AI Article Synopsis
- Two series of pyrrole derivatives were synthesized and tested for their ability to inhibit the enzyme tyrosinase, which is important in melanin production.
- Among the compounds, A12 showed the strongest inhibitory effect, being approximately 30 times more effective than the standard inhibitor, kojic acid.
- The study found that A12 acts as a reversible and mixed-type inhibitor and effectively reduced tyrosinase activity in B16 melanoma cells, suggesting potential for further development as a lead compound for new inhibitors.
Article Abstract
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 IC values of 0.97 μM, which is ∼30 times stronger than the reference inhibitor kojic acid (IC: 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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9247258 | PMC |
| http://dx.doi.org/10.3389/fchem.2022.914944 | DOI Listing |
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