Phorbol ester-induced activation inhibition

Kundu JK, Surh YJ. 2007. Epigallocatechin gallate inhibits phorbol ester-induced activation of NF-kappa B and CREB in mouse skin Role of p38 MAP K. Ann N Y Acad Sci 1095 504-512. 

Luyengi, L. et al., Rotenoids and chalcones from Mundulea sericea that inhibit phorbol ester-induced ornithine decarboxylase activity. Phytochemistry, 36, 1523, 1994. 

Xu, . X., Jin, H, Chung, Y. S., Shin, J. Y., Lee, . H., Beck, G. R., Palmos, G. N., Choi, B. D., and Cho, M. H. (2008a). Chondroitin sulfate extracted from ascidian tunic inhibits phorbol ester-induced expression of inflammatory factors VCAM-1 and COX-2 by blocking NF- activation in mouse skin. J. Agric. Food Chem. 56, 9667-9675. 

Kundu JK, Shin YK, Kim SH, Surh Y-J. 2006a. Resveratrol inhibits phorbol ester-induced expression of COX-2 and activation of NF-kB in mouse skin by blocking I B kinase activity. Carcinogenesis 27 1465-1474... 

Gupta, A.K., Fisher, G.J., Elder, J.T., Nickoloff, B.J., and Voorhees, J.J., Sphingosine inhibits phorbol ester-induced inflammation, ornithine decarboxylase activity, and activation of protein kinase C in mouse skin, J. Invest. Dermatol., 91, 486-491, 1988. 

Cytotoxicity (MCF-7 and Hepa lclc7 cells) of the stilbenes in cube resin from Lonchocarpus utilus and L. urucu roots paralleled their inhibition of NADHmbiquinone oxidoreductase activity and phorbol ester-induced ornithine decarboxylase activity [50,467]. 

Chun, K.S. et al., Curcumin inhibits phorbol ester-induced expression of cyclooxygenase-2 in mouse skin through suppression of extracellular signal-regulated kinase activity and NF-kappaB activation. Carcinogenesis, 24 (9), 1515, 2003. 

Effect of panaxadiol saponin (PDS) on phorbol ester induced change of protein kinase C activity in cardiomyocytes of rats was investigated[19]. Partially purified protein kinase C was incubated with PDS at concentration of 1 to 1000 U g/ml for ten minutes in vitro. The activity of kinase C was inhibited in a dose-dependent manner by PDS. In cardiomyocytes preincubated with PDS at concentration of250, 500,1000 P g/ml, respectively, for ten minutes, PMA-induced decrease of cytosol protein kinase C activity and increase of membrane protein kinase C activity were greatly inhibited in the same manner. PDS not only inhibited protein kinase C in vitro, but also inhibited activation of protein kinase C in cardiomyocytes. 

Phorbol ester-induced ornithine decarboxylase (EC 4.1.1.17) activity associated with tumour promotion (O Brien 1976) was inhibited by deguelin, tephrosin, (-)-13a-hydroxytephrosin, and (-)-13a-hydroxydeguelin, four rotenoids obtained from the African legume Mundulea sericea (Gerhauser et al. 1995). 17 nmole of retinoic add, when applied 1 h before treatment of mouse skin with 5 nmole of... 

Lee, K.W., Kim, J.H., Lee, H.J., Surh, Y.J. 2005. Curcumin inhibits phorbol ester induced up-regulation of cyclooxygenase-2 and matrix metalloproteinase-9 by blocking ERKl/2 phosphorylation and NF-kB transcriptional activity in MCFIOA human breast epithelial cells. Antioxidants and redox signaling., 7 1612-1620. 

In previous studies it has been demonstrated that not only protein kinase C (PKC) activators including phorbol esters (TPA) and diacylglycerol (DAG) inhibited the ability of cell-permeant CER to induce apoptosis (Jarvis et al. 1996), but also that PKC inhibitors enhanced CER-induced apoptosis (Jarvis et al, 1994). From these studies it has been suggested that PKC is a key negative regulator of CER-induced apoptosis. 

A fully aromatic pyrazole derivative, FPL 62064 (107), also inhibited 5-LO in the usual cellular and enzymatic systems, but was not seleetive with respect to CO [276]. This compound inhibited AAE (ED50 values against PGE2, LTC4, and oedema were 3.7,28.3, and 40.8 //g/ear, respeetively), guinea-pig UV-induced erythema and phorbol ester ear oedema. The aetivi-ty for FPL 62064 was also attributed to its antioxidant activity presumably in this case the 4-methoxyaniline group is the redox-active moiety. 

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