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. 2010 Dec;62(12):1711-6.
doi: 10.1111/j.2042-7158.2010.01145.x. Epub 2010 Oct 4.

Lutein is a competitive inhibitor of cytosolic Ca²+-dependent phospholipase A₂

Ho Sun Song  1 , Hee Rae Kim, Myung Cheul Kim, Yeon Hee Hwang, Sang Soo Sim
Affiliations

Lutein is a competitive inhibitor of cytosolic Ca²+-dependent phospholipase A₂

Ho Sun Song et al. J Pharm Pharmacol. 2010 Dec.

Abstract

Objectives: We have investigated the effect of lutein on phospholipase A₂ (PLA₂) isozymes.

Methods: We measured arachidonic acid release in [³H]arachidonic acid-labelled Raw 264.7 cells and PLA₂ activity using 1-palmitoyl-2-[¹⁴C]arachidonyl phosphatidylcholine ([¹⁴C]AA-PC) and 10-pyrene phosphatidylcholine in vitro.

Key findings: Lutein suppressed the release of arachidonic acid and inhibited Raw 264.7 cell-derived cytosolic Ca²+-dependent PLA₂ (cPLA₂-induced hydrolysis of [¹⁴C]AA-PC in a dose- and time-dependent manner. In contrast, lutein did not affect secretory Ca²+-dependent PLA₂ (sPLA₂)-induced hydrolysis of [¹⁴C]AA-PC. A Dixon plot showed that the inhibition by lutein on cPLA₂ appeared to be competitive with an inhibition constant, K(i) , of 13.6 µm.

Conclusions: We suggest that lutein acted as a competitive inhibitor of cPLA₂ but did not affect sPLA₂.

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