TY - JOUR
T1 - Singlet oxygen production and in vitro phototoxicity studies on fenofibrate, mycophenolate mofetil, trifusal, and their active metabolites
AU - Molins-Molina, Oscar
AU - Bresolí-Obach, Roger
AU - Garcia-Lainez, Guillermo
AU - Andreu, Inmaculada
AU - Nonell, Santi
AU - Miranda, Miguel A.
AU - Jiménez, M. Consuelo
N1 - Publisher Copyright:
Copyright © 2017 John Wiley & Sons, Ltd.
PY - 2017/9
Y1 - 2017/9
N2 - 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.
AB - 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.
KW - neutral red uptake assay
KW - photosensitization
KW - phototoxicity
KW - singlet oxygen time-resolved near-infrared phosphorescence
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U2 - 10.1002/poc.3722
DO - 10.1002/poc.3722
M3 - Article
AN - SCOPUS:85021292763
SN - 0894-3230
VL - 30
JO - Journal of Physical Organic Chemistry
JF - Journal of Physical Organic Chemistry
IS - 9
M1 - e3722
ER -