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Volume 62, Issue 2
Displaying 1-13 of 13 articles from this issue
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Neslihan Üstündağ Okur, Altuğ Yavaşoğlu, Hatice Yeşim Karasulu2014 Volume 62 Issue 2 Pages 135-143
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLNaproxen (Np) is an example of a non-steroidal anti-inflammatory drug (NSAID) commonly used for the reduction of pain and inflammation. In order to develop an alternative formulation for the topical administration of Np, microemulsions were evaluated as delivery vehicles. Four formulations were prepared using isopropyl myristate (IPM) as oil phase, Span 80, Labrafil M, Labrasol, Cremophor EL as surfactants, ethanol as co-surfactant and distilled water or 0.5 N NaOH solution as aqueous phase. The final concentration of Np in the microemulsion system was 100 mg/g (w/w). The physicochemical properties such as electrical conductivity, droplet size, viscosity, pH and phase inversion temperature of microemulsions were measured. Stability tests of the formulations were also performed at 5±2, 25±2 and 40±2°C. The abilities of various microemulsions and selected commercial (C) formulation to deliver Np through the skin were evaluated in vitro using diffusion cells fitted with rat skins. The in vitro permeation data showed that microemulsions increased the permeation rate of Np between 4.335–9.040 times over the C formulation. Furthermore Np successfully permeated across the skin from the microemulsion with the highest flux rate (1.347±0.005 mg·cm−2·h−1) from a formulation (M4Np) consisting of IPM (2.36 g), Labrosol (0.13 g), Span 80 (0.62 g), ethanol (5.23 g), 0.5 N NaOH solution (0.66 g) and Np (1 g). According to the histological investigations, no obvious skin irritation was observed for the studied microemulsions. These results indicate that the microemulsion formulation may be appropriate vehicles for the topical delivery of Np.View full abstractDownload PDF (2081K) Full view HTML -
Ayşegül Bektaş, Erdal Cevher, Sevgi Güngör, Yıldız Özsoy2014 Volume 62 Issue 2 Pages 144-152
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLIt was aimed to develop the matrix type polysaccharide-based transdermal films of nifedipine (NFD) to provide its long term plasma concentration. The mechanical tests were carried out on gel formulations which were utilised in the fabrication of transdermal films to determine the type of polymer (pectin, sodium alginate) and plasticizer (propylene glycol, glycerine) as well as their concentrations. The mechanical strength, elasticity, bioadhesiveness and the drug release characteristics of optimised films containing NFD were evaluated. Permeation of NFD from the films with/without adding an enhancer (nerolidol) was followed through excised rat skin using Franz diffusion cells. Results showed that the gels composed of either pectin or sodium alginate were appropriate for the fabrication of transdermal films of NFD, and the addition of propylene glycol improved mechanical strength, flexibility, and bioadhesiveness of the films. Permeation data showed that nerolidol was an effective permeation enhancer for the polysaccharide-based transdermal films of NFD.View full abstractDownload PDF (1069K) Full view HTML -
Tatsuhiro Kodama, Hiroyuki Sawada, Hiroshi Hosomi, Masahito Takeuchi, ...2014 Volume 62 Issue 2 Pages 153-159
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLThe purpose of this study was to develop a novel simulation program to accurately predict the maximum product temperature and the primary drying time in lyophilization using the predictive model for dry layer resistance, which is the resistance of dried cake against water vapor flow. Ten percent sucrose aqueous solution was selected as a model formulation. It was demonstrated that the deviations between the predicted and measured maximum product temperature were attributed to the error of dry layer resistance at a given drying condition, which was different from the measured dry layer resistance in a preliminary lyophilization run for the simulation program. However, when the predictive model of dry layer resistance was used for the simulation program, the model remarkably enhanced the accuracy of the simulation program to predict the maximum product temperature and primary drying time under various operating conditions. Furthermore, the primary drying condition required for minimized drying at a close collapse temperature was successfully discovered through one preliminary run. Therefore, it is expected that the developed simulation program is useful for designing the lyophilization cycle without a trial and error approach.View full abstractDownload PDF (674K) Full view HTML -
Emilia Szymańska, Katarzyna Winnicka, Aleksandra Amelian, Urszula Cwal ...2014 Volume 62 Issue 2 Pages 160-167
