Shikonin derivatives for cancer prevention and therapy

• Published in: Cancer letters Vol. 459; pp. 248 - 267
• Main Authors: Boulos, Joelle C., Rahama, Muhammad, Hegazy, Mohamed-Elamir F., Efferth, Thomas
• Format: Journal Article
• Language: English
• Published: Ireland Elsevier B.V 10.09.2019; Elsevier Limited
• Subjects: Acids; Angiogenesis; Antineoplastic drugs; Antitumor agents; Apoptosis; Autophagy; Biosynthesis; Breast cancer; Cancer; Cancer therapies; Cell adhesion & migration; Cell culture; Cell cycle; Chemical composition; Chemotherapy; Clinical trials; Colorectal cancer; Dermatitis; DNA damage; Drugs; Hydrocarbons; Immunotherapy; Inflammation; Kinases; Liver cancer; Lung cancer; Metabolism; Metabolites; Metastasis; Microorganisms; Nanotechnology; Naphthoquinone; Natural resources; Oncology; Peptides; Phytochemical; Prostate cancer; Proteins; Radiation therapy; Shikonin; Synergistic interactions; Chemotherapy; Immunotherapy; Naphthoquinone; Nanotechnology; Phytochemical; Synergistic interactions
• ISSN: 0304-3835; 1872-7980
• DOI: 10.1016/j.canlet.2019.04.033

Phytochemicals gained considerable interest during the past years as source to develop new treatment options for chemoprevention and cancer therapy. Motivated by the fact that a majority of established anticancer drugs are derived in one way or another from natural resources, we focused on shikonin, a naphthoquinone with high potentials to be further developed as preventive or therapeutic drug to fight cancer. Shikonin is the major chemical component of Lithospermum erythrorhizon (Purple Cromwell) roots. Traditionally, the root extract has been applied to cure dermatitis, burns, and wounds. Over the past three decades, the anti-inflammatory and anticancer effects of root extracts, isolated shikonin as well as semi-synthetic and synthetic derivatives and nanoformulations have been described. In vitro and in vivo experiments were conducted to understand the effect of shikonin at cellular and molecular levels. Preliminary clinical trials indicate the potential of shikonin for translation into clinical oncology. Shikonin exerts additive and synergistic interactions in combination with established chemotherapeutics, immunotherapeutic approaches, radiotherapy and other treatment modalities, which further underscores the potential of this phytochemical to be integrated into standard treatment regimens. •Shikonin is a natural product with activity in vitro, in vivo and preliminary clinical trials.•Shikonin can be modified chemically for derivatives with improved pharmacological features.•Shikonin can be produced by methods of molecular biotechnology.•Shikonin produces synergistic interactions with established anticancer drugs.