Document Detail

Differential inhibition of reverse transcriptase and various DNA polymerases by digallic acid and its derivatives.
MedLine Citation:
PMID:  1705574     Owner:  NLM     Status:  MEDLINE    
Digallic acid (gallic acid 5,6-dihydroxy-3-carboxyphenyl ester) [4] was found to be a potent inhibitor of the activities of the reverse transcriptases from murine leukemia virus (MLV) and human immunodeficiency virus (HIV). Under the reaction conditions specified for each of MLV and HIV reverse transcriptases, both enzymes were inhibited by approximately 90% in the presence of 0.5 micrograms/ml digallic acid. Under the same conditions, however, gallic acid had no effect on the reverse transcriptase activity. The mode of the inhibition by digallic acid was partially competitive with respect to the template.primer, (rA)n.(dT)12-18', and noncompetitive to the triphosphate substrate, dTTP. The Ki value of digallic acid for HIV-reverse transcriptase was determined to be 0.58 microM. Examination of several derivatives of digallic acid have shown that all three hydroxyl groups at the 3, 4, and 5 positions seem to be required for the inhibitory activity of these compounds. Besides reverse transcriptase, DNA polymerases alpha and beta were moderately inhibited by digallic acid, whereas DNA polymerase gamma, terminal deoxynucleotidyltransferase, and E. coli DNA polymerase I were virtually insensitive to inhibition by this compound.
H Nakane; M Fukushima; K Ono
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of natural products     Volume:  53     ISSN:  0163-3864     ISO Abbreviation:  J. Nat. Prod.     Publication Date:    1990 Sep-Oct
Date Detail:
Created Date:  1991-04-10     Completed Date:  1991-04-10     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7906882     Medline TA:  J Nat Prod     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1234-40     Citation Subset:  IM; X    
Laboratory of Viral Oncology, Aichi Cancer Center Research Institute, Nagoya, Japan.
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MeSH Terms
DNA-Directed DNA Polymerase / antagonists & inhibitors*
Gallic Acid / analogs & derivatives*,  pharmacology
HIV / enzymology*
RNA-Directed DNA Polymerase / isolation & purification
Rauscher Virus / enzymology*
Reverse Transcriptase Inhibitors*
Structure-Activity Relationship
Reg. No./Substance:
0/Depsides; 0/Reverse Transcriptase Inhibitors; 149-91-7/Gallic Acid; 536-08-3/digallic acid; EC DNA Polymerase; EC DNA Polymerase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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