RRC ID 44913
著者 Tsuchiya A, Kanno T, Shimizu T, Nakao S, Tanaka A, Nishizaki T.
タイトル DCP-LA-phosphatidylinositol and its enantiomer exhibit different bioactivities.
ジャーナル Cell Physiol Biochem
Abstract BACKGROUND/AIMS:The present study was conducted to understand biochemical and biological characteristics of the phosphatidylinositol (PI) derivative 1,2-O-bis-[8-{2-(2-pentyl-cyclopropylmethyl)-cyclopropyl}-octanoyl]-Sn-glycero-3-phosphatidyl-D-1-inositol (diDCP-LA-PI) and its enantiomer 1,2-O-bis-[8-{2-(2-pentyl-cyclopropylmethyl)-cyclopropyl}-octanoyl]-Sn-glycero-3-phosphatidyl-L-1-inositol (diDCP-LA-PIe), with 8-[2-(2-pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) on the α and β position.
METHODS:Activities of protein kinase C (PKC) and protein phosphatases such as protein phosphatase 1 (PP1), PP2A, and protein tyrosine phosphatase 1B (PTP1B) were assayed under the cell-free conditions and in PC-12 cells. Akt1/2 activity was monitored by quantifying phosphorylation at Thr308/309 and Ser473/474 in PC-12 cells.
RESULTS:diDCP-LA-PI significantly activated PKCα, -βΙ, -δ, and -ε, to an extent greater than that for diDCP-LA-PIe. diDCP-LA-PI still activated PKC in PC-12 cells, with the potential higher than that for diDCP-LA-PIe. Both diDCP-LA-PI and diDCP-LA-PIe reduced PP1 activity to a similar extent (30% of basal levels). diDCP-LA-PI enhanced PP2A activity to 180% of basal levels, while diDCP-LA-PIe had no effect. Drastic inhibition of PTP1B was obtained with diDCP-LA-PI and diDCP-LA-PIe, the extent reaching nearly 0% of basal levels. diDCP-LA-PI and diDCP-LA-PIe increased phosphorylation of Akt1/2 at Thr308/309 and Ser473/474 in PC-12 cells in the presence and absence of the PP2A inhibitor okadaic acid, respectively.
CONCLUSION:The results of the present study show that diDCP-LA-PI and diDCP-LA-PIe exhibit different bioactivities with the different potentials each other.
巻・号 33(2)
ページ 300-9
公開日 2014-1-1
DOI 10.1159/000356670
PII 000356670
PMID 24525749
MeSH Animals PC12 Cells Phosphatidylinositols* / chemical synthesis Phosphatidylinositols* / chemistry Phosphatidylinositols* / pharmacology Phosphoprotein Phosphatases / metabolism* Phosphorylation / drug effects Protein Kinases / metabolism* Rats
IF 5.5
引用数 2
WOS 分野 PHYSIOLOGY CELL BIOLOGY
リソース情報
ヒト・動物細胞 PC-12(RCB0009)