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Volume 54, Issue 1
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Ugur Sezai Yigit, Fatma Yurt Lambrecht, Perihan Ünak, Fazilet Z&u ...2006 Volume 54 Issue 1 Pages 1-3
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSThe aim of this study was to label ascorbic acid with 99mTc and to investigate its radiopharmaceutical potential in rats. Ascorbic acid was labeled with 99mTc using the stannous chloride method. The radiochemical purity of [99mTc]ascorbic acid (99mTc-AA) was determined by RTLC, paper electrophoresis, and RHPLC methods. The labeling yield was found to be 93±5.0%. The maximum labeling yield of 99mTc-AA was determined at pH 5 and 25ºC. The biodistribution studies related to 99mTc-AA were done in male albino Wistar rats. 99mTc-AA, which has a specific activity of 13.02 GBq/mmol, was administered into the tail vein of the rats. The rats were sacrificed at 15, 30, 60, and 120 min after the injection by heart puncture under ether anaesthesia. The organs were weighed after removal. Their activities were counted using a Cd(Te) detector equipped with a RAD 501 count system. The %ID/g (% of injected dose per gram of tissue weight) in each organ and in blood was calculated. Maximum uptake of 99mTc-AA was observed in prostate and kidneys at the 60th min. 99mTc-AA may be a promising radiopharmaceutical for the imaging of prostate and kidneys.View full abstractDownload PDF (267K) -
Shengan Tang, Yuehu Pei, Hongzheng Fu, Zhiwei Deng, Jun Li, Peter Prok ...2006 Volume 54 Issue 1 Pages 4-8
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSA chemical investigation of Jaspis sp., the marine sponge collected from the South China Sea led to the isolation of six new isomalabaricane-type compounds, jaspolides A—F (1—6). The structures of those compounds were elucidated by extensive spectroscopic methods. The structure-types of 1 to 6 could be classified into triterpenes (1, 2), sesterterpene (6), diterpenes (3, 4), and nortriterpene (5). The biogenetic transformation of the isolated compounds was also speculated.View full abstractDownload PDF (129K) -
Pirouzpanah Saieed, Rashidi Mohammad Reza, Delazar Abbas, Razavieh Sey ...2006 Volume 54 Issue 1 Pages 9-13
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSRuta graveolens L. is a flavonoid-containing medicinal plant with various biological properties. In the present study, the effects of R. graveolens extract on aldehyde oxidase, a molybdenum hydroxylase, are investigated. Aldehyde oxidase was partially purified from liver homogenates of mature male guinea pigs by heat treatment and ammonium sulphate precipitation. The total extract was obtained by macerating the aerial parts of R. graveolens in MeOH 70% and the effect of this extract on the enzyme activity was assayed using phenanthridine, vanillin and benzaldehyde as substrates. Quercetin and its glycoside form, rutin were isolated, purified and identified from the extract and their inhibitory effects on the enzyme were investigated. R. graveolens extract exhibited a high inhibition on aldehyde oxidase activity (89—96%) at 100 μg/ml which was comparable with 10 μM of menadione, a specific potent inhibitor of aldehyde oxidase. The IC50 values for the inhibitory effect of extract against the oxidation of benzaldehyde, vanillin and phenanthridine were 10.4, 10.1, 43.2 μg/ml, respectively. Both quercetin and rutin at 10 μM caused 70—96% and 27—52% inhibition on the enzyme activity, respectively. Quercetin was more potent inhibitor than rutin, but both flavonols exerted their inhibitory effects mostly in a linear mixed-type.View full abstractDownload PDF (166K) -
Tsutomu Warashina, Yoshimi Nagatani, Tadataka Noro2006 Volume 54 Issue 1 Pages 14-20
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSThirteen new phenolic glycosides were obtained by further study of constituents from the bark of Tabebuia impetiginosa (MART. ex DC) Standley (Bignoniaceae). The structures of these compounds were determined based on NMR, mass spectral and chemical evidence. Most of them have a glycosyl unit esterified by a benzoic acid derivative.View full abstractDownload PDF (230K) -
Xiao-Yu Guo, Jue Wang, Nai-Li Wang, Susumu Kitanaka, Hong-Wei Liu, Xin ...2006 Volume 54 Issue 1 Pages 21-25
