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Volume 55, Issue 4
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Review
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Kenji Hamase2007 Volume 55 Issue 4 Pages 503-510
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSD-Amino acids are the candidates of novel physiologically active substances and the marker molecules of diseases in mammals. In the present study, the two-dimensional determination of small amounts of D-amino acids in mammals has been performed after sensitive pre-column fluorescence derivatization with 4-fluoro-7-nitro-2,1,3-benzoxadiazole (NBD-F). The two-dimensional HPLC system includes the isolation of the target amino acids as D+L mixtures using the micro-ODS column, and the determination of the enantiomers using the chiral column. This method enables the sensitive and selective determination of small amounts of D-amino acids in mammals without the interference of L-amino acids and peptides, and the presence and distribution of D-Leu, D-Ala, D-Pro, D-Thr and D-allo-Thr has been demonstrated in rats and mice. The regulation and the origins of these D-amino acids, and their relationships to the biological rhythms are also discussed.View full abstractDownload PDF (468K)
Regular Articles
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Hari Narayan Pati, Umashankar Das, Irving Javier Ramirez-Erosa, Donna ...2007 Volume 55 Issue 4 Pages 511-515
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSA series of 1-aryl-2-dimethylaminomethyl-2-propenone hydrochlorides 1 were prepared which possessed IC50 values of less than 10 μM when examined towards human WiDr colon cancer cells. The related 1-aryl-2-dimethylaminomethyl-3-hydroxypropanone hydrochlorides 2, formed by hydration of the analogs in series 1, also had IC50 values in the low micromolar range. On the other hand, conversion of 2-dimethylaminomethyl-1-(4-nitrophenyl)-2-propenone hydrochloride 1c into the corresponding 2-mercaptoethanol of adduct 3c led to a 37-fold reduction in potency. Two thirds of the compounds prepared in this study were more potent than a reference drug cisplatin while one third of these molecules displayed greater cytotoxicity to the WiDr cells than human CRL-2522 fibroblasts. A stability study of the 4-nitrophenyl analog in each of the series 1—3 in deuterium oxide was undertaken. In the case of 1c, replacement of the dimethylamino hydrochloride group by a hydroxy function was noted while in series 2, the loss of both water and dimethylamine hydrochloride gave rise to a mixture of two enones. The mercaptoethanol adduct 3c underwent deamination. The data obtained provide guidelines for amplifying the project in the future.View full abstractDownload PDF (101K) -
Bina Shaheen Siddiqui, Huma Aslam, Syed Tariq Ali, Sabira Begum, Nasim ...2007 Volume 55 Issue 4 Pages 516-519
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSStudies on the chemical constituents of the aerial parts of Ocimum basilicum have led to the isolation of three new compounds, basilol (1), ocimol (2), and basilimoside (3), along with two known constituents betulinic acid and oleanolic acid. The structures of the new constituents have been elucidated through spectral studies including 2D-NMR experiments (HMQC, HMBC, COSY, NOESY, and J-resolved) and chemical transformation, as p-formylphenyl 3β-hydroxyolean-12-en-28-oate (1), 2-methoxy-4-carbomethoxyphenyl 3β-hydroxy-lup-20(29)-en-28-oate (2), and (22E)-24ξ-ethyl-25-methylcholesta-5,22-diene-3β-ol-3-O-D-glucopyranoside (3).View full abstractDownload PDF (119K) -
Yuhki Koyama, Sachie Kikuchi, Sayaka Nakagawa, Shigeki Kobayashi2007 Volume 55 Issue 4 Pages 520-525
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSAlthough both cis-diamminedichloroplatinum(II) (cisplatin or cis-DDP) and trans-diamminedichloroplatinum(II) bind to DNA, only cis-DDP is widely used as a chemotherapeutic agent; the stereoisomer trans-DDP is inactive. DNA, generally, is wound around the histone core in the nucleus of living cells and forms the nucleosome structure. To understand the essentially different anticancer activities of cis-DDP and trans-DDP, it is necessary to investigate the interaction of cis-DDP (or trans-DDP) with DNA around the histone in the nucleosome. Here, we used φX174DNA–histoneLNCaP complexes prepared by the reaction of φX174DNA with histoneLNCaP extracted from LNCaP cells. We first show that the ability of cis-DDP to dissociate the DNA from φX174DNA–histoneLNCaP, as a nucleosome model, is much stronger than that of trans-DDP. As a result of the action of cis-DDP, the DNA in the nucleosome is rendered naked, and the naked DNA is vulnerable to cis-DDP (or other drugs). This study describes a new model showing that the difference in the activities of cis-DDP and trans-DDP is related to the difference in their abilities to dissociate the DNA from the nucleosome.View full abstractDownload PDF (1138K) -
Shigeki Kobayashi, and Yuhki Koyama2007 Volume 55 Issue 4 Pages 526-531
