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  • 1
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    Online Resource
    Anti-Bovine Viral Diarrhoea Virus and Hepatitis C Virus Activity of the Cyclooxygenase Inhibitor SC-560
    SAGE Publications ; 2009
    In:  Antiviral Chemistry and Chemotherapy Vol. 20, No. 1 ( 2009-08), p. 47-54
    Details
    In: Antiviral Chemistry and Chemotherapy, SAGE Publications, Vol. 20, No. 1 ( 2009-08), p. 47-54
    Abstract: A number of compounds were examined for their inhibitory effect on bovine viral diarrhoea virus (BVDV) replication in cell cultures and found that some cyclooxygenase (COX) inhibitors had antiviral activity against the virus. Methods: Determination of compounds for their anti-BVDV activity was on the basis of the inhibition of virus-induced cytopathogenicity in Mardin–Darby bovine kidney (MDBK) cells. Anti-hepatitis C virus (HCV) activity was assessed by the inhibition of viral RNA synthesis in the subgenomic HCV RNA replicon cells. Results: Among the test compounds, 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1 H-pyrazole (SC-560) was the most active against BVDV, and its 50% effective and cytotoxic concentrations were 10.9 ±2.8 and 93.9 ±24.5 μM in virus and mock-infected MDBK cells, respectively. The compound also suppressed BVDV RNA synthesis in a dose-dependent fashion. Studies on the mechanism of action revealed that SC-560 did not interfere with viral entry to the host cells. Furthermore, it was assumed that the antiviral activity of SC-560 was not associated with its inhibitory effect on COX. The combination of SC-560 and interferon-α was additive to synergistic in inhibiting BVDV replication. More importantly, the compound proved to be a selective inhibitor of HCV replication. Conclusions: SC-560 and its derivative might have potential as novel antiviral agents against HCV.
    Type of Medium: Online Resource
    ISSN: 2040-2066 , 2040-2066
    URL: Article
    DOI: 10.3851/IMP1372
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2009
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  • 2
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    Adding items that assess changes in activities of daily living does not improve the predictive accuracy of the Palliative Prognostic Index
    SAGE Publications ; 2017
    In:  Palliative Medicine Vol. 31, No. 3 ( 2017-03), p. 258-266
    Details
    In: Palliative Medicine, SAGE Publications, Vol. 31, No. 3 ( 2017-03), p. 258-266
    Abstract: Changes in activities of daily living in cancer patients may predict their survival. The Palliative Prognostic Index is a useful tool to evaluate cancer patients, and adding an item about activities of daily living changes might improve its predictive value. Aim: To clarify whether adding an item about activities of daily living changes improves the accuracy of Palliative Prognostic Index. Design: Multicenter prospective cohort study. Setting: A total of 58 palliative care services in Japan. Participants: Patients aged 〉 20 years diagnosed with locally extensive or metastatic cancer (including hematological neoplasms) who had been admitted to palliative care units, were receiving care by hospital-based palliative care teams, or were receiving home-based palliative care. Palliative care physicians recorded clinical variables at the first assessment and followed up patients 6 months later. Results: A total of 2425 subjects were recruited and 2343 of these had analyzable data. The C-statistic of the original Palliative Prognostic Index was 0.801, and those of modified Palliative Prognostic Indices ranged from 0.793 to 0.805 at 3 weeks. For 6-week survival predictions, the C-statistic of the original Palliative Prognostic Index was 0.802, and those of modified Palliative Prognostic Indices ranged from 0.791 to 0.799. The weighted kappa of the original Palliative Prognostic Index was 0.510, and those of modified Palliative Prognostic Indices ranged from 0.484 to 0.508. Conclusion: Adding items about activities of daily living changes to the Palliative Prognostic Index did not improve prognostic value in advanced cancer patients.
