Milk thistle nomenclature: Why it matters in cancer research and pharmacokinetic studies
Milk thistle nomenclature: Why it matters in cancer research and pharmacokinetic studies
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DOI：
10.1177/1534735407301825
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发表时间：
2007-06-01
影响因子：
2.9
通讯作者：
Oberlies, Nicholas H.
中科院分区：
文献类型：
--
作者：
Kroll, David J.;Shaw, Heather S.;Oberlies, Nicholas H.
几个世纪以来，奶蓟提取物一直被认为是“肝脏滋补品”，并且众所周知可以预防或逆转反应性药物代谢物或天然毒素的肝毒性。目前，奶蓟提取物在癌症的化学预防、治疗和改善化疗副作用的实验治疗学中处于紧张的研究中。然而，命名的精确性却落后于这一进展。水飞蓟的粗商业产品被称为水飞蓟素，其是至少7种黄酮木脂素和1种类黄酮的复合物，其包含65%至80%的水飞蓟提取物。从水飞蓟素衍生出水飞蓟宾，一种半纯化级分，曾经被认为是单一化合物，但现在被认为是2种非对映异构体水飞蓟宾A和水飞蓟宾B的1：1混合物。水飞蓟素和水飞蓟宾之间的区别不仅对理解历史文献很重要，而且在临床前和临床研究中彻底表征和使用化学定义的混合物对于这些植物化合物作为人类治疗剂的进展至关重要。因此，我们敦促临床医生和临床前研究人员严格使用命名法，并在后续研究中使用纯化合物或精确定义的化学混合物。在这里，我们提供了一个指南，正确的命名和组成的奶蓟提取物，并讨论了这些植物药的已知的药代动力学研究。这些提取物的药物相互作用潜力似乎相当低，事实上，水飞蓟宾似乎与一些常用的化疗药物的抗肿瘤作用协同作用。然而，在进行高剂量II期研究时，建议采取一些预防措施。
Extracts of milk thistle have been recognized for centuries as "liver tonics" and are well-known to prevent or reverse hepatotoxicity of reactive drug metabolites or naturally occurring toxins. Milk thistle extracts are now under intense study in the experimental therapeutics of cancer for chemoprevention, treatment, and amelioration of chemotherapy side effects. Precision in nomenclature, however, has lagged behind this progress. The crude commercial product of milk thistle is termed silymarin, a complex of at least 7 flavonolignans and I flavonoid that comprises 65% to 80% of milk thistle extract. From silymarin is derived silibinin, a semipurified fraction once thought to be a single compound but now recognized as a 1: 1 mixture of 2 diastereoisomers, silybin A and silybin B. The distinction between silymarin and silibinin is not only important to understanding the historical literature, but thorough characterization and use of chemically defined mixtures in preclinical and clinical studies are essential to the progress of these botanical compounds as human therapeutics. As a result, we urge clinicians and preclinical investigators alike to exercise rigor in nomenclature and use pure compounds or precisely defined chemical mixtures in subsequent studies. Herein, we provide a guide to the proper nomenclature and composition of milk thistle extracts and discuss the known pharmacokinetic studies of these botanical medicines. The drug-interaction potential of these extracts appears to be quite low, and in fact, silibinin appears to synergize with the antitumor effects of some commonly used chemotherapeutics. However, some precautions are advised as high-dose, phase II studies are conducted.