Cancer chemopreventive activity of resveratrol, a natural product derived from grapes
Abstract
Resveratrol, a phytoalexin found in grapes and other food products, was purified and shown to have cancer chemopreventive activity in assays representing three major stages of carcinogenesis. Resveratrol was found to act as an antioxidant and antimutagen and to induce phase II drug-metabolizing enzymes (anti-initiation activity); it mediated anti-inflammatory effects and inhibited cyclooxygenase and hydroperoxidase functions (antipromotion activity); and it induced human promyelocytic leukemia cell differentiation (antiprogression activity). In addition, it inhibited the development of preneoplastic lesions in carcinogen-treated mouse mammary glands in culture and inhibited tumorigenesis in a mouse skin cancer model. These data suggest that resveratrol, a common constituent of the human diet, merits investigation as a potential cancer chemopreventive agent in humans.
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Resveratrol has anticancer properties.
“The scientific interest in resveratrol dates back to 1997 when studies on animal models demonstrated its anticancer properties [7].”
From The Role of Resveratrol Administration in Human Obesity (2021) · cites this paper as [7]
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BackgroundAdministration of resveratrol: What formulation solutions to bioavailability limitations?
Amri, A., Chaumeil, J. C., Sfar, S., & Charrueau, C. (2011) · Journal of Controlled Release · doi:10.1016/j.jconrel.2011.09.083 · Cited by 622 · see citing works
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“Another anticarcinogenic study conducted by Jang et al .”
Solid‐phase microextraction: a powerful sample preparation tool prior to mass spectrometric analysis
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“[17] reported that resveratrol has a number of biological activities that are consistent with cancer chemoprevention and that the agent can inhibit carcinogenesis in experimental animals.”
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Shimada, T. (2006) · Drug Metabolism and Pharmacokinetics · doi:10.2133/dmpk.21.257 · Cited by 606 · see citing works
Resveratrol and health—A comprehensive review of human clinical trials
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“Resveratrol further inhibits cyclooxygenases [19], and could therefore act through some of the same mechanisms as aspirin.”
BackgroundCancer Chemoprevention Through Dietary Antioxidants: Progress and Promise
Khan, N., Afaq, F., & Mukhtar, H. (2007) · Antioxidants and Redox Signaling · doi:10.1089/ars.2007.1740 · Cited by 592 · see citing works
“According to their study, resveratrol significantly reduced the number of tumors per mouse in a two-stage skin carcinogenesis model (120).”
Polyphenols: do they play a role in the prevention of human pathologies?
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Resveratrol, Pterostilbene, and Piceatannol in Vaccinium Berries
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“Among the myriad of plant natural products, compounds issuing from the phenylpropanoid pathway (Figure 1) have been reported to have antioxidant effects, estrogen-like and vasodilatation activities, and anti-inflammatory and anticancer chemopreventive action (Jang et al., 1997; Kahkonen et al., 1999; Burns et al., 200…”
BackgroundInfluentialPerspectives for Cancer Prevention With Natural Compounds
Amin, A. R. M. R., Küçük, Ö., Khuri, F. R., & Shin, D. M. (2009) · Journal of Clinical Oncology · doi:10.1200/jco.2008.20.6235 · Cited by 568 · see citing works
Sirtuins: Sir2-related NAD-dependent protein deacetylases.
North, B. J., & Verdin, E. M. (2004) · Genome biology · doi:10.1186/gb-2004-5-5-224 · Cited by 568 · see citing works
Plant-derived anticancer agents
Pezzuto, J. M. (1997) · Biochemical Pharmacology · doi:10.1016/s0006-2952(96)00654-5 · Cited by 564 · see citing works
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“Examples include the inhibition of cyclooxygenases (Jang et al., 1997), PI 3 kinase (PozoGuisado et al.”
BackgroundInfluentialOxidative stress and dietary phytochemicals: Role in cancer chemoprevention and treatment
Chikara, S., Nagaprashantha, L. D., Singhal, J., Horne, D. A., Awasthi, S., & Singhal, S. S. (2017) · Cancer Letters · doi:10.1016/j.canlet.2017.11.002 · Cited by 561 · see citing works
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“Resveratrol has antioxidant, anti-inflammatory and anticarcinogenic properties [34,128,129].”
