Abstract

BackgroundWe have investigated the potential anticancer effects of karanjin, a principal furanoflavonol constituent of the Chinese medicine Fordia cauliflora, using cytotoxic assay, cell cycle arrest, and induction of apoptosis in three human cancer cell lines (A549, HepG2 and HL-60 cells).ResultsMTT cytotoxic assay showed that karanjin could inhibit the proliferation and viability of all three cancer cells. The induction of cell cycle arrest was observed via a PI (propidium iodide)/RNase Staining Buffer detection kit and analyzed by flow cytometry: karanjin could dose-dependently induce cell cycle arrest at G2/M phase in the three cell lines. Cell apoptosis was assessed by Annexin V-FITC/PI staining: all three cancer cells treated with karanjin exhibited significantly increased apoptotic rates, especially in the percentage of late apoptosis cells.ConclusionKaranjin can induce cancer cell death through cell cycle arrest and enhance apoptosis. This compound may be effective clinically for cancer pharmacotherapy.

Highlights

  • We have investigated the potential anticancer effects of karanjin, a principal furanoflavonol constituent of the Chinese medicine Fordia cauliflora, using cytotoxic assay, cell cycle arrest, and induction of apoptosis in three human cancer cell lines (A549, HepG2 and HL-60 cells)

  • Effect of Karanjin on growth of tumor cells Prompted by our interest in the antitumor activity of flavonoid compounds, we have investigated the cytotoxic effect and apoptotic property of karanjin in various human cancer cell lines A549, HepG2, and HL-60 representing respectively lung adenocarcinoma, hepatocarcinoma and promeylocytic leukemia that are prevalent with high mortality in humans

  • IC50 values of A549 cells decreased steeply with increased drug exposure time, and they were higher than the corresponding IC50 values of HepG2 and HL-60 cells

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Summary

Introduction

We have investigated the potential anticancer effects of karanjin, a principal furanoflavonol constituent of the Chinese medicine Fordia cauliflora, using cytotoxic assay, cell cycle arrest, and induction of apoptosis in three human cancer cell lines (A549, HepG2 and HL-60 cells). Fordia cauliflora Hemsl, belongs to the family of Leguminosae and is, known in Chinese as “Shuiluosan”. It has been used in China as a traditional folk medicine for bronchitis, rheumatism, bruise, dementia of children, and valetudinarianism [1, 2]. Karanjin (structure depicted in Figure 1) is a major active furanoflavonol constituent of Fordia cauliflora Hemsl. It is associated with the above pharmacological activities, and has been reported to exert anti-hyperglycemic action [7] and ability of inducing GLUT4 translocation in skeletal muscle cells by increasing AMPactivated protein kinase activity [8]. Michaelis et al found that karanjin could interfere with drug

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