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J Ethnopharmacol. 2014;151(1):386-93. doi: 10.1016/j.jep.2013.10.054. Epub 2013 Nov 7.

Eupafolin, a skin whitening flavonoid isolated from Phyla nodiflora, downregulated melanogenesis: Role of MAPK and Akt pathways.

Author information

1
Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan.
2
Center for Drug Abuse and Addiction, China Medical University Hospital, Taichung, Taiwan.; China Medical University, Taichung, Taiwan.
3
Department of Pediatrics, Division of Neonatology and Pediatric Hematology/Oncology, Chang Gung Memorial Hospital, Yunlin, Taiwan.
4
Department of Nutrition and Health Sciences, Chang-Gung Institute of Technology, Taoyuan, Taiwan.; Research Center for Industry of Human Ecology, Chang Gung University of Science and Technology, Taoyuan, Taiwan.
5
Department of Respiratory Care, Chang Gung University of Science and Technology, Chia-Yi, Taiwan.
6
Department of Pharmacy, College of Pharmacy & Health Care, Tajen University, Taiwan.
7
Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan. Electronic address: flyen@kmu.edu.tw.
8
Research Center for Industry of Human Ecology, Chang Gung University of Science and Technology, Taoyuan, Taiwan; Department of Nursing, Division of Basic Medical Sciences, Chang Gung University of Science and Technology, Chia-Yi, Taiwan; Chronic Diseases and Health Promotion Research Center, Chang Gung University of Science and Technology, Chia-Yi, Taiwan. Electronic address: cwlee@gw.cgust.edu.tw.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE:

In hyperpigmentation disorders marked by melanin overproduction in the skin, including melisma and freckles, melanogenesis is caused by tyrosinase overexpression. Natural medicinal resources, like Phyla nodiflora, a traditional Chinese herbal medicine, have been used for a long time to management of dermatological conditions, such as skin inflammation and melanogenesis. Eupafolin, a functional flavonoid isolated from Phyla nodiflora, is an herbal tea constituent and possesses anti-inflammatory and anticancer activities. However, molecular mechanisms of eupafolin-mediated antimelanogenesis remain unknown. We thus focused on its antimelanogenesis effects in B16F10 mouse melanoma cells.

MATERIAL AND METHODS:

B16F10 cells were treated with eupafolin (0.01, 0.1, 1, and 10μM) in a dose-escalation-dependent manner for the determination of melanin, tyrosinase activity and melanogenesis protein levels by ELISA or western blot analysis.

RESULTS:

Eupafolin treatment significantly reduced cellular melanin content and tyrosinase activity in a dose-dependent manner (P<0.05), and no cytotoxic effects were observed. Eupafolin was associated with reduction in the levels of phospho-cAMP response element-binding protein and microphthalmia-associated transcription factor (MITF), and downregulation of tyrosinase synthesis and tyrosinase-related protein expression, leading to inhibit melanin production. In addition, eupafolin significantly induced the phosphorylation of ERK1/2 and p38 MAPK, whereas the decreased effect was observed in the phosphorylation of Akt. Moreover, inhibitors of these signals recovered or attenuated the inhibitory effects of eupafolin on melanogenesis.

CONCLUSIONS:

Our results seem that inhibition of Akt and activation of phospho-ERK or p38 MAPK may lead to the suppression of melanogenesis in eupafolin-treated B16F10 mouse melanoma cells.

KEYWORDS:

Eupafolin; Melanogenesis; Microphthalmia-associated transcription factor; Tyrosinase

PMID:
24212072
DOI:
10.1016/j.jep.2013.10.054
[Indexed for MEDLINE]

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