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.

中文翻译：

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Arctium lappa L的Arctigenin和Arctiin的抗炎作用，药代动力学特性和临床疗效概述。

Arctigenin（AR）及其糖苷Arctiin是Arctium lappa L（A lappa）的两种主要活性成分，Arctium lappa L（A lappa）是一种流行的草药和健康补充剂，在亚洲经常使用。在过去的几十年中，来自A lappa的生物活性成分因其有希望的治疗作用而引起了研究人员的关注。在当前的文章中，我们旨在概述AR和Arctiin的药理作用，重点是它们的抗炎作用，药代动力学特性和临床疗效。与a啶酶相比，在大多数研究中，AR被报告为A lappa中最有效的生物活性成分。AR通过调节几种细胞因子来抑制诱导型一氧化氮合酶（iNOS），从而表现出强大的抗炎活性。由于其有效的抗炎作用，AR可以作为针对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AR在肝脏，肠和血浆中广泛的葡糖醛酸苷化和水解，这可能会阻碍口服后AR的体内和临床疗效。基于已审查的AR的药理和药代动力学特征，建议通过替代给药途径对AR进行进一步的药代动力学和药效学研究，以增强其作为A lappa的治疗剂和理想生物活性标记物的能力。口服后可能会影响其体内和临床疗效。基于已审查的AR的药理和药代动力学特征，建议通过替代给药途径对AR进行进一步的药代动力学和药效学研究，以增强其作为A lappa的治疗剂和理想生物活性标记物的能力。口服后可能会影响其体内和临床疗效。基于已审查的AR的药理和药代动力学特征，建议通过替代给药途径对AR进行进一步的药代动力学和药效学研究，以增强其作为A lappa的治疗剂和理想生物活性标记物的能力。