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSSix new stilbenoids, a (bibenzyldihydrophenanthrene) ether designated phoyunnanin D (1), a bis(dihydrophenanthrene) ether designated phoyunnanin E (2), and four stilbenes designated phoyunbene A—D (3—6), were isolated from the air-dried whole plant of Pholidota yunnanensis ROLFE. The new compounds were identified as 7-[2-(3-hydroxyphenethyl)-4-hydroxy-6-methoxyphenoxy]-4-hydroxy-2-methoxy-9,10-dihydrophenanthrene (1), 1-[(9,10-dihydro-4-hydroxy-2-methoxy-7-phenanthrenyl)oxy]-4,7-dihydroxy-2-methoxy-9,10-dihydrophenanthrene (2), trans-3,3′-dihydroxy-2′,4′,5-trimethoxystilbene (3), trans-3,4′-dihydroxy-2′,3′,5-trimethoxystilbene (4), trans-3,3′-dihydroxy-2′,5-dimethoxystilbene (5), and trans-3-hydroxy-2′,3′,5-trimethoxystilbene (6) based on spectroscopic evidence. Furthermore, the inhibitory effects of compounds 1—6 on nitric oxide production in a murine macrophage-like cell line (RAW 264.7) activated by lipopolysaccharide and interferon-γ were examined.View full abstractDownload PDF (129K) -
Yoshiyuki Hagiwara, Hidetoshi Arima, Yuji Miyamoto, Fumitoshi Hirayama ...2006 Volume 54 Issue 1 Pages 26-32
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSTo evaluate the potential use of a drug/cyclodextrin (CyD) conjugate for efficient entrapment in liposomes and prolonged residence of a drug in tissues, we synthesized a salicylic acid (SA) conjugate bound covalently with γ-cyclodextrin (SA/γ-CyD conjugate), a model drug/CyD conjugate, and then liposomes entrapping the conjugate (conjugate-in-liposome) were prepared by a freezing-thawing method. The chemical and physicochemical properties of the SA/γ-CyD conjugate in solution and solid state were investigated and then the physicochemical properties of conjugate-in-liposome, in vitro cellular uptake/release and in vivo disposition of SA/γ-CyD conjugate after intravenous administration of aqueous suspension containing conjugate-in-liposome in rats, were evaluated, comparing with those of the liposome-entrapped SA alone (SA-in-liposome) or the liposome-entrapped noncovalent SA/γ-CyD complex (complex-in-liposome). As a result, it was found that the conjugate was amorphous powder and the release of SA from the conjugate in phosphate-buffered saline (PBS) was tolerated to chemical and enzymatic degradation. Meanwhile, the particle sizes and stability of these liposomes were almost identical, and the entrapment ratio of SA/γ-CyD conjugate in liposomes was higher than those of SA alone and SA/γ-CyD complex. The cellular uptake of these liposomes was almost equivalent, but the release of SA/γ-CyD conjugate from RAW264.7 cells was markedly slower, compared with that of SA from cells following cellular uptake of the SA-in-liposome and complex-in-liposome. The disposition of SA or SA/γ-CyD conjugate following intravenous administration of aqueous suspensions containing each liposome system in rats was comparable, but the residence time of the conjugate in tissues significantly prolonged, compared with that of the SA-in-liposome and complex-in-liposome systems. These results suggest the potential use of SA/γ-CyD conjugate for efficient entrapment in liposomes as well as of liposomes containing SA/γ-CyD conjugates for prolonged residence of drugs in tissues.View full abstractDownload PDF (238K) -
Optimized and Validated Initial-Rate Method for the Determination of Perindopril Erbumine in TabletsNafisur Rahman, Nishat Anwar, Mohammad Kashif2006 Volume 54 Issue 1 Pages 33-36
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSA simple and sensitive kinetic spectrophotometric method for the determination of perindopril in pharmaceutical preparations is described. The method is based on the interaction of drug with 1-chloro-2,4-dinitrobenzene (CDNB) in dimethylsulfoxide (DMSO) at 40±1 °C. The reaction is followed spectrophotometrically by measuring the rate of change of the absorbance at 420 nm. Under the optimized experimental conditions, the calibration curve showed a linear relationship over the concentration range of 20—140 μg/ml. The activation parameter such as Ea, ΔH*, ΔS* and ΔG* for this reaction were calculated and found to be 27.31 kJ/mol, 24.69 kJ/mol, −138.84 J/K/mol and 61.50 kJ/mol, respectively. The method has been successfully applied to the determination of perindopril in commercial dosage forms. Statistical comparison of the results with the Abdellatef's spectrophotometric method6) shows excellent agreement and indicates no significant difference between the methods compared in terms of accuracy and precision.View full abstractDownload PDF (115K) -
Liang Wang, Fu De Cui, Hisakazu Sunada2006 Volume 54 Issue 1 Pages 37-43
