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      Three New 9,11-Secosterols from the Formosan Soft CoralSinularia leptoclados

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      Bulletin of the Chemical Society of Japan

      The Chemical Society of Japan

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          Sinugibberol, a new cytotoxic cembranoid diterpene from the soft coral Sinularia gibberosa.

          Bioactivity-guided fractionation of a chloroform extract of the soft coral Simularia gibberosa afforded a new cytotoxic cembranoid diterpene, sinugibberol [1]. The structure of 1 was determined by spectral and X-ray crystallographic analysis.
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            Identification of C-24 alkyl epimers of marine sterols by 13C nuclear magnetic resonance spectroscopy

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              Cell-dependent interference of a series of new 6-aminoquinolone derivatives with viral (HIV/CMV) transactivation.

              Quinolone derivatives have been shown to inhibit human immunodeficiency virus (HIV) replication at the transcriptional level. Recently, a series of new 6-aminoquinolones that are endowed with more pronounced anti-HIV activities compared with the formerly reported quinolone derivatives have been published. These potent 6-aminoquinolones were further evaluated for their broad-spectrum antiviral properties. Latently HIV-1-infected cell lines as well as cytomegalovirus (CMV)-infected fibroblasts were used to evaluate the antiviral potency of the 6-aminoquinolone derivatives. Additionally green fluorescent protein (GFP) transactivation experiments using different promoters were conducted. The compounds completely suppressed tumour necrosis factor alpha (TNF-alpha)- and phorbol 12-myristate 13-acetate (PMA)-induced HIV-1 expression in latently HIV-1-infected OM-10.1 and U1 cell lines at non-toxic concentrations. In addition, HIV-1 mRNA production was dramatically suppressed in both cell lines in a dose-dependent manner. In the same concentration range, the compounds inhibited TNF-alpha release from PMA-induced OM-10.1 cells but allowed TNF-alpha production from PMA-induced U1 cells at all concentrations tested. The 6-aminoquinolone derivatives were not only inhibitory to the Tat-mediated transactivation of the HIV-1 LTR promoter, but were also found to interfere in a cell-dependent way with the transactivation process mediated from the human CMV immediate early and the human EF-1alpha promoter. Additionally, the 6-aminoquinolone derivatives were also found to be inhibitory to CMV replication in fibroblast cells. It thus appears that the antiviral spectrum of this class of compounds is not confined to the specific inhibition of HIV but encompasses CMV as well. This broad-spectrum activity window might provide an interesting platform for future applications for the 6-aminoquinolone derivatives.
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                Author and article information

                Journal
                Bulletin of the Chemical Society of Japan
                BCSJ
                The Chemical Society of Japan
                0009-2673
                1348-0634
                June 15 2011
                June 15 2011
                : 84
                : 6
                : 648-652
                Article
                10.1246/bcsj.20110046
                © 2011
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