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Shivsagar Ashok Randale, Chandu Somatbhai Dabhi, Avinash Ramrao Tekade ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
443-448
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
JOURNAL
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The purpose of this study was to mask the intensely bitter taste of metoclopramide HCl and to formulate a rapid disintegrating tablet (RDT) of the taste-masked drug. Taste masking was done by complexing metoclopramide HCl with aminoalkyl methacrylate copolymer (Eudragit
® EPO) in different ratio by the extrusion–precipitation method. Drug–polymer complexes (DPCs) were tested for drug content,
in vitro taste in simulated salivary fluid (SSF) of pH 6.8, taste evaluation in oral cavity and molecular property. The complex having drug–polymer ratio of 1 : 2 shows significant taste masking, confirmed by drug release in SSF and
in-vivo taste evaluation; therefore, it was selected for further study. Taste evaluation of DPCs in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value (0.5) within 10 s, whereas, metoclopramide HCl was rated intensely bitter with a score of +3 for 10 s. Tablets were evaluated for various parameters like tensile strength, wetting time, water absorption ratio,
in-vitro disintegration time, and disintegration in oral cavity. The effect of diluents, lubricants and sweetening agent (Xylisorb) on the disintegration time was also evaluated. Tablets of batch F3 containing mannitol and microcrystalline cellulose in the ratio 1 : 1 and 8% w/w crosspovidone showed faster disintegration (within 20 s) than the marketed formulation (180 s). Good correlation between
in vitro disintegration behavior and in the oral cavity was recognized. Tablets of batch F3 also revealed rapid drug release (
t90, 90 s) in SGF compared with marketed formulation (
t90, 600 s).
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Miyako Yoshida, Emi Tokuyama, Mai Hazekawa, Takahiro Uchida
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
449-453
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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The purpose of this study was to evaluate the effect of various flavoured jellies on the palatability and bitterness of the Kampo medicine ‘Orengedokuto’, using human gustatory sensation testing. In the gustatory sensation test, eight items were evaluated according to the semantic differential (SD) method and four taste intensities (sweetness, astringency, sourness, and bitterness) were determined. Factor analysis of the results identified two main factors ‘Disagreeable taste’ and ‘Agreeable taste and odour’ as predominantly determining the palatability of Orengedokuto. To investigate the influence of jelly odour, evoked images were obtained for five fundamental tastes after smelling jellies. The inhibitory effect of the jelly odour on the bitterness of Orengedokuto was found to be small. When the influence of the various jellies on the disagreeable taste of Orengedokuto was investigated, the bitterness intensities of Orengedokuto mixed with chocolate or strawberry–chocolate jelly were found to be significantly lower than the bitterness of the control. The bitterness intensity of Orengedokuto was found to be significantly and negatively correlated with sweetness intensity using simple linear regression analysis. These results suggest that the sweetness intensity of various jellies inhibits the bitterness intensity of Orengedokuto.
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Yoko Sakuda, Akihiko Ito, Masanaho Sasatsu, Yoshiharu Machida
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
454-457
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Medicinal carbon (MC) films, which can be taken more easily than other dosage forms, were prepared using sodium carboxymethyl cellulose (CMC), hydroxypropylmethyl cellulose (HPMC) and alginic acid sodium (ALG) as film base materials. Brilliant blue FCF (BB) was used as a model drug. The films containing MC had sufficient strength and disintegration time, but their ability to adsorb BB was clearly inhibited compared to that of MC in powder form. When ALG was used as the film base, the BB adsorption capacity of MC film was approximately 50% of that of MC powder. In an attempt to improve this adsorption ability, two saccharides, sorbitol (SOR) and maltitol (MT), were separately added to MC at a mixing ratio of 1 : 1 by weight. When ALG was the film base, MC films containing SOR or MT showed rapid adsorption profiles and had greatly increased capacities for BB adsorption compared with films containing MC alone. SOR was superior to MT as an additive, though both gave MC-containing films a BB adsorption capacity almost equal to that of MC powder after 24 h, and physical mixtures tended to have better BB adsorption capacities than pre-treatment mixture. In addition, both SOR and MT tended to increase vertical strength of films, but neither additive in either type of mixture had a clear effect on disintegration time. When CMC or HPMC was used as the film base, on the other hand, the addition of SOR or MT caused hardly any improvement in adsorption ability. The above results demonstrate that ALG is useful as a film base material for the preparation of MC films, and that MC films with sufficient strength and adsorption capacities equal to those of MC powders can be produced using a physical mixture of MC and SOR on an ALG base.
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Yukako Ito, Tomohiro Maeda, Keizo Fukushima, Nobuyuki Sugioka, Kanji T ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
458-463
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Ascorbic acid (AA) loaded self-dissolving micropiles (SDMP) were prepared using chondroitin sulfate as the base for the percutaneous administration of AA. AA solution was added to dense solution of chondroitin solution, glue, and array tip, 1.0 cm
2, containing 100 SDMPs of which length was 500 μm and basal diameter was 300 μm, were prepared. Two kinds of AA array tips containing 1344.2±1.7 μg (high content ones) and 638.7±4.3 μg (low content ones) were used.
In vitro dissolution study showed that more than 90% of AA were released from both SDMP array tips within 5 min. Stability experiment showed that 99.2—99.4% of AA was detected in SDMP array tips when stored at 23 °C for 1 week. When
in vitro permeation experiments were performed after AA SDMP array was inserted to the isolated rat abdominal skin, extremely high amounts of AA, 1285.3±369.0 μg (95.3%) for high content SDMP tip and 405.6±84.3 μg (65.8%) for low content SDMP tip, were permeated for 6 h into the receptor compartment due to the break down of the skin barrier function. When AA SDMP array tip was administered to the rat skin under anesthetized condition with the different contact times, 10, 20 and 30 min, the permeated amount of AA was dependent on both the AA content in SDMP array tips and the contact time. When AA SDMP was contact to the skin for 30 min, permeated amounts of AA were 146.8±22.9 μg (10.9%) for high content-SDMP tip and 61.2±18.2 μg (9.6%) for low content SDMP tip. These results suggest the usefulness of SDMP array tip for the percutaneous absorption of AA.
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Yi Lu, Jui-Hsin Su, Chiung-Yao Huang, Yung-Chun Liu, Yao-Haur Kuo, Zhi ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
464-466
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Two new cembranoids, namely granosolides C (1) and D (2), along with one known cembranoid 4, were isolated from the soft coral
Sinularia granosa. Chemical investigation of
Sinularia querciformis also afforded one new cembranoid, querciformolide E (3), along with four known cembranoids 4—7. The structures of these compounds were elucidated on the basis of their spectroscopic data. Both 4 and 5 were shown to significantly inhibit the accumulation of the pro-inflammatory inducible nitric oxide synthase protein in lipopolysaccharide-stimulated RAW264.7 macrophage cells.
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Dong-Qing Fei, Qiu-Hong Wu, Shi-Gang Li, Kun Gao
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
467-469
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Two new asymmetric eremophilane-type sesquiterpene dimers, ligulamulienin A (1) and B (2), were isolated from the rhizomes of
Ligularia muliensis. Their structures were determined based on their spectroscopic data, including IR, EI-MS, HR-electrospray ionization (ESI)-MS, 1D and 2D-NMR spectroscopy. The cytotoxicity of compounds 1 and 2 was measured in
in vitro human carcinoma (MGC-803), human hepatoma (HEP-G2), and murine sarcoma (S-180) cell lines.
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Ke Pan, Masanori Inagaki, Nagisa Ohno, Chiaki Tanaka, Ryuichi Higuchi, ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
470-474
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Twenty-one galactocerebrosides (1—21), including sixteen new compounds (3—7, 9—17, 19, 21), were identified from a cerebroside molecular species obtained from the chloroform/methanol extract of pyloric caeca dissected from the starfish
Protoreaster nodosus. The structures of these galactocerebrosides were determined on the basis of chemical and spectroscopic evidences. Especially, one-pot GC-MS analysis following methanolysis and periodate oxidation of these galactocerebrosides gave efficient structural information of ceramide moiety rapidly in minute amounts.
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Xiaoyin Chen, Zonghua Wang, Feifei Zhang, Lingyan Zhu, Yanhui Li, Yanz ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
475-478
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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The electrochemical behaviors of rutin at a poly(
p-aminobenzene sulfonic acid) modified glassy carbon electrode (PABSA/GC) have been investigated. Rutin can generate a pair of well-defined redox peaks at the PABSA/GC located at 0.440 V (
Epa) and 0.396 V (
Epc) (
vs. saturated calomel electrode (SCE)), respectively. The results indicate that the reaction involves two electrons transfer, accompanied by two protons and the electrochemical process is controlled by adsorption. The electrochemical parameters of rutin on the modified electrode were calculated with the results of the charge transfer coefficient (α), the number of electron transfer (
n) and the electrode reaction rate constant (
ks) as 0.61, 2.08 and 2.18 s
−1, respectively. Under the selected conditions, the oxidation peak current was linear to the rutin concentration over the range of 2.5×10
−7—1.0×10
−5 M with a detection limit of 1.0×10
−7 M. The proposed method has been successfully applied to the determination of compound rutin tablets with no interference from the coexisting ascorbic acid.
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Bahira Hegazi, Hanan Ahmed Mohamed, Kamal Mohamed Dawood, Farid Abdel- ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
479-483
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Benzo[
d]imidazole 3 and 1,2,4-triazin-5(2
H)-one 6 were prepared by the reaction of starting ethyl (3-hydroxy-1
H-inden-2-yl)(oxo)-acetate 2 with
o-phenylenediamine and thiosemicarbazide respectively. Reaction of 1,4-dihydro-1-phenylindeno[1,2-
c]pyrazole-3-carbohydrazide 8 with phenylisothiocyanate gave thiosemicarbazide 9, and its reaction with chloroacetic acid or phenacylbromides led to the formation of thiazolidinone-4-one 10 or 1,3-thiazoles 12a, b. The reactivity of hydrazide 8 towards fluorinated aldehyde, phthalic anhydride, and hydrazonoyl chlorides 15a, b was studied to give fluorinated hydrazones, imide bis-hydrazones 13—16. The newly synthesized compounds were screened for their cytotoxic activities and compounds 6, 8, 9 and 10 were found the most potentially cytotoxic. The detailed synthesis, spectroscopic and biological data are reported.
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Tomoyoshi Fuchise, Hideki Kishimura, Zhi-hong Yang, Mareshige Kojoma, ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
484-487
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Atlantic cod trypsin-catalyzed peptide synthesis has been studied by using
p-amidino- and
p-guanidinophenyl esters of
N-(
tert-butyloxycarbonyl)amino acid as acyl donor components. The reaction temperature was optimized at 0 °C. The method was shown to be successful as effectively for synthesizing the peptide and useful for preparing dipeptide between
D-amino acid with
D-amino acid and β-amino acid with β-amino acid, respectively. The enzymatic hydrolysis of the resulting products was negligible.
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Hiroki Tsumoto, Ryo Taguchi, Kohfuku Kohda
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
488-494
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Protein nitration at tyrosine residues proceeds to form 3-nitrotyrosine; this product is today used as a biomarker of nitrative stress. We have developed an efficient method with which to identify nitrated peptides and to quantify protein nitration levels in different biological samples by a combination of the chemical derivatization of nitrotyrosine-containing peptides and mass spectrometry. Our strategy includes: 1) the protection of both N-terminal amines and ε-amines of lysine residues by acetylation with
13C
0/
13C
4– or D
0/D
6–acetic anhydride; 2) the reduction of nitrotyrosine to aminotyrosine with sodium hydrosulfite; and 3) the derivatization of aminotyrosine with 1-(6-methyl[D
0/D
3]nicotinoyloxy)succinimide. The utility of our method is demonstrated with nitrotyrosine-containing angiotensin II and bovine serum albumin as the model compounds.
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Kazusa Nishiyama, Atsushi Yamada, Miki Takahashi, Tomoharu Takeuchi, K ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
495-500
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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To search for the endogenous glyco-epitope in
Caenorhabditis elegans, we synthesized labeled Galβ1-3Fuc and Galβ1-4Fuc and examined their binding affinity for
C. elegans galectin LEC-6 using frontal affinity chromatography analysis. We developed a new strategy for synthesizing the labeled saccharides, in which the labeling unit, the 2-aminopyridine moiety, is coupled with a spacer unit derived from
D-mannitol. Our results indicate that Galβ1-4Fuc is the endogenous glyco-epitope present in
C. elegans N-glycans.
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Sherine Nabil Khattab
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
501-506
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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A new family of sulfonate ester-type coupling reagents is described which differs in its leaving group. The sulfonate ester coupling reagents ethyl 2-cyano-2-(naphthalen-2-ylsulfonyloxyimino)acetate (NpsOXY), and ethyl 2-cyano-2-(tosyloxyimino)acetate (TsOXY) are more efficient alternatives to the benzotriazole sulfonate esters in terms of racemization suppression and coupling effectiveness. Both oxyma and its related sulfonate esters can be handled with a considerably lower risk than the explosive benzotriazole and its derivatives. 2-Oxopyridin-1(2
H)-yl naphthalene-2-sulfonate (NpsOPy) and 2-oxopyridin-1(2
H)-yl 4-methylbenzenesulfonate (TsOPy) sulfonate esters derived from 1-hydroxypyridin-2(1
H)-one were also successfully used as new coupling reagents requiring a longer preactivation time during the coupling process. An improvement in yield and almost comparable optical purity to that of the 1-hydroxy-benzotriazole (HOBt) and 1-hydroxy-7-azabenzotriazole (HOAt) analogues was observed.
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Cai-Xia Dong, Kyoko Hayashi, Jung-Bum Lee, Toshimitsu Hayashi
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
507-510
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Three polysaccharides including a neutral polysaccharide (RN), an acidic polysaccharide (RA) and a pectic polysaccharide (RP) were isolated from aerial part of
Portulaca oleracea L. and evaluated for their anti-herpes simplex virus type 2 (HSV-2) and anti-influenza A virus (IFV-A). RN was found to consist of glucose (Glc), mannose (Man) and arabinose (Ara) with small amounts of galactose (Gal), and identified to be an arabinoglucomannan. RA was mainly composed of Gal and Ara with a small proportion of glucuronic acid (GlcA). It was characterized as a type II arabinogalactan (AGII), which consisted of a 1,3-, 1,6- and 1,3,6-linked galactopyranosyl (Gal
p) and non-reducing terminal and 1,5-linked arabinofuranosyl (Ara
f) residues. RP was deduced to be a pectin, which consisted of a predominant amount of galacturonic acid (GalA) with small amounts of Gal, rhamnose (Rha) and Ara. The GalA residues were found to be highly methyl-esterified and partially acetylated. Results of antiviral tests showed that only RP had anti-HSV-2 activity. Furthermore, its anti-HSV-2 target was elucidated to be the step of virus penetration into host cells. No marked virucidal activity of RP was observed.
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Yasuyoshi Agata, Yasunori Iwao, Atsuo Miyagishima, Shigeru Itai
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
511-515
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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A mechanistic mathematical model was designed to predict dissolution patterns under non-sink conditions. Sulfamethoxazole was used as a model drug, and its physico-chemical properties such as solubility, density, and intrinsic dissolution rate constant
etc., were investigated in order to apply these experimental values to the proposed model. Dissolution tests were employed as a way of validating the mathematical model, and it was found that the predictions given by the model were surprisingly accurate for all particle sizes. In addition, a simulation focused on forecasting the fraction of the drug that was dissolved at a certain time point when various initial particle diameters were used was also particularly valuable. Therefore, these results demonstrated that the model enables dissolution profiles to be analyzed under non-sink conditions.
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Ramin Ghahremanzadeh, Fatemeh Fereshtehnejad, Ayoob Bazgir
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
516-520
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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A simple and one-pot synthesis of new chromeno[2,3-
d]pyrimidine-triones by a three-component condensation reaction of barbituric acids, aldehydes and cyclohexane-1,3-diones in refluxing ethanol in the presence of
p-toluenesulfonic acid (
p-TSA) for 3—10 h is reported. Two cyclohexane-1,3-diones, four barbituric acids and six substituted aldehydes were chosen for the library validation. Prominent among the advantages of this new method are operational simplicity, good yields and easy work-up procedures employed.
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Bui Huu Tai, Vu Thi Huyen, Tran Thu Huong, Nguyen Xuan Nhiem, Eun-Mi C ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
521-525
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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The new pyrano-pyrone, (+)-8-epi-9-deoxygoniopypyrone (1) and (+)-9-deoxygoniopypyrone (2) were isolated from a chloroform extract of
Goniothalamus tamirensis leaves. Their absolute stereostructures were discussed and confirmed by using infrared (IR), Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR-MS), one (1D) and two-dimensional (2D) nuclear magnetic resonance (NMR) spectra, Mosher's method, and comparison with the known compounds leiocapin A (3), deoxygoniopypyrone A (4), and (−)-8-epi-9-deoxygoniopypyrone (5). At concentrations of 2.67 μ
M, compounds 1 and 2 significantly increased the growth of osteoblastic MC3T3-E1 cells and caused a significant elevation of collagen content, alkaline phosphatase activity, and nodule mineralization in the cells (
p<0.05). Our data suggest that the enhancement of osteoblast function by 1 and 2 may result in the prevention of osteoporosis.
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Suresh Thareja, Ganesh Rajendra Kokil, Saurabh Aggarwal, Tilak Raj Bha ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
526-532
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
JOURNAL
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Protein tyrosine phosphatase 1B (PTP 1B), a cytosolic PTP involved in down-regulation of receptor tyrosine kinase activity following stimulation of the insulin or leptin receptors. Thus, PTP 1B inhibitors could potentially ameliorate insulin resistance and normalize plasma glucose and insulin levels without inducing hypoglycemia, and could therefore be a major advancement in the treatment of type 2 diabetes. A three-dimensional quantitative structure–activity relationship (3D-QSAR) study has been performed on a novel class of sulphonamides using self-organizing molecular field analysis (SOMFA) to correlate their chemical structures with their observed PTP 1B inhibitory activities. The master grid obtained for the various SOMFA models indicates electrostatic and shape potential contributions that can be mapped back onto structural features relating to the trends in inhibitory activities. On the basis of the spatial arrangement, steric and electrostatic factors should appropriately be taken into account for development of new potent inhibitors of PTP 1B for the management of type 2 diabetes.
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Tatsuya Maruyama, Kenichi Onda, Masahiko Hayakawa, Takayuki Suzuki, Te ...
Article type: Regular Article
2010 Volume 58 Issue 4 Pages
533-545
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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In the search for potent and selective human β3-adrenergic receptor (AR) agonists as potential pharmacotherapies for the treatment of obesity and non-insulin dependent (type II) diabetes, we prepared a novel series of phenylethanolamine derivatives containing acetanilides and evaluated their biological activities at the human β3-, β2-, and β1-ARs. Among these compounds, the 6-amino-2-pyridylacetanilide (36b), 2-amino-5-methylthiazol-4-ylacetanilide (36g), and 5-amino-1,2,4-thiadiazol-3-ylacetanilide (36h) derivatives showed potent agonistic activity at the β3-AR with functional selectivity over the β1- and β2-ARs. In addition, these compounds exhibited significant hypoglycemic activity in a rodent diabetic model.
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Mehdi Mohammadi, Maryam Yousefi, Zohreh Habibi, Abbas Shafiee
Article type: Notes
2010 Volume 58 Issue 4 Pages
546-548
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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The aerial parts of several
Angelica species of the Apiaceae as natural medicine, are rich sources of various coumarins with biological, to a lesser extent, toxicological activities. From the chloroform extract of the aerial parts of
Angelica urumiensis M
OZAFF. two new coumarins (1, 2), together with six known coumarins and two known flavonoids were isolated. On the basis of comprehensive spectroscopic analyses, including electron ionization-mass spectra (EI-MS),
1H-NMR,
13C-NMR, 1D nuclear Overhauser effect (NOE), distortionless enchancement by polarization transfer (DEPT), H, H correlation spectroscopy (COSY), heteronuclear multiple quantum coherence (HMQC), heteronuclear multiple bond correlation (HMBC), rotating frame Overhauser enhancement spectroscopy (ROESY) spectra and comparison with spectral data of known compounds, the structure of new compounds were established as pyranocoumarin dimmer (1) and (+)-8,9-dihydro-8-(2-hydroxypropan-2-yl)-2-oxo-2
H-furo[2,3-
h]chromen-9-yl-3-methylbut-2-enoate (2). The eight known compounds (3—10) were isosamidin, laserpitin, pteryxin, isolaserpitin,
cis-khellactone, angelicin, genkwanin and salvigenin, respectively. These known structures are isolated from the aerial parts of
A. urumiensis for the first time. Antioxidant activities of the two new coumarins were evaluated by using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and exhibited a moderate antioxidant activity.
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Jian-Feng Liu, Kang-Ping Xu, Fu-Shuang Li, Jian Shen, Chang-Ping Hu, H ...
Article type: Notes
2010 Volume 58 Issue 4 Pages
549-551
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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A new flavonoid, 6-(2-hydroxy-5-carboxyphenyl)-apigenin (1), together with two new natural products, 3-(4-hydroxyphenyl)-6,7-dihydroxy coumarin (2), 1-methoxy-3-methylanthraquinone (3) and four known compounds, were isolated from
Selaginella tamariscina (B
EAUV.) S
PRING. The structures of the new isolated compounds were elucidated on the basis of 1D and 2D NMR as well as ESI-HR-MS spectroscopic analysis.
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Jing Zhang, Sheng-Xin Yang, Xiao-Bo Yang, Min-Yi Li, Gang Feng, Jian-Y ...
Article type: Notes
2010 Volume 58 Issue 4 Pages
552-555
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Two new mexicanolides, named xylomexicanolides A and B, were isolated from the seeds of an Indian mangrove,
Xylocarpus moluccensis, together with four known limonoids, khayasin, angolensic acid methyl ester, khayasin T, and 2′
S-methylbutanoylproceranolide. The structures of these limonoids were established on the basis of spectroscopic data. The
13C-NMR data of khayasin were reported for the first time. Khayasin was found to exhibit marked insecticidal activity against the fifth instar larvae of
Brontispa longissima (G
ESTRO) at a concentration of 10 mg/l.
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Hiroshi Ishii, Hiroaki Todo, Kenji Sugibayashi
Article type: Notes
2010 Volume 58 Issue 4 Pages
556-561
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Effects of thermodynamic activity and the state (solution/suspension) of triamcinolone acetonide (TA) on skin permeation and concentration were physicochemically and kinetically analyzed. Permeation of TA through a silicone membrane, hairless rat skin (full-thickness skin or stripped skin) or a three-dimensional cultured human skin model (LSE-high) was determined and a permeability coefficient (
P), partition coefficient (
K) , diffusion coefficient (
D) and steady-state flux (
J) were calculated. The resulting
J values proportionally increased with an increase in the TA activity in the drug solution and similar
P,
K and
D values were obtained independent of the TA state (solution/suspension) in all membranes except for full-thickness hairless rat skin. On the other hand, the TA permeation through full-thickness hairless rat skin with the 1000 μg/ml suspension was higher than that expected judging by the thermodynamic acidity of TA. Higher
D and
P values were also obtained in the skin permeation of TA from the 1000 μg/ml suspension. Morphological observation of the skin surface by scanning electron microscope (SEM) showed the presence of TA solids in the hair follicles after application of the TA suspension. These results suggest that dissolved TA may be permeated predominantly through the stratum corneum, but that solid TA may be passed through the hair follicles to enter the dermis. The present physicochemical and kinetic analysis provides useful information to develop topical steroid formulations.
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Wimal Herath, Ikhlas Ahmad Khan
Article type: Notes
2010 Volume 58 Issue 4 Pages
562-564
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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The yeast culture,
Rhodotorula mucilaginosa (ATCC 20129) transformed flutamide (1) to three metabolites: 4-nitro-3-(trifluoromethyl)aniline (2), 2-methyl-
N-[4-amino-3-(trifloromethyl)phenyl]propanamide (3) and
N-[4-amino-3-(trifluoromethyl)phenyl]acetamide (4). The structures were established by spectroscopic methods.
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Min Wu, Ping Wu, Haihui Xie, Liangxiong Xu, Yueming Jiang, Xiaoyi Wei
Article type: Notes
2010 Volume 58 Issue 4 Pages
565-567
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Further chemical investigation of the whole plants of
Gentiana loureirii led to the isolation and characterization of three new compounds, cyclic 4-
O-β-
D-glucopyranosylcaffeic acid dimer (1), a new α-tetralone, 4-hydroxy-6-methyl-α-tetralone 4-
O-β-
D-glucopyranoside (2), and 3β,30-dihydroxy-12-ursen-28-oic acid 28-
O-β-
D-glucopyranosyl ester (3), along with five known compounds. To the best of our knowledge, compound 1 is the first cyclic phenolic acid glycoside dimer.
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Takashi Kikuchi, Masatoshi Nihei, Hisashi Nagai, Hidekuni Fukushi, Kei ...
Article type: Notes
2010 Volume 58 Issue 4 Pages
568-571
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
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Albanol A (1), isolated from the root bark extract of
Morus alba (mulberry), was evaluated for the cytotoxic and apoptosis-inducing activities in human leukemia (HL60) cells, and for the inhibitory activity in human DNA topoisomerases (Topo) I and II. This compound showed potent cytotoxic activity (IC
50 1.7 μ
M) on the cells, and potent inhibitory activity on topoisomerase II (IC
50 22.8 μ
M). In addition, albanol A induced early apoptosis which was detected by observing the membrane phospholipid exposure in flow cytometry. Western blot analysis showed that albanol A markedly reduced the levels of procaspases-3, 8, and 9, while being increased the levels of cleaved caspases-3, 8, and 9. The Bax/Bcl-2 ratio was significantly increased by albanol A treatment. Furthermore, albanol A induced caspase-2 activation. These results suggested that albanol A induces apoptotic cell death in HL60
via both the cell death receptor pathway by stimulation of death receptor, and the mitochondrial pathway by Topo II inhibition through caspase-2 activation. Therefore, albanol A may be a promising lead compound for developing an effective drug for treatment of leukemia.
