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Natural Stilbenoids Have Anti-Inflammatory Properties in Vivo and Down-Regulate the Production of Inflammatory Mediators NO, IL6, and MCP1 Possibly in a PI3K/Akt-Dependent Manner
Journal of Natural Products ( IF 3.3 ) Pub Date : 2018-05-04 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00384 Heikki Eräsalo 1 , Mari Hämäläinen 1 , Tiina Leppänen 1 , Ilari Mäki-Opas 1 , Mirka Laavola 1 , Raisa Haavikko 2 , Jari Yli-Kauhaluoma 2 , Eeva Moilanen 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2018-05-04 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00384 Heikki Eräsalo 1 , Mari Hämäläinen 1 , Tiina Leppänen 1 , Ilari Mäki-Opas 1 , Mirka Laavola 1 , Raisa Haavikko 2 , Jari Yli-Kauhaluoma 2 , Eeva Moilanen 1
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Stilbenoids are a group of polyphenolic compounds found in plants, trees, berries, and nuts. Stilbenoids have been shown to serve an antimicrobial and antifungal function in plants. There is also evidence that as a part of the human diet, stilbenoids play an important role as antioxidants and may have anti-inflammatory effects. The PI3K/Akt pathway is a well-characterized signaling pathway controlling cellular functions involved in growth and cell cycle and in metabolism. There is also increasing evidence to show the involvement of this pathway in the regulation of inflammatory responses. In the present study, an attempt was made to investigate the anti-inflammatory properties of the naturally occurring stilbenoids pinosylvin (1), monomethylpinosylvin (2), resveratrol (3), pterostilbene (4), piceatannol (5), and rhapontigenin (6). Glycosylated derivatives of piceatannol and rhapontigenin, namely, astringin (7) and rhaponticin (8), respectively, were also investigated. In addition to the natural stilbenoids, pinosylvin derivatives (9–13) were synthesized and subjected to the testing of their effects on the PI3K/Akt pathway in inflammatory conditions. The investigated natural stilbenoids (except the glycosylated derivatives) were found to down-regulate Akt phosphorylation, which is a well-acknowledged marker for PI3K activity. It was also found that all of the studied natural stilbenoids had anti-inflammatory effects in vitro. The three most potent stilbenoids, piceatannol, pinosylvin, and pterostilbene, were selected for in vivo testing and were found to suppress inflammatory edema and to down-regulate the production of inflammatory mediators IL6 and MCP1 in carrageenan-induced paw inflammation in mice. When compared to the commercial PI3K inhibitor LY294002, the anti-inflammatory effects appeared to be quite similar. The results reveal hitherto unknown anti-inflammatory effects of natural stilbenoids and suggest that those effects may be mediated via inhibition of the PI3K/Akt pathway.
中文翻译：
天然类胡萝卜素在体内具有抗炎特性，并可能以PI3K / Akt依赖性方式下调炎性介质NO，IL6和MCP1的产生
Stilbenoids是在植物，树木，浆果和坚果中发现的一组多酚化合物。已证明类胡萝卜素在植物中具有抗微生物和抗真菌功能。也有证据表明，类胡萝卜素作为人类饮食的一部分，起着抗氧化剂的重要作用，并且可能具有抗炎作用。PI3K / Akt途径是一个特征明确的信号传导途径，可控制参与生长，细胞周期和代谢的细胞功能。也有越来越多的证据表明该途径参与了炎症反应的调节。在本研究中，已尝试研究天然存在的类雌二醇类松油醇（1），单甲基松油醇（2），白藜芦醇（3）的抗炎特性。），紫檀（4），白皮杉醇（5），和rhapontigenin（6）。还研究了皮卡替诺醇和rapontigenin的糖基化衍生物，分别是苦丁素（7）和rapanticin（8）。除了天然茋类，赤松素衍生物（9 - 13）的合成，并进行其对在炎性疾病的PI3K / Akt通路的效果进行测试。发现研究的天然stilbenoids（糖基化衍生物除外）下调Akt磷酸化，这是公认的PI3K活性标记。还发现所有研究过的天然西til类化合物均具有抗炎作用体外。选择了三种最有效的类胡萝卜素，苦味酚，皮诺西林和蝶草烯进行体内测试，结果发现它们抑制炎症性水肿并下调角叉菜胶诱发的小鼠爪炎症中炎性介质IL6和MCP1的产生。当与市售PI3K抑制剂LY294002相比时，抗炎作用似乎非常相似。结果揭示了迄今为止尚未发现的天然类胡萝卜素的抗炎作用，并表明这些作用可能是通过抑制PI3K / Akt途径介导的。
更新日期：2018-05-04
中文翻译：
天然类胡萝卜素在体内具有抗炎特性，并可能以PI3K / Akt依赖性方式下调炎性介质NO，IL6和MCP1的产生
Stilbenoids是在植物，树木，浆果和坚果中发现的一组多酚化合物。已证明类胡萝卜素在植物中具有抗微生物和抗真菌功能。也有证据表明，类胡萝卜素作为人类饮食的一部分，起着抗氧化剂的重要作用，并且可能具有抗炎作用。PI3K / Akt途径是一个特征明确的信号传导途径，可控制参与生长，细胞周期和代谢的细胞功能。也有越来越多的证据表明该途径参与了炎症反应的调节。在本研究中，已尝试研究天然存在的类雌二醇类松油醇（1），单甲基松油醇（2），白藜芦醇（3）的抗炎特性。），紫檀（4），白皮杉醇（5），和rhapontigenin（6）。还研究了皮卡替诺醇和rapontigenin的糖基化衍生物，分别是苦丁素（7）和rapanticin（8）。除了天然茋类，赤松素衍生物（9 - 13）的合成，并进行其对在炎性疾病的PI3K / Akt通路的效果进行测试。发现研究的天然stilbenoids（糖基化衍生物除外）下调Akt磷酸化，这是公认的PI3K活性标记。还发现所有研究过的天然西til类化合物均具有抗炎作用体外。选择了三种最有效的类胡萝卜素，苦味酚，皮诺西林和蝶草烯进行体内测试，结果发现它们抑制炎症性水肿并下调角叉菜胶诱发的小鼠爪炎症中炎性介质IL6和MCP1的产生。当与市售PI3K抑制剂LY294002相比时，抗炎作用似乎非常相似。结果揭示了迄今为止尚未发现的天然类胡萝卜素的抗炎作用，并表明这些作用可能是通过抑制PI3K / Akt途径介导的。
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