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The Treatment of Hypertension with Nutrition, Nutritional Supplements, Lifestyle and Pharmacologic Therapies
Published in Stephen T. Sinatra, Mark C. Houston, Nutritional and Integrative Strategies in Cardiovascular Medicine, 2022
Resveratrol administration to humans reduces augmentation index, improves arterial compliance and lowers central arterial pressure when administered as 250 mL of either regular or dealcoholized red wine [226–230]. Aortic augmentation index fell by 6.1% with the dealcoholized red wine and by 10.5% with regular red wine, central arterial pressure was reduced with dealcoholized red wine by 7.4 and with regular red wine by 5.4 mmHg. Resveratrol increases flow-mediated vasodilation in a dose-related manner, improves ED, prevents uncoupling of eNOS, and blocks the effects of angiotensin II [226–230]. The recommended dose is 250 mg/day of trans-resveratrol [2–5,228].
Resveratrol-Loaded Phytomedicines for Management of Cancer
Published in Mahfoozur Rahman, Sarwar Beg, Mazin A. Zamzami, Hani Choudhry, Aftab Ahmad, Khalid S. Alharbi, Biomarkers as Targeted Herbal Drug Discovery, 2022
Shakir Saleem, Ruqaiyah Khan, Sandeep Arora
The trans-isoform is the major isoform ofresveratrol and is also extensively studied for several pharmacological actions. Trans-isoform is transformed into cis isoform on exposure to heat and ultraviolet radiation. Resveratrol has been classed as a phytoestrogen as its structure is like that of the synthetic estrogen diethylstilbestrol. Its biological sources are very common as, resveratrol is easily available in common food items and augments health in ways similar to viniferins, pterostilbene, and piceid (Jeandet et al., 2002). More-over, few semi-synthetic resveratrol analogs were found to have specific pharmacological benefits like chemopreventive actions (Cai et al., 2004), antioxidant effects (Colin et al., 2008) and anti-aging properties (Moran et al., 2009). It had also been reported that resveratrol can reverse the resistance to some drugs in different types and sizes of a tumor by over-sensitizing them to chemotherapeutic agents (Mondal et al., 2016; Lee et al., 2016). Many pharmacological effects have been elucidated by the trans-resveratrol and its glucoside including cardio-protective, anti-oxidative, anti-inflammatory, estrogenic, and anti-estrogenic, and anti-tumor activities (Stagos et al., 2012; Carter et al., 2014). Additionally, the antimicrobial action (Stagos et al., 2012) of trans-resveratrol was reported to be useful in the management of cognitive impairments like dementia (Mazzanti et al., 2016; Molino et al., 2016).
Emerging Highlights on Natural Prodrug Molecules with Multifarious Therapeutic Perspectives
Published in Debarshi Kar Mahapatra, Cristóbal Noé Aguilar, A. K. Haghi, Applied Pharmaceutical Practice and Nutraceuticals, 2021
Mojabir Hussen Ansari, Vaibhav Shende, Debarshi Kar Mahapatra
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
Development of self-microemulsifying lipid-based formulations of trans-resveratrol by systematically constructing lipid-surfactant-water phase diagrams using long-chain lipids
Published in Drug Development and Industrial Pharmacy, 2021
Carolina Aloisio, Ankita V. Shah, Marcela Longhi, Abu T. M. Serajuddin
Based on phase diagrams and the drug solubility, formulations with 6:4 to 4:6 lipid-surfactant mixtures corresponding to Systems D and F were selected for further studies, in which trans-resveratrol was dissolved such that the concentrations were kept at about 80% of saturation solubility. Compositions of the formulations are given in Table 3(A). Although the drug solubility was lower at the higher lipid to surfactant ratio, all three combinations were selected as it was also of importance to investigate the performance of the formulations in the dispersion test. The dietary supplements for trans-resveratrol are supplied as 20-50 mg doses [37]. Table 3(A) shows that the development of a suitable lipid-based formulation using long-chain lipids to provide such a dose is feasible.
Can the cavi-precipitation process be exploited to generate smaller size drug nanocrystal?
Published in Drug Development and Industrial Pharmacy, 2021
Biswadip Sinha, Rainer H. Müller, Jan P. Möschwitzer
trans-Resveratrol (RVT) [E.Denk Feinchemie GmbH, Munich, Germany] was used in this study. HPLC Grade organic solvents such as methanol, isopropanol (IPA), acetone, tertrahydrofuran (THF), dimethylformamide (DMF) were purchased from VWR International (Leuven, Belgium). Analytical grade Ethanol and dimethylsulfoxide (DMSO) were purchased from Merck Schuchardt OHG (Hohenbrunn, Germany). Sodium dodecyl sulfate (SDS) and polyvinylpyrrolidone MW 40,000 (PVPK40) were purchased from Sigma-aldrich chemie GmbH (Steinheim, Germany) and used as stabilizers in the aqueous phase. Organic phase stabilizers such as Labrafac lypophile, Labrafac PG, Labrafil M1944 CS, Labrafil M2130 CS, and Brij 52 were received as a gift sample from Gattefosse SAS (Cedex, France). Plantacare 2000 UP was purchased from Cognis GmbH (Dusseldorf, Germany). Poloxamer 188 (Lutrol F68®, BASF, Ludwigshafen, Germany), sorbitan mono-oleate (Span 80), and sorbitan mono-laurate (Span 20) (Sigma-aldrich chemie GmbH (Steinheim, Germany) were the other stabilizers used in the study. MilliQ grade water (MQ Water) from a Milli-Q PLUS system (Millipore GmbH, Germany) was used whenever required.
Neuroprotection by trans-resveratrol against collagenase-induced neurological and neurobehavioural deficits in rats involves adenosine A1 receptors
Published in Neurological Research, 2020
Noor Azliza Wani Abd. Aziz, Igor Iezhitsa, Renu Agarwal, Roqiah Fatmawati Abdul Kadir, Azian Abd. Latiff, Nafeeza Mohd Ismail
Trans-resveratrol (3,5,4ʹ-trihydroxy-trans-stilbene) is a natural phenol produced by several plants in response to environmental stress, including injury and extended drought-like conditions [30]. It has been used as a dietary supplement, but there is no clear evidence of its beneficial effects on human health. The fundamental mechanisms of its action are linked to its structural similarity to the amino acid tyrosine due to the presence of the phenolic ring [31]. In terms of neuroprotective properties, trans-resveratrol has been reported to have pleiotropic effects including anti-inflammatory [7,32,33], anti-oxidative [34,35], and anti-apoptotic activities [36,37]. To date, several translational studies on trans-resveratrol in human participants have reported major issues related to its low bioavailability [38–40]. Although it is lipophilic and is capable of crossing the blood–brain barrier, trans-resveratrol is rapidly metabolized by the liver upon administration before it reaches the brain. Current approaches to enhance its bioavailability include combining its administration with other phenolic compounds to increase its absorption [41], developing prodrugs to produce high levels of active trans-resveratