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Volume 54, Issue 8
Displaying 1-35 of 35 articles from this issue
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Regular Articles
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Balasubramanian Narasimhan, Afaque Mehboob Ansari, Nartaj Singh, Vishn ...2006 Volume 54 Issue 8 Pages 1067-1071
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSA method consisting of quantitative structure–activity relationship (QSAR) (MLR) was developed to predict the hydrolytic rate constant of 37 benzoglycolamide ester prodrugs. The regression method was used as a calibration model for calculating the hydrolytic rate constant and investigating their linear characteristics. The QSAR study indicated the importance of the descriptors charge on amide nitrogen (AN), lipophilic parameter (log P) and nucleophilic frontal density (NUFD) in contribution to the ester hydrolysis with the correlation coefficient value of 0.908 for the developed MLR model. The models were validated by leave one out (LOO) technique as well as by the calculation of statistical parameters for the developed MLR models.View full abstractDownload PDF (100K) -
Tsutomu Harada, Ryuichi Narazaki, Shinsuke Nagira, Takayuki Ohwaki, Sh ...2006 Volume 54 Issue 8 Pages 1072-1075
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSThe purpose of this study was to demonstrate the usefulness and broad-applicability of a simple disintegration test method for orally disintegrating tablets (ODT). Eight types of commercial famotidine 20 mg orally disintegrating tablets with different physical properties (formulation, manufacturing method, tablet weight, shape, diameter, thickness, etc.), were used. Disintegration times of these tablets were evaluated employing human sensory test, conventional disintegration test, and the new proposed disintegration test. The human sensory test was performed in 5 healthy volunteers. In the conventional disintegration test, the disintegration apparatus described in the Japanese Pharmacopeia (JP 1st) was used. Our proposed new test which is characterized by a rotating shaft with a low weight (10, 15 g) and rotation speed (10, 25, 50 rpm) was evaluated using tablets with and without storage under severe conditions (60 °C/75%RH for 1 week). The disintegration times of famotidine 20 mg orally disintegrating tablets in human sensory test varied from 9 to 32 s. In contrast, disintegration times in the conventional test were prolonged to over 300 s. Disintegration times in the new proposed test were close to those in human sensory test. Especially, when the new test was conducted with 15 or 10 g weight and 25 rpm, the slope (human sensory test vs. new proposed test) was almost 1. We were able to demonstrate that the new proposed test was useful to estimate the actual human disintegration time.View full abstractDownload PDF (754K) -
Witold Musial, Aleksander Kubis2006 Volume 54 Issue 8 Pages 1076-1081
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSThe aim was to evaluate the interaction between selected alcoholamines and components of artificial skin sebum. The rate and depth of penetration into the lipophilic bead imitating pilosebaceous unit lumen was applied for alcoholamine penetration activity assay. The activity differentiation of 0.5% aqueous alcoholamine solutions with a potential cleansing effect on the pilosebaceous unit was performed. The depth of aminomethylpropanol penetration increased from 0.080 mm after 15 min to 3.049 mm after 72 h. The depth of aminomethylpropendiol penetration increased with time from 0.148 to 4.064, respectively, of diisopropanolamine from 0.481 to 4.626, triethanolamine from 0.236 to 4.342, triisopropanolamine from 0.275 to 2.392 and trometamol from 0.338 to 4.580. The products of alcoholamines reaction with the model skin sebum are easily dispersed in water. The rate of alcoholamines reaction with the model skin sebum depends on the alcoholamine, being the highest in the case of diisopropanolamine, decreasing to minimum for triisopropanolamine. Selected alcoholamines would be applied in ex vivo and in vivo research.View full abstractDownload PDF (743K) -
Chang-Chin Kwan, Wen-Hweu Chu, Saburo Shimabayashi2006 Volume 54 Issue 8 Pages 1082-1087
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSSuspension of concentrated kaolinite (20 g/30 ml-medium) in the presence of polyvinylpyrrolidone (PVP) and sodium lauroyl isethionate (SLI) was allowed to evaluate its degree of dispersion based on their rheological studies. Flow curves at low shear rate, measured by means of cone-plate method, showed a non-Newtonian flow. Plastic viscosity and Bingham yield value were derived from the flow curves. Relative viscosity, effective volume fraction and void fraction of secondary particle were also obtained. Results of dispersity and fluidity of the suspension were explained. PVP acted as a flocculant at a concentration lower than 0.1% but as a dispersant at a higher concentration. The presence of SLI could decrease both the Bingham yield value and suspension viscosity. Cooperative and competitive effects of PVP and SLI were found. Results indicated that SLI enhanced the degree of dispersion of kaolinite when PVP was less than 0.1%. The suspension, however, showed a maximum flocculation (i.e., aggregation) at 4 mM SLI when the concentration of PVP was higher than 0.1%.View full abstractDownload PDF (202K) -
