N-pentyl-nitrofurantoin induces apoptosis in HL-60 leukemia cell line by upregulating BAX and downregulating BCL-xL gene expression

Abstract

The results indicate that NFP induces apoptosis in HL-60 cells by upregulating BAX and downregulating BCL-xL.

Inclusion of Nitrofurantoin into the Realm of Cancer Chemotherapy via Biology-Oriented Synthesis and Drug Repurposing

“…24 First of which, nifuroxazide demonstrated STAT3 inhibitory and antiproliferative activities against melanoma cell lines. 25 Along the same track and as a typical illustration for the application of derivatized repurposed drugs in oncology, N-pentyl nitrofurantoin was found to induce apoptosis in the HL-60 leukemia cell line via upregulating Bax and downregulating Bcl-xL expression 14 (Figure 1).…”

“…Of particular interest to this study, nitrofurantoin is a pharmacophore-rich molecule that has pro-oxidant properties and is engaged in the mitochondrial reactive oxygen species (ROS) pathway, resulting in oxidative stress, which accounts for its anticancer activity. 3,14 Intriguingly, chemical derivatization of nitrofurantoin gave rise to beneficial anticancer lead compounds, acting by induction of apoptosis. Within the context of apoptosis in cancer cells, p53, also known as "the guardian of the human genome", controls the expression of downstream genes that are known to be implicated in tumor formation, and hence it is not surprising that over 50% of human malignancies possess p53 mutations.…”

“…Of particular interest to this study, nitrofurantoin is a pharmacophore-rich molecule that has pro-oxidant properties and is engaged in the mitochondrial reactive oxygen species (ROS) pathway, resulting in oxidative stress, which accounts for its anticancer activity. , Intriguingly, chemical derivatization of nitrofurantoin gave rise to beneficial anticancer lead compounds, acting by induction of apoptosis …”

Atorvastatin and Nitrofurantoin Repurposed in the Context of Breast Cancer and Neuroblastoma Cells

“…The nitro group gives this molecule a toxicophore function, which acts as an electron acceptor, thereby inhibiting enzymes involved in pyruvate metabolism, an essential pathway of cellular metabolism. Nitrofurantoin has also been shown to be cytotoxic against cancer cells, inhibiting proliferation of human leukemia, colon, cervix, and prostate cancer cell lines [ 11 ].…”

“…These radicals can interact with DNA, resulting in inhibition of nucleic acid synthesis and breaks of single- and double-stranded DNA. Nitrofurantoin has been shown to be cytotoxic against cancer cells, inhibiting proliferation of human leukemia, colon, cervical, and prostate cancer cell lines [ 11 ].…”