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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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“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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“types has been demonstrated also in many preclinical animal models (Baur and Sinclair, 2006), starting with the seminal work of Pezzuto’s lab in a mouse skin cancer model (Jang et al., 1997).”
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“Resveratrol (trans-3,4′,5-trihydroxystilbene) is a polyphenolic phytoalexin that has been shown to inhibit tumor cell growth (Aziz et al., 2003; Jang et al., 1997).”
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Curcumin Synergizes With Resveratrol to Inhibit Colon Cancer
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“Like curcumin, resveratrol (3,5,4′-trihtdroxy- trans -stilbene), a phytoalexin produced by more than 70 different plant species including grapes and peanuts, has also been shown to inhibit the processes of carcinogenesis at different stages of initiation, promotion, and progression ( 20 , 21 ).”
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“Studies performed in vivo and in vitro have shown that resveratrol exerts pleiotropic effects and can prevent or slow the progression of several pathological conditions, including cardiovascular and metabolic diseases, ischemic brain injuries, and cancer (Jang et al., 1997; Inoue et al., 2003), as well as extend lifes…”
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Self-citationThe Impact of Aqueous Solubility and Dose on the Pharmacokinetic Profiles of Resveratrol
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“... could increase resveratrol solubility to a great extent and HP-β-CD did not change the pharmacokinetic profile of resveratrol after intravenous administration, (2) oral bioavailability of resveratrol was not influenced by the formulation types (solution and suspension), although the suspended dosage form (CMC susp…”
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“(B) Level of expression of the SIRT1 gene evaluated using with Western blot analysis in the following cells: [1] granulosa cells (GCs); [2] cumulus cells in the GV stage (CCs, GV); [3] cumulus cells in the MII stage in the control group (CCs, MII-C); [4] cumulus cells in the MII stage in the resveratrol-treated group…”
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“Jang et al (1997) first reported the chemopreventive role of resveratrol in skin cancer in mice treated with a carcinogen.(10) In SKH-1 hairless mice, topically applied resveratrol showed greater inhi-”
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“For example, both resveratrol and NO possess anti-inflammatory and antiplatelet activities (21, 23) and can exert vasodilatory effects on blood vessels (29).”
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“Resveratrol, found to be linked to the cardiovascular benefits of red wine, has been shown to significantly increase SIRT1 activity through allosteric interaction, resulting in the increase of SIRT1 affinity for both NAD and the acetylated substrate [15, 16].”
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“The molecule has antioxidant and anti-inflammatory properties, and it seems able to inhibit cyclooxygenase and hydroperoxidase activities (4).”
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“The biological activity of resveratrol as an anticarcinogenic and an antioxidant has been reported (Jang et al., 1997).”
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Resveratrol prevents apoptosis in K562 cells by inhibiting lipoxygenase and cyclooxygenase activity
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“It is believed that two glasses of red wine could provide a 10–30 µM concentration of resveratrol in vivo, where most of the pharmacological effects of resveratrol are observed ( 2 ).”
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“Since then resveratrol has been shown to be effective in preventing and delaying the progression of various diseases such as cancer (Jang et al., 1997), cardiovascular disease and glucose intolerance (Timmers et al.”
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“Resveratrol was first found as a potential antitumor agent (21).”
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“Jang et al. (1997) reported that resveratrol inhibited a number of events associated with the initiation, promotion, and progression of cancer.”
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“Resveratrol has received a great deal of attention because it blocks the multistep process of carcinogenesis at various stages: carcinogen activation, tumor initiation, tumor promotion, and tumor progression (Jang et al. 1997).”
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Resveratrol directly targets COX‐2 to inhibit carcinogenesis
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InfluentialPharmacognosy in the 21st century
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“Resveratrol, which also occurs in grapes and red wine, was found to be active as an inhibitor of cyclooxygenase 1, and then to show significant activity in the mouse mammary organ culture assay and in a full-term mouse skin carcinogenesis study (Jang et al 1997).”
BackgroundSelf-citationDietary antiaging phytochemicals and mechanisms associated with prolonged survival
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Postharvest UV-C-Irradiated Grapes as a Potential Source for Producing Stilbene-Enriched Red Wines
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“Resveratrol was found to inhibit tumorigenesis in rodent cancer models (16); to inhibit proliferation and induce apoptosis in several human cancer cells, including B-cell malignancies (17); and to affect a series of critical events associated with tumor initiation and progression, including up-regulation of p53 and p2…”
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Resveratrol transport and metabolism by human intestinal Caco-2 cells
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“Introduction Resveratrol is a naturally-occurring polyphenolic compound with a distinct chemical structure (Figure 1), which has received much attention for its potential preventive actions in human disease (Jang et al 1997; Fre mont 2000; Gusman et al 2001; Wu et al 2001).”
BackgroundTherapeutic and Nutraceutical Potential of Bioactive Compounds Extracted from Fruit Residues
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“Another study conducted by Jang et al. (1997) illustrated that resveratrol, a natural product derived from grapes, inhibited tumor initiation, promotion, and progression.”
BackgroundInfluentialA family of plant-specific polyketide synthases: facts and predictions
Schröder, J. (1997) · Trends in Plant Science · doi:10.1016/s1360-1385(97)87121-x · Cited by 188
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“The chemopreventive activities of resveratrol have been demonstrated in numerous cancers, including hepatocellular [26], colon [27] and breast [28], and occur at all three stages of carcinogenesis: initiation, promotion and progression [29].”
BackgroundResveratrol nanoformulation for cancer prevention and therapy
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“Resveratrol has been shown to inhibit cancer initiation , promotion, and progression in several experimental models (Jang et al, 1997).”
BackgroundResveratrol: A Natural Compound with Pharmacological Potential in Neurodegenerative Diseases
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“The attention came back to resveratrol after 1997, when it was shown that it could have chemopreventive activity [20].”
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“In 1997, a report described the ability of resveratrol to inhibit development of preneoplastic lesions in carcinogen-treated mouse mammary glands in culture and tumorigenesis in a mouse skin cancer model (Jang et al., 1997).”
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Metadata
- 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 (medical) › 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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