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    Novel anti-inflammatory compounds from Myrsine seguinii, terpeno-benzoic acids, are inhibitors of mammalian DNA polymerases

    机译:来自Myrsine seguinii的新型抗炎化合物,萜烯-苯甲酸,是哺乳动物DNA聚合酶的抑制剂

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    Novel anti-inflammatory compounds, terpeno-benzoic acids, were found from the plant, Myrsine seguinii. The strongest of these antiinflammatory agents, 3-gerany1-4-hydroxy-5-(3'-methyl-2'-butenyl) benzoic acid (compound 1), showed an inhibitory effect against enzymes involved in replication, such as calf DNA polymerase α(pol. α), rat DNA polymerase β(pol. β) and one of the β family polymerases, calf thymus terminal deoxynucleotidyl transferase (TdT). The minimum inhibitory concentration (MIC) and IC_(50) values were 82 and 22 μM for pol. α, 86 and 11 μM for pol. β, 140 and 46 μM 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.
    机译:从植物Myrsine seguinii中发现了新型抗炎化合物,萜烯-苯甲酸。这些抗炎剂中最强的是3-gerany1-4-羟基-5-(3'-甲基-2'-丁烯基)苯甲酸(化合物1),对复制涉及的酶(例如小牛DNA聚合酶)具有抑制作用。 α(pol.α),大鼠DNA聚合酶β(pol.β)和一种β家族聚合酶,小牛胸腺末端脱氧核苷酸转移酶(TdT)。 pol的最小抑菌浓度(MIC)和IC_(50)值为82和22μM。 pol的α,86和11μM TdT分别为β,140和46μM。但是,化合物1不会影响植物DNA聚合酶,人类免疫缺陷病毒1型逆转录酶,任何原核DNA聚合酶或DNA和RNA代谢酶的活性。观察到四种衍生物的抗炎活性和DNA聚合酶抑制活性之间的剂量依赖性关系?;衔锏谋郊姿嶂械聂人岵糠炙坪跤胍种谱饔糜泄?。讨论了萜烯-苯甲酸对聚合酶的作用方式及其与抗炎活性的关系。

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