巻号一覧
63 巻, 11 号
選択された号の論文の16件中1～16を表示しています
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Bharati Shivajirao Patil, Hitendra Shaligram Mahajan, Sanjay Javerilal ...2015 年 63 巻 11 号 p. 851-857
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLIn the present work the absorption of flutamide from suppositories containing hydrophilic tamarind alginate microparticles after rectal administration in rats was investigated with the purpose of enhancing bioavailability and to avoid hepatic toxicity. Microparticles were developed by ionic gelation method and optimized using one factorial design of response surface methodology. The optimized batch of microparticles had tamarind gum–sodium alginate (1 : 3) ratio and showed entrapment efficiency 94.969% and mucoadhesion strength 94.646% with desirability of 0.961. Suppositories loaded with microparticles were developed by fusion method using poloxamer 407 and poloxamer 188 in combination as suppository base. Kinetic analysis of the release data of microparticle-loaded suppositories showed time-independent release of drug. Higher values of ‘n’ (>0.89) represent Super Case II-type drug release. The pharmacokinetics of flutamide from flutamide tamarind alginate microparticle-loaded suppository were compared with oral suspension. Cmax of microparticle-loaded suppository was significantly larger than that of oral suspension (1.711 and 0.859 µg/mL, respectively).Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (875K) HTML形式で全画面表示 -
Shoko Takeuchi, Takashi Kojima, Kentaro Hashimoto, Bunnai Saito, Hiroy ...2015 年 63 巻 11 号 p. 858-865
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLDifferent crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability in an anhydrous/hydrate system, are crucial to prevent an undesired transition during the manufacturing process and storage. Only one anhydrous form of T-3256336, a novel inhibitor of apoptosis (IAP) protein antagonist, was discovered during synthesis, and no hydrate form has been identified. In this study, we conducted hydrate screening such as dynamic water vapor sorption/desorption (DVS), and the slurry experiment, and characterized the solid-state properties of anhydrous/hydrate forms to determine the most desirable crystalline form for development. New hydrate forms, both mono-hydrate and hemi-hydrate forms, were discovered as a result of this hydrate screening. The characterization of two new hydrate forms was conducted, and the anhydrous form was determined to be the most desirable development form of T-3256336 in terms of solid-state stability. In addition, the stability of the anhydrous form was investigated using the water content and temperature controlled slurry experiment to obtain the desirable crystal form in the crystallization process. The water content regions of the stable phase of the desired form, the anhydrous form, were identified for the cooling crystallization process.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (1905K) HTML形式で全画面表示 -
Marwa Sayed Salem, Mahmoud Farhat, Asma Omar Errayes, Hassan Mohamed F ...2015 年 63 巻 11 号 p. 866-872
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTML6-(Benzo[d][1,3]dioxol-5-yl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile has been utilized for synthesis of the fused heterocyclic compounds namely thiazolopyrimidines, tetrazolopyrimidine, pyrimidoquinazoline, pyrimidothiazolopyrimidine, pyrimidothiazolotriazine and pyrrolothiazolopyrimidine derivatives. The newly synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, and mass spectral data. Antioxidant activities of all synthesized compounds were investigated.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (615K) HTML形式で全画面表示 -
Ling Feng, Yang Li, Zhi-fang Song, Hui-jing Li, Qi-yong Huai2015 年 63 巻 11 号 p. 873-881
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLMany curcuminoid derivatives have been reported to have multiple biological activities. The aim of this study was to improve the biological activity of curcuminoids by synthesizing 16 new derivatives which combined cinnamic acids with curcuminoids, and we also analyzed the structure–activity relationship of the new compounds. Almost all the new compounds showed encouraging activity, especially compound 7g. It had much better antioxidant activity than curcuminoids and Vitamin C (VC), and also had the most significant antibacterial activity, which was 5-folder better than ampicillin (one of the best marketed antibiotics) with a minimum inhibitory concentration (MIC) of 0.5 µg/mL against Gram-positive cocci (Staphylococcus aureus and Streptococcus viridans) as well as Escherichia coli and 0.6 µg/mL against Enterobacter cloacae. Compound 7g also showed the greatest anticancer activity with a much lower IC50, which was 0.51 µM against MCF-7, 0.58 µM against HepG-2, 0.63 µM against LX-2, and 0.79 µM against 3T3. The results suggest that these compounds have promising potential as candidates for the treatment of cancer and thus further studies are warranted.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (573K) HTML形式で全画面表示 -
