Drug intelligence / Profile preview

shikonin

Development stage
Phase 2
Modality
Small Molecules
Administration
Topical
01

Overview

Shikonin is a naturally occurring naphthoquinone compound primarily isolated from the roots of Lithospermum erythrorhizon and related species in the Boraginaceae family. It is well known for its diverse pharmacological activities including potent anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, and wound healing effects[2][3][4][5]. Shikonin exerts anticancer activity by inducing apoptosis through upregulation of Death Receptor 5 (DR5) via ROS-mediated JNK signaling and by triggering necroptosis through activation of MLKL and modulation of RIP1/RIP3 pathways[6]. It also disrupts autophagic flux to enhance cancer cell death. In addition to its antitumor properties across various cancer types such as breast cancer[8], shikonin demonstrates strong antibacterial activity against Gram-positive bacteria (e.g., Staphylococcus aureus), fungicidal effects against Candida species, and significant anti-inflammatory action by modulating cytokine production (IL-1, IL-2, IFN-gamma) and reducing vascular permeability at sites of inflammation[2]. Traditionally used in herbal medicine for skin diseases like dermatitis and burns due to its wound healing capabilities[4][5], shikonin has also shown potential as a pan-chemokine receptor inhibitor with possible applications in HIV therapy[2].

Other names
5,8-dihydroxy-2-[(1R)-1-hydroxy-4-methyl-3-pentenyl]-1,4-naphthoquinoneNEZONWMXZKDMKF-SNVBAGLBSA-N
02

Targets

TNFRSF10B (DR5)EGFR (Epidermal growth factor receptor)MLKL (Mixed lineage kinase domain-like protein)LY96 (Myeloid differentiation factor 2)RIPK1 (Receptor-interacting serine/threonine-protein kinase 1)RIPK3TXNRD1 (Thioredoxin reductase 1)

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