Shikonin

製品コードS8279 バッチS827901

印刷

化学情報

Chemical Structure Synonyms C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H16O5
分子量 288.30 CAS No. 54952-43-1
Solubility (25°C)* 体外 DMSO 57 mg/mL (197.71 mM)
Ethanol 23 mg/mL (79.77 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
in vitro

At nanomolar concentrations, shikonin inhibits monocyte chemotaxis and calcium flux in response to a variety of CC chemokines (CCL2 [monocyte chemoattractant protein 1], CCL3 [macrophage inflammatory protein 1α], and CCL5 [regulated upon activation, normal T-cell expressed and secreted protein]), the CXC chemokine (CXCL12 [stromal cell-derived factor 1α]), and classic chemoattractants (formylmethionyl-leucine-phenylalanine and complement fraction C5a). Shikonin down-regulates surface expression of CCR5, a primary HIV-1 coreceptor, on macrophages. The anti-HIV and anti-inflammatory activities of shikonin may be related to its interference with chemokine receptor expression and function[1]. Shikonin inhibits enterocyte calcium-activated chloride channels, the inhibitory effect is partially through inhibition of basolateral K+ channel activity[2].
in vivo

Shikonin significantly delays intestinal motility in mice and reduces stool water content in a neonatal mice model of rotaviral diarrhea without affecting the viral infection process in vivo. Shikonin has been reported to have antioxidant, antibacterial, antiparasitic, antiviral and wound-healing activities. Shikonin inhibits allergic action as well as tracheal hyperresponsiveness in vivo. Intraperitonal injection of shikonin has been demonstrated to result in some toxicity, with an LD50 of 20 mg/kg. Shikonin absorption is fast if given by oral gavage and muscle injection, as it is barely detected in the plasma after 1 min, with a oral gavage yielding a bioavailability of about 34%[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human monocytes
濃度 10, 1, 0.1, 0.01 μM
反応時間 12 and 24 hours
実験の流れ

Freshly isolated human monocytes are plated in a 96-microwell plate (Costar) at 105 cells per well with shikonin at a final concentration of 10, 1, 0.1, 0.01 μM. The numbers of viable cells, as detected by MTS test and the trypan blue exclusion assay, were measured 12 and 24 h after incubation at 37°C in humidified air with 5% CO2.
動物実験 動物モデル Neonatal ICR mice
投薬量 0.4 and 1.7 μg in 30 μL PBS
投与方法 oral administration

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

PKM2-mediated neuronal hyperglycolysis enhances the risk of Parkinson's disease in diabetic rats [ J Pharm Anal, 2023, 13(2):187-200] PubMed: 36908857
Shikonin reverses pyruvate kinase isoform M2-mediated propranolol resistance in infantile hemangioma through reactive oxygen species-induced autophagic dysfunction [ Cancer Sci, 2023, 114(3):806-821] PubMed: 36369903
Metabolic Reprogramming by Ribitol Expands the Therapeutic Window of BETi JQ1 against Breast Cancer [ Cancers (Basel), 2023, 15(17)4356] PubMed: 37686632
Metabolic Reprogramming by Ribitol Expands the Therapeutic Window of BETi JQ1 against Breast Cancer [ Cancers (Basel), 2023, 15(17)4356] PubMed: 37686632
Shikonin improves pulmonary vascular remodeling in monocrotaline‑induced pulmonary arterial hypertension via regulation of PKM2 [ Mol Med Rep, 2023, 27(3)60] PubMed: 36734266
Celastrol mitigates inflammation in sepsis by inhibiting the PKM2-dependent Warburg effect [ Mil Med Res, 2022, 9(1):22] PubMed: 35596191
Pyruvate Facilitates FACT-Mediated γH2AX Loading to Chromatin and Promotes the Radiation Resistance of Glioblastoma [ Adv Sci (Weinh), 2022, 10.1002/advs.202104055] PubMed: 35048565
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] PubMed: 35332332
Integrin β3-PKM2 pathway-mediated aerobic glycolysis contributes to mechanical ventilation-induced pulmonary fibrosis [ Theranostics, 2022, 12(14):6057-6068] PubMed: 36168620
Capsaicin ameliorates inflammation in a TRPV1-independent mechanism by inhibiting PKM2-LDHA-mediated Warburg effect in sepsis [ Cell Chem Biol, 2022, S2451-9456(22)00243-4] PubMed: 35858615

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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