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Volume 61, Issue 11
Displaying 1-15 of 15 articles from this issue
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Regular Articles
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Yao-Jie Shi, Xue-Jiao Song, Xiao Li, Ting-Hong Ye, Ying Xiong, Luo-Tin ...2013 Volume 61 Issue 11 Pages 1099-1104
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
Advance online publication: August 10, 2013JOURNAL FREE ACCESS FULL-TEXT HTMLA series of new 3-amino-5-sulfanyl-1,2,4-triazole and 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives have been synthesized and their cytotoxicities were evaluated on a panel of human cancer cell lines (BxPC-3, H1975, SKOV-3, A875, HCT116, etc.). The best one (compound 5m) exhibited activities with IC50 values ranging from 0.04 to 23.6 µM against nine human cancer cell lines. Further biological evaluation indicated that DNA replication was blocked by treatment with compound 5m in HCT116 cells.View full abstractDownload PDF (541K) Full view HTML -
Sanapalli Subba Reddy, Ramjee Pallela, Dong-Min Kim, Mi-Sook Won, Yoon ...2013 Volume 61 Issue 11 Pages 1105-1113
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
Advance online publication: September 05, 2013JOURNAL FREE ACCESS FULL-TEXT HTMLA series of isatin derivatives, 1-butyl-5/7-chloro/fluoro-3-((4-methoxybenzyl)imino)indolin-2-ones (3a–d), 6-butyl-chloro/fluoro-6H-indolo[2,3-b]quinoxalines (4a–h), and 5/7-chloro/fluoro-3-((4-methoxybenzyl)imino)indolin-2-ones (5a–h) were synthesized and characterized by using Fourier transform (FT)-IR, 1H- and 13C-NMR spectroscopy, mass spectrometric and elemental analysis. The substances were further subjected to in vitro cytotoxicity evaluation against HeLa, SK-BR-3, and MCF-7 cells. The results showed that quinoxalines 4d, 4e, and 4g; and indolin-2-one 5f display significant in vitro cytotoxic activities against HeLa cells and further the compound 4d has resulted in highest cytotoxicity in the entire series studied. In addition, 5f was shown to display substantial activity against all the three cell lines used in the current study.View full abstractDownload PDF (2012K) Full view HTML -
Lakkireddy Srinivasula Reddy, Tirumalareddy Ram Reddy, Reddy Bodireddy ...2013 Volume 61 Issue 11 Pages 1114-1120
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialAn efficient green multi-component reaction (MCR) method has been developed for the synthesis of 2-amino-4-aryl/heteroaryl-6-(pyridin-2-ylthio)pyridine-3,5-dicarbonitrile(s) via a 3-component reaction of aryl aldehyde(s), malononitrile and 2-mercaptopyridine in the presence of K2CO3 under solvent free reaction conditions (SFRC) using grinding technique at room temperature in a single step. The advantages of the present protocol is operationally simple, environmentally benign, solvent-free reaction conditions (SFRC), simple work up, excellent isolated yields of desired products and viable method for large scale applications in pharmaceutical industry. Interestingly, the synthesized compounds showed moderate to excellent antibacterial activities against Gram-positive and Gram-negative bacterial strains.View full abstractDownload PDF (608K) Full view HTML -
Mio Tange, Yusuke Hattori, Makoto Otsuka, Miyako Yoshida, Jun Haginaka ...2013 Volume 61 Issue 11 Pages 1121-1129
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
Advance online publication: August 16, 2013JOURNAL FREE ACCESS FULL-TEXT HTMLThis study aimed to compare the dissolution rate of eight different formulations of ceftriaxone sodium preparation for injection, the original product and seven generic versions. The dissolution time was measured precisely as the point at which the freeze-dried ceftriaxone sodium preparation became a transparent solution on the addition of 0.9% sodium chloride solution. To investigate whether differences in the crystalline structure may explain the differences in dissolution rates, the eight products were subjected to X-ray diffraction (XRD) and differential scanning calorimetry (DSC). Powder surface characteristics were examined, including surface area, amount of water adsorbed, water interactions and morphology. The measurement of near-infrared spectroscopy of powder preparations was conducted, and we predicted dissolution time by partial least squares (PLS). The dissolution time of the eight products were different. There were no differences in XRD and DSC findings between the original and generic products, surface characteristics, i.e., surface area, morphology etc., were different between preparations. On near-infrared (NIR) spectroscopy, a good relationship was demonstrated between the actual and predicted dissolution time for each ceftriaxone preparation. The difference in dissolution time between the eight products was due to differences in powder surface characteristics, such as water interaction and crystal shape. Finally, it was shown that the dissolution rates of the products could be predicted by NIR analysis.View full abstractDownload PDF (3098K) Full view HTML -
