Calixarbutin: A Novel Calixarene-based Potential Water-soluble Anti-tyrosinase Agent with High Anti-melanoma Activity

Document Type: Research article

Authors

1 Deputy of Food and Drug Administration, Urmia University of Medical Sciences, Urmia, Iran.

2 Health Technology Incubation Center, Urmia University of Medical Sciences, Urmia, Iran.

Abstract

Since melanocytes are the origin of melanoma and some skin disorders such as melasma, they are important cells from the perspective of medicinal chemistry. Therefore, a medication that can simultaneously overcome these diseases will be a successful potential therapeutic agent. Arbutin with phenolic structure is a powerful natural anti-tyrosinase agent. Hence, the phenolic structure of this drug, prompted us to design its novel calix [4]arene-based cluster. Therefore, the present study reports the synthesis and in-vitro bio-activities of cyclic tetramer of arbutin in comparison to its simple drug unit as the reference medication. The in-vitro biological results showed amplified anti-tyrosinase (6-fold) and anti-melanoma (27-fold) activities, in addition to more aqueous solubility (8-fold) for this cluster in relation to arbutin. Therefore, compared to arbutin, more bioactive cluster can be considered as a novel water-soluble melanogenesis inhibitor with high anti-melanoma activity.

Graphical Abstract

Calixarbutin: A Novel Calixarene-based Potential Water-soluble Anti-tyrosinase Agent with High Anti-melanoma Activity

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