Plumbagin

製品コードS4777 バッチS477701

印刷

化学情報

Chemical Structure Synonyms Plumbagine, Plumbaein, Plumbagone Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C11H8O3
分子量 188.18 CAS No. 481-42-5
Solubility (25°C)* 体外 DMSO 37 mg/mL (196.62 mM)
 
 
* <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 Plumbagin (Plumbagine, Plumbaein, Plumbagone), a quinoid constituent isolated from the root of the medicinal plant Plumbago zeylanica L, exerts anticancer and antiproliferative activities in animal models and in cell culture.
in vitro Plumbagin exhibits cell proliferation inhibition by inducing cells to undergo G2-M arrest and autophagic cell death. Blockade of the cell cycle is associated with increased p21/WAF1 expression and Chk2 activation, and reduced amounts of cyclin B1, cyclin A, Cdc2, and Cdc25C. Plumbagin also reduces Cdc2 function by increasing the association of p21/WAF1/Cdc2 complex and the levels of inactivated phospho-Cdc2 and phospho-Cdc25C by Chk2 activation. Plumbagin triggers autophagic cell death but not pre-dominantly apoptosis. It inhibits survival signaling through the phosphatidylinositol 3-kinase/AKT signaling pathway by blocking the activation of AK Tand downstream targets, including the mammalian target of rapamycin, forkhead transcription factors, and glycogen synthase kinase 3B. Phosphorylation of both of mammalian target of rapamycin downstream targets, p70 ribosomal protein S6 kinase and 4E-BP1, are also diminished[1].
in vivo Plumbagin inhibits tumor growth in nude mice[1]. Mice treated with liposomal formulation of plumbagin are shown to achieve higher plasma and tissue level and area under the concentration-time curve (AUC) compared with those treated with the water-soluble plumbagin. Moreover, high concentration is found in liver and spleen of mice. In vivo pharmacokinetics study also demonstrates that orally administered plumbagin produces only 39% systemic bioavailability due to its limited biopharmaceutical properties such as high lipophilicity (log P 3.04) and insolubility in water[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MDA-MB-231 and MCF-7 cell lines
濃度 0, 2.5, 5, 10, and 20 μmol/L
反応時間 48 h
実験の流れ Inhibition of cell proliferation by plumbagin is measured by XTT assay. Cells are plated in 96-well culture plates (1×104 per well). After 24-h incubation, the cells are treated with plumbagin (0, 2.5, 5, 10, and 20 μmol/L) for 48 h. Fifty microliters of XTT test solution, which is prepared by mixing 5 mL of XTT-labeling reagent with 100 μL of electron coupling reagent, are then added to each well. The absorbance is measured on an ELISA reader at test wavelength of 492 nm and a reference wavelength of 690 nm.
動物実験 動物モデル 6 weeks old; BALB/cA-nu (nu/nu) mice with xenograft tumor
投薬量 2 mg/kg
投与方法 i.p.

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：

Plumbagin is a novel GPX4 protein degrader that induces apoptosis in hepatocellular carcinoma cells [ Free Radic Biol Med, 2023, 203:1-10] PubMed: 37011699
Plumbagin protects H9c2 cardiomyocytes against TBHP-induced cytotoxicity by alleviating ROS-induced apoptosis and modulating autophagy [ Exp Ther Med, 2022, 24(2):501] PubMed: 35837065
Novel Mechanistic Observations and NES-Binding Groove Features Revealed by the CRM1 Inhibitors Plumbagin and Oridonin [ J Nat Prod, 2021, 10.1021/acs.jnatprod.0c01231] PubMed: 33890470
Engineering Chromosome Region Maintenance 1 Fragments That Bind to Nuclear Export Signals [ Protein Sci, 2020, 29(6):1366-1372] PubMed: 31495993
Plumbagin attenuated oxygen-glucose deprivation/reoxygenation-induced injury in human SH-SY5Y cells by inhibiting NOX4-derived ROS-activated NLRP3 inflammasome. [ Biosci Biotechnol Biochem, 2020, 84(1):134-142] PubMed: 31490096

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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