Anti-Aids Agents, 2: Inhibitory Effect of Tannins on HIV Reverse Transcriptase and HIV Replication in H9 Lymphocyte Cells

Authors:
  • GNGen-Ichiro Nonaka
    Gen-Ichiro Nonaka
  • INItsuo Nishioka
    Itsuo Nishioka
  • MNMakoto Nishizawa
    Makoto Nishizawa
  • TYTakashi Yamagishi
    Takashi Yamagishi
  • YKYoshiki Kashiwada
    Yoshiki Kashiwada
  • GDGinger E. Dutschman
    Ginger E. Dutschman
  • ABAnne J. Bodner
    Anne J. Bodner
  • RKRobert E. Kilkuskie
    Robert E. Kilkuskie
  • YCYung-Chi Cheng
    Yung-Chi Cheng
  • KLKuo-Hsiung Lee
    Kuo-Hsiung Lee
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Abstract
Nine tannins, including gallo- and ellagitannins, were evaluated as potential inhibitors of HIV replication. 1,3,4-Tri-O-galloylquinic acid [1], 3,5-di-O-galloyl-shikimic acid [2], 3,4,5-tri-O-galloylshikimic acid [3], punicalin [6], and punicalagin [7] inhibited HIV replication in infected H9 lymphocytes with little cytotoxicity. Two compounds, punicalin and punicacortein C [8], inhibited purified HIV reverse transcriptase with ID50 of 8 and 5 microM, respectively. Further studies with H9 lymphocytes indicated that chebulagic acid [5] and punicalin did not inactivate virus directly. However, 1,3,4-tri-O-galloylquinic acid and 3,5-di-O-galloylshikimic acid were more effective inhibitors under those conditions. All tannins appear to inhibit virus-cell interactions. Thus, inspite of their anti-RT activity, the mechanism by which tannins inhibit HIV may not be associated with this enzyme.

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