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Volume 60, Issue 10
Displaying 1-19 of 19 articles from this issue
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Regular Articles
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Xiaoying Cao, Jianning Geng, Suwen Su, Linan Zhang, Qian Xu, Li Zhang, ...2012 Volume 60 Issue 10 Pages 1227-1233
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
Advance online publication: August 01, 2012JOURNAL FREE ACCESSA novel drug delivery system of doxorubicin (DOX)-loaded Zein in situ gel for interstitial chemotherapy was investigated in this study. The possible mechanisms of drug release were described according to morphological analysis by optical microscopy and scanning electronic microscope (SEM). In vitro and in vivo anti-tumor activity studies showed that DOX-loaded Zein in situ gel was superior to DOX solution. Local pharmacokinetics in tumor tissue was studied by quantitative analysis with confocal laser scanning microscopy (CLSM) combined with microdialysis technology. A pharmacokinetics mathematical model of DOX-loaded Zein in situ gel in tumors was then built.View full abstractDownload PDF (3600K) -
Huaping Zhang, Hashim Motiwala, Abbas Samadi, Victor Day, Jeffrey Aub& ...2012 Volume 60 Issue 10 Pages 1234-1239
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESS
Supplementary materialIn our recent publication on bioactive guided isolation of compounds from Physalis longifolia (Solanaceae) novel anti-proliferative agents withalongolides A (4) and B (5), and their highly cytotoxic analogues, withalongolide A 4,19,27-triacetate (4a) and withalongolide B 4,19-diacetate (5a) were elucidated. In this study, the two lead compounds (4, 5) were re-isolated in gram quantities for the purpose of further analogue preparation and in vivo testing that would continue to probe structure–activity relationships. During this process, two additional withanolides, named withalongolides O (1) and P (2), were elucidated. Their structures were determined by spectroscopic techniques with 1 being subsequently confirmed by X-ray crystallographic analysis. Utilizing a MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium] viability assay, withalongolide O (1) and its 4,7-diaceatate (1a), both containing the functionalities of Δ2-1-oxo- in A ring, a 5β,6β-epoxy in B ring, and a lactone ring in the nine-carbon side chain, exhibited potent cytotoxicity against human head and neck squamous cell carcinoma (JMAR and MDA-1986), melanoma (B16F10 and SKMEL-28), and normal fetal lung fibroblast (MRC-5) cells with IC50 values in the range between 0.15 and 2.95 µM. In addition, the previously reported α orientation of 7-acetate group in acnistins C and D should be revised to the β orientation on the basis of NMR data comparison.View full abstractDownload PDF (668K) -
Keita Kondo, Toshiyuki Niwa, Kazumi Danjo2012 Volume 60 Issue 10 Pages 1240-1248
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSThis report describes a new disintegration tester that can determine not only the disintegration time of orally rapidly disintegrating tablets (ODT), but also the disintegration behavior and mechanism. Using the tester, the disintegration properties of the tablets prepared in a previous study were examined. The purpose of this study is to confirm the utility of the tester as an instrument for evaluating the disintegration properties of ODT and determine relations among time, behavior and mechanism of the disintegration. Results demonstrated that in vitro disintegration time in the tester is similar to that in the commercial disintegration tester for ODT and is highly correlated with oral disintegration time. Observations of disintegration process revealed that a difference in disintegration behavior between tablets compressed at 50–75 MPa and 100 MPa; the disintegration behavior of the tablets were designated immediate disintegrating type and gradual disintegrating type, respectively. The dynamic swelling profile and water absorption profile indicated that the disintegration mechanism of the tablets involved wicking action induced by swelling of the disintegrant; the disintegration time was closely related to the initial rates of swelling and water absorption. Furthermore, the mechanism of water absorption of tablets compressed at 50–75 MPa and 100 MPa shows anomalous diffusion and case-II transport, respectively. The shift in this mechanism is consistent with differences in disintegration time and behavior between the tablets. These findings suggest that information on disintegration properties obtained by our tester is useful for understanding of disintegration phenomena of ODT.View full abstractDownload PDF (2397K) -
