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Volume 41, Issue 4
Displaying 1-36 of 36 articles from this issue
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Takayuki KAWAGUCHI, Kunio SAITO, Kenji MATSUKI, Takeo IWAKUMA, Mikio T ...1993 Volume 41 Issue 4 Pages 639-642
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAsymmetric reduction of the N-protected amino ketone (2) with serveral chiral reducing agents, i.e., (R)-(+)-2-amino-3-methyl-1, 1-diphenylbutanol (6)-borane complex (method A), (S, S')-N, N'-dibenzoylcystine (7)-LiBH4-ROH complex (method B), and sodium (S)-prolinate-borane complex (8) (method C), was investigated in an attempt to synthesize denopamine (1) enantioselectively. Reduction of 2f by method B in tetrahydrofuran at 2-3°C gave the best result (88% ee with 95% chemical yield).View full abstractDownload PDF (627K) -
Kenji MATSUKI, Masao SOBUKAWA, Akiyoshi KAWAI, Hirozumi INOUE, Mikio T ...1993 Volume 41 Issue 4 Pages 643-648
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAsymmetric reduction of some 3-keto esters (6, 8, and 11) to 3-hydroxy esters (7, 9, and 12) with various chiral reducing agents was investigated. The products (9 and 12) were converted to methyl (2R, 3S)-3-(4-methoxy-phenyl)glycidate (2R, 3S-3), a key intermediate in the practical enantioselective synthesis of dilitazem (1).View full abstractDownload PDF (923K) -
Haruo NUKAYA, Yasunori INAOKA, Hitoshi ISHIDA, Kuniro TSUJI, Yoshihide ...1993 Volume 41 Issue 4 Pages 649-653
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethylglyoxal is directly mutagenic to Salmonella typhimurium TA100 and its mutagenicity is markedly enhanced in the presence of hydrogen peroxide. We found that methylglyoxal in phosphate buffer was decomposed easily by hydrogen peroxide at room temperature to yield acetic acid and formic acid as major products and diacetyl as a minor product; acetyl radical was detected in the solution by ESR spectroscopy by the use of a spin-trapping reagent, 5, 5-dimethyl-1-pyrroline N-oxide. Furthermore, guanosine was coverted into N2-acetylguanosine by a combination of methylglyoxal and hydrogen peroxide in 0.1 M phosphate buffers (pH 6.1 to 7.4). This acetylation may be related to the enhancement of methylglyoxal mutagenicity by hydrogen peroxide. Other α-ketoaldehydes such as glyoxal and phenylglyoxal also yielded the corresponding acids and α-dicarbonyls upon reaction with hydrogen peroxide under the same conditions as above. These acids would have been produced through Baeyer-Villiger reaction or coupling of acyl radical with hydroxy radical, and dicarbonyls by dimerization of acyl radicals. In addition, when phenylglyoxal was used, the generation of benzoyl radial and the conversion of guanosine to N2-benzoylguanosine were observed. However, it remains to be established whether the generation of acyl radicals is directly involved in the N-2 acylation of guanosine.View full abstractDownload PDF (826K) -
Haruhiro FUJIMOTO, Yuji NAKAYAMA, Mikio YAMAZAKI1993 Volume 41 Issue 4 Pages 654-658
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree metabolites having a suppressive effect on proliferation of mouse lymphocytes stimulated with mitogens such as concanavalin A (Con A) and lipopolysaccharide (LPS) were isolated from a mushroom, Lactarius flavidulus, and identified as geranylphenols, flavidulols A, B and C, respectively, which had previously been isolated from the same mushroom. The IC50 values of flavidulols A, B and C were found to be 8.9, 4.9 and 36.3 μg/ml against Con A-induced proliferation of mouse lymphocytes, and 6.7, 3.9 and 28.3 μg/ml against LPS-induced proliferation, respectively.View full abstractDownload PDF (711K) -
Tsuneatsu NAGAO, Ryuichiro TANAKA, Yukiko IWASE, Hikaru OKABE1993 Volume 41 Issue 4 Pages 659-665