Sadia Ferheen, Ejaz Ahmed, Abdul Malik, Nighat Afza, Muhammad Arif Lod ...2006 Volume 54 Issue 8 Pages 1088-1090
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSHyperinols A (1) and B (2) are new taraxastane type triterpenes which have been isolated from the chloroform soluble fraction of Hypericum oblongifolium and their structures elucidated on the basis of spectroscopic data. Both showed significant inhibitory activity against chymotrypsin enzyme.View full abstractDownload PDF (85K) -
Atsuko Fukui, Ryuta Fujii, Yorinobu Yonezawa, Hisakazu Sunada2006 Volume 54 Issue 8 Pages 1091-1096
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSIn the pharmaceutical preparation of a controlled release drug, it is very important and necessary to understand the entire release properties. As the first step, the dissolution test under various conditions is selected for the in vitro test, and usually the results are analyzed following Drug Approval and Licensing Procedures. In this test, 3 time points for each release ratio, such as 0.2—0.4, 0.4—0.6, and over 0.7, respectively, should be selected in advance. These are analyzed as to whether their values are inside or outside the prescribed aims at each time point. This method is very simple and useful but the details of the release properties can not be clarified or confirmed. The validity of the dissolution test in analysis using a combination of the square-root time law and cube-root law equations to understand all the drug release properties was confirmed by comparing the simulated value with that measured in the previous papers. Dissolution tests under various conditions affecting drug release properties in the human body were then examined, and the results were analyzed by both methods to identify their strengths and weaknesses. Hereafter, the control of pharmaceutical preparation, the manufacturing process, and understanding the drug release properties will be more efficient. It is considered that analysis using the combination of the square-root time law and cube-root law equations is very useful and efficient. The accuracy of predicting drug release properties in the human body was improved and clarified.View full abstractDownload PDF (192K) -
Yuichi Tozuka, Aya Takeshita, Ayako Nagae, Arpansiree Wongmekiat, Kuni ...2006 Volume 54 Issue 8 Pages 1097-1101
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSThe inclusion compound formation between linear amylose of molecular weight 102500 (AS100) and p-aminobenzoic acid (PA) during the sealed-heating process was investigated by powder X-ray diffractometry, infrared spectroscopy and solid state NMR spectroscopy. Sealed-heating of AS100 and PA at 100 °C for 6 h provided an inclusion compound with 61-helix structure, while a 71-helix structure was found when sealed-heating was carried out at 150 °C for 1 h. The formation of an inclusion compound was not observed when sealed-heating was performed at 50 °C for 6 h. The 71-helix inclusion compound maintained its structure even during storage at high temperature while the 61-helix inclusion compound decomposed and returned to the original Va-amylose upon heating to 180 °C. Quantitative determination revealed that one PA molecule could be included per one helical turn of AS100 for both 61-helix and 71-helix inclusion compounds. Solid state NMR spectroscopy suggested that PA molecules were included in the amylose helix core in the 71-helix inclusion compound, while in the case of 61-helix inclusion compound, PA molecules were accommodated in the interstices between amylose helices. Moreover, the inclusion compound formation by sealed-heating of AS100 was also observed when using PA analogues as guest compounds. The binding ratio of AS100 and PA analogues varied depending on the size of guest molecules.View full abstractDownload PDF (973K) -
Sengodan Gurusamy Vijaya Kumar, Dina Nath Mishra2006 Volume 54 Issue 8 Pages 1102-1106
