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Volume 47, Issue 6
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Hideko KAWAKI1999 Volume 47 Issue 6 Pages 723-726
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe descriptor μ2/α was introduced by the classical equations for the orientation and induction energies. As the descriptor has the dimension of energy, it is not convenient to discuss in detail. The dipole moment in the benzene series μaro is evaluated from both the bond moment μb and the mesomeric moment μm. We redefine the new descriptors σbd and σms modifind to dimensionless values from μb and μm for the standard benzene as well as the descriptor σS°. The relative retention values logγ on monosubstituted benzene derivatives are analyzed satisfactorily, using σS°, σbd, and σ+ms for electron-donating group, and a new descriptor (σS°·σbd)1/2(N), which has a relation to the depole moment of the excited state in C<ipno&tg;-N bond of the aniline series.logγ=4.41(0.561)σS°+0.209(0.042)σbd+ 0.336(0.153)σ+ms + 1.592(0.441)(σS°·σbd)1/2(N)+0.004(0.096)n=22, r=0.981, F=110.21, S.D.=0.064 It is suggested that EHB of aniline or N, N-dimethylaniline can be expressed by EES in gaseous interaction.View full abstractDownload PDF (642K) -
Manabu MATSUMURA, Kazutaka YAMADA, Masayoshi FUJIMAKI, Hiroshi SUGIHAR ...1999 Volume 47 Issue 6 Pages 727-731
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhysicochemical properties of a newly developed oral negative contrast agent, oral magnetic particles (OMP, Ferristene), for abdominal magnetic resonance (MR) imaging were evaluated in a preformulation study. X-Ray diffiraction pattern and transmission electron micrograph showed that a fine ferrite of iron oxide (diameter less than 30 nm) is absorbed onto the latex particles (approximately 3.5 μm). The longitudinal proton relaxation of an aqueous system containing OMP proceeded mono-exponentially. The transverse proton relaxation, which was much faster than the longitudinal one, proceeded multi-exponentially, where initial fast decay within first echo followed by bi- or mono-exponential decay was observed. This initial fast decay was characterized as percentage of initial magnetic loss (%IML), which increased with increase in OPM concentration, echo time (TE), or both.The %IML is believed to be a result of water protons which diffiuse through strong magnetic field gradient close to the OMP causing them to lose phase coherence of spins prior to the first echo. For the practical use of spin echo sequence in a clinical MR imaging system (TE≥10 ms), the OMP concentration around 100 μg Fe/ml for oral suspension seemed preferable for suppression of the signal intensity from the gastrointestinal tract.View full abstractDownload PDF (1181K) -
Lee-Yong LIM, Mei-Lin GO1999 Volume 47 Issue 6 Pages 732-737
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe interaction of halofantrine with phosphatidylcholine and phosphatidylethanolamine bilayers has been investigated by differential scanning calorimetry. Halofantrine caused a broadening of the gel to liquid crystalline phase transition endotherm of the phosphatidylcholines. A decrease in the transition temperature Tm and enthalpy (ΔH) of transition was also observed. The varied with the chain length of the phospholipid and was more pronounced with short cahain members. Halofantrine-induced changes to the thermotropic characteristics of dipalmitoylphosphatidylcholine (DPPC)/cholesterol bilayers suggested that the penetration of halofantrine into the bilayer was diminished in the presence of cholesterol. A more complex calorimetric profile was observed in the intetaction of halofantrine with phosphatidylethanolamines and the results suggested that halofantrine did not disrupt the cooperativity of the phosphatidylethanolamine bilayers to the same extent as that observed with the phosphatidylcholines. Halofantrine caused significant perturbation of phospholipids and this property might have an important bearing on its pharmacodynamic effects.View full abstractDownload PDF (896K) -
Yoshihiro MIMAKI, Minpei KURODA, Tetsuichi FUKASAWA, Yutaka SASHIDA1999 Volume 47 Issue 6 Pages 738-743