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new echinocystic acid 3, 28-O-bisdesmosides, scaberosides Ha, Hb1, Hb2 and Hc1, were isolated as their methyl esters from the ground part of Aster scaber THUNB. (Compositae) along with foetidissimoside A and scaberoside A2, and their structures were determined based on spectral and chemical evidence. These glycosides have a common prosapogenin structure, echinocystic acid-3-O-glucopyranosiduronic acid, and differ in the structures of the 28-O-linked sugar moieties.Scaberoside Ha1 is a 28-[O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)]-β-D-xylopyranosyl] ester, Hb1, a 28-[O-β-D-xylopyranosyl-(1→4)-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)-β-D-xylopyranosyl] ester, Hb2, a 28-[O-β-D-xylopyranosyl-(1→3)-O-β-D-xylopyranosyl-(1→4)-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)-β-D-xylopyranosyl] ester, and Hc1, a 28-[O-β-D-xylopyranosyl-(1→3)-O-β-D-xylopyranosyl-(1→3)-[O-β-D-xylopyranosyl-(1→4)-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)]-β-D-xylopyranosyl] ester of the prosapogenin.View full abstractDownload PDF (907K) -
Kunio HIROI, Masayuki UMEMURA, Aki FUJISAWA1993 Volume 41 Issue 4 Pages 666-671
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA chiral α-sulfinyl α, β-unsaturated ketone served as a good chiral diene or enophile in intramolecular Lewis acid-catalyzed asymmetric pericyclic reactions, giving hetero-Diels-Alder reaction products, together with ene reaction products in some cases, in high optical yields. The reaction pathways for Diels-Alder or ene reactions were readily controlled depending on the Lewis acids used. A chiral α-sulfinyl α, β-unsaturated ester served as a good enophile to give ene reaction products with high enantioselectivity. The mechanistic pathway for the asymmetric induction is proposed on the basis of the stereochemical results obtained.View full abstractDownload PDF (1106K) -
Takashi YOSHIDA, Atallah F. AHMED, Takuo OKUDA1993 Volume 41 Issue 4 Pages 672-679
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new dimeric hydrolyzable tannins, hirtellins C, D, E and F, besides previously reported hirtellins A and B, have been isolated from the leaf extract of Reaumuria hirtella JAUB, et SP. (Tamaricaceae). Macrocyclic structures, 1 and 12, having both dehydrodigalloyl (DHDG) and isodehydrodigalloyl (isoDHDG) groups as the connecting units between monomers, were respectively assigned for hirtellin C and F, based on chemical methods, two-dimensional nuclear magnetic resonance measurement and other spectroscopic analyses. Hirtellin D (7) was characterized as an isomer of hirtellin F (12). Hirtellin E (15), having a dehydrotrigalloyl (hellinoyl) group, was characterized as an analog of hirtellin B.View full abstractDownload PDF (1171K) -
Hiroyuki AKITA, Isao UMEZAWA, Michika TAKANO, Takeshi OISHI1993 Volume 41 Issue 4 Pages 680-684
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of (±) methyl 4, 5-trans-epoxy-(2E)-hexenoate (1) with nucleophile having heteroatoms in the presence of BF3·Et2 O gave the 4, 5-anti-5-hydroxy-4- and/or 2, 5-anti-5-hydroxy-2-substituted products. Among them, the (±)-4, 5-anti-5-hydroxy-4-thiophenoxy ester 12a was enantioselectively acetylated with acylating reagent in the presence of lipase "PL 266" from Alcaligenes sp. to provide the (4S, 5R)-5-acetoxy ester 12b and (4R, 5S)-12a quantitatively.View full abstractDownload PDF (821K) -
Yoshio TAKEDA, Yukako FUTATSUISHI, Teruyoshi ICHIHARA, Takashi MATSUMO ...1993 Volume 41 Issue 4 Pages 685-687
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the dried aerial parts of Rabdosia longituba (MIQ). HARA, two new diterpenes, named rabdokaurin C (1) and rabdokaurin D (8), were isolated together with the known compounds ordonin, lasiokaurin, effusanin B, rabdophyllin G, and rabdokaurin B. The structures of the two new compounds were determined on the basis of spectroscopic and chemical evidence.View full abstractDownload PDF (657K) -
Makoto TAKEUCHI, Shuichi SAKAMOTO, Makoto YOSHIDA, Tetsushi ABE, Yasuo ...1993 Volume 41 Issue 4 Pages 688-693
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of aminomethylenebisphosphonate derivatives was synthesized and evaluated for their antiresorptive activities using a parathyroid hormone (PTH)-induced hypercalemia model in rats (PIH model). Among these compounds, (cycloheptylamino)methylenebis(phosphonic acid) (3j) was finally selected for further investigation, proving 10-fold as potent as pamidronate in the PIH model and an immobilization bone atrophy model in rats (DA model). The structure-activity relationships of this series of bisphosphonates are discussed.View full abstractDownload PDF (943K) -