Cancer Prevention and Treatment with Resveratrol: From Rodent Studies to Clinical Trials
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“(12), the first animal study of the chemopreventive effects of resveratrol was reported in a two-stage mouse skin carcinogenesis model.”
BackgroundIMPROVING THE NUTRIENT COMPOSITION OF PLANTS TO ENHANCE HUMAN NUTRITION AND HEALTH
Grusak, M. A., & DellaPenna, D. (1999) · Annual Review of Plant Physiology and Plant Molecular Biology · doi:10.1146/annurev.arplant.50.1.133 · Cited by 530 · see citing works
“These include flavonoids, flavones, phytosterols, phenols and polyphenols, phytoestrogens, glucosinolates, and indoles, to name but a few (11, 27, 33, 37, 69, 82, 152).”
BackgroundWang, H., Khor, T., Shu, L.-M., Su, Z.-C., Fuentes, F., Lee, J.-H., & Kong, A. (2012) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/187152012803833026 · Cited by 532 · see citing works
“Jang et al reported cancer chemopreventive activity of resveratrol [164].”
Resveratrol Acts as a Mixed Agonist/Antagonist for Estrogen Receptors α and β*
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“It is further supported by the results of our recent study of the relation between beer, wine, and spirits and cancer of the upper digestive tract (41), although these cancers are rare.”
ResultResveratrol and cancer: focus on in vivo evidence
Carter, L. G., D'Orazio, J. A., & Pearson, K. J. (2014) · Endocrine Related Cancer · doi:10.1530/erc-13-0171 · Cited by 523 · see citing works
“After Jang et al .”
Health benefits of resveratrol: Evidence from clinical studies
Singh, A. P., Singh, R., Verma, S. S., Rai, V., Kaschula, C. H., Maiti, P., & Gupta, S. C. (2019) · Medicinal Research Reviews · doi:10.1002/med.21565 · Cited by 523 · see citing works
“Since its identification in 1939, resveratrol’s pleiotropic activities have been reported in a number of studies.(3,257) However, most of these discussions are based on preclinical work.”
BackgroundResveratrol: from grapevines to mammalian biology
Pervaiz, S. (2003) · The FASEB Journal · doi:10.1096/fj.03-0168rev · Cited by 518 · see citing works
“Results indicated that the presence of RSV prevented the activation of NF- B triggered by exposure of these cell types to TNF, PMA, H2O2, LPS, okadaic acid, and ceramide (15).”
BackgroundInfluentialTsai, S., Lin‐Shiau, S., & Lin, J. (1999) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0702357 · Cited by 512 · see citing works
Biological Effects of Resveratrol
Bhat, K., Kosmeder, J. W., & Pezzuto, J. M. (2001) · Antioxidants and Redox Signaling · doi:10.1089/152308601317203567 · Cited by 510 · see citing works
“Resveratrol has been shown to in-BHAT hibit the activity of the COX-1 enzyme derived from sheep seminal vesicles (68, 112).”
InfluentialSelf-citationXia, C., Meng, Q., Liu, L.-Z., Rojanasakul, Y., Wang, X., & Jiang, B. (2007) · Cancer Research · doi:10.1158/0008-5472.can-07-0783 · Cited by 508 · see citing works
Resveratrol for cancer therapy: Challenges and future perspectives
Ren, B., Kwah, M. X.-Y., Liu, C., Ma, Z., Shanmugam, M. K., Ding, L., Xiang, X., Ho, P. C., Wang, L., Ong, P. S., et al. (2021) · Cancer Letters · doi:10.1016/j.canlet.2021.05.001 · Cited by 505 · see citing works
Resveratrol: a review of plant sources, synthesis, stability, modification and food application
Tian, B., & Liu, J. (2019) · Journal of the Science of Food and Agriculture · doi:10.1002/jsfa.10152 · Cited by 500 · see citing works
Waterhouse, A. L. (2002) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.2002.tb02903.x · Cited by 494 · see citing works
Resveratrol as an anticancer nutrient: molecular basis, open questions and promises
Signorelli, P., & Ghidoni, R. (2005) · The Journal of Nutritional Biochemistry · doi:10.1016/j.jnutbio.2005.01.017 · Cited by 493 · see citing works
“Resveratrol noncompetitively inhibited both the COX and hydroperoxidase activities of COX1 in vitro [13,89].”
