All issues
Volume 49, Issue 11
Displaying 1-26 of 26 articles from this issue
- |<
- <
- 1
- >
- >|
Regular Articles
-
Otilia May Yue KOO, Paul Wan Sia HENGArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1383-1387
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSIn this study, five microcrystalline cellulose (MCC) grades were physically characterized and their extrusion-spheronization behaviours were characterized in terms of water requirements and pellet shape profiles. It was found that the MCC grades differed significantly in the physical properties investigated. Physical properties of MCC were found to influence the water requirement for extrusion-spheronization. MCC grades of higher bulk densities, lower porosities and water retentive capacities required less water to produce pellets of equivalent size. These MCC grades were also found to produce pellets of lower sphericity and wider shape distributions. Packing of MCC particles within the agglomerate played a role in determining amount of water retention and pellet rounding during spheronization. However, there was a limit to the influence of packing density on the rate of pellet rounding because poor packing resulted in higher water retentive capacity, which also limited the rate of rounding.View full abstractDownload PDF (151K) -
Yoshimi NAGATANI, Tsutomu WARASHINA, Tadataka NOROArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1388-1394
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSThe new glycosides, named dracunculifosides A—J, were isolated along with sixteen known glycosides from the aerial part of Baccharis dracunculifolia DC. (Compositae). The structures of these glycosides were determined on the basis of spectral and chemical evidence. These new glycosides consisted of β-D-glucopyranose or β-D-apiofuranosyl-(1→6)-β-D-glucopyranose, and most possess an (E)-caffeoyl group.View full abstractDownload PDF (81K) -
Haranath Kumar VADDI, Ling Zhi WANG, Paul Chi-Lui HO, Yew Weng CHAN, S ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1395-1400
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSPermeation of haloperidol through the human skin in vitro was studied with two enhancers, cetrimide and ascorbic acid, at various concentrations. Amber glass Franz-type diffusion cells were used for the permeation studies and haloperidol was made soluble in aqueous solution with the aid of lactic acid. Donor solutions were prepared by adding excess of haloperidol to 0.03% (v/v) lactic acid solution with or without enhancers at concentrations 0.1, 0.3 and 0.6% (w/v) and stirred for 36 h at 32 °C before filtering. Ascorbic acid gradually increased the solubility of the haloperidol from that of the control where as cetrimide did not show any effect. Cetrimide concentration dependent increase in the permeability coefficient of haloperidol was observed. Mechanism of enhancement by cetrimide was probed with the diffusion profile kinetics and Fourier transform infrared (FT-IR) spectroscopy. Cetrimide was found to increase the thermodynamic activity of the drug in the skin. IR spectra of the stratum corneum treated with cetrimide showed time-dependent decrease in the intensity of the spectrum and dose-dependent decrease of lipid band but no change in the protein conformation. Cetrimide appears to interact with both the dermal keratin and lipids and this interaction was found to be irreversible. Ascorbic acid although increased the flux of haloperidol to the same extent at all concentrations from that of the control, decreased the permeability coefficient and enhancer index in a concentration dependent manner and this is due to the increased solubility of the drug in the vehicle. Both the enhancers did not change the lag time from that of the control.View full abstractDownload PDF (77K) -
Akikazu KAKEHI, Suketaka ITO, Hiroyuki SUGA, Shinji SAKURAI, Tomoshige ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1401-1405
