Literature DB >> 29648716

FLUPHENAZINE AND PERPHENAZINE IMPACT ON MELANOGENESIS AND ANTIOXIDANT ENZYMES ACTIVITY IN NORMAL HUMAN MELANOCYTES.

Michał Otreba, Dorota Wrześniok, Artur Beberok, Jakub Rok, Ewa Buszman.   

Abstract

Fluphenazine and perphenazine as a phenothiazine-class antipsychotic drugs are widely used to treat psychoses and schizophrenia, however their use is associated with significant side effects such as extrapyramidal symptoms as well as ocular and skin disorders. The aim of this study was to examine the effect of fluphenazine and perphenazine on cell viability, melanogenesis and antioxidant defense system in normal human melanocytes. It has been shown that both phenothiazines induce concentration-dependent loss in cell viability. The value of EC₅₀. was calculated to be 1.24 and 2.76 μM for fluphenazine and perphenazine, respectively. Fluphenazine in concentration of 1.0 μM and perphenazine in concentrations of 1.0 and 3.0 μM inhibied melanogenesis and decreased microphthalmia-associated transcription factor content. To study the effect of both analyzed drugs on antioxidant defense system in melanocytes, the level of hydrogen peroxide and the activities of antioxidant enzymes: superoxide dismutase, catalase and glutathione peroxidase were determined. Fluphenazine and perphenazine in higher analyzed concentrations caused depletion of melanocytes antioxidant status, what indicated the induction of oxidative stress. The observed changes in melanization process and antioxidant defense system in pigmented cells exposed to fluphenazine and perphenazine in vibo suggest a significant role of melanin and melanocytes in the mechanisms of undesirable side effects of these drugs in vivo, especially directed to pigmented tissues. Moreover, the presented differences in modulation of biochemical processes in melanocytes may be an explanation for various toxic activity of the analyzed phenothiazine derivatives in vivo.

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Year:  2016        PMID: 29648716

Source DB:  PubMed          Journal:  Acta Pol Pharm        ISSN: 0001-6837            Impact factor:   0.330


  3 in total

1.  Antimelanoma activity of perphenazine and prochlorperazine in human COLO829 and C32 cell lines.

Authors:  Michał Otręba; Monika Pajor; Jared D Warncke
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2019-06-06       Impact factor: 3.000

2.  In vitro melanogenesis inhibition by fluphenazine and prochlorperazine in normal human melanocytes lightly pigmented.

Authors:  Michał Otręba; Artur Beberok; Dorota Wrześniok; Ewa Buszman
Journal:  Daru       Date:  2018-07-24       Impact factor: 3.117

3.  Effect of Selected Anionic and Cationic Drugs Affecting the Central Nervous System on Electrical Properties of Phosphatidylcholine Liposomes: Experiment and Theory.

Authors:  Joanna Kotyńska; Monika Naumowicz
Journal:  Int J Mol Sci       Date:  2021-02-25       Impact factor: 5.923

  3 in total

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