In the present study, the effects of tannins obtained from various plant sources on the activity of 5-LOX and AT were examined. With IC50 values ranging from 1.0 to 18.7 muM, hamamelitannin and the galloylated proanthocyanidins isolated from Hamamelis virginiana L. were found to be most potent inhibitors of 5-LOX. Unlike the 5-LOX study, hamamelitannin proved to be ineffective in the AT assay. Potent candidates are represented by the group of B-type proanthocyanidins. Structure-activity relationships regarding the in vitro inhibitory potency of the polyphenols in the biological assays are discussed.
Eine Hemmung der Cyclooxygenase‐Reaktion bei der Prostaglandinbildung des Rattennierenmarks in vitro ist durch verschiedene Flavonoide mit o‐Dihydroxystrukturen möglich. Diese Flavonoide mit einer Brenzcatechin‐Anordnung im Molekül besitzen ausgeprägte Radikalfängereigenschaften für Peroxid‐Anion‐Radikale. Dagegen können einige Flavonoide und Phenolderivate, die starke O2−•‐Radikalfänger sind, die Prostaglandinsynthetase aber auch aktivieren oder unbeeinflußt lassen. Eine Korrelation zwischen den Radikalfängereigenschaften und der Beeinflussung des Cyclooxygenase‐Enzyms besteht folglich bei den untersuchten Verbindungen nicht.
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