De Novo Molecular Design of a Novel Octapeptide That Inhibits In Vivo Melanogenesis and Has Great Transdermal Ability
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2018 |
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| Erschienen: |
2018 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:61 |
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| Enthalten in: |
Journal of medicinal chemistry - 61(2018), 15 vom: 09. Aug., Seite 6846-6857 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Feng, Lan [VerfasserIn] |
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| Links: |
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| Themen: |
EC 1.14.18.1 |
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| Anmerkungen: |
Date Completed 18.06.2019 Date Revised 18.06.2019 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1021/acs.jmedchem.8b00737 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM28652094X |
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| 245 | 1 | 3 | |a De Novo Molecular Design of a Novel Octapeptide That Inhibits In Vivo Melanogenesis and Has Great Transdermal Ability |
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| 500 | |a Date Completed 18.06.2019 | ||
| 500 | |a Date Revised 18.06.2019 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 7 | |a Melanins |2 NLM | |
| 650 | 7 | |a Oligopeptides |2 NLM | |
| 650 | 7 | |a Monophenol Monooxygenase |2 NLM | |
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| 700 | 1 | |a Shi, Nannan |e verfasserin |4 aut | |
| 700 | 1 | |a Cai, Shasha |e verfasserin |4 aut | |
| 700 | 1 | |a Qiao, Xue |e verfasserin |4 aut | |
| 700 | 1 | |a Chu, Peng |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Hui |e verfasserin |4 aut | |
| 700 | 1 | |a Long, Feida |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, Huaixin |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, Yongliang |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Yipeng |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Haining |e verfasserin |4 aut | |
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