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSChemical examination of the bulbs of Allium karataviense led to the isolation of five new spirostanol saponins (7-11) and a new furostanol saponin (12), together with a known steroidal sapogenin (1) and five known saponins (2-6). The structures of the new saponins were determined by detailed analysis of their spectral data, including two-dimensional NMR spectroscopy. The steroidal saponins produced by A. karataviense, except for 5 and 6, were found to be based upon (25R)-5α-spirostane-2α, 3β, 5, 6β-tetrol (alliogenin) and contain a β-D-glucopyranosyl moiety with the formation of an O-glycoside linkage to C-2 of the polyhudroxylated steroidal skeleton as the common structural feature. The isolated compounds were evaluated for cytostatic activity against human promyelocytic leukemia HL-60 cells.View full abstractDownload PDF (987K) -
Masato SHIGEYAMA, Toyoaki OHGAYA, Yoshiaki KAWASHIMA, Hirofumi TAKEUCH ...1999 Volume 47 Issue 6 Pages 744-748
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA desired ointment bases for better treatment of bedsores was developed to improve the release rate of minocycline hydrochloride (MH) and the water absorption capacity using various types of hydrophobic to hydrophilic ointment base. The influence of purified lanolin (PL) on the release behavior of MH from hydrophilic ointment (HO) base was primarily focused on. It wsa found that the release rate of drug increased with increase in the hydrophilicity of the base. A linear correlation between the apparent release rate constant of drug from the HO and PL mixed ointment base at various combination ratios and the elution of ointment base was noted.The HO ointment base containing 30% PL had the highest apparent release rate constant of MH. The mixed ointment base with the lowest viscosity showed the highest absorption of water and elution of ointment base. In conclusion, it was found that HO (70%) and PL (30%) mixed ointment base was a promising candidate for better treatment of bedsores.View full abstractDownload PDF (747K) -
Go YANAGIMOTO, Teruaki HAYASHI, Tetsuya HASEGAWA, Toshinobu SEKI, Kazu ...1999 Volume 47 Issue 6 Pages 749-754
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDrug fraction transported from a topical formulation on skin to subsutaneous tissues or muscles is dependent on the physicochemical properties of the entrapped drug. Cutaneous disposition of model drugs, antipyrine(ANP), lidocaine (LC) and piroxicam (PXC) as well as flurbiprofen (FP) was thus evaluated in hairless rats in which an agar gel disc was subcutaneously inserted into abdominal region as a drug receptor and a drug donor cell was placed above it. Time courses of plasma level and agar gel amount were measured after topical application of 50% ANP, 3% LC, 1% PXC and 1% FP in hydroxypropylcellulose gel. Percutaneous absorption clearance of unionized from, CL*ab was proportional to true octanol/water distribution coefficient and the order of FP>PXC>LC>ANP, suggesting that permeation of the drug was determined mainly by its distribution from the formulation to the skin barrier. PXC, however, had a relatively low flux compared to the other three drugs, probably due to its high molecular weight and meltiong point. Migration clearance of unionized form from systemic cirsulation to the subcutaneous agar gel, CL*g was also influenced by the lipophilicity of drugs. On the other hand, fraction from the formulation to the systemic circulation was in the order of PXC>FP>ANP>LC.This fraction was much higher than the direct migration fraction from the formulation to the subcutaneous agar gel. Factors determining for these fractions are still unclear. A drug having a low lipophilicity and a low prorein binding, however, had a tendency to have a great targeting ability to the subcutaneous agar gel. In addition, most of the drug in the agar gel was contributed by the direct flow from formulation, not from the systemic circulation. The present in situ experimental method is a useful tool to evaluate skin disposition of drugs. Detailed understanding of the skin disposition of drugs from several formulations will enable the finding of a good drug and formulation candidates.View full abstractDownload PDF (896K) -
Yasuyuki TAKEDA, Keiichi KAWAGOE, Aki YOKOMIZO, Yoshihiro YOKOMIZO, To ...1999 Volume 47 Issue 6 Pages 755-771
