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Volume 59, Issue 5
Displaying 1-24 of 24 articles from this issue
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Regular Articles
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Jun Sang Park, Ji Yeon Shim, Jung Soo Park, Myung Jae Lee, Jong Min Ka ...Article type: Regular Article
2011 Volume 59 Issue 5 Pages 529-535
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSIn order to develop a preferable once-a-day oral tablet formulation, various formulations of three-layered tablets containing tamsulosin HCl as a hydrophilic model drug were evaluated and compared with a commercial reference, tamsulosin OCAS®. When the test tablet was exposed to a release medium, the medium quickly permeated to the mid-layer and the two barrier layers swelled surrounding the mid-layer rapidly. Volume expansion showed faster and enough swelling of the three-layered tablet up to 2 h. Larger amount of barrier layers caused reduced release kinetics and a high molecular weight polymer showed more resistance against agitation force. A formulation with water-soluble mid-layer showed fast erosion decreasing its volume significantly. On the pharmacokinetic study, the mean ratio of area under the curve (AUC) and Cmax for the test formulation to the reference was 0.69 and 0.84, respectively, showing that the absorption of the drug was less complete than the reference. Plasma concentration at 24 h of the test formulation was higher than the reference. The Wagner–Nelson method showed that decreased initial dissolution rate might be the cause of the less complete absorption. On considering in vitro–in vivo correlation (IVIVC), level A, the reference (R2=0.981) showed more linear relationship than the test (R2=0.918) due to the decreased dissolution and absorption rate of the formulation. This result suggests that the in vitro dissolution profiles and release kinetics might be useful in correlating absorption kinetics as well as overall plasma drug concentration–time profiles for formulation studies.View full abstractDownload PDF (853K) -
Tamami Haraguchi, Miyako Yoshida, Mai Hazekawa, Takahiro UchidaArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 536-540
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSAminoleban® EN, a nutritional product for patients with liver failure, contains three branched-chain amino acids (BCAAs): L-leucine, L-isoleucine, and L-valine. As BCAAs are extremely bitter, Aminoleban® EN has a low palatability, which is a major cause of patient noncompliance. Nutrients for liver failure often need to be taken for long periods, and poor medication compliance can cause serious problems, such as encephalopathy. Therefore it is important to suppress the bitter taste of Aminoleban® EN and thereby improve patient compliance. There are already six different flavoured powders (coffee, green-tea, apple, fruit, plum and pineapple) which can be added to Aminoleban® EN to reduce its unpleasant taste and smell, but it is possible that other factors, such as temperature, may also improve the palatability of Aminoleban® EN. In this study, flavours alone significantly decreased the bitterness intensity of Aminoleban® EN. It was thought that the sweetness and sourness of the flavoured powder would be the main factors involved in decreasing the bitterness. However, low temperature (0—5 °C) decreased the bitterness intensity of Aminoleban® EN, with or without the flavoured powders, compared with normal room temperature (25—30 °C). The sourness intensity of flavoured powders was not decreased at low temperatures, but the sweetness intensity of some flavoured powders did decrease. These results suggest that sourness can be tasted even at low temperatures. As not only the addition of flavoured powders but also low temperatures can reduce the bitterness of Aminioleban® EN, the combination of a sour-flavoured powder and a low temperature will improve the palatability of Aminoleban® EN the most.View full abstractDownload PDF (841K) -
Cui-Ling Zhang, Xiao-Ping Ding, Zheng-Fang Hu, Xin-Tang Wang, Lin-Lin ...Article type: Regular Article
2011 Volume 59 Issue 5 Pages 541-545