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Hiroyuki Tsutsumi, Takashi Sato, Takashi Ishizu
Article type: Notes
2010 Volume 58 Issue 4 Pages
572-574
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
JOURNAL
FREE ACCESS
The single crystal of (−)-gallocatechin-3-
O-gallate (GCg) was prepared using a solution containing an equimolecular amount of GCg and (−)-epigallocatechin-3-
O-gallate (EGCg) in water. The crystal structure of GCg determined by X-ray crystallographic analysis was monoclinic with the space group
P2
1 at 223 K. Offset π–π interactions formed between the A and A rings, B and B rings, and gallate and gallate rings of GCg, and five intermolecular hydrogen bonds formed between GCgs, GCg and water. The B ring of GCg bonded to C2 was in the axial position and the gallate ring of GCg bonded to C3 was in the pseudoaxial position with respect to the C ring of GCg.
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Yingni Pan, Toshio Morikawa, Kiyofumi Ninomiya, Katsuya Imura, Dan Yua ...
Article type: Notes
2010 Volume 58 Issue 4 Pages
575-578
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
JOURNAL
FREE ACCESS
Four new acylated phenylethanoid oligoglycosides, kankanosides J
1 (1), J
2 (2), K
1 (3), and K
2 (4), were isolated from stems of
Cistanche tubulosa (Orobanchaceae) together with isocampneoside I (5). Their structures were elucidated on the basis of chemical and physicochemical evidence. Among them, 3—5 were found to inhibit
D-galactosamine-induced cytotoxicity in primary cultured mouse hepatocytes.
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Yong-Xia Tan, Ting Gong, Chao Liu, Ruo-Yun Chen, De-Quan Yu
Article type: Notes
2010 Volume 58 Issue 4 Pages
579-581
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
JOURNAL
FREE ACCESS
Five new 2-arylbenzofuran derivatives wittifurans A—C, F and G (1—5) have been isolated from the stem bark of
Morus wittiorum. Their structures were determined on the basis of spectroscopic analysis. Compounds 1, 3—5 were evaluated for their antioxidant and anti-inflammatory activities respectively.
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Ya-Bei Huang, Shi-Jun Wang, Yan-Qin Zi, Zhang Yu, Xiao-Yan Gao, Ying-C ...
Article type: Notes
2010 Volume 58 Issue 4 Pages
582-586
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
JOURNAL
FREE ACCESS
The interaction between prulifloxacin (PUFX) and human serum albumin (HSA) was investigated under simulated physiologic conditions with fluorescence spectra. The fluorescence quenching process of HSA may be mainly governed by a static quenching mechanism. The apparent binding constant
Kb between PUFX and HSA at different temperatures were 2.08±1.04, 2.74±0.50, and 4.98±1.61×10
8 l/mol. The thermodynamic parameters, with a negative value of Δ
G0, revealed that the binding is a spontaneous process. A binding distance
R of 1.19 nm between donor and acceptor was obtained from the Fŏrster energy transfer theory.
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Yukiko Matsuo, Yoshihiro Mimaki
Article type: Notes
2010 Volume 58 Issue 4 Pages
587-590
Published: April 01, 2010
Released on J-STAGE: April 10, 2010
JOURNAL
FREE ACCESS
A new neolignan, (7
R,8
R)-5-
O-demethylbilagrewin (1), together with four known lignans (2—5), were isolated from the heartwood of
Santalum album (Santalaceae). The structure of 1 was determined by analysis of extensive spectroscopic data. The isolated compounds and derivatives were evaluated for their cytotoxic activities against HL-60 human promyelocytic leukemia cells and A549 human lung adenocarcinoma cells. Compounds 1 and 2 exhibited cytotoxicity against HL-60 cells with IC
50 values of 1.5±0.02 and 4.3±0.13 μ
M, and against A549 cells with IC
50 values of 13.6±0.32 and 19.9±1.27 μ
M, respectively. The aldehyde group of 1 and 2 was revealed to be a structural requirement for the appearance of cytotoxicity in this type of lignans. These tumor cell deaths were shown to be mediated through induction of apoptosis.
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