Chisako YAMAGAMI, Narao TAKAO1993 Volume 41 Issue 4 Pages 694-698
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe log k' values (k' : capacity factor) of m- and p-substituted benzyl N, N-dimethylcarbamates, I, were obtained by reversed-phase high-performance liquid chromatography (RPLC) on C18-bonded columns with methanol-buffer (pH 7.4) solutions as the mobile phase. The log kw value, which is considered as a measure of the octanol-water log P value (P : partitoin coefficient), was calculated by linear extrapolation of the plot of log k' against methanol content in eluents. The log kw values and the k' values at 30, 50 and 70% MeOH concentrations were correlated with log P in terms of the hydrogen-bond ability of the substitutent. As is usually observed the amphiprotic substituents, which act as both H-donor and H-acceptor, behaved differently from the others. A log k'-log P plot with very good linearity was obtained with an eluent containing 50% MeOH except for the above mentioned amphiprotic substituents. The log kw values were much higher than the log P values. This was ascribed to the strong hydrogen accepting ability of the fixed substituent, CH2 OCONMe2.View full abstractDownload PDF (781K) -
Shingo HORIMOTO, Masanari MABUCHI, Kiyoshi BANNO, Tadashi SATO1993 Volume 41 Issue 4 Pages 699-702
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA very rapid and highly sensitive method using desorption chemical ionization (DCI)-tandem mass spectrometry (MS/MS) with selected reaction monitoring is reported for the simultaneous determination of imidapril and its active metabolite (M1) in human plasma. Imidapril and M1 in plasma were extracted by a C18 solid phase exraction cartridge after deproteinization, and derivatized with pentafluorobenzyl bromide. One μl of prepared sample was applied to the DCI filament and analyzed by DCI/MS/MS within a few minutes. The limits of determination of imidapril and M1 were 0.2 and 0.5 ng/ml in human plasma, respectively. The features of this method make it appropriate for use in pharmacokinetic studies with human plasma after oral administration of imidapril.View full abstractDownload PDF (592K) -
Shoji YAHARA, Choko SHIGEYAMA, Takeshi URA, Kaori WAKAMATSU, Tadashi Y ...1993 Volume 41 Issue 4 Pages 703-709
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe chemical structures of four cyclic peptides, lyciumins A-D (1-4), three acyclic diterpene glycosides, lyciumosides I-III (5-7) and other three compounds, a tryptophan derivative glycoside (8), a monoterpene glycoside (9) and a steroidal glycoside (10) isolated from Lycium chinense, have been elucidated by a combination of chemical, 1H- and 13C-NMR, and mass spectrometric studies. Lyciumins are interesting because of their monocyclic octapeptides containing a novel C-N linkage between tryptophan N1 and glycine Cα.View full abstractDownload PDF (939K) -
Masahiro TANABE, Yuh-Dan CHEN, Ken-ichi SAITO, Yoshihiro KANO1993 Volume 41 Issue 4 Pages 710-713
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWe previously reported on the isolation and identification of (E)-8β, 17-epoxylabd-12-ene-15, 16-dial (ZT) from ginger (rhizome of Zingiber officinale ROSCOE, Zingiberaceae).In this paper, the pharmacological effects of ZT are reported. The experimental mouse hypercholesterolemia induced by Triton WR-1339 was treated after oral administration of ZT. In homogenated rat liver with ZT, cholesterol biosynthesis was decreased. In addition, the same activity was observed in the homogenated rat liver which was resected after the oral administration of ZT.According to the results of general pharmacological screening, no remarkable activity of ZT was observed except for an inhibitory effect on the cholesterol biosynthesis.View full abstractDownload PDF (568K) -
Satoko SUGIYAMA, Kaoru UMEHARA, Masanori KUROYANAGI, Akira UENO, Takao ...1993 Volume 41 Issue 4 Pages 714-719
