Effects of six compounds with different chemical structures on melanogenesis.
10.1016/S1875-5364(18)30116-X
- Author:
Rakotomalala Manda HERINIAINA
1
,
2
;
Jing DONG
3
,
4
;
Praveen Kumar KALAVAGUNTA
1
,
2
;
Hua-Li WU
1
,
2
;
Dong-Sheng YAN
3
,
4
;
Jing SHANG
1
,
5
Author Information
1. State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China
2. Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing 211198, China.
3. School of Ophthalmology and Optometry, Eye Hospital, Wenzhou Medical University, Wenzhou 325035, China
4. State Key Laboratory of Ophthalmology, Optometry and Visual Science, Wenzhou 325035, China.
5. Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing 211198, China. Electronic address: shangjing21cn@163.com.
- Publication Type:Journal Article
- Keywords:
MITF;
Melanogenesis;
Tyrosinase;
Vitiligo;
Zebrafish
- MeSH:
Alkaloids;
chemistry;
pharmacology;
Animals;
Benzodioxoles;
chemistry;
pharmacology;
Benzyl Compounds;
chemistry;
pharmacology;
Cholecalciferol;
chemistry;
pharmacology;
Flavonoids;
chemistry;
pharmacology;
Humans;
Kaempferols;
chemistry;
pharmacology;
Melanins;
genetics;
metabolism;
Monophenol Monooxygenase;
genetics;
metabolism;
Pigmentation;
drug effects;
Piperidines;
chemistry;
pharmacology;
Polyunsaturated Alkamides;
chemistry;
pharmacology;
Purines;
chemistry;
pharmacology;
Scopoletin;
chemistry;
pharmacology;
Vitiligo;
drug therapy;
enzymology;
metabolism;
Zebrafish
- From:
Chinese Journal of Natural Medicines (English Ed.)
2018;16(10):766-773
- CountryChina
- Language:English
-
Abstract:
Several chemical compounds can restore pigmentation in vitiligo through mechanisms that vary according to disease etiology. In the present study, we investigated the melanogenic activity of six structurally distinct compounds, namely, scopoletin, kaempferol, chrysin, vitamin D, piperine, and 6-benzylaminopurine. We determined their effectiveness, toxicity, and mechanism of action for stimulating pigmentation in B16F10 melanoma cells and in a zebrafish model. The melanogenic activity of 6-benzylaminopurine, the compound identified as the most potent, was further verified by measuring green fluorescent protein concentration in tyrp1 a: eGFP (tyrosinase-related protein 1) zebrafish and mitfa: eGFP (microphthalmia associated transcription factor) zebrafish and antioxidative activity. All the tested compounds were found to enhance melanogenesis responses both in vivo and in vitro at their respective optimal concentration by increasing melanin content and expression of TYR and MITF. 6-Benzyamino-purine showed the strongest re-pigmentation action at a concentration of 20 μmol·Lin vivo and 100 μmol·Lin vitro, and up-regulated the strong fluorescence expression of green fluorescent protein in tyrp1a: eGFP and mitfa: eGFP zebrafish in vitro. However, its relative anti-oxidative activity was found to be very low. Overall, our results indicated that 6-benzylaminopurine stimulated pigmentation through a direct mechanism, by increasing melanin content via positive regulation of tyrosinase activity in vitro, as well as up-regulating the expression of the green fluorescent protein in transgenic zebrafish in vivo.
