Acetylshikonin

Acetylshikonin is a naphthoquinone that has been found in L. erythrorhizon and has diverse biological activities.^1,2,3 It inhibits a panel of 10 cytochrome P450 (CYP) enzymes, including CYP1A2, CYP2D6, and CYP3A (IC₅₀s = 1.4-4.0 µM).¹ Acetylshikonin is cytotoxic to H1975, A549, PC-9, and H460 non-small cell lung cancer (NSCLC) cells (IC₅₀s = 3.9, 4.7, 20.7, and 17.3 µM, respectively).² It inhibits the migration of, as well as reduces EGFR and STAT3 signaling and induces apoptosis in, H1975, PC-9, and H460 cells when used at concentrations of 0.5, 1, and 2 µM. In vivo, acetylshikonin (1 mg/kg) reduces tumor weight and intratumoral STAT3 phosphorylation in an H1975 mouse xenograft model. It also inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) papain-like protease (PL^pro; IC₅₀ = 5.05 µM) and reduces bronchoalveolar lavage fluid (BALF) levels of Tnf-α, Il-1α, and Il-6 in a mouse model of acute lung injury induced by poly (I:C) and SARS-CoV-2 spike glycoprotein, also known as surface glycoprotein, when administered at a dose of 300 mg/kg.³

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1. Shon, J.C., Phuc, N.M., Kim, W.C., et al. Acetylshikonin is a novel non-selective cytochrome P450 inhibitor. Biopharm. Drug Dispos. 38(9), 553-556 (2017).

2. Tang, Y., Wang, Y., Wang, X., et al. Acetylshikonin exerts anti-tumor effects on non-small cell lung cancer through dual inhibition of STAT3 and EGFR. Phytomedicine 101, 154109 (40144).

3. Lu, N., Gu, T., Tian, X., et al. Acetylshikonin inhibits inflammatory responses and Papain-like protease activity in murine model of COVID-19. Signal Transduct. Target Ther. 7(1), 371 (2022).