Nitrogen Mustard Disrupts Bioenergetics and Activates Oxidative Stress-Induced Cell Death Pathways in Human Keratinocytes

Nitrogen mustard (HN2) is a highly reactive bifunctional alkylating agent that causes severe skin injury. To define its impact on keratinocyte bioenergetics and stress responses, we examined mitochondrial function, metabolism, and cell death signaling in human HaCaT cells. Seahorse analysis showed that HN2 caused time- and concentration-dependent suppression of oxidative phosphorylation, including reductions in basal, adenosine 5′-triphosphate-linked, and maximal oxygen consumption. Glycolytic activity was similarly impaired, with decreased extracellular acidification, reduced glucose-stimulated glycolysis, and loss of glycolytic capacity and reserve, indicating broad metabolic dysfunction. HN2-induced bioenergetic impairment triggered rapid nuclear accumulation of nuclear factor erythroid 2-related factor 2 (Nrf2) and upregulation of antioxidant and mitochondrial regulatory genes (HO-1, NQO1, GSTA4, and PGC1α). In parallel, HN2 activated multiple programmed cell death pathways, including apoptosis, autophagy, and ferroptosis, as evidenced by corresponding alterations in Bax, Bcl-xL, LC3-II, SQSTM1/p62, caspase-2, caspase-9, GPx4, TFRC, and ACSL4. Cell cycle analysis identified cells in G2/M as particularly susceptible to HN2, which exhibited enhanced apoptotic signaling. N-acetylcysteine attenuated Nrf2 activation, preserved mitochondrial and glycolytic function, and reduced activation of cell death pathways, demonstrating a central role for oxidative and electrophilic stress in HN2 toxicity. These findings reveal a novel mechanism by which HN2 disrupts keratinocyte bioenergetics to drive stress-dependent cell death and highlight antioxidant intervention as a potential strategy to mitigate HN2-induced skin injury.

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Publication Details

Journal
Chemical Research in Toxicology
Published
2026-05-28
DOI
https://doi.org/10.1021/acs.chemrestox.6c00099
Primary Topic
Pesticide Exposure and Toxicity
Type
article
Field-Weighted Citation Impact
0.00

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article

Nitrogen Mustard Disrupts Bioenergetics and Activates Oxidative Stress-Induced Cell Death Pathways in Human Keratinocytes

Debra L. Laskin, Jeffrey D. Laskin, Laurie B. Joseph, Bożena Michniak-Kohn et al.
Chemical Research in Toxicology
Pesticide Exposure and Toxicity
article

Nitrogen Mustard Disrupts Bioenergetics and Activates Oxidative Stress-Induced Cell Death Pathways in Human Keratinocytes

Debra L. Laskin, Jeffrey D. Laskin, Laurie B. Joseph, Bożena Michniak-Kohn, Yi-Hua Jan
article en

Abstract

Nitrogen mustard (HN2) is a highly reactive bifunctional alkylating agent that causes severe skin injury. To define its impact on keratinocyte bioenergetics and stress responses, we examined mitochondrial function, metabolism, and cell death signaling in human HaCaT cells. Seahorse analysis showed that HN2 caused time- and concentration-dependent suppression of oxidative phosphorylation, including reductions in basal, adenosine 5′-triphosphate-linked, and maximal oxygen consumption. Glycolytic activity was similarly impaired, with decreased extracellular acidification, reduced glucose-stimulated glycolysis, and loss of glycolytic capacity and reserve, indicating broad metabolic dysfunction. HN2-induced bioenergetic impairment triggered rapid nuclear accumulation of nuclear factor erythroid 2-related factor 2 (Nrf2) and upregulation of antioxidant and mitochondrial regulatory genes (HO-1, NQO1, GSTA4, and PGC1α). In parallel, HN2 activated multiple programmed cell death pathways, including apoptosis, autophagy, and ferroptosis, as evidenced by corresponding alterations in Bax, Bcl-xL, LC3-II, SQSTM1/p62, caspase-2, caspase-9, GPx4, TFRC, and ACSL4. Cell cycle analysis identified cells in G2/M as particularly susceptible to HN2, which exhibited enhanced apoptotic signaling. N-acetylcysteine attenuated Nrf2 activation, preserved mitochondrial and glycolytic function, and reduced activation of cell death pathways, demonstrating a central role for oxidative and electrophilic stress in HN2 toxicity. These findings reveal a novel mechanism by which HN2 disrupts keratinocyte bioenergetics to drive stress-dependent cell death and highlight antioxidant intervention as a potential strategy to mitigate HN2-induced skin injury.

Chemical Research in Toxicology
Rutgers Sexual and Reproductive Health and Rights (NL), Center for Health Justice (US)
National Institutes of Health, National Institute of Environmental Health Sciences, National Institute of Arthritis and Musculoskeletal and Skin Diseases
Life below water
Openalex Percentile: Top 7%
Pesticide Exposure and Toxicity
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