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLTopical administration of clotrimazole represents the common use therapy in the antimycotic genitourinary tract treatment. Due to the fast self-cleaning action of the vagina, commercially available vaginal dosage forms with clotrimazole cannot assure prolonged contact time with mucosa, therefore the main objective of this study was to develop a dosage form for vaginal administration of clotrimazole using chitosan—a biodegradable and biocompatible derivative of chitin. Tablets mucoadhesive properties were examined using texture analyser under the presence of porcine vaginal mucosa and two different models of adhesive layers— mucin gel and gelatine discs. In addition, friability, hardness, swelling behaviour, residence time, surface morphology of the performed tablets, the in vitro release profile of clotrimazole and clotrimazole release kinetics were determined. The release of clotrimazole from formulations with 25 or 40% of chitosan (F2 and F3) followed non Fickian diffusion through chitosan-gel layer and was retarded up to 6 h. Additionally, tablets F2 showed the best results in terms of mucoadhesive properties and appeared to be a good alternative to commercially available antimycotic vaginal dosage forms.View full abstractDownload PDF (2426K) Full view HTML -
Gavara Govinda Rajulu, Halehatty Seephya Bhojya Naik, Abhilash Viswana ...2014 Volume 62 Issue 2 Pages 168-175
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
Advance online publication: November 23, 2013JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialA series of new hydroxamic acid derivatives (6a–f) at C-3 position of fluoroquinolones were designed and synthesized through multistep synthesis. The design concept involved replacement of the 3-carboxylic acid in fluoquinolones with hydroxamic acid as an acid mimicking group. The synthetic work employed in this work provides a good example for the synthesis of pure hydroxamic acid based fluoroquinolones. The synthesized compounds were characterized by 1H-NMR, electrospray ionization (ESI)-MS and IR. The new compounds were tested for their in vitro antimicrobial and anti-proliferative activity. Out of the six derivatives, compound 6e exhibited moderate antibacterial activity by inhibiting the growth of Escherichia coli and Klebsiella pneumoniae (MIC: 4.00–8.00 µg/mL). Compounds 6b and 6f displayed good growth inhibition against A549 Lung adenocarcinoma and HCT-116 Colon carcinoma cell lines.View full abstractDownload PDF (672K) Full view HTML -
Tamer Zekry Attia, Taku Yamashita, Mohamed Abdelkhalek Hammad, Akinori ...2014 Volume 62 Issue 2 Pages 176-181
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLAlthough cytochromes P450 2C9 (CYP2C9) and 2C19 (CYP2C19) have 91% amino acid identity, they have different substrate specificities. Previous studies have suggested that several amino acid residues may be involved in substrate specificity. In this study, we focused on the roles of two amino acids, residues 72 and 241. The amino acids in these positions have opposite charges in CYP2C9 and 2C19; the former has lysines in both positions (Lys72 and Lys241), and the latter has glutamic acids (Glu72 and Glu241). Reciprocal mutants for both CYP2C19 and 2C9 were produced, and their metabolic activities and spectroscopic properties were examined using three tricyclic antidepressant (TCA) drugs: amitriptyline, imipramine, and dothiepin. Although CYP2C19 wild-type (WT) had a high metabolic activity for all three drugs, the E72K mutation decreased enzymatic activity by 29–37%, while binding affinities were diminished 2.5- to 20-fold. On the other hand, low activity and low affinity of CYP2C9 WT were recovered notably by K72E mutation. The metabolic activities and binding affinities were minimally affected by CYP2C19 E241K and CYP2C9 K241E mutations. We could also show linear correlations between metabolic activities and binding affinities, and hence we conclude that amino acid residue 72 plays a key role in TCA drug metabolism by limiting the binding affinities of CYP2C19 and CYP2C9.View full abstractDownload PDF (977K) Full view HTML
Notes
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Masashi Takano, Saori Ohya, Kaori Yasuda, Miyu Nishikawa, Akiko Takeuc ...2014 Volume 62 Issue 2 Pages 182-184
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLOur previous studies revealed that recombinant human CYP3A4 converted 2α-(3-hydroxypropoxy)-1α,25-dihydroxyvitamin D3 (O2C3), which was a more potent binder to vitamin D receptor (VDR) than the natural hormone, 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3, 1), to 1α,2α,25-trihydroxyvitamin D3 (2). Here, we synthesized 2 using the Trost Pd-mediated coupling reaction between an A-ring precursor and a CD-ring bromoolefin and evaluated its preliminary biological activity. We found that metabolite 2 from O2C3 was still active as a VDR ligand while maintaining human VDR binding affinity (27.3% of 1α,25(OH)2D3) and HL-60 cell differentiation activity (62% of 1α,25(OH)2D3).View full abstractDownload PDF (500K) Full view HTML -
Tran Thi Thu Trang, To Dao Cuong, Tran Manh Hung, Jeong Ah Kim, Jeong ...2014 Volume 62 Issue 2 Pages 185-190
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLA new megastigmane glycoside, galloyl linarionoside A (1), together with 13 known compounds (2–14) were isolated from the aerial parts of Aceriphyllum rossii ENGLER. (Saxifragaceae). The chemical structures of the isolated compounds were established mainly by using nuclear magnetic resonance spectra, mass spectrometry, and modified Mosher’s method. Among the isolates, compounds 4, 5, 6 and 7 showed potent inhibitory activity against the lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophage cells with IC50 values of 12.5, 9.5, 10.5 and 9.3 µM, respectively. The anti-inflammatory effect of compound 7 was accompanied by dose-dependent decreases in the production of inducible nitric oxide synthase and cyclooxygenase-2 proteins not in the inhibitor kappa B (IκB)-dependent nuclear factor-kappa B activation.View full abstractDownload PDF (708K) Full view HTML -
