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Catechin and epicatechin as an adjuvant in the therapy of hemostasis disorders induced by snake venoms.
Journal of Biochemical and Molecular Toxicology ( IF 3.6 ) Pub Date : 2020-08-24 , DOI: 10.1002/jbt.22604
Pedro H S Cesar 1 , Marcus V C Trento 1 , Isaac F M Konig 1 , Silvana Marcussi 1
Affiliation  

Snake toxins, such as phospholipases A2 and proteases, are used as research tools to evaluate biological activities and to understand physiopathological processes of natural compounds better. In the present study, the phenolic compounds catechin and epicatechin were incubated with snake venoms to evaluate their inhibition against different substrates. Catechin and epicatechin exerted inhibitions between 20% and 95% on the activity of phospholipases A2 present in the venom of Bothrops alternatus. In the hemolytic activity, catechin exerted inhibitions between 20% and 25% in all proportions evaluated on the B. jararacussu venom, whereas epicatechin inhibited 20% of the venom activity. Coagulation induced by B. atrox and B. jararacussu venoms was significantly inhibited by catechin and epicatechin, where the time for coagulation was two to three times higher after previous incubation of the venoms with the compounds. The most significant inhibitions for the proteolytic activity on casein were 17% and 27%, respectively, by both compounds. Catechin inhibited serine protease activity induced by B. atrox venom by 64% and epicatechin by 65%. Regarding B. atrox‐induced thrombolysis, catechin exerted 40% inhibition and epicatechin around 30%. The fibrinogen proteolysis was completely inhibited by catechin acting on the B. atrox venom in the proportion of 1:1 and by epicatechin on B. jararacussu venom. Catechin and epicatechin showed promising inhibitory action on proteases and phospholipases A2. Therefore, these compounds can be explored as an adjuvant for serum therapy or pharmaceutical purposes, once they act on homologous enzymes that are present in humans.

中文翻译:

儿茶素和表儿茶素作为治疗蛇毒引起的止血障碍的佐剂。

蛇毒素(例如磷脂酶A 2和蛋白酶)被用作研究工具,以评估生物活性并更好地了解天然化合物的生理病理过程。在本研究中,将酚类化合物儿茶素和表儿茶素与蛇毒一起孵育,以评估其对不同底物的抑制作用。儿茶素和表儿茶素对存在于互变种蛇毒中的磷脂酶A 2的活性产生20%至95%的抑制作用。在溶血活性中,儿茶素对jararacussu毒液的所有比例均具有20%至25%的抑制作用,而表儿茶素则抑制20%的毒液活性。B. atrox诱导的凝血儿茶素和表儿茶素可显着抑制雅加达毕加索壶状芽胞杆菌的毒液,在先前将毒液与化合物孵育后,凝血时间要长两到三倍。两种化合物对酪蛋白的蛋白水解活性的最显着抑制分别为17%和27%。儿茶素抑制了约B. atrox毒液诱导的丝氨酸蛋白酶活性,而表儿茶素抑制了65%。关于B. atrox引起的溶栓,儿茶素具有40%的抑制作用,表儿茶素具有30%的抑制作用。儿茶素以1:1的比例作用在约氏芽孢杆菌毒液上,而儿茶素对坛芽孢杆菌则完全抑制了纤维蛋白原的蛋白水解毒液。儿茶素和表儿茶素对蛋白酶和磷脂酶A 2具有抑制作用。因此,一旦这些化合物对人类中存在的同源酶起作用,便可以作为佐剂用于血清疗法或药学目的。
更新日期:2020-08-24
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