New hits as phase II enzymes inducers from a focused library with heteroatom–heteroatom and Michael-acceptor motives
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چکیده
منابع مشابه
New hits as phase II enzymes inducers from a focused library with heteroatom–heteroatom and Michael-acceptor motives
The increased activity of phase-II-detoxification enzymes, such as quinone reductase (QR) and glutation S-transferase (GST), correlates with protection against chemically induced carcinogenesis. Herein we studied 11 different chemotypes, pyrazole, 1,2,4-oxadiazole, 1,2,5-oxadiazole, 1,2,3-thiadiazole, 1,2,4-thiazole, 1,3,4-oxathiazole, thienyl hydrazone, α,β-unsaturated-oxime, α,β-unsaturated-N...
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Watercress is an exceptionally rich dietary source of beta-phenylethyl isothiocyanate (PEITC). This compound inhibits phase I enzymes, which are responsible for the activation of many carcinogens in animals, and induces phase II enzymes, which are associated with enhanced excretion of carcinogens. In this study, we show that watercress extracts are potent inducers of quinone reductase (QR) in m...
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Article history: Received 5 May 2014 This study examines the motives mentors have for providing developmental support to their protégés. Based on qualitative interviewswith 20 informalmentors, we show five broad categories of mentor motives: self-focused motives (based on individual reasons), protégé-focused motives (directed at the protégé), relationship-focused motives (directed at the relati...
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Induction of phase 2 enzymes and elevations of glutathione are major and sufficient strategies for protecting mammals and their cells against the toxic and carcinogenic effects of electrophiles and reactive forms of oxygen. Inducers belong to nine chemical classes and have few common properties except for their ability to modify sulfhydryl groups by oxidation, reduction, or alkylation. Much evi...
متن کاملMechanism of differential potencies of isothiocyanates as inducers of anticarcinogenic Phase 2 enzymes.
Isothiocyanates occur in many edible plants and are consumed in substantial quantities by humans. A number of isothiocyanates block chemical carcinogenesis in a variety of animal models by inhibiting Phase 1 enzymes involved in carcinogen activation and by inducing Phase 2 enzymes that accelerate the inactivation of carcinogens. There are large but unexplained potency differences among individu...
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ژورنال
عنوان ژورنال: Future Science OA
سال: 2015
ISSN: 2056-5623
DOI: 10.4155/fso.15.18