intact form A, respectively, and the solubility in 50% (v/v) aqueous isopropyl alchohol was about twice that of intact form A.View full abstractDownload PDF (808K) -
JOHJI YAMAHARA, HITOSHI KIMURA, MASAAKI KOBAYASHI, TOSHIHIRO OKAMOTO, ...1985 Volume 33 Issue 4 Pages 1669-1675
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was shown previously that α-terpineol is the cholagogic principle in cardamom. Two monoterpenoid glucoside, (±)-α-terpineol-2, 3, 4, 6-tetra-O-acetyl-β-D-glucopyranoside (TAG) and (±)-α-terpineol-β-D-O-glucopyranoside (TG), were synthesized in order to develop new drugs whose structures are based on those of natural products. The cholagogic properties of these compounds were investigated in this study. TG administered by the oral and intraduodendal routes in rats showed a significant cholagogic effect, while TAG showed little effect. The effect of TG was to increase both the fluid weight and the solid weight of bile. The total bile acid content was significantly increased 30 min after administration of TG as compared to that of untreated rats. An analysis of bile acid contents in the bile showed that ursodeoxycholic acid and chenodeoxycholic acid, which are known to have a dissolving effect on gallstones, were increased by TG. The analysis of biliary lipids also demonstrated that biliary cholesterol was decreased by TG. These results raise the possibility that TG may be useful as a dissolving agent for gallstones. In an acute toxicity test, the LD50 value for TG was about one-fourth of the value for (±)-α-terpineol, and when their molecular weights are taken into consideration, the toxicity of TG was much lower than that of (±)-α-terpineol. Since TG not only has a cholagogic effect and increases solid components of bile but also has low toxicity, it may be clinically useful as a cholagogic agent.View full abstractDownload PDF (702K) -
JOHJI YAMAHARA, MUTSUO KOZUKA, TOKUNOSUKE SAWADA, HAJIME FUJIMURA, KIM ...1985 Volume 33 Issue 4 Pages 1676-1680
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe anti-allergic effects of "Cnidii monnieri"and its constituents were examined. Imperatorine, a coumarin derivative in "Cnidii monnieri, "showed anti-allergic activity.View full abstractDownload PDF (484K) -
NOBUO CHO, MASAAKI HIROBE, ISSEI TAKAYANAGI1985 Volume 33 Issue 4 Pages 1681-1686
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of epoxidation of normorphine, norcodeine, N-allylnormorphine (nalorphine) and N-allylnorcodeine on the twitch response of guinea pig ileum to electrical stimulation were studied. Normorphine, norcodeine and their epoxides are narcotic agonists, while nalorphine, N-allylnorcodeine and their epoxides are agonist-antagonists. The agonistic effects (via mu-receptor) of normorphine and norcodeine were not influenced by epoxidation of the 7, 8-double bond. Epoxidation also little influenced the competitive antagonistic action (via mu-receptor) of nalorphine and N-allylnorcodeine against morphine. On the other hand, the agonistic action (via kappa-receptor) of nalorphine and N-allylnorcodeine was considerably decreased by epoxidation.View full abstractDownload PDF (575K) -
MIKI SHOJI, MASAAKI MORI, KIYOMI MOTOO, HIROSHI KOZUKA, TAKASHI HONDA1985 Volume 33 Issue 4 Pages 1687-1693
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSUrinary metabolites of 2, 4-dinitrotoluene (2, 4-DNT) were quantitated by high-performance liquid chromatography (HPLC) after administration to male Wistar rats. The urine was extracted with ether after adjusting the pH to 11 and 2. The ether extracts were evaporated to dryness, and each residue was dissolved in aqueous methanol and subjected to HPLC analysis. A 54 μl portion of aqueous methanol solution was analyzed by HPLC on a reversed-phase column. The mobile phases were 40% methanol, 40% methanol in 0.0018 M tetra-n-butylammonium chloride (TBACl), 20% methanol in 0.0018 M TBACl, pH 7.4 phosphate buffer and 20% methanol in 0.0027 M sodium 1-hexanesulfonate (HSANa), pH 3.7 acetate buffer, at a flow rate of 0.6 ml/min. 2, 4-Dinitrobenzoic acid (2, 4-DNBA) was excreted most abundantly, followed by 2, 4-dinitrobenzyl alcohol glucuronide (2, 4-DNBG), 2-amino-4-acetylaminobenzoic acid (2A4AABA), 2, 4-dinitrobenzyl alcohol (2, 4-DNB), 4-amino-2-nitro (2-amino-4-nitro) benzyl alcohol glucuronides (4A2N (2A4N) BG), 4-amino-2-nitro (2-amino-4-nitro) benzyl alcohols (4A2N (2A4N) B) and 4-amino-2-nitrotoluene (4A2NT). Though 2, 4-dinitrobenzaldehyde (2, 4-DNAl), a potent mutagen, was not detected in this study, the oxidative conversion of 2, 4-DNB to 2, 4-DNBA in vivo might be correlated to the carcinogenicity of 2, 4-DNT, since 2, 4-DNBA are the major metabolites of 2, 4-DNT.View full abstractDownload PDF (690K) -
JUNICHI SUDO, TSUNEYOSHI TANABE1985 Volume 33 Issue 4 Pages 1694-1702
Published: April 25, 1985
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDistributions of post-proline cleaving enzyme-, converting enzyme-, chymotrypsin- and trypsin-like activities, were investigated in nephron segments and in brush-border membrane fraction isolated from rat kidney. These activities were found to be higher in the proximal tubule than in other segments, and were hardly detectable in the cortical collecting tubule. In the proximal tubule, trypsin-like activity showed the highest value in the pars convoluta, while the other peptidases showed their highest activities in the pars recta. Post-proline cleaving enzyme- and trypsin-like activities were also high in the glomerulus. In addition, post-proline cleaving enzymeand converting enzyme-like activities were found in the brush-border membrane, while chymotrypsin- and trypsin-like activities were found in the cell component (s) other than the brush-border membrane. From these distributions of the peptidases, it is speculated that peptides are degraded both in the glomerulus and in the proximal tubule, and that in the proximal tubule the peptides are degraded both in the brush-border membrane and in other cell component (s).View full abstractDownload PDF (956K)