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSNew compounds having two indolizine nuclei in a molecule were prepared in low to moderate yields from the reactions of potassium 2-indolizinethiolates with 1,ω-dihalides such as 1,2-diiodoethane, 1,3-dibromopropane, 1,4-dibromobutane, α,α'-dichloro-o-xylene, and α,α'-dichloro-p-xylene. Most of the products had the conformation in which the two indolizine rings in the molecule are as remote as possible, but only 1,2-bis[[(2-indolizinyl)thio]methyl]benzene derivatives, prepared from potassium 2-indolizinethiolates and α,α'-dichloro-o-xylene, showed a weak attractive interaction between the two indolizine nuclei in the X-ray analysis and the nuclear Overhauser and exchange spectroscopy (NOESY) spectrum.View full abstractDownload PDF (92K) -
Gérard Aimè PINNA, Giovanni LORIGA, Gabriele MURINEDDU, ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1406-1411
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSIn our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) values in the submicromolar range.View full abstractDownload PDF (93K) -
Noriko KATORI, Nobuo AOYAGI, Shigeo KOJIMAArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1412-1419
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSThis study intends to determine the rational criteria (e.g., threshold value) for applying the weight variation test and to investigate the adequacy of the acceptance value for existing commercial products in Japan. The studied products were 489 lots (3 lots×163 products) of compressed tablets (plain, film-coated, sugar-coated) and 42 lots (3 lots×14 products) of hard capsules marketed in Japan. The individual drug content and the weight of 10 units in a lot were determined for each product and the acceptance values were calculated according to the Japanese Pharmacopoeia thirteenth edition (JP13) Content Uniformity Test (M=100.0, k=2.2). Product-specific intra-lot relative standard deviation of content (RSDD), weight (RSDW) and concentration (RSDC) were calculated by analysis of variance (ANOVA) using three lots of data per product. The RSDD and RSDC tended to increase with the decrease of the label strength for plain tablets, but not for film-coated and sugar-coated tablets, and hard capsules. A good correlation was found between RSDD and RSDC but not between RSDD and RSDW. These findings indicate that 1) it is difficult to rationally set the threshold level for weight variation, especially regarding the dosage forms except for plain tablets, 2) the application of weight variation tests should, in principle, be decided on the mixing homogeneity that is RSDC. 3) Most (99.6%) of the tablets and all the capsules investigated met the requirement of content uniformity test of JP13. Therefore the criteria of the JP13 content uniformity test are considered acceptable from the viewpoint of manufacturing capability.View full abstractDownload PDF (110K) -
Shinya NAGASHIMA, Seijiro AKAMATSU, Eiji KAWAMINAMI, Souichirou KAWAZO ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1420-1432
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSIn attempt to find novel integrin αvβ3 antagonists, we selected SC65811 and its guanidine analogue (1) as lead compounds. Modification of the glycine part of SC65811 led to a new series of malonamide derivatives that exhibited αvβ3 inhibitory activity. Among them, (R,S)-3-{3-[6-(3-benzylureido)indolin-1-yl]-3-oxopropanoyl-amino}-3-(pyridin-3-yl)propanoic acid (43a) showed not only potent activity with an IC50 value of 3.0 nM but also good selectivity for αvβ3 relative to αIIbβ3, α5β1, and αvβ5 with IC50 values of 19000, 11000, and 14 nM, respectively. Furthermore, optimization of 43a led to the most potent αvβ3 antagonist, (R,S)-3-(3-{6-[4,5-dihydro-1H-imidazol-2-yl)amino]indolin-1-yl}-3-oxopropanoylamino)-3-(quinolin-3-yl)propanoic acid (43l) with an IC50 value of 0.42 nM. The synthesis and the structure-activity relationships of these malonamide derivatives are presented.View full abstractDownload PDF (152K) -
Yasuyuki YOSHITAKE, Hidetoshi NAKAGAWA, Kazunobu HARANOArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1433-1439