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSSolid dispersions (SD) of nitrendipine (NTD), a poorly water-soluble drug, were prepared using the melt-mixing method with hydrophilic silica particles (Aerosil and Sylysia) with different particle size and specific surface areas as carriers. Powder X-ray diffraction and differential scanning calorimetry evaluation showed that NTD in the SDs treated with the melt-mixing method was dispersed in the amorphous state. FT-IR spectroscopy obtained with the SDs indicated the presence of hydrogen bonding between the secondary amine groups of NTD and silanol groups of silica particles. The dissolution property of NTD in the SDs was remarkably improved regardless of the grade of silica. At the end of the dissolution test (60 min) the concentrations of NTD for the SDs with Aerosil 200 and Sylysia 350 were 8.88 and 10.09 μg/ml, corresponding to 28 and 31 times that of the original NTD crystals, respectively. The specific surface area and the adsorbed water amount of the SDs were also significantly improved. The rapid dissolution rate from the SDs was attributed to the amorphization of drug, improved specific surface area and wettability than the original drug crystals. In the stability test, powder X-ray diffraction pattern indicated that amorphous NTD in the SD with Aerosil 200 was stable for at least 1 month under the humid conditions (40 °C/75% RH).View full abstractDownload PDF (707K) -
Pittaya Tuntiwachwuttikul, Photchana Phansa, Yupa Pootaeng-on, Walter ...2006 Volume 54 Issue 1 Pages 44-47
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSFour new chromones, perforamone A, B, C, and D have been isolated together with six known compounds, peucenin-7-methyl ether, O-methylalloptaeroxylin, perforatic acid, eugenin, saikochromone A and greveichromenol, from the branches of Harrisonia perforata (Simaroubaceae). The structures were identified by spectroscopic data. The compounds were tested for antimycobacterial and antiplasmodial activities.View full abstractDownload PDF (129K) -
Yueling Xie, Wei Lu, Shilei Cao, Xinguo Jiang, Ming Yin, Wenlu Tang2006 Volume 54 Issue 1 Pages 48-53
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSRadix Bupleuri is widely used in traditional medicine for the treatment of fever, pain, and inflammation associated with influenza or the common cold. The essential oil extracted from the herb is generally claimed to play the major role in the efficacious treatment of fever. The purpose of the present study was to formulate an intranasal delivery system for the essential oil in an aqueous solution used in the form of nasal spray. From 450 g Radix Bupleuri was extracted the essential oil in the amount of about 0.2 ml, which was slightly water-soluble and viscous with low-fluidity. In order to dissolve the essential oil evenly in the aqueous solution, tween-80 (TW-80, used in 10% (w/v) solution), propylene glycol (PG) and diethylene glycol monoethyl ether (TC) were selected as the favorable solubilizing agents, whose amount was respectively determined by L16(45) orthogonal design. An aqueous solution with clarity and no ciliotoxicity was prepared when TW-80 8% (v/v), PG 14.4% (v/v) and TC 14.4% (v/v) were added. Employed to evaluate the acute toxicity, the rats grew well and were kept active and healthy within 14 d after an intranasal administration of this preparation at the dose of oil from 10 g Bupleuri/kg (50-fold higher than the clinical dose), indicating that there would be no serious toxicity at the normal dose. Intranasal administration of this preparation to 2 kg rabbits with fever induced by subcutaneous injection of turpentine decreased body temperature markedly (0.5, 0.8 and 1.0 °C respectively at the dose of oil from 1, 2 and 4 g Bupleuri/body). In addition, the administration significantly reduced fever in 200 g rats induced by intramuscular injection of colicine suspension (0.6 °C at the dose of oil from 0.8 g Bupleuri/body). The results suggest that the formulation of nasal spray for the essential oil from Radix Bupleuri can be potentially effective in the treatment of fever.View full abstractDownload PDF (951K) -
Elizabeth Gómez, Guadalupe Contreras-Ordoñez, Teresa Ram ...2006 Volume 54 Issue 1 Pages 54-57
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSThe synthesis of pentacoordinated Tin(IV) compounds derived from aminoalcohols is described. The compounds were characterized by IR, 1H-, 13C-, and 119Sn-NMR, the mass spectrometry exhibits molecular ions corresponding to monomeric species. All compounds were evaluated for in vitro cytotoxic activities against five human tumor cell lines, U251 (human glioblastoma), PC-3 (human prostatic adenocarcinoma), K-562 (human chronic myelogenous leukemia), HCT-15 (human colorectal adenocarcinoma), MCF-7 (human mammary adenocarcinoma). The cytotoxic evaluation revealed that all compounds possess higher cytotoxic potency than that of the cisplatin, which was used as reference. Additionally, MT2 cells (human T-lymphocytes) were also evaluated.View full abstractDownload PDF (96K) -