Penglong Wang, Yuzhong Zhang, Yawen An, Kuo Xu, Xin Xu, Chao Fu, Jinxu ...2013 Volume 61 Issue 11 Pages 1130-1135
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
JOURNAL FREE ACCESS FULL-TEXT HTMLA new heptapeptide GAGPHGG (OC1) was isolated from Carapax trionycis which was a traditional Chinese medicine (TCM) used for treatment of hepatic diseases. The structure of OC1 was characterized by MS, NMR techniques, together with amino acid sequence analysis. The hepatoprotective activity of OC1 was evaluated in vivo using the CCl4-induced acute liver injury model. Combining the pathological examination and the biochemical assays, OC1 (0.34 mg/kg, hypodermic injection) displayed better hepatoprotective effect than bifendate (100 mg/kg, intragastric administration) against the acute liver injury induced by carbon tetrachloride (CCl4) in mice. Compared with the model group, OC1 could significantly suppress the increase of serum level of aminotransferase (alanine transaminase (ALT) and aspartate aminotransferase (AST)), decrease the formation of malondialdehyde (MDA) and elevate the activity of glutathione peroxidase (GSH-Px) in liver (p<0.01). And the acute toxic test showed that median lethal dose (LD50) of OC1 exceeded 6.8 mg/kg, via hypodermic injection in mice.View full abstractDownload PDF (2021K) Full view HTML -
Kouki Ukida, Takashi Doi, Sachiko Sugimoto, Katsuyoshi Matsunami, Hide ...2013 Volume 61 Issue 11 Pages 1136-1142
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
JOURNAL FREE ACCESS FULL-TEXT HTMLFrom the branches of Schoepfia jasminodora collected in Okinawa, three new dihydrochalcone C-glycosides, one dihydrochalcone di-O-glucopyranoside, two flavanone C-glycosides, one flavanone O-glycoside and one flavone O-glycoside were isolated. Their structures were elucidated by extensive study of one- and two-dimensional NMR spectroscopic data.View full abstractDownload PDF (548K) Full view HTML -
Takeaki Uchimoto, Yasunori Iwao, Hiroaki Hattori, Shuji Noguchi, Shige ...2013 Volume 61 Issue 11 Pages 1143-1148
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
JOURNAL FREE ACCESS FULL-TEXT HTMLThe interaction of the effects of the triglycerin full behenate (TR-FB) concentration and the mixing time on lubrication and tablet properties were analyzed under a two-factor central composite design, and compared with those of magnesium stearate (Mg-St). Various amounts of lubricant (0.07–3.0%) were added to granules and mixed for 1–30 min. A multiple linear regression analysis was performed to identify the effect of the mixing conditions on each physicochemical property. The mixing conditions did not significantly affect the lubrication properties of TR-FB. For tablet properties, tensile strength decreased and disintegration time increased when the lubricant concentration and the mixing time were increased for Mg-St. The direct interaction of the Mg-St concentration and the mixing time had a significant negative effect on the disintegration time. In contrast, any mixing conditions of TR-FB did not affect the tablet properties. In addition, the range of mixing conditions which satisfied the lubrication and tablet property criteria was broader for TR-FB than that for Mg-St, suggesting that TR-FB allows tablets with high quality attributes to be produced consistently. Therefore, TR-FB is a potential lubricant alternative to Mg-St.View full abstractDownload PDF (1310K) Full view HTML -
Dai-Ying Zhou, Kun Zhang, Allan H. Conney, Ning Ding, Xiao-Xing Cui, H ...2013 Volume 61 Issue 11 Pages 1149-1155
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