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSAn on-line HPLC-diode array detection-flow injection chemiluminescence (HPLC-DAD-FICL) method was applied to estimate the difference of Puerariae lobatae and Puerariae thomsonii. Their chemical and active profiles could be obtained by HPLC-DAD-FICL in one run. Seventeen compounds in two species were tentatively identified by HPLC-electrospray ionization-MS (HPLC-ESI-MS) method. The main antioxidants were rapidly screened by active fingerprints coupled with MS data. Similarity and Hierarchical clustering analysis (HCA) were used to distinguish different samples. The results suggested that the chemical fingerprints of 16 batches of samples were similar by similarity evaluation, while HCA could discriminate the two species. The active fingerprints of Puerariae lobatae and Puerariae thomsonii were significantly different. More antioxidants were found in Puerariae lobatae than in Puerariae thomsonii. Main antioxidants, including 3′-hydroxypuerarin, genistein 8-C-glycoside-xyloside, puerarin, 6″-O-xylosylpuerarin, mirificin and daidzein in two species, may be reasonable markers for the discrimination of the two species. The integrated fingerprint based on the chemical and active characteristics may provide an objective quality evaluation for Puerariae lobatae and Puerariae thomsonii.View full abstractDownload PDF (805K) -
Wen-Te Chang, Young Hae Choi, Rob Van der Heijden, Meng-Shiou Lee, Min ...Article type: Regular Article
2011 Volume 59 Issue 5 Pages 546-552
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSThe processing of biological raw materials is considered to have an important role in the therapeutic application in Traditional Chinese Medicine. The root of Rehmannia glutinosa has to be processed by nine cycles of rice wine immersing, steaming and drying before using in clinical applications. In order to understand the chemical changes resulting from the processing, a comprehensive analysis of Rehmanniae radix was made using 1H-NMR and Fourier transform (FT)-mass spectrometry in combination with multivariate data analysis. After 1H-NMR and principle component analysis, hydrolysis was found to be the major chemical process during the treatments. Catalpol, raffinose and stachyose levels gradually decreased during processing, whereas monosaccharides including galactose and glucose were found to be higher in processed roots. The metabolic profile changed gradually through the processing cycles although the differences became smaller after the fifth processing cycle. The positive and negative ion-mode mass spectra by high resolution FT-MS revealed several series of ion clusters with mass differences of 162.053 Da, indicating a difference of a hexose moiety. During the processing, the number and signal intensity of the smaller glycosides were increased. Therefore, these results indicate that the fresh Rehmanniae radix is rich in polysaccharides, which are hydrolyzed during the processing.View full abstractDownload PDF (707K) -
Sadahiro Fujiki, Yasunori Iwao, Mika Kobayashi, Atsuo Miyagishima, Shi ...Article type: Regular Article
2011 Volume 59 Issue 5 Pages 553-558
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSIt has been reported that tablets of clarithromycin (CAM), a 14-membered macrolide antibiotic, are especially stable under low pH conditions such as in gastric fluid, and showed excellent antibacterial efficiency even though CAM molecules themselves are rapidly decomposed. Therefore, we aimed to clarify the stabilization mechanism of CAM tablets under low pH conditions. From the results of stability and dissolution tests, the optimal decomposition rate constant (Kdec) and dissolution rate constant (Kdis) at various pH values were calculated by curve-fitting to consecutive reactions. Consequently, log(Kdec) increased as pH decreased. On the other hand, log(Kdis) increased as pH decreased from 3.0 to 1.5, but decreased as pH decreased from 1.5 to 1.0. In addition, the disintegration time of commercially available tablets at pH 1.0 and 1.2 was found to be delayed, resulting in a decrease of Kdis. Furthermore, from powder X-ray diffraction, HPLC and elemental analysis, the delay in disintegration time might be attributable to the formation of a transparent gel, formed by the reaction between CAM molecule and hydrochloric acid under low pH conditions, on the surface of CAM tablet. On the basis of these results, this report can be considered the first case where a transparent gel prevents gastric fluid from penetrating the tablet, resulting in reduced decomposition of CAM following oral administrating.View full abstractDownload PDF (1732K) -
Liping An, Yapei Wang, Xiaomei Liu, Ning Ma, Haiying Du, Minghua Jin, ...Article type: Regular Article
2011 Volume 59 Issue 5 Pages 559-563