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSThe transition structures of the thione-to-thiol rearrangement of O-(2-dimethylaminoethyl and 2-methylthio-) S-methyl xanthates in several solvents were located by semiempirical molecular orbital method (PM3) using the conductor-like screening model (COSMO) approach. Each transition state transforms into the ion-pair intermediate with a three-membered ring structure (aziridinium or thiiranium), indicating that the rearrangement proceeds through an ionic intermediate with the anchimeric assistance of the neighboring group. The intermediary structures in gas phase are also analyzed by ab initio and density functional theory calculations.View full abstractDownload PDF (88K) -
Xing-Hua ZHU, Jun ANDO, Masanao TAKAGI, Tsuyoshi IKEDA, Akira YOSHIMIT ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1440-1443
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSFour novel withanolide-type steroids named cilistols p, pm, p1 and u (1—4, respectively), were isolated from the leaves of Solanum cilistum. The respective structures were characterized by spectroscopic means as follows: cilistol p (1) was (22R,24R,25R,26S)-1-oxo-22,26-epoxy-3α,5α-cycloergostane-6β,17α,24,25,26-pentaol 26-O-β-D-glucopyranoside, cilistol pm (2) corresponded to the 6-O-methyl ether derivative of 1; cilistol p1 (3) was represented as the 24-O-methyl ether of 1, and cilistol u (4) was shown to be the epoxide between C-24 and -25, presumably bearing cilistols p, pm and p1 by ring-opening.View full abstractDownload PDF (69K) -
Da-Bing CHEN, Tian-zhi YANG, Wang-Liang LU, Qiang ZHANGArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1444-1447
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSPaclitaxel (Taxol), a diterpenoid isolated from Taxus brevifolia, is effective against several murine tumors, and is one of the most exciting anticancer molecules currently available. Due to its low solubility in water, it is clinically administered with polyethoxylated castor oil (Cremophor EL), which causes serious side effects. Inclusion of paclitaxel in solid lipid nanoparticles (SLNs) has proved to be a good approach to eliminate the need for Cremophor EL and improve the drug’s antitumor efficacy. This paper describes the development of two types of long-circulating SLNs as colloidal carriers for paclitaxel. SLNs are constituted mainly of bioacceptable and biodegradable lipids. In vitro release kinetics showed that the release was very slow, the release of paclitaxel from F68-SLN is linear, and the release of paclitaxel from Brij78-SLN followed the Weibull equation. Pharmacokinetics was evaluated in KM mice after injection of paclitaxel formulated in Cremophor EL or in Brij78-SLN and F68-SLN. Encapsulation of paclitaxel in both SLNs produced marked differences compared with the free drug pharmacokinetics. F68-SLN and Brij78-SLN are long-circulating (t1/2β, 10.06 and 4.88 h, respectively) compared with paclitaxel injection (t1/2β, 1.36 h).View full abstractDownload PDF (162K) -
Yorinobu YONEZAWA, Sumio ISHIDA, Hisakazu SUNADAArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1448-1451
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSRelease properties from a wax matrix tablet was examined. To obtain basic release properties, the wax matrix tablet was prepared from a physical mixture of drug and wax powder (hydrogenated caster oil) at a fixed mixing ratio. Properties of release from the single flat-faced surface or curved side surface of the wax matrix tablet were examined. The applicability of the square-root time law and of Higuchi equations was confirmed. The release rate constant obtained as g/min1/2 changed with the release direction. However, the release rate constant obtained as g/cm2·min1/2 was almost the same. Hence it was suggested that the release property was almost the same and the wax matrix structure was uniform independent of release surface or direction at a fixed mixing ratio. However, these equations could not explain the entire release process. The applicability of a semilogarithmic equation was not as good compared with the square-root time law or Higuchi equation. However, it was revealed that the semilogarithmic equation was available to simulate the entire release process, even though the fit was somewhat poor. Hence it was suggested that the semilogarithmic equation was sufficient to describe the release process. The release rate constant was varied with release direction. However, these release rate constants were expressed by a function of the effective surface area and initial amount, independent of the release direction.View full abstractDownload PDF (56K) -