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn attempt was made to isolate differentiation inducers from Aurantii Nobilis Pericarpium and the fruit peel of Citrus reticulata BLANCO (Rutaceae). Twenty-seven kinds of flavones, including five new flavones, were isolated after repeated chromatography from methanol extracts of these plants and their structures were established, from their physicochemical data, to be highly methoxylated flavones. Each compound, except for two flavone glucosides, showed the differentiation inducing activity toward mouse myeloid leukemia cells (M1), and the cells came to have phagocytic activity. Furthermore, differentiation inducing activity was tested using human acute promyelocytic leukemia cell line (HL-60).View full abstractDownload PDF (774K) -
Yasushi MATSUNAGA, Ryoko OHTA, Nobuyuki BANDO, Hiroaki YAMADA, Hiroshi ...1993 Volume 41 Issue 4 Pages 720-724
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(E)-4-[1-[4-[2-(Dimethylamino)ethoxy]phenyl]-2-(4-isopropyl)phenyl]-1-butenyl]phenyl monophosphate (TAT-59) is a new drug for the treatment of breast cancer. Physical and chemical stability of a tablet consisting of TAT-59 powder and a few excipients (Formulated tablet), a tablet consisting of only TAT-59 power (TAT-59 tablet) and TAT-59 powder itself itself was evaluated based on water content, tensile strenght, porosity, the amount of TAT-59 and its hydrolysis product, DP-TAT-59.The water content of Formulated tablet increased with relative humidity (RH), whereas that of TAT-59 tablet and TAT-59 powder scarcely changed. The equilibrium water content of Formulated tablet was much greater than that of the TAT-59 tablet or TAT-59 powder due to adsorbed moisture by the excipients. The tensile strength and porosity of Formulated tablet decreased and increased linearly, respectively, with increasing water content. The degradation rate of TAT-59 decreased in the following order : Formulated tablet>TAT-59 tablet>TAT-59 powder. The relationship between equilibrium water content and degradation rate of the Formulated tablet was determined by the Carstensen equation, in which the interaction order between the durg and water content was 1.9, and the degration of TAT-59 in Formulated tablet was related to water content. Thus, it was found that the degradation of TAT-59 was accelerated by compression and addition of excipients.View full abstractDownload PDF (615K) -
Yoshinobu FUKUMORI, Hideki ICHIKAWA, Kaori JONO, Tomoaki FUKUDA, Yoshi ...1993 Volume 41 Issue 4 Pages 725-730
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWater-soluble hydroxypropyl cellulose (HPC) was applied to fine lactose powder (53-63 μm) by the Wurster process. The effects of various additives on agglomeration were studied by the binding strength of membrane materials, the droplet size and the surface morphology of coated particles. The agglomeration was also computer-simulated by a previously reported model.Methyl cellulose (MC) and sodium alginate (ALG) increased the mass median diameter of droplets at 10% addition to HPC, while the other additives exhibited no significant effect on the droplet size distribution. The production of coarse droplets induced by MC and ALG led to the agglomeration of 76 and 87% cores, respectively, though they reduced the binding strength of HPC. Polyethyleneglycol (PEG) reduced the agglomeration by weakening the binding strength of HPC in particular. NaCl, which was incompatible with HPC, reduced agglomeration by hindering HPC from forming homogeneous film. The computer simulation indicated that the smalleste sizes of droplets causing the agglomeration were 44-71 μm. With MC and ALG the weight fraction of coarse droplets causing the agglomeration reached 5.7 and 4.4%, respectively; however, it was less than 1% with the other additives. Such a minor quantity of droplets caused the agglomeration of cores of 18% (PEG and NaCl) to 69% (polyvinyl alcohol). It was suggested that the agglomeration enhancing factor, K, migth well reflect the state of fluidization.View full abstractDownload PDF (1448K) -
Hiroshi YUASA, Junko YAMASHITA, Yoshio KANAYA1993 Volume 41 Issue 4 Pages 731-736