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSA novel block ionomer complex micelles as drug carrier is developed utilizing self-assemble of poly(ethylene glycol)-block-poly(acrylic acid) (PEG-b-PAA) and cadmium chloride. This micelles are characterized to be have good bio-compatibility, hydrophilicity, passive targeting and sustained slow release property which shows great potential for liver cancer therapy. Block ionomer complex micelles based on PEG-b-PAA and cadmium chloride can self-assemble in distilled water, and Cd2+ agent is entrapped into the core stabilized by PEG shells. Results showed the block ionomer complex micelles to be spherically shaped. Cadmium was incorporated easily into the ionic core with remarkably high efficiency (34.25% weight (wt)/wt). The cadmium-loaded polymeric micelles exhibited sustained and slow release behavior of cadmium and a potent cytotoxicity against SMMC-7721 in vitro. This novel block ionomer complex micelles with cores of metal antitumor drug indicates to be potential carriers for effective drug delivery.View full abstractDownload PDF (1179K) -
Masaaki Ozawa, Akio Kishida, Ayumi OhsakiArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 564-567
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSFour new Erythrinan alkaloids (1—4) were isolated from the seeds of Erythrina velutina. The structures of these new compounds 1—4 were elucidated by spectroscopic methods including 2D-NMR. Three of four were found to be novel sulfated Erythrinan alkaloids.View full abstractDownload PDF (624K) -
Mohammad Sayed Alam, Lijun Liu, Yong-Eok Lee, Dong-Ung LeeArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 568-573
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSA new series of 2-arylidenehydrazinyl-4-arylthiazole derivatives (2a—k) was designed and synthesized through a rapid, simple, and efficient methodology in excellent isolated yield. These compounds were screened for in vitro antimicrobial activities against eight bacteria, e.g. Bacillus cereus, Staphylococcus aureus, Bacillus subtilis, Bacillus megaterium, Pseudomonas aeruginosa, Shigella dysenteriae, Salmonella typhi, Escherichia coli, and three fungi e.g. Aspergillus oryzae, Candida albicans, and Saccharomyces cerevis. The results indicate that some of the compounds exhibit strong antibacterial activity, depending on the bacterial strain, but show virtually no antifungal activity. The structure–antibacterial activity relationships were studied using some physicochemical and quantum-chemical parameters with the ab initio Hartree–Fock model at the RHF/6-31G level of theory. A good qualitative correlation between predicted lipophilic parameters and antibacterial activity has been found.View full abstractDownload PDF (1326K) -
Jun Chiba, Nobuo MachinagaArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 574-578
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSThis contribution describes a novel synthetic approach to very late antigen-4 (VLA-4) antagonist trans-4-[1-[[2,5-dichloro-4-(1-methyl-3-indolylcarboxyamide)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid (1) via tert-butyl trans-[(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate (2b) as a key intermediate. The synthesis, which includes n-Bu4NSO3H that catalyzed basic etherification of 12 and iodine-mediated cyclization to provide the 2,4-disubstituted pyrrolidine frame of 2b, is designed to utilize trans-4-hydroxycyclohexanecarboxylic acid (9) as a commercially available starting material.View full abstractDownload PDF (681K) -
Naoki Ando, Shiro TerashimaArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 579-596
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSSynthesis of the 37 ageladine A analogs was accomplished by employing the total synthetic route of natural ageladine A previously explored by us. From the matrix metalloproteinase-12 (MMP-12) inhibitory activity assay carried out using the novel analogs, it appeared evident that the halogen atom at the 2-position of pyrrole ring was essential for the inhibitory activity and that the introduction of a bromine atom into the 4-position of pyrrole ring is very effective for producing potent activity. In addition, exchange of the pyrrole ring to an imidazole ring was extremely effective in increasing activity, and the analog 29 thus obtained was found to show approximately 4 times more potent activity than natural ageladine A.View full abstractDownload PDF (1156K) -
Yuki Sato, Mitsuno Shindo, Naoki Sakura, Yoshiki Uchida, Ikuo KatoArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 597-602