Masayuki YOSHIKAWA, Toshio MORIKAWA, Kenichi YASHIRO, Toshiyuki MURAKA ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1452-1456
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSNew dammarane-type triterpene saponins, notoginsenosides-L, -M, and -N, were isolated from the glycosidic fraction of the dried roots of Panax notoginseng (BURK.) F.H. Chen. Their structures were elucidated on the basis of chemical and physicochemical evidence. Immunological adjuvant activities of the principal notoginsenosides and related dammarane-type triterpene saponins were examined and notoginsenosides-D, -G, -H, and -K were found to increase the serum IgG level in mice sensitized with ovalbumin.View full abstractDownload PDF (80K) -
Yuko TSUDA, Mayako TADA, Keiko WANAKA, Utako OKAMOTO, Akiko HIJIKATA-O ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1457-1463
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSBased on the structure of Tra-Tyr(O-Pic)-octylamide, a portion of the octylamine was replaced with moieties bearing hydrophobic, basic or acidic groups. Replacement of the C-terminal residue with a moiety bearing a hydrophobic group gave the proper affinity of the inhibitor to both plasmin (PL) and plasma kallikrein (PK). While addition of a basic residue did not improve the affinity of the inhibitor, a carboxylic acid attached to the phenyl ring increased the PK selectivity of the inhibitor.View full abstractDownload PDF (77K) -
Noriyasu HADA, Koji SATO, Jun-ichiro SAKUSHIMA, Yukihiro GODA, Mutsumi ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1464-1467
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSTwo kinds of amphoteric glycosphingolipid analogues from the earthworm Pheretima hilgendorfi were synthesized as follows: The key reaction is a coupling of a phosphocholine group at the position C-6 of 1 and 6 which was attempted using 2-chloro-2-oxo-1,3,2-dioxaphospholane, followed by reaction of the resulting cyclic phosphate intermediate with anhydrous trimethylamine to give 2 and 7. Subsequent debenzylation afforded target compounds (3,8). Their ability to inhibit the histamine release in vitro was examined.View full abstractDownload PDF (63K)
Notes
-
Qing-Wen ZHANG, Wen-Cai YE, Wendy W.-L. HSIAO, Shou-Xun ZHAO, Chun-Tao ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1468-1470
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSA new cycloartane bisdesmoside and two new trinorcycloartane glycosides, along with four known cycloartane compounds, were isolated from the rhizomes of Cimicifuga dahurica (Ranunculaceae). The structures of the new compounds were elucidated as 3-O-α-L-arabinopyranosyl cimigenol 15-O-β-D-glucopyranoside, 24-hydroxy-12β-acetoxy-25,26,27-trinorcycloartan-16,23-dione 3β-O-α-L-arabinopyranoside, and 16α,24α-dihydroxy-12β-acetoxy-25,26,27-trinor-16,24-cyclocycloartan-23-one 3β-O-α-L-arabinopyranoside by extensive NMR methods, FAB-MS, and hydrolysis.View full abstractDownload PDF (51K) -
Shuang-Cheng MA, Zhen-Dan HE, Xue-Long DENG, Paul Pui-Hay BUT, Vincent ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1471-1473
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSSix secoiridoid glucosides, lucidumoside C (1), oleoside dimethylester (2), neonuezhenide (3), oleuropein (4), ligustroside (5) and lucidumoside A (6), isolated from the fruits of Ligustrum lucidum (Oleaceae), were examined in vitro for their activities against four strains of pathogenic viruses, namely herpes simplex type 1 virus (HSV-1), influenza type A virus (Flu A), respiratory syncytial virus (RSV) and parainfluenza type 3 virus (Para 3). Antiviral activities were evaluated by the cytopathic effect (CPE) inhibitory assay. The purpose was to check if the antioxidative potency of these