Abstract
ScopeUrsolic acid (UA) is a pentacyclicterpenoid carboxylic acid that is present in a wide variety of plant foods. There are many beneficial health effects that are attributed to the properties of UA. However, the specific cellular targets of UA and the mechanism underlying downstream signal transduction processes linked to the anti‐inflammation pathway have not been thoroughly elucidated to date.Methods and resultsChemical biology strategies such as target fishing, click reaction synthesis of a UA probe and molecular imaging were used to identify potential target proteins of UA. Cysteinyl aspartate specific proteinase 3 (CASP3) and its downstream signaling pathway were verified as potential targets by molecular docking, intracellular enzyme activity evaluation and accurate pathway analysis. The results indicated that UA acted on CASP3, ERK1 and JNK2 targets, alleviated inflammation‐associated downstream multiple signal transduction factors, including ERK1, NF‐κB and STAT3, and exhibited anti‐inflammation activities.ConclusionAs a natural dietary supplement, UA demonstrated anti‐inflammation activity via inhibition of CASP3 and shows the potential to improve the therapy effect of several inflammation‐associated diseases.
Highlights
Introduction ofUrsolic acid (UA) and its ramification as the potential therapeutics
A fluorescence signal associated with the click product was observed in the cytoplasm of BEAS-2B cells, and we demonstrated that the click product can be displaced from the cells by the addition of 10 μmol L−1 of free UA (Figure 1D)
The results indicated that Cysteinyl aspartate specific proteinase 3 (CASP3) and ERK1 were the primary target proteins of UA within the MAPK signaling pathway
Summary
Introduction ofUA and its ramification as the potential therapeutics. Zhang et al summarized the anti-tumor actions of UA,[10] includ-There is growing interest in the health benefits associated with ing anti-cell DNA damage, anti-tumor cell proliferation, antithe consumption of phytochemicals from fruits, vegetables and angiogenesis, regulation of the immunological surveillance sysherbal medicines.[1].
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