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffects of the pore size of controlled pore glass (CPG) on whisker growth in mixtures composed of aspirin and CPG were studied. When the powder mixture and the tablets, both composed of five kinds of the CPG having different pore sizes, aspirin and micro-crystalline cellulose, were preserved in glass containers under various temperatures for 5 d, whisker growth was observed in some samples. The main component of whisker was salicylic acid, and the amount of whisker was measured using high-performance liquid chromatography at fixed time intervals. The pore size distribution was determined by mercury intrusion porosimetry. The growht rate and amount of whisker were both larger with a higher preservative temperature. Furthermore, the amount of whisker was almost proportional to the surface area of samples under the same preservative temperature above 60°C, except for the samples containing CPG350, while in the samples containing CPG350, a larger amount anda higher growth rate than expected were observed. These results suggest the participation of a particular pore size in the whisker growth.View full abstractDownload PDF (1375K) -
Nobuo KONDO, Toru IWAO, Hirotoshi MASUDA, Kouichi YAMANOUCHI, Yoshiaki ...1993 Volume 41 Issue 4 Pages 737-740
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN-[[[4-(5-Bromo-2-pyrimidinyloxy)-3-chlorophenyl]amino]carbonyl]-2-nitrobenzamide (HO-221) is being developed as an anticancer agent with a novel mode of action. HO-221 shows poor oral absorption and is only slighytly soluble in water (0.055 μg/ml at 37°C). In this study, it was shown that the reduction in particle size of HO-221 to the submicron region (0.453 μm, mean by volume) could be achieved by a wet milling in a decaglycerin monolaurate aqueous solution with small glass beads. The wet milling suspension obtained showed improved dissolution rate and oral absorption in rats. A solid sodage form be could also made from that suspension with addition of sucrose palmitate which prevented aggregation caused by the hydrophobic interaction. The solid dosage form thus obtained showed twice as much oral absorption in dogs as the preparation made by dry milling.View full abstractDownload PDF (1023K) -
Takayuki OHWAKI, Masahiro NAKAMURA, Hiroshi OZAWA, Yoshiaki KAWASHIMA, ...1993 Volume 41 Issue 4 Pages 741-746
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFor the application of water-in-oil-in-water (w/o/w) emulsions to a nasal dosage form of secretin, permeation tests were conducted in vitro to assess the effects of hydrophilic surfactants in the internal aqueous compartment on the release rate of secretin. The amount of secretin that permeated through an artificial membrane from a donor cell to a receptor cell was affected by the addition of sodium chloride or sodium alkylsulfonate to the internal aqueous compartment of w/o/w emulsions in the donor cell. Sodium chloride decreased apparent permeation rate constants from the internal aqueous compartment to the external aqueous phase (K'1) as the difference in osmolartiy between the internal compartment and the external phase increased. While sodium alkylsulfonates increased K'1 in proportion to the values of (partition coefficient between the oil phase and the internal aqueous phase/partition coefficient between the oil phase and the external aqueous phase)/osmolarity ratio of the internal aqueous phase to the external aqueous phase. These results demonstrate that the release rate of secretion from w/o/w emulsions are affected by partition of the drug between aqueous and oil phases and by osmotic difference between the outer and internal phases.View full abstractDownload PDF (1188K) -
Isao TAKEUCHI, Yoshiki HAMADA, Minoru HIROTA1993 Volume 41 Issue 4 Pages 747-751
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNaphtho[2, 1-f][1, 7]naphthyridine (5, angular type) and naphtho[2, 1-b][1, 5]naphthyridine (6, linear type) were obtained by the Skraup reaction of 3-aminobenzo[h]quinoline (4), but 3-aminobenzo[g]quinoline gave only naphtho-[2, 3-f][1, 7]naphthyridine (18, angular type).View full abstractDownload PDF (743K) -
Katsuhiro SAITO, Hiroshi FUSHIHARA, Kensuke TAKAHASHI, Noritaka ABE1993 Volume 41 Issue 4 Pages 752-754
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe addition reactions of 3-(2-chloro-1-azaazulenyl)methylene with cis- and trans-stilbenes proceeded in a stereospecific manner to afford the corresponding cyclopropane derivatives. The substitution effects on the relative rate ratio of the addition reactions of the carbene with styrenes having various substituents on the p-positions were measured to investigate the electronic nature of carbene.View full abstractDownload PDF (532K) -
