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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2008.1
- 수록면
- 336 - 342 (7page)
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The resveratrol analogue piceatannol (3,5,3',4'-tetrahydroxy-trans-stilbene) is a polyphenol present in grapes and wine and reported to have anti-carcinogenic activities. To investigate the mechanism of anticarcinogenic activities of piceatannol, the effects on CYP 1 enzymes were determined in Escherichia coli membranes coexpressing recombinant human CYP1A1, CYP1A2 or CYP1B1 with human NADPH-P450 reductase. Piceatannol showed a strong inhibition of CYP1A1 and CYP1B1 in a concentration-dependent manner, and $IC_{50}$ of human CYP1A1 and CYP1B1 was 5.8 ${\mu}M$ and 16.6 ${\mu}M$, respectively. However, piceatannol did not inhibit CYP1A2 activity in the concentration of up to 100 ${\mu}M$. Piceatannol exhibited 3-fold selectivity for CYP1B1 over CYP1A1. The mode of inhibition of piceatannol was non-competitive for CYP1A1 and CYP1B1. The result that piceatannol did not inhibit CYP1B1-mediated $\alpha$-naphthoflavone ($\alpha$-NF) metabolism suggests piceatannol may act as a non-competitive inhibitor as well. In human prostate carcinoma PC-3 cells, piceatannol induces apoptosis and prevents Aktmediated signal pathway. Taken together, abilities of piceatannol to induce apoptotic cell death as well as CYP1 enzyme inhibition make this compound a useful tool for cancer chemoprevention.
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참고문헌 (36)
참고문헌 신청
Altomare, D. A / 2005 / Perturbations of the AKT signaling pathway in human cancer / Oncogene 24:7455~7464
Aziz, M. H / 2006 / Resveratrol-caused apoptosis of human prostate carcinoma LNCaP cells is mediated via modulation of phosphatidylinositol 3’-kinase/Akt pathway and Bcl-2 family proteins / Mol. Cancer Ther 5:1335~1341
Benistant, C / 2000 / A specific function for phosphatidylinositol 3-kinase alpha (p85 alphap110 alpha) in cell survival and for phosphatidylinositol 3- kinase beta (p85 α-p110 α) in de novo DNA synthesis of human colon carcinoma cells / Oncogene 19:5083~5090
Burke, M. D / 1985 / Ethoxy-, pentoxy- and benzyloxyphenoxazones and homologues: a series of substrates to distinguish between different induced cytochromes P-450 / Biochem. Pharmacol 34:3337~3345
Cecchinato, V / 2007 / Resveratrolinduced apoptosis in human T-cell acute lymphoblastic leukaemia MOLT-4 cells / Biochem. Pharmacol 74:1568~1574
Aziz, M. H / 2006 / Resveratrol-caused apoptosis of human prostate carcinoma LNCaP cells is mediated via modulation of phosphatidylinositol 3’-kinase/Akt pathway and Bcl-2 family proteins / Mol. Cancer Ther 5:1335~1341
Benistant, C / 2000 / A specific function for phosphatidylinositol 3-kinase alpha (p85 alphap110 alpha) in cell survival and for phosphatidylinositol 3- kinase beta (p85 α-p110 α) in de novo DNA synthesis of human colon carcinoma cells / Oncogene 19:5083~5090
Burke, M. D / 1985 / Ethoxy-, pentoxy- and benzyloxyphenoxazones and homologues: a series of substrates to distinguish between different induced cytochromes P-450 / Biochem. Pharmacol 34:3337~3345
Cecchinato, V / 2007 / Resveratrolinduced apoptosis in human T-cell acute lymphoblastic leukaemia MOLT-4 cells / Biochem. Pharmacol 74:1568~1574
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