    Type of Medium: Online Resource
    ISSN: 0269-2163 , 1477-030X
    URL: Article
    DOI: 10.1177/0269216316650788
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2017
    detail.hit.zdb_id: 2027566-3
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  • 3
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    Isolation and characterization of hepatitis C virus resistant to a novel phenanthridinone derivative
    SAGE Publications ; 2015
    In:  Antiviral Chemistry and Chemotherapy Vol. 24, No. 5-6 ( 2015-12), p. 148-154
    Details
    In: Antiviral Chemistry and Chemotherapy, SAGE Publications, Vol. 24, No. 5-6 ( 2015-12), p. 148-154
    Abstract: The novel phenanthridinone derivative HA-719 has recently been identified as a highly potent and selective inhibitor of hepatitis C virus replication. To elucidate its mechanism of inhibition, we have isolated and analyzed a clone of hepatitis C virus replicon cells resistant to HA-719. Methods To isolate HA-719-resistant replicon cells, Huh-7 cells containing subgenomic hepatitis C virus replicons (genotype 1b) with a luciferase reporter (LucNeo#2) were cultured in the presence of G418 and escalating concentrations of HA-719. After several passages, total RNA was extracted from the growing cells, and Huh-7 cells were transfected with the extracted RNA. Limiting dilution of the transfected cells was performed to obtain an HA-719-resistant clone. Results The 50% effective concentration (EC 50 ) of HA-719 for hepatitis C virus replication was 0.058 ± 0.012 µM in LucNeo#2 cells. The replicon cells capable of growing in the presence of G418 and 3 µM HA-719 were obtained after 18 passages (72 days). The HA-719-resistant clone LucNeo719R showed 98.3-fold resistant to the compound (EC 50  = 5.66 ± 0.92 µM), but the clone had no cross-resistance to telaprevir (NS3 inhibitor), daclatasvir (NS5A inhibitor), and VX-222 (NS5B inhibitor). The sequence analysis for the wild-type and LucNeo719R identified 3, 2 and 7 mutations in NS3/4 A, NS4B, and NS5A, respectively, but no mutations in NS5B. Conclusion None of the amino acid mutations in the resistant clone corresponds to those reported to confer drug-resistance to current anti-hepatitis C virus agents, suggesting that the target of HA-719 for hepatitis C virus inhibition differs from those of the existing agents.
    Type of Medium: Online Resource
    ISSN: 2040-2066 , 2040-2066
    URL: Article
    DOI: 10.1177/2040206616663956
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2015
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  • 4
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    Design, synthesis, and anti-HIV-1 activity of 1-substituted 3-(3,5-dimethylbenzyl)triazine derivatives
    SAGE Publications ; 2015
    In:  Antiviral Chemistry and Chemotherapy Vol. 24, No. 2 ( 2015-04), p. 62-71
    Details
    In: Antiviral Chemistry and Chemotherapy, SAGE Publications, Vol. 24, No. 2 ( 2015-04), p. 62-71
    Abstract: The reverse transcriptase (RT) of human immunodeficiency virus type 1 (HIV-1) is an attractive target for the development of drugs used in the treatment of HIV-1 infection and acquired immune deficiency syndrome (AIDS). We have continued the search for novel anti-HIV-1 agents using the structure–activity relationships of the successful 1,3-disubstituted and 1,3,6-trisubstituted uracil-type HIV-1 RT inhibitors. Methods A series of new triazine analogs were synthesized using an established method. The anti-HIV-1 activities of these compounds were determined based on the inhibition of virus-induced cytopathogenicity in MT-4 cells. The cytotoxicity of the compounds was evaluated by assessing the viability of mock-infected cells. Results Some of the compounds showed good-to-moderate activities against HIV-1, with half-maximal effective concentrations (EC 50 ) in the submicromolar range. In particular, a dihydro-1-(4-aminobenzyl)triazine analog showed satisfactory anti-HIV-1 activity with an EC 50 of 0.110 µM and a selectivity index (SI) of 909. Furthermore, molecular modeling analyses were performed to explore the major interactions between HIV-1 RT and potent inhibitors. These results may be important for further development of this class of compounds as anti-HIV-1 agents. Conclusion The satisfactory anti-HIV-1 activity of triazine analogs may serve as the basis for further investigations of the behavior of this class of compounds against drug-resistant mutants.
