Maioli Emanuela, Greci Lucedio, Soucek Karel, Hyzdalova Martina, Pecorelli Alessandra, Fortino Vittoria, Valacchi Giuseppe
Dipartimento di Fisiologia, University of Siena, Italy.
J Biomed Biotechnol. 2009;2009:742936. doi: 10.1155/2009/742936. Epub 2010 Feb 3.
Rottlerin, a polyphenol isolated from Mallotus Philippinensis, has been recently used as a selective inhibitor of PKC delta, although it can inhibit many kinases and has several biological effects. Among them, we recently found that Rottlerin inhibits the Nuclear Factor kappaB (NFkappaB), activated by either phorbol esters or H(2)O(2). Because of the redox sensitivity of NFkappaB and on the basis of Rottlerin antioxidant property, we hypothesized that Rottlerin could prevent NFkappaB activation acting as a free radicals scavenger, as other natural polyphenols. The current study confirms the antioxidant property of Rottlerin against the 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) in vitro and against oxidative stress induced by H(2)O(2) and by menadione in culture cells. We also demonstrate that Rottlerin prevents TNFalpha-dependent NFkappaB activation in MCF-7 cells and in HT-29 cells transfected with the NFkappaB-driven plasmid pBIIX-LUC, suggesting that Rottlerin can inhibit NFkappaB via several pathways and in several cell types.
鱼藤素是从菲律宾叶下珠中分离出的一种多酚，尽管它能抑制多种激酶并具有多种生物学效应，但最近已被用作蛋白激酶Cδ（PKCδ）的选择性抑制剂。其中，我们最近发现鱼藤素能抑制由佛波酯或过氧化氢激活的核因子κB（NFκB）。由于NFκB对氧化还原敏感，且基于鱼藤素的抗氧化特性，我们推测鱼藤素可能像其他天然多酚一样，作为自由基清除剂来阻止NFκB的激活。当前的研究证实了鱼藤素在体外对2,2-二苯基-1-苦基肼自由基（DPPH）以及在培养细胞中对过氧化氢和甲萘醌诱导的氧化应激具有抗氧化特性。我们还证明，鱼藤素可阻止MCF-7细胞和转染了NFκB驱动质粒pBIIX-LUC的HT-29细胞中肿瘤坏死因子α（TNFα）依赖性NFκB的激活，这表明鱼藤素可通过多种途径在多种细胞类型中抑制NFκB。
