Journal Article10.1007/BF02975172
Induction of quinone reductase activity by stilbene analogs in mouse Hepa 1c1c7 cells.
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TL;DR: Several compounds including 3,4,5,3′,5′-pentamethoxy-trans-stilbene were found to potentially induce QR activity in this cell line and substitution with 3-thiofurane ring instead of phenyl ring in the stilbenes skeleton also exhibited potential induction of QR activity.
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Abstract: Based on the potential cancer chemopreventive activity of resveratrol, a trihydroxystilbene with the induction of quinone reductase activity, this study was designed to determine if stilbene-related compounds were inducers of phase II detoxifying metabolic enzyme quinone reductase (QR) in the mouse hepatoma Hepa 1c1c7 cells. Among the thirteen compounds tested, several compounds including 3,4,5,3',5'-pentamethoxy-trans-stilbene were found to potentially induce QR activity in this cell line. In addition, substitution with 3-thiofurane ring instead of phenyl ring in the stilbene skeleton also exhibited potential induction of QR activity. This result will give primary information to design the potential inducers of QR activity in the stilbene analogs.
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Citations
The Role of Resveratrol in Cancer Therapy
Jeong-Hyeon Ko,Gautam Sethi,Jae-Young Um,Muthu K. Shanmugam,Frank Arfuso,Alan Prem Kumar,Anupam Bishayee,Kwang Seok Ahn +7 more
TL;DR: The current focus of this review is resveratrol’s in vivo and in vitro effects in a variety of cancers, and intracellular molecular targets modulated by this polyphenol.
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A review of the effects and mechanisms of polyphenolics in cancer.
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DT-diaphorase: a target for new anticancer drugs.
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Resveratrol as an Inhibitor of Carcinogenesis
TL;DR: The current cancer chemopreventive profile of resveratrol provides promise for widespread use in the future, and data from small-scale human trials are necessary prior to drawing any conclusions.
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Quinone reductase induction activity of methoxylated analogues of resveratrol
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TL;DR: Compared to resveratrol, analogues with ortho-methoxy substituents were found to be more potent inducers of QR and to exert their activity in a qualitatively different manner.
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References
Cancer Chemopreventive Activity of Resveratrol, a Natural Product Derived from Grapes
Mei-Shiang Jang,Lining Cai,George Udeani,Karla Slowing,Cathy F. Thomas,Chris Beecher,Harry H. S. Fong,Norman R. Farnsworth,A. Douglas Kinghorn,Rajendra G. Mehta,Richard C. Moon,John M. Pezzuto +11 more
TL;DR: It is suggested that resveratrol, a common constituent of the human diet, merits investigation as a potential cancer chemopreventive agent in humans.
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Anticarcinogenic activities of sulforaphane and structurally related synthetic norbornyl isothiocyanates.
TL;DR: It is reported that sulforaphane and three synthetic analogues, designed as potent phase 2 enzyme inducers, block the formation of mammary tumors in Sprague-Dawley rats treated with single doses of 9,10-dimethyl-1,2-benzanthracene.
754
Direct measurement of NAD(P)H:quinone reductase from cells cultured in microtiter wells: a screening assay for anticarcinogenic enzyme inducers.
TL;DR: A rapid and direct assay of NAD(P)H:(quinone-acceptor) oxidoreductase (EC 1.6.99.2) activity in cultured cells suitable for identifying and purifying inducers of this detoxication enzyme is described.
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•Journal Article
Regulatory mechanisms of monofunctional and bifunctional anticarcinogenic enzyme inducers in murine liver.
Hans J. Prochaska,Paul Talalay +1 more
TL;DR: It is the view that bifunctional inducers bind to the Ah receptor thereby enhancing transcription of genes encoding both AHH and QR, and induction of QR by monofunctionals inducers does not depend on a competent Ah receptor or AHH activity and appears to involve an electrophilic chemical signal.
437
•Journal Article
Chemoprevention of chemically-induced mammary carcinogenesis by indole-3-carbinol.
Clinton J. Grubbs,Vernon E. Steele,Casebolt T,M. Margaret Juliana,Isao Eto,Whitaker Lm,Konstantin H. Dragnev,G J Kelloff,Lubet Rl +8 more
TL;DR: The results support previous studies that indole-3-carbinol can prevent mammary carcinogenesis by direct and indirect acting carcinogens and might be a good candidate for chemoprevention of breast cancer in women.
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