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Volume 42, Issue 7
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Makoto SUNAGAWA, Akira SASAKI, Haruki MATSUMURA, Koshiro GODA, Katsumi ...1994 Volume 42 Issue 7 Pages 1381-1387
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn efficient synthesis of 1β-methylcarbapenem from the 1-(2-oxoazetidinyl)acetate 8 was developed by application of the Dieckmann reaction. Dieckmann-type cyclization of 8 and conversion to the enolphosphate 10 were achieved without epimerization to the 1α-methyl isomer in a one-pot procedure. Treatment with the mercaptan 22 after the phosphorylation resulted in a practical one-pot preparation of the 1β-methylcarbapenem derivative 23 from 8.View full abstractDownload PDF (1074K) -
Koichi MACHIDA, Masao KIKUCHI1994 Volume 42 Issue 7 Pages 1388-1392
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree new γ-lactone glycosides, named viburnolides A (1), B (4) and C (6), were isolated from the leaves of Viburnum wrightii MIQ., and their structures have been determined on the basis of spectral analysis and chemical evidence.View full abstractDownload PDF (724K) -
Masahiro SAKAGAMI, Hideaki MURATAKE, Mitsutaka NATSUME1994 Volume 42 Issue 7 Pages 1393-1398
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn important chiral ketone derivative, (3S, 4R)-3-methyl-4-pivaloyloxy-3-vinylcyclohexan-1-one (16) was prepared from (R)-(-)-carvone (10) using a stereo-controlled conjugate addition of the vinyl group to (R)-3-methyl-6-(1-methylethylidene)-4-pivaloyloxy-2-cyclohexen-1-one (13). The first enantiospecific total synthesis of a terrestrial blue-green alga constituent, hapalindole O (1) was accomplished by condensation of this ketone 16 with α, α-dimethyl-1-(p-toluenesulfonyl)-1H-indole-4-methanol (6) to construct the fundamental carbon framework of the hapalindole 21, followed by introduction of the nitrogen function, stereoselective reduction of the tetra-substituted double bond with lithium aluminum hydride, and subsequent isothiocyanate formation.View full abstractDownload PDF (1040K) -
Li HAN, Tsutomu HATANO, Takashi YOSHIDA, Takuo OKUDA1994 Volume 42 Issue 7 Pages 1399-1409
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new complex tannins, camelliatannins F (3) and G (4), were isolated from the leaves of Camellia japonica L. (Theaceae), and their structures, each consisting of an epicatechin unit and a C-glucosidic ellagitannin moiety, were elucidated. A new dimeric hydrolyzable tannin, named camelliatannin H (5), was isolated from the fruits of this plant. Camelliins A (6) and B (7), and camelliatannin A (1) and 3 were also isolated from the fruits.View full abstractDownload PDF (1177K) -
Motomasa KOBAYASHI, Kohji KANZAKI, Seiji KATAYAMA, Kazuyoshi OHASHI, H ...1994 Volume 42 Issue 7 Pages 1410-1415
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFollowing the characterization of theonellapeptolides Ia-Ie (2-6), another new tridecapeptide lactone named theonellapeptolide IId (1) was isolated from the Okinawan marine sponge Theonella swinhoei. The structure of 1 has been determined on the bases of chemical and physicochemical examinations which included an HPLC-CD combined analysis of the amino acid composition. Theonellapeptolide IId (1) prevented fertilization of the sea urchin Hemicentrotus pulcherrimus at the concentration of 25 μg/ml or greater but did not affect early embryonic development of fertilized eggs up to the gastrula stage.View full abstractDownload PDF (788K) -
Isao KITAGAWA, Taifo MAHMUD, Partomuan SIMANJUNTAK, Kazuyuki HORI, Tah ...1994 Volume 42 Issue 7 Pages 1416-1421
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree new apotirucallane-type triterpenoids named bruceajavanin A (1) dihydrobruceajavanin A (2), and bruceajavanin B (3), and a novel β-carboline alkaloidal glycoside named bruceacanthinoside (4) were isolated from the stems of Brucea javanica (Simaroubaceae), a traditional medicine used to treat malaria in the Bengkulu area, Sumatra, Indonesia. Their chemical structures have been elucidated on the bases of their chemical and physicochemical properties. Bruceajavanin A (1), dihydrobruceajavanin A (2) and bruceacanthinoside (4) were shown to inhibit growth of the cultured malarial parasite Plasmodium falciparum K1 of a chloroquine-resistant strain.View full abstractDownload PDF (825K) -
