Hair Dyes Resorcinol and Lawsone Reduce Production of Melanin in Melanoma Cells by Tyrosinase Activity Inhibition and Decreasing Tyrosinase and Microphthalmia-Associated Transcription Factor (MITF) Expression

Lee, Shu-Mei; Chen, Yi-Shyan; Lin, Chih-Chien; Chen, Kuan‐Hung

doi:10.3390/ijms16011495

Cited by 18 publications

(9 citation statements)

References 31 publications

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“…Thus, a modulation of tyrosinase may restore cancer cell sensitivity to chemotherapy by the depletion of pigment amount and increasing the concentration of unbound drug (Buitrago et al 2016). An important point is the fact that TYR expression is observed in nevi and in 80-90% of primary and metastatic melanomas, which makes it a useful diagnostic marker (Pitcovski et al 2017) as well as that decrease of tyrosinase amount is frequently observed and correlates with the MITF level (Hashemi-Shahri et al 2018, Lee et al 2015. In the present study, we observed a significant decrease of tyrosinase in C32 cells after prochlorperazine treatment only in concentration of 3 μM.…”

Section: Discussionsupporting

confidence: 53%

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

Otręba

Pajor

Warncke

2019

Naunyn-Schmiedeberg's Arch Pharmacol

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Cutaneous melanoma is least common (only about 1% of skin cancers) but is the deadliest malignant tumor. Moreover, amelanotic types of melanoma are very difficult for clinical diagnosis. The standard therapy can cause a lot of side effects, e.g., nausea, vomiting, and headaches, which means that novel and effective strategies are required. Interestingly, phenothiazine derivatives possess sedative, antiemetic, and anticancer activity. Our goal was to determine the effect of perphenazine and prochlorperazine on cell viability, motility, microphthalmia-associated transcription factor (MITF) and tyrosinase content in melanotic and amelanotic melanoma cells. The viability of C32 and COLO829 melanoma cells was evaluated by the WST-1 colorimetric assay; impact on motility of human melanoma was performed by wound-healing assay, while tyrosinase and MITF content were determined by Western blot. In the present study, we explore the anticancer effect of perphenazine and prochlorperazine in human melanotic (COLO829) and amelanotic (C32) melanoma cells concluding that prochlorperazine inhibits cell viability in a concentration-dependent manner, impairs motility, and decreases tyrosinase and MITF amounts. Moreover, the analyzed drugs decrease/increase MITF amount depending on the type of melanoma. We demonstrated that the decrease of MITF and tyrosinase protein induces motility inhibition of C32 cells, which suggests the ability of those drugs to restore cancer cell sensitivity to treatment. The ability of prochlorperazine to contain the spread of the amelanotic melanoma in vivo may be helpful in the development of a new and effective antimelanoma therapies.

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Section: Discussionsupporting

confidence: 53%

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

Otręba

Pajor

Warncke

2019

Naunyn-Schmiedeberg's Arch Pharmacol

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“…Resorcinol has been found to have various beneficial properties [12,13,18]. In addition, a recent study reported that resorcinol inhibits melanin biosynthesis [19,20]. However, the detailed mechanisms by which this occurs remain to be elucidated.…”

Section: Discussionmentioning

confidence: 99%

Anti-melanogenic effects of resorcinol are mediated by suppression of cAMP signaling and activation of p38 MAPK signaling

Kang

Park

et al. 2018

Bioscience, Biotechnology, and Biochemistry

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In this study, we investigated the inhibitory mechanisms of resorcinol in B16F10 mouse melanoma cells. We found that resorcinol reduced both the melanin content and tyrosinase activity in these cells. In addition, resorcinol suppressed the expression of melanogenic gene microphthalmia-associated transcriptional factor (MITF) and its downstream target genes tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2. In addition, we found that resorcinol reduced intracellular cAMP levels and protein kinase A (PKA) activity, and increased phosphorylation of the p38 mitogen-activated protein kinase (MAPK). Resorcinol was also found to directly inhibit tyrosinase activity. However, resorcinol-induced decrease in melanin content, tyrosinase activity, and tyrosinase protein levels were attenuated by SB203580, a p38 MAPK inhibitor. Taken together, these data indicate that anti-melanogenic activity of resorcinol is be mediated through the inhibition of cAMP signaling and activation of p38 MAPK, indicating that resorcinol may be a possible ameliorating agent in the treatment of hyperpigmentation skin disorders.

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“…[76]. The ability of compound 46 to inhibit tyrosinase was credited to its ability to reduce microphthalmia-associated transcription factor (MITF) [77] and tyrosinase mRNA expression as high as 73% and 82%, respectively. The results showed that compound 46 has the potential to be used together with other bioactive ingredients for protection against hyperpigmentation [76].…”

Section: Cinnamic Acid Derivatives With Antioxidant and Anti-inflammamentioning

confidence: 99%

Cinnamic Acid Derivatives and Their Biological Efficacy

Ruwizhi

Aderibigbe

2020

IJMS

249

134

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The role played by cinnamic acid derivatives in treating cancer, bacterial infections, diabetes and neurological disorders, among many, has been reported. Cinnamic acid is obtained from cinnamon bark. Its structure is composed of a benzene ring, an alkene double bond and an acrylic acid functional group making it possible to modify the aforementioned functionalities with a variety of compounds resulting in bioactive agents with enhanced efficacy. The nature of the substituents incorporated into cinnamic acid has been found to play a huge role in either enhancing or decreasing the biological efficacy of the synthesized cinnamic acid derivatives. Some of the derivatives have been reported to be more effective when compared to the standard drugs used to treat chronic or infectious diseases in vitro, thus making them very promising therapeutic agents. Compound 20 displayed potent anti-TB activity, compound 27 exhibited significant antibacterial activity on S. aureus strain of bacteria and compounds with potent antimalarial activity are 35a, 35g, 35i, 36i, and 36b. Furthermore, compounds 43d, 44o, 55g–55p, 59e, 59g displayed potent anticancer activity and compounds 86f–h were active against both hAChE and hBuChE. This review will expound on the recent advances on cinnamic acid derivatives and their biological efficacy.

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Hair Dyes Resorcinol and Lawsone Reduce Production of Melanin in Melanoma Cells by Tyrosinase Activity Inhibition and Decreasing Tyrosinase and Microphthalmia-Associated Transcription Factor (MITF) Expression

Cited by 18 publications

References 31 publications

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

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

Anti-melanogenic effects of resorcinol are mediated by suppression of cAMP signaling and activation of p38 MAPK signaling

Cinnamic Acid Derivatives and Their Biological Efficacy

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