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Volume 62, Issue 5
Displaying 1-16 of 16 articles from this issue
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Regular Articles
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Ranjan Kumar Barman, Yasunori Iwao, Yuka Funakoshi, Abdul-Hackam Ranne ...2014 Volume 62 Issue 5 Pages 399-406
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLTo improve the solubility of the drug nifedipine (NI), highly stabilized solid–lipid nanoparticles (SLNs) of nifedipine (NI-SLNs) were prepared by high pressure homogenization using two phospholipids, followed by lyophilization with individual sugar moieties (four monosaccharides and four disaccharides). The mean particle diameter, polydispersity index (PDI), zeta potential, drug loading, and the encapsulation efficiency of the NI-SLN suspension were determined to be 68.5 nm, 0.3, −62.1 mV, 2.7%, and 97.5%, respectively. In comparison with the NI-SLNs, the NI-SLNs lyophilized with trehalose (NI-SLN-Tre) showed a slight increase in the particle size from 68.5 to 107.7 nm, but the PDI decreased from 0.38 to 0.33, and no significant change in zeta potential was observed. Aqueous re-dispersibility study demonstrated that NI-SLNs lyophilized with trehalose had the maximum concentration (14.7 µg/mL) at 5 min, compared with lyophilized SLNs using other sugars; the use of other sugars also resulted in significant changes in the particle size, PDI, and zeta potential. A trehalose concentration of 2.5% w/v and a two-fold dilution of the SLN suspension were found to be the best conditions for lyophilization. Data from lyophilized SLNs using differential scanning calorimetry, powder X-ray diffraction, Fourier-transform infrared spectroscopy, and scanning electron microscopy indicated eventual transformation of NI-SLN-Tre from a crystalline to an amorphous state during the homogenization process. Finally, a stability study was performed with NI-SLN-Tre for up to 6 months at 30°C and 65% relative humidity, with no significant deterioration observed, suggesting that trehalose might be a useful cryoprotectant for NI-SLNs.View full abstractDownload PDF (1871K) Full view HTML -
Yutaka Okuda, Yasunobu Okamoto, Yosuke Irisawa, Kazuto Okimoto, Takash ...2014 Volume 62 Issue 5 Pages 407-414
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLThe purpose of this study was to investigate the applicability of our newly developed technology (RACTAB® technology) for preparing orally disintegrating tablets (ODTs) containing enteric-coated particles. Tamsulosin hydrochloride (TAM) was used as a model drug contained in the enteric-coated particles. Enteric-coated particles containing TAM (ECP-T) were prepared by spray coating a mixture of TAM with controlled-release materials. ECP-T was then mixed with rapidly disintegrating granules (RDGs), which were prepared using the suspension spray-coating method, and was tableted to form ODTs (ODTRAC). ODTRAC was evaluated for its hardness, thickness, internal structure (X-ray-CT scanning), functional properties (controlled-release profile), and in vivo disintegration time. Since RDGs with micronized ethylcellulose (MEC) increased tablet hardness by increasing the contact frequency between granules, ODTRAC containing ECP-T exhibited high hardness (>50 N) and low friability (<0.5%) with a relatively low compression force. After tableting, the structure of ECP-T in ODTRAC remained intact and no damage was observed on the surface. ECP-T recovered from ODTRAC showed the same dissolution profile of TAM in Japanese Pharmacopoeia (JP) 1st and JP 2nd media as that of intact ECP-T, which indicated that the tableting process did not affect the acid-resistibility of the particle. In addition, ODTRAC rapidly disintegrated in vivo (< 30 s), even at a high compression force (at 9 kN). These findings clearly suggest that RACTAB® technology is a useful approach to prepare ODTs containing enteric-coated particles.View full abstractDownload PDF (2557K) Full view HTML -
Shu-Ting Chung, Pei-Yu Chien, Wen-Hsin Huang, Chen-Wen Yao, An-Rong Le ...2014 Volume 62 Issue 5 Pages 415-421
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