Roberto Ruiz-Caro, Manuel Gago-Guillan, Francisco Javier Otero-Espinar ...2012 Volume 60 Issue 10 Pages 1249-1257
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
Advance online publication: August 02, 2012JOURNAL FREE ACCESSMucoadhesive chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) tablets for gastric drug delivery of acyclovir (ACV) have been developed in order to improve the ACV oral bioavailability. Swelling, bioadhesive and dissolution studies were carried out in two acidic media (pH 1.5 and 4) in order to determine the tablets behaviour in both fed and fasted states. All the designed tablets showed good mucoadhesive properties on gastric mucosa due to the presence of CS and/or HPMC. In vitro dissolution of ACV from tablets was influenced by the swelling behaviour of each polymer. All data release of the studied tablets fitted to Hopfenberg model, which describes drug release from tablets displaying heterogeneous erosion. HPMC and CS/HPMC tablets revealed a sustained release for 24 h, but a complete dissolution of the tablets was not produced at this time. On the contrary, tablets which contained only CS as polymer were able to release the total amount of ACV for 4 h, due to the CS imbibition and erosion processes in pH 1.5 medium. These results allowed us to conclude that CS is the excipient to be chosen to obtain gastroretentive formulations, due to its demonstrated gastric compatibility.View full abstractDownload PDF (1970K) -
Mamoru Haratake, Eisuke Hatanaka, Takeshi Fuchigami, Makoto Akashi, Mo ...2012 Volume 60 Issue 10 Pages 1258-1263
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSIn this study, hydrophilic porous polymer beads with phosphonic acid groups (PGMA-EGDMA-TTA-MP) were synthesized, and assessed as a radioactive strontium-90 sequestrant for the treatment of the radiation emergency. Strontium ions were rapidly absorbed into the blood from the gastrointestinal (GI) tract after oral administration to rats, and distributed to the target organ, i.e., bones. Over 40% of the administered strontium was absorbed into the blood, while the remainder was discharged in the feces within 48 h after the administration. When the PGMA-EGDMA-TTA-MP beads were administered to rats subsequent to the strontium solution, the strontium had accumulated less in the femur. Consequently, the oral administration of the PGMA-EGDMA-TTA-MP beads was effective in suppressing the absorption of strontium from the GI tract.View full abstractDownload PDF (664K) -
Syuji Iwanaga, Tsutomu Warashina, Toshio Miyase2012 Volume 60 Issue 10 Pages 1264-1274
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSEleven new triterpene saponin components (1–11) were isolated from the MeOH extract of pericarp of Akebia trifoliata (THUNB.) KOIDZ. Each of their structures was determined using NMR techniques and mass spectrometry.View full abstractDownload PDF (596K) -
Satoshi Kubo, Minpei Kuroda, Yukiko Matsuo, Daichi Masatani, Hiroshi S ...2012 Volume 60 Issue 10 Pages 1275-1282
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSChemical investigation of the seeds of Adonis aestivalis has led to the isolation of a new cardenolide (3β,5α,14β,17β-tetrahydroxycard-20,22-enolide) (1), two new glycosides (2, 3) of 1, and a new strophanthidin hexaglycoside (4), together with a known compound, strophanthidin 3-O-β-D-glucopyranoside (5). The structures of 1–4 were determined by 1D- and 2D-NMR spectroscopic analysis and the results of hydrolytic cleavage. The isolated compounds (1–5) were examined for their cytotoxic activity against neoplastic HSC-2, HSC-3, HSC-4, and HL-60 cells, as well as HGF, HPLF, and HPC normal cell lines. Compounds 2, 4, and 5 were found to display selective cytotoxicity toward malignant tumor cell lines. Although the morphological observations of HL-60 and HSC-2 cell deaths by 2, 4, and 5 revealed changes characteristic of apoptosis, neither DNA degradation nor activation of caspase-3 was observed. Our findings demonstrated that 2, 4, and 5 may trigger caspase-3-independent apoptotic cell death in HL-60 and HSC-2 cells.View full abstractDownload PDF (1098K) -
