TY - JOUR
T1 - Attenuation of experimental TPA-induced dermatitis by acetylenic acetogenins is associated with inhibition of PLA 2 activity
AU - Otuki, Michel Fleith
AU - Schwob, Ouri
AU - Silveira Prudente, Arthur
AU - Zaltsman, Igor
AU - Meretski, Shai
AU - Segal, Joseph
AU - Yedgar, Saul
AU - Rosenblat, Gennady
PY - 2011/12/15
Y1 - 2011/12/15
N2 - Topical application of acetylenic acetogenins (AAG) from avocado (0.01-1.0 mg/ear), was effective in inhibiting both 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema, and in decreasing tissue myeloperoxidase activity (indicative of polymorphonuclear leukocyte influx). Maximum edema inhibition of 72% was achieved by AAG at lower concentration (0.6 mg/ear) than that of the anti-inflammatory drug indomethacin (2 mg/ear). The maximum myeloperoxidase inhibition of 60% was obtained at AAG concentration 0.1 mg/ear. Chemical reduction of unsaturated bonds in aliphatic chain of AAG molecules almost abrogated inhibition effect of AAG at high concentration. In vitro AAG administration reduced secretion of PGE 2 in TPA-induced keratinocytes, and inhibited total PLA 2 and sPLA 2 activities in HaCaT cells. The results indicate a topical anti-inflammatory effect of acetylenic acetogenins which is associated with inhibition of PLA 2 activity in skin.
AB - Topical application of acetylenic acetogenins (AAG) from avocado (0.01-1.0 mg/ear), was effective in inhibiting both 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema, and in decreasing tissue myeloperoxidase activity (indicative of polymorphonuclear leukocyte influx). Maximum edema inhibition of 72% was achieved by AAG at lower concentration (0.6 mg/ear) than that of the anti-inflammatory drug indomethacin (2 mg/ear). The maximum myeloperoxidase inhibition of 60% was obtained at AAG concentration 0.1 mg/ear. Chemical reduction of unsaturated bonds in aliphatic chain of AAG molecules almost abrogated inhibition effect of AAG at high concentration. In vitro AAG administration reduced secretion of PGE 2 in TPA-induced keratinocytes, and inhibited total PLA 2 and sPLA 2 activities in HaCaT cells. The results indicate a topical anti-inflammatory effect of acetylenic acetogenins which is associated with inhibition of PLA 2 activity in skin.
KW - Acetylenic acetogenins
KW - Avocado
KW - Experimental dermatitis
KW - Phospholipase A inhibitor
UR - http://www.scopus.com/inward/record.url?scp=81255160659&partnerID=8YFLogxK
U2 - 10.1016/j.ejphar.2011.09.184
DO - 10.1016/j.ejphar.2011.09.184
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C2 - 22001563
AN - SCOPUS:81255160659
SN - 0014-2999
VL - 672
SP - 175
EP - 179
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 1-3
ER -