Yan Han, Chunlei Wu, Haifeng Lv, Na Liu, Huaying Deng2015 年 63 巻 11 号 p. 882-889
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLNovel tranylcypromine/hydroxylcinnamic acid hybrids 15a, b, and 19a–l were designed and synthesized by connecting tranylcypromine with hydroxylcinnamic acid, and their biological activities were evaluated. The in vitro assay of their inhibitory activities against lysine-specific demethylase 1 (LSD1) showed that most of the target compounds displayed high potency with IC50 values ranging from submicromolar to single-digit micromolar levels. In particular, compound 19l had robust, selective LSD1 inhibitory activity, which was obviously higher than the inhibitory activity against homologues monoamine oxidase-A (MAO-A) and MAO-B, respectively. Furthermore, the most potent compound 19l selectively inhibited cancer cell but not nontumor colon cell proliferation in vitro. In addition, compound 19l also dose-dependently increased the expression of H3K4me2 at the cellular level. Our findings suggest that tranylcypromine/hydroxylcinnamic acid hybrids as LSD1 inhibitors may hold great promise as therapeutic agents for the treatment of human cancers.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (763K) HTML形式で全画面表示 -
Saori Otoguro, Yoshihiro Hayashi, Takahiro Miura, Naoto Uehara, Shunic ...2015 年 63 巻 11 号 p. 890-900
発行日: 2015/11/01
公開日: 2015/11/01
[早期公開] 公開日: 2015/08/15
ジャーナル フリー HTMLThe stress distribution of tablets after compression was simulated using a finite element method, where the powder was defined by the Drucker–Prager cap model. The effect of tablet shape, identified by the surface curvature, on the residual stress distribution was investigated. In flat-faced tablets, weak positive shear stress remained from the top and bottom die walls toward the center of the tablet. In the case of the convexly curved tablet, strong positive shear stress remained on the upper side and in the intermediate part between the die wall and the center of the tablet. In the case of x-axial stress, negative values were observed for all tablets, suggesting that the x-axial force always acts from the die wall toward the center of the tablet. In the flat tablet, negative x-axial stress remained from the upper edge to the center bottom. The x-axial stress distribution differed between the flat and convexly curved tablets. Weak stress remained in the y-axial direction of the flat tablet, whereas an upward force remained at the center of the convexly curved tablet. By employing multiple linear regression analysis, the mechanical properties of the tablets were predicted accurately as functions of their residual stress distribution. However, the multiple linear regression prediction of the dissolution parameters of acetaminophen, used here as a model drug, was limited, suggesting that the dissolution of active ingredients is not a simple process; further investigation is needed to enable accurate predictions of dissolution parameters.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (3429K) HTML形式で全画面表示 -
Yoshinori Onuki, Naoki Hasegawa, Akihiro Horita, Naomi Ueno, Chihiro K ...2015 年 63 巻 11 号 p. 901-906
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTML
電子付録The physical stability of pharmaceutical emulsions is an important quality attribute to be considered. To obtain a better understanding of this issue, this study investigated the contribution of the state of water to the physical stability of pharmaceutical emulsions. The key technology to evaluate the state of water was magnetic resonance imaging (MRI). For sample preparation, model emulsions with different formulation variables (surfactant content, water content, and hydrophilic–lipophilic balance) were prepared. The T1 relaxation time, diffusion coefficient, and viscosity were measured as physical properties. The physical stability of the samples was evaluated using apparent diffusion coefficient maps acquired by MRI. Data analysis of the observed data was performed using the nonlinear response surface method and Kohonen’s self-organizing map (SOM). It was determined that, depending on the formulation variables, the state of water was substantially changed and it played a significant role in the physical stability. SOM analysis successfully classified the conditions of formulation variables into four distinct clusters in terms of the similarity of the physical properties of the resultant emulsions, and then clarified the characteristics of the stable emulsions. This study provided us with a comprehensive understanding of the formulation variables, physical properties, and stability concerning the preparation of the model emulsion.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (1593K) HTML形式で全画面表示 -
Young Taek Han, Zheng Wang, Eun Ju Bae2015 年 63 巻 11 号 p. 907-912
発行日: 2015/11/01
公開日: 2015/11/01
[早期公開] 公開日: 2015/08/20