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSWe show that the trefoil, figure-eight knot, and mini circular closed DNA are formed by the reaction of cis-DDP-modified φX174DNA–histoneLNCaP complexes as a new nucleosome model with human DNA topoisomease I. The yields from cis-DDP-modified complexes were far higher than that of trans-DDP. The topologically-distinct invariant DNA such as the trefoil and figure-eight knot are not produced in the reaction of DNA topo I with φX174DNA–histoneLNCaP complexes that are not modified by platinum. Therefore, the anti-cancer activity of cis-DDP may be related to the production of the trefoil, figure-eight knot, and mini circular closed DNA forms in the living cell. We subsequently demonstrate that the yield mechanism and identification of the topologically-distinct invariant DNA can be explained by the topological method using a Jones polynomial and recombination through the topo I path intra-twisted looped DNA model. These results suggest that the distinguishing of anti-neoplastic activity of cis- and trans-DDP can be partially explained by the distinct topologies of DNA, trefoil, figure-eight knot, and mini circular closed DNA that they produce.View full abstractDownload PDF (943K) -
Tadatoshi Yamaguchi, Shigeru Ito, Nobuhiro Kashige, Kazuhide Nakahara, ...2007 Volume 55 Issue 4 Pages 532-536
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSDihydropyrazine, a compound derived from sugars, possesses DNA strand-breakage activity. The relationship between the activity as assayed using pBR 322 ccc-DNA and the chemical structures of derivatives of dihydropyrazine (DHPs) has been investigated. The addition of Cu2+ enhanced the activity remarkably. The introduction of a methyl or phenyl group onto the DHP ring or a cyclohexyl group fused onto the DHP ring also increased the activity. These properties indicated that the activity was due to the facility of electron release from the DHP ring, followed by radical generation. The determination of ionization potential and electrostatic potential values, and bond dissociation energy via semi-empirical MO calculations suggested strongly that the activity is induced by a DHP ring structure that contains a configuration suitable for hyperconjugation.View full abstractDownload PDF (307K) -
Haidy Nasr Kamel, Frank Rolf Fronczek, Sherief Ibrahim Khalifa, Marc S ...2007 Volume 55 Issue 4 Pages 537-540
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESS5-Episinuleptolide (1) is an abundant norcembranolide diterpene isolated from several species of the soft coral genus Sinularia. Biocatalytic transformation studies of 1 using Streptomyces lavendulea ATCC 8664 resulted in the isolation and characterization of two new metabolites 2 and 3. Compound 2, 6α-hydroxy-5-episinuleptolide was produced via a stereoselective reduction of 1 and was further metabolized into compound 3 which has a 3,8-bicylized cembranoid skeleton. The structures and configurations of the metabolites were determined by spectroscopic and X-ray crystallographic analyses.View full abstractDownload PDF (265K) -
Nadia Fayek Youssef, Elham Anwer Taha2007 Volume 55 Issue 4 Pages 541-545
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSThree reliable, rapid and selective methods have been developed and validated for the determination of lamotrigine in the presence of its impurity, 2,3-dichlorobenzoic acid. The first method is spectrophotometric method using p-chloranilic acid forming a colored product with λmax 519±2 nm. All variables affecting the reaction have been investigated and the conditions were optimized. Beer's law was obeyed over a concentration range of 10—200 μg ml−1 with mean accuracy 100.13±0.44%. The molar ratio of the formed ion-association complex is found to be 1 : 1 as deduced by Job's method. The conditional stability constant (Kf), standard free energy (ΔG), molar absorptivity(ε), and sensitivity index were evaluated. The second method is based on TLC separation of the cited drug (Rf=0.75±0.01) from its impurity (Rf=0.23±0.01) followed by densitometric measurement of the intact drug spots at 275 nm. The separation was carried on silica gel plates using ethyl acetate : methanol : ammonia 35% (17 : 2 : 1 v/v/v) as a mobile phase. The linearity range was 0.5—10 μg/spot with mean accuracy 99.99±1.33%. The third method is accurate and sensitive stability-indicating HPLC method based on separation of lamotrigine from its impurity on a reversed phase C18 column, using a mobile phase of acetonitrile : methanol : 0.01 M potassium orthophosphate (pH 6.7±0.1) (30 : 20 : 50 v/v/v) at ambient temperature 25±5 °C and UV detection at 275 nm in an overall analysis time of about 6 min., based on peak area. The injection repeatability, intraday and interday repeatability were calculated. The procedure provided a linear response over the concentration range 1—12 μg ml−1 with mean accuracy of 99.50±1.30%. The proposed methods were successfully applied for the determination of lamotrigine in bulk powder, in dosage form and in presence of its impurity. The results obtained were analyzed by ANOVA to assess that no significant difference between each of the three methods and the reported one. The validation was performed according to USP guidelines.View full abstractDownload PDF (131K) -