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSIn the present study, the solubilizing and amorphizing properties of Valdecoxib (a poorly water soluble anti inflammatory drug) with low molecular weight chitosan (a polymer), have been investigated. Binary systems of varying drug/polymer ratios were prepared using different techniques (physical mixing, co-grinding, kneading) and were tested for dissolution. Drug carrier interactions were investigated in both the liquid and solid state, by phase solubility analysis, differential scanning calorimetry, powder X-ray diffractrometry, FT-IR spectroscopy and scanning electron microscopy. The solubility of the drug increased with increasing polymer concentration showing AN type phase solubility diagram. Differential scanning calorimetry, powder X-ray diffractrometry and scanning electron microscopic studies of binary systems suggested generation of amorphous form of drug (in kneading and co ground mixtures). IR spectroscopy revealed the presence of hydrogen bonding in kneading and co ground mixtures. Drug dissolution was improved with increasing the polymer concentration in the mixture (Kneaded>co ground>physical mixture), which was attributed to the amorphonization and/or decreased drug crystallinity, size and polymer wetting effect. Enhanced dissolution combined with its direct compression feasibility and anti ulcerogenic action results in low molecular weight chitosan for developing fast release oral solid dosage forms of valdecoxib.View full abstractDownload PDF (662K) -
Susan Sadeghi, Esmat Karimi2006 Volume 54 Issue 8 Pages 1107-1112
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSTwo simple and accurate spectrophotometric methods for determination of Rifampicin (RIF) are described. The first method is based on charge transfer (CT) complex formation of the drug with three π-electron acceptors either 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), 7,7,7,8-Tetracyanoquinodimethane (TCNQ) or 2,3,5,6-Tetrachloro-1,4-benzoquinone (p-chloranil) in acetonitrile. The method is followed spectrophotometrically by measuring the maximum absorbance at 584 nm, 761 nm (680 nm) or 560 nm for DDQ, TCNQ and p-chloranil, respectively. Under the optimized experimental conditions, the calibration curves showed a linear relationship over the concentration ranges of 5—140 μg/ml, 2—45 μg/ml (5—120 μg/ml) and 15—200 μg/ml, respectively. The second method is based on the reaction of RIF with iron(III) forming a water insoluble violet complex which is extracted into chloroform. The method determines RIF in concentration range of 10—240 μg/ml at 540 nm. The proposed methods applied to determination of RIF in capsule, human serum and urine samples with good accuracy and precision. The results were compared statistically with the official method and showed no significant different between the methods compared in terms of accuracy and precision.View full abstractDownload PDF (230K) -
Chavalit Sittisombut, Sabrina Boutefnouchet, Hanh Trinh Van-Dufat, Wen ...2006 Volume 54 Issue 8 Pages 1113-1118
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSCondensation of 2-hydroxy-1-naphthalenecarboxylic acid with phloroglucinol afforded 9,11-dihydroxy-12H-benzo[a]xanthen-12-one (6). Construction of an additional dimethylpyran ring onto this skeleton, by alkylation with 3-chloro-3-methyl-1-butyne followed by Claisen rearrangement, gave access to 6-hydroxy-3,3-dimethyl-3H,7H-benzo[a]pyrano[3,2-h]xanthen-7-one (12) and 5-hydroxy-2,2-dimethyl-2H,6H-benzo[a]pyrano[2,3-i]xanthen-6-one (13), which were methylated into 6-methoxy-3,3-dimethyl-3H,7H-benzo[a]pyrano[3,2-h]xanthen-7-one (14) and 5-methoxy-2,2-dimethyl-2H,6H-benzo[a]pyrano[2,3-i]xanthen-6-one (15), respectively. Osmium tetroxide oxidation of 14 and 15 gave the corresponding (±)-cis-diols 16 and 17, which afforded the corresponding esters 18—21 upon acylation. Similarly, condensation of 2-hydroxy-1-naphthalenecarboxylic acid with 3,5-dimethoxyaniline gave 11-amino-9-methoxy-12H-benzo[a]xanthen-12-one (23) which was converted into 11-amino-9-hydroxy-12H-benzo[a]xanthen-12-one (24) upon treatment with hydrogen bromide in acetic acid. Alkylation with 3-chloro-3-methyl-1-butyne followed by Claisen rearrangement afforded 6-amino-3,3-dimethyl-3H,7H-benzo[a]pyrano[3,2-h]xanthen-7-one (25) and 5-amino-2,2-dimethyl-2H,6H-benzo[a]pyrano[2,3-i]xanthen-6-one (26). The new benzopyranoxanthone derivatives only displayed marginal antiproliferative activity when tested against L1210 and KB-3-1 cell lines. The only compounds found significantly active against L1210 cell line, 16 and 20, belong to the benzo[a]pyrano[3,2-h]xanthen-7-one series, which possess a pyran ring fused angularly onto the xanthone basic core.View full abstractDownload PDF (172K) -
Swapnali Sawant, Diaa Youssef, Alejandro Mayer, Paul Sylvester, Vikram ...2006 Volume 54 Issue 8 Pages 1119-1123
