Evaluation of the in vitro Inhibitory Impact of Hypericin on Placental Glutathione S-Transferase pi

St John’s Wort (SJW) extracts are herbal products which are available without prescription in most countries and widely used in the treatment of mild to moderate depression. Since it is a herbal product and available without prescription, use of SJW is common among pregnant and/or lactating woman. T...

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Veröffentlicht in:The Protein Journal 2012-10, Vol.31 (7), p.544-549
Hauptverfasser: Dalmizrak, Ozlem, Kulaksiz-Erkmen, Gulnihal, Ozer, Nazmi
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Ozer, Nazmi
description St John’s Wort (SJW) extracts are herbal products which are available without prescription in most countries and widely used in the treatment of mild to moderate depression. Since it is a herbal product and available without prescription, use of SJW is common among pregnant and/or lactating woman. The principal of the study was to clarify the effects of hypericin, one of the components of SJW, on glutathione S-transferase-pi (GST-pi) purified from human placenta. The K m values of GST-pi were 0.21 ± 0.03 mM for glutathione (GSH) and 2.29 ± 0.54 mM for 1-chloro-2,4-dinitrobenzene (CDNB). At fixed [GSH], the V m value calculated was about 3 times higher than the conditions in which [CDNB] was fixed; 201 ± 30 U/mg protein versus 74 ± 3 U/mg protein. At constant substrate concentrations (1 mM), an average IC 50 value of 0.70 ± 0.02 μM was obtained. Hypericin inhibited GST-pi competitively with respect to both substrates. When GSH was the varied substrate a K i value of 0.31 ± 0.05 μM was found; when CDNB was the varied substrate, a K i value of 0.85 ± 0.02 μM was obtained. On the basis of these data considering transplacental transfer of hypericin and immature hepatic clearance of the baby, using this herbal product may cause abnormalites due to the inhibition of one of the most important placental detoxification enzymes, GST-pi.
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subjects Animal Anatomy
Biochemistry
Bioorganic Chemistry
Birth defects
Chemistry
Chemistry and Materials Science
Detoxification
Dinitrochlorobenzene
Electrophoresis, Polyacrylamide Gel
Enzymes
Ethylenediaminetetraacetic acid
Female
Glutathione - metabolism
Glutathione S-Transferase pi - antagonists & inhibitors
Glutathione S-Transferase pi - isolation & purification
Glutathione S-Transferase pi - metabolism
Glutathione transferase
Herbal medicine
Herbs
Histology
Humans
Hypericum - chemistry
Kinetics
Medicine, Botanic
Medicine, Herbal
Morphology
Organic Chemistry
Perylene - analogs & derivatives
Perylene - pharmacology
Placenta - drug effects
Placenta - enzymology
Pregnancy
Proteins
Substrate Specificity
Substrates
Thiols
title Evaluation of the in vitro Inhibitory Impact of Hypericin on Placental Glutathione S-Transferase pi
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