Noboru Sekiya, Nobutaka Abe, Masanobu Yamamoto, Kazuhisa Takeda2007 Volume 55 Issue 4 Pages 546-550
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSIn stability studies on moisture-resistant Opalmon tablets in press-through-packages (PTP), which were placed in aluminum bags, we found that the degradation rate of the dextran formulation is faster than that of the lactose formulation. The fast degradation of the dextran formulation is attributed to residual moisture in the package because drying the tablets before packaging suppressed the degradation and there is a good correlation between the stability of the drug and the water-activity of the tablets. Therefore, we developed a new drying method for the tablets, i.e. the rotary vacuum drying method, and investigated the effects of the operating conditions such as heating temperature, rotation speed, and vacuum degree on the drying time, and the appearance of the tablets. Using the rotary vacuum drying method, the tablets were dried over a short time (30 min) on a mass production scale so that the water activity was less than 0.03. Furthermore, the tablets suffered negligible damage such as breaking and chipping during the drying process. These results indicate that the rotary vacuum drying method is useful for drying tablets on mass production scales.View full abstractDownload PDF (176K) -
Masateru Ono, Chika Takamura, Fumie Sugita, Chikako Masuoka, Hitoshi Y ...2007 Volume 55 Issue 4 Pages 551-556
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSTwo new steroid glycosides, named trikamsterosides A and B, and a new sesquiterpenoid glycoside named trikamsesuquiside A were isolated from the underground parts of Trillium kamtschaticum PALL. along with 18 known compounds comprising 12 steroids, one sesquiterpenoid glycoside, one phenylpropanoid, one flavonoid glycoside, and three phenylpropanoid sucrose esters. Their chemical structures were determined on the basis of spectroscopic data and chemical evidence. Among them, one phenylpropanoid sucrose ester showed almost the same radical-scavenging effect on 1,1-diphenyl-2-picrylhydrazyl as that of α-tocopherol.View full abstractDownload PDF (170K) -
Mailavaram Raghu Prasad, John Prashanth, Kalghatgi Shilpa, Deb Pran Ki ...2007 Volume 55 Issue 4 Pages 557-560
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSA novel series of some novel 5-substituted-1,2,4-triazolo[4,3-c]8,9,10-trihydrocyclopenta/8,9,10,11,12-pentahydrocyclohepta[b]thieno[3,2-e]pyrimidin-3-thiones has been synthesized. The intermediates 4-chloro-2-substituted-5,6,7-trihydrocyclopenta/5,6,7,8,9-pentahydrocyclohepta[b]thieno[2,3-d]pyrimidines were prepared by warming 2-substituted-5,6,7-trihydrocyclopenta/5,6,7,8,9-pentahydrocyclohepta[b]thieno[2,3-d]pyrimidin-4[3H]-ones with oxalyl chloride. Thieno[2,3-d]pyrimidin-4[3H]-ones were prepared by a novel, microwave assisted, solvent free, synthetic route under basic conditions hitherto unreported in the literature from ortho amino ester of thiophene. The chloro derivatives, without further purification, were hydrazinated to yield 2-substituted-4-hydrazino-5,6,7-trihydrocyclopenta/5,6,7,8,9-pentahydrocyclohepta[b]thieno[2,3-d]pyrimidines. These compounds were cyclized with carbon disulphide to give the title compounds in quantitative yields. The final compounds were screened for antibacterial activity by Kirby Bauer's method using ampicillin as the standard against various gram positive and gram negative bacteria. All the compounds showed antibacterial activity comparable with the standard.View full abstractDownload PDF (90K) -
Yoshio Satoh, Mitsuru Satoh, Kimiaki Isobe, Kunihiko Mohri, Yuki Yoshi ...2007 Volume 55 Issue 4 Pages 561-564
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSA new Panax acetylene, 3-oxo-PQ-1 (1), was isolated from Panax quinquefolium. The absolute configurations of 3-oxo-PQ-1 (1) and PQ-1 (2) were determined to be (9R,10R) and (3R,9R,10R), respectively, by synthesizing 1 and 2 starting from D-(−)-diethyl tartrate, and by synthesizing their stereoisomers from L-(+)-diethyl tartrate. The growth inhibitory effects of Panax acetylenes (1—8) and their stereoisomers against leukemia cells were tested. Unnatural acetylenes having the (3S)-configuration (2, 5, 6, 7, 8; IC50=0.01—0.1 μg/ml) were found to be approximately ten times more potent than natural acetylenes (IC50=0.1—1.0 μg/ml) with the (3R)-configuration. Potency differences due to the configuration at C-9 and C-10 were unrelated to this stereochemistry. The C14-polyacetylenes, PQ-8 (4) and its isomer (IC50=1.0—10.0 μg/ml), were found to exhibit weaker cytotoxicity than the C17-polyacetylenes.View full abstractDownload PDF (561K) -
Ken-ichi Izutsu, Chikako Yomota, Nobuo Aoyagi2007 Volume 55 Issue 4 Pages 565-570
