Premium
Prehispanolone, a novel platelet activating factor receptor antagonist from Leonurus heterophyllus
Author(s) -
Lee ChiMing,
Jiang LiMing,
Shang HongSheng,
Hon PoMing,
He Yun,
Wong Henry N.C.
Publication year - 1991
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1991.tb09853.x
Subject(s) - platelet activating factor , chemistry , antagonist , pharmacology , platelet activating factor receptor , potency , radioligand , receptor antagonist , ic50 , receptor , platelet , stereochemistry , in vitro , biochemistry , biology , endocrinology , immunology
1 Using an in vitro radioligand binding assay for the platelet activating factor (PAF) receptor, we have identified a novel, specific PAF antagonist, prehispanolone, from a Chinese medicinal herb Leonurus heterophyllus.2 The presence of sodium ions inhibited specific [ 3 H]‐PAF binding to rabbit platelet membrane with an IC 50 of 5.2 m m , decreased the inhibitory potency of PAF but increased the inhibitory potency of prehispanolone. 3 Prehispanolone and several of its derivatives inhibited the binding of [ 3 H]‐PAF to rabbit platelets with potencies closely resembling that of inhibition of PAF‐induced aggregation. 4 The integrity of the tetrahydrofuran ring of prehispanolone is critical for its interaction with the PAF receptor. 5 By hydrogenating the dihydrofuran ring and replacing the keto group of prehispanolone with a hydroxyl group, we obtained a compound, LC5507, that is more stable and more active than prehispanolone as a PAF receptor antagonist.