Role of Natural Stilbenes in the Prevention of Cancer.
Role of Natural Stilbenes in the Prevention of Cancer.
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DOI：
10.1155/2016/3128951
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发表时间：
2016
影响因子：
--
通讯作者：
Ortega AL
中科院分区：
文献类型：
--
作者：
Sirerol JA;Rodríguez ML;Mena S;Asensi MA;Estrela JM;Ortega AL
天然二苯乙烯是一类重要的非黄酮类植物化学物质，其多酚结构以1,2-二苯乙烯核的存在为特征。二苯乙烯在预防和治疗包括癌症在内的各种疾病方面具有非凡的潜力，因为它们具有抗氧化、细胞死亡活化和抗炎特性，并且在体内条件下具有低毒性。本文就其作用机制、在动物模型和人体中的药理活性以及在临床研究中的潜在化学预防等方面的研究进展进行综述。天然二苯乙烯的生物活性尚不完全清楚。此外，在给药给动物或人类后，这些分子被迅速代谢。因此，天然结构及其代谢产物的药代动力学和/或活性可能非常不同。为了提高稳定性和生物利用度，减少副作用，并促进与靶蛋白中的结构域的相互作用，已经假设了新的药物配方。这些药理上的改进将使二苯乙烯成为有效的候选抗癌药物。
Natural stilbenes are an important group of nonflavonoid phytochemicals of polyphenolic structure characterized by the presence of a 1,2-diphenylethylene nucleus. Stilbenes have an extraordinary potential for the prevention and treatment of different diseases, including cancer, due to their antioxidant, cell death activation, and anti-inflammatory properties which associate with low toxicity under in vivo conditions. This review aims to discuss various approaches related to their mechanisms of action, pharmacological activities in animal models and humans, and potential chemoprevention in clinical studies. The biological activity of natural stilbenes is still incompletely understood. Furthermore, after administration to animals or humans, these molecules are rapidly metabolized. Thus pharmacokinetics and/or activities of the natural structures and their metabolites may be very different. Novel drug formulations have been postulated in order to improve stability and bioavailability, to minimize side effects, and to facilitate interaction with their domains in target proteins. These pharmacological improvements should lead stilbenes to become effective candidates as anticancer drugs.