Amine derivatives of furocoumarin induce melanogenesis by activating Akt/GSK-3 beta/beta-catenin signal pathway
文献类型:期刊论文
作者 | Zang, D (Zang, Deng)[ 1,2 ]; Niu, C (Niu, Chao)[ 1 ]; Aisa, HA (Aisa, Haji Akber)[ 1 ]![]() |
刊名 | DRUG DESIGN DEVELOPMENT AND THERAPY
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出版日期 | 2019 |
卷号 | 13期号:2页码:623-632 |
关键词 | amine derivatives of furocoumarin melanogenesis Akt/GSK-3 beta/beta-catenin |
ISSN号 | 1177-8881 |
DOI | 10.2147/DDDT.S180960 |
英文摘要 | Background: Melanogenesis, or the biosynthesis of melanin, plays a critical role in the pigmentation of skin, hair, and eyes. Reduced melanogenesis may lead to depigmentation conditions such as vitiligo. Psoralen, a furocoumarin derivative, is closely associated with melanogenesis, and its derivative 8-methoxypsoralen is used in psoralen and ultraviolet A therapy for pigmentation disorders. In a previous study, we synthesized a new series of amine derivatives of furocoumarin, of which 5-(morpholinomethyl)-3-phenyl-7H-furo[3,2-g]chromen-7-one (encoded as D206008) showed a remarkable melanogenic effect in B16 murine cells. Methods: In this study, we examined the effects of D206008 on the melanogenesis-related pathways in B16 cells. D206008 increased melanin production and tyrosinase (TYR) activity, as well as the mRNA and protein expression levels of the melanogenic enzymes TYR, TRP-1 and TRP-2, and the melanogenesis-related transcription factor microphthalmia-associated transcription factor (MITF) in a dose-dependent (0-100 mu M) and time-dependent (0-48 hours) manner. Results: Mechanistically, D206008 inhibited beta-catenin degradation by enhancing the phosphorylation of Akt and glycogen synthase kinase-3 beta (GSK-3 beta), which increased the accumulation of beta-catenin in the cytoplasm. Nuclear translocation of beta-catenin also increased in response to D206008 treatment. Conclusion: Taken together, these data indicate that D206008 promotes melanin synthesis by stimulating the nuclear translocation of beta-catenin, which activates MITF transcription and eventually melanogenesis. |
WOS记录号 | WOS:000458896000002 |
源URL | [http://ir.xjipc.cas.cn/handle/365002/5679] ![]() |
专题 | 新疆理化技术研究所_省部共建新疆特有药用资源利用重点实验室 新疆理化技术研究所_资源化学研究室 |
通讯作者 | Aisa, HA (Aisa, Haji Akber)[ 1 ] |
作者单位 | 1.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Key Lab Plant Resources & Chem Arid Reg, Urumqi 830011, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
推荐引用方式 GB/T 7714 | Zang, D ,Niu, C ,Aisa, HA . Amine derivatives of furocoumarin induce melanogenesis by activating Akt/GSK-3 beta/beta-catenin signal pathway[J]. DRUG DESIGN DEVELOPMENT AND THERAPY,2019,13(2):623-632. |
APA | Zang, D ,Niu, C ,&Aisa, HA .(2019).Amine derivatives of furocoumarin induce melanogenesis by activating Akt/GSK-3 beta/beta-catenin signal pathway.DRUG DESIGN DEVELOPMENT AND THERAPY,13(2),623-632. |
MLA | Zang, D ,et al."Amine derivatives of furocoumarin induce melanogenesis by activating Akt/GSK-3 beta/beta-catenin signal pathway".DRUG DESIGN DEVELOPMENT AND THERAPY 13.2(2019):623-632. |
入库方式: OAI收割
来源:新疆理化技术研究所
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