Bufadienolides from Kalanchoe daigremontiana modulate the enzymatic activity of plasmin - In vitro and in silico analyses
PBN-AR
Instytucja
Instytut Uprawy Nawożenia i Gleboznawstwa - Państwowy Instytut Badawczy
Informacje podstawowe
Główny język publikacji
en
Czasopismo
International Journal of Biological Macromolecules (35pkt w roku publikacji)
ISSN
0141-8130
EISSN
Wydawca
ELSEVIER SCIENCE BV
DOI
URL
Rok publikacji
2018
Numer zeszytu
Strony od-do
1591-1600
Numer tomu
120
Identyfikator DOI
Liczba arkuszy
Słowa kluczowe
en
Bufadienolide
Inhibitor
Plasmin
Plasminogen
Streszczenia
Język
en
Treść
Plasmin (EC 3.4.21.7) is a key enzyme of the fibrinolytic system, responsible for the degradation of fibrin clot and maintaining blood fluidity. Hence, alterations of the fibrinolytic capacity of blood plasma may contribute to thrombotic or bleeding complications. The aim of this study was to determine effects of a bufadienolide-rich fraction, isolated from roots of Kalanchoe daigremontiana (0.05–50 μg/ml) on enzymatic properties of plasmin. Hydrolysis of a synthetic substrate S-2251 (H-D-Valyl-l-leucyl-l-lysine-p-nitroaniline dihydrochloride) by plasmin revealed that the bufadienolide-rich fraction had a diverse effect on this enzyme, dependently on the concentration range. While the lower concentrations of the examined fraction (0.05–2.5 μg/ml) significantly enhanced the amidolytic activity of plasmin, at 25–50 μg/ml concentrations, the enzyme was evidently inhibited (by about 60%). The Lineweaver-Burk plot indicated on an uncompetitive inhibition of plasmin. Inhibitory effects (up to 80%) were also found in the streptokinase-induced plasminogen activation to plasmin. Docking results suggest that only some of compounds (mostly bersaldegenin 1-acetate (10), bryotoxin (13) and hovetrichoside C (17)) were bound to plasminogen/plasmin, depending on the presence or absence of the substrate in the active site. The obtained findings suggest allosteric regulation of plasminogen activation and plasmin activity by components of the examined fraction.
Cechy publikacji
Original article
Inne
System-identifier
PBN-R:879336
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