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to improve the biological characteristics of DA-3934 (5), a novel gastrin/cholecystokinin (CCK)-B receptor antagonist, phenoxyacetic acid derivatives replacing the N-methyl-N-phenylcarbamoylmethyl moiety of 5 with various alkyl chains have been synthesized and their biological activity evaluated. The relationship between the structure of these compounds and their human gastrin receptor binding affinity showed that there should be the optimal size among the various N-alkyl chains. Also a significant increase in the receptor binding affinity was achieved by several compounds. Among those compounds, 2-[3-[3-[N-cyclohexylmethyl-N-[2-(N-methyl-N-phenylcarbamoylmethoxy)phenyl]carbamoylmethyl]ureido]phenyl]acetic acid (22c) and (±)-2-[3-[3-[N-[2-(N-methyl-N-phenylcarbamoylmethoxy)phenyl]-N-(3-methylpentyl)carbamoylmethyl]ureido]phenyl]acetic acid (22h) exhibitted high affinity for human gastrin receptors and were also more potent inhibitors in a penta-gastrin-induced gastric acid secretion model than the parent compound, 5. The ED50 values of these compounds when adiministered intraduodenally to rats were 0.12 and 0.63 mg/kg, respectively.View full abstractDownload PDF (2469K) -
Serwanis Fahim SERWANIS, Piroska SZABO-REVESZ, Klara PINTYT-HODI, Pete ...1999 Volume 47 Issue 6 Pages 772-776
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSurface treatment of acetylsalicylic acid (ASA) crystals was examined in a Wurster fluid bed system with water-soluble and water-insoluble lubricants. The influence of the coating process on the flowability, the compressibility and the dissolution rate of the crystals was studied, and the results were compared with the corresponding parameters of ASA crystals processed by a conventional (mixing) method. The coating materials were Carbowax[○!R] 6000 as water-soluble and stearin as water-insoluble lubricant. The control sample was unprocessed(commercial) ASA crystals. The Strea-1 fluid bed coater with the Wurster column could be used for the production of a lubricant coating on crystal surfaces. The coated crystals, in comparison with mixed samples, had very good compactibility, cohesivity and compressibility values. Their lubrication coefficient was higher and the friction work was less than those of mixed crystals. The dissolution of the active agent could be regulated by the lubricant coat. The rate of dissolution of ASA was primarily promoted by a film coat of Carbowax[○!R] 6000 from a capsule.View full abstractDownload PDF (2001K) -
Zhe-Bin ZHENG, Sachie NAGAI, Naoko IWANAMI, Ayako KOBAYASHI, Shunji NA ...1999 Volume 47 Issue 6 Pages 777-782
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwelve analogues of the antibacterial phenolic peptide 5-S-glutathionyl-N-β-alanyl-L-dopa (5-S-GA-L-D, 1)were synthesized via orthoquinone using tyrosinase. Several synthesized compounds inhibited the v-Src autophosphorylation tyrosine kinase reaction with an IC50 value comparable to that of herbimycin A. The inhibition of c-Src substrate phosphorylation was much less active than v-Src autophosphorylation inhibition. 5-S-GA-L-D (1) and its analogous competed with peptide substrate and non-competed with ATP. The analogues showed no effects on substrate phosphorylation by epidermal crowth factor receptor (EGFR), and this selectivity is the most charagteristic feature of the 5-S-GA-L-D and its analogues (1-12).View full abstractDownload PDF (993K) -
Shigeki KOBAYASHI, Mitsue FURUKAWA, Chikako DOHI, Hajime HAMASHIMA, Ta ...1999 Volume 47 Issue 6 Pages 783-790
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of cis-Pt(NH3)2Cl2(cis-DDP)-closed circular DNA adducts with DNA topoisomerse I(topo I)were studied by electron microscopy. We identified unique topoisomers such as a singly-linked catenane (221), trefoil (31), and dimetric catenane (221), etc., by analysis with electron micrographs. These unique recombination products resulted from cis-DDP-intra-twisting looped DNA adducts by DNA topo I, and the products could be explained a new mechanism based on an odd-even number rule. Our results suggest a new model on the working mechanisms for DNA topology of cis-DDP which enhances the recombination of DNA. Based on our results, we propose the topological idea that the yields of a mini closed circular DNA and pseudo trefoil DNA, etc., can be expected by reaction of cis-DDP-DNA-histone complexes with DNA topo I in the body.View full abstractDownload PDF (1460K) -