glucosides correlated with their antiviral potency. Results showed that none of the glucosides had any significant activity against HSV-1 and Flu A. Oleuropein, however, showed significant antiviral activities against RSV and Para 3 with IC50 value of 23.4 and 11.7 μg/ml, respectively. Lucidumoside C, oleoside dimethylester and ligustroside showed potent or moderate antiviral activities against Para 3 with IC50 values of 15.6-20.8 μg/ml. These results also documented that the anti-oxidative potency of these secoiriodoid glucosides was not directly related to their antiviral effects.View full abstractDownload PDF (47K) -
Changqi ZHAO, Wei CAO, Akito NAGATSU, Yukio OGIHARAArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1474-1476
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSTwo new aryltetralin-type lignan glycosides: methyl epipodophyllate 7'-O-β-D-glucopyranoyl-(1→6)-β-D-glucopyranoside (1), 4-demethylepipodophyllotoxin 7'-O-β-D-glucopyranoside (2), and a new phenyl ethanol glycoside: phenyl ethanol 4-O-β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside (3), along with three known compounds: junipetriolosides (4), 3,4-dihydroxy-phenyl ethanol (5), and 4-hydroxy-phenyl ethanol (6) were isolated and identified from the n-butanol extract of the roots and rhizomes of Sinopodophyllum emodi (WALL.) YING. The structures of the above were established by means of spectral data and chemical methods.View full abstractDownload PDF (52K) -
Christina A. WOOD, Kit LEE, Abraham J. VAISBERG, David G.I. KINGSTON, ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1477-1478
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSHimatanthus sucuuba is an Amazonian tree with abundant, yet conflicting ethnobotanical information. Investigation of the polar and non-polar constituents led to the isolation of plumericin, a bioactive spirolactone iridoid, and four known pentacylic triterpenes: lupeol acetate, lupeol cinnamate, lupeol β-phenyl propionate, and α-amyrin cinnamate.View full abstractDownload PDF (43K) -
Du XIAO, Masanori KUROYANAGI, Tomio ITANI, Hiromichi MATSUURA, Manabu ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1479-1481
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSIn the course of our research for biologically active constituents from coniferous plants, a chromone derivative (1) and an abietane derivative (2) were isolated along with several diterpenes from Chamaecyparis pisifera. Structures of the new compounds were determined to be 5,7-dihydroxy-2-(1-acetyl-2-methoxycarbonylethyl)-chromone and rel-(8R,10R,20S)-8,10,20-trihydroxy-9(10→20)-abeo-abieta-9,13-dien-12-one by means of spectral methods including two-dimensional NMR experiments. Some of these abietane-type compounds isolated from this plants showed antibacterial activity against the gram-positive bacteria Staphylococcus aureus and Bacillus subtilis.View full abstractDownload PDF (55K) -
Erdal BEDIR, Irem Iffet TATLI, Ihsan CALIS, Ikhlas Ahmad KHANArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1482-1486
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSThree new cycloartane-type triterpene glycosides have been isolated from the aerial parts of Astragalus trojanus. The structures were established mainly by a combination of one- and two-dimensional NMR techniques [1H-1H-correlation spectroscopy (COSY), 1H-13C-heteronuclear multiple quantum correlation spectroscopy (HMQC), and 1H-13C-heteronuclear multiple-bond correlation spectroscopy (HMBC)] and high resolution electrospray ionization mass spectrometry (HR-ESI-MS) as 3-O-β-(2',3'-di-O-acetyl)-D-xylopyranosyl-6-O-β-D-glucopyranosyl-16-O-acetoxy-20(R),24(S)-epoxycycloartane-3β,6α,16β,25-tetrol, 3-O-[α-L-rhamnopyranosyl-(1→2)-β-(3',4'-di-O-acetyl)-D-xylopyranosyl]-6-O-β-D-xylopyranosyl-20(R),24(S)-epoxycycloartane-3β,6α,16β,25-tetrol, 3-O-β-D-xylopyranosyl-6,16-di-O-β-D-glucopyranosyl-20(R),24(S)-epoxycycloartane-3β,6α,16β,25-tetrol.View full abstractDownload PDF (68K) -
Daisuke TSUKAMOTO, Makio SHIBANO, Genjiro KUSANOArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1487-1491
