(±)-Shikonin

製品コードS8279 バッチS827903

印刷

化学情報

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

20 mg/mL (69.37 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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は、強力かつ特異的なピルビン酸キナーゼM2（PKM2）阻害剤であり、様々な生物学的活性を持つ中国漢方薬である紫草（ムラサキ科植物Lithospermum erythrorhizonの乾燥根）の主要成分です。また、細胞ベースの蛍光クエンチングアッセイを用いて、TMEM16A塩化物チャネル活性の阻害剤でもあります。(±)-Shikoninは、腫瘍壊死因子-α（TNF-α）を阻害することで抗炎症作用を発揮し、プロテアソーム阻害を介して核因子-κB（NF-κB）経路の活性化を防ぎます。
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. Shikonin inhibits enterocyte calcium-activated chloride channels, the inhibitory effect is partially through inhibition of basolateral K+ channel activity.
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%.

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

参考

https://pubmed.ncbi.nlm.nih.gov/12936978/
http://journal.frontiersin.org/article/10.3389/fphar.2016.00270/full
https://pubmed.ncbi.nlm.nih.gov/21516121/

https://pubmed.ncbi.nlm.nih.gov/26265618

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UCHL3 augments cuproptosis via PKM2 deubiquitination in hepatocellular carcinoma [ Free Radic Biol Med, 2025, 237:65-75]	PubMed: 40451468
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The Activation of PKM2 Induces Pyroptosis in Hippocampal Neurons via the NLRP3/Caspase-1/GSDMD Pathway in Neonatal Rats With Hypoxic-Ischemic Brain Injury [ Brain Behav, 2024, 14(10):e70108]	PubMed: 39444090
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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。