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSPolymyxin B (PMB) is a cationic cyclic decapeptide antibiotic with a fatty acyl (FA) modification at the α-amino group of Dab1 (Dab: L-α,γ-diaminobutyric acid). In this study, which is part of a series of PMB structure–activity relationship investigations focused on identifying clinically useful peptide antibiotics, we synthesized ten des-FA PMB derivatives whose N-terminal moieties were changed to basic or hydrophilic amino acids. The antimicrobial and lipopolysaccharide (LPS) binding activities of these synthetic analogs were tested. The analogs showed more potent antimicrobial activity against Pseudomonas aeruginosa (P. aeruginosa) compared with the PMB nonapeptide. In particular, [Ser2-Dap3]-PMB(2—10), Guanyl-[Thr2-Dab3]-PMB(2—10), Guanyl-[Dab1-Thr2-Dab3]-PMB(1—10), and Nα,γ-diguanyl-[Dap3]-PMB(3—10) had antimicrobial activity equivalent to PMB. In LPS binding assays, the displacement curves shifted in a manner proportional to the number of positive charges available to bind to Escherichia coli (E. coli) and P. aeruginosa. Furthermore, peptides with basic side chains were comparable to PMB in binding activity assays against E. coli and P. aeruginosa. The acute toxicities of the peptides were evaluated by intravenously administering the peptides to mice through the tail vein. The toxicities of [Ser2-Dap3]-PMB(2—10), [Dap3]-PMB(3—10), and [Ser3]-PMB(3—10) were lower that of PMB (LD50, 4.8 μmol/kg).View full abstractDownload PDF (807K) -
John Rojas, Alvin López, Yudy Gamboa, Christian González ...Article type: Regular Article
2011 Volume 59 Issue 5 Pages 603-607
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSMicrocrystalline cellulose I (MCCI) is an excipient used as a diluent, disintegrant, glidant and binder for the production of pharmaceutical tablets. In this work, microcrystalline cellulose II (MCCII) was obtained from cotton fibers by basic treatment with 7.5 N NaOH followed by an acid hydrolysis. MCCI and MCCII materials were processed by wet granulation, dry granulation and spray drying. Either the polymorphic form or processing had no effects on the particle morphology or particle size. However, MCCII powders had a higher porosity, less packing tendency, degree of crystallinity, degree of polymerization and density, but a faster disintegration than MCCI. The tensile strength of MCCI was highly affected by the wet and dry granulation processes. Most of the resulting powder and tableting properties were dependent on the polymorphic form of cellulose, rather than on the processing employed.View full abstractDownload PDF (1271K) -
Hiroaki Arai, Tatsuya Suzuki, Shuichi Yada, Chosei Kaseda, Yoshinori O ...Article type: Regular Article
2011 Volume 59 Issue 5 Pages 608-617
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSThe design space of the granulation process of mefenamic acid tablets, based on Box and Behnken design datasets, was described by a response surface method incorporating multivariate spline interpolation. The reliability of the optimal solutions and the acceptance ranges were evaluated by a bootstrap (BS) resampling technique. The distribution of the BS optimal solutions was almost symmetrical; however, several solutions, which were quite different from the original solution, were mixed. The reason for this problem was considered to be the mixing of the global and the local optima. Therefore, we applied self-organizing map (SOM) clustering for dividing data into several clusters and identified the cluster containing the global optima. The accuracy and reproducibility of the optimal solution in the cluster containing the optimal solution were quantitatively evaluated. In addition, the response surfaces modeled from all the BS datasets contained in the cluster were plotted into the same coordinates with the original response surface. The plots of BS optimal solutions were distributed around the original solution. Moreover, the average of all the BS response surfaces sufficiently corresponded with the original response surface. The conservative limits of the 95% confidence intervals of the acceptance ranges in three response variables could be calculated using the standard deviations of the BS response surfaces. Consequently, it was considered that a novel evaluation method based on BS resampling and SOM could be used for quantitatively evaluating the precision of the nonlinear response surface model.View full abstractDownload PDF (9114K) -
KeXin Li, XiuLi Zhao, ShiYi Xu, DaHai Pang, ChunRong Yang, DaWei ChenArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 618-623