Yoko MORI, Kazuho HARADA, Naohiko MORISHIMA, Shonosuke ZEN1993 Volume 41 Issue 4 Pages 755-757
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThr reactions of 3-O-benzyl-6-deoxy-1, 2-O-isopropylidene-5-O-methanesulfonyl-α-D-gluco- and β-L-idofurnoses (1 and 2) with tetrabutylammonium fluoride in N, N-dimethylformamide gave (E)- and (Z)-3-O-benzyl-5, 6-dideoxy-1, 2-O-isopropylidene-β-L-threo-hex-4-enofuranoses (3 and 4), respectively, as the major products. The structure of the (E)-isomer 3 was determined by single-crystal X-ray analysis. 3-O-Benzyl-5, 6-dideoxy-5-fluoro-1, 2-O-isopropylidene-β-L-ido- and α-D-glucofuranoses (6 and 7) were formed as minor products in the respective reactions.View full abstractDownload PDF (471K) -
Masaharu KUME, Tadatoshi KUBOTA, Yasuo KIMURA, Hiromu NAKASHIMIZU, Kiy ...1993 Volume 41 Issue 4 Pages 758-762
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis, antibacterial activity and oral absorption of 3-(1H-1, 2, 3, -trazol-4-yl)thiomethylthio-3-cephem-4-carboxylic acids with various C-7 side chains (2) are described. The (1H-1, 2, 3-triazol-4-yl)thiomethylthio C-3 side chain was found to be an effective substituent for good oral absorption of cephalosporins with some C-7 side chains.View full abstractDownload PDF (731K) -
Takashi IIDA, Shinji NISHIDA, Frederic C. CHANG, Toshifumi NIWA, Junic ...1993 Volume 41 Issue 4 Pages 763-765
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new method for the preparation of allochenodeoxycholic and allocholic acids is described. The key steps in the synthesis are 1) simultaneous oxidation-dehydrogenation reaction of 3α-hydroxy 5β-bile acid formyl esters with iodoxybenzene catalyzed by benzeneseleninic anhydride, 2) reductive allomerization at C-5 of the 1, 4-dien-3-oxo hydroxy acids with lithium/liq. ammonia, and 3) subsequent reduction of the resulting 3-oxo 5α-compounds with K-Selectride.View full abstractDownload PDF (661K) -
Kazuhiko ARIMORI, Megumi DESHIMARU, Emiko FURUKAWA, Masahiro NAKANO1993 Volume 41 Issue 4 Pages 766-768
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAdsorption studies in vitro of mexilletine onto activated charcoal were performed in macrogol (polyethylene glycol)-electrolyte solutoin (PEG-ELS) and JP XII disintegration medium No. 2 (second medium). Mexiletine was adsorbed more extensively onto activated charcoal in PEG-ELS than that in JP XII second medium. The maximum adsorptive capacity of activated charcoal for the durg was 328 and 284 mg per gram of charcoal in PEG-ELS and JP XII second medium, respectively. In addition, the equilibrium constant of activated charcoal estimated according to the Langmuir equation was 0.079 and 0.034 l per gram of charcoal in PEG-ELS and JP XII second medium, respectively. Adsorption of mexiletine onto activated charcoal was decreased by omitting macrogol, sodium sulfate or sodium bicarbonate from a standard PEG-ELS formulation. Oral activated charcoal will be useful in combination with whole bowel irrigation with PEG-ELS in mexiletine overdose because of its excellent adsorbability in the solution.View full abstractDownload PDF (538K) -
Kazuo SAKAI, Nozomu MURATA, Hideki FUKINO, Yasuhiro YAMANE1993 Volume 41 Issue 4 Pages 769-771
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe main aim of this research was to clarify that nutritional dietary copper may participate in the protective action against hepatocarcinogenesis in rats by N-nitrosodimethylamine (NDMA). The copper concentrations in serum and liver from 2 to 8 d after rats were first fed a copper deficient diet (copper, 0.6 ppm) decreased significantly compared to those of pair-fed rats (copper in a control diet, 7 ppm). The subcellular distribution of copper in the liver at 5 d after feeding of a copper deficient diet began was measured and the copper concentrations in soluble and nuclear fractions decreased at a similar rate in copper deficient rats treated with or without NDMA, compared to those of pair-fed rats. The incorporation of [3H]thymidine into rat liver DNA at 48 h after treatment with NDMA markedly increased under the experimental conditions used. By giving rats a copper deficient diet for a few days the increased incorporation of [3H]thymidine into liver DNA of rats treated with NDMA was enhanced compared to that of pair-fed rats treated with NDMA. The activity of thymidine kinase in liver of copper deficient rats treated with NDMA was also found to increase ingnificantly compared to that of pair-fed rats treated with NDMA.View full abstractDownload PDF (581K) -