Yasuoki MURAKAMI, Hiroshi YOKOO, Yuusaku YOKOYAMA, Toshiko WATANABE1999 Volume 47 Issue 6 Pages 791-797
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of a variety of additional substituents of ethyl pyruvate 2-(2-methanesulfonyloxy)phenylhydrazone (7) in Fischer indolization were examined, When the substituent was a methyl group at the 3-, 4-, or 5-position, the yields of normal 7-methanesulfonyloxyindoles depended upon the position. The hydrazones having a methyl group at the position nearer to the methanesulfonyloxy group tended to give normal 7-methanesulfonyloxyindole in a higher percentage to total indolic products. In a series of 4-substituted phenylthydrazones (7d, e, f), more electron-withdrawing substituents tended to give normal 7-methanesulfonyloxyindole in a higher percentage to total indolic products than electron-donating ones. A hydrazone with a strong electron-withdrawing subsitiuent at the 4-position (7f) underwent intramolecular aromatic nucleophilic substitution by the enehydrazine moiety to give the cinnoline derivative.View full abstractDownload PDF (1015K) -
Kazuko YOSHIKAWA, Koji MATSUCHIKA, Kumiko TAKAHASHI, Masami TANAKA, Sh ...1999 Volume 47 Issue 6 Pages 798-804
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structural elucidation of eleven new related polyoxypregnane glycosides, gymnepregosides G (1), H (2), I (3), J (4), K (5), L (6), M (7), N (8), O (9), P (10) and Q (11), from the roots of Gymnema alternifolium (Asclepiadaceae) was achieved by a detailed study of 1H- and 13C-NMR spectral data chemical means. The results obtained for new compounds, 1-11, show that they are (20S)-pregn-6-ene-3β, 5α, 8β, 12β, 14β, 17β, 20-heptaol 3-O-glycosides, and all the sugars at C-3 are β(1→4)linked. Some of them possess benzoyl, (E)- and (Z)-cinnamoyl, and tigloyl residues as the ester linkages located at C- 12 and/or C-20 of the aglycone.View full abstractDownload PDF (981K) -
Toru ISHIKAWA, Yasuko TANAKA, Junichi KITAJIMA, Yoshiteru IDA1999 Volume 47 Issue 6 Pages 805-808
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree monoterpenoid alcohols (one new fenchane-type and two new acyclic) and four monoterpenoid glycosides (two new thujane-type, one camphane-type and one new norfenchane-typ) were isolated from the watersoluble portion of the methanolic extract of fennel. Their structures were clarified by spectral investigation.View full abstractDownload PDF (643K) -
Akito YASUHARA, Mitsuyoshi KAMEDA, Takao SAKAMOTO1999 Volume 47 Issue 6 Pages 809-812
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe monodesulfonylation reaction of N, N-bis(methylsulfonyl)-, N, N-bis(phenylsulfonyl)-, and N, N-bis(p-tolysulfonyl)arylamines easily proceeded using tetrabutylammonium fluoride in tetrahydrofuran under mild conditions to give the corresponding N-monosulfonylarylamines in excellent yields.View full abstractDownload PDF (771K) -
Hiroshi YAMASE, Kimie UMEMOTO, Takashi OOI, Takenori KUSUMI1999 Volume 47 Issue 6 Pages 813-818
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFive new secospatane diterpenoids, secospatacetal A, B, C, D, and E have been isolated from the brown alga Dilophus okamurai DAWSON, and their structures as well as absolute configurations have been elucidated by means of NMR spectroscopy and chemical transformations Also, the structure of a known spatane diterpene has been revised.View full abstractDownload PDF (916K) -
Takashi ITOH, Yuji MATSUYA, Hiromi MAETA, Michiko MIYAZAKI, Kazuhiro N ...1999 Volume 47 Issue 6 Pages 819-823
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to clarify the role of oxygen in the reaction of amines with nitric oxide, secondary amines were allowed to react with nitric oxide in the presence of oxygen. Although N-nitrosamines were obtained as the main products in every case, the yields depended on the substituents and reaction solvents. Detailed investigation revealed that the rection proceeded by at least two pathways : one involving oxygen as a catalyst, and the other consuming the stoichiometric amount of oxygen. Both paths afforded the same nitroso adducts. It was suggested that a third path, a catalytic process via Drago's salts was also possible. The same reaction was applied to a tertiary amine, and it was found that the oxygen was consumed stoichiometrically in this case.View full abstractDownload PDF (780K) -