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSSix new alkaloids, broussonetines W,X,M1,U1,J1, and J2 (1—6) were isolated from the branches of Broussonetia kazinoki SIEB. (Moraceae) as minor constituents. They were formulated as (2R,3R,4R,5R)-2-hydroxymethyl-3,4-dihydroxy-5-[7-(cyclohexy-2-on-1(6)-enyl)heptyl]pyrrolidine (1), (2R,3S,4R,5R)-2-hydroxymethyl-3,4-dihydroxy-5-[7-(cyclohexy-2-on-1(6)-enyl)heptyl]pyrrolidine-4-O-β-D-glucopyranoside (2), (2R,3R,4R,5R)-2-hydroxymethyl-3,4-dihydroxy-5-[(9R)-9,13-dihydroxytridecyl]pyrrolidine (3), (2S,3S,4S)-2-hydroxymethyl-3,4-dihydroxy-5-(10-oxo-13-hydroxytridecyl)-5-pyrroline (4), (2R)-2-{(1S,2S)-1,2-dihydroxy-8-[(2R,3R,4R,5R)-5-(2-hydroxymethyl-3,4-dihydroxy-1-acetylpyrrolidinyl)]octyl}piperidine (5), (2R)-2-{(1S,2S)-1,2-dihydroxy-8-[(2R,3R,4R,5R)-5-(2-hydroxymethyl-3,4-dihydroxypyrrolidinyl)]octyl}piperidine (6).View full abstractDownload PDF (71K) -
Anne-Claire MITAINE-OFFER, Abderrazak MAROUF, Bernard HANQUET, Nicolas ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1492-1494
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSBidentatoside II (1) and chikusetsusaponin V methyl ester (2) are two further triterpene saponins isolated from the roots of Achyranthes bidentata. Chemical and homo and heteronuclear two-dimensional (2D) NMR techniques have led to the structural elucidation of 1 which is a new seco-glycoside of oleanolic acid and the full 1H- and 13C-NMR assignments of 2. These compounds did not show any potentiation of the in vitro cytotoxicity of cisplatin in the HT 29 human colon cancer cell line.View full abstractDownload PDF (50K) -
Takaaki YASUDA, Joji UEDA, Keisuke OHSAWAArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1495-1497
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSIn a study on the metabolism of flavonoids, the isoflavone genistein was administered orally to rats. Urine samples were collected and treated with β-glucuronidase and arylsulfatase. Genistein and its metabolites, 4',5,7-trihydroxyisoflavanone (M1), 4',7-dihydroxyisoflavan (M2), and p-ethylphenol (M3) were isolated from the urine following treatment with enzymes. The structures of M1, M2, and M3 were determined on the basis of chemical and spectral data.View full abstractDownload PDF (45K) -
Tsuneo IWAKAWA, Yoshimi TANAKA, Akira TAKASHIMAArticle type: scientific monograph
2001 Volume 49 Issue 11 Pages 1498-1499
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSA new galloylglucoside, 3-hydroxy-5-methylphenol 1-O-β-D-(6'-galloyl)glucopyranoside (1) was isolated from Cleyera ochnacea DC. (Theaceae). Its structure was elucidated on the basis of chemical and spectral analysis. Compound 1 showed inhibitory activity against rat cerebellar nitric oxide synthase (NOS).View full abstractDownload PDF (42K) -
Takashi HASHIHAYATA, Hiroki SAKOH, Yasuhiro GOTO, Masaaki HIROSE, Shun ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1500-1502
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSImproved synthesis of the trans-3,5-disubstituted pyrrolidin-3-ylthio side-chain of the novel carbapenem 1 was achieved via stereoselective reduction of the 1-aryl-1-butanone derivative 5 and successive intramolecular cyclization of the resulting chiral alcohol 6. The 1-aryl-1-butanone derivative 5 was obtained by a coupling reaction of protected 4-hydroxy-2-pyrrolidone with aryl-Grignard reagent.View full abstractDownload PDF (60K)
Communications to the Editor
-
Osamu MURAOKA, Shao YING, Kazuya YOSHIKAI, Yoshiharu MATSUURA, Eriko Y ...Article type: scientific monograph
2001 Volume 49 Issue 11 Pages 1503-1505
Published: 2001
Released on J-STAGE: June 28, 2002
JOURNAL FREE ACCESSA nitrogen analogue 4 of the naturally occurring sulfonium ion salacinol (1), a potent α-glucosidase inhibitor isolated from the Ayruvedic medicine Salacia reticulata, was synthesized and its inhibitory activity against α-glucosidase tested. Substitution of the sulfur atom in 1 with a nitrogen reduced the activity considerably. The solid-state stereostructure of the related compound (5) was determined on the basis of single crystal X-ray measurement.View full abstractDownload PDF (55K)
- |<
- <
- 1
- >
- >|