Detail of "152815-51-5"

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Inhibitory effect of a new butadiene derivative on the production of plasminogen activator inhibitor-1 in cultured bovine endothelial cells

Inhibitory effect of a new butadiene derivative on the production of plasminogen activator inhibitor-1 in cultured bovine endothelial cells. Ohtani, Akio; Takagi, Tamotsu; Hirano, Ayako; Murakami, Jun; Sasaki, Yasuhiko (Lead Optimization Res. Lab., Tanabe Seiyaku Co., Ltd., Toda 335, Japan). Journal of Biochemistry (Tokyo), 120(6), 1203-1208 (English) 1996 Japanese Biochemical Society. CODEN: JOBIAO. ISSN: 0021-924X. DOCUMENT TYPE: Journal CA Section: 4 (Toxicology) Section cross-reference(s): 15 Tissue-type plasminogen activator (t-PA) and its physiol. inhibitor, plasminogen activator inhibitor-1 (PAI-1), are known to be synthesized by vascular endothelial cells and to play important roles in regulating the fibrinolytic activity of plasma. The authors found that a new butadiene deriv., (3E,4E)-3-benzylidene-4-(3,4,5-trimethoxybenzylidene)pyrolidine-2,5-di one (T-686), inhibits PAI-1 prodn. without affecting plasminogen activator (PA) synthesis in cultured bovine endothelial cells.Several substances with their cas registry numbers 106-99-0 and 152815-51-5 may be metioned in this study. T-686 (1-10 mM) dose-dependently decreased the accumulation of PAI-1 in conditioned medium from the treated cells and elevated PA activity in the conditioned medium. Anal. of the conditioned medium by the zymog. technique indicated that T-686 decreased the activities of PAI-1 with an Mr of 55,000 and t-PA/PAI-1 complex with an Mr of 99,000. Furthermore, T-686 attenuated the augmentation of PAI-1 antigen induced by lipopolysaccharide in the conditioned medium. The decrease of PAI-1 antigen was in parallel with the redn. of the PAI-1 mRNA level (Northern blots). These results suggest that T-686 can promote net fibrinolytic activity through suppression of PAI-1 prodn. without affecting PA elaboration in endothelial cells. .