Takashi YOSHIDA, Fumihisa NAKATA, Takuo OKUDA1999 Volume 47 Issue 6 Pages 824-827
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree new hydrolyzable tannins, nobotanins L, M and N, were isolated from the water-soluble portion of the leaf extract of Tibouchina semidecandra, and their trimeric structures were elucidated from spectral and chemical evidence. Nobotanins L and N exist as equilibrium mixtures of four anomers due to the presence of two unacylated anomeric centers.View full abstractDownload PDF (705K) -
Yohei HAMANO, Kenzo ITO, Hajime MATSUDA, Hedeyuki SUMIYOSHI, Hidetoshi ...1999 Volume 47 Issue 6 Pages 828-832
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Hydroxypropyl-β-cyclodextrin (HP-β-CyD) was examined for potential use as an inhibitor of foaming generated by L-ascorbic acid 2-[3, 4-dihydro-2, 5, 7, 8-tetramethyl-2-(4, 8, 12-trimethyl-tridecyl)-2H-1-benzopyran-6-yl-hydrogen phosphatel potassium salt (EPC-K1). Ultraviolet (UV), circular dichroism (CD) and proton nuclear magnetic resonance (1H-NMR) spectroscopic studies suggested the formation of inclusion complexes of EPC-K1 with HP-β-CyD in aqueous solution. HP-β-CyD inhibited the foaming generated by EPC-K1 in aqueous solution in a concentration dependent manner. The inhibitory effect of HP-β-CyD on the foaming was consistent with a restoring effect on the lowered surface tension of aqueous solutions containing EPC-K1. In addition, there is a negative correlation between the free EPC-K1 concentration calculated from the stability constants of the 1 : 1 and 1 : 2 EPC-K1/HP-β-CyD complexes and the surface tension of aqueous solutions containing EPC-K1 and HP-β-CyD. Therefore, the inhibitory effect of HP-β-CyD on the foaming generated by EPC-K1 could be attributable to the abatement in the surface activity of EPC-K1 by inclusion complexation with HP-β-CyD. These data suggest that HP-β-CyD is useful in topical liquid preparations such as lotions of EPC-K1 used in pharmaceutics and cosmetics.View full abstractDownload PDF (750K) -
Hitoshi ABE, Daisuke TSUCHIDA, Setsuko KASHINO, Yasuo TAKEUCHI, Takash ...1999 Volume 47 Issue 6 Pages 833-837
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA vinyl sulfoxide, which is considered to be a moderately reactive dienophile, could be activated by neighboring participation of an epoxide group. The Diels-Alder reaction of ortho-epoxyphenyl vinyl sulfoxide with cyclopentadiene in the presence of Yb(OTf)3 proceeded smoothly even at room temperature to afford the epoxyopened cycloadducts with moderate stereoselectivity.View full abstractDownload PDF (756K) -
Hiroyuki TOKUMITSU, Hideki ICHIKAWA, Yoshinobu FUKUMORI, Lawrence H. B ...1999 Volume 47 Issue 6 Pages 838-842
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBiodegradable gadopentetic acid (Gd-DTPA)-loaded chitosan microparticles (Gd-μCPs) were prepared as a device for gadolinium neutron-capture therapy (Gd-NCT) by a novel emulsion-droplet coalescence technique : a water-oil (w/o) emulsion A containing chitosan and Gd-DTPA in droplets and a w/o emulsion B containing NaOH in droplets were mixed and stirred to solidify chitosan as a result of collision and coalescence between droplets of each emulsion. Gd-μCPs prepared by using 100% deacetylated chitosan in 25% Gd-DTPA solution were 4.1 μm (non-lyophilized) and 3.3 μm (lyophilized) in mass median diameter, and were 3.4% in gadolinium content, corresponding to 11.7% as Gd-DTPA. The particle size and gadolinium content of Gd-μCPs were not affected by Gd-DTPA concentration in the chitosan medium. However, the deacetylation degree of chitosan influenced the particle size; as the deacetylation degree of chitosan decreased, the particle size increased. The incorporated Gd-DTPA was not released entirely from Gd-μCPs in an isotonic phosphate buffered saline solution despite the high water-solubility of Gd-DTPA (less than 0.8% with every type of Gd-μCPs). These results indicated that ion-complex formation might be contributable to incorporation of Gd-DTPA. As a preliminary study, it was confirmed that the loss of γ-ray emission by gadolinium-loading in microparticle was negligible in the thermal neutron irradiation test in vitro. These results suggested that Gd-μCPs could be usefle device for intratumoral injection into solid tumor on Gd-NCT.View full abstractDownload PDF (1208K) -
