一种新型天然前列腺素5,6-二氢前列腺素E3的鉴定及其生物活性

Identification and biological activity of a novel natural prostaglandin, 5,6-dihydro-prostaglandin E3.

作者信息

Samel N, Järving I, Lõhmus M, Lopp A, Kobzar G, Sadovskaya V, Välimäe T, Lille U

出版信息

Prostaglandins. 1987 Jan;33(1):137-46. doi: 10.1016/0090-6980(87)90311-x.

Abstract

A novel natural E-prostaglandin was detected by HPLC among the endogenous prostaglandins extracted from ram seminal vesicles. The corresponding precursor - all-cis-eicosa-8, 11, 14, 17-tetraenoic acid was isolated from bovine liver lipids and the preparative biosynthesis with the microsomal fraction of ram seminal vesicles was performed. The isolated product was purified by HPLC and identified by GC-MS as 5,6-dihydro-PGE3. The results of in vitro tests demonstrate that 5,6-dihydro-PGE3 is 14 times less active uterine stimulant than PGE1, at the same time retaining 75% of the anti-aggregatory potency of PGE1. Thus, 5,6-dihydro-PGE3 meets the requirements of a selective antithrombotic agent more than PGE1.

摘要

在从公羊精囊中提取的内源性前列腺素中，通过高效液相色谱法检测到一种新型天然E-前列腺素。从牛肝脂质中分离出相应的前体——全顺式-8,11,14,17-二十碳四烯酸，并利用公羊精囊的微粒体部分进行制备性生物合成。分离得到的产物通过高效液相色谱法纯化，并通过气相色谱-质谱联用仪鉴定为5,6-二氢-PGE3。体外试验结果表明，5,6-二氢-PGE3作为子宫刺激剂的活性比PGE1低14倍，同时保留了PGE1 75%的抗聚集能力。因此，与PGE1相比，5,6-二氢-PGE3更符合选择性抗血栓药物的要求。