Osamu MURAOKA, Tomoaki SAWADA, Eiichiro MORIMOTO, Genzoh TANABE1993 Volume 41 Issue 4 Pages 772-774
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA facile synthetic route was developed to (±)-magnosalicin (1), a new type of neolignan with antiallergy activity isolated from Magnolia salicifolia, starting from a chalcone, 1, 3-bis(2', 4', 5'-trimethoxyphenyl)prop-2-en-1-one (3).View full abstractDownload PDF (517K) -
Takamasa IIMORI, Yasushi MURAI, Yasuhiro WAKIZAWA, Yasuo OHTSUKA, Shok ...1993 Volume 41 Issue 4 Pages 775-777
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSConformational restrictions of sangivamycin (1) could be achieved by the use of the gauche effect of the substitutents on the ribofranose moiety. The conformational deviations obtained by this method were found to nicely correlate with the inhibitory activity of PKC.View full abstractDownload PDF (487K) -
Yoshinori NAKAMURA, Taishin AKIYAMA, Yoshiyuki YONEDA, Kiyoshi TANAKA, ...1993 Volume 41 Issue 4 Pages 778-780
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOligodeoxynucleotide linked to 5-deazaflavin was synthesized and its redox potential was investigated from the viewpoint of duplex formation with a complementary strand.View full abstractDownload PDF (400K) -
Hiroshi MORITA, Tetsuo YAMAMIYA, Koichi TAKEYA, Hideji ITOKAWA, Chisek ...1993 Volume 41 Issue 4 Pages 781-783
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS^1H NMR spectroscopy has been used to demonstrate specific binding of rat 80S ribosomes to the major conformer of an antitumor bicyclic hexapeptidic glucoside, RA-XII, isolated from Rubia cordifolia, in a fast exchange process.View full abstractDownload PDF (411K) -
Mugio NISHIZAWA, Dulce M. GARCIA, Toshiyuki SHIN, Hidetoshi YAMADA1993 Volume 41 Issue 4 Pages 784-785
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA 0.1 eq of zinc p-tert-butylbenzoate significantly accelerates glycosylation of alcohol with glycopyranosyl chloride in the presence of 2-methyl-2-butene to give β-glycoside in high yield with fair to good β-selectivity.View full abstractDownload PDF (363K) -
Hitoshi YOSHIMITSU, Kazuhiro HAYASHI, Miki KUMABE, Toshiro NOHARA1993 Volume 41 Issue 4 Pages 786-788
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structures of two cycloartane glycosides isolated from the methanolic extract of Thalictri Herba (Takatogusa), the dried aerial parts of Thalictrum sp. plants (Ranunculaceae), have been established on the basis of chemical evidence and spectroscopic means.View full abstractDownload PDF (418K) -
Yuko TAKEMURA, Yoshiko ISONO, Motoharu JU-ICHI, Mitsuo OMURA, Chihiro ...1993 Volume 41 Issue 4 Pages 789-790
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAzacridone-A (1), the first naturally occurring azaacridone alkaloid, was isolated from the roots of Marsh grapefrit (Citrus paradisi Macf.), and its structure was determined by spectroscopic evidence.View full abstractDownload PDF (352K) -
Mugio NISHIZAWA, Hideyuki TAKENAKA, Tetsuyuki KOHNO, Hiroko TAKAO, Hid ...1993 Volume 41 Issue 4 Pages 791-792
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSChiral oxygen functionality located in a polyene chain controls the chirality during mercury (II) triflate induced biomimetic olefin cyclization to give carbocycles under a virtually complete chirality transfer.View full abstractDownload PDF (362K) -
Akimori WADA, Miho SAKAI, Yasushi IMAMOTO, Yoshinori SHICHIDA, Toru YO ...1993 Volume 41 Issue 4 Pages 793-795
Published: April 15, 1993
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS11Z-8, 18-Ethanoretinal was synthesized from the β-ionone alaog (5) via the Witting reaction, and its binding experiment with bovine opsin afforded the new rhodopsin analog, whose opsin shift and CD spectrum were similar to those of the native rhodopsin.View full abstractDownload PDF (434K)
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