Advance online publication: February 25, 2014JOURNAL FREE ACCESS FULL-TEXT HTMLA series of novel flavones derivatives were synthesized based on modification of the active ingredients of a traditional Chinese medicine Scutellaria baicalensis GEORGI and screened for anti-influenza activity. The synthetic baicalein (flavone) analogs, especially with the B-rings substituted with bromine atoms, were much more potent than oseltamivir or ribavirin against H1N1 Tamiflu-resistant (H1N1 TR) virus and usually with more favorable selectivity. The most promising were 5b, 5c, 6b and 6c, all displaying an 50% effective concentration (EC50) at around 4.0–4.5 µM, and a selective index (SI=50% cytotoxic concentration (CC50)/EC50)>70. For seasonal H3N2-infected influenza virus, both 5a and 5b with SI >17.3 indicated superior to ribavirin. The flavonoids having both not-naturally-occurring bromo-substituted B-rings and appropriate hydroxyls positioning on the A-rings might be critical in determining the activity and selectivity against H1N1-Tamiflu-resistant infected influenza viruses.View full abstractDownload PDF (576K) Full view HTML -
Usharani Nagarajan, Kohsaku Kawakami, Shaoling Zhang, Bangaru Chandras ...2014 Volume 62 Issue 5 Pages 422-428
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialCollagen is a promising biomaterial for drug delivery due to advantages including high biocompatibility and biodegradable property. However, transforming collagen into solid nanoparticles is difficult, although the solid dosage form is advantageous for some administration routes including pulmonary and oral drug delivery. In this study, collagen solid nanoparticles are prepared in one-step using electrospray deposition under ambient temperature and pressure conditions. Although collagen molecules formed micron-sized aggregates in acetic acid solutions spontaneously, electrospraying the collagen solutions resulted in formation of nanofibers. Solid nanoparticles were obtained by increasing conductivity of the solution and/or inducing structural perturbation of the collagen molecules using salts. The ability of solid collagen particles as a drug carrier was demonstrated by incorporating theophylline as a model drug using a coaxial spray technique. Release of theophylline was controlled by cross-linking collagen molecules. Electrospray deposition was proved to be a powerful method for producing solid collagen nanoparticles for drug delivery.View full abstractDownload PDF (3364K) Full view HTML -
Fumiko Fujisaki, Hatsumi Aki, Ayumi Naito, Enko Fukami, Nobuhiro Kashi ...2014 Volume 62 Issue 5 Pages 429-438
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLIn connection with our studies on hydantoin derivatives, a conventional regioselective chemical transformation of 5-methylene hydantoins 4a–c to 5-aminomethyl-substituted hydantoins 5–10 or to 5-amino-5-methyl-disubstituted hydantoins 11–14 is described. Synthesis of bivalent twin-drug type hydantoin derivatives 19–24 and the binding property of a bivalent symmetrical hydantoin derivative 24b to sulfated glycosaminoglycans are also described.View full abstractDownload PDF (769K) Full view HTML -
Kamal Mohamed Dawood, Hussein Khalaf-Allah Abu-Deif2014 Volume 62 Issue 5 Pages 439-445
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLN,N′-Diarylethylene-bis-thiourea derivatives 1 and 8 were synthesized and their reactions with hydrazonoyl chlorides yielded the corresponding bis-(2-(N-arylimino)-1,3-thiazolidine derivatives 5a–d and 11a–c. The reaction of compound 1 with several α-haloketones afforded the bis-(5-methyl-2-(N-phenylimino)-1,3-thiazolidine derivatives 15a–c and 19a, b. The newly synthesized compounds were tested for their antimicrobial activity against four fungi, two Gram-positive and two Gram-negative bacteria and showed high antibacterial and antifungal activities against all the test microorganisms except Pseudomonas aeruginosa and Candida albicans. Compounds 5b, 15b and 19a exhibited the highest activities against the test microorganisms. The MIC evaluation showed that compound 15b has higher activity than Amphotericin B and Ampicillin against all tested fungi and Gram-positive bacteria (Staphylococcus pneumonia) and showed similar activity like Ampicillin against Gram-negative bacteria (Escherichia coli).View full abstractDownload PDF (625K) Full view HTML -
Dongguk Min, Minkyu Kim, Jérémy Ricci, Sora Jung, Kirim Kim, Won-Yoon ...2014 Volume 62 Issue 5 Pages 446-453
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
Advance online publication: March 07, 2014JOURNAL FREE ACCESS FULL-TEXT HTMLThe practical synthesis and anticancer activity of novel deoxoartemisinin–glycolipid hybrids, which incorporate two drugs into a single molecule and can impact multiple targets simultaneously are presented. These hybrids exhibited potent in vitro anticancer activity against several human cancer cell lines. The deoxoartemisinin–glycolipid hybrids generally demonstrated better anticancer activity than either artemisinin or daumone alone and cisplatin.View full abstractDownload PDF (762K) Full view HTML -
Asmaa Said Ali Yassen, Hosam Eldin Abd Elhamed Ahmed Elshihawy, Mohame ...2014 Volume 62 Issue 5 Pages 454-466
