Stone K J, Willis A L, Hart W M, Kirtland S J, Kernoff P B, McNicol G P
Lipids. 1979 Feb;14(2):174-80. doi: 10.1007/BF02533869.
Orally administered dihomo-gamma-linolenic acid (DHLA) is well absorbed in man; it appears in blood after ca. 4 hr first as triglyceride ester and later as phospholipid. After sustained-dosing, DHLA penetrated membrane pools and all phospholipid components but, depending on the dosage, reached a metabolic equilibrium in 4-16 days. Intact platelets do not accumulate arachidonate following DHLA administration, and species differences occur in the capacity of animals to metabolize DHLA to arachidonic acid (AA). The rat appears to be unusual in having a very active hepatic delta5-desaturase enzyme system. Potentially antithrombotic changes in platelet function which followed the administration of DHLA to man were accompanied by a significant increase in the capacity of platelets to synthesize PGE1. Concomitant increases in PGE2 synthesis do not apparently result from an increased production of AA and suggest that DHLA, or a DHLA metabolite, interferes with the metabolism of AA. Effects on thromboxane and prostacyclin synthesis are being studied.
口服给予的二高 -γ- 亚麻酸(DHLA)在人体中吸收良好;约4小时后它首先以甘油三酯酯的形式出现在血液中,随后以磷脂形式出现。持续给药后,DHLA渗透到膜池和所有磷脂成分中,但根据剂量不同,在4 - 16天内达到代谢平衡。给予DHLA后,完整的血小板不会积累花生四烯酸,并且动物将DHLA代谢为花生四烯酸(AA)的能力存在种属差异。大鼠似乎不同寻常,其肝脏具有非常活跃的δ5-去饱和酶系统。给予人体DHLA后血小板功能发生的潜在抗血栓形成变化伴随着血小板合成PGE1能力的显著增加。PGE2合成的同时增加显然不是由AA产量增加导致的,这表明DHLA或DHLA代谢物干扰了AA的代谢。目前正在研究其对血栓素和前列环素合成的影响。