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSEffects of co-solutes on the physical property of mannitol and sorbitol in frozen solutions and freeze-dried solids were studied as a model of controlling component crystallinity in pharmaceutical formulations. A frozen mannitol solution (500 mM) showed a eutectic crystallization exotherm at −22.8 °C, whereas sorbitol remained amorphous in the freeze-concentrated fraction in the thermal scan. Various inorganic salts reduced the eutectic mannitol crystallization peak. Trisodium and tripotassium phosphates or citrates prevented the mannitol crystallization at much lower concentrations than other salts. They also raised transition temperatures of the frozen mannitol and sorbitol solutions (Tg′: glass transition temperature of maximally freeze-concentrated amorphous phase). Crystallization of some salts (e.g., NaCl) induced crystallization of mannitol at above certain salt concentration ratios. Thermal and near-infrared analyses of cooled-melt amorphous sorbitol solids indicated increased intermolecular hydrogen-bonding in the presence of trisodium phosphate. The sodium phosphates and citrates should prevent crystallization of mannitol in frozen solutions and freeze-dried solids by the intense hydrogen-bonding and reduced molecular mobility in the amorphous phase.View full abstractDownload PDF (232K) -
Masayuki Yoshikawa, Sachiko Sugimoto, Seikou Nakamura, Hisashi Matsuda2007 Volume 55 Issue 4 Pages 571-576
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSSix new dammarane-type triterpene diglycosides with a hydroperoxide group, floralginsenosides A, B, C, D, E, and F, were isolated from ginseng flower, the flower buds of Panax ginseng C. A. MEYER, together with seven known dammarane-type triterpene oligoglycosides. The structures of new floralginsenosides were elucidated on the basis of chemical and physicochemical evidence.View full abstractDownload PDF (230K) -
Dong Qing Fei, Gang Wu, Chun Mei Liu, Kun Gao2007 Volume 55 Issue 4 Pages 577-579
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSA novel benzofuran derivative (R)-(+)-Ligulaodonin A (1) and a new olean-12-ene triterpene (5), as well as 10 known compounds were isolated from the whole plant of Ligularia odontomanes HAND.-MAZZ. The structures of the new compounds were determined by spectroscopic evidence, including IR, UV, EI-MS, positive HR-ESI-MS, 1D-NMR and 2D-NMR. The absolute configuration of 1 was elucidated on the basis of circular dichroism (CD) data.View full abstractDownload PDF (82K) -
Hao Zou, Xuetao Jiang, Lingshan Kong, Shen Gao2007 Volume 55 Issue 4 Pages 580-585
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSA blend of floating and pulsatile principles of drug delivery system seems to present the advantage that a drug can be released in the upper GI tract after a definite time period of no drug release. The objective of this study was to develop and evaluate a floating and pulsatile drug delivery system based on an impermeable cylinder. Pulsatile capsule was prepared by sealing the drug tablet and the buoyant material filler inside the impermeable capsule body with erodible plug. The drug delivery system showed typical floating and pulsatile release profile with a lag time followed by a rapid release phase. The lag time prior to the pulsatile drug release correlated well with the erosion properties of plugs and the composition of the plug could be controlled by the weight of the plug. The buoyancy of the whole system depended on the bulk density of the dosage form. Gamma-scintigraphic evaluation in humans was used to establish methodology capable of showing the subsequent in vivo performance of the floating and pulsatile release capsule. Developed formulations showed instantaneous floating with no drug release during the lag time followed by a pulse drug release. From the gamma-scintigraphic results, the pulsatile release capsule we prepared could achieve a rapid release after lag time in vivo, which was longer than that in vitro. The scintigraphic evaluation could confirm qualitatively that the system with in vitro lag time of 4.0 h provided, with relatively high reproducibility, a pulsatile release occurred around 5.0 h after administration.View full abstractDownload PDF (1114K) -
Hiroaki Arai, Tatsuya Suzuki, Chosei Kaseda, Koichi Ohyama, Kozo Takay ...2007 Volume 55 Issue 4 Pages 586-593
