[Effect in vitro of albendazole on the kinetics of cytosolic glutathione transferase from the rat liver].

Abstract

INTRODUCTION:

Since the idea of multifunctional mode of action of anthelmintics is considered and in experimental trichinellosis in vivo albendazole seems to act as an allosteric activator of cytosolic GST from mice muscles, in this study a termosensitivity after in vitro incubation with albendazole of purified commercial cytosolic glutathione transferase (GST) from the rat liver was investigated.

METHODS:

Two extremal temperatures: -80 degrees C and +30 degrees C were used to destroy the dimer in quaternary structure of this enzyme.

RESULTS:

In control preparations both extremal temperatures destroy this structure, so the Michaelis-Menten kinetic curves of substrate saturation show the typical hyperbolic shape. After a long (15 h) freezing at -80 degrees C or heating (up to 14 h at +30 degrees C) the kinetics of substrate saturation of GST after incubation with albendazole show the sigmoidal or "double sigmoidal" shape, pointing out the quaternary GST structure as a complex of "frozen subunits". Drug inhibits about 6-times the total activity of GST after incubation at +30 degrees C. We conclude that albendazole in vitro influences the structure of cytosolic GST from the rat liver and inhibits its activity, but, in opposite to in vivo study in mouse muscles infected with Trichinella spiralis larvae, does not act as an activator of this enzyme.

• Authors: Agnieszka Wojtkowiak, Krystyna Boczoń, Elzbieta Wandurska-Nowak
• Journal: Wiadomosci parazytologiczne (Wiad Parazytol) Vol. 53 Issue 2 Pg. 97-102 ( 2007) ISSN: 0043-5163 [Print] Poland
• Vernacular Title: Badania in vitro wpływu albendazolu na kinetyke reakcji ka- talizowanej przez cytozolowa transferaze glutationowa (GST) z watroby szczura.
• PMID: 17912804 (Publication Type: English Abstract, Journal Article)

Chemical References

• Anthelmintics
• Glutathione Transferase
• Albendazole

Topics

• Albendazole (pharmacology)
• Allosteric Regulation
• Animals
• Anthelmintics (pharmacology)
• Cytosol (enzymology)
• Enzyme Activation
• Glutathione Transferase (chemistry, drug effects, metabolism)
• Host-Parasite Interactions
• In Vitro Techniques
• Kinetics
• Larva (enzymology)
• Liver (enzymology)
• Mice
• Muscle, Skeletal (enzymology)
• Protein Structure, Quaternary (drug effects)
• Rats
• Temperature
• Trichinella spiralis (enzymology)
• Trichinellosis (drug therapy, enzymology)