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A General Method for Detecting Nitrosamide Formation in the In Vitro Metabolism of Nitrosamines by Cytochrome P450s
Published on: September 25, 2017
DNA adduct formation from tobacco-specific N-nitrosamines
1University of Minnesota Cancer Center Box 806, Mayo, 420 Delaware Street SE, Minneapolis, MN 55455, USA. hecht002@gold.tc.umn.edu
Abstract:
Tobacco-specific N-nitrosamines are a group of carcinogens derived from the tobacco alkaloids. They are likely causative factors for cancers of the lung, esophagus, pancreas, and oral cavity in people who use tobacco products. The most carcinogenic tobacco-specific nitrosamines in laboratory animals are 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL), and N'-nitrosonornicotine (NNN). DNA adduct formation from NNK and NNN has been studied extensively and is reviewed here. NNK is metabolically activated by cytochromes P450 to intermediates which methylate and pyridyloxobutylate DNA. The resulting adducts have been detected in cells and tissues susceptible to NNK carcinogenesis in rodents. The methylation and pyridyloxobutylation pathways are both important in carcinogenesis by NNK. NNK also induces single strand breaks and increases levels of 8-oxodeoxyguanosine in DNA of treated animals. NNAL, which like NNK is a potent pulmonary carcinogen, is also metabolically activated to methylating and pyridyloxobutylating intermediates. NNN pyridyloxobutylates DNA in its rat target tissues, esophagus and nasal mucosa. Methyl and pyridyloxobutyl DNA adducts are detected in human tissues. The methyl adducts most likely result in part from exposure of smokers to NNK, but these adducts are also detected in non-smokers. Some of the methyl adducts detected in non-smokers may be due to environmental tobacco smoke exposure. There are also potential dietary and endogenous sources of these adducts. Pyridyloxobutyl DNA adducts in human tissues result mainly from exposure to tobacco-specific N-nitrosamines. In laboratory animals, DNA adduct formation and carcinogenicity of tobacco-specific N-nitrosamines are closely correlated in many instances, and it is likely that similar relationships will hold in humans.
Insights
Tobacco-specific nitrosamines cause cancer by damaging DNA. These carcinogens form DNA adducts, which are linked to various cancers in tobacco users and potentially non-users.
Area of Science:
- Toxicology
- Carcinogenesis
- Molecular Biology
Background:
- Tobacco-specific nitrosamines are potent carcinogens found in tobacco products.
- These compounds are implicated in cancers of the lung, esophagus, pancreas, and oral cavity.
- Key carcinogens include 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL), and N'-nitrosonornicotine (NNN).
Purpose of the Study:
- To review the mechanisms of DNA adduct formation by NNK and NNN.
- To discuss the significance of these adducts in the context of tobacco-related carcinogenesis.
- To explore the presence and potential sources of these DNA adducts in human tissues.
Main Methods:
- Review of existing literature on NNK and NNN metabolism and DNA adduct formation.
- Analysis of studies investigating DNA adducts in animal models and human tissues.
- Correlation of DNA adduct levels with carcinogenicity data.
Main Results:
- NNK is metabolically activated to form methylating and pyridyloxobutylating intermediates that damage DNA.
- NNAL, a pulmonary carcinogen, also generates methylating and pyridyloxobutylating DNA adducts.
- NNN primarily pyridyloxobutylates DNA in target tissues like the esophagus and nasal mucosa.
- Both methyl and pyridyloxobutyl DNA adducts are found in human tissues, with pyridyloxobutyl adducts strongly linked to tobacco use.
Conclusions:
- DNA adduct formation is a key mechanism in the carcinogenicity of tobacco-specific nitrosamines.
- Methyl DNA adducts in humans may arise from NNK exposure, environmental tobacco smoke, or other sources.
- Pyridyloxobutyl DNA adducts in humans are predominantly from tobacco-specific nitrosamine exposure.
- A strong correlation exists between DNA adduct formation and carcinogenicity in animal models, suggesting similar mechanisms in humans.
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