酪氨酸酶
化学
色素沉着
透皮
小眼畸形相关转录因子
真皮
药理学
体内
生物化学
医学
酶
生物技术
生物
病理
作者
Lan Feng,Nannan Shi,Shasha Cai,Xue Qiao,Peng Chu,Hui Wang,Feida Long,Huaixin Yang,Yongliang Yang,Yipeng Wang,Haining Yu
标识
DOI:10.1021/acs.jmedchem.8b00737
摘要
Cutaneous hyperpigmentation from excess melanogenesis causes serious pigmentary disorders and even melasma. Short peptides (SPs) are garnering attention lately owing to their therapeutic potential in dermatological diseases and low systemic side effects. Here, we show an octapeptide, ansin2, designed de novo from antioxidant SPs we previously reported, significantly inhibiting melanogenesis in B16 cells by decreasing tyrosinase production via regulating the MITF pathway. Ansin2 could also inhibit tyrosinase function by covering its catalytic pocket, which was simulated in docking and LIGPLOT studies. Topical application of ansin2 exhibited evident protection in UVB-induced pigmentation in guinea pig models both in terms of prophylaxis and treatment. Interestingly, unlike other hydrophilic and peptidic drugs that need delivery systems, ansin2 can be efficiently delivered topically to the epidermis and dermis per se without an affiliated moiety. Given that ansin2 lacks unwanted toxicities and immunogenicity, it holds great potential in treating hyperpigmentation in the cosmetics and pharmaceutical industries.
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