Masami Yamada, Takashi Ichikawa, Toru Yamano, Fumio Kikumoto, Yuji Nis ...2006 Volume 54 Issue 1 Pages 58-62
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSTwo new synthetic methods were established for the efficient synthesis of optically active cyclohexene antisepsis agent, ethyl (6R)-6-[N-(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate [(R)-1: TAK-242)]. The first method involved recrystallization from methanol of the diastereomeric mixture (6RS,1′R)-7, obtained by esterification of carboxylic acid 3 with (S)-1-(4-nitrophenyl)ethanol [(S)-5)] to give the desired isomer (6R,1′R)-7 with 99% de in 32% yield. Subsequent catalytic hydrogenolysis and esterification gave (R)-1 with >99% ee. The second method employed enantioselective hydrolysis of acetoxymethyl ester 9a (prepared by alkylation of 3 with bromomethyl acetate) with Lipase PS-D to give the eutomeric enantiomer (R)-9a with excellent enantioselectivity (>99% ee) and high yield (48%). The desired (R)-1 was then obtained by transesterification with ethanol in the presence of concentrated sulfuric acid without loss of ee. Of these, the procedure employing enzymatic kinetic resolution using Lipase PS-D is the more efficient and practical preparation of (R)-1.View full abstractDownload PDF (176K) -
Masashi Ohba, Rie Izuta, Emi Shimizu2006 Volume 54 Issue 1 Pages 63-67
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSA full account of the total synthesis of two monoterpene alkaloids, (−)-plectrodorine [(−)-1] and (+)-oxerine [(+)-3], is presented. The key steps involved are the formation of the oxazole alcohol 10 from the γ-butyrolactone 9 and the intramolecular Diels–Alder reaction of the oxazole–olefins 13a, b. Since the sign of specific rotation for the synthetic (+)-3 was different from that reported for natural oxerine, the absolute configuration of this alkaloid is not yet fully understood.View full abstractDownload PDF (176K) -
Yoshinori Onuki, Mariko Morishita, Yoshiyuki Chiba, Shinji Tokiwa, Koz ...2006 Volume 54 Issue 1 Pages 68-71
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSWe investigated the effect of fatty acids such as stearic acid (SA, 18:0), oleic acid (OA, 18:1), eicosapentaenoic acid (EPA, 20:5), and docosahexaenoic acid (DHA, 22:6) on a dipalmitoylphosphatidylcholine (DPPC) bilayer by determining the phase transition temperature, fluorescence anisotropy of 1,6-diphenyl-1,3,5-hexatriene (DPH), and detergent insolubility. Treatment with unsaturated fatty acid broadened and shifted the phase transitions of the DPPC bilayer to a lower temperature. The phase transition temperature and the value of fluorescence anisotropy of DPH at 37 °C decreased progressively with increasing treatment amounts of unsaturated fatty acid. A large amount of the DPPC bilayer treated with unsaturated fatty acid was dissolved in Triton X-100, obtaining a low level of detergent insolubility. These modifications of the bilayer physical properties were most pronounced with DHA and EPA treatment. These data show that unsaturated fatty acids, particularly DHA and EPA, induce a marked change in the lipid bilayer structure. The composition of fatty acids in the DPPC bilayer was similar after treatment with various unsaturated fatty acids, suggesting that the different actions of unsaturated fatty acids are attributed to change in the molecular structure (e.g., kinked conformation by double bonds). We further explored the change in physical properties induced by fatty acids dispersed in a water-in-oil-in-water multiple emulsion and found that unsaturated fatty acids acted efficiently on the DPPC bilayer, even when incorporated in emulsion form.View full abstractDownload PDF (125K) -
Hong-Ji Quan, Jyunichi Koyanagi, Ken Hagiwara, Xing-Ri Cui, Yasunori I ...2006 Volume 54 Issue 1 Pages 72-79
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESS26-Iodopseudodiosgenin (8) and 26-iodopseudodiosgenone (9) were reacted with various nucleophiles (KSCN, KOCN, NaCN, NaN3 and various amines) to give pseudodiosgenin derivatives (4, 12, 16—20, 26) and pseudodiosgenone derivatives (5, 13, 21—25, 27), respectively. The reactions of 8 and 9 with KOCN gave the elimination products (10) and (11), respectively. The reaction of 9 with NaCN gave 5α,26- (14) and 5β,26-dicyanocholestan-3-one (15). The reaction of 8 with NaN3 gave triazepine derivative (30), while that of 9 gave 26-azidopseudodiosgenone (31). Compound 31 was converted into triazepine derivative (32) by heating at 120 °C. The cytotoxicity of the pseudodiosgenins and pseudodiosgenones on P-gp-underexpressing HCT 116 cells and P-gp-overexpressing Hep G2 cells was examined by MTT assay. Pseudodiosgenins 2, 4, 12 and 30 showed strong cytotoxic activity (IC50 values: 2.6±0.3—6.7±1.4 μM), as did pseudodiosgenones 3, 5, 11, 13, 21—25 and 27 (IC50 values: 1.3±0.3—6.4±0.3 μM) toward HCT 116 cells. Pseudodiosgenins 12, 16 and 30 (IC50 values: 1.2±0.7—2.2±0.6 μM) and pseudodiosgenones 22, 23, 25 and 27 (IC50 values: 0.6±0.1—2.5±0.3 μM) were highly cytotoxic to Hep G2 cells. Compounds 3 and 27 showed efficient antibacterial activity (MIC: 15.6, 10.4 μg/ml) and (MIC: 7.8, 15.6 μg/ml) against Bacillus subtilis and Staphylococcus aureus, respectively.View full abstractDownload PDF (208K) -
