Hong K H, Bonventre J C, O'Leary E, Bonventre J V, Lander E S
Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142, USA.
Proc Natl Acad Sci U S A. 2001 Mar 27;98(7):3935-9. doi: 10.1073/pnas.051635898. Epub 2001 Mar 13.
Although nonsteroidal antiinflammatory drugs (NSAIDs) show great promise as therapies for colon cancer, a dispute remains regarding their mechanism of action. NSAIDs are known to inhibit cyclooxygenase (COX) enzymes, which convert arachidonic acid (AA) to prostaglandins (PGs). Therefore, NSAIDs may suppress tumorigenesis by inhibiting PG synthesis. However, various experimental studies have suggested the possibility of PG-independent mechanisms. Notably, disruption of the mouse group IIA secretory phospholipase A(2) locus (Pla2g2a), a potential source of AA for COX-2, increases tumor number despite the fact that the mutation has been predicted to decrease PG production. Some authors have attempted to reconcile the results by suggesting that the level of the precursor (AA), not the products (PGs), is the critical factor. To clarify the role of AA in tumorigenesis, we have examined the effect of deleting the group IV cytosolic phospholipase A(2) (cPLA(2)) locus (Pla2g4). We report that Apc(Min/+), cPLA(2)(-/-) mice show an 83% reduction in tumor number in the small intestine compared with littermates with genotypes Apc(Min/+), cPLA(2)(+/-) and Apc(Min/+), cPLA(2)(+/+). This tumor phenotype parallels that of COX-2 knockout mice, suggesting that cPLA(2) is the predominant source of AA for COX-2 in the intestine. The protective effect of cPLA(2) deletion is thus most likely attributed to a decrease in the AA supply to COX-2 and a resultant decrease in PG synthesis. The tumorigenic effect of sPLA(2) mutations is likely to be through a completely different pathway.
尽管非甾体抗炎药(NSAIDs)作为结肠癌的治疗方法显示出巨大的前景,但关于其作用机制仍存在争议。已知NSAIDs可抑制环氧化酶(COX),该酶将花生四烯酸(AA)转化为前列腺素(PGs)。因此,NSAIDs可能通过抑制PG合成来抑制肿瘤发生。然而,各种实验研究表明存在不依赖PG的机制的可能性。值得注意的是,小鼠IIA组分泌型磷脂酶A2基因座(Pla2g2a)的破坏,这是COX-2的潜在AA来源,尽管预测该突变会减少PG产生,但肿瘤数量却增加了。一些作者试图通过表明前体(AA)的水平而非产物(PGs)的水平是关键因素来调和这些结果。为了阐明AA在肿瘤发生中的作用,我们研究了删除IV组胞质磷脂酶A2(cPLA2)基因座(Pla2g4)的效果。我们报告说,与基因型为Apc(Min/+), cPLA(2)(+/-)和Apc(Min/+), cPLA(2)(+/+)的同窝小鼠相比,Apc(Min/+), cPLA(2)(-/-)小鼠小肠中的肿瘤数量减少了83%。这种肿瘤表型与COX-2基因敲除小鼠的表型相似,表明cPLA2是肠道中COX-2的主要AA来源。因此,cPLA2缺失的保护作用很可能归因于COX-2的AA供应减少以及PG合成的相应减少。sPLA2突变的致瘤作用可能是通过完全不同的途径。