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLIn this study, four series of 4-anilinoquinazoline derivatives were designed and synthesized as potential anti-proliferative agents. Mechanism of anticancer activity was explained through molecular docking of the target compounds into epidermal growth factor receptor tyrosine kinase (EGFR-TK) active site which displayed comparable binding mode of certain compounds to that of lapatinib. Moreover, the newly synthesized compounds were tested for their anti-proliferative activity on breast carcinoma cell line (MCF-7). 6-(4-Benzylpiperazin-1-ylsulfonyl)-4-(4-bromoanilino)quinazoline (14g) exhibited the most potent inhibitory activity (IC50=5.52 µM).View full abstractDownload PDF (5186K) Full view HTML
Notes
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Sul-Young Yoo, Thi Kim Van Le, Jin Ju Jeong, Dong-Hyun Kim2014 Volume 62 Issue 5 Pages 467-471
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLThe rhizome of Polygala tenuifolia WILLD (PT, family Polygalaceae) has been used in traditional Chinese medicine for inflammation, dementia, amnesia, neurasthenia and cancer. The phosphoinositide 3-kinase (PI3K)/Akt inhibitor(s) was isolated from PT by using the cytoprotective phenotype of human immunodeficiency virus type 1 (HIV-1) Tat-transduced CHME5 cells against lipopolysaccharide/cycloheximide. We isolated 9 constituents (1)–(9) from ethyl acetate fraction of PT, which potently showed anti-cytoprotective effect against HIV-1 TAT-transduced cells. Of them, (9R)-(−)-9-peptandecanolide (2), a new compound named poligapolide, most potently abolished the cytoprotective effect of HIV-1 Tat-transduced CHME5 cells. The compound (2) inhibited the phosphorylation of Akt and its downstream molecule, glycogen synthase kinase-3 beta (GSK3β) in PI3K/Akt cell survival signaling pathway, but did not suppress the phosphorylation of PI3K and pyruvate dehydrogenase lipoamide kinase isozyme 1. Based on these finding, poligapolide may abolish the cytoprotective phenotype of HIV-1 Tat-transduced CHME5 cells by inhibiting Akt phosphorylation in PI3K/Akt pathway.View full abstractDownload PDF (832K) Full view HTML -
Hua-wei Lv, Jian-guang Luo, Meng-di Zhu, Si-ming Shan, Ling-yi Kong2014 Volume 62 Issue 5 Pages 472-476
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialTwo new neo-clerodane diterpenoids, teucvisins A and B (1, 2), and three new 19-nor-neoclerodane diterpenoids, teucvisins C–E (3–5), together with ten known constituents (6–15) were isolated from the whole plants of Teucrium viscidum. All the isolates were evaluated for their inhibitory activities of lipopolysaccharide (LPS)-induced nitric oxide production in RAW264.7 macrophages. The results indicated that compounds 11 and 15 showed moderate inhibition with an IC50 value of 21.9 and 22.4 µM, respectively.View full abstractDownload PDF (407K) Full view HTML -
Toshihiro Nohara, Yukio Fujiwara, Tsuyoshi Ikeda, Koki Yamaguchi, Hide ...2014 Volume 62 Issue 5 Pages 477-482
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLSix novel acyclic sulfides, named garlicnins L-1–L-4 (1–4), E (5), and F (6), were isolated from the acetone extracts, with the ability to suppress M2 macrophage activation, of the bulbs of garlic (Allium sativum L.), and their chemical structures were characterized.View full abstractDownload PDF (695K) Full view HTML -
Toshihiro Nohara, Hideyuki Manabe, Yukio Fujiwara, Tsuyoshi Ikeda, Mas ...2014 Volume 62 Issue 5 Pages 483-487
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLHere reports new conversions methods of tomato saponins, esculeoside A (1) and a mixture of esculeosides B-1 (2) and B-2 (3), (the latter two were obtained from tomato cans) into pregnane derivative (5) by an alkal treatment followed by acid treatment. Compound 1 or a mixture of 2 and 3 were each refluxed with 1 N KOH to afford a characteristic pyridine steroidal glycoside (4), which was then treated with 2 N HCl–MeOH to afford a pregnane derivative, 3β-hydroxy-5α-pregn-16-en-20-one (5). The results of the above two reactions indicated that tomato saponins are chemically closely related to pregnane hormones. We assume that the assimilated tomato saponins via the small intestine are metabolized into pregnane derivatives, demonstrating various bioactivities such as anti-cancer, anti-osteoporosis, and anti-menopausal disorder activities.View full abstractDownload PDF (846K) Full view HTML -
Yasunori Miyazaki, Tomonobu Uchino, Yoshiyuki Kagawa2014 Volume 62 Issue 5 Pages 488-490
