Saller Reinhard, Melzer Jörg, Reichling Jürgen, Brignoli Reto, Meier Remy
Institute of Complementary Medicine, Department of Internal Medicine, University Hospital Zurich, Zurich, Switzerland.
Forsch Komplementmed. 2007 Apr;14(2):70-80. doi: 10.1159/000100581. Epub 2007 Apr 23.
Recent years have seen an explosion of scientific papers that deal with drugs from the fruits of milk thistle and its active substances silymarin (standardized mixture of flavonolignanes), thus justifying an updated systematic review.
Electronic databases identified silymarin, silibinin, silicristin or milk thistle as descriptors in >700 papers (34% published in last 5 years; 92% dealt with animal pharmacological). Only papers adequately reporting on experimental conditions, dosing, variables tested and statistics were analysed.
Silymarin was found to modify specifically the functions related to various transporters and receptors located in the cell membranes; that is, organic anion uptake transporter peptides (OATP), ABC transporters (P-gp), bile salt export pump, as well as TNF-alpha-dependent and possibly selectin-dependent phenomena. In the cytoplasm, some antioxidant properties and the inhibition of the lipoxygenase pathway seem quite selective and could concur to the antitoxic effects. Some effects like the inhibition of inducible nitric-oxide synthase, of nuclear factor kappa B, and reduction of collagen synthesis are indicative of DNA/RNA-mediated effects. Several studies using 'in vitro' and 'in vivo' cancer models suggest a potential of silymarin in such diseases. Topical and systemic silymarin has skin protective properties against UV-induced damage in epidermis and causes an up-regulation of tumour-suppressor genes p53- and p21CIP1. There were no data on hepatic viral replication, viremia or spontaneous tumours in the data examined.
Data presented here do not solve the question about the complex mechanism(s) of action of the medicinal herbal drug silymarin. Silymarin may be a natural multi-functional and multi-target drug.
近年来，涉及水飞蓟果实中的药物及其活性成分水飞蓟素（黄酮木脂素的标准化混合物）的科学论文激增，因此有必要进行一次更新的系统综述。
电子数据库检索到700多篇论文中以水飞蓟素、水飞蓟宾、水飞蓟宁或水飞蓟作为关键词（34%在过去5年发表；92%涉及动物药理学）。仅分析了充分报告实验条件、给药剂量、测试变量和统计学方法的论文。
发现水飞蓟素能特异性地改变与位于细胞膜上的各种转运体和受体相关的功能；即有机阴离子摄取转运肽（OATP）、ABC转运体（P-gp）、胆盐输出泵，以及肿瘤坏死因子-α依赖性和可能的选择素依赖性现象。在细胞质中，一些抗氧化特性和对脂氧合酶途径的抑制似乎具有相当的选择性，可能有助于产生抗毒作用。一些作用，如对诱导型一氧化氮合酶、核因子κB的抑制以及胶原蛋白合成的减少，表明存在DNA/RNA介导的效应。几项使用“体外”和“体内”癌症模型的研究表明水飞蓟素在这类疾病中具有潜在作用。局部和全身应用水飞蓟素对紫外线诱导的表皮损伤具有皮肤保护特性，并能上调肿瘤抑制基因p53和p21CIP1。在所审查的数据中，没有关于肝病毒复制、病毒血症或自发肿瘤的数据。
本文提供的数据并未解决药用植物水飞蓟素复杂作用机制的问题。水飞蓟素可能是一种天然的多功能、多靶点药物。
