Open Access Peer-reviewed

Coumarin, a Lead Compound of Warfarin, Inhibits Melanogenesis via Blocking Adenylyl Cyclase

Dong-Chan Kim1,, Seong-Hwan Rho2, Dongjin Kim3, Sung In Kim1, Chul-Soo Jang1, Jae Ki Ryu1, Byung Weon Kim1, Chang Oh Kweon1, Hyun-kyung Kim1, Suk Jun Lee1

1Department of Biomedical Laboratory Science, Gimcheon University, Gimcheon City, South Korea

2Institute for Physics, University of Freiburg, Freiburg, Germany

3School of Civil and Environmental Engineering, Georgia Institute of Technology, Atlanta, U.S.A

American Journal of Biomedical Research. 2013, 1(3), 43-47. DOI: 10.12691/ajbr-1-3-1
Published online: August 25, 2017


Due to Its multiple biological activities, coumarin (a main ingredient of Cinnamon extracts) has gained attention as potentially useful therapeutics for various diseases. However, the efficacy of coumarin for the use of dermatological health has not been fully explored. To clarify the action mechanism of the skin protecting property of coumarin, we firstly investigated the molecular docking property of coumarin on the mammalian adenylyl cyclase, which is the key enzyme of cAMP-induced melanogenesis in the skin cells. In binding study, the benzopyran moiety of coumarin occupies dual sites of the hydrophobic cleft at the interface of two subunits of adenylyl cyclase. We also examined the involvement of coumarin in alpha-MSH and forskolin induced cAMP signaling within a cell based assay. In addition, we inquired into the inhibitory effect of coumarin on melanogenesis and found that the pretreatment with coumarin inhibited the forskolin-induced melanin contents significantly without annihilating the cell viability. Our results strongly suggest that coumarin directly inhibits the activity of adenylyl cyclase, downregulates forskolin-induced cAMP-production pathway, consequently inhibiting melanogenesis. Thus, coumarin may also be used as an effective inhibitor of hyperpigmentation.


coumarin, melanin production inhibitor, cyclic AMP
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