Deoxyshikonin is a natural product isolated from Lithospermum erythrorhizon Sieb with antitumor activity[1]. Deoxyshikonin has proangiogenesis effect by increasing the expression of VEGF-C and VEGF-A mRNA in human microvascular endothelial cells–dermal lymphatic (HMVEC-dLy), promoting HIF-1α and HIF-1β subunit interaction and binding to specific DNA sequences targeted by HIF[2]. Deoxyshikonin is also an antibacterial agent against methicillin-resistant S. aureus (MRSA) and S. pneumonia[3]. Deoxyshikonin is usually used in research related to tumors and infections[4][5].
In vitro, Deoxyshikonin (2.5-20μM; 24h) dose-dependently reduced viability, induced sub-G1 arrest, and triggered apoptosis in human osteosarcoma U2OS and HOS cells[6].
In vivo, Deoxyshikonin (10mg/kg/day; 21 days; topical) shortened telogen and prolonged anagen, increased hair-follicle density, diameter and length, elevated VEGF/IGF-1, and reduced TGF-β1 in depilated alopecia areata C57BL/6 mice[7].
References:
[1] Zhu Y, Zhong Y, Long X, et al. Deoxyshikonin isolated from Arnebia euchroma inhibits colorectal cancer by down-regulating the PI3K/Akt/mTOR pathway. Pharm Biol. 2019;57(1):412-423.
[2] Prangsaengtong O, Park JY, Inujima A, Igarashi Y, Shibahara N, Koizumi K. Enhancement of Lymphangiogenesis In Vitro via the Regulations of HIF-1α Expression and Nuclear Translocation by Deoxyshikonin. Evid Based Complement Alternat Med. 2013;2013:148297.
[3] Zhang S, Wang J, Xu W, et al. Antibacterial effects of Traditional Chinese Medicine monomers against Streptococcus pneumoniae via inhibiting pneumococcal histidine kinase (VicK). Front Microbiol. 2015;6:479.
[4] Zhang S, Wang Y. Deoxyshikonin inhibits cisplatin resistance of non-small-cell lung cancer cells by repressing Akt-mediated ABCB1 expression and function. J Biochem Mol Toxicol. 2020;34(10):e22560.
[5] Cho WK, Ma JY. Deoxyshikonin Inhibits Influenza A Virus Infection at an Early Stage. Int J Mol Sci. 2025;26(17):8158.
[6] Hsieh MC, Hsieh YH, Chou CH, et al. Apoptotic effect and cell arrest of deoxyshikonin in human osteosarcoma cells through the p38 pathway. J Cell Mol Med. 2023;27(11):1592-1602.
[7] Li Y, Mu Y, Chen X, et al. Deoxyshikonin from Arnebiae Radix promotes hair growth by targeting the Wnt/β-catenin signaling pathway. Phytomedicine. 2025;140:156590.
Deoxyshikonin是从紫草（Lithospermum erythrorhizon Sieb）中分离得到的一种具有抗肿瘤活性的天然产物[1]。Deoxyshikonin通过上调人皮肤微淋巴管内皮细胞（HMVEC-dLy）中VEGF-C和VEGF-A mRNA的表达，促进HIF-1α与HIF-1β亚基的相互作用并增强HIF对特定DNA序列的结合，从而发挥促血管生成作用[2]。Deoxyshikonin还对耐甲氧西林金黄色葡萄球菌（MRSA）和肺炎链球菌具有抗菌活性[3]。Deoxyshikonin常用于肿瘤及感染相关研究[4][5]。
体外实验显示，Deoxyshikonin（2.5-20μM，24h）可浓度依赖性地降低人骨肉瘤U2OS和HOS细胞的活力，诱导sub-G1期阻滞并触发凋亡[6]。
体内实验表明，Deoxyshikonin（10mg/kg/天；连续21天；外用）可缩短脱毛C57BL/6斑秃小鼠休止期、延长生长期，增加毛囊密度、直径和长度，提升VEGF/IGF-1水平并降低TGF-β1含量[7]。