Soraci A, Benoit E
Department of Metabolic Toxicology, School of Veterinary Medicine of Lyon, Marcy-l'Etoile, France.
Chirality. 1995;7(7):534-40. doi: 10.1002/chir.530070707.
In vitro coenzyme A thioester formation from (-)-(R)-fenoprofen (FPF) and palmitic acid has been studied using liver microsomes from rat, guinea pig, sheep, and dog. In every species with both palmitic acid or (-)-(R)-fenoprofen, the Lineweaver-Burk plot was linear in the substrate concentration range used and as a consequence agrees with the involvement of only one isoenzyme (or different isoenzymes of similar Km values). The Vmax values for the thioesterification of (-)-(R)-fenoprofen present large species variations from 2.1 +/- 1.0 with sheep liver microsomes to 60.6 +/- 11 nmol/min/mg with dog liver microsomes. These values statistically significantly correlate (r = 0.94) to the Vmax values observed when palmitic acid was used as a substrate. Furthermore palmitic acid inhibited (-)-(R)-fenoprofen-CoA formation in the same extent in all animal species. The stereoselectivity of the thioesterification was also species dependent.
利用大鼠、豚鼠、绵羊和狗的肝脏微粒体,对(-)-(R)-非诺洛芬(FPF)和棕榈酸在体外形成辅酶A硫酯的过程进行了研究。在每一个同时使用棕榈酸或(-)-(R)-非诺洛芬的物种中,Lineweaver-Burk图在所用底物浓度范围内呈线性,因此表明只有一种同工酶(或Km值相似的不同同工酶)参与反应。(-)-(R)-非诺洛芬硫酯化反应的Vmax值在不同物种间差异很大,从绵羊肝脏微粒体的2.1±1.0到狗肝脏微粒体的60.6±11 nmol/min/mg。这些值与以棕榈酸为底物时观察到的Vmax值在统计学上显著相关(r = 0.94)。此外,棕榈酸在所有动物物种中对(-)-(R)-非诺洛芬-CoA形成的抑制程度相同。硫酯化反应的立体选择性也因物种而异。