Plumbagin

Catalog No.S4777 Batch:S477701

Technical Data

Formula	C₁₁H₈O₃
Molecular Weight	188.18	CAS No.	481-42-5
Solubility (25°C)*	In vitro	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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description	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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines MDA-MB-231 and MCF-7 cell lines Concentrations 0, 2.5, 5, 10, and 20 μmol/L Incubation Time 48 h Method 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.
Animal Study:^{^[1]}	Animal Models 6 weeks old; BALB/cA-nu (nu/nu) mice with xenograft tumor Dosages 2 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
MDA-MB-231 and MCF-7 cell lines
Concentrations
0, 2.5, 5, 10, and 20 μmol/L
Incubation Time
48 h
Method
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.

Animal Study:^{^[1]}

Animal Models
6 weeks old; BALB/cA-nu (nu/nu) mice with xenograft tumor
Dosages
2 mg/kg
Administration
i.p.

References

Selleck's Plumbagin has been cited by 5 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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