Satoru WATANO, Kei MIYANAMI1999 Volume 47 Issue 6 Pages 843-846
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThis paper describes experimental and numerical analyses on the heat transfer between air and particles in an agitation fluidezed bed drying process. Spherical particles made of crystalline cellulose having been dampened to 15% were dried in an agitation fluidized bed. The effects of the operating variables such as air temperature, air velocity, agitator rotational speed and particle size on the heat transfer coefficient between air and particles were investigated experimentally. An empirical equation was then proposed to predict the heat transfer coefficient suder various operating variables and particle size. The empirical equation could predict the heat transfer coefficient very accurately.View full abstractDownload PDF (633K) -
Yasunori YAOITA, Makiko ENDO, Yoshino TANI, Kaori MACHIDA, Keiko AMEMI ...1999 Volume 47 Issue 6 Pages 847-851
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSix new sterols, 5α, 6α;8α, 9α-diepoxy-(22E, 24R)-ergost-22-ene-3β, 7α-diol (1), 5α, 6α;8α, 9α-diepoxy-(22E, 24R)-ergost-22-ene-3β, 7β-diol (2), 5α, 6α-epoxy-(22E, 24R)-ergosta-8, 22-diene-3β, 7β-diol (3), (22E, 24R)-23-methylergosta-7, 22-diene-3β, 5α, 6β-triol (4), (22E, 24R)-23-methulergosta-7, 22-diene-3β, 5α, 6β, 9α-tetrol (5) and (24S)-ergost-7-ene-3β, 5α, 6β, 9α-tetrol (6), have been isolated from seven mushrooms, Amanita pantherina, Amantia virgineoides, Lactarius piperatus, Lyophyllum shimeji, Tricholoma portentosum, Hypsizigus marmoreus and Lentinula edodes together with eighteen known ones (7-24). The structures of these new compounds were elucidated on the basis of their spectral data.View full abstractDownload PDF (814K) -
Makoto OTSUKA, Hitoshi HASEGAWA, Yoshihisa MATSUDA1999 Volume 47 Issue 6 Pages 852-856
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of polymorphic forms of bulk powder on the pharmaceutical properties of carbamazepine (CBZ)granules were investigated by using X-ray diffraction analysis, thermal analysis and Brunauer-Emmett-Teller surface area measurement. A mixture consisting of 50% CBZ forms I, II, III or IV (dehydrate) as a bulk powder, 35% crystalline α-lactose monohydrate and 15% corn starch was used as a pharmaceutical powder, with binder aqueous solutions containing 5% hydroxypropylcellulose (HPC). After kneading with the binder solution, granules were obtained using an extruding granulator. After granulation forms I, II and III were 2.5, 80.3 and 35.2%transformed into dihydrate, respectively. Next, the wet granules were dried at 60°C for 24 h, and the transformed dihydrates were dehydrated into fine particles containing form III. The yield of granules obtained from forms I, II, III and IV was 73.8, 0.0, 0.0 and 76.3%, respectively. The lower granule yields of forms II and III appeared to be due to a lack of kneading water due to absorption of CBZ as crystalline water. Therefore, to the granules of forms II and III was added extra water (60 and 30 ml/kg) to the mixture, respectively, which improved yield markedly, (to 65.1 and 69.2%), indicating the decrease in granule yield was caused by the absorption of water on transformation of dihydrate. The specific surface area (Sw) results suggested that the granules obtained from form II bulk powder had the largest Sw, and those from form I the lowest. In the order of Sw and tablet hardness of the granules, the powders ranked form II>III>IV>I. This indicated that the mechanical strength of the tablet was proportional to the Sw of the particles. The dissolution profiles of the CBZ tablets were investigated in JP XIII, 1st fluid (ph 1.2, 37±0.5°C), and the time required for 50% dissolution (T50) was measured. In the order of T50 ranking was IV≤I<III<II. These results suggested that the polymorphic transformation during the granulation and drying processes induced a change in pharmaceutical properties.View full abstractDownload PDF (734K) -