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSSarcophine (1), a cembranoid diterpene is known to inhibit the process of tumorigenesis. Sarcophine can be isolated in large amounts from the Red Sea soft coral Sarcophyton glaucum and hence is an ideal target for semisynthetic or biocatalytic modifications. Hydroxylated derivatives of 1 were reported to improve its anticancer activity. Despite the promising results and ready availability, there are limited attempts towards further diversifying the library of sarcophine derivatives. Hence, the current study targets the epoxide ring to generate sulfur-containing derivatives of sarcophine by reacting it with ammonium thiocyanate and Lawesson's reagent. Structure elucidation of the products was based on extensive 1D and 2D NMR and high resolution mass spectrometry, in addition to mechanistic considerations. The effect of these derivatives on highly malignant +SA mammary epithialial cell proliferation is reported. Anti-inflammatory potential of sarcophine and its derivatives is also demonstrated.View full abstractDownload PDF (198K) -
Abolghasem Jouybana, Maryam Khoubnasabjafari, William Eugene Acree, Jr ...2006 Volume 54 Issue 8 Pages 1124-1130
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSQuantitative structure property relationships were proposed to calculate the binary interaction terms of the Jouyban–Acree model using coefficients of Abraham solvational models. The applicability of the proposed methods for reproducing solubility data of anthracene in binary solvents has been evaluated using 56 solubility data sets collected from the literature. The mean percentage deviation (MPD) of experimental and calculated solubilities, using predicted mole fraction solubility of anthracene in solvents 1 and 2, has been computed as a measure of accuracy and the MPD of the proposed methods were 5.5 and 4.2%. The accuracy of the method was compared with that of a previously reported method where the MPD was 14.4% and the mean differences between proposed and previous methods was statistically significant. To provide a predictive model, solubility of anthracene was computed using Abraham solvational models and employed to predict the solubility in binary solvents using derived model constants of Jouyban–Acree model and the obtained MPDs were 37.9 and 22.2%, respectively.View full abstractDownload PDF (70K) -
Zhi-Tao Liang, Zhi-Hong Jiang, Kelvin Sze-Yin Leung, Zhong-Zhen Zhao2006 Volume 54 Issue 8 Pages 1131-1137
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSHerba Oldenlandiae, the dried herb of Oldenlandia diffusa (WILLD.) ROXB. (Family Rubiaceae), is officially listed in the Chinese Pharmacopoeia. In the herbal market, two substitutes originated from O. corymbosa (L.) LAM and O. tenelliflora BL. are commonly used. In light of this, the target in setting up a method for quality assessment of Herba Oldenlandiae is urgently needed. In this article, a simple and reliable high-performance liquid chromatographic (HPLC) method was developed for quantifying asperuloside (1), E-6-O-p-coumaroyl scandoside methyl ester (2) and E-6-O-p-coumaroyl scandoside methyl ester-10-methyl ether (3) in Herba Oldenlandiae derived from O. diffusa. Among them, compound 3 is a new compound isolated from O. diffusa. All these unique compounds were used as markers for the first time in the quality assessment of Herba Oldenlandiae. The results showed that the contents of compounds 1—3 were significantly varied among different samples whilst those of compounds 2 and 3 were found to be lower in contents in the two substitutes of O. diffusa. The analytical method is suitable for quality control of Herba Oldenlandiae and useful in differentiation from its confusable species. The method has been fully validated with satisfactory linearity, accuracy, precision and stability.View full abstractDownload PDF (295K) -
Construction of Tricyclic Enone, a Common Precursor for Aphidicolane and Stemodane B/C/D-Ring SystemTetsuaki Tanaka, Sachiko Yamamoto, Kei Hiramatsu, Kazuo Murakami, Hito ...2006 Volume 54 Issue 8 Pages 1138-1143
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSSynthesis of a tricyclic enone (B/C/D ring system), a common key precursor for the aphidicolane- and stemodane-type diterpene, is described. The key reaction for the construction of the quaternary carbon center is allylation of epoxide at the more substituted carbon with an organotitanium reagent. Asymmetric reduction with DIP-Cl followed by stereoselective cyclization of spirocyclic ketone and the functional group modification gave the desired tricyclic enone in good yield.View full abstractDownload PDF (218K) -
Hao Wang, Fei-Hua Wu, Fei Xiong, Jia-Jun Wu, Lu-Yong Zhang, Wen-Cai Ye ...2006 Volume 54 Issue 8 Pages 1144-1149
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSFour new non-glycosidic iridoids, piscrocins D (1), E (2), F (6), and G (7), as well as two new iridoid glycosides, piscrosides A (8) and B (9), were isolated from the roots of Neopicrorhiza scrophulariiflora (Scrophulariaceae), together with seven known iridoids. The structures of the isolated compounds were established by means of 1D and 2D NMR spectroscopy and chemical methods. The hepatoprotective activities of these compounds were evaluated by measuring their effects on CCl4-induced hepatocytes damage in vitro, and the structure–activity relationships were also discussed.View full abstractDownload PDF (188K) -