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSThe conjugation of Ulex europaeus agglutinin I (UEAI) onto surface of liposomes has been demonstrated to effectively improve the intestinal absorption of antigen, subsequently induced strong mucosal and systemic immune responses. In this context, we prepared bovine serum albumin (BSA)-encapsulating UEAI-modified liposomes (UEAI-LIP) and unmodified ones (LIP). The specific bioadhesion on mice gastro-intestinal mucosa was studied ex vivo. An important increase of interaction between UEAI-conjugated liposomes and the intestinal segments with Peyer's Patches (PPs) was observed compared with the unconjugated one (p<0.01). However, under the presence of α-L-fucose, which is the reported specific sugar for UEAI, specifically inhibited the activity of these conjugates. The immune-stimulating activity in vivo was studied by measuring immunoglobulin G (IgG) levels in serum and immunoglobulin A (IgA) levels in intestinal mucosal secretions following oral administration of BSA solution, LIP and UEAI-LIP in mice. Results indicate that antigen encapsulated in liposomes, especially the UEAI-modified ones, was favorable for inducing immune response. At 42 d after the first immunization, the highest IgG and IgA antibody levels produced by UEAI-LIP occurred, respectively showing 4.4-fold and 5-fold higher levels compared to those of the groups receiving BSA alone. This data demonstrated high potential of UEAI-modified liposomes for their use as carrier for oral vaccines.View full abstractDownload PDF (667K) -
Keizo Takeshita, Shoko Okazaki, Hisao KansuiArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 624-628
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSPerchlorotriphenylmethyl triethylester radical (PTM-TE) is a hydrophobic, stable radical giving a narrow singlet ESR signal with a small satellite signal for 13C in organic solvents. In order to use PTM-TE as a label of liposomal membranes, its manner of incorporation into liposomal membranes was studied. Two components, broad and narrow signals, were observed on the ESR spectrum of PTM-TE incorporated into liposomal membranes composed of egg yolk phosphatidylcholine (egg-PC). The broad signal was increased by the presence of cholesterol in the membranes. The spectral anisotropy of the broad signal was very small as analyzed with oriented planar multilamellar membranes. The narrow signal increased with an increase in temperature in the absence of cholesterol, whereas only a small increase in the signal was observed in the presence of cholesterol. The g-value and line width of the narrow signal were very close to those of PTM-TE in mineral oil, whose viscosity is close to the microviscosity in the hydrophobic region of egg-PC membranes. On the other hand, the g-value and line width of the broad signal were close to those of solid PTM-TE. These observations indicate that the broad signal observed in liposomes originates from PTM-TE clusters in the membranes. The clusters were dissolved in egg-PC membranes at a PTM-TE/egg-PC molar ratio of less than 0.017. However, the clusters were hardly dissolved in the presence of cholesterol.View full abstractDownload PDF (782K) -
Amit Kumar Aggarwal, Shweta JainArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 629-638
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSPurpose: The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug ketoconazole using solid dispersion technique. Methods: Solid dispersions of ketoconazole were prepared in ratios of 90 : 10, 70 : 30, 50 : 50, 30 : 70 and 10 : 90 by the melting method using nicotinamide as carrier. These solid dispersions were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (XRD) and Fourier transform infrared (FT-IR) spectroscopy to ascertain if there were any physicochemical interactions between drug and carrier that could affect dissolution. Solubility and dissolution studies were conducted with pure ketoconazole, physical mixtures and solid dispersions. Results: Solubility studies indicated that nicotinamide increased significantly the solubility of ketoconazole in water. The Gibbs free energy (ΔG°tr) values were negative indicating the spontaneous nature of ketoconazole solubilization, and it decreased with increase in concentration of the carrier, demonstrating that the reaction became more favorable as the concentration of the carrier increased. The cumulative release of ketoconazole within 120 min from solid dispersion at a drug-to-nicotinamide ratio of 10 : 90 (w/w) was 6 times higher than the pure drug in phosphate buffer of pH 6.8. Conclusion: Solid state characterization indicated that there is no interaction between ketoconazole and nicotinamide in the solid state. In contrast to the very slow dissolution rate of pure ketoconazole, the dispersion of the drug in nicotinamide considerably enhanced the dissolution rate. The drug dissolution rate was highest at a drug-to-nicotinamide ratio of 10 : 90 (w/w).View full abstractDownload PDF (1390K) -
Vishal Kumar, Upendra Sharma, Praveen Kumar Verma, Neeraj Kumar, Bikra ...Article type: Regular Article
2011 Volume 59 Issue 5 Pages 639-645