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Cancer Prevention With Natural Compounds
Gullett, N. P., Amin, A. R. M. R., Bayraktar, S., Pezzuto, J. M., Shin, D. M., Khuri, F. R., Aggarwal, B. B., Surh, Y., & Küçük, Ö. (2010) · Seminars in Oncology · doi:10.1053/j.seminoncol.2010.06.014 · Cited by 490 · see citing works
Self-citationImproving industrial yeast strains: exploiting natural and artificial diversity
Steensels, J., Snoek, T., Meersman, E., Nicolino, M. P., Voordeckers, K., & Verstrepen, K. J. (2014) · FEMS Microbiology Reviews · doi:10.1111/1574-6976.12073 · Cited by 486 · see citing works
“Resveratrol is a compound that, apart from its antifungal characteristics, has been proposed to reduce the risk of cancer and coronary heart disease (Jang et al., 1997; Becker et al., 2003).”
BackgroundMarier, J., Vachon, P., Gritsas, A., Zhang, J., Moreau, J., & Ducharme, M. P. (2002) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.102.033340 · Cited by 480 · see citing works
“Finally, trans-resveratrol was shown to have cancer chemoprotective properties and to induce apoptosis in leukemia and human breast carcinoma (Jang et al., 1997; Mgbonyebi et al., 1998; Lu and Serrero, 1999).”
BackgroundTargeting NOX, iNOS and COX-2 in inflammatory cells: chemoprevention using food phytochemicals
Murakami, A., & Ohigashi, H. (2007) · International Journal of Cancer · doi:10.1002/ijc.23161 · Cited by 478 · see citing works
“Resveratrol is a well-known compound that regulates both COX-1 and COX-2.”
BackgroundThe molecular targets of resveratrol
Kulkarni, S. S., & Cantó, C. (2015) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2014.10.005 · Cited by 477 · see citing works
Cyclooxygenase-2 and carcinogenesis
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Functional foods: their role in disease prevention and health promotion
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- Authors
- Jang, M., Cai, L., Udeani, G. O., Slowing, K. V., Thomas, C. F., Beecher, C. W. W., Fong, H. H. S., Farnsworth, N. R., Kinghorn, A. D., Mehta, R. G., Moon, R. C., & Pezzuto, J. M.
- Affiliations
- University of Illinois Chicago (US)
- Universidad Complutense de Madrid (ES)
- M. Jang, L. Cai, C. W. W. Beecher, H. H. S. Fong, N. R. Farnsworth, A. D. Kinghorn, J. M. Pezzuto, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA.
- Corresponding author
- Cai, Lining
- Pezzuto, John M.
- Venue
- Science
- Published
- 1997-01-10
- Volume
- 275
- Issue
- 5297
- Pages
- 218-220
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2151089147
- Cited by
- 4,935
- References
- 33
- Citations by year
- 2026: 45 · 2025: 75 · 2024: 105 · 2023: 95 · 2022: 148 · 2021: 166 · 2020: 179 · 2019: 168 · 2018: 181 · 2017: 202 · 2016: 179 · 2015: 222 · 2014: 225 · 2013: 264 · 2012: 252
- FWCI
- 96.50
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Science (publishedVersion)
- Funders
- National Cancer Institute (P01CA048112)
- Topics
- Health Sciences › Medicine › Geriatrics and Gerontology › Sirtuins and Resveratrol in Medicine
- Health Sciences › Medicine › Biochemistry › Phytochemicals and Antioxidant Activities
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics, phytochemicals, and oxidative stress
- Keywords
- resveratrol, chemoprevention, phytoalexins, grapes, antioxidant activity, antimutagenic activity, phase II enzymes, anti-inflammatory activity, cyclooxygenase inhibition, mammary carcinogenesis, precancerous lesions
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