Hosenkosides F, G, H, I, J, and K, Novel Baccharane Glycosides from the Seeds of Impatiens balsaminaNoboru SHOJI, Akemi UMEYAMA, Nobuaki SAITOU, Kazuko YOSHIKAWA, Masahir ...1994 Volume 42 Issue 7 Pages 1422-1426
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the seeds of Impatiens balsamina we have isolated six novel baccharane glycosides, hosenkosides F-K. The structures of all isolates were determined by the use of two dimensional (2D) NMR techniques (1H-1H correlation spectroscopy (COSY), heteronuclear multiple quantum coherence (HMQC), heteronuclear multiple-bond correlation (HMBC), rotating frame Overhauser enhancement spectroscopy (ROESY), total correlation spectroscopy (TOCSY)) and chemical derivatization. Hosenkosides F, H and I are hosenkol B 3-O-sambubiosido-26-O-glucoside, 3-O-sambubioside and 3, 26-O-diglucoside, respectively. Hosenkoside G is hosenkol C 3-O-sambubiosido-28-O-glucoside. Hosenkosides J and K are hosenkol A 3-O-sophoroside and 3-O-sophorosido-26-O-glucosyl-28-O-glucoside, respectively.View full abstractDownload PDF (820K) -
Sanan SUBHADHIRASAKUL, Hiromitsu TAKAYAMA, Norio AIMI, Dhavadee PONGLU ...1994 Volume 42 Issue 7 Pages 1427-1431
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSChemical investigation of the leaves of Rauwolfia sumatrana JACK. collected in Thailand resulted in the isolation of three new indole alkaloids, 11-methoxystrictamine (1), rausutrine (4) and rausutranine (7), along with ten known bases, harman, tetraphyllicine, flexicorine, lanceomigine, perakine, β-carboline, peraksine, 10-hydroxystrictamine, cabufiline and compactinervine. Rausutrine (4) and rausutranine (7) are novel bis-indole alkaloids composed of an akuammilane unit and a vincorane unit, the latter of which has a unique iminoquinone function.View full abstractDownload PDF (723K) -
Kazuaki OKABE, Mitsutaka NATSUME1994 Volume 42 Issue 7 Pages 1432-1436
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA non-opioid analgesic, epibatidine (1), isolated from Ecuadoran poison frogs was synthesized in the racemic form starting from a readily available compound 2. A partial Curtius rearrangement product 5 of 2 was converted into 12c by way of the ketone 3 and its condensation product with the pyridine moiety 9c, and catalytic hydrogenation of 12c was specifically conducted in hydrochloric acid-containing 2-propanol for the preferential formation of an exo-product 15b. Conversion of the substituent from 15b to 15a in a single operation using the Vilsmeier reagent, followed by deprotection of the p-toluenesulfonyl group with hydrobromic acid completed an eight-step synthesis of (±)-1 from 2.View full abstractDownload PDF (991K) -
Jyoji KURITA, Makoto ISHII, Shuji YASUIKE, Takashi TSUCHIYA1994 Volume 42 Issue 7 Pages 1437-1441
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe Group 14 (Si, Ge, and Sn), Group 15 (P, As, Sb, and Bi), and Group 16 (Se and Te) 2-trimethylsilyl-1-benzometalloles (7) were prepared by the reaction of the corresponding metal reagents with β, o-dilithio-β-trimethyl-silylstyrene intermediate (6), which was derived from phenylacetylene or o-bromoiodobenzene via three steps. The trimethylsilyl group in 7 could be readily removed by treatment with tetrabutylammonium fluoride to give the C-unsubstituted 1-banzometalloles (10).View full abstractDownload PDF (778K) -
Youichi KIMURA, Shohgo ATARASHI, Masanobu TAKAHASHI, Isao HAYAKAWA1994 Volume 42 Issue 7 Pages 1442-1454
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of 7-[3-(1-aminoalkyl and 1-aminocycloalkyl)-1-pyrrolidinyl]quinolones have been prepared and their biological properties evaluated. Among them, 1-(S)-aminoalkyl derivatives exhibited potent antibacterial activities against gram-positive and gram-negative organisms. They had moderate lipophilicity and high aqueous solubility compared to their aminomethyl counterparts; e.g., the 3-(1-aminoethyl)-1-pyrrolidinyl compound (83) showed superior pharmacokinetic properties to its aminomethyl counterpart (6).View full abstractDownload PDF (1725K) -
Rin-ichi YAMASHITA, Takahiro TOMIMOTO, Yushin NAKAMURA1994 Volume 42 Issue 7 Pages 1455-1458