Kaname Hashizaki, Hiroyuki Taguchi, Hideki Sakai, Masahiko Abe, Yoshih ...2006 Volume 54 Issue 1 Pages 80-84
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSThe effects of fetal bovine serum (FBS) on carboxyfluorescein (CF) leakage from poly(ethylene glycol)-grafted liposomes (PEG-liposomes) were investigated. PEG-liposomes were prepared from dipalmitoylphosphatidylcholine (DPPC) and distearoyl-N-monomethoxy poly(ethylene glycol)-succinyl-phosphatidylethanolamines (DSPE-PEG) having PEG molecular weights of 1000, 2000, 3000 and 5000. The presence of FBS dramatically increased CF leakage from liposomes near the gel–liquid crystalline phase transition temperature, but had little effect at lower and higher temperatures. The CF leakage from PEG-liposomes whose molecular weight in PEG units was above 2000 was suppressed compared with that of liposomes without PEG. And, there was hardly any difference in the effect of the PEG molecular weight of the PEG-lipids on CF leakage from PEG-liposomes with FBS when PEG-lipids with a molecular weight in PEG units above 2000 were used. On the other hand, the leakage of CF from liposomes containing 0.145 mol fractions of DSPE-PEG1000 was larger than that of liposomes without PEG. Furthermore, the effects of FBS on the cooperative units of lipid molecules during the gel–liquid crystalline phase transition of liposomes were examined. However, the cooperative units of liposomes with FBS had little change compared with that of liposomes without FBS.View full abstractDownload PDF (203K) -
Nour-Eddine Es-Safi, Samira Khlifi, Albert Kollmann, Lucien Kerhoas, A ...2006 Volume 54 Issue 1 Pages 85-88
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSFrom the hydromethanolic extract of the aerial parts of Globularia alypum grown in Morocco, a new chlorinated iridoid glucoside, globularioside has been isolated beside 5 known iridoid glycosides, globularin, globularicisin, globularidin, globularinin and globularimin. This is the first report of a chlorinated iridoid in G. alypum and in the Globulareaceae. Unlike all other known 7-chlorinated iridoid glucosides where the chlorine atom exhibits an α configuration, globularioside incorporate the chlorine atom as a 7β substituent. The structures of the isolated compounds were established on the basis of ESI-MS, MS-MS, 1D and 2D NMR spectral analysis.View full abstractDownload PDF (144K) -
Ping Gao, Pingtian Ding, Hui Xu, Zhenting Yuan, Dawei Chen, Jing Wei, ...2006 Volume 54 Issue 1 Pages 89-93
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSThe purpose of this work was to develop biodegradable microspheres for long term delivery of a potent acetyl cholinesterase inhibitor, huperzine A (Hup-A), which is of interest in the palliative treatment of Alzheimer's disease. Microspheres were successfully prepared with specifically end-group uncapped poly(d,l-lactide acid) and poly(d,l-lactide-co-glycolide acid) using a simple o/w solvent evaporation method. The morphology, particle size and size distribution, drug loading capacity, drug entrapment efficiency (EE) and in vitro drug release were studied in detail. It was found that the terminal group and the inherent viscosity (IV) of the polymers played key role in the drug encapsulation: higher EE was achieved with end-group uncapped and low IV polymers. In vitro drug release from microspheres made from the selected three kinds of polymers revealed sustained release of Hup-A without significant burst release. Preliminary pharmacokinetic study following subcutaneous injection of Hup-A loaded microspheres illustrated the sustained release of the drug over 6—8 weeks at clinically relevant doses in vivo. The studies demonstrated the feasibility of long term delivery of Hup-A using biodegradable microspheres.View full abstractDownload PDF (392K) -
Masaki Mifune, Kenji Kawata, Kurumi Tanaka, Youji Kitamura, Ikuko Tsuk ...2006 Volume 54 Issue 1 Pages 94-98
