Bufadienolides from Kalanchoe daigremontiana as thrombin inhibitors-In vitro and in silico study
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
2017
Numer zeszytu
Strony od-do
141-150
Numer tomu
99
Identyfikator DOI
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Autorzy
Pozostali autorzy
+ 4
Słowa kluczowe
en
Bufadienolide
Inhibitor
Thrombin
Streszczenia
Język
en
Treść
Thrombin is an active plasma coagulation factor II, critical for the formation of fibrin clot during blood coagulation. For that reason, this protein is also a crucial target for different anti-thrombotic therapies. The work is based on in vitro evaluation of the inhibitory effect of bufadienolide-rich fraction, isolated from roots of Kalanchoe daigremontiana (1-50μg/ml) on enzymatic properties of a serine proteinase - thrombin. The efficacy of the inhibition of amidolytic activity of thrombin (measured as a hydrolysis of the chromogenic substrate S-2238, Chromogenix) attained about 10 and 66%, respectively. The IC50, established for the examined bufadienolide fraction was 2.79μg/ml, while the IC50 calculated for argatroban (reference compound) was 0.78μg/ml. Linearization conducted using Lineweaver-Burk plot indicated that the K. daigremontiana fraction contains compounds that are uncompetitive inhibitors of thrombin. K. daigremontiana fraction was also able to reduce the proteolytic activity of thrombin towards its physiological substrate, i.e. fibrinogen. Additionally, this study is supported by in silico analysis of interactions of the most common compounds, identified in the examined in Kalanchoe extract to crystal structure of this enzyme.
Cechy publikacji
Original article
Oryginalny artykuł naukowy
Inne
System-identifier
PBN-R:822649
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