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBenzidine derivatives, especially 2, 7-diaminofluorene and benzidine, accelerated the cleavage of a plasmid DNA (form I) under weakly acidic conditions at 37°C. The acceleration was not inhibited by EDTA, superoxide dismutase, catalase, or hydroxyl radical scavengers. The rate of the cleavage was influenced by the pH value of the reaction buffer. The decrease in form I DNA in this reaction obeyed first-order kinetics. It was confirmed that the cleavage was enhanced by the amines themselves, and not by their oxidized derivatives. 2, 7-Diaminofluorene also cleaved a 3'-end-labeled 40-mer DNA with A and G base specificity. These results indicate that the acceleration is caused by depurination followed by breakage of the DNA sugar backbone.View full abstractDownload PDF (780K) -
Hiroyuki SAWANISHI, Shinya WAKUSAWA, Rieko MURAKAMI, Ken-ichi MIYAMOTO ...1994 Volume 42 Issue 7 Pages 1459-1462
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDiamines, dicarboxamides, and disulfonamides that have terminal benzene, methyl- or chloro-substituted benzene rings were synthesized and evaluated for the activity of [3H]vinblastine accumulation in multidrug-resistant P388/ADR cells. The efficacy of these compounds was generally in the order of dicarboxamides<diamines<disulfonamides. N-Methylated diamine and disulfonamide compounds having terminal methyl- or chloro-substituted benzene rings in their structure also showed rather potent efficacy. From these findings, we synthesized a novel disulfonamide compound, 1, 2, 3, 4, 5, 6-hexahydro-2, 5-bis(p-toluenesulfonyl)benzo[2, 5]diazocine (22). Compound 22 suppressed the efflux of vinblastine from P388/ADR cells and increased its intracellular accumulation, while it barely increased the vinblastine accumulation in sensitive cells (P388/S). Compound 22 significantly potentiated the growth-inhibitory effects of vinblastine, vincristine, colchicine and Adriamycin against P388/ADR cells in vitro.View full abstractDownload PDF (707K) -
Sachio OHNO, Yuko ADACHI, Masayuki KOUMORI, Kiyoshi MIZUKOSHI, Mitsuak ...1994 Volume 42 Issue 7 Pages 1463-1473
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of new (5R, 8R, 10R)-ergoline derivatives was synthesized, and their antihypertensive and dopaminergic activities were tested in conscious spontaneously hypertensive rats and in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra. (5R, 8R, 10R)-6-Alkyl-8-ergolinemethanols, prepared from the corresponding ergolinecarboxylates, were converted to the tosylates, which were treated with various five-membered heterocycles containing nitrogen atoms to afford the new ergolines. (5R, 8R, 10R)-8-(1, 2, 4-Triazol-1-ylmethyl)-6-methylergoline (4s, maleate : BAM-1110) exhibited potent dopaminergic activity, about 18-fold greater than that of bromocriptine mesylate. (5R, 8R, 10R)-8-(1, 2, 4-Triazol-1-ylmethyl)-6-propylergoline (8b, fumarate : BAM-1602) showed extremely potent dopaminergic activity, being about 220 and 1.15 times more active than bromocriptine mesylate and pergolide mesylate, respectively. Several compounds exhibited potent antihypertensive activity. Structure-activity relationships for antihypertensive and dopaminergic activities are discussed.View full abstractDownload PDF (1191K) -
Ryoichi UNNO, Takuji YAMAGUCHI, Toshinao USUI, Takuji KAKIGAMI, Masato ...1994 Volume 42 Issue 7 Pages 1474-1478
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOptically active and racemic 2-substituted 6-fluoro-2, 3-dihydrospiro[4H-1-benzopyran-4, 4'-imidazolidine]-2', 5'-diones were synthesized stereoselectively from (+)-, (-)-, and (±)-6-fluoro-3, 4-dihydro-4-oxo-2H-1-benzopyran-2-carboxylic acid [(+)-1, (-)-1, and (±)-1], respectively, for evaluation as new aldose reductase inhibitors. Among these compounds, the 2S, 4S compounds were found to be more potent inhibitors of aldose reductase in vitro and in vivo than the corresponding 2R, 4R enantiomers. The chloromethyl compound [(+)-5] showed highly potent activities in inhibiting cataract formation in the lenses and polyol accumulation in the sciatic nerve of rats.View full abstractDownload PDF (812K) -
Takashi IIDA, Shinnosuke TAZAWA, Yukari OHSHIMA, Toshifumi NIWA, Junic ...1994 Volume 42 Issue 7 Pages 1479-1484
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe glucuronide, glucoside and N-acetylglucosaminide conjugates of hyodeoxycholic acid were synthesized. In addition, murideoxycholic acid 3-glycosides and some of their C-5 epimeric analogs were also prepared. The principal reactions used are 1) the Koenigs-Knorr condensation reaction of 3-oxo-6α-hydroxy and 6-oxo-3α-hydroxy esters with an appropriate α-acetohalosugar catalyzed by cadmium carbonate in benzene under reflux, 2) reduction of the resulting bile acid glycoside methyl ester-acetates with tert-butylamine-borane complex, and 3) subsequent hydrolysis with aqueous lithium hydroxide.View full abstractDownload PDF (935K) -
