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。
Cas No.:43043-74-9
Sample solution is provided at 25 µL, 10mM.
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]。
| Cell experiment [1]: | |
Cell lines | Human osteosarcoma U2OS and HOS cells |
Preparation Method | U2OS cells (osteogenic sarcoma; human, 15-year-old female) were cultured in DMEM supplemented with 10% FBS, 1% penicillin/streptomycin and 5mL of glutamine. HOS cells (human osteosarcoma; 13-year-old female) were cultured in Eagle's MEM supplemented with 10% FBS, 1% penicillin/streptomycin, and 5mL glutamine. Cells were cultured at 37°C in a humidified atmosphere of 5% CO2 in an incubator and treated with Deoxyshikonin (2.5, 5, 10 and 20μM) for 24h. MTT colorimetric assay was performed to examine cell viability. FITC Annexin V Apoptosis Detection Kit was used to determine the apoptotic effect and flow cytometry was performed to analyse cell cycles. |
Reaction Conditions | 2.5-20μM; 24h |
Applications | Deoxyshikonin dose-dependently reduced viability, induced sub-G1 arrest, and triggered apoptosis in human osteosarcoma U2OS and HOS cells. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 mice (age=6 weeks, male, weight=21±2g) were kept at 23±2℃ in 12h dark/light cycle and 55% humidity with ad libitum access to chow and water. The alopecia mice model was established by topically applying depilatory paste to a 6cm² dorsal skin area using a cotton swab once daily for 21 days. Skin color and hair growth were monitored daily, and photographs were taken to document treatment effects over time. After hair removal, Deoxyshikonin (10mg/kg) were topically applied to mice. On day 14, after the depilator application, regrown hairs were randomly plucked from each mouse to measure average hair length. On day 21, a 1cm diameter circular skin sample was biopsied from the depilated area on each mouse’s back using a biopsy punch. Furthermore, hairs were scraped off, and their total weight was measured. Moreover, the lengths of 10 randomly selected hairs from the scraped sample were measured using a vernier caliper. The skin tissue content of TGF-β1, VEGF, and IGF-1 in alopecia mice was assessed by ELISA kit. |
Dosage form | 10mg/kg/day; 21 days; topical |
Applications | Deoxyshikonin 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. |
References: | |
| Cas No. | 43043-74-9 | SDF | |
| 别名 | 去氧紫草素 | ||
| Canonical SMILES | O=C1C(CC/C=C(C)/C)=CC(C2=C1C(O)=CC=C2O)=O | ||
| 分子式 | C16H16O4 | 分子量 | 272.3 |
| 溶解度 | DMSO : 33.33 mg/mL (122.40 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6724 mL | 18.3621 mL | 36.7242 mL |
| 5 mM | 734.5 μL | 3.6724 mL | 7.3448 mL |
| 10 mM | 367.2 μL | 1.8362 mL | 3.6724 mL |
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2.
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