Anti-AIDS agents, 2: Inhibitory effects of tannins on HIV reverse transcriptase and HIV replication in H9 lymphocyte cells.
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.
Nonaka
G
G
Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599.
Nishioka
I
I
Nishizawa
M
M
Yamagishi
T
T
Kashiwada
Y
Y
Dutschman
G E
GE
Bodner
A J
AJ
Kilkuskie
R E
RE
Cheng
Y C
YC
Lee
K H
KH
D000998:Antiviral Agents / Q000302:isolation & purification*; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000502:physiology; D006801:Humans; D008214:Lymphocytes; D015394:Molecular Structure; D010944:Plants / Q000032:analysis*; D012194:RNA-Directed DNA Polymerase / Q000378:metabolism*; D013634:Tannins / Q000302:isolation & purification / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects*
D000998:Antiviral Agents; D013634:Tannins; D012194:RNA-Directed DNA Polymerase