フラボノイドによるプロテインキナーゼC活性抑制作用

概要

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Plant-derived flavonoids, quercetin, catechin, catechin and ipriflavone, inhibited the purified rat brain Protein kinase C (PKC) in a concentration-dependent manner. Their order of potency was quercetin > catechin ≒ ipriflavone. Most isozymes of PKC were known to be activated by phorbol 12-myristate 13-acetate (PMA) and undergo translocation from the cytosol to the plasma membrane. We used BL-9 cells, a cell line derived from rat liver hepatocytes, because in these cells the cytosolic PKC rapidly translocated to the membrane fraction after PMA treatment. The membrane-associated PKC activity was inhibited by flavonoids. The effectiveness of flavonoids was classified as follows : ipriflavone > catechin > quercetin. These results indicated that flavonoids efficiently suppressed PMA-induced PKC activation both in vitro and in vivo. However, the suppression mechanism of PKC activity by flavonoids in culture cells was different from that in vitro.
東海大学の論文