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSAs one of approaches of developing novel HPLC stationary phases, we prepared Cu-octabromotetrakis(4-carboxyphenyl)porphine derivative-immobilized silica gels (Cu-OBTCPPD), and evaluated the availability of the resultant Cu-OBTCPPD as a stationary phase for separation of poly-aromatic-hydrocarbons (PAHs) and their related compounds. A Cu-OBTCPPD column was revealed to have an ability to separate simple PAHs and be useful as a stationary phase in both polar and non-polar eluents. The retention property of the Cu-OBTCPPD column was evaluated in various comparative experiments using commercially available columns. In comparison with 2-(1-pyrenyl)ethyl dimetylsilyl silica gel column (PYE column) regarding the retention behavior for PAHs etc., the Cu-OBTCPPD column showed stronger interactions involving π electron in non-polar eluent than PYE column. In comparison with a pentabromobenzyloxy propylsilyl silica gel column (PBB column) regarding the influence of bromination, the Cu-OBTCPPD column was affected differently from the PBB column. In comparison with nitrophenylethyl silica gel column (NPE column) regarding the retention behavior for compounds having a dipole in a non-polar eluent, the Cu-OBTCPPD column showed electrostatic interactions such as dipole–dipole interaction equivalent to or larger than the NPE column.View full abstractDownload PDF (315K)
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Dina Nath Mishra, Madhu Bindal, Shailendra Kumar Singh, Sengodan Gurus ...2006 Volume 54 Issue 1 Pages 99-102
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSOrally disintegrating tablets (ODT) are gaining popularity over conventional tablets due to their convenience in administration and suitability for patients having dysphagia. Moreover no water is required for swallowing the tablets and hence suitable for geriatric, pediatric and traveling patients. The purpose of this study is to assess the suitability of spray dried excipient base in the formulation of ODTs of Valdecoxib (low aqueous solubility) and Metoclopramide (high aqueous solubility). Spray dried excipient base was prepared using Scientech spray drier. Super disintegrants (such as Ac-Di-Sol, Kollidon CL, sodium starch glycolate), diluent (mannitol) alongwith sweetening agent (aspartame) were used in the formulation of tablets. The tablets were evaluated for hardness, friability, water absorption ratio, disintegration time (DT) and in vitro drug release. Using the same excipients, the tablets were prepared by direct compression and were evaluated in the similar way. Maximum drug release and minimum DT were observed with Kollidon CL excipient base as compared to tablets prepared by direct compression, showing the superiority of the spray dried excipient base technique over direct compression technique.View full abstractDownload PDF (621K) -
Ejaz Ahmed, Abdul Malik, Sadia Ferheen, Nighat Afza, Azhar-ul-H2006 Volume 54 Issue 1 Pages 103-106
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSMarianine, the new lanostane triterpene (1) and marianosides A (2) and B (3) have been isolated from the whole plant of Silybum marianum. Their structures were elucidated on the basis of extensive analysis of their one dimensional and two dimensional nuclear magnetic resonance (1D, 2D-NMR) spectral data. All inhibited chymotrypsin in a concentration-dependent manner.View full abstractDownload PDF (108K)Xian-Tao Zhang, Lei-Hong Zhang, Wen-Cai Ye, Xiao-Ling Zhang, Zhi-Qi Yi ...2006 Volume 54 Issue 1 Pages 107-110
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSFour new cycloartane glycosides were isolated from the aerial parts of Thalictrum fortunei (Ranunculaceae). The chemical structures of these new glycosides were elucidated as 3-O-β-D-glucopyranosyl-(1→4)-β-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3β,22,26-triol 26-O-β-D-glucopyranoside, 3-O-β-D-glucopyranosyl-(1→4)-β-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3β,22,26-triol 26-O-β-D-quinovopyranosyl-(1→6)-β-D-glucopyranoside, 3-O-β-D-glucopyranosyl-(1→4)-β-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3β,22,26-triol 26-O-β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside, and 3-O-β-D-glucopyranosyl-(1→4)-β-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3β,22,26-triol 26-O-α-L-arabinopyranosyl-(1→6)-β-D-glucopyranoside by extensive NMR methods, HR-ESI-MS, and hydrolysis. This is the first report of (22S,24Z)-3β,22,26-trihydroxycycloartan-24-ene (thelictogenin A, 5) being glycosylated at C-26.View full abstractDownload PDF (88K)Prenylated Xanthone Derivatives with Antiplasmodial Activity from Allanblackia monticola STANER L.C.Anatole Guy Blaise Azebaze, Michèle Meyer, Alexis Valentin, Edw ...2006 Volume 54 Issue 1 Pages 111-113
