Kinase Assay: |
Planta Medica, 2015 ,81(16). | Evaluation of protein kinase C-activating effect of different type of Euphorbia diterpene phorbol esters in human platelets[Reference: WebLink] | Therefore, finding novel phorbol diterpene esters from natural sources seems to be an important task. Human platelets contain 5 isoforms of PKC, including α, β, δ, θ, and ζ, and activation of PKC results in platelet aggregation. Therefore, in the present study, platelets were used to evaluate PKC-activating activities of five phorbol diterpene esters, which were isolated from European Euphorbia species.
METHODS AND RESULTS:
We found that 20-Deoxyingenol 3-angelate (1) and 12-deoxy-16-hydroxyphorbol-20-acetate-6-angelate-13-isobutyrate (2) induced significant platelet aggregation accompanied by induction of phosphorylation of PKC substrates in platelets. In contrast, two jatrophanes (3, 4), and a myrsinol-type diterpene (5) neither induced platelet aggregation nor PKC activation. PKD, a substrate of PKCδ, was phosphorylated in response to 1 and 2, indicating that these two compounds are able to activate PKCδ.
CONCLUSIONS:
Our results suggest that 1 and 2 are PKC activator, but their selectivity to different isoforms of PKC remains to be determined. |
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