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSA rapid and efficient silica-supported boric acid/ionic liquid ([bmim][PF6]), catalyzed, one-pot three-component Mannich reaction has been carried out to synthesize β-amino carbonyl compounds at room temperature. The reaction afforded desired products in excellent yields with moderate to good diastereoselectivity. The method provides a novel modification of three-component Mannich reaction in terms of mild reaction conditions, clean reaction profiles, low amount of catalyst, recyclability of catalyst and a simple workup procedure. The present report first time describes the preparation of H3BO3–SiO2 catalyst and its use with [bmim][PF6], to synthesize Mannich products. The catalyst can be reused at least seven times.View full abstractDownload PDF (644K) -
Mitali Kakran, Nanda Gopal Sahoo, Lin Li, Zaher JudehArticle type: Regular Article
2011 Volume 59 Issue 5 Pages 646-652
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSThe main objective of this research is to improve the dissolution rate of artemisinin (ART) by fabrication with β-cyclodextrin (β-CD) as a hydrophilic carrier. Artemisinin nanoparticles and ART/β-CD complexes were successfully fabricated by means of evaporative precipitation of nanosuspension. Characterization of the samples was done by scanning electron microscopy (SEM), Fourier transform infrared (FT-IR), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and dissolution tester. Percent dissolution efficiency, mean dissolution time, relative dissolution and similarity factor were calculated for the statistical analysis of dissolution data. FT-IR showed some interaction between ART and β-CD, which can be due to the formation of some ART/β-CD complexes. XRD study indicated the presence of two polymorphs of ART, i.e. orthorhombic and triclinic form. Original ART particles and ART nanoparticles fabricated were orthorhombic whereas the free ART in the ART/β-CD complexes (not forming complex with β-CD) was of triclinic form. The crystallinity of ART reduced and more and more ART/β-CD complexes were formed with increasing concentration of β-CD as indicated by the DSC, XRD and FT-IR studies. Artemisinin nanoparticles and ART/β-CD complexes showed significantly faster dissolution than the pure drug due to smaller size (larger surface area), formation of the inclusion complex with β-CD, formation of the triclinic form for remaining free ART (not forming complex with β-CD), and amorphous state formation. Evaporative precipitation of nanosuspension was able to successfully fabricate artemisinin in the nanoparticles and complex forms with significantly faster dissolution rates than that of the original artemisinin. The two polymorphic forms of ART were also fabricated and studied.View full abstractDownload PDF (1709K)
Notes
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Shuang Liang, Jun-Mian Tian, Yi Feng, Xiao-Hua Liu, Zhi Xiong, Wei-Don ...Article type: Note
2011 Volume 59 Issue 5 Pages 653-656
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSChemical examination of the methanolic extract from the stem bark of Daphne aurantiaca led to the isolation of three new flavonoids (1—3), and 29 known flavonoids. All 32 compounds were isolated for the first time from Daphne aurantiaca. The isolates were tested for inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 macrophages. Compounds 21 and 24 showed potent inhibitory activities against the production of NO with IC50 values of 0.006 and 0.076 μM, respectively.View full abstractDownload PDF (559K) -
Takashi Ohgita, Takashi Okuno, Susumu Hama, Hiroyuki Tsuchiya, Kentaro ...Article type: Note
2011 Volume 59 Issue 5 Pages 657-661
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSATP-dependent proteases unfold their substrates and then refold (via chaperone activity) or degrade (via protease activity) them. The proteases choose between these two activities by selecting their substrates; however, little is known about their substrate selection mechanism. The present study attempts to clarify this mechanism by investigating the role of the Escherichia coli (E. coli) ATP-dependent protease ClpAP. To address this, a reaction system that can measure both chaperone and protease activities simultaneously must be constructed. However, the chaperone activities cannot be evaluated in the presence of protease units. Green fluorescent protein (GFP) is usually used as a model substrate of ClpAP; the fluorescence decrease reflects the degradation of substrates. However, it is difficult to evaluate the chaperone activity of ClpAP using this system, because it cannot distinguish between intact and refolded substrates. Therefore, it is necessary to evaluate the exact unfolding activity while avoiding restoration of substrate spectroscopic characteristics due to chaperone activity. In this study, E. coli Ferredoxin (Fd) was used as a new model substrate for ClpAP to evaluate its unfolding activity. Intact and refolded substrates may be distinguished by the existence of an Fd Fe–S cluster. To verify this hypothesis, the absorption spectrum of Fd complexed with ClpA, the chaperone unit of ClpAP, was measured. A decrease in two peaks derived from the Fe–S cluster was observed, indicating that the Fe–S cluster of Fd was disrupted by the ClpA chaperone. This reaction system should prove useful to evaluate the exact unfolding activity of ATP-dependent proteases.View full abstractDownload PDF (846K) -