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSOptimal solutions of theophylline tablet formulations were derived from three types of experimental datasets, composed of different numbers of data-points using the response surface method incorporating multivariate spline interpolation (RSMS). The reliability of these optimal solutions was evaluated by a bootstrap re-sampling technique. Different levels of three causal factors were used as factors of response surface analysis: the lactose/cornstarch ratio (X1), the amount of carmellose calcium (X2), and the amount of hydroxypropylcellulose (X3). The target responses were the dissolution ratio of theophylline for the first 15 min (Y1) and the hardness (Y2) of each of the prepared tablets. Similar optimal solutions were estimated in three different sizes of datasets. A bootstrap re-sampling with replacements from the original dataset was applied, and optimal solutions for each bootstrap dataset were estimated. The frequency of the distribution of the optimal solution generated by the bootstrap re-sampling technique demonstrated almost normal distribution. The average and standard deviation of the optimal solution distribution were calculated as evaluation indices reflecting the accuracy and reproducibility of the optimal solution. It was confirmed that the accuracy was sufficiently high, irrespective of the dataset size; however, the reproducibility worsened with a decrease in the number of the experimental datasets. Consequently, it was considered that the novel evaluation method based on the bootstrap re-sampling technique was suitable for evaluating the reliability of the optimal solution.View full abstractDownload PDF (909K) -
Jui-Hsin Su, Chang-Feng Dai, Hsin-Hui Huang, Yang-Chang Wu, Ping-Jyun ...2007 Volume 55 Issue 4 Pages 594-597
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSTwo new sesquiterpenoidal natural products chabrolidiones A and B (1 and 2), two C18 terpenoid-related carboxylic acids, ketochabrolic acid (3) and isoketochabrolic acid (4), and one naphthoquinone derivative chabrolonaphthoquinone C (5), along with two known compounds (+)-aristolone (6) and teuhetenone A (7) were isolated from a Formosan soft coral Nephthea chabrolii. The structures of the new metabolites were determined on the basis of extensive spectroscopic analysis and by comparison of NMR data with those of related metabolites. Metabolite 1 has been synthesized previously, but was isolated for the first time from natural sources. Cytotoxic activity of metabolites 1—3 and 5—7 against a limited panel of cancer cell lines is also described.View full abstractDownload PDF (137K) -
Masayuki Yoshikawa, Seikou Nakamura, Yasuyo Kato, Koudai Matsuhira, Hi ...2007 Volume 55 Issue 4 Pages 598-605
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSThe methanolic extract from the flower buds of Chinese tea plant (Camellia sinensis (L.) O. KUNTZE) was found to inhibit release of β-hexosaminidase from RBL-2H3 cells. From the methanolic extract, six new acylated oleanane-type triterpene oligoglycosides, floratheasaponins D—I, were isolated together with 21 known compounds including floratheasaponins A—C. The chemical structures of floratheasaponins D—I were elucidated on the basis of chemical and physicochemical evidence. The principal constituents, floratheasaponins A—F, were found to show the inhibitory activity on the release of β-hexosaminidase from RBL-2H3 cells.View full abstractDownload PDF (203K) -
Masayuki Yoshikawa, Toshio Morikawa, Yasunobu Asao, Emi Fujiwara, Seik ...2007 Volume 55 Issue 4 Pages 606-612
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSThe methanolic extract from the flowers buds of Camellia japonica L. (Theaceae) were found to exhibit potent inhibitory activities on ethanol- or indomethacin-induced gastric mucosal lesions in rats. Through bioassay-guided separation, 28-noroleanane-type triterpene oligoglycosides, camelliosides A, B, and C, and an oleanane-type triterpene oligoglycoside, camellioside D, were isolated from the methanolic extract together with five known compounds. The absolute stereostructures of camelliosides were determined on the basis of chemical and physicochemical evidence, which included the structure revision of the nortriterpene aglycons (camellenodiol and camelledionol). The principal oligoglycosides, camelliosides A and B, showed platelet aggregation activity in addition to the gastroprotective effects on ethanol- or indomethacin-induced gastric mucosal lesions in rats.View full abstractDownload PDF (233K) -
Hideyuki Sugiyama, Masato Yoshida, Kouji Mori, Tomohiro Kawamoto, Sato ...2007 Volume 55 Issue 4 Pages 613-624
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSAs a novel class of IKKβ inhibitors, a series of tricyclic furan derivatives was designed and synthesized based on the structure of known thiophene IKKβ inhibitors. Among the various fused furan derivatives synthesized, a benzothieno[3,2-b]furan derivative 13a displayed potent inhibitory activity towards IKKβ in enzymatic and cellular assays. The potent inhibitory activity originates from an intramolecular non-bonded S…O interaction which was confirmed by the X-ray structure of JNK3 with 16k. The introduction of further substituents on the core structure led to the discovery of the 6-alkoxy derivatives, which possessed a comparable IKKβ inhibitory activity to 13a and an improved metabolic stability. Among these, appropriately lipophilic compounds 16a, h, i, and 13g (log D>2) were found to possess good oral bioavailability.View full abstractDownload PDF (745K)
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Dafeng Chu, Jingwei Tian, Wanhui Liu, Zi Li, Youxin Li2007 Volume 55 Issue 4 Pages 625-628