    Type of Medium: Online Resource
    ISSN: 2040-2066 , 2040-2066
    URL: Article
    DOI: 10.1177/2040206615612208
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2015
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  • 5
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    The Determinants of Patients in a Palliative Care Unit Being Discharged Home in Japan
    SAGE Publications ; 2014
    In:  American Journal of Hospice and Palliative Medicine® Vol. 31, No. 3 ( 2014-05), p. 244-246
    Details
    In: American Journal of Hospice and Palliative Medicine®, SAGE Publications, Vol. 31, No. 3 ( 2014-05), p. 244-246
    Abstract: In Japan, regarding the place of end-of-life care, many people preferred the home. However, there is a discrepancy between patients’ wishes and the actual circumstances. The primary aim of this study was to explore the factors that determine discharge home of patients in a palliative care unit. A total of 31 patients met the criteria. The patients who could be discharged home (group 1; n = 23) were compared with the others (group 2; n = 8). Palliative prognostic index was significantly lower in group 1 than in group 2 ( P = .032). Regarding routes of feeding, oral intake was significantly higher in group 1 than in group 2 ( P = .043). That is to say, factors determining discharge home of patients may be influenced by the patient’s prognosis and the necessity of a feeding device.
    Type of Medium: Online Resource
    ISSN: 1049-9091 , 1938-2715
    URL: Article
    DOI: 10.1177/1049909113484384
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2014
    detail.hit.zdb_id: 2236674-X
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  • 6
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    Potent and Selective Inhibition of Tat-Dependent HIV-1 Replication in Chronically Infected Cells by a Novel Naphthalene Derivative JTK-101
    SAGE Publications ; 2007
    In:  Antiviral Chemistry and Chemotherapy Vol. 18, No. 4 ( 2007-08), p. 201-211
    Details
    In: Antiviral Chemistry and Chemotherapy, SAGE Publications, Vol. 18, No. 4 ( 2007-08), p. 201-211
    Abstract: In search for effective human immunodeficiency virus type 1 (HIV-1) transcription inhibitors, we have evaluated more than 100,000 compounds for their inhibitory effects on HIV-1 long terminal repeat (LTR)-driven reporter gene expression, and identified a novel naphthalene derivative, JTK-101. This compound could suppress tumour necrosis factor (TNF)-α-induced HIV-1 production in latently infected OM-10.1 cells at nanomolar concentrations. JTK-101 could also potently inhibit constitutive HIV-1 production in MOTL-4/III B . However, the antiviral activity of JTK-101 was found to be much weaker in acutely infected cells and the chronically infected cells U937/III B cells than in OM-10.1 and MOLT-4/III B cells. JTK-101 selectively suppressed TNF-α-induced HIV-1 mRNA synthesis in OM-10.1 cells in a dose-dependent fashion. JTK-101 modestly inhibited TNF-α-induced HIV-1 LTR-driven reporter gene expression, but potently inhibited Tat-induced gene expression. Immunoblot analysis revealed that low-level expression of the Tat cofactors CDK9 and cyclin T1 might contribute to the diminished antiviral activity in U937/III B cells. Furthermore, JTK-101 could not inhibit HIV-1 replication in chronically infected monocytes/macrophages, in which CDK9 and cyclin T1 were undetectable. These results suggest that JTK-101 exerts its anti-HIV-1 activity through the inhibition of known or unknown Tat cofactors, presumably CDK9/cyclin T1.