Shinji NARISAWA, Hiroyuki YOSHINO, Yoshiyuki HIRAKAWA, Kazuo NODA1994 Volume 42 Issue 7 Pages 1485-1490
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPorous ethylcellulose (EC) film coating technique was used in preparing a capsule-type controlled release dosage form, in which theophylline (TP) was used as a poorly water-soluble model drug. The TP-loaded uncoated beads were spray-coated with an aqueous ethanolic or ethanolic EC solution, and the drug release characteristics and productivity of each product were examined. When the aqueous ethanol was used as the solvent of the coating solution, a large number of micropores were formed in the coating, and the porosity of coating and drug release rate could be controlled by altering the ethanolic concentration in the coating solution. In addition, few agglomerates were produced in the coating process, even though there was no anti-agglomeration agent in the coating solution. The drug release rate from the coated beads could be changed by film porosity as well as film thickness. Superposition analysis revealed that the EC-coated beads with different film porosities or different coating levels had the same drug release mechanism. It was further found that the drug release behavior of the porous EC film-coated beads was not affected by any simulated physiological conditions such as pH, surface tension, ionic strength or paddle rotation speed, indicating that in vivo drug release should not be affected by such physiological conditions in the gastrointestinal tract.View full abstractDownload PDF (1178K) -
Shinji NARISAWA, Hiroyuki YOSHINO, Yoshiyuki HIRAKAWA, Kazuo NODA1994 Volume 42 Issue 7 Pages 1491-1495
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe mechanical characteristics of porous ethylcellulose (EC) film as a barrier in a controlled release dosage form were investigated. Sprayed EC films with various porosities were prepared by changing the ethanolic concentrations in the EC spraying solution, and their film porosities (ε) and tensile strength (Ts) were measured. It was found that the Ts of EC films decreased with an increase in ε, and that the quantitative relationship between both parameters was considerably adapted to the equation proposed by Bal'shin. By using the permeability-ε and Ts-ε relations, the mechanical strength of two EC films with different porosities were estimated under the assumption that the drug permeation rate through the two films was equal. The result suggested that, when the permeation rate was equal, a film with higher porosity would have higher mechanical strength. This was also proved by a high-shear dissolution test for theophylline beads coated with EC film. The in vivo drug release behavior from porous EC film-coated beads agreed well with the in vitro drug release, indicating that the porous EC film-coated beads had sufficient strength to withstand the mechanical stress of the gastrointestinal tract, and that the porous EC film coating could be used as a barrier for controlled release preparations.View full abstractDownload PDF (1126K) -
Toru HAKATA, Hiroshi SATO, Yoshiteru WATANABE, Mitsuo MATSUMOTO1994 Volume 42 Issue 7 Pages 1496-1500
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of storage temperature on the physicochemical properties of soft gelatin capsule shells was studied to interpret a change in the internal structure of those capsule shells whose disintegration time was remarkably prolonged by storage at 40°C or more. The capsules were stored at 25, 40 or 60°C for a maximum of 6 months. The time-courses of the disintegration time of these capsules were determined and compared with those of the following three physicochemical properties of the shells : the equilibrium swelling ratio (Seq), the gel strength of the swollen shells, and the percent of gelatin dissolved after 10 min (D10) from the shells. From these evaluations, it was found that the prolongation of the disintegration time of the capsules stored at 40°C was based on a decrease in Seq of the shells and/or D10 of gelatin from the shells, and/or an increase in the gel strength of the swollen shells.In addition, these physicochemical properties