Journal
JOURNAL OF ETHNOPHARMACOLOGY
Volume 282, Issue -, Pages -Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.jep.2021.114607
Keywords
High-resolution inhibition profiling; Paeonia lactiflora; Monophenolase; Diphenolase; Radical scavenging
Categories
Funding
- National Natural Science Foundation of China [82073979]
- Zhejiang Provincial Natural Science Foundation of China [LY20H290009]
- Hebei Province Natural Science Foundation of China [H2019204287]
- Project of Education Department of Zhejiang Province [Y201941089]
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This study focused on identifying active components from the root of Paeonia lactiflora, discovering tyrosinase inhibitors and antioxidants, and exploring their mechanisms for skin whitening, offering a new approach for developing natural whitening agents.
Ethnopharmacological relevance: The root of Paeonia lactiflora is a traditionally-used whitening medicine in China for thousands of years. Although some tyrosinase inhibitors and/or antioxidants such as 1,2,3,4,6-pentagalloyl-glucose, gallic acid, have been isolated and identified, their tyrosinase inhibition pathway (monophenolase or diphenolase inhibition, or both two) have not been systematically studied and the underlying tyrosinase inhi-bition mechanism has not been revealed yet. Moreover, the exploring of new natural tyrosinase inhibitors and antioxidants is urgently needed. Aim of the study: This review aimed to develop a new microplate-based high-resolution tyrosinase inhibition profiling assay and establish a furthermore triple high-resolution monophenolase/diphenolase/radical scav-enging profiling for accelerating identification bioactive compounds from complicated plant extract. Materials and methods: The targeted isolation and structure elucidation were performed with high-performance liquid chromatography-high-resolution mass spectrometry and preparative high-performance liquid chroma-tography. It allows to be a proof of concept with the root of Paeonia lactiflora crude extract as a natural whitening herbal drug. Results: The result showed that galloylpaeoniflorin specifically inhibited monophenolase activity. While 1,2,3,4,6-pentagalloylglucose, gallic acid and catechin demonstrated the inhibition towards both monophenolase and diphenolase. Among them, 1,2,3,4,6-pentagalloylglucose can inhibit monophenolase activity was reported for the first time. In addition, antioxidant properties were attributed to catechin, 1,2,3,4,6-pentagalloylglucose and gallic acid. Due to its low content and complicated configuration in the root of Paeonia lactiflora, a new potential tyrosinase inhibitor and radical scavenger which tentatively identified as hexagalloylglucose by high-resolution MS was still need further verification. What's more, the molecular docking unveiled that bioactive enzymatic inhibitors mainly interacted with amino acid catalytic residues of tyrosinase via H-bonds and van der wals, which may be helpful to understand their inhibition mechanisms with tyrosinase in the skin whitening. Conclusions: The platform provided a promising and efficient strategy for the rapid screening of whitening active components from natural sources.
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