    Type of Medium: Online Resource
    ISSN: 2040-2066 , 2040-2066
    URL: Article
    DOI: 10.1177/095632020701800404
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2007
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  • 7
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    Online Resource
    Establishment of an antiviral assay system and identification of severe fever with thrombocytopenia syndrome virus inhibitors
    SAGE Publications ; 2017
    In:  Antiviral Chemistry and Chemotherapy Vol. 25, No. 3 ( 2017-12), p. 83-89
    Details
    In: Antiviral Chemistry and Chemotherapy, SAGE Publications, Vol. 25, No. 3 ( 2017-12), p. 83-89
    Abstract: Severe fever with thrombocytopenia syndrome (SFTS) is an emerging tick-borne infectious disease. SFTS is epidemic in Asia, and its fatality rate is around 30% in Japan. The causative virus severe fever with thrombocytopenia syndrome virus (SFTSV) is a phlebovirus of the family Phenuiviridae (the order Bunyavirales). Although effective treatments are required, there are no antiviral agents currently approved for clinical use. Ribavirin and favipiravir were examined for their anti-SFTSV activity and found to be selective inhibitors of SFTSV replication in vitro. However, their activity was not sufficient. Therefore, it is mandatory to identify novel compounds active against SFTSV. To this end, we have established a safe and rapid assay system for screening selective inhibitors of SFTSV. Methods The virus was isolated from SFTS patients treated in Kagoshima University Hospital. Vero cells were infected with SFTSV and incubated in the presence of various concentrations of test compounds. After three days, the cells were examined for their intracellular viral RNA levels by real-time reverse transcription-PCR without extracting viral RNA. The cytotoxicity of test compounds was determined by a tetrazolium dye method. Results Among the test compounds, the antimalarial agent amodiaquine was identified as a selective inhibitor of SFTSV replication. Its 50% effective concentration (EC 50 ) and cytotoxic concentration (CC 50 ) were 19.1 ± 5.1 and 〉 100 µM, respectively. The EC 50 value of amodiaquine was comparable to those of ribavirin and favipiravir. Conclusion Amodiaquine is considered to be a promising lead of novel anti-SFTSV agents, and evaluating the anti-SFTSV activity of its derivatives is in progress.
    Type of Medium: Online Resource
    ISSN: 2040-2066 , 2040-2066
    URL: Article
    DOI: 10.1177/2040206617740303
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2017
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  • 8
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    Online Resource
    Anti-Bovine Viral Diarrhoea Virus Activity of Novel Diphenylmethane Derivatives
    SAGE Publications ; 2010
    In:  Antiviral Chemistry and Chemotherapy Vol. 20, No. 5 ( 2010-06), p. 193-200
    Details
    In: Antiviral Chemistry and Chemotherapy, SAGE Publications, Vol. 20, No. 5 ( 2010-06), p. 193-200
    Abstract: A number of compounds were examined for their inhibitory effects on bovine viral diarrhoea virus (BVDV), a surrogate model of hepatitis C virus, in cell cultures. Among them, some diphenylmethane derivatives were found to be selective inhibitors of BVDV. Methods: Determination of compounds for their anti-BVDV activity was based on the inhibition of virus-induced cytopathic effect in Madin–Darby bovine kidney cells and reduction of infectious virus particles in culture supernatants. To gain insight into the mechanism of action, the inhibition of viral entry and RNA synthesis in the host cells was also determined by real-time reverse transcription-PCR. Results: Among the test compounds, four diphenylmethane derivatives significantly inhibited BVDV replication with a 50% effective concentration ranging between 6.3 and 10.8 μM. They were not cytotoxic at concentrations up to 100 μM. The representative compound, SH-595A, reduced the virus titre of culture supernatants in a dose-dependent manner. In addition, the compound appeared to somewhat affect viral entry to the host cells. Although SH-595A was inhibitory to viral RNA synthesis, the inhibition was achieved only at high concentrations and was not comparable to its antiviral activity. Conclusions: The novel diphenylmethane derivatives are effective against BVDV replication and might have a unique mechanism of action.