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLWe developed a color difference signal method to evaluate the degree of blending powdered medicines in pharmacies. In the method, the degree of blending is expressed as the relative standard deviation of the color difference signal value (Cb or Cr) of the YCbCr color space after digital photos of the blended medicines are analyzed by image processing. While the method is effective to determine the degree of blending colored medicines, it remains unknown whether it can be applied to uncolored or white-colored medicines. To investigate this, we examined colored diluents to identify an indicator of the degree mixtures are blended. In this study, we applied this method to Pontal® and Prednisolone® powders, which were used as uncolored and white-colored medicines, respectively. Each of these medicines was blended with the colored lactose using a pestle and mortar, and then the uniformity of blending was evaluated. The degree of blending was well-monitored in both mixtures with various blending ratios (1 : 9–9 : 1), showing a sufficient uniformity at 60 rotations of the pestle. Moreover, the Cr values of the mixtures with various blending ratios were correlated with the concentration of active pharmaceutical ingredients in these medicines, which was determined using HPLC. This indicated the usefulness of the color difference signal method for the quantitative determination of medicines. Thus, we demonstrated the applicability and effectiveness of this method to check dispensing powders.View full abstractDownload PDF (447K) Full view HTML -
Kanae Gamo, Takuma Shiraki, Nobuyasu Matsuura, Hiroyuki Miyachi2014 Volume 62 Issue 5 Pages 491-493
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLHesperidin, a flavanone glycoside present abundantly in citrus fruits, is predominantly metabolized to hesperetin-7-O-β-D-glucuronide (H7-OG) and hesperetin-3′-O-β-D-glucuronide (H3′-OG), which exhibit partial agonistic activity towards peroxisome proliferator-activated receptor gamma (PPARγ). Here, in order to understand the mechanism(s) of action of PPARγ transactivation elicited by hesperetin glucuronides, we compared the transactivation activities of PPARγ (ligand-binding domain (LBD)) mutants by hesperetin glucuronides and troglitazone, a thiazolidine-2,4-dione class PPARγ full agonist. The assay results indicated that the mechanisms of activation of PPARγ by hesperetin glucuronides and by troglitazone are distinct, probably due to a difference in the binding sites of these compounds on the PPARγ LBD. Flavanone-class PPARγ partial agonists, luteolin and hesperetin glucuronides, showed similar activation profiles of the PPARγ LBD mutants, even though they have different side chain functionalities.View full abstractDownload PDF (684K) Full view HTML -
Xiaopo Zhang, Yifeng Tan, Youbin Li, Lifeng Jin, Na Wei, Haifeng Wu, G ...2014 Volume 62 Issue 5 Pages 494-498
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLSix new acyclic diterpenoids named Aphanamixins A–F (1–6), together with two known compounds of nemoralisin and nemoralisin C, were isolated from the stem bark of Aphanamixis polystachya (WALL) J. N. BARKER. Their structures were established through a comprehensive analysis of NMR spectroscopic data and high resolution mass spectrometric data. The absolute configurations of carbon stereocenters were determined by means of auxiliary chiral α-methoxy-α-(trifluoromethyl)phenylacetic acid (MTPA) derivatives and circular dichroism (CD), respectively. All the new isolates were tested for their antiproliferative activity against HepG2, AGS, MCF-7, and A-549 cancer cell lines and they exhibited weak cytotoxicities (IC50>10 µM). Moreover, we highlighted that the six new diterpenoids characterized by acyclic skeleton was rarely seen in nature.View full abstractDownload PDF (464K) Full view HTML -
Taishi Kusama, Naonobu Tanaka, Azusa Takahashi-Nakaguchi, Tohru Gonoi, ...2014 Volume 62 Issue 5 Pages 499-503
Published: May 01, 2014
Released on J-STAGE: May 01, 2014
JOURNAL FREE ACCESS FULL-TEXT HTMLFive new bromopyrrole alkaloids, 2-bromokeramadine (1), 2-bromo-9,10-dihydrokeramadine (2), tauroacidins C (3) and D (4), and mukanadin G (5), were isolated from an Okinawan marine sponge Agelas sp. The structures of 1–5 were elucidated on the basis of spectroscopic data and conformational analysis. Mukanadin G (5) has a tricyclic skeleton consisting of a fused tetrahydrobenzaminoimidazole and 2,5-dioxopyrrolidine moieties. Antimicrobial activities of 1–3, and 5 as well as three related known bromopyrrole alkaloids, keramadine (6), tauroacidin A (7), and taurodispacamide A (8) were evaluated.View full abstractDownload PDF (576K) Full view HTML
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