Chemical Name: 5,8-Dihydroxy-2-[(1R)-1-hydroxy-4-methyl-3-penten-1-yl]-1,4-naphthalenedione
Biological Activity(R)-Shikonin is a PTEN and inflammasome inhibitor. Inhibits PTEN's phosphatase activity (IC50 = 2.7 μM) and NLRP3 activation. Also blocks TNF-α and NF-κB signaling. Attenuates HIV-1 replication at nanomolar concentrations. Suppresses glycolysis in cancer cells by inhibiting tumor-specific pyruvate kinase M2 (PKM2) (IC50 = 0.3 μM). Induces necroptosis in MCF-7 and HEK293 cancer cell lines. Displays anti-inflammatory activity in a mouse model of collagen-induced arthritis.
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The therapeutic potential of PTEN modulation: targeting strategies from gene to protein.
McLoughlin et al.
Cell Chem.Biol., 2018;25:19
A naphthoquinone derivative, shikonin, has insulin-like actions by inhibiting both phosphatase and tensin homolog deleted on chromosome 10 and tyrosine phosphatases.
Nigorikawa et al.
NLRP3 lacking the leucine-rich repeat domain can be fully activated via the canonical inflammasome pathway.
Hafner-Bratkovic et al.
Shikonin and its analogs inhibit cancer cell glycolysis by targeting tumor pyruvate kinase-M2.
Chen et al.
Shikonin circumvents cancer drug resistance by induction of a necroptotic death.
Han et al.
Mol. Cancer Ther., 2007;6:1641
Shikonin, a Component of Chinese Herbal Medicine, Inhibits Chemokine Receptor Function and Suppresses Human Immunodeficiency Virus Type 1
Chen et al.
Antimicrob. Agents Chemother., 2003;47:2810
The efficacy of shikonin on cartilage protection in a mouse model of rheumatoid arthritis.
Kim et al.
Korean J.Physiol.Pharmacol., 2010;14:199
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