Kewei Lei, Weisheng Liu, Xiaofeng Huang, Daqi Wang2006 Volume 54 Issue 8 Pages 1150-1154
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSA 2,2′-[2,3-naphthylenebis(oxy)]-bis(N,N-diisopropyl(acetamide)) ligand (L) and its Gd(III) complex have been prepared and characterized. The crystal and molecular structure of the complex was determined by single-crystal X-ray diffraction. The interactions of complex with calf thymus DNA were investigated by UV–vis, fluorescence and viscosity measurements. Experimental results indicated that the complex can bind to DNA by intercalation modes. Its intrinsic binding constant is 1.03×106 M−1.View full abstractDownload PDF (292K) -
Noriaki Funasaki, Ikumi Uratsuji, Takashi Okuno, Shun Hirota, Saburo N ...2006 Volume 54 Issue 8 Pages 1155-1161
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSThe masking mechanisms of the bitter taste of propantheline bromide (PB) and oxyphenonium (OB) bromide by native and modified cyclodextrins, saccharides, surfactants, organic acids, nonionic and anionic polymers, and other compounds were investigated with ion selective electrodes. The intensity of the bitter taste for a mixed solution of cyclodextrin with PB or OB was quantitatively explained from the observed electromotive force with the following assumptions: the complex and the masking agent do not have any tastes and the bitter taste is independent of other tastes. Sodium dodecyl sulfate reduced the bitter taste remarkably, and this reduction was also explicable on the basis of the same mechanism. Sodium taurodeoxycholate enhanced the bitter taste, because of its strong bitterness, although it formed 1 : 1 complexes with PB and OB. The masking mechanism of saccharides was ascribed to overcoming the weak bitterness of the drug by the strong sweetness. λ-Carrageenan suppressed the bitter taste remarkably. This suppression was ascribed to the binding of PB and OB to λ-carrageenan, the effect of the solution viscosity on the bitter taste, and the covering of the bitter taste receptor by λ-carrageenan. It was suggested that the moderate masking by other polymers was attributable to the effect of the solution viscosity or the receptor covering. Native and modified β-cyclodextrins, sodium dodecyl sulfate, λ-carrageenan, Tween 20, and sodium carboxymethyl cellulose are good masking agents for the bitter tastes of PB and OB. The drug ion selective electrode is a useful tool for understanding of the masking mechanism of the bitter taste, screening of masking agents, and estimation of appropriate concentrations of the masking agents.View full abstractDownload PDF (131K) -
Kenji Hoshi, Junko Kawakami, Wataru Sato, Kenichi Sato, Akira Sugawara ...2006 Volume 54 Issue 8 Pages 1162-1169
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSPatients with hyperthyroidism sometimes take much time to receive the final diagnosis. To improve patient QOL, simple screening for hyperthyroidism by thyroid non-specialists at the physical check-up is highly expected. Therefore, we applied both Bayesian-type and SOM-type neural networks since we assured the approach useful in analysing thyroid function diagnosis in the previous work. Routine test (14 parameters) data from 66 subjects with a known diagnosis (18 patients with hyperthyroidism and 48 healthy volunteers) were adopted as learning data, and then 142 individuals who also received the same routine tests at the Tohoku University Hospital were screened to predict patients with hyperthyroidism. Both neural networks using 14 parameters predicted several patients as having hyperthyroidism with high probability, including all three hyperthyroid patients diagnosed later by the physician. Further detailed analysis of the routine test parameters that were important for classification found that screening with a set of three parameters (alkaline phosphatase, serum creatinine and total cholesterol) or plus aspartate aminotransferase allowed for quite accurate screening. These results showed that the same neural networks as previous work allows simple screening of patients for hyperthyroidism on the basis of routine test data, and that physicians not specializing in the thyroid can rapidly identify individuals suspected of having hyperthyroidism, to permit a rapid referral for examination and treatment by thyroid specialists.View full abstractDownload PDF (2153K) -
Tadashi Shiraiwa, Yuka Kawashima, Atsushi Ikaritani, Yumiko Suganuma, ...2006 Volume 54 Issue 8 Pages 1170-1174