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSFurther study of the methanol extract of the stem bark of Allanblackia monticola STANER L.C. resulted in the isolation of a new prenylated xanthenedione, designated allanxanthone C, together with the five known xanthones, garciniafuran, tovophyllin A, rubraxanthone, norcowanin and mangostin and one saponin, stigmasterol-3-O-β-D-glucopyranoside. The structure of the new compound was established by detailed spectroscopic analysis to be 1,2-dihydro-3,6,8-trihydroxy-1,1,7-tri(3-methylbut-2-enyl)xanthen-2,9-dione (3-hydroxyapetalinone C). The methanol extract and pure compounds were tested on two strains of Plasmodium falciparum, F32 (chloroquine sensitive) and FcM29 (chloroquine resistant). The IC50 values obtained ranged from 0.6 to 8.9 μg/ml. Their cytotoxicity was estimated on human melanoma cells (A375) and the cytotoxicity/antiplasmodial ratio was found to be between 15.45 and 30.46. The antimicrobial activities against a range of microorganisms of the crude extract and some of these compounds are also reported.View full abstractDownload PDF (94K)Bing-Sheng Yu, Shu-Guang Lai, Qiao-Lin Tan2006 Volume 54 Issue 1 Pages 114-116
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSA capillary GC method was established for simultaneous determination of cinnamaldehyde (CNMD), eugenol (EL) and paeonol (PL) in two traditional Chinese herbal medicinal preparations, Weitongding tablet (WTDT) and Guifu Dihuang pill (GDHP). The assays were based on a programmed temperature GC in a 30 m×0.53 mm capillary column with nitrogen as carrier and FID detector. Good linearities were obtained over ranges of 0.45—452 mg/l CNMD, 0.31—625 mg/l EL and 0.30—610 mg/l PL, respectively. The spike recoveries were within 84—111%.View full abstractDownload PDF (85K)Feng Gao, Dong-Lin Chen, Feng-Peng Wang2006 Volume 54 Issue 1 Pages 117-118
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSTwo new C19-diterpenoid alkaloids, circinadines A (1) and B (2), were isolated from the roots of Aconitum hemsleyanium var. circinacum. Their structures were elucidated by chemical evidence and spectral analyses, including ESI-MS, HR-EI-MS, 1D- and 2D-NMR.View full abstractDownload PDF (91K)Effat Souri, Massoud Amanlou, Hassan Farsam, Alma Afshari2006 Volume 54 Issue 1 Pages 119-122
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSA zero-crossing first-derivative spectrophotometric method is applied for the simultaneous determination of naphazoline hydrochloride and antazoline phosphate in eye drops. The measurements were carried out at wavelengths of 225 and 252 nm for naphazoline hydrochloride and antazoline phosphate, respectively. The method was found to be linear (r2>0.999) in the range of 0.2—1 μg/ml for naphazoline hydrochloride in the presence of 5 μg/ml antazoline phosphate at 225 nm. The same linear correlation (r2>0.999) was obtained in the range of 1—10 μg/ml of antazoline phosphate in the presence of 0.5 μg/ml of naphazoline hydrochloride at 252 nm. The limit of determination was 0.2 μg/ml and 1 μg/ml for naphazoline hydrochloride and antazoline phosphate, respectively. The method was successfully used for simultaneous analysis of naphazoline hydrochloride and antazoline phosphate in eye drops without any interference from excipients and prior separation before analysis.View full abstractDownload PDF (202K)Yuanqiang Guo, Jing Xu, Yushan Li, Ryuichi Watanabe, Yasukatsu Oshima, ...2006 Volume 54 Issue 1 Pages 123-125
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSA new iridoid glycoside, 10-isovaleryl kanokoside C (1), and a new sesquiterpene (2) together with two known compounds (3, 4) were isolated from the rhizomes and roots of Valeriana fauriei. Their structures were elucidated on the basis of spectroscopic analysis. Compounds 2 and 4 showed enhancing activity of nerve growth factor (NGF)-induced neurite outgrowth in PC 12D cells.View full abstractDownload PDF (100K)Jie Shen, Jun-Shan Yang2006 Volume 54 Issue 1 Pages 126-128
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSTwo new xanthones, 1,5,6-trihydroxy-3-methoxy-4-(3-hydroxyl-3-methylbutyl)xanthone (1) and 1,5-dihydroxy-3-methoxy-6′,6′-dimethyl-2H-pyrano(2′,3′:6,7)-4-(3-methylbut-2-enyl)xanthone (2), have been isolated together with six known xanthones: 1,3,5-trihydroxy-6′,6′-dimethyl-2H-pyrano(2′,3′:6,7)xanthone (3), dulxanthone A (4), 1,5,6-trihydroxy-3,7-dimethoxyxanthone (5), 1,7-dihydroxyxanthone (6), 1,3,5-trihydroxy-6-methoxyxanthone (7), 1,3,6,7-tetrahydroxyxanthone (8), from the stems of Garcinia cowa (Guttiferae).View full abstractDownload PDF (89K)Quan-Zhong Sun, Dao-Feng Chen, Pei-Lan Ding, Chao-Mei Ma, Hiroko Kakud ...2006 Volume 54 Issue 1 Pages 129-132