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSHuperzine A loaded poly(D,L-lactic-co-glycolic acid) (PLGA) microspheres were prepared by an oil/water (o/w) solvent evaporation technique. With a decrease of the ratio of o/w from 1 : 100 to 1 : 50, the encapsulation efficiency was reduced about 4%. Increasing the PVA concentration from 0.5 to 2% reduced the percentage encapsulation efficiency of huperzine A from 60.7 to 47.4% and the particle size of microspheres from 84.2 to 26.2 μm. The addition of stearic acid improved the encapsulation efficiency, but also accelerated the in vitro release of hupezine A from microspheres. After i.m. administration of huperzine A loaded microspheres in mice, huperzine A was sustained released from the PLGA microspheres up to 12 d with a low initial burst. Passive avoidance test of mice showed that the microspheres formulation offered an improved therapeutic efficiency in the treatment of the impaired memory of the mice superior to injection gastric (i.g.) administration of huperzine A suspension at the same dose, whose therapeutic efficiency was similar as that of a 50% reduced dose of the microspheres formulation.View full abstractDownload PDF (322K) -
Armağan Önal, Sena Çağlar2007 Volume 55 Issue 4 Pages 629-631
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSSimple and reproducible spectrophotometric methods have been developed for determination of dopaminergic drugs used for Parkinson's disease, cabergoline (CAB) and ropinirole hydrochloride (ROP), in pharmaceutical preparations. The methods are based on the reactions between the studied drug substances and ion-pair agents [methyl orange (MO), bromocresol green (BCG) and bromophenol blue (BPB)] producing yellow colored ion-pair complexes in acidic buffers, after extracting in dichloromethane, which are spectrophotometrically determined at the appropriate wavelength of ion-pair complexes. Beer's law was obeyed within the concentration range from 1.0 to 35 μg ml−1. The developed methods were applied successfully for the determination of these drugs in tablets.View full abstractDownload PDF (71K) -
Masateru Ono, Naoki Ishimatsu, Chikako Masuoka, Hitoshi Yoshimitsu, Ry ...2007 Volume 55 Issue 4 Pages 632-634
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSThree new monoterpenoids, called genipacetal, genipamide, and genipaol, were isolated from the fruit of Genipa americana L. (Rubiaceae), along with the four known iridoids genipin, gardendiol, deacetyl asperulosidic acid methyl ester, and shanzhiside. Their chemical structures were determined on the basis of spectroscopic data.View full abstractDownload PDF (291K) -
An-Shen Lin, Fang-Rong Chang, Hsin-Fu Yen, HannaMaria Björkeborn, ...2007 Volume 55 Issue 4 Pages 635-637
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSIn our continuing research on cytotoxic components from the Formosan pteridophyte Thelypteris torresiana (GAUD.) ALSTONONE, two new compounds, a novel flavonoid, flavotorresin (1), and a flavonoid diglycoside, multiflorin C (2), along with five known compounds, were isolated. The structural elucidation was established on the basis of spectroscopic data analysis. The possible biosynthetic pathway of the flavonoids from this fern is summarized.View full abstractDownload PDF (129K) -
Khalil Farhadi, and Ahmad Karimpour2007 Volume 55 Issue 4 Pages 638-642
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSThe adsorptive and electrochemical behaviors of meloxicam (MLC) was investigated on a glassy carbon electrode that was electrochemically treated by anodic oxidation at +1.8 V, following potential cycling in the potential range from −0.8 to 1.0 V vs. Ag/AgCl reference electrode. The resulting electrode showed a good activity to improve the electrochemical response of the drug. MLC was accumulated at an electrochemically activated glassy carbon electrode (phosphate buffer pH 6) in a certain time and then determined by linear sweep voltammetry. The oxidative peak currents showed a linear function in the concentration ranges of 0.02 to 10 μM using a 240 s preconcentration time. The preconcentration medium-exchange approach was utilized for the selective determination of the drug in spiked urine and plasma samples with satisfactory results. The recovery values of the proposed method obtained 105% (RSD 2.5%) and 100% (RSD 1.8%) for urine and plasma samples, respectively. Also, the proposed method has been successfully used for determination of MLC in tablets.View full abstractDownload PDF (111K) -
Alexis Zamble, Thierry Hennebelle, Sevser Sahpaz, François Bail ...2007 Volume 55 Issue 4 Pages 643-645
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSPurification of a Microdesmis keayana hydromethanolic root extract led to the isolation of two new natural compounds, xanthoquininamide (6-hydroxyquinoline-4-carboxamide) and tris(4-hydroxycinnamoyl)spermine (N5-(p-coumaroyl)-N1,N14-diferuloylspermine) which was named keayanine. Their structures were determined using spectroscopic analyses (ESI-MS, 1D- and 2D-NMR).View full abstractDownload PDF (81K) -