Pattama Wongsirisin, Supachai Yodkeeree, Wilart Pompimon, Pornngarm Li ...2012 Volume 60 Issue 10 Pages 1283-1289
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
Advance online publication: August 03, 2012JOURNAL FREE ACCESSIn this study, we focused the effects of crebanine, an alkaloid isolated from the tuber of Stephania venosa, on various human cancer cells. Crebanine treatment was found to significantly inhibit the proliferation of human leukemic cells (HL-60, U937 and K562), human fibrosarcoma cells (HT1080) and cervix cancer cell lines (KB-3-1 and KB-V1), of which HL-60 cells were the most sensitive to its treatment. In contrast, crebanine caused much less toxicity in human normal fibroblast cells. Our results demonstrated that crebanine mediated cell cycle arrest at G0/G1 phase and this was associated with down-regulation of cyclins A and D. In addition, crebanine induced apoptosis, which was detected by observation of the membrane phospholipid exposure in flow cytometry. Its induction of apoptosis was accompanied by an increase in cleavage of caspase-3, -8, -9 and poly(ADP-ribose) polymerase (PARP), and was attributable to the augmentation of Bax/Bcl proteins level. Crebanine also decreased mitochondrial membrane potential. Taken together, crebanine exerts anti-proliferative effects on human cancer cells through the induction of cell cycle arrest at the G1 phases and apoptosis. Our results suggest that crebanine is a promising new candidate as a chemotherapeutic agent for cancer therapy.View full abstractDownload PDF (3199K) -
Amal Abdel Haleem Mohamed Eissa, Gamal Abd El-Hakeem Soliman, Moayad H ...2012 Volume 60 Issue 10 Pages 1290-1300
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
Advance online publication: August 02, 2012JOURNAL FREE ACCESSSimple, three classes of new anthranilic acid derivatives were aimed at, synthesized and tested for their toxicity, anti-inflammatory, analgesic, antipyretic activity. Also, their potential protective role against ulcerative colitis in rats was performed. Furthermore, their effect on liver and kidney functions was detected through measurement of the serum level of alanine transaminase (ALT), aspartate aminotransferase (AST), urea, creatinine and other parameters. Compounds 4, 5, 6b, 6c, 7c and 7e showed significant anti-inflammatory activity. From those 6b and 7e best improved the inflammatory indices even producing better reduction in the intensity of lesion score, ulcer area and wet weight/length ratio and showed good analgesic activity. Fortunately, none of the tested compounds showed any hepatotoxicity or nephrotoxicity. None of the tested compounds showed any antipyretic activity. Conclusively, presence of a phenyl ring in the substituent added is a must, since any alteration in its nature led to decrease in activity. Also, the presence of an extra halogen in addition to the one already embedded in the main structure was detrimental to activity.View full abstractDownload PDF (789K) -
Shoji Maehara, Partomuan Simanjuntak, Chinami Kitamura, Kazuyoshi Ohas ...2012 Volume 60 Issue 10 Pages 1301-1304
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
Advance online publication: August 02, 2012JOURNAL FREE ACCESSWe report that an endophytic filamentous fungus species of the genus Diaporthe isolated from Cinchona ledgeriana (Rubiaceae) produces Cinchona alkaloids (quinine, quinidine, cinchonidine, and cinchonine) upon cultivation in a synthetic liquid medium. This study provides evidence that Cinchona alkaloids are produced not only in Cinchona plant cells, but also in the endophytic microbe cells, and will help to elucidate the relationship between endophytic microbes and their host plants.View full abstractDownload PDF (790K) -