Advance online publication: August 27, 2013JOURNAL FREE ACCESS FULL-TEXT HTMLEleven curcumin-related compounds containing a benzyl piperidone moiety were synthesized and evaluated for their effects on cultured prostate cancer PC-3 cells, pancreas cancer BxPC-3 cells, colon cancer HT-29 cells and lung cancer H1299 cells. Inhibitory effects of these compounds on the growth of PC-3, BxPC-3, HT-29 and H1299 cells were determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and trypan blue exclusion assay. Compounds benzyl piperidone 2 (P2), P4, P7, 4-bromo-2-fluoro-benzyl piperidone 2 (PFBr2), PFBr3 and PFBr4 (see syntheses and structures in Figs. 1, 2) exhibited potent inhibitory effects on the growth of cultured PC-3, BxPC-3, HT-29 and H1299 cells. The IC50 for these compounds was lower than 2 µM in all four cell lines. PFBr4 was 41-, 36-, 40- and 46-fold more active than curcumin for inhibiting the growth of PC-3, BxPC-3, HT-29 and H1299 cells, respectively. The benzyl piperidone-containing compounds studied also stimulated apoptosis in PC-3 cells. Mechanistic studies indicate that the effects of both curcumin and PFBr4 on PC-3 cells were associated with a decrease in phospho-Akt and phospho-extracellular signal-regulated kinase (Erk)1/2. The present study indicates that P2, P4, P7, PFBr2, PFBr3 and PFBr4 may have useful effects on human cancer cells.View full abstractDownload PDF (818K) Full view HTML -
Supachai Yodkeeree, Pattama Wongsirisin, Wilart Pompimon, Pornngarm Li ...2013 Volume 61 Issue 11 Pages 1156-1165
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
Advance online publication: August 28, 2013JOURNAL FREE ACCESS FULL-TEXT HTMLThe alkaloids isolated from Stephania venosa (S. venosa) have been shown to inhibit the proliferation and to induce the apoptosis of cancer cells. However, the anti-metastatic effect of the alkaloids on cancer cell invasion is unknown. In this study, we investigated the anti-invasive properties of four alkaloids from S. venosa, crebanine (CN), O-methylbulbocapnine (OMBC), tetrahydropalmatine (THP), and N-methyltetrahydropalmatine (NMTHP), in HT1080 human fibrosacroma cells. Treatment of the cells with 15 µg/mL of CN and OMBC reduced the chemo-invasion of HT1080 cells to 45 and 50%, respectively, whereas THP and NMTHP had a negative effect. On the other hand, CN and OMBC had no effect on cell migration. Matrix metalloproteinases (MMPs) and urokinase plasminogen activator (uPA) are the extracellular matrix (ECM) degradation enzymes that play an important role in cancer cell metastasis. Results from zymography and western blot analysis showed that CN and OMBC comparatively reduced MMP-2, MMP-9, MT1-MMP and uPA expression in a dose-dependent manner. However, CN and OMBC had no effect on the activity of collagenase, MMP-2 and MMP-9. We also found that CN and OMBC reduced the nuclear translocation and DNA binding activity of nuclear factor kappa B (NF-κB), which is the expressed mediator of ECM degradation enzymes. These findings demonstrated that CN and OMBC mediated HT1080 cell invasion by the reduction of MMP-2, MMP-9, uPA and MT1-MMP expression, possibly by targeting of NF-κB signaling pathway in the HT1080 cells.View full abstractDownload PDF (1872K) Full view HTML -
Zhong-Zhen Zhou, Guang-Hua Yan, Wen-Hua Chen, Xue-Mei Yang2013 Volume 61 Issue 11 Pages 1166-1172
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
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Supplementary materialThis paper describes an operationally simple, green and efficient approach for the synthesis of 2-hydroxydeoxybenzoins bearing diverse substituents from the microwave-assisted alkali degradation of 3-aryl-4-hydroxycoumarins in water. The latter compounds were readily prepared from the intramolecular Claisen condensation reaction of methyl 2-(2-arylacetoxy)benzoates in the presence of Cs2CO3–acetone, in excellent yields and without laborious workup procedures. This method is highly atom-economic and thus applicable for the large-scale synthesis of 2-hydroxydeoxybenzoins.View full abstractDownload PDF (500K) Full view HTML
Notes
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Tatsuya Iida, Yoshimasa Amano, Motoi Machida, Fumio Imazeki2013 Volume 61 Issue 11 Pages 1173-1177
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
JOURNAL FREE ACCESS FULL-TEXT HTMLIn this study, the removal of acidic functional groups and introduction of basic groups/sites on activated carbons (ACs) by outgassing and ammonia gas treatment were respectively carried out to enhance the nitrate ion adsorption in aqueous solution. Then, the relationships between nitrate ion adsorption and solution pH as well as surface charge of AC were investigated to understand the basic mechanisms of nitrate ion adsorption by AC. The result showed that the nitrate ion adsorption depended on the equilibrium solution pH (pHe) and the adsorption amount was promoted with decreasing pHe. The ACs treated by outgassing and ammonia gas treatment showed larger amount of nitrate ion adsorption than that by untreated AC. These results indicated that, since basic groups/sites could adsorb protons in the solution, the AC surface would be charged positively, and that the nitrate ion would be electrically interacted with positively charged carbon surface. Accordingly, it was concluded that basic groups/sites on the surface of AC could promote nitrate ion adsorption.View full abstractDownload PDF (422K) Full view HTML -