Quan Zheng, Wei Li, Likun Han, Kazuo Koike2007 Volume 55 Issue 4 Pages 646-650
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSThree new triterpenoid saponins, gypsosaponins A—C (1—3), were isolated from the roots of Gypsophila oldhamiana (Caryophyllaceae). Their structures were established as 3-O-β-D-galactopyranosyl-(1→2)-[β-D-xylopyranosyl-(1→3)]-β-D-glucuronopyranosyl quillaic acid 28-O-α-L-arabinopyranosyl-(1→2)-α-L-arabinopyranosyl-(1→3)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-β-D-fucopyranoside (1), 3-O-β-D-galactopyranosyl-(1→2)-[β-D-xylopyranosyl-(1→3)]-methyl-β-D-glucuronopyranosyl gypsogenin 28-O-β-D-glucopyranosyl-(1→3)-[β-D-xylopyranosyl-(1→4)]-α-L-rhamnopyranosyl-(1→2)-β-D-fucopyranoside (2), and 23-O-β-D-glucopyranosyl gypsogenic acid 28-O-β-D-glucopyranosyl-(1→3)-[β-D-glucopyranosyl-(1→6)]-β-D-glucopyranoside (3), on the basis of various spectroscopic analyses and chemical degradations. The biological activities of 1—3 were examined inhibitory activity against pancreatic lipase, which showed inhibition of 58.2%, 99.2% and 50.3% at concentration of 1 mg/ml, respectively.View full abstractDownload PDF (107K) -
Takanori Nakamura, Tomomi Noguchi, Hiroyuki Miyachi, Yuichi Hashimoto2007 Volume 55 Issue 4 Pages 651-654
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSPutative hydrolyzed metabolites of thalidomide were prepared and characterized, and their inhibitory activity on tumor necrosis factor (TNF)-α production in the human monocytic leukemia cell line THP-1 was evaluated. α-(2-Carboxybenzamido)glutarimide was a more potent TNF-α production inhibitor than thalidomide.View full abstractDownload PDF (158K) -
Ping Chen, and Jun-Shan Yang2007 Volume 55 Issue 4 Pages 655-657
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSChemical examination of the stems of Caesalpinia millettii HOOK. et ARN. led to the isolation of new flavonol glycoside caffeiate ester (1) and homoisoflavone (2), along with four known homoisoflavones: eucomin (3), bonducellin (4), 8-methoxybonducellin (5) and intricatinol (6). The structures of 1 and 2 were established to be tamarixetin 3-O-(6″-O-E-caffeoyl)-β-D-galactopyranoside (1) and (Z)-7-hydroxy-8-methoxy-3-(4-methoxybenzyl) chroman-4-one (2) on the basis of detailed analyses of physical, chemical, and spectral data. Compounds 3—6 were isolated from this plant for the first time.View full abstractDownload PDF (101K) -
Lihong Lin, Haihua Huang, Peng Zhang, Xiulan Qi, Dafang Zhong2007 Volume 55 Issue 4 Pages 658-661
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSThe capability of Cunninghamella blakesleeana AS 3.153 to transform CYP2D6 probe drug dextromethorphan was investigated. Metabolites produced by strain AS 3.153 were detected by liquid chromatography-tandem mass spectrometry (LC-MSn) and the metabolite dextrorphan was identified by reference to confirm its structure. The yield of dextrorphan produced by C. blakesleeana AS 3.153 was over 90%. Quinidine, a CYP2D6 selective inhibitor, was applied to investigate its effect on biotransformation. The concentration of quinidine was 4-folds higher than that of dextromethorphan and the yield of dextrorphan was reduced by 84%, which proved there was drug metabolism enzyme similar to CYP2D6 in C. blakesleeana AS 3.153. It is concluded that C. blakesleeana AS 3.153 can be used as the suitable model strain in vitro to mimic human CYP2D6 metabolism.View full abstractDownload PDF (119K) -
Tatsuya Higashi, Tadashi Nishio, Noriko Hayashi, Kazutake Shimada2007 Volume 55 Issue 4 Pages 662-665
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSA derivatization procedure has been examined to enhance the electrospray ionization (ESI)-MS detectabilities of steroids that charged derivatization is not suitable for. The derivatization procedure with 2-hydrazinopyridine or isonicotinoyl azide was very effective for the sensitive detection of di-oxosteroids or di-hydroxysteroids, respectively, and the detection limits of the resulting derivatives were as low as about 2 fmol. The derivatives also provided intense characteristic product ions in the MS–MS, which are expected to be usable for the selected reaction monitoring mode.View full abstractDownload PDF (120K) -
Ping-Jyun Sung, Mei-Ru Lin, Jih-Jung Chen, Shen-Fan Lin, Yang-Chang Wu ...2007 Volume 55 Issue 4 Pages 666-668
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSTwo 27C hydroperoxysterols, 7β-hydroperoxycholesterol (1) and its stereoisomer 7α-hydroperoxycholesterol (2), were isolated from the lipophilic extracts of a Formosan tunicate belonging to the genus Eudistoma. The structures of sterols 1 and 2 were elucidated on the basis of extensive spectral data analyses. Cytotoxicity of sterols 1 and 2 against a limited panel of cancer cell lines is also described. Sterol 1 show weak inhibitory effects on human neutrophil elastase release.View full abstractDownload PDF (61K) -
Jahanbakhsh Ghasemi, Saadi Saaidpour2007 Volume 55 Issue 4 Pages 669-674