Noriaki KUDO, Satoru FURUTA, Misa TANIGUCHI, Takeshi ENDO, Kazuo SATO1999 Volume 47 Issue 6 Pages 857-868
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of diarylpyrazolecarboxylates and carboxamides were prepared, and their herbicidal activities were investigated. Some of these compounds showed noticeable pre-emergent herbicidal activities against various kinds of weeds. Among the synthesized compounds, methyl 4-chloro-1-(2, 5-difluorophenyl)-5-(4-flurophenyl)-pyzazole-3-carboxylate 19t exhibited good activity. Diarylimidazolecarboxylates and carboxamides were also synthesized, but they did not show any herbicidal activities.View full abstractDownload PDF (1434K) -
Fumiko ABE, Hikaru OKABE, Tatsuo YAMAUCHI, Keiichi HONDA, Nanao HAYASH ...1999 Volume 47 Issue 6 Pages 869-875
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSixteen glycosides of polyoxypregnanes, including two new pregnanes, isokidjoladinin and isotemontosin, were isolated form the leaves and caules of Marsdenia tomentosa collected in Fukuoka. The structures of fourteen new glycosides were elucidated and named marstomentosides A-N.View full abstractDownload PDF (963K) -
Tomoo SUZUKI, Hiroshi UESAKA, Hitoshi HAMAJIMA, Takao IKAMI1999 Volume 47 Issue 6 Pages 876-879
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn our development of srugs effective against Alzheimer's disease, we have researched a series of aromatic compounds having a characteristic cyclic amine, 1-azabicyclo[3.3.0]octane ring.In this report, we descride synthesis of a series of aromatic heterocycles with the 1-azabicyclo[3.3.0]octane ring and their pharmacological evaluation. 3-Amino-5-(1-azabicyclo[3.3.0]octan-5-yl)methyl-1, 2, 4-oxadiazole(2b) showed the highest M1 selectivity.View full abstractDownload PDF (653K) -
Tomoo SUZUKI, Hideaki INAGAKI, Hitoshi HAMAJIMA, Hiroshi UESAKA, Kohsu ...1999 Volume 47 Issue 6 Pages 880-883
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree metabolites of N-[2-(1-azabicyclo[3.3.0]octan-5-yl)ethyl]-2-nitroaniline fumarate (SK-946), a novel central muscarinic cholinergic receptor agonist, were prepared to confirm their proposed structures, and tested for muscarinic receptor affinity in vitro.View full abstractDownload PDF (642K) -
Makoto IWASHIMA, Katsumi OKAMOTO, Yoshihiko MIYAI, Kazuo IGUCHI1999 Volume 47 Issue 6 Pages 884-886
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new marine prostanoids, 4-epiclavulone II and 4-epiclavulone III, were isolated from the Okinawan soft coral, Clavularia viridis. Their structures including absolute configurations were determined based on the results of spectroscopic analysis and chemical conversion.View full abstractDownload PDF (557K) -
Yu-Yi CHAN, Yann-Lii LEU, Tian-Shung WU1999 Volume 47 Issue 6 Pages 887-889
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSInvestigation of the fresh leaves of Aristolochia heterophylla resulted in the isolation of three new compounds, madolin-N (1), madolin-O (2) and aristophyll-C(3), together with 42 known compounds. Their structures were determined by spectral method.View full abstractDownload PDF (633K) -
Luiz Claudio DI STASI, Jose Carlos GOMES, Wagner VILEGAS1999 Volume 47 Issue 6 Pages 890-893
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe anti-allergic active fractionation of hexane extracts of the leaves and stems of Anchietia salutaris var.martiana (family Violaceae) was performed by monitoring their activities with an in vitro bioassay system measuring the inhibitory effects on induced histamine release from guinea pig lung cells. Three known pentacyclic triterpenes (friedelin, α-amyrin, β-amyrin) were isolated, but these compounds were inactive. Aliphatic hydrocarbons and methyl esters of fatty acids (palmitic, oleic, linoleic, linolenic acids) were detected in active fractions.All compounds isolated were detected for the first time in this medicinal plant.View full abstractDownload PDF (588K) -
Yasunori YAOITA, Kaori MACHIDA, Masao KIKUCHI1999 Volume 47 Issue 6 Pages 894-896
