genotoxic

1,3-Dithiane (1,3-Dithian) is a protected formaldehyde anion equivalent that could serve as a useful labeled synthon. 1,3-Dithiane is also a sulfur-containing Maillard reaction products found in boiled beef extracts.

4-Hydroxynonenal (4-HNE) (4-HNE) is an oxidative/nitrosative stress biomarker. It is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2).

Lucidin primeveroside (Lucidin 3-O-primeveroside) is a natural product isolated from the root powder of akane (Rubia akane) and can be used as a coloring agent and a food pigment. Lucidin primeveroside can be metabolically converted to genotoxic compound Lucidin in mice.

4'-Methylacetophenone can be used as a fragrance material. It is wildly occurred in volatile compounds in food and in some natural complex substances.

Levofloxacin N-oxide is an inactive metabolite of the antibiotic levofloxacin . Levofloxacin N-oxide is also a degradation product of levofloxacin that is formed through exposure to daylight or hydrogen peroxide.

1. Skimmianine (Chloroxylonine) is a spasmolytic agent. 2. Skimmianine (Chloroxylonine) shows pharmacol. props. similar to 2-(Methylamino)-1-phenyl-1-propanol BCJ45-G.

Azobenzene is a phototrigger that can be used to design and synthesize a variety of photoresponsive systems.Azobenzene is genotoxic and induces aggressive sarcomas of the spleen and other abdominal organs.

Diaveridine (AI3-23935) (DVD) is a popular antibacterial synergist that is widely used in combination with sulfonamide. It has been reported to be genotoxic to mammalian cells, but more studies are required to clarify this.

1-Hydroxyanthraquinone is an anthraquinone that has been found in Morinda officinalis and has genotoxic and carcinogenic activities. 1-Hydroxyanthraquinone generates strong DNA repair response.

N-Acetylglycine is a minor constituent of food that is not genotoxic or acutely toxic and is capable of being used in biological studies of mimetic peptides.N-Acetylglycine acts as a blocker of the N-terminus of a peptide.3-Hydroxyanthranilic acid is a competitive succinate dehydrogenase inhibitor.

Sunset Yellow FCF (Sunset yellow) is an orange azo dye with pH-dependent absorbance.Sunset Yellow FCF is used in food, cosmetics and pharmaceuticals.It is used as a colorant food additive in many food products.They may be cytotoxic and genotoxic, so care must be taken when using these materials as food additives.

Inauhzin (INZ)(INZ) is a novel small molecule that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human Y cells without causing apparently genotoxic stress(IC50=3 uM, in A549 cell).

Perfluoroundecanoic acid is an orally effective inducer of oxidative stress and DNA damage. It exhibits genotoxic and reproductive toxicity in Swiss mice. Due to its thermal stability and pressure resistance, as well as featuring both hydrophobic and hydrophilic groups on the same molecule, Perfluoroundecanoic acid is utilized as a processing aid in the manufacture of fluoropolymers.

1-Nitropyrene (3-Nitropyrene) is one of the important components of atmospheric pollutants such as tobacco smoke. It is carcinogenic and genotoxic, and can damage mitochondrial function and intracellular redox balance.

Dapagliflozin impurity A (Compound A) is a peroxidized form of dapagliflozin known to be a genotoxic impurity. Even at low concentrations, it can damage human genetic material, potentially causing gene mutations and potentially promoting tumor development.

2,5-Dimethyl-3(2H)-furanone (2,5-Dimethyl-2,3-dihydrofuran-3-one) is a non-genotoxic flavoring substance [1].

Illudin S (ILS) is a fungal sesquiterpene secondary metabolite with potent genotoxic and cytotoxic properties.

MSN-50, an inhibitor of Bax and Bak oligomerization, inhibits liposome permeabilization, prevents genotoxic cell death and promotes neuroprotection.

Nafenopin is a peroxisome proliferator with hepatotumor-promoting activity and can also be used as an anti-hyperlipoproteinemia agent. Nafenopin induces oxidative stress in vivo and exerts hepatic effects, with a mechanism of action significantly different from other non-genotoxic carcinogens.

Jatropham is a natural compound isolated from lily of the valley. It has been shown to have the potential to modulate and reduce the cytotoxic and genotoxic/labile effects of zeocin.

Cylindrospermopsin, a tricyclic uracil derivative, is a cyanobacterial toxin that was first discovered in an algal bloom contaminating a local drinking supply on Palm Island in Queensland, Australia after an outbreak of a mysterious disease. Cylindrospermopsin targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 µM, respectively), leading to cell death. [1] It has been shown to inhibit the activity of the uridine monophosphate synthase complex with a Ki value of 10 µM.[2] Cylindrospermopsin is genotoxic, inducing DNA damage as evidenced by double strand breaks and reducing cell viability in HepG2 cells at 0.1-0.5 µg/ml.[3]

5-Chlorouracil is a chlorinated derivative of the pyrimidine nucleoside base uracil . In vivo, it is converted into chlorodeoxyuridine, which is mutagenic and genotoxic.1 Uracil is chlorinated at the 5 position in a cell-free myeloperoxidase, peroxide, and chloride system in which hypochlorous acid is formed.2 5-Chlorouracil has been found in human neutrophils stimulated with phorbol 12-myristate 13-acetate in vitro and in inflammatory human exudate isolated from sites of superficial infection. Levels of 5-chlorouracil are increased in exudate isolated from the site of inflammation in a rat model of carrageenan-induced inflammation and in patient-derived human atherosclerotic aortic tissue.3,4References 5-Chlorouracil is a chlorinated derivative of the pyrimidine nucleoside base uracil . In vivo, it is converted into chlorodeoxyuridine, which is mutagenic and genotoxic.1 Uracil is chlorinated at the 5 position in a cell-free myeloperoxidase, peroxide, and chloride system in which hypochlorous acid is formed.2 5-Chlorouracil has been found in human neutrophils stimulated with phorbol 12-myristate 13-acetate in vitro and in inflammatory human exudate isolated from sites of superficial infection. Levels of 5-chlorouracil are increased in exudate isolated from the site of inflammation in a rat model of carrageenan-induced inflammation and in patient-derived human atherosclerotic aortic tissue.3,4 References

Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol/kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg/fly.4 1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)

N-Nitroso fluoxetine is a derivative of fluoxetine.1It is genotoxic toS. typhimuriumwhen used at concentrations ranging from 0.06 to 0.12 mg/ml.