ジャーナル フリー HTMLConcise and efficient synthesis of the proposed structure of damaurone D is accomplished in five steps without protection-deprotection operations. The key feature of our synthesis includes a versatile aldol reaction of the benzofuranone, provided by selective α-halogenation and intramolecular O-alkylation. However, the H- and C-NMR spectral data of the synthesized damaurone D did not agree with previous reports. The structure of the synthesized damaurone D was confirmed using combined two dimensional (2D)-NMR analysis, including heteronuclear single quantum coherence (HSQC), heteronuclear multiple bond connectivity (HMBC), and nuclear Overhauser effect spectroscopy (NOESY). The synthesized damaurone D was found to exhibit potent anti-inflammatory activity in murine macrophage RAW264.7 cells, which was demonstrated by the findings that damaurone D treatment in cells resulted in the inhibition of lipopolysaccharide (LPS)-stimulated inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression and nitrite production.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (575K) HTML形式で全画面表示 -
Yasufumi Fuchi, Shigeki Sasaki2015 年 63 巻 11 号 p. 913-919
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTML8-Nitroguanosine is formed by the nitration of guanosine, and has been conventionally classified as a genotoxic material. Recently, 8-nitroguanosine 3′,5′-cyclic monophosphate (8-nitro-cGMP) has become of great interest due to its biological role as an intracellular signaling molecule. In an attempt to develop recognition molecules for 8-nitroguanosine, we have determined a 1,3-diazaphenoxazine nucleoside derivative (nitroG-grasp) bearing a thiol group with a urea linker, which efficiently displaces the nitro group through the formation of multiple hydrogen-bonded complexes with 8-nitroguanosine. However, a drawback of this capture molecule was that the displacement efficiency was not sufficient to capture 8-nitroguanosine in water. Taking into account that both the flexibility of the linker and the pKa value of the thiol group are determinants of the reactivity, new nitroG-grasp molecules were designed to have a fixed linker structure with different pKa values. Compared to the previous nitroG-grasp, the new compounds with the (2-aminophenyl)methanethiol or the propylene acetal of 3-amino-1-mercaptopropan-2-one unit have exhibited more than 10–100 times faster reactivity in the aqueous media. These compounds may be potential components to construct new nitroG-grasp molecules to capture 8-nitro-cGMP in the biological systems.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (952K) HTML形式で全画面表示 -
Yosuke Taniguchi, Akira Tomizaki, Nozomu Matsueda, Hidenori Okamura, S ...2015 年 63 巻 11 号 p. 920-926
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLThis paper reports the preparation of 14-mer triplex-forming oligonucleotides (TFOs) containing a 2-O-methyl-1-β-phenyl-α-propargyl-ribose unit, which was conjugated with azide-modified molecules via a click reaction. Modification of these TFOs with pyrene assisted triplex formation, improving the stability of the triplex DNA and the anti-proliferative effects against A549 cells.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (2760K) HTML形式で全画面表示
Notes
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Dong Gu Lee, Ah Young Lee, Kyung-Tack Kim, Eun Ju Cho, Sanghyun Lee2015 年 63 巻 11 号 p. 927-934
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLFour phytochemical constituents were isolated from Panax ginseng root by repeated column chromatography (CC), medium pressure liquid chromatography (MPLC), high-speed counter current chromatography (HSCCC), and semi-preparative HPLC. Their structures were elucidated as the dammarane-type triterpene saponins ginsenoside-Rg18 (1), 6-acetyl ginsenoside-Rg3 (2), ginsenoside-Rs11 (3), and ginsenoside-Re7 (4) based on spectral data. Compounds 1–4 from P. ginseng root were new compounds from nature. They showed good hydroxyl radical scavenging activity and anti-bacterial activity against Escherichia coli and Staphylococcus aureus. However, they did not show any anti-inflammatory activity. In addition, they inhibited the growth of adenocarcinoma gastric stomach cells. Among them, ginsenoside-Rs11 (3) showed the best anti-oxidative, anti-bacterial, and anti-cancer activities.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (387K) HTML形式で全画面表示 -
Nobuko Mibu, Kazumi Yokomizo, Hatsumi Aki, Norimasa Ota, Hiroyuki Fuji ...2015 年 63 巻 11 号 p. 935-944
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTML
電子付録As one of our projects, we here report some new molecular modifications of 2,4,6-trichloro-1,3,5-triazine (TCTAZ: 1) to symmetrical 2,4,6-trialkoxy- or 2,4,6-triaryloxy-substituted 1,3,5-triazine (TAZ) molecules, as well as the results of anti-herpes simplex virus type 1 (anti-HSV-1) activity evaluation of synthesized 2,4,6-trisubstituted TAZ derivatives. Among the tested 2,4,6-trisubstituted TAZ derivatives, we reconfirmed that a C3-symmetrical TAZ derivative, 4e, shows the highest level of anti-HSV-1 activity with a good selectivity index. In this paper, we also report the results of the preparation of newly targeted TAZ derivatives and the structure–activity relationships (SARs) of these trialkoxy-substituted TAZ derivatives and related compounds. The sugar recognition properties of C3-symmetrical TAZ derivative 4e are also described.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (772K) HTML形式で全画面表示 -
