Effects of coumarin and 7OH‐coumarin on bcl‐2 and Bax expression in two human lung cancer cell lines in vitro

Abstract

Coumarin and its derivative 7-hydroxycoumarin (7-OHC) have antitumor and antimetastatic properties. The purpose of this study was to investigate the possible effects of these compounds on expression of the bcl-2 and Bax oncoproteins in two human lung cancer cell lines, A427 and Calu-1. The cells were cultured in vitro for 24 h in RPMI 1640 with 1.5% (v/v) ethanol, 1.0 mM ethanolic coumarin or 1.0 mM ethanolic 7-OHC. Viability was determined in each cell line by an MTT assay. Total protein was extracted from cell lysates and the bcl-2 and Bax oncoproteins were identified. Western blotting showed a decrease in bcl-2 and an increase in Bax in A427 cells cultured with coumarin or 7-OHC. Neither drug changed bcl-2 expression in Calu-1 cells compared to solvent controls, and Bax expression was only slightly increased by coumarin. We conclude that 7-OHC is a more potent inhibitor of cell proliferation than coumarin and has more marked effects on oncoprotein expression. Also, the A427 cell line was more sensitive to the drugs than Calu-1.

Cell cycle arrest and differentiation induction by 5,7-dimethoxycoumarin in melanoma cell lines

“…Coumarins and their derivative compounds have been used in clinical treatment, alone or in combination therapy, of various malignant cancers, such as renal, lung and kidney carcinoma and malignant melanoma (15). Various in vitro data showed antineoplastic activity of these compounds, such as 7-hydroxycoumarin against lung adenocarcinoma and other cell lines (16)(17)(18)(19), the synthetic 6-nitro-7-hydroxycoumarin against renal and melanoma cell lines (20)(21)(22), esculetin against human leukemia cells (23), decursin against human prostate carcinoma cells (24), and daphnetin against human renal carcinoma cells (22).…”

Crystal structure of 2-amino-4-(3,5-difluoro-phenyl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile, C16H12F2N2O2

“…as anticoagulant, insecticidal, antihelminthic, hypnotic, and antifungal activities, phytoalexin production, and HIV protease inhibition [1][2][3]. Moreover, these kinds of compounds are gaining increasing interest because of their versatile activities through chemical modi cations (di erent substituents on the aromatic ring) [4].…”

Apoptosis of Human Jurkat T Cells Induced by the Methylene Chloride Extract from the Stems of Zanthoxylum schinifolium is Associated with Intrinsic Mitochondria-Dependent Activation of Caspase Pathway

“…As a well-studied chemical component in root bark of Z. schinifolium, the coumarin is known to exert cytotoxic effect on cancer cells [7]. However, the cellular mechanism underlying this cytotoxicity still remains obscure.…”

“…Phytochemical investigations on the components of the root bark of Z. schinifolium resulted in the isolation of cis-fagaramide [5], coumarin, peroxyterpenyl coumarin [4,23,24], schinifolin, 5'-acetoxyschinifolin [6], and others [9,17]. The bioactive ingredients from Z. schinifolium have been reported for their medicinal activities including anti-platelet aggregation [6,23], anti-oxidant activity [19,20], inhibition of the production of monoamine oxidase [9], antimicrobial activity [18], and antitumor activity [7].…”