Cardamonin suppresses melanogenesis by inhibition of Wnt/beta-catenin signaling.
Wnt/beta-catenin signaling plays important roles in many developmental processes, including neural crest-derived melanocyte development. Here we show that cardamonin, a calchone from Aplinia katsumadai Hayata, inhibited pigmentation in melanocytes through suppression of Wnt/beta-catenin signaling pathway. Cardamonin significantly suppressed the expression of microphthalmia-associated transcription factor (MITF) and tyrosinase, which are melanocyte differentiation-associated markers, in human normal melanocytes, thereby decreasing intracellular melanin production. In addition, cardamonin promoted the degradation of intracellular beta-catenin that was accumulated by Wnt3a-conditioned medium (Wnt3a CM) or bromoindirubin-3'-oxime (BIO), a glycogen synthase kinase-3beta (GSK-3beta) inhibitor, in HEK293 reporter cells and human normal melanocytes. Our findings indicate that cardamonin may be a potential whitening agent for use in cosmetics and in the medical treatment of hyperpigmentation disorders.
PharmacoGenomics Research Center, Inje University, Busan 614-735, Republic of Korea.
Munju
M
Cho
Minjung
M
Ryu
Yongsu
Y
Jeong
Young-Hwa
YH
Chung
Dong-Eun
DE
Kim
Ho-Song
HS
Cho
Sangjin
S
Kang
Jong-Sub
JS
Han
Min-Youl
MY
Chang
Cheon-Koo
CK
Lee
Muhyun
M
Jin
Ho-Jeoung
HJ
Kim
Sangtaek
S
Oh
D002460:Cell Line; D047188:Chalcones / Q000494:pharmacology*; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors; D006801:Humans; D007211:Indoles / Q000494:pharmacology; D008543:Melanins / Q000037:antagonists & inhibitors*; D008544:Melanocytes / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology; D010091:Oximes / Q000494:pharmacology; D012880:Skin Pigmentation / Q000187:drug effects*; D051153:Wnt Proteins / Q000037:antagonists & inhibitors*; D051176:beta Catenin / Q000037:antagonists & inhibitors*
D047188:Chalcones; D007211:Indoles; D008543:Melanins; D010091:Oximes; D051153:Wnt Proteins; D051176:beta Catenin; C474021:indirubin-3'-monoxime; D038362:Glycogen Synthase Kinase 3; C436747:cardamonin