Nguyen Manh Cuong, Tran Thu Huong, Pham Ngoc Khanh, Nguyen Van Tai, Vu ...2015 年 63 巻 11 号 p. 945-949
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLTwo new dimeric monoterpene-linked coumarin glucosides, paratrimerins A (1) and B (2), and three known coumarins, 6-(6-hydroxy-3,7-dimethylocta-2,7-dienyl)-7-hydroxycoumarin (3), ostruthin (4), and ninhvanin (5), were isolated from the roots and stems of Paramignya trimera (OLIV.) GUILL. collected in Khanh Hoa province, Vietnam. Compound 1 comprises two 7-O-β-D-glucopyranoside coumarins linked at positions 6,6′ via a 1,3,4,4-tetrasubstituted cyclohexene containing a monoterpene bridge, whereas compound 2 is a β-D-apiofuranosyl(1→6)-β-D-glucopyranosyl derivative of 1. The chemical structures of these compounds were determined by one dimensional (1D) and 2D-NMR and high resolution-electrospray ionization (HR-ESI)-MS spectroscopy.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (556K) HTML形式で全画面表示 -
Thi Hong Van Le, Gwang Jin Lee, Huynh Kim Long Vu, Sung Won Kwon, Ngoc ...2015 年 63 巻 11 号 p. 950-954
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLChemical and pharmacological studies of Panax vietnamensis (Vietnamese ginseng; VG) have been reported since its discovery in 1973. However, the content of each saponin in different parts of VG has not been reported. In this study, 17 ginsenosides in the different underground parts of P. vietnamensis were analyzed by HPLC/evaporative light scattering detector (ELSD). Their contents in the dried rhizome, radix, and fine roots were 195, 156, and 139 mg/g, respectively, which were extremely high compared to other Panax species. The content of protopanaxatriol (PPT)-type saponins were not much different among underground parts; however, the content of protopanaxadiol (PPD)- and ocotillol (OCT)-type saponins were greatly different. It is noteworthy that the ginsenoside pattern in the fine roots is different from other underground parts. In particular, despite the content of PPD-type saponins being the highest in the fine roots, which is similar to other Panax species, the total content of saponins was the lowest in the fine roots, which is different from other Panax species. The ratios of PPT : PPD : OCT-type saponins were 1 : 1.7 : 7.8, 1 : 1.6 : 5.5, and 1 : 4.8 : 3.3 for the rhizome, radix, and fine roots, respectively. OCT-type saponins accounted for 36–75% of total saponins and contributed mostly to the difference in the total saponin content of each part.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (779K) HTML形式で全画面表示 -
Hee Jin Jung, Hyun Ah Jung, Byung-Sun Min, Jae Sue Choi2015 年 63 巻 11 号 p. 955-960
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTMLTwo new compounds (2, 3) and 20 known compounds (1, 4–22) were isolated from the heartwood of Juniperus chinensis LINNE (Cupressaceae), and their structures were elucidated as 9′-methoxycalocedrin (1); α-methyl artoflavanocoumarin (2); 5,7,4′-trihydroxy-2-styrylchromone (3); cedrol (4); widdrol (5); savinin (6); calocedrin (7); 10-oxowiddrol (8); 12-hydroxywiddrol (9); (+)-naringenin (10); vanillic acid methyl ester (11); (+)-taxifolin (12); (+)-aromadendrin (13); kaempferol (14); quercetin (15); (7S,8R)-dihydro-3′-hydroxy-8- hydroxymethyl-7-(4-hydroxy-3-methoxyphenyl)-1′-benzofuranpropanol (16); styraxlignolide C (17); protocatechuic acid (18); vanillic acid (19); (7R,8S)-dihydro-3′-methoxy-8-hydroxymethyl-7-(4-hydroxy-3-methoxyphenyl)-1′-benzofuranpropanol 4-O-β-D-glucopyranoside (20); (7S,8S)-dihydro-3′-hydroxy-8-hydroxymethyl-7-(4-hydroxy-3-methoxyphenyl)-1′-benzofuranpropanol 4-O-α-L-rhamnopyranoside (21); and (+)-catechin (22) on the basis of spectroscopic evidence. The new compounds (2, 3) exhibited good inhibitory activities against β-site amyloid precursor protein cleaving enzyme 1 (BACE1), with IC50 values of 6.25, and 11.91 µM, respectively.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (547K) HTML形式で全画面表示 -
Ming Zhang, Shun-ichi Wada, Fuyuki Amemiya, Takumi Watanabe, Masakatsu ...2015 年 63 巻 11 号 p. 961-966
発行日: 2015/11/01
公開日: 2015/11/01
ジャーナル フリー HTML
電子付録The synthesis of lentztrehalose A, a naturally occurring trehalose derivative exhibiting various biological activities including autophagy-inducing activity, was achieved. The synthesis commenced with the selective protection of hydroxyl groups of commercially available trehalose, followed by the introduction of the side chain moiety by two methods: 1) prenylation and successive diastereoselective dihydroxylation; or 2) etherification by opening of the chiral epoxide. The present synthetic study clarified the unreported absolute configuration of the secondary alcohol part in the side chain portion.Graphical Abstract Fullsize Image抄録全体を表示PDF形式でダウンロード (619K) HTML形式で全画面表示
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