Singlet oxygen production and in vitro phototoxicity studies on fenofibrate, mycophenolate mofetil, trifusal, and their active metabolites

Singlet oxygen photosensitization (studied by time‐resolved near‐infrared emission spectroscopy) and in vitro phototoxicity (by means of the 3T3 neutral red uptake assay) have been investigated for the prodrugs fenofibrate (FFB), mycophenolate mofetil (MMP), and trifusal (TFS) as well as for their a...

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Bibliographic Details
Published in:Journal of physical organic chemistry 2017-09, Vol.30 (9), p.n/a
Main Authors: Molins‐Molina, Oscar, Bresolí‐Obach, Roger, Garcia‐Lainez, Guillermo, Andreu, Inmaculada, Nonell, Santi, Miranda, Miguel A., Jiménez, M. Consuelo
Format: Article
Language:English
Subjects:
Benzoic acid
Chemical compounds
Drugs
Emission analysis
In vitro testing
Infrared spectroscopy
Irritation
Metabolites
Near infrared radiation
neutral red uptake assay
Oxygen production
photosensitization
phototoxicity
Singlet oxygen
singlet oxygen time‐resolved near‐infrared phosphorescence
Spectroscopic analysis
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Summary:Singlet oxygen photosensitization (studied by time‐resolved near‐infrared emission spectroscopy) and in vitro phototoxicity (by means of the 3T3 neutral red uptake assay) have been investigated for the prodrugs fenofibrate (FFB), mycophenolate mofetil (MMP), and trifusal (TFS) as well as for their active metabolites fenofibric acid (FFA), mycophenolic acid (MPA), and 2‐hydroxy‐4‐(trifluoromethyl)benzoic acid (HTB). The results show that FFB and its active metabolite FFA generate 1O2 with a quantum yield in the range 0.30 to 0.40 and show a photo‐irritation factor (PIF) higher than 40. By contrast, MMP/MPA and TFS/HTB are not photoactive in the used assays. These results correlate well with the previously reported in vivo phototoxicity in treated patients. Time‐resolved near‐infrared emission measurements and 3T3 neutral red uptake assays have been performed for the title compounds.
ISSN:0894-3230
1099-1395
DOI:10.1002/poc.3722