Azza Taher Taher, Amira Atef Helwa2012 Volume 60 Issue 10 Pages 1305-1313
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
Advance online publication: August 03, 2012JOURNAL FREE ACCESSThe synthesis of some new 4-chloro-pyrimidine-5-carbonitriles (3b–d), 4-substituted-amino-pyrimidine-5-carbonitriles (4a–g), trioxo and dioxo-thiazolo[3,2-a]pyrimidine-6-carbonitriles (5a–c and 6a–h) have been described. The obtained compounds were evaluated for their in-vitro antitumor activity. A single dose (10 µM) of the test compounds was used in the National Cancer Institute (NCI) 60 cell lines panel assay. Compounds 3c and 4f showed high inhibitory activity against leukemia, whereas, compounds 3b and 4d, g displayed moderate activity. On the other hand, all compounds were screened for their in-vitro antibacterial and antifungal activities. Compounds 3d and 4b exhibited significant antibacterial activity against Staphylococcus aureus. Compound 4e showed two folds inhibitory activity against Entrobacter aerogener compared with the reference drug Tobramycin.View full abstractDownload PDF (880K)
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Masateru Ono, Yoshie Takatsu, Tetsuya Ochiai, Shin Yasuda, Yoichiro Ni ...2012 Volume 60 Issue 10 Pages 1314-1319
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSTwo new norlanostane-type triterpenoid glycosides and a new phenylpropanoid glycoside were isolated from the bulbs of Scilla scilloides DRUCE (Liliaceae), along with two known alkaloids. Their chemical structures were determined on the basis of spectroscopic data as well as chemical evidence.View full abstractDownload PDF (777K) -
Hikaru Sugihara, Hiromitsu Yamamoto, Yoshiaki Kawashima, Hirofumi Take ...2012 Volume 60 Issue 10 Pages 1320-1323
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSThe gastrointestinal transition of mucoadhesive drug carriers may be affected by food intake, since food changes the physiological conditions of the gastrointestinal tract, and the food content itself is a physical obstruction for the drug carriers. Here we investigated the effects of food intake on the gastrointestinal transition and mucoadhesive function of submicron-sized chitosan-coated liposomes (ssCS-Lip). The stomach and small intestine were removed after oral administration of ssCS-Lip and non-coated liposomes (ssLip) containing fluorescent dye to fasted or fed rats, and retentive properties were quantitatively confirmed by measuring the amount of dye in each part of the gastrointestinal tract. Both types of liposome were retained in the stomach at approx. 40% in the fed rats at 1 h after oral administration, whereas transitions in the intestine were reduced compared to the fasted rats. However, the transition of ssCS-Lip in intestine was prolonged compared to ssLip even, in the fed state. The mucoadhesive behavior of ssCS-Lip was evaluated by confocal laser scanning microscopy. The ssCS-Lip tended to penetrate into the mucosal part of the intestine, and in addition, ssCS-Lip was detected in the basolateral side in both conditions, and therefore the mucopenetrative function was confirmed in the fed condition. Based on these results, we confirmed that ssCS-Lip shows a predominant gastrointestinal transition and mucopenetration, even after food intake.View full abstractDownload PDF (951K) -
Chao Huang, Wei Li, Fenghua Ma, Qin Li, Yoshihisa Asada, Kazuo Koike2012 Volume 60 Issue 10 Pages 1324-1328
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSChemical investigation on the roots of Tinospora sagittata resulted in the isolation of three novel cis-clerodane diterpenoids, tinospinosides D, E, and tinospin E, together with two known compounds, columbin and columbin glucoside, and their structures were determined by extensive spectroscopic analyses, chemical reactions and computer-assisted calculations. The inhibitory activity of the isolated compounds and their chemical derivatives on nitric oxide production in lipopolysaccharide and interferon-γ activited J774.1 macrophage-like cells was also evaluated.View full abstractDownload PDF (804K) -