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSThree new lignans, longipedunins A (1), B (2) and C (3), together with three known compounds, benzoyl-binankadsurin A (4), acetyl-binankadsurin A (5) and schisanlactone A (6), were isolated from Kadsura longipedunculata. Their structures and stereochemistry were determined by spectral and single-crystal X-ray analyses. Compounds 1 and 6 showed appreciable inhibitory activity against HIV-1 protease with IC50 values of 50 and 20 μM, respectively.View full abstractDownload PDF (144K)Hui Yao, Zhi-Xin Liao, Qiong Wu, Guang-Qing Lei, Zhi-Jun Liu, Dao-Feng ...2006 Volume 54 Issue 1 Pages 133-135
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSTwo new flavanone glucosides, (2S)-homoeriodictyol 7,4′-di-O-β-D-glucopyranoside (4) and (2R)-eriodictyol 7,4′-di-O-β-D-glucopyranoside (5) were isolated from the branches and leaves of Viscum coloratum (KOMAR) NAKAI (Loranthaceae), along with three known flavanone glucosides: (2S)-homoeriodictyol 7-O-β-D-glucopyranoside (1), (2S)-eriodictyol 7-O-β-D-glucopyranoside (2), and (2S)-naringenin 7-O-β-D-glucopyranoside (3). The structures of these compounds were elucidated using spectroscopic methods. The antioxidant activities of these isolated compounds were evaluated by colorimetric methods based on their scavenging effects on hydroxyl radicals and superoxide anion radicals, respectively. All the compounds showed potent albeit varied degrees of antioxidative activities and the structure–activity relationship is discussed.View full abstractDownload PDF (82K)Yukinori Miyaichi, Norihisa Nunomura, Yukio Kawata, Haruhisa Kizu, Tsu ...2006 Volume 54 Issue 1 Pages 136-138
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSFrom the underground parts of Eskemukerjea megacarpum HARA, two new stilbenes (14, 15) were isolated, together with a known coumarin, 5,7-dihydroxycoumarin (1), a tyramine derivative, trans-feruloyltyramine (2), two pyrogallol derivatives, gallic acid (3) and β-glucogallin (4), four flavonoids, trifolin (5), hyperin (6), myricetin 3-O-β-D-galactopyranoside (7), and myricitrin (8), five stilbenes, resveratorol (9), astringenin (10), piceid (11) astringin (12), and resveratorol 3-O-β-D-(6-O-galloyl)glucopyranoside (13), a flavan-3-ol, (−)-epigallocatechin 3-O-gallate (16), two proanthocyanidins, catechin-(4α→8)-epigallocatechin 3-O-gallate (17) and epicatechin 3-O-gallate-(4β→8)-epigallocatechin 3-O-gallate (18), and an anthocyanin, idaein (19). Compounds 14 and 15 were identified as (E)-3,5,3′,4′-tetrahydroxystilbene 3-O-β-D-(6-O-galloyl)glucopyranoside and (E)-3,5,4′-trihydroxystilbene 3-O-β-D-(6-O-galloyl)glucopyranoside, respectively, based on spectral and chemical data.View full abstractDownload PDF (177K)Phan Minh Giang, Phan Tong Son, Katsuyoshi Matsunami, Hideaki Otsuka2006 Volume 54 Issue 1 Pages 139-140
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSTwo new diarylheptanoids, designated muricarpones A and B, together with three known diarylheptanoids, 1,7-di-(3′,4′-dihydroxyphenyl)-4-hepten-3-one, 1-(3′,4′-dihydroxyphenyl)-7-(4″-hydroxyphenyl)-4-hepten-3-one, and 1,7-bis(p-hydroxyphenyl)-4-hepten-3-one, were isolated from the rhizomes of Amomum muricarpum ELMER (Zingiberaceae). Their structures were determined using spectroscopic analyses.View full abstractDownload PDF (105K)Manabu Matoba, Tetsuya Kajimoto, Kiyoharu Nishide, Manabu Node2006 Volume 54 Issue 1 Pages 141-146
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESS2-Dodecyl-1,3-propanedithiol (2a) was prepared without a malodorous procedure as an odorless reagent that was usable in place of 1,3-propanedithiol (1) in organic reactions, e.g., in the reduction of azides and protection of carbonyl groups. The 1,3-dithioacetals obtained in the latter reaction were effectively reduced to methylene with Raney nickel and reconverted to the original carbonyl compounds by hydrolysis with N-bromosuccinimide in aqueous 2-butanone. In addition, the anion of 1,3-dithiane prepared from 2a and formaldehyde could be utilized as a synthetic equivalent of an anionic carbonyl carbon.View full abstractDownload PDF (200K)Communications to the Editor-
Masatoshi Kawahata, Kazuaki Shikii, Hiroko Seki, Tsutomu Ishikawa, Ken ...2006 Volume 54 Issue 1 Pages 147-148
Published: 2006
Released on J-STAGE: January 01, 2006
JOURNAL FREE ACCESSStoichiometry-controlled complexation of o-phenylenebis-(N,N′-dimethyl-N,N′-ethylene)guanidine (BG) and benzoic acid (BA), which is forming 1 : 1, 1 : 2, 1 : 3, and 1 : 4 BG+BA systems, was observed in solution by using cold-spray ionization mass spectrometry CSI-MS and pulsed field gradient PFG NMR diffusion and in the solid state by X-ray structure analysis.View full abstractDownload PDF (436K)
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