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new marasmane sesuquiterpenoids, lactapiperanols A-D (1-4), were isolated from the fruit bodies of Lactarius piperatus (SCOP. : FR.) S. F. GRAY (Russulaceae) along with two known compounds. The structures of the new compounds were elucidated on the basis of spectroscopic evidence.View full abstractDownload PDF (500K) -
Takeshi KOIKE, Naoki TAKEUCHI, Takashi OHTA, Seisho TOBINAGA1999 Volume 47 Issue 6 Pages 897-899
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRacemic ligularone (2) and isoligulatone (18) were synthesized from the cis-4aβ, 5, 6, 7, 8, 8a-hexahydro-8β, 8aβ-dimethylnapthalen-1, 3(2H, 4H)-dione (11) by furannulation reaction with diethylprop-2-ynylsulphonium bromide, prepared from diethyl sulfide and propargyl bromide.View full abstractDownload PDF (528K) -
Won-Jea CHO, Myun-Ji PARK, Takeshi IMANISHI, Byung-Ho CHUNG1999 Volume 47 Issue 6 Pages 900-902
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBenzo[c]phenanthridine skeleton was synthesized from easily available starting N-methyl-o-toluamide 2 and o-methylbenzonitrile 5 in 7 steps. Radical cyclization of styrene 10 afforded 6, 11-dimethyl-6, 11 -dihydro-5H-in-deno[1, 2-c]isoquinolin-5-one 13. Most 3-arylisoquinolines have displayed strong activities against human tumor cell lines. Especially, indenoisoquinolinone 13 exhibited excellent cytotoxicity (IC50=0.002 μg/ml; HCT 15).View full abstractDownload PDF (546K) -
Tamotsu NIKAIDO, Kazuo KOIKE, Katsuyoshi MITSUNAGA, Tsuyoshi SAEKI1999 Volume 47 Issue 6 Pages 903-904
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new triterpenoid saponins, platycoside D [3-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl-2β, 3β, 16α, 23-tetrahydroxyolean-12-ene-28-oic acid 28-O-β-D-apiofuranosyl-(1→3)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside] and platycoside E [3-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl-2β, 3β, 16α, 23, 24-pentahydroxyolean-12-ene-28-oic acid 28-O-β-D-apiofuranosyl-(1→3)-β-D-xylopyranosyl-(1→4)-α-L-rhambopyranosyl-(1→2)-α-L-arabinopyranoside] were isolated from the roots of Platycodon grandiflorum. Structural determination is based on spectral and chemical evidence.View full abstractDownload PDF (425K) -
Yasuo TAKEUCHI, Hitoshi ABE, Takashi HARAYAMA1999 Volume 47 Issue 6 Pages 905-906
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRacemic compounds (1 and 2) of the antimalarial agents febrifugine (d-1) and isofebrilugine (d-2) were synthesized using an unusual Claisen rearrangement of allyl enol ether (7) and the stereoselective reduction of 2-allyl-3-piperidone (8). This method is widely applicable to the synthesis of derivatives needed to study the structure-activity relationship of febrifugine.View full abstractDownload PDF (392K) -
Makio SHIBANO, Daisuke TSUKAMOTO, Genjiro KUSANO1999 Volume 47 Issue 6 Pages 907-908
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new pyrrolizidine alkaloid, broussonetine N, was isolated from the branches of Broussonetia kazinoki SIEB. (Moraceae).Broussonetine N was formulated as (1R, 2R, 3R, 5S, 8R)-1, 2-dihydroxy-3-hydroxymethyl-5[(1R)-1, 10-dihydroxy-6-oxo-decyl]pyrrolizidine (1) by spectoroscopic and chemical methods. 1 inhibited β-glucosidase, β-galactosidase, and β-mannosidase. Absolute stereostructures of broussonetines A (2) and B (3) as well as that of 1 were also determined by a new version of Mosher's method.View full abstractDownload PDF (426K) -
Han-Xun WEI, Zhi-Min WANG, Min SHI1999 Volume 47 Issue 6 Pages 909-910
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome hindered chiral 1, 3-diketones were successfully synthesized from the reaction of (+)-3α-bromocamphor with acyl chlorides in the presence of samarium diiodide (SmI2) under mild reaction conditions in high yields.View full abstractDownload PDF (411K) -
Hirotaka SHIBUYA, Takako BOHGAKI, Kazuyoshi OHASHI1999 Volume 47 Issue 6 Pages 911-912
Published: June 15, 1999
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new migrated pimarane-type diterpenes called neoorthosiphols A and B have been isolated from a water decoction of the leaves of Orthosiphon aristatus (Lamiaceae) cultivated in Java, Indonesia. Their chemical structures have been elucidated on the basis of physicochemical evidence.View full abstractDownload PDF (428K)
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