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSTo obtain optically active threo-2-amino-3-hydroxy-3-phenylpropanoic acid (1) via optical resolutions by replacing and preferential crystallization, the racemic structure of (2RS,3SR)-1 hydrochloride [(2RS,3SR)-1·HCl] was examined based on the melting point, solubility, and infrared spectrum. (2RS,3SR)-1·HCl was indicated to exist as a conglomerate at room temperature, although it forms a racemic compound at the melting point. When, in optical resolution by replacing crystallization, L-phenylalanine methyl ester hydrochloride (L-2) was used as the optically active co-solute, (2R,3S)-1·HCl was preferentially crystallized from the supersaturated racemic solution; the use of D-2 as the co-solute afforded (2S,3R)-1·HCl with an optical purity of 95%. In addition, optical resolution by preferential crystallization was successfully achieved to give successively (2R,3S)- and (2S,3R)-1·HCl with optical purities of 90—92%. The (2R,3S)- and (2S,3R)-1·HCl purified by recrystallization from 1-propanol were treated with triethylamine in methanol to give optically pure (2R,3S)- and (2S,3R)-1.View full abstractDownload PDF (123K) -
Muhammad Zia-ur-Rehman, Jamil Anwar Choudary, Saeed Ahmad, Hamid Latif ...2006 Volume 54 Issue 8 Pages 1175-1178
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSA series of potential biologically active 2-(4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)quinazolin-4(3H)-ones was synthesized in a straight forward manner by condensation of respective 4-hydroxy-1,2-benzothiazine-1,1-dioxides with anthranilamide followed by simple and high throughput cyclization of N-[2-(aminocarbonyl)phenyl]-4-hydroxy-1,2-benzothiazine-3-carboxamide-1,1-dioxides. All the synthesized compounds were subjected to preliminary evaluation for their biological activity against Gram positive and Gram negative bacteria. Some of the assayed compounds showed marked activity against Bacillus subtilis.View full abstractDownload PDF (93K) -
Guangsheng Qian, Sik-Yuen Leung, GuangHua Lu, Kelvin Sze-Yin Leung2006 Volume 54 Issue 8 Pages 1179-1186
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSAn HPLC-DAD fingerprinting profile of Rhizoma Et Radix Polygoni Cuspidati was established basing on the consistent chromatographic features of 24 authentic herb samples. The major types of chemical constituents, stilbenes and anthraquinones, were analyzed and included in the fingerprint. Eight common peaks of Polygonum Cuspidatum were identified by using HPLC-MS. The developed fingerprint was applied to differentiate Rhizoma Et Radix Polygoni Cuspidati from Radix Polygoni Multiflori and Radix Et Rhizoma Rhei. Although the three herbs belong to the family of Polygonaceae, the results indicated that these could be differentiated by using the established method.View full abstractDownload PDF (1009K)
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Stefano Dall'Acqua, Giampietro Viola, Michela Giorgetti, Maria Cecilia ...2006 Volume 54 Issue 8 Pages 1187-1189
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSAs a part of our ongoing interest in new bioactive compounds from natural sources, we studied Laurus nobilis (Lauraceae). This plant is widespread in the Mediterranean area and is used for medicinal and economic purposes. Chromatographic separations on active extracts led to the isolation of two new sesquiterpene lactones, 5a,9-dimethyl-3-methylene-3,3a,4,5,5a,6,7,8-octahydro-1-oxacyclopenta[c]azulen-2-one (1) and 3β-chlorodehydrocostuslactone (2). The structures of the new compounds were identified by 1D and 2D NMR experiments, as well as high resolution mass spectrometry. The cytotoxic activity was also evaluated against three different tumor cell lines of human origin.View full abstractDownload PDF (85K) -
Nai Li Wang, Jue Wang, Xin Sheng Yao, Susumu Kitanaka2006 Volume 54 Issue 8 Pages 1190-1192
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSTwo new neolignan glucosides, bidenlignasides A (1) and B (2), were isolated from the whole plant of Bidens parviflora WILLD. The structures of the two new compounds 1 and 2 established to be 3-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-3-[5E-(3-hydroxypropenyl)-3-methoxy-2-O-β-D-glucosyl)phenyl] propan-1-one and 3-{3-[1,3-dihydroxy-3-(4-hydroxy-3-methoxyphenyl)propyl]-4-hydroxy-5-methoxyphenyl}-allyl-O-β-D-glucuside, respectively, on the basis of spectral and chemical evidence. Compounds 1 and 2 were found to inhibit histamine release from peritoneal exudate mast cells induced by antigen-antibody reaction.View full abstractDownload PDF (81K) -
Muchchintala Maheswara, Vidavalur Siddaiah, Chunduri Venkata Rao2006 Volume 54 Issue 8 Pages 1193-1195
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSTwo new homoisoflavonoids, (E)-7-methoxy-3-(4′-methoxybenzylidene)chroman-4-one (1) and (E)-7-hydroxy-3-(3′,4′,5′-trimethoxybenzylidene)chroman-4-one (5), along with three known homoisoflavonoids (Z)-7-hydroxy-3-(4′-methoxybenzylidene)chroman-4-one (isobon ducellin) (2), (E)-7-hydroxy-3-(4′-methoxybenzylidene)chroman-4-one (bonducellin) (3) and (E)-7-hydroxy-3-(2′,4′-dimethoxybenzylidene)chroman-4-one (4) were isolated from the whole plant of Caesalpinia pulcherrima. The structures of these new compounds were elucidated by electron impact mass spectrometry (EI-MS) and 1D and 2D-NMR spectral studies. Antimicrobial activity of the new compounds was evaluated.View full abstractDownload PDF (97K) -