Masaki Uchida, Hideshi Natsume, Toshinobu Seki, Tateki Uchida, Yasunor ...Article type: Note
2011 Volume 59 Issue 5 Pages 662-665
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSRecently, it has been suggested that a microparticulate bombardment system would be a very useful tool for the delivery of a variety of powdered drugs as an alternative to parenteral injection via a needle. However the relationship between the particle dynamics and introduction into the skin has not been researched using this system. In the present study, we analyzed the velocity of microparticles bombarded by the HeliosTM gun system under various conditions using particle image velocimetry (PIV). The particle kinetic energy, which depended on the particle velocity and particle mass, was increased with increasing helium pressure and particle size, decreasing bombardment dose, resulting in the increased percentage introduction and relative bioavailability (F0—24 h). The particle velocity had a greater influence than the particle mass. Therefore, in order to be the most effective system for introduction into the skin, it is necessary to use a high helium pressure and microparticles of high density. However, it is also necessary to consider the skin damage after bombardment.View full abstractDownload PDF (603K) -
Qingbin Wu, Yan Wang, Meili GuoArticle type: Note
2011 Volume 59 Issue 5 Pages 666-671
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSThree new triterpenoid saponins, named celosin E (1), celosin F (2) and celosin G (3), together with a known compound cristatain (4), were isolated from the seeds of Celosia argentea L. (Amaranthaceae). All the isolated compounds were obtained for the first time from this plant. The structures of new compounds were characterized on the basis of extensive NMR experiments and mass spectrometry data. The antitumor and anti-inflammatory activities of the four compounds were tested in vitro.View full abstractDownload PDF (808K) -
Ai Ogawa, Yusaku Miyamae, Atsushi Honma, Tomoyuki Koyama, Kazunaga Yaz ...Article type: Note
2011 Volume 59 Issue 5 Pages 672-675
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSA new compound, pycnalin (1), together with four known compounds, ginnalins A (2), B (3), C (4), and 3,6-di-O-galloyl-1,5-anhydro-D-glucitol (3,6-di-GAG) (5), were isolated from Acer pycnanthum. The structure of 1 was determined on the basis of 2D-NMR spectral data and synthesis of 1. Pycnalin (1) is the first 1,5-anhydro-D-mannitol linked to a gallic acid, while compounds 2—5 were 1,5-anhydro-D-glucitol linked to gallic acids. All compounds were tested in vitro for α-glucosidase inhibitory and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities. Pycnalin (1) exhibited moderate α-glucosidase inhibitory activity as well as free radical scavenging activity. Ginnalin A (2) and 3,6-di-GAG (5), which have two galloyl groups, exhibited potent α-glucosidase inhibition, compared to those of other compounds 1, 3, and 4 containing a galloyl group. These results suggest that α-glucosidase inhibition is influenced by the number of galloyl groups.View full abstractDownload PDF (756K) -
Wei-Hua Huang, Qing-Wen Zhang, Lan-Zhen Meng, Chun-Su Yuan, Chong-Zhi ...Article type: Note
2011 Volume 59 Issue 5 Pages 676-679
Published: May 01, 2011
Released on J-STAGE: May 01, 2011
JOURNAL FREE ACCESSThree new phenolic glycosides, named oplopanphesides A—C (1—3), have been isolated from the root barks of Oplopanax horridus. Their structures were elucidated by a combination of spectroscopic analyses, including 1D- and 2D-NMR techniques. These phenolic glycosides possess a novel feature in their sugar moieties that a 3-hydroxy-3-methylglutaryl moiety was connected with C-6 of the β-D-glucopyranosyl group. Those compounds showed no cytotoxic effects against human cancer cell lines (MDA-231 and MCF-7) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method.View full abstractDownload PDF (647K)
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