title: Diverse inhibition of plasminogen activator inhibitor type 1 by theaflavins of black tea.
abstract: Fruits, vegetables, spices and a variety of teas are suggested for the prevention of many diseases. They encompass active, non-nutritional ingredients called nutraceuticals which are defined as food products that provide health benefits. Many nutraceuticals have been tested to identify inhibitors of plasminogen activator inhibitor (PAI-1). PAI-1 is the major and fast acting physiological inhibitor of fibrinolysis. However, preclinical studies of PAI-1 inhibitors have revealed an additional role of PAI-1 in the pathogenesis of vascular remodeling, renal injury, diabetes, obesity, Alzheimer's disease and cancer. Thus PAI-1 is a potential therapeutic target in some of these diseases. Our previous study revealed that a black tea extract (containing mostly theaflavins) inhibits PAI-1. In this study we report results for four pure (>98%) theaflavins. Inactivation of PAI-1 was tested by clot formation and by its lysis using thromboelastometry and measurements of human plasma turbidity. Among four tested theaflavins, theaflavin-3'-gallate was the most potent in PAI-1 inhibition trailed by theaflavin-3,3'-digallate, while the other two i.e., theaflavin and theaflavin-3-gallate did not show inhibitory activity.
authors.affiliation: Urology Research Center, Department of Urology, The University of Toledo-Health Science Campus, 3000 Arlington Ave., Toledo, OH 43614, USA. jerzy.jankun@utoledo.edu
authors.forename: Jerzy
authors.initials: J
authors.lastname: Jankun
authors.forename: Magdalena
authors.initials: M
authors.lastname: Skotnicka
authors.forename: Wiesława
authors.initials: W
authors.lastname: Łysiak-Szydłowska
authors.forename: Abdulrahman
authors.initials: A
authors.lastname: Al-Senaidy
authors.forename: Ewa
authors.initials: E
authors.lastname: Skrzypczak-Jankun
mesh_terms: D000975:Antioxidants / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D044946:Biflavonoids / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D002392:Catechin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D005342:Fibrinolysis / Q000187:drug effects; D006801:Humans; D017395:Plasminogen Activator Inhibitor 1 / Q000378:metabolism*; D011485:Protein Binding / Q000187:drug effects; D011994:Recombinant Proteins / Q000378:metabolism; D013662:Tea / Q000737:chemistry; D013927:Thrombosis / Q000188:drug therapy
chemical_list: D000975:Antioxidants; D044946:Biflavonoids; D017395:Plasminogen Activator Inhibitor 1; D011994:Recombinant Proteins; D013662:Tea; C056068:theaflavin; D002392:Catechin