Etsuko Ichikawa, Michio Kimura, Hiromi Mori, Futoshi Yamazaki, Kazuyuk ...2006 Volume 54 Issue 8 Pages 1196-1199
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSThe peak area of insulin in a mixture of K.C.L.® injection and hyperalimentation fluid was found to increase in a time dependent manner up to 24 h in measurement by a high-performance liquid chromatograph. The increase of peak area corresponding to the insulin was detected at wavelengths of both 210 and 280 nm. This increase was only observed in the presence of the sugars, tryptophan, riboflavin, and insulin, and ascorbate was shown to counteract the increase. These results suggest the possibility that insulin forms a mixture caused by the oxidation reaction in a hyperalimentation fluid.View full abstractDownload PDF (124K) -
Jian-Guang Luo, Ling-Yi Kong, Yoshiaki Takaya, Masatake Niwa2006 Volume 54 Issue 8 Pages 1200-1202
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSTwo new monodesmosidic triterpene saponins were isolated from the roots of Gypsophila oldhamiana (Caryophyllaceae). Their structures were elucidated on the basis of spectral data to be quillaic acid, α-L-arabinopyranosyl-(1→4)-α-L-arabinopyranosyl-(1→3)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-β-D-fucopyranosyl ester (1), and vaccaric acid, β-D-glucopyranosyl-(1→3)-[β-D-xylopyranosyl-(1→4)]-α-L-rhamnopyranosyl-(1→2)-β-D-fucopyranosyl ester (2). Compound 1 showed a significant enhancement of granulocyte phagocytosis in vitro.View full abstractDownload PDF (113K) -
Ding-Wa Zhang, Zheng-Yin Yang, Bao-Dui Wang, Shi-Ping Zhang, Ru-Dong Y ...2006 Volume 54 Issue 8 Pages 1203-1206
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSA novel ligand, diethylenetriamine-N,N″-bis(acetyl-isoniazid)-N,N′,N″-triacetic acid (H3L) has been synthesized from diethylene triamine pentaacetic acid (DTPA) and isoniazid. Ligand and its five neutral rare earth (RE=La, Sm, Eu, Gd, Tb) complexes holding promise of magnetic resonance imaging (MRI) were characterized on the basis of elemental analysis, molar conductivity, 1H-NMR spectrum, FAB-MS, TG-DTA analysis and IR spectrum. The relaxivity (R1) of complexes and Gd(DTPA)2− used as a control were determined. The relaxivity of LaL, SmL, EuL, GdL, TbL and Gd(DTPA)2− were 0.14, 1.66, 3.14, 6.08, 2.79 and 4.34 l·mmol−1·s−1, respectively. The spin-lattice relaxivity of GdL was larger than that of Gd(DTPA)2−. The relaxivity of GdL had also been investigated in human serum albumin (HSA) solution, the relaxivity of GdL was enhanced from 6.08 l·mmol−1·s−1 in water solution to 9.09 l·mmol−1·s−1 in HSA solution. In addition, thermodynamics stability constant of GdL complex was determined, the thermodynamic stability constant of GdL complex (KGdL=1020.84) was a few larger than that of Gd(DTPA)2− (KGd-DTPA=1020.73). The results showed that complex of GdL may be a prospective MRI contrast agent with low osmotic pressure due to non-ion complex, high spin-lattice relaxivity, good stability and binding affinity for the serum protein.View full abstractDownload PDF (200K) -
Tamaki Miyazaki, Sumie Yoshioka, Yukio Aso2006 Volume 54 Issue 8 Pages 1207-1210
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSCrystallization rates of drug-polymer solid dispersions prepared with acetaminophen (ACA) and p-aminoacetanilide (AAA) as model drugs, and polyvinylpyrrolidone and polyacrylic acid (PAA) as model polymers were measured in order to further examine the significance of drug–polymer interactions. The crystallization of AAA and ACA was inhibited by mixing those polymers. The most effective inhibition was observed with solid dispersions of AAA and PAA. The combination of AAA and PAA showed a markedly longer enthalpy relaxation time relative to drug alone as well as a higher Tg than predicted by the Gordon–Taylor equation, indicating the existence of a strong interaction between the two components. These observations suggest that crystallization is effectively inhibited by combinations of drug and polymer that show a strong intermolecular interaction due to proton transfer between acidic and basic functional groups.View full abstractDownload PDF (210K) -
Kun Zou, Yu-Ying Zhao, Ru-Yi Zhang2006 Volume 54 Issue 8 Pages 1211-1212
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSA new triterpenoidal saponin (1: Julibroside J21) with a xylopyranosyl moiety located at its C-21 side chain was isolated from Albizia julibrissin DURAZZ. (Leguminosae), and its structure was determined on the basis of comprehensive spectroscopic analyses. Compound 1 showed marked inhibitory action against Bel-7402 cancer cell line at 10 μg/ml.View full abstractDownload PDF (74K) -
Yoshiaki Amakura, Kazunari Kondo, Hiroshi Akiyama, Hideyuki Ito, Tsuto ...2006 Volume 54 Issue 8 Pages 1213-1215
