title: Gossypol-induced inhibition of plasminogen activator activity in human and ovine acrosomal extract.
abstract: The effect of gossypol--a polycyclic compound isolated from cotton seeds--on the plasminogen activator activity of man and ram acrosomal extracts was explored in vitro. The action of gossypol on the plasminogen activator activity was investigated by a spectrophotometric method using the chromogenic substrate S-2251. Gossypol, a known antispermatogenic agent, was found to effectively inhibit human and ovine acrosomal plasminogen activator activity. The inhibition was dose-dependent. Plasminogen activator activity from man and ram extracts was completely inhibited by 350 mumol l-1 and 300 mumol l-1 of gossypol, respectively. In additional experiments, low, non-spermicidal concentrations of gossypol (2.5-40 mumol l-1) were found to significantly inhibit plasmin activity in a dose-dependent manner. The results suggest that inhibition of both acrosomal plasminogen activator and plasmin activity is a possible mechanism by which gossypol exerts its antifertility effect, since the plasminogen activator/plasmin system plays a role in the whole process of ovum fertilization.
authors.affiliation: Department of Physiology, Faculty of Veterinary Medicine, University of Thessaly, Karditsa, Greece.
authors.forename: I A
authors.initials: IA
authors.lastname: Taitzoglou
authors.forename: M
authors.initials: M
authors.lastname: Tsantarliotou
authors.forename: D
authors.initials: D
authors.lastname: Kouretas
authors.forename: N A
authors.initials: NA
authors.lastname: Kokolis
mesh_terms: D000177:Acrosome / Q000378:metabolism*; D000818:Animals; D002863:Chromogenic Compounds; D005341:Fibrinolysin / Q000494:pharmacology; D006072:Gossypol / Q000494:pharmacology*; D006801:Humans; D008297:Male; D009842:Oligopeptides; D010960:Plasminogen Activators / Q000037:antagonists & inhibitors*; D012756:Sheep
chemical_list: D002863:Chromogenic Compounds; D009842:Oligopeptides; C018788:valyl-leucyl-lysine 4-nitroanilide; D010960:Plasminogen Activators; D005341:Fibrinolysin; D006072:Gossypol