    Type of Medium: Online Resource
    ISSN: 2040-2066 , 2040-2066
    URL: Article
    DOI: 10.3851/IMP1528
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2010
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  • 9
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    Design, synthesis, and anti-HIV-1 activity of 1-aromatic methyl-substituted 3-(3,5-dimethylbenzyl)uracil and N -3,5-dimethylbenzyl-substituted urea derivatives
    SAGE Publications ; 2015
    In:  Antiviral Chemistry and Chemotherapy Vol. 24, No. 1 ( 2015-02), p. 3-18
    Details
    In: Antiviral Chemistry and Chemotherapy, SAGE Publications, Vol. 24, No. 1 ( 2015-02), p. 3-18
    Abstract: A new series of 1-aromatic methyl-substituted 3-(3,5-dimethylbenzyl)uracil and N-3,5-dimethylbenzyl-substituted urea derivatives were synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Methods A series of new 6-azido and 6-amino derivatives of 1-substituted-3-(3,5-dimethylbenzyl)uracils were synthesized using our previously reported method, and three acyclic derivatives were synthesized from urea. The anti-HIV-1 activities of these compounds were determined based on the inhibition of virus-induced cytopathogenicity in MT-4 cells. The cytotoxicities of the compounds were evaluated using the viability of mock-infected cells. Results Some of these compounds showed good-to-moderate activities against HIV-1 with half maximal effective concentration (EC 50 ) values in the submicromolar or subnanomolar range. Compared with emivirine, compound 6-amino-3-(3,5-dimethylbenzyl)-1-(4-aminobenzyl)uracil showed significant anti-HIV-1 activity with an EC 50 value of 10 nM and a high selectivity index of 1923. Preliminary structure–activity relationship studies and molecular modeling analyses were carried out to explore the major interactions between HIV-1 reverse transcriptase and the potent inhibitor 6-amino-3-(3,5-dimethylbenzyl)-1-(4-aminobenzyl)uracil; these results may be important for further development of this class of compounds as anti-HIV-1 agents. Conclusion The excellent activity of 6-amino-3-(3,5-dimethylbenzyl)-1-(4-aminobenzyl)uracil (EC 50 : 0.010 ± 0.006 µM, SI: 〉 1923) may serve as the basis for conducting further investigations on the behavior of this class of compounds against drug-resistant mutants.
    Type of Medium: Online Resource
    ISSN: 2040-2066 , 2040-2066
    URL: Article
    DOI: 10.1177/2040206614566584
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2015
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  • 10
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    The Stoic Male : How Avatar Gender Affects Help-Seeking Behavior in an Online Game
    SAGE Publications ; 2012
    In:  Games and Culture Vol. 7, No. 1 ( 2012-01), p. 29-47
    Details
    In: Games and Culture, SAGE Publications, Vol. 7, No. 1 ( 2012-01), p. 29-47
    Abstract: Men are more reluctant to seek help for their problems than women. This difference is attributed to social expectations regarding the male gender role. Today, help-seeking is moving online: instead of traditional peer groups and counselors, people depend on online communities and e-counselors. But online users can appear in guises that differ from their physical sex. An empirical study was conducted in an online game to examine whether users’ avatars’ gender influences how they seek and receive help. Analysis is based on user-to-user communications and back-end data. Results indicate that male avatars are less likely to receive sought-for help than female avatars and more likely to be the recipients of indirectly sought help. The authors conclude that avatar gender influences help seeking independent of physical sex: Men overcome their inhibition for help seeking when using female avatars. Practitioners should ensure that means for indirect help seeking are available in order not to exclude male-pattern help seekers.
    Type of Medium: Online Resource
    ISSN: 1555-4120 , 1555-4139
    URL: Article
    DOI: 10.1177/1555412012440307
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2012
    detail.hit.zdb_id: 2213152-8
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