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSThree novel conjugated long-chain fatty acids (1—3) were obtained from aqueous methanol extracts of Pleurocybella porrigens together with nine known constituents including (8E,10E)-7,12-dioxo-8,10-octadecadienoic acid (ostopanic acid) (4). The structures of the new fatty acids were characterized as (14RS)-(10E,12E)-14-hydroxy-9-oxo-10,12-octadecadienoic acid (1), (12RS)-(8E,10E)-12-hydroxy-7-oxo-8,10-octadecadienoic acid (2), and (10E,12E)-9,14-dioxo-10,12-octadecadienoic acid (3) by spectroscopic methods.View full abstractDownload PDF (71K) -
Jue Wang, Keiichi Matsuzaki, Susumu Kitanaka2006 Volume 54 Issue 8 Pages 1216-1218
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSEthyl acetate extract of Pholidota chinensis L. showed strong NO production inhibitory activity in murine macrophage-like cell line, RAW 264.7, which was activated by a lipopolysaccharide (LPS) and interferon-γ (IFN-γ). Fractionation of the active extract led to the isolation of two new stilbene derivatives, 2,3′-dihydroxy-5-methoxy-3,4-methylenedioxydihydrostilbene (Pholidotol A) and 2-hydroxy-5-methoxy-3,4,3′,4′-dimethylenedioxydihydrostilbene (Pholidotol B) together with six known stilbene derivatives. Pholidotols A both B and inhibited Nitric oxide (NO) production with an IC50 value at 24.3 and 17.1 μM, respectively.View full abstractDownload PDF (108K) -
Yoshiyasu Fukuyama, Momoko Nakaoka, Tomoko Yamamoto, Hironobu Takahash ...2006 Volume 54 Issue 8 Pages 1219-1222
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSBrine shrimp lethality test (BST)-guided fractionation of a methanol extract of the roots of Melia azedarach resulted in the isolation of two new limonoids, 9α-hydroxy-12α-acetoxyfraxinellone (1) and 7,14-epoxy-azedarachin B (2), together with the known compounds, 12α-hydroxyfraxinellone (4), 9α-hydroxyfraxinellone (5), azedarachin B (6), and neoazedarachin B (7). The structures of 1 and 2 were elucidated by analysis of spectroscopic data and comparison of their NMR data with those of the known compounds. Compounds 1, 2 and 4—7 exhibited significant activity in the BST, in particular, azedarachin B (6) showed remarkable BST activity with an LC50 value of 0.0098 μM.View full abstractDownload PDF (148K) -
Shwu-Jen Wu, Tian-Shung Wu2006 Volume 54 Issue 8 Pages 1223-1225
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSThree new arylnaphthalene lignans, namely phyllanthusmins A—C, together with nine known compounds were isolated and characterized from the stems and roots of Phyllanthus oligospermus by a bioassay-guided purification. The structures of the new compounds were elucidated by means of spectroscopic data interpretation. Among them, phyllanthusminA displayed significant cytotoxicity against KB and P-388 cancer cell lines.View full abstractDownload PDF (119K) -
Trypanocidal Constituents in Plants 6. Minor Withanolides from the Aerial Parts of Physalis angulataFumiko Abe, Shinya Nagafuji, Masafumi Okawa, Junei Kinjo2006 Volume 54 Issue 8 Pages 1226-1228
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSFurther study of the methanol extract of the aerial parts of Physalis angulata (Solanaceae) resulted in the isolation of new withanolides, designated physagulins L, M and N, together with known withanolide, physagulin D and flavonol glycoside, quercetin 3-O-rhamnosyl-(1→6)-galactoside. The chemical structures of these new withanolides were elucidated by detailed spectroscopic analyses to be (20R,22R)-15α-acetoxy-5α,6β,14β,17β,27-pentahydroxy-1-oxo-witha-2, 24-dienolide, (20S,22S)-15α-acetoxy-5α,6β,14α,23β-tetrahydroxy-1-oxo-witha-2,16,24-trienolide and (20S,22R)-15α-acetoxy-5β,6β-epoxy-14α-hydoxy-3β-methoxy-1-oxo-witha-16,24-dienolide, respectively. All these compounds showed weak trypanocidal activity against trypomastigotes, an infectious form of Trypanosoma cruzi, the etiologic agent for Chagas' disease. Withanolides obtained in the previous paper showed considerable trypanocidal activity, suggesting the structure–activity relationships.View full abstractDownload PDF (80K) -
Guizhi Ma, Wei Li, Deqiang Dou, Xiaolong Chang, Hong Bai, Tadaaki Sato ...2006 Volume 54 Issue 8 Pages 1229-1233
Published: 2006
Released on J-STAGE: August 01, 2006
JOURNAL FREE ACCESSFive new monoterpene glycosides, rhodiolosides A—E (1—5), were isolated from the roots of Rhodiola rosea (Crassulaceae). Their structures were elucidated as (2E,6E,4R)-4,8-dihydroxy-3,7-dimethyl-2,6-octadienyl β-D-glucopyranoside (1), (2E,4R)-4-hydroxy-3,7-dimethyl-2,6-octadienyl α-D-glucopyranosyl(1→6)-β-D-glucopyranoside (2), (2E,4R)-4-hydroxy-3,7-dimethyl-2,6-octadienyl β-D-glucopyranosyl(1→3)-β-D-glucopyranoside (3), (2E,4R)-4,7-dihydroxy-3,7-dimethyl-2-octenyl β-D-glucopyranoside (4), and (2E)-7-hydroxy-3,7-dimethyl-2-octenyl α-L-arabinopyranosyl(1→6)-β-D-glucopyranoside (5), on the basis of various spectroscopic analyses and chemical degradation.View full abstractDownload PDF (133K)
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