Khem Raj Joshi, Hari Prasad Devkota, Takashi Watanabe, Shoji Yahara2014 Volume 62 Issue 2 Pages 191-195
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
Advance online publication: November 30, 2013JOURNAL FREE ACCESS FULL-TEXT HTMLThree new glycosides: thotneoside A (quercetin 3-O-(6″-O-phenylacetyl)-β-D-galactopyranoside) (1), thotneoside B (quercetin 3-O-(6″-O-phenylacetyl)-β-D-glucopyranoside) (2) and thotneoside C (3-methyl-2-butenoic acid 1-O-β-D-glucopyranoside) (3), together with nine known compounds; quercetin (4), quercetin 3-O-β-D-galactopyranoside (5), quercetin 3-O-(6″-O-galloyl)-β-D-galactopyranoside (6), quercetin 3-O-β-D-galacturonopyranoside (7), quercetin 3-O-β-D-glucuronopyranoside (8), quercetin 3-O-α-L-rhamnopyranoside (9), rutin (10), quercetin 3-O-α-L-arabinopyranoside (11) and 2,4,6-trihydroxyacetophenone 2-O-β-D-glucopyranoside (12) have been isolated from the shade dried leaves of Aconogonon molle, commonly known as “Thotne″ in Nepal. The structures were elucidated on the basis of chemical and spectroscopic methods. All of these compounds were isolated for the first time from A. molle and their in vitro antioxidant activity was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay. Quercetin (4) and its glycosides (1–2, 5–11) showed potent free radical scavenging activity.View full abstractDownload PDF (482K) Full view HTML -
Wei Li, Seo Young Yang, Xi Tao Yan, Ya Nan Sun, Seok Bean Song, Hee Ky ...2014 Volume 62 Issue 2 Pages 196-202
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialZanthoxylum schinifolium is an aromatic shrub, the pericarp and leaves of which are widely used in culinary applications in East Asian countries. In the present study, one new neolignan glycoside, zanthoxyloside A (1) together with 16 known glycosides (2–12) and alkaloids (13–17), were isolated from methanol extract of the stems of Z. schinifolium. The absolute configuration of one known monoterpenoid glycoside (2) was determined. The structures of the isolated compounds were established by one dimensional (1D), 2D NMR and mass spectrometry. The nuclear factor-κB (NF-κB) inhibitory activities of the isolated compounds stimulated with tumor necrosis factor alpha (TNFα) were measured using a luciferase reporter system. Compounds 1, 5, 16, and 17 exhibited significant inhibition of NF-κB activation in a dose-dependent manner. Furthermore, compounds 1, 5, 16, and 17 inhibited TNFα-induced expression of inducible nitric oxide synthase (iNOS) and intercellular adhesion molecule-1 (ICAM-1) mRNA and dose-dependent inhibition of iNOS promoter activity.View full abstractDownload PDF (829K) Full view HTML -
Nguyen Xuan Cuong, Nguyen Phuong Thao, Bui Thi Thuy Luyen, Nguyen Thi ...2014 Volume 62 Issue 2 Pages 203-208
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialNine cembranoid diterpenes 1–9, including four new compounds, crassumols D–G (1–4), were isolated from the methanol extract of the Vietnamese soft coral Lobophytum crassum. Spectroscopic methods were used to elucidate the structures of these compounds. Compound 5 exhibited a potent inhibitory effect on tumor necrosis factor-alpha (TNFα)-induced nuclear factor-kappa B (NF-κB) transcriptional activation in HepG2 cells and significantly inhibited the mRNA expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) in a dose-dependent manner.View full abstractDownload PDF (816K) Full view HTML -
Haruna Suzuki, Takaaki Kubota, Azusa Takahashi-Nakaguchi, Jane Fromont ...2014 Volume 62 Issue 2 Pages 209-212
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLNew meroterpenoids, nakijiquinone S (1) and nakijinol C (2), have been isolated from an Okinawan marine sponge of the family Spongiidae. The gross structures and relative stereochemistries of 1 and 2 were elucidated on the basis of their spectral data. Nakijiquinone S (1) and nakijinol C (2) were new meroterpenoids consisting of a clerodane-type decalin ring connected to a 2-butoxy-5-hydroxy-benzoquinone unit or methyl 2,3,4-trihydroxybenzoate unit through a methylene, respectively. Nakijiquinone S (1) and nakijinol C (2) showed antimicrobial activities against several bacteria and fungi.View full abstractDownload PDF (451K) Full view HTML -
Takahiro Iwai, Takaaki Kubota, Jane Fromont, Jun’ichi Kobayashi2014 Volume 62 Issue 2 Pages 213-216
Published: February 01, 2014
Released on J-STAGE: February 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLNew dimeric bromopyrrole–imidazole alkaloids, nagelamide I (1) and 2,2′-didebromonagelamide B (2), have been isolated from an Okinawan marine sponge Agelas species. The structures of 1 and 2 were elucidated based on analyses of the spectral data. Nagelamide I (1) was the first symmetric dimeric bromopyrrole–imidazole alkaloid consisting of two subunits connected with a single bond.View full abstractDownload PDF (453K) Full view HTML
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