Armelle Tsamo Tontsa, Pierre Mkounga, Fréderic Nico Njayou, José Manau ...2013 Volume 61 Issue 11 Pages 1178-1183
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
JOURNAL FREE ACCESS FULL-TEXT HTMLThree new limonoids, rubescins A–C (1–3), and three known compounds including, havanensin type limonoid TS3 (4), β-sitosterol, and stigmasterol were isolated from the root bark of Trichilia rubescens. Their structures were elucidated by means of extensive spectroscopic analyses, particularly one dimensional (1D)- and 2D-NMR techniques in conjunction with mass spectrometry. Rubescins A–C (1–3) and limonoid TS3 (4) were evaluated for their protective effects against oxidative stress induced in HC-04 cells by H2O2. Compound (1) showed strong inhibitory effects on lactase dehydrogenase (LDH) leakage, being as active (IC50 value of 0.0026 µM) as the positive control quercetin (IC50 value of 0.0030 µM).View full abstractDownload PDF (451K) Full view HTML -
Toru Masaka, Takuya Matsuda, Yingpeng Li, Yuki Koide, Akira Takami, Ke ...2013 Volume 61 Issue 11 Pages 1184-1187
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
Advance online publication: August 23, 2013JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialA new component for the solid phase peptide synthesis of lipopeptide, 2-[(4R,5R)-5-({[(9H-fluoren-9-yl)methoxy]carbonylaminomethyl}-2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]acetic acid (2), was designed and synthesized from (−)-2,3-O-isopropylidene-D-threitol (3) in 4 steps. The key step was the selective alkylation of 3 with benzyl bromoacetate in the presence of Cs2CO3. Vasoactive intestinal peptide (VIP)-lipopeptide (1) incorporating this linker was synthesized by solid phase peptide synthesis.View full abstractDownload PDF (859K) Full view HTML -
Kiminobu Nakamura, Tomohiro Seki, Yuya Egawa, Ryotaro Miki, Yoshiki Od ...2013 Volume 61 Issue 11 Pages 1188-1191
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
Advance online publication: August 21, 2013JOURNAL FREE ACCESS FULL-TEXT HTML
Supplementary materialSupramolecular structures were developed from phenylboronic acid-modified cyclodextrins (PBA-CyDs). The intermolecular interaction between the PBA moiety and the CyD cavity was proved using two dimensional (2D)-NMR and powder X-ray diffraction techniques. PBA-α-CyD formed a head-to-tail supramolecular polymer, whereas PBA-β-CyD formed a head-to-head dimer. The supramolecular structures were disintegrated in the presence of sugars owing to the resulting boronate sugar interactions.View full abstractDownload PDF (518K) Full view HTML -
Xiaoming Yang, Wen Xu, Weijia Zhao, Yahong Zhao, Yumin Yang, Yong Ling2013 Volume 61 Issue 11 Pages 1192-1196
Published: November 01, 2013
Released on J-STAGE: November 01, 2013
JOURNAL FREE ACCESS FULL-TEXT HTMLSalidroside (Sal) is a natural antioxidant extracted from the root of Rhodiola rosea L., a traditional Chinese medicinal plant, which elicits neuroprotective effects in the treatment of ischemic stroke. In an attempt to improve its neuroprotective effects, fluorine substituted Sal analogues were synthesized and their neuroprotective activities against the hypoglycemia and serum limitation induced cell injury in differentiated PC12 cells were evaluated. The target compounds displayed strong protective effects on the cell viability against the damage caused by hypoglycemia and serum limitation, especially for D1, which had a great potency superior to Sal and efficiently inhibited hypoglycemia and serum limitation induced cell nuclear morphologic changes and the increased apoptotic rate in a dose-dependent manner. These new findings may provide potentially important information for further development of Sal analogues and lay the basis for further studies on the cerebral ischemic stroke and neurodegenerative diseases for human clinical treatment.View full abstractDownload PDF (990K) Full view HTML
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