| Autor: |
Ya-Guang Hu, Zhu-Peng Gao, Ying-Ying Zheng, Chun-Mei Hu, Jing Lin, Xiao-Zheng Wu, Xin Zhang, Yong-Sheng Zhou, Zhuang Xiong, Dao-Yong Zhu |
| Rok vydání: |
2022 |
| Předmět: |
|
| Zdroj: |
Frontiers in chemistry. 10 |
| ISSN: |
2296-2646 |
| Popis: |
In order to find potential inhibitors of tyrosinase, two series of pyrrole derivatives A (1–17) and B (1–8) were synthesized and screened for their inhibitory activities on tyrosinase. Most of the 2-cyanopyrrole derivatives exhibited effective inhibitory activities. In particular, A12 exhibited the strongest inhibitory activities, with the IC50 values of 0.97 μM, which is ∼30 times stronger than the reference inhibitor kojic acid (IC50: 28.72 μM). The inhibitory mechanism analysis results revealed that A12 was a reversible and mixed-type inhibitor. Molecular docking experiments clarified the interaction between A12 with tyrosinase. Furthermore, A12 (100 μM) presented effective inhibitory effect on tyrosinase in B16 melanoma cells with inhibition of 33.48%, which was equivalent to that of Kojic acid (39.81%). Accordingly, compound A12 may serve as the lead structure for the further design of potent tyrosinase inhibitors. Molecular docking studies confirmed the interaction between the compound and tyrosinase. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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