Boucrot P, Bourass J, Elkihel L, Letourneux Y, Gandemer G
Laboratoire d'Etude des Intéractions des Molécules Alimentaires, I. N.R.A. BP7 1627, 44316 Nantes Cedex 3, France.
Pharmacol Res. 1997 Aug;36(2):135-9. doi: 10.1006/phrs.1997.0215.
The phospholipid analogue with two short fatty chains, 1-dodecyl-2-[1-14C] octanamido-sn-2-deoxy-glycero-3-phosphocholine ([14C] phospholipid analogue), with a non-hydrolyzable bond at position 2 of the glycerol, is an inhibitor of phospholipase A2. It was obtained after chemical synthesis and 0.5 micromol was solubilized in Na+ taurocholate with an equimolar amount of 1-octadecanoyl 2-[3H]eicosatetraenoyl-sn- glycero-3-phosphocholine which is the current substrate of phospholipases A2. Both molecules were introduced into the duodenum of rats in order to follow their captations by intestinal mucosa cells for 30, 60 or 90 min. The [14C] phospholipid analogue was poorly split by phospholipases A2 (pancreatic juice and intracellular enzymes). It disappeared from the intestinal contents (87% of the dose gone in 90 min) as rapidly as the tritiated lecithin (81%) but this was later split by the phospholipases at a higher rate.
具有两条短脂肪链的磷脂类似物，1-十二烷基-2-[1-¹⁴C]辛酰胺基-sn-2-脱氧甘油-3-磷酸胆碱（[¹⁴C]磷脂类似物），在甘油的2位具有不可水解的键，是磷脂酶A2的抑制剂。它是通过化学合成获得的，0.5微摩尔溶解于牛磺胆酸钠中，并与等摩尔量的1-十八烷酰基-2-[³H]二十碳四烯酰基-sn-甘油-3-磷酸胆碱混合，后者是磷脂酶A2的当前底物。将这两种分子引入大鼠十二指肠，以便观察肠黏膜细胞在30、60或90分钟内对它们的摄取情况。[¹⁴C]磷脂类似物被磷脂酶A2（胰液和细胞内酶）分解的程度很低。它从肠内容物中消失的速度（90分钟内87%的剂量消失）与氚标记的卵磷脂（81%）一样快，但后来被磷脂酶分解的速度更高。
