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KMID : 0811720220260020113
Korean Journal of Physiology & Pharmacology
2022 Volume.26 No. 2 p.113 ~ p.123
Diarylpropionitrile inhibits melanogenesis via protein kinase A/cAMP-response element-binding protein/microphthalmia-associated transcription factor signaling pathway in ¥á-MSH-stimulated B16F10 melanoma cells
Lee Hyun-Jeong

An Sung-Kwan
Bae Seung-Hee
Lee Jae-Ho
Abstract
Diarylpropionitrile (DPN), a selective agonist for estrogen receptor ¥â (ER¥â), has been reported to regulate various hormonal responses through activation of ER¥â in tissues including the mammary gland and brain. However, the effect of DPN on melanogenesis independent of ER¥â has not been studied. The aim of this study is to examine the possibility of anti-melanogenic effect of DPN and its underlying mechanism. Melanin contents and cellular tyrosinase activity assay indicated that DPN inhibited melanin biosynthesis in alpha-melanocyte stimulating hormone-stimulated B16F10 melanoma cell line. However, DPN had no direct influence on in vitro tyrosinase catalytic activity. On the other hand, 17¥â-estradiol had no effect on inhibition of melanogenesis, suggesting that the DPN-mediated suppression of melanin production was not related with estrogen signaling pathway. Immunoblotting analysis showed that DPN down-regulated the expression of microphthalmia-associated transcription factor (MITF), a central transcription factor of melanogenesis and its down-stream genes including tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2. Also, DPN attenuated the phosphorylation of protein kinase A (PKA) and cAMP-response element-binding protein (CREB). Additionally, DPN suppressed the melanin synthesis in UVB-irradiated HaCaT conditioned media culture system suggesting that DPN has potential as an anti-melanogenic activity in physiological conditions. Collectively, our data show that DPN inhibits melanogenesis via downregulation of PKA/CREB/MITF signaling pathway.
KEYWORD
CREB, Diarylpropionitrile, Melanogenesis, MITF, PKA
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