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSA quantitative structure property relationship (QSPR) study was performed to develop a model that relates the structures of 150 drug organic compounds to their aqueous solubility (log Sw). Molecular descriptors derived solely from 3D structure were used to represent molecular structures. A subset of the calculated descriptors selected using stepwise regression that used in the QSPR model development. Multiple linear regression (MLR) is utilized to construct the linear QSPR model. The applied multiple linear regression is based on a variety of theoretical molecular descriptors selected by the stepwise variable subset selection procedure. Stepwise regression was employed to develop a regression equation based on 110 training compounds, and predictive ability was tested on 40 compounds reserved for that purpose. The final regression equation included three parameters that consisted of octanol/water partition coefficient (log P), molecular volume (MV) and hydrogen bond forming ability (HB), of the drug molecules, all of which could be related to solubility property. Application of the developed model to a testing set of 40 drug organic compounds demonstrates that the new model is reliable with good predictive accuracy and simple formulation. The use of descriptors calculated only from molecular structure eliminates the need for experimental determination of properties for use in the correlation and allows for the estimation of aqueous solubility for molecules not yet synthesized. The prediction results are in good agreement with the experimental values. The root mean square error of prediction (RMSEP) and square correlation coefficient (R2) of prediction of log Sw were 0.0959 and 0.9954, respectively.View full abstractDownload PDF (99K) -
Yuko Ogawa, Hisae Oku, Emiko Iwaoka, Munekazu Iinuma, Kyoko Ishiguroa2007 Volume 55 Issue 4 Pages 675-678
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSAllergy-preventive activity was demonstrated for an extract of resins from Xanthorrhoea hastilis R. BR. in a search for allergy-preventive substances from natural sources. By bioassay-directed fractionation of this plant extract, a new flavanone, 3′,5′-dihydroxy-7,4′-dimethoxyflavanone (1), and two new chalcones, 3,5,2′-trihydroxy-4,4′-dimethoxychalcone (2) and 5,2′-dihydroxy-3,4,4′-trimethoxychalcone (3), were isolated together with five known compounds, 5′-hydroxy-7,3′,4′-trimethoxyflavanone (4), 3′-hydroxy-7,4′-dimethoxyflavanone (5), liquiritigenin 7-methyl ether (6), 4,2′-dihydroxy-4′-methoxychalcone (7) and sakuranetin (8). The structures of 1, 2 and 3 were elucidated by spectroscopic methods. All of these compounds showed allergy-preventive effects.View full abstractDownload PDF (165K) -
Junzhi Wang, Kun Zou, Yanming Zhang, Chuang Liu, Jun Wu, Yuan Zhou, Fe ...2007 Volume 55 Issue 4 Pages 679-681
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSA novel 18-norspirostanol saponin (1), along with Trillenoside A (2), was obtained from the underground parts of Trillium tschonoskii MAXIM., collected in Shennongjia Forest District, China. Based on the chemical and spectroscopic evidences, their structures were determined as shown in Fig. 1. 1 and 2 displayed marked inhibitory action towards COX-2 production in macrophagocytes of the mouse abdominal cavity stimulated by LPS at 10 μg/ml.View full abstractDownload PDF (64K) -
Krishna Prasad Devkota, Muhammad Iqbal Choudhary, Sarfaraz Ahmed Nawaz ...2007 Volume 55 Issue 4 Pages 682-684
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESSThe microbial transformation of a steroidal alkaloid, dictyophlebine (1) with Rhizopus stolonifer (ATCC 10404) afforded three oxidized metabolites 2—4. Compound 2 was found to be a new product. These metabolites were structurally characterized on the basis of modern spectroscopic techniques. Their inhibitory activity towards acetyl- and butyrylcholinesterase has been evaluated and the new product 2 has been found to be more potent than the parent compound and other metabolites.View full abstractDownload PDF (98K) -
Shinya Kida, Mitsuko Maeda, Keiko Hojo, Yusuke Eto, Shinsaku Nakagawa, ...2007 Volume 55 Issue 4 Pages 685-687
Published: 2007
Released on J-STAGE: April 01, 2007
JOURNAL FREE ACCESS6-Maleimidohexanoic acid N-hydroxysuccinimide ester has been used widely for preparation of enzyme immunoconjugates as a unique heterobifunctional cross-linking reagent. Its heterobifunctional reactivity is good, but its ester portion hydrolyzes easily in the presence of water. Several 6-maleimidohexanoic acid active esters (6-maleimidohexanoic acid 4-nitrophenyl ester, 6-maleimidohexanoic acid N-hydroxy-5-norbornene-endo-2,3-dicarboximide ester, and 6-maleimidohexanoic acid pentafluorophenyl ester) were prepared and their reactivity and stability in an aqueous media were tested. Of the synthetic esters, the pentafluorophenyl ester exhibited the highest reactivity and stability in aqueous media.View full abstractDownload PDF (100K)
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