Nguyen Huu Tung, Yukihiro Shoyama2012 Volume 60 Issue 10 Pages 1329-1333
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
Advance online publication: August 06, 2012JOURNAL FREE ACCESSGinsenosides, the major active component of American ginseng, were analyzed using eastern blotting with anti-ginsenoside Rb1 and Rg1 monoclonal antibodies (MAbs). Immunoassay-guided fractionation of the methanol extract of American ginseng and column chromatography led to the isolation of two new minor dammarane-type saponins, named quinquenosides Ja (1) and Jb (2). Their structures were elucidated to be 6-O-[α-L-rhamnopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-[β-D-glucopyranosyl(1→4)-β-D-glucopyranosyl]-3β,6α,12β,20β-tetrahydroxydammar-24-ene (1) and 3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-{[α-L-arabinofuranosyl(1→6)-β-D-glucopyranosyl](1→6)-β-D-glucopyranosyl}-3β,12β,20β-trihydroxydammar-24-ene (2) on the basis of chemical and spectroscopic methods.View full abstractDownload PDF (1714K) -
Hikaru Yoshimura, Kohei Eto, Keisuke Takahashi, Jun Ishihara, Susumi H ...2012 Volume 60 Issue 10 Pages 1334-1339
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSAn effective method for the protection of carboxylic acids with a triisopropylsiloxymethyl (TIPSOCH2) group is described. The reactions of various carboxylic acids with C12H25SCH2OTIPS in the presence of CuBr2, Et3N, and molecular sieves 4A afford the corresponding triisopropylsiloxymethyl esters in good yields.View full abstractDownload PDF (724K) -
Hiromasa Yokoe, Kentaro Noboru, Yuki Manabe, Masahiro Yoshida, Hirofum ...2012 Volume 60 Issue 10 Pages 1340-1342
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
Advance online publication: July 25, 2012JOURNAL FREE ACCESS
Supplementary materialAn enantioselective synthesis of 8-epi-xanthatin (9) has been accomplished starting from the bicyclic lactone 3, which has been used for the synthesis of other xanthanolides, sundiversifolide (4) and diversifolide (5), through a synthetic route without the use of a selenium species. Additionally we have evaluated antimicrobial activities of five natural xanthanolides and their derivatives. Although the synthetic xanthanolides did not show any activity against methicillin-resistant Staphylococcus aureus (MRSA), some of the synthetic intermediates did exhibit moderate antimicrobial activities.View full abstractDownload PDF (568K) -
Daisuke Sawada, Yuya Tsukuda, Kaori Yasuda, Toshiyuki Sakaki, Hiroshi ...2012 Volume 60 Issue 10 Pages 1343-1346
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSA previous report has demonstrated the existence of a C4-hydroxylated vitamin D2 metabolite in serum of rats treated with pharmacological doses of vitamin D2. However, the biological significance and metabolic fate of this metabolite have not been described. To explore its potential biological activities, we therefore synthesized 1α,4α,25-trihydroxyvitamin D3 and its diastereoisomer, 1α,4β,25-trihydroxyvitamin D3, using Trost Pd-mediated coupling reaction, and studied their vitamin D receptor (VDR) binding affinity, osteocalcin promoter transactivation activity, and their further metabolism by human CYP24A1 as well as by human liver microsomal fraction based on CYP- and UDP-glucuronosyltransferases (UGTs)-reactions.View full abstractDownload PDF (624K) -
Yukiko Yamashita-Higuchi, Sachiko Sugimoto, Katsuyoshi Matsunami, Hide ...2012 Volume 60 Issue 10 Pages 1347-1350
Published: October 01, 2012
Released on J-STAGE: October 01, 2012
JOURNAL FREE ACCESSFrom the leaves of Grevillea robusta, compounds whose NMR data were superimposable on those of robustasides B and C were isolated along with two new compounds, (E)-2,5-dihydroxycinnamic acid esters of arbutin and D-glucose, and two known compounds, robustaside A and (E)-2,5-dihydroxycinnamic acid. The structures of robustasides B and C were not arbutin caffeates, being revised to arbutin (E)-2,5-dihydroxycinnamic acid esters.View full abstractDownload PDF (575K)
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