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天然芪类化合物的抗炎活性:综述。

Anti-inflammatory activity of natural stilbenoids: A review.

机构信息

Laboratory of Plant Biotechnologies, Institute of Experimental Botany, The Czech Academy of Sciences, v.v.i., Rozvojova 263, 165 02 Prague, Czech Republic.

出版信息

Pharmacol Res. 2017 Oct;124:126-145. doi: 10.1016/j.phrs.2017.08.002. Epub 2017 Aug 9.

Abstract

Resveratrol and other natural stilbenoids, including piceatannol, pterostilbene, and gnetol, are well-known anti-inflammatory compounds with indisputable activity in vitro as well as in vivo. Their molecular targets include inducible nitric oxide synthase, cyclooxygenases, leukotrienes, nuclear factor kappa B, tumor necrosis factor α, interleukins and many more. This anti-inflammatory activity together with their antioxidant activity is believed to stand behind their other positive health effects against cancer, cardiovascular and neurodegenerative diseases or diabetes. Thus, they are nowadays commercially marketed as nutraceuticals. Naturally, they are present in wine, grapes or berries. However, there is a rigorous debate about the real effect of these compounds on human health. It is argued that the concentration of stilbenoids in food and beverages is too low to have any therapeutic potential and this concentration is further reduced by their low bioavailability and extensive metabolism. Therefore, this review focuses on in vitro, in vivo, preclinical as well as clinical data available for various natural stilbenoids and summarizes the anti-inflammatory targets on molecular level, compares the relevance of the experimental studies, discusses the metabolism of stilbenoids and the potential activity of their metabolites and relates this knowledge to human health. Moreover, the ways to augment stilbenoidś efficacy are suggested with special focus on multitargeted therapy and nanocarriers.

摘要

白藜芦醇和其他天然芪类化合物,包括白皮杉醇、紫檀芪和 Gnetin,是众所周知的抗炎化合物,具有无可争议的体外和体内活性。它们的分子靶点包括诱导型一氧化氮合酶、环氧化酶、白三烯、核因子 kappa B、肿瘤坏死因子 α、白细胞介素等。这种抗炎活性以及它们的抗氧化活性被认为是它们对癌症、心血管和神经退行性疾病或糖尿病等其他积极健康影响的背后原因。因此,它们如今被商业化作为营养保健品。天然存在于葡萄酒、葡萄或浆果中。然而,关于这些化合物对人类健康的实际影响存在激烈的争论。有人认为,食物和饮料中芪类化合物的浓度太低,无法产生任何治疗潜力,而且由于其生物利用度低和广泛的代谢,其浓度进一步降低。因此,本综述重点关注各种天然芪类化合物的体外、体内、临床前和临床数据,并总结了分子水平上的抗炎靶点,比较了实验研究的相关性,讨论了芪类化合物的代谢及其代谢物的潜在活性,并将这些知识与人类健康联系起来。此外,还提出了增强芪类化合物疗效的方法,特别关注多靶点治疗和纳米载体。

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