Synthetic Dipeptide, N-Stearoyl-D-Ser-L-Pro-OEt, Induces Release of Tissue-Type Plasminogen-Activator in Cultured Cells and in Experimental Animals.

Okayama, Toru; Nakano, Masaharu; Odake, Shinjiro; Hagiwara, Makoto; Morikawa, Tadanori; Ueshima, Shigeru; Okada, Kiyotaka; Fukao, Hideharu; Mtsuo, Osamu

doi:10.1248/cpb.42.1854

Cited by 8 publications

(9 citation statements)

References 1 publication

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…For thrombotic diseases, many attempts have been made to develop chemical compounds which would enhance t-PA release from endothelial cells (27,28). However, these compounds have undesirable side effect.…”

Section: Discussionmentioning

confidence: 99%

Antithrombotic Effect of Oral Administration of Mozuku (<i>Cladosiphon okamuranus</i>, Brown Seaweed) Extract in Rat

Yasuzawa

Mima

Ueshima

2019

J Nutr Sci Vitaminol

Self Cite

View full text Add to dashboard Cite

Dysfunction of vascular endothelial cells causes the risk of thrombosis. Aim of this study is to evaluate the antithrombotic effect of Okinawa mozuku (brown seaweed, Cladosiphon okamuranus) extract by using cultured vascular endothelial cells and rat carotid arterial thrombosis model induced by ferric chloride (FeCl3). The cell line (TKM-33) established from human umbilical vein endothelial cells were cultured with or without Okinawa mozuku extract. After incubation for 24 h, the conditioned medium was collected to evaluate urokinase-type plasminogen activator (u-PA) activity. Next, rats were fed with water or water containing 5% of Okinawa mozuku extract for 8 wk. After 8 wk of treatments, the rats were provided for the carotid arterial thrombosis model, and fibrinolytic factor and coagulation factor in blood were measured. Okinawa mozuku extract significantly augmented u-PA activity in the conditioned medium. The decrease of carotid artery blood flow induced by 40% FeCl3 injury in rats fed with Okinawa mozuku extract was less than that in control rats. Thus, oral administration of Okinawa mozuku extract prevented thrombus formation in this model. Oral administration of Okinawa mozuku extract significantly increased u-PA activity in euglobulin fraction, compared with control group. On the other hand, platelet aggregation activity, activated partial thromboplastin time, and active PAI-1 level in plasma exhibited no significant differences between control and Okinawa mozuku groups. These results indicate that oral administration of Okinawa mozuku enhances fibrinolytic activity in plasma and prevents thrombus formation which is induced by injury of vascular endothelial cells.

show abstract

Section: Discussionmentioning

confidence: 99%

Antithrombotic Effect of Oral Administration of Mozuku (<i>Cladosiphon okamuranus</i>, Brown Seaweed) Extract in Rat

Yasuzawa

Mima

Ueshima

2019

J Nutr Sci Vitaminol

Self Cite

View full text Add to dashboard Cite

show abstract

“…The use of chemical agents which enhance t-PA release from endothelial cells has been adopted in attempts to develop clinical therapy of thrombotic diseases [18][19][20]. However, these developments have failed due to undesirable side effect.…”

Section: Discussionmentioning

confidence: 99%

Profibrinolytic effect of Enzamin, an extract of metabolic products from Bacillus subtilis AK and Lactobacillus

Tamura

Okada

Kawao

et al. 2011

J Thromb Thrombolysis

Self Cite

View full text Add to dashboard Cite

Fibrinolytic system impairment contributes to the development of thrombotic disease such as cardiovascular disease and stroke. Therefore, an agent that increases fibrinolytic activity may be useful for the prevention of these diseases. In this study, to explore novel profibrinolytic agents, we examined the profibrinolytic effect of Enzamin, an extract of metabolic products from Bacillus subtilis AK and Lactobacillus in vitro and in vivo. Enzamin directly enhanced plasmin activity generated by tissue-type plasminogen activator (t-PA) by twofold but not by urokinase-type plasminogen activator (u-PA) in vitro, which was measured employing both the chromogenic substrate H-D: -Val-Leu-Lys-pNA (S-2251) and fibrin plate. Enzamin also increased plasmin activity generated by t-PA in the cell lysate and culture medium of endothelial cells, measured by fibrin zymography. Furthermore, the oral administration of a 1% concentration of Enzamin increased plasmin activity generated by t-PA by 1.7-fold but not by u-PA in the euglobulin fraction of mouse plasma. In conclusion, Enzamin has a unique ability to enhance the fibrinolytic activity through an increase in endogenous plasmin activity generated by t-PA released from endothelial cells, and may be a beneficial supplement for the prevention of thrombotic episodes.

show abstract

“…Wir entschieden uns dafür, das komplette Dipeptid 20 mit der freien Säure zu verknüpfen, was in sehr guter Ausbeute gelang (Schema ). Das Dipeptid 20 war aus L ‐Prolin in sechs Stufen und einer Gesamtausbeute von 49 % leicht zugänglich 30. Die befürchtete Diketopiperazinbildung unterblieb, wenn man das Ammoniumsalz von 20 zusammen mit 19 und dem Reagens TOTU vorlegte und dann die Base ( i Pr 2 NEt) tropfenweise zugab.…”

Section: Methodsunclassified

Totalsynthese des Thiazolylpeptids GE2270 A

2007

View full text Add to dashboard Cite

Die Umkehrung zum Guten: In der Synthese des Thiazolylpeptids GE2270 A (1) werden durch zwei aufeinander folgende Kreuzkupplungen die Bindungen am zentralen Pyridinring geknüpft (I und II). Die Bildung der Amidbindung (IV) mit anschließender intramolekularer Stille‐Reaktion (III) ist deutlich effektiver als das ursprünglich geplante, umgekehrte Vorgehen (III vor IV). Eine Gesamtausbeute von 4.8 % über 20 Stufen belegt eindrucksvoll den Erfolg der konvergenten Synthesestrategie.

show abstract

Synthetic Dipeptide, N-Stearoyl-D-Ser-L-Pro-OEt, Induces Release of Tissue-Type Plasminogen-Activator in Cultured Cells and in Experimental Animals.

Cited by 8 publications

References 1 publication

Antithrombotic Effect of Oral Administration of Mozuku (<i>Cladosiphon okamuranus</i>, Brown Seaweed) Extract in Rat

Antithrombotic Effect of Oral Administration of Mozuku (<i>Cladosiphon okamuranus</i>, Brown Seaweed) Extract in Rat

Profibrinolytic effect of Enzamin, an extract of metabolic products from Bacillus subtilis AK and Lactobacillus

Totalsynthese des Thiazolylpeptids GE2270 A

Contact Info

Product

Resources

About