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Bioorg Med Chem Lett ; 27(2): 156-161, 2017 01 15.
Artículo en Inglés | MEDLINE | ID: mdl-27956348

RESUMEN

Sixteen porphyrins, including neutral, anionic and cationic meso-(aryl)porphyrins and meso-(1-methyl-4-pyridinium)porphyrins were herein evaluated in terms of their photosensitizing properties against HaCaT keratinocytes. After an initial screening, the cationic porphyrins were studied in more details, by both determining their log POW and performing PDT assays in lower porphyrin concentrations. Porphyrins presenting two or more adjacent positively charged groups, directly linked to the macrocycle meso positions, appeared to be the most effective photosensitizers. The present study also included the dicationic 5,10-diphenyl-15,20-di(1-methylpyridinium-4-yl)porphyrin (14b), which has previously shown promising results on a psoriasis-like in vivo model. Overall results indicated that the beneficial effect related to porphyrins on psoriasis can be related to the decreasing of keratinocyte viability. Furthermore, some of the cationic porphyrins studied appeared as candidates to be utilized as photosensitizers for psoriasis treatment.


Asunto(s)
Queratinocitos/efectos de los fármacos , Fármacos Fotosensibilizantes/farmacología , Porfirinas/farmacología , Compuestos de Piridinio/farmacología , Línea Celular , Humanos , Queratinocitos/citología , Luz , Fármacos Fotosensibilizantes/síntesis química , Porfirinas/síntesis química , Psoriasis/tratamiento farmacológico , Compuestos de Piridinio/síntesis química
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