Shikonin: From Biosynthesis and Pharmacological Mechanisms to Translational Safety and Drug Delivery
4 affiliations
- 1Plant Biotechnology Laboratory, Department of Biotechnology Graphic Era Deemed to be University Uttarakhand India
- 2School of Agriculture Graphic Era Hill University Dehradun Uttarakhand India
- 3Department of Chemistry College of Basic Sciences and Humanities G.B. Pant University of Agriculture and Technology U.S. Nagar Uttarakhand India
- 4Departamente de Química Instituto Federal de Educação Ciência e Tecnologia do Pará (IFPA) Redenção Brazil
Abstract
Shikonin (SHK) is a red naphthoquinone produced mainly in the roots of Boraginaceae species and has been investigated for anticancer, anti‐inflammatory, antimicrobial, neuroprotective, cardioprotective, hepatoprotective, and wound‐healing activities. This review critically integrates botanical sources and biosynthesis with pharmacological mechanisms, preclinical evidence, safety, and delivery strategies. Across cancer models, SHK converges on redox imbalance and regulated cell‐death programmes, including apoptosis, cell‐cycle arrest, autophagy, necroptosis, ferroptosis, and immunogenic cell death, while modulating NF‐κB, MAPK, PI3K/Akt, and related signalling networks. However, the evidence is dominated by heterogeneous in vitro experiments and small‐animal studies, with limited pharmacokinetic standardisation, incomplete assessment of selectivity toward diseased versus normal tissues, and almost no robust clinical evaluation. Poor aqueous solubility, chemical and photochemical instability, rapid metabolism, route‐dependent exposure, and a context‐dependent therapeutic window remain central translational barriers. Liposomes, polymeric micelles, nanoparticles, nanogels, nanoemulsions, and ligand‐ or stimulus‐responsive systems can improve dispersion, tissue accumulation, controlled release, and combination therapy; nevertheless, their long‐term safety, manufacturing reproducibility, and comparative advantage over free SHK require rigorous validation. SHK should therefore be regarded as a mechanistically versatile therapeutic lead rather than a clinically established treatment. Translation will depend on exposure–response studies, standardised formulations, clinically relevant models, and well‐designed human trials.
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BibTeX
@article{joshi2026shikonin,
title = {{Shikonin: From Biosynthesis and Pharmacological Mechanisms to Translational Safety and Drug Delivery}},
author = {Namini Joshi and Prabhakar Semwal and Balwant Rawat and Ravendra Kumar and Mozaniel Santana de Oliveira and Nishant Rai and Janhvi Mishra Rawat},
journal = {Chembiochem},
year = {2026},
month = nov,
doi = {10.1002/cbic.70586},
url = {https://doi.org/10.1002/cbic.70586},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Shikonin: From Biosynthesis and Pharmacological Mechanisms to Translational Safety and Drug Delivery
AU - Namini Joshi
AU - Prabhakar Semwal
AU - Balwant Rawat
AU - Ravendra Kumar
AU - Mozaniel Santana de Oliveira
AU - Nishant Rai
AU - Janhvi Mishra Rawat
PY - 2026
DA - 2026/11/05
JO - Chembiochem
DO - 10.1002/cbic.70586
UR - https://doi.org/10.1002/cbic.70586
AB - Shikonin (SHK) is a red naphthoquinone produced mainly in the roots of Boraginaceae species and has been investigated for anticancer, anti‐inflammatory, antimicrobial, neuroprotective, cardioprotective, hepatoprotective, and wound‐healing activities. This review critically integrates botanical sources and biosynthesis with pharmacological mechanisms, preclinical evidence, safety, and delivery strategies. Across cancer models, SHK converges on redox imbalance and regulated cell‐death programmes, including apoptosis, cell‐cycle arrest, autophagy, necroptosis, ferroptosis, and immunogenic cell death, while modulating NF‐κB, MAPK, PI3K/Akt, and related signalling networks. However, the evidence is dominated by heterogeneous in vitro experiments and small‐animal studies, with limited pharmacokinetic standardisation, incomplete assessment of selectivity toward diseased versus normal tissues, and almost no robust clinical evaluation. Poor aqueous solubility, chemical and photochemical instability, rapid metabolism, route‐dependent exposure, and a context‐dependent therapeutic window remain central translational barriers. Liposomes, polymeric micelles, nanoparticles, nanogels, nanoemulsions, and ligand‐ or stimulus‐responsive systems can improve dispersion, tissue accumulation, controlled release, and combination therapy; nevertheless, their long‐term safety, manufacturing reproducibility, and comparative advantage over free SHK require rigorous validation. SHK should therefore be regarded as a mechanistically versatile therapeutic lead rather than a clinically established treatment. Translation will depend on exposure–response studies, standardised formulations, clinically relevant models, and well‐designed human trials.
SN - 1439-4227
SN - 1439-7633
ER -