of the shells stored at different temperatures were compared with those of shells treated with formaldehyde. The three properties of the shells stored at 40°C for 6 months were, on the whole, similar to those of the shells treated with a 1% formaldehyde solution. Furthermore, in the relationships between D10 or gel strength, and Seq, no fundamental difference was observed between the shells stored at various temperatures and those treated with formaldehyde.Thus, we demonstrated that the prolongation of the disintegration time of the soft gelatin capsules stored at 40°C or more is brought about by a change in the internal structure of the capsule shells in a manner similar to the case of shells treated with formaldehyde.View full abstractDownload PDF (801K) -
Hiroyuki SAITO, Kenzo KITAMURA, Toshiro HIGASHI, Yasuhiko NAKAMURA1994 Volume 42 Issue 7 Pages 1501-1505
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to elucidate the factors affecting drug release characteristics from triglyceride suppositories, we have measured the solid fat index (SFI) of triglyceride suppository bases by the differential scanning calorimetry method. When Witepsol H15, widely used for suppository bases, was stored at 30°C for 2 weeks, an increase in the SFI value of Witepsol H15 occurred, resulting in decreases in the release rate of morphine hydrochloride from stored suppositories. However, the degree of increase in SFI of stored Witepsol H15 was found to be different among some lots. To further investigate the relation between SFI and drug release rate in triglyceride bases, mixed bases of Witepsol H15 and Witepsol E85, which have various SFI values, were prepared. The addition of Witepsol E85 to Witepsol H15 resulted in an increase in SFI of the Witepsol H15-Witepsol E85 (H15-E85) mixed base. The increase of SFI brought about changes in some physicochemical properties of the H15-E85 mixed base such as increases in the melting point and the apparent viscosity. The release profiles of brilliant blue as a model drug from the H15-E85 mixed base could be expressed by Jander's equation. The logarithms of the release rate constants of brilliant blue from the H15-E85 mixed base, as well as those of morphine hydrochloride from stored Witepsol H15, were found to have a linear relation with SFI. These results indicate that SFI, which is considered to directly represent the melting state of suppository bases, is closely correlated with the drug release rate from triglyceride suppository bases.View full abstractDownload PDF (625K) -
Hiroyuki SAITO, Toshihito TAKATORI, Toshiro HIGASHI, Yasuhiko NAKAMURA1994 Volume 42 Issue 7 Pages 1506-1509
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel controlled release suppository consisting of Witepsol H15 as a triglyceride base and polyglycerol ester of fatty acid (PGEF) has been designed and developed. The addition of PGEF to Witepsol H15 resulted in an increase in the solid fat index (SFI), which is correlated with melting point and apparent viscosity, of the Witepsol H15-PGEF (H15-PGEF) mixed base in a similar manner to the case of Witepsol H15-Witepsol E85 (H15-E85) mixed base. In the in vitro release tests, the release rate of Brilliant Blue from the H15-PGEF mixed base was reduced with increase of PGEF content, indicating that the drug release rate from the H15-PGEF mixed base depended on SFI. The change in the drug release rate from the H15-PGEF mixed base with temperature in release tests ranging from 36°C to 39°C was small, whereas the release rate in the H15-E85 mixed base changed significantly with temperature. These changes in drug release rate with temperature in the H15-E85 and H15-PGEF mixed bases were found to be attributable to the variation of SFI of both the mixed bases. In addition, the change in SFI during storage at 30°C in the H15-PGEF mixed base was relatively small as compared with that of the H15-E85 mixed base. From these results, the H15-PGEF mixed base is expected to be useful for stable controlled release suppositories.View full abstractDownload PDF (667K) -
Yukihiro GODA, Kyoko SATO, Natsuko HORI, Mitsuharu TAKEDA, Tamio MAITA ...1994 Volume 42 Issue 7 Pages 1510-1513
