Inhibition characteristics of hypericin on rat small intestine glutathione-S-transferases

Chemico-biological Interactions
Gamze TunaNazmi Ozer

Abstract

Glutathione-S-transferases constitute a family of enzymes involving in the detoxification of xenobiotics, signalling cascades and serving as ligandins or/and catalyzing the conjugation of various chemicals and drugs. The widely expressed cytosolic GST-pi is a marker protein in various cancers and its increased concentration is linked to drug resistance. GST-pi is autoregulated by S-glutathionylation and it catalyzes the S-glutathionylation of other proteins in response to oxidative or nitrosative stress. S-glutathionylation of GST-pi results in multimer formation and the breakage of ligand binding interactions with c-Jun NH(2)-terminal kinase (JNK). Another widely expressed GST enzyme, GST-alpha is assumed as a marker in hepatocellular damage, is implicated in cancer, asthma, cardiovascular disease and response to chemotherapy. Although, it was shown that hypericin binds and inhibits GST-alpha and GST-pi, the inhibition characteristics have not been investigated in detail. The aim of this study was to investigate the effects of hypericin on major GSTs; GST-alpha and GST-pi purified from rat small intestine. When GSH used as varied substrate the inhibition pattern with hypericin was uncompetitive for GST-alpha (K(i)=0.16 + or - ...Continue Reading

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Citations

Dec 18, 2015·The International Journal of Biochemistry & Cell Biology·Shengchao LinJianwen Liu
Dec 21, 2010·Chemico-biological Interactions·Guoying NiJiezhong Chen
Aug 19, 2015·Chemico-biological Interactions·Rajiv BalyanMajid Y Moridani
Dec 8, 2011·Journal of Enzyme Inhibition and Medicinal Chemistry·Gulnihal Kulaksiz-ErkmenNazmi Ozer
Feb 24, 2015·Infectious Agents and Cancer·Kenneth AlibekAizada Chinybayeva
Jul 25, 2015·Archiv der Pharmazie·Mustafa Muhlis Alparslan, Özkan Danış
Jul 28, 2012·Chemical Biology & Drug Design·Taner KeskinFunda Yukruk
Dec 9, 2020·Journal of Natural Products·Olga N PetrovaMichel Negrerie

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