Muller A, Rechencq E, Kugel C, Lellouche J P, Beaucourt J P, Niel G, Girard J P, Rossi J C, Bonne C
Laboratoire de Physiologie Cellulaire, Faculté de Pharmacie, Université Montpellier I, France.
Prostaglandins. 1989 Dec;38(6):635-44. doi: 10.1016/0090-6980(89)90046-4.
(5,6)-dihydroxy-7,9-trans-11,14-cis-eicosatetraenoic acids [5,6)-DiHETEs) were synthesized and separated into four pure diastereoisomers. They were tested for comparative binding affinities to leukotriene receptors (LTC4, LTD4, LTB4) in guinea pig lung membranes. Only (5S,6R)-DiHETE was recognized by the LTD4 receptor, the other receptors interacted with neither of the four isomers. (5S,6R)-DiHETE also contracted ileum in vitro and this effect was inhibited by the LTD4 receptor antagonists ICI 198,615 and SKF104,353. These data suggest that the bioproduct (5S,6R)-DiHETE generated by enzymatic conversion of LTA4 could have some LTD4-like activity when produced in large concentrations.
合成了(5,6)-二羟基-7,9-反式-11,14-顺式-二十碳四烯酸[5,6)-二氢二十碳四烯酸(DiHETEs)]，并将其分离为四种纯的非对映异构体。对它们与豚鼠肺膜中白三烯受体(LTC4、LTD4、LTB4)的比较结合亲和力进行了测试。只有(5S,6R)-二氢二十碳四烯酸被LTD4受体识别，其他受体与这四种异构体均无相互作用。(5S,6R)-二氢二十碳四烯酸在体外也能使回肠收缩，LTD4受体拮抗剂ICI 198,615和SKF104,353可抑制这种效应。这些数据表明，LTA4经酶促转化产生的生物产物(5S,6R)-二氢二十碳四烯酸在大量产生时可能具有一些LTD4样活性。
