Delivery Strategies and Formulation Approaches of Anticancer Nutraceuticals
Sheeba Varghese Gupta, Yashwant V. Pathak in Advances in Nutraceutical Applications in Cancer, 2019
Resveratrol is a natural phenol produced by many fruits and plants such as grapes, blueberries, raspberries, and peanuts with antiproliferative activity due to its role as a plant antibiotic. It is believed to possess multiple bioactivities including anticancer, anticarcinogenesis, and anti-inflammatory effects [31]. In vivo studies have shown protective effects of resveratrol against several types of cancers, such as breast, skin, gastric, colon, prostate, and pancreatic, by interfering with multiple stages of carcinogenesis [32]. Clinical trials have established the safety and potential anticancer effects of resveratrol as both a single agent and a constituent of foods [33]. A phase I pilot study conducted in colorectal cancer patients (women with high risk for developing breast cancer) to determine the anticancer effects of freeze-dried grape powder containing a low dose of resveratrol in combination with other bioactive components suggested that dietary intake of the dry grape powder inhibited the Wnt signaling pathway in the colon, demonstrating the suppression of carcinogenesis [34]. Despite several clinical trials, pharmacokinetics studies of resveratrol have shown poor bioavailability (only 1%) due to extensive glucuronidation and sulfation as well as metabolism by gut bacterial enzymes [35].
Herbal Drug Discovery Against Inflammation: From Traditional Wisdom to Modern Therapeutics
Amit Baran Sharangi, K. V. Peter in Medicinal Plants, 2023
A polyphenolic compound hydroxytyrosol, from extra virgin olive oil, exhibits strong anti-inflammatory activity by improvement in a model of DSS-induced colitis (Sánchez et al., 2015). Resveratrol mainly present in grapes, wine, and peanut products, etc., is a polyphenolic stilbene which occurs in cis or trans configuration. Laboratory studies on animals, human cultured cells suggest that it possess therapeutic potential as anti-inflammatory, anti-carcinogenic, anti-oxidants which may further prove relevant for the treatment of chronic diseases (Smoliga, Baur, and Hausenblas, 2011). Another important flavonol, kaempferol [3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one] has a wide range of pharmacological activities, including antioxidant, anti-inflammatory, anticancer, cardioprotective, neuroprotective, antiallergic, and antidiabetic (Somani et al., 2015).
Emerging Highlights on Natural Prodrug Molecules with Multifarious Therapeutic Perspectives
Debarshi Kar Mahapatra, Cristóbal Noé Aguilar, A. K. Haghi in Applied Pharmaceutical Practice and Nutraceuticals, 2021
Resveratrol (trans-3, 5, 4-trihydroxystilbene), a plant-derived polyphenolic phytoalexin found in grapes, wine, peanuts, and cranberries has been said to have anticarcinogenic, antioxidative, phytoestrogen, platelet aggregation, and coagulation, modifies eicosanoid synthesis, modulate lipoprotein mechanisms, and cardioprotective activities.55,56 Resveratrol has also proven to increase the lifespan of evolutionarily distant species which include S. cerevisiae, C. elegans, and D. melanogaster in a Sir2-dependent manner.57 The scientific study reported that trans-resveratrol has health benefits including anticarcinogenic effects and protection against cardiovascular disease as well as in Alzheimer’s disease.58,59 The phytochemical additionally play a crucial role in the cellular response by modulating the enzymes concerned with the stress response, which include quinone reductase 2 (QR2), a cytosolic enzyme that facilitates the production of damage-activated quinone and reactive oxygen species (ROS).60 Resveratrol is like a phytoestrogen and has some structural similarity to diethylstilboestrol. But, it has a more affinity for the estrogen receptor-β (ER-β) than α and transcriptionally activates ER-β at small concentrations.61,62
Cancer prevention and treatment using combination therapy with natural compounds
Published in Expert Review of Clinical Pharmacology, 2020
Resveratrol (3,4,5-trihydroxystilbene) belongs to a class of polyphenolic compounds termed stilbenes that have strong antioxidant properties [23]. Certain plants produce resveratrol and other stilbenes in response to stress, injury, fungal infection or UV radiation [24]. Resveratrol, a fat soluble compound that is present in trans and cis configurations, is found in plant derived foods including grape skin, red wine, purple grape juice, peanuts and some berries. Resveratrol has been reported to have a multitude of anticancer properties through its ability to influence extracellular growth factors and receptor tyrosine kinases, leading to increased apoptosis, alterations in inflammation, immune surveillance and hormone signaling [25]. 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]. Resveratrol seems to be well tolerated although little information is available on its long term administration [30]. For use in chronic diseases such as cancer, resveratrol administration would occur over months to years. As such, long term toxicity studies should be conducted before chronic administration is recommended.
Encapsulation of Nutraceutical Ingredients in Liposomes and Their Potential for Cancer Treatment
Published in Nutrition and Cancer, 2018
Sayantani Dutta, Jeyan Arthur Moses, C. Anandharamakrishnan
Resveratrol (trans-3,4′,5-trihydroxystilbene) is a natural polyphenol commonly found in fruits, vegetables, and medicinal plants such as grapes, nuts, and polygonum roots (22). Resveratrol has been particularly studied in the past for its antioxidant, anti-inflammatory, anti-diabetic, anti-cancer, and neuro-protective activities (23). Wang et al. (24) have formulated mitochondria targeting resveratrol liposomes to combat the MDR nature of cancer cells, by targeting the ‘mitochondria apoptosis pathway’. As reported, liposomes were formulated with dequlinium-polyethylene glycol di-stearoyl phosphatidyl ethanol amine (DQA-PEG2000-DSPE) conjugate (lipids:drug = 20:1). The authors also prepared mitochondria targeting coumarin liposomes that worked as fluorescence probe in ‘laser confocal microscopy’, to ensure the reach of mitochondria targeting liposomes to the site, i.e., mitochondria of cancerous cells.
Preparation, characterization and antimicrobial activity evaluation of electrospun PCL nanofiber composites of resveratrol nanocrystals
Published in Pharmaceutical Development and Technology, 2020
Resveratrol is a most commonly found compound in grape skins and seeds. It shows its antioxidant effect by removing free radicals and bonding metal ions. Resveratrol is known to be effective in metabolic syndrome, chronic inflammation, cancer, neurodegenerative diseases, blood-sugar stabilization, and obesity (Nakata et al. 2012; Moshawih et al. 2019). It also has antiviral, antimicrobial and wound healing effects when administered topically. Resveratrol has anti-inflammatory effect and antimicrobial properties against P. acnes in acne treatment (Ahmad et al. 2005; Chachay et al. 2011). Hence, it is a new therapeutic alternative to acne treatment and can be more effective than currently available commercialized products (Docherty et al. 2007). The efficacy of resveratrol in the treatment of acne varies depending on the dose administered. In vivo studies have shown that topical resveratrol reduces lesions (Docherty et al. 2004). The solubility of resveratrol in water is very low and is easily affected by heat. Chemical structure of resveratrol is 3,4,5 trihydroxystylbene and has two isomers: trans and cis. Biological activities of trans isomers are higher than cis isomers (Bradamante et al. 2004). In order to increase the dermal permeation of resveratrol, both the stability of the trans form and the solubility in water need to be increased (Scognamiglio et al. 2013).