Plumbagin

Catalog No.S4777 Synonyms: Plumbagine, Plumbaein, Plumbagone

For research use only.

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.

Plumbagin Chemical Structure

CAS No. 481-42-5

Selleck's Plumbagin has been cited by 3 Publications

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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 Research:[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.
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: 6 weeks old; BALB/cA-nu (nu/nu) mice with xenograft tumor
  • Dosages: 2 mg/kg
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 37 mg/mL
(196.62 mM)


* 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.

Chemical Information

Molecular Weight 188.18
Formula

C11H8O3

CAS No. 481-42-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=O)C2=C(C1=O)C=CC=C2O

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