Abstract
The selective activity of an antineoplastic drug is related to its ability to promote cytotoxic action on tumor cells and preserve the integrity of non-neoplastic cells. Beta-lapachone is extracted from the sawdust of Ipe wood, a thick bark tree from the Ipe wood found in the Brazilian Cerrado biome. This study aimed to evaluate the cytotoxic action of beta-lapachone in an endothelial cell line. The EA.hy926 cells were seeded in two groups, G1 and G2, cultured and exposed to beta-lapachone at concentrations of 0.0, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM for 24 hours. G1 remained under normal cultivation conditions and G2 was subjected to oxidative stress through an ischemia and reperfusion assay, in a deoxygenated sealed chamber. The cytotoxicity assay was performed using the tetrazolium reduction method. In G1, the cytotoxicity ranged from 0.0 to 10.0%; and in G2 between 0.0 and 6.3%. No statistically significant difference was observed between the obtained values. Moreover, we found no cytotoxic action of beta-lapachone on endothelial cells, and the results point out that the drug might have preserved the cell’s integrity against oxidative stress under the conditions of this experiment. This promising result suggests the possibility of beta-lapachone as a chemotherapy drug with selective activity.
Highlights
The selective activity of an antineoplastic drug is related to its capacity to promote cytotoxic action in tumor cells and to preserve the integrity of non-neoplastic cells
We aimed to evaluate the cytotoxic action of beta-lapachone in an endothelial cell line, in order to analyze the possibility of using it as a chemotherapy drug with selective activity
The cells were cultured in Dulbecco's Modified Eagle Medium (DMEM) enriched with 10% fetal bovine serum (FBS), penicillin and streptomycin (10,000 IU mL-1 - 10 mg mL-1), amphotericin B and L-glutamine, and kept in a humidified incubator at 37oC with 5% CO2 atmosphere
Summary
The selective activity of an antineoplastic drug is related to its capacity to promote cytotoxic action in tumor cells and to preserve the integrity of non-neoplastic cells. Neoplastic cells are sensitive to topoisomerase inhibitors, as they multiply quickly (Kleiner & Silva, 2003) In this context, labile cells, which maintain a constant renewal of tissues, such as the epithelium of the gastrointestinal tract, capillaries, and the immune system, are damaged during treatment with non-specific antitumor agents. Labile cells, which maintain a constant renewal of tissues, such as the epithelium of the gastrointestinal tract, capillaries, and the immune system, are damaged during treatment with non-specific antitumor agents This results in undesirable adverse effects on oncology patients, such as nausea, vomiting, diarrhea, alopecia and decreased immunity (Almeida et al, 2005). Its chemical structure was unveiled in 1896, but it only started to be prepared in 1971 It has a molecular weight of 243.3 KDa (Dalton-A unit of molecular weight) and a melting point between 158 and 159°C. It is lipophilic and water-insoluble (Pardee, Li, & Li, 2002)
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