Drug intelligence / Profile preview

arctiin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal, Intraarticular
01

Overview

Arctiin is a **natural lignan glycoside** isolated primarily from the seeds of *Arctium lappa* (burdock) and is a major active component of the medicinal herb known as Fructus Arctii[4][8]. It acts as a **prodrug** for arctigenin, meaning it is converted into the active form arctigenin in vivo[1][4]. Arctiin exhibits a variety of biological activities, including **anti-inflammatory, antioxidant, antiviral, and antiproliferative (anti-cancer) effects**[1][2][3][4][6][7][9]. Its mechanism of action is multifaceted and includes suppression of cyclin D1 protein expression, inhibition of inflammatory pathways (by reducing nitric oxide, prostaglandin E2, TNF-α, interleukin-1β, and IL-6), and antioxidant effects through activation of nuclear factor erythroid 2-related factor 2 (NRF2)[2][4][6][7]. Studies have shown efficacy in models of metabolic disorders, osteoarthritis, neuroprotection, and various cancers, though most human data are preclinical[1][2][4][6][7]. Arctiin is also reported to have anti-osteoporotic and anti-diabetic potential[2][6].

Other names
ArctinArctiiArctlin(-)-arctiinArctiin-RMArctigenin4GlucosideArctigenin-4GlucosideArctigenin 4Glucoside
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)IL-6 (Interleukin 6)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)CCND1 (Cyclin D1)TNFA (Tumor necrosis factor alpha (soluble))NOS2 (Nitric Oxide Synthase 2)IL1B (Interleukin-1 beta)

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