Important note: Information in this article was accurate in 2000. The state of the art may have changed since the publication date.
Novel anti-inflammatory compounds from Myrsine seguinii, terpeno-benzoic acids, are inhibitors of mammalian DNA polymerases.
Biochim Biophys Acta. 2000 Jun 1;1475(1):1-4. Unique Identifier : AIDSLINE MED/20267566 Mizushina Y; Miyazaki S; Ohta K; Hirota M; Sakaguchi K; Department of Applied Biological Science, Faculty of Science and; Technology, Science University of Tokyo, 2641 Yamazaki, Noda,; Chiba, Japan.
Abstract:
Novel anti-inflammatory compounds, terpeno-benzoic acids, were found from the plant, Myrsine seguinii. The strongest of these anti-inflammatory agents, 3-geranyl-4-hydroxy-5-(3'-methyl-2'-butenyl) benzoic acid (compound 1), showed an inhibitory effect against enzymes involved in replication, such as calf DNA polymerase alpha (pol. alpha), rat DNA polymerase beta (pol. beta) and one of the beta family polymerases, calf thymus terminal deoxynucleotidyl transferase (TdT). The minimum inhibitory concentration (MIC) and IC50 values were 82 and 22 microM for pol. alpha, 86 and 11 microM for pol. beta, 140 and 46 microM for TdT, respectively. However, compound 1 did not influence the activities of plant DNA polymerases, human immunodeficiency virus type-1 reverse transcriptase, any of the prokaryotic DNA polymerases or DNA and RNA metabolic enzymes tested. Dose-dependent relationships were observed between the anti-inflammatory activities and the DNA polymerase-inhibitory activities of the four derivatives. The carboxylic acid moiety in the benzoic acid of the compounds appeared to be related to the inhibitory effects. The mode of action of the terpeno-benzoic acids against the polymerases and their relationships to the anti-inflammatory activity are discussed.
Keywords: JOURNAL ARTICLE Animal Anti-Inflammatory Agents, Non-Steroidal/ISOLATION & PURIF/ *PHARMACOLOGY Benzoic Acids/ISOLATION & PURIF/*PHARMACOLOGY Cattle Dose-Response Relationship, Drug DNA-Directed DNA Polymerase/*ANTAGONISTS & INHIB Enzyme Inhibitors/ISOLATION & PURIF/PHARMACOLOGY Molecular Structure Plant Extracts/CHEMISTRY Support, Non-U.S. Gov't Terpenes/ISOLATION & PURIF/*PHARMACOLOGY
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Important note: Information in this article was accurate in 2000. The state of the art may have changed since the publication date.
