Loratadine, an H1 Antihistamine, Inhibits Melanogenesis in Human Melanocytes.

Loratadine, an H1 Antihistamine, Inhibits Melanogenesis in Human Melanocytes.
Biomed Res Int. 2019;2019:5971546
Authors: Moon HR, Jo SY, Kim HT, Lee WJ, Won CH, Lee MW, Choi JH, Chang SE
Abstract
It has long been believed that histamine is associated with cutaneous melanogenesis. Specifically, H2-receptor antagonists reportedly inhibit melanogenesis, but H1-receptor antagonists, which are some of the most commonly prescribed medicines in dermatology, have not been studied to determine whether and how they regulate melanogenesis. Therefore, we screened H1-receptor antagonists to determine whether they inhibit melanogenesis and found that loratadine was particularly effective, in this regard without compromising cellular viability. Loratadine downregulated microphthalmia-associated transcription factor (MITF) and tyrosinase in melanocytes. To determine the intracellular signaling pathways, Akt was consistently activated by loratadine. PI3K/Akt pathway inhibitor, LY294002, restored the reduced melanin content that was induced by loratadine. In addition, phospho-GSK-3β also was found to be increased following loratadine treatment. Loratadine reduced the amount of PKC-βII in the membrane fraction, thereby decreasing its activity. Taken together, our data indicate that loratadine regulates melanogenesis via Akt/MITF and PKC-βII signaling, thereby leading to the inhibition of melanogenic proteins. The antimelanogenic effects of loratadin...

Source: Biomed Res - April 24, 2019 Category: Research Authors: Moon HR, Jo SY, Kim HT, Lee WJ, Won CH, Lee MW, Choi JH, Chang SE Tags: Biomed Res Int Source Type: research