School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong SAR, China.
Acta Pharmacol Sin. 2018 May;39(5):787-801. doi: 10.1038/aps.2018.32. Epub 2018 Apr 26.
Arctigenin (AR) and its glycoside, arctiin, are two major active ingredients of Arctium lappa L (A lappa), a popular medicinal herb and health supplement frequently used in Asia. In the past several decades, bioactive components from A lappa have attracted the attention of researchers due to their promising therapeutic effects. In the current article, we aimed to provide an overview of the pharmacology of AR and arctiin, focusing on their anti-inflammatory effects, pharmacokinetics properties and clinical efficacies. Compared to acrtiin, AR was reported as the most potent bioactive component of A lappa in the majority of studies. AR exhibits potent anti-inflammatory activities by inhibiting inducible nitric oxide synthase (iNOS) via modulation of several cytokines. Due to its potent anti-inflammatory effects, AR may serve as a potential therapeutic compound against both acute inflammation and various chronic diseases. However, pharmacokinetic studies demonstrated the extensive glucuronidation and hydrolysis of AR in liver, intestine and plasma, which might hinder its in vivo and clinical efficacy after oral administration. Based on the reviewed pharmacological and pharmacokinetic characteristics of AR, further pharmacokinetic and pharmacodynamic studies of AR via alternative administration routes are suggested to promote its ability to serve as a therapeutic agent as well as an ideal bioactive marker for A lappa.
牛蒡子中的牛蒡苷元和牛蒡苷是牛蒡（Arctium lappa L.）的两种主要活性成分，牛蒡是一种在亚洲广泛应用的药用植物和保健品。在过去几十年中，牛蒡子的生物活性成分因其有希望的治疗效果而引起了研究人员的关注。在本文中，我们旨在概述牛蒡子苷元和牛蒡苷的药理学特性，重点介绍它们的抗炎作用、药代动力学特性和临床疗效。与牛蒡苷相比，在大多数研究中，牛蒡子苷元被报道为牛蒡子中最有效的生物活性成分。牛蒡子苷元通过调节几种细胞因子抑制诱导型一氧化氮合酶（iNOS）来发挥其强大的抗炎作用。由于其强大的抗炎作用，牛蒡子苷元可能成为治疗急性炎症和各种慢性疾病的潜在治疗化合物。然而，药代动力学研究表明，牛蒡子苷元在肝脏、肠道和血浆中广泛发生葡萄糖醛酸化和水解，这可能会阻碍其口服后的体内和临床疗效。基于对牛蒡子苷元的药理学和药代动力学特性的综述，建议通过替代给药途径进一步进行牛蒡子苷元的药代动力学和药效学研究，以提高其作为治疗剂的能力以及作为牛蒡子的理想生物活性标志物的能力。