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIon-chromatographic analyses were performed to quantitate the halide ions liberated by photo-irradiation from halogen-substituted xanthene colors (Food Red Nos. 3, 104 and 105). To elucidate the wavelength dependency of this phenomenon, aqueous solutions of the xanthene colors were photo-irradiated through various optical filters to provide selected transmission bands. The results suggest that the liberation of bromide and iodide from the xanthene moiety and chloride from the benzene moiety follows irradiation with visible light and UV light, respectively. It is known that solutions of these xanthene colors produce singlet oxygens via phtoactivation of the dye molecule and transfer of the energy to dissolved oxygen. Therefore, the liberation was also studied in the presence of the substances which alter the life-time of singlet oxygen. The results suggest that singlet oxygen has some effect on the liberation of halide ions from these food colors.View full abstractDownload PDF (693K) -
Akira KATOH, Mika INOKAWA, Junko OHKANDA, Keiryo MITSUHASHI1994 Volume 42 Issue 7 Pages 1514-1517
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA commercially available L-glutamic acid γ-methyl ester was converted into the corresponding urea-containing α-amino acid via the hydrazide, the azide, and then the isocyanate. The condensation of the urea-containing α-amino acid with β-diketones under acidic conditions afforded 2(1H)-pyrimidinone-containing α-amino acid derivatives in reasonable yields. The 1H-NMR analysis of the dipeptide indicated that no detectable racemization had occurred during the chemical modification of L-glutamic acid.View full abstractDownload PDF (587K) -
Ayumi FUJII, Satoshi TSUBOI, Keiichi ASADA, Yoko NAGAMATSU, Junichiro ...1994 Volume 42 Issue 7 Pages 1518-1521
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA nonapeptide, H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OH, corresponding to sequence 41-49 of eglin c inhibited leukocyte cathepsin G and α-chymotrypsin with Ki values of 2.2×10-5 and 7.2×10-6M, respectively, although eglin c itself inhibited leukocyte elastase, cathepsin G and α-chymotrypsin with Ki values of 6.0×10-9, 5.5×10-9 and 2.5×10-9M, respectively. The inhibitory activity of the nonapeptide decreased following incubation with cathepsin G due to the cleavage of the Leu45-Asp46 peptide bond. Therefore, Leu45 and/or Asp46 were replaced with D-amino acids and the inhibitory activities of the resultant nonapeptides were examined. Their inhibitory activities against cathepsin G and α-chymotrypsin were much weaker than those of the all-L-type nonapeptide, suggesting that the amino acids at the active site, Leu45 and Asp46 are required to be in the L-configuration for potent activity.View full abstractDownload PDF (702K) -
Masahiro KAJIWARA, Ryuichi UEGAKI, Katsumi IIDA, Yoko WADA1994 Volume 42 Issue 7 Pages 1522-1524
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS^<13>C-Nuclear magnetic resonance (13C-NMR) spectroscopy has been used to locate deuterium atoms incorporated biosynthetically into erythromycin from [3-13CD3]- and [3-13C]sodium propionate and L-[13CD3]- and L-[13C]methionine in Saccharopolyspora erythraea JCM 4748. The α-shifts of deuterated methyl groups were clearly observed in broad-band deuterium and proton-decoupled 13C-NMR spectra. The seven propionate-derived methyl groups and the four methionine-derived methyl groups were shown to undergo no exchange of methyl protons during the biosynthesis of erythromycin.View full abstractDownload PDF (450K) -
Yasushi ISHIHAMA, Yoshiya ODA, Kiyohiko UCHIKAWA, Naoki ASAKAWA1994 Volume 42 Issue 7 Pages 1525-1527
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMicellar electrokinetic chromatography (MEKC) was used to measure hydrophobicity of 18 aromatic compounds. The capacity factors, which are proportional to the micelle-water distribution coefficients, were closely correlated with the octanol-water partition coefficients. The addition of Brij 35 to the charged micelle was effective in improving the correlation because the surface charges of the micelle were shielded.View full abstractDownload PDF (455K) -
Toshihiro HASHIMOTO, Shigenobu TAHARA, Shigeru TAKAOKA, Motoo TORI, Yo ...1994 Volume 42 Issue 7 Pages 1528-1530
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel binaphthyl (1) and three novel benzophenone derivatives (2-4) have been isolated from the fungus (Ascomycetes) Daldinia concentrica. Their structures have been established by a combination of high resolution NMR spectra, X-ray crystallographic analysis and chemical degradation. Compounds 2 and 3 possess plant-growth inhibitory activity.View full abstractDownload PDF (441K) -
Toshihiro HASHIMOTO, Kyoko AKAZAWA, Motoo TORI, Yukiko KAN, Takenori K ...1994 Volume 42 Issue 7 Pages 1531-1533
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree novel polyacetylene triglycerides, named lycogarides A-C (1-3), have been isolated from the Myxomycetes Lycogala epidendrum. Their relative structures have been established by a combination of two-dimension NMR spectroscopy and chemical degradation. The absolute structures of compounds 1 and 2 were deduced from the modified Mosher's and dibenzoate exiton chirality methods of their derivatives.View full abstractDownload PDF (415K) -
Yuko YAMANISHI, Keiko TAMURA, Kazuo SHIMIZU, Masayuki NAITO, Tsutomu M ...1994 Volume 42 Issue 7 Pages 1534-1535
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo split laser beams were introduced from the bottom side of the stage of an optical microscope, and combined at the sample position on the stage. The straight stripes which were produced by the interference of the two beams were observed in the focal plane of the objective lens. The distance between two adjacent stripes was 630nm and gave the scale for two-dimensional microscopic image, and the displacement of the stripes gave us information about the thickness and/or concentration of the sample. This optical scale is the measure for dimensional scaling of a microbody in sub-micron resolution.View full abstractDownload PDF (649K) -
Noriko KOBAYASHI, Chiaki HAGIWARA, Masuo MORISAKI, Masatoshi YURI, Yos ...1994 Volume 42 Issue 7 Pages 1536-1538
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIncubation of 3α, 7α-dihydroxy-5β-cholestan-26-oic acid and its Δ24- analog with rat liver homogenate produced a mixture of C-24, 25 diastereoisomers of 3α, 7α, 24-trihydroxy-5β-cholestan-26-oic acid, a key intermediate of chenodeoxycholic acid biosynthesis.View full abstractDownload PDF (397K) -
Kiyoshi TANAKA, Kaoru FUJI, Toshio YOKOI, Tetsuro SHINGU, Bo LI, Hando ...1994 Volume 42 Issue 7 Pages 1539-1541
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structures of taxchinin E, H, I, J, K and taxchin B, isolated from Taxus chinensis, have been elucidated by means of NMR spectroscopy. The former five possess a rearranged taxoid skeleton, and the latter has an ordinary taxane framework.View full abstractDownload PDF (453K) -
Toshihiro HASHIMOTO, Hironao TANAKA, Yoshinori ASAKAWA1994 Volume 42 Issue 7 Pages 1542-1544
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe stereostructure of plagiochiline A (1) isolated from the liverwort Plagiochila fruticosa has been established by X-ray crystallographic analysis. Plagiochiline A was converted into plagiochilal B (2) and furanoplagiochilal (3) by human saliva, and stearoylvelutinal (4) isolated from the fungus Lactarius vellerus was converted into velleral (5), also by human saliva.View full abstractDownload PDF (438K) -
Mitsuo NAGAI, Hiroyuki YOSHIMURA, Shigeki HIBI, Kouichi KIKUCHI, Shiny ...1994 Volume 42 Issue 7 Pages 1545-1547
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPractical and facile total syntheses of the remarkably unstable (R)-(+)-14-hydroxy-4, 14-retro-retinol [(R)-14HRR] 1 and of its enantiomer 2 have been achieved via an acid-catalyzed dehydration reaction of the respective tetraeneol intermediates 10 and its enantiomer obtained from (R)-(+)-1, 2-O-isopropylidene-butane-1, 2, 3-triol 3.View full abstractDownload PDF (429K) -
Yuko TAKEMURA, MOTotoharu JU-ICHI, Toshihiro HASHIMOTO, Yukiko KAN, Sh ...1994 Volume 42 Issue 7 Pages 1548-1549
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel type bisacridone alkaloid, named citbismine-A, was isolated from the roots of Marsh grapefruit; its structure was elucidated by spectroscopic method and unequivocally by X-ray crystal analysis as 1.View full abstractDownload PDF (385K) -
Takashi HARAYAMA, Keiko KATSUNO, Yoshitaka NISHITA, Masako FUJII1994 Volume 42 Issue 7 Pages 1550-1552
Published: July 15, 1994
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour coumarins (1-4) were synthesized by routes shown in Charts 2-5, respectively. A proposed structure for a new coumarin isolated from Artemisia carviforia was incorrect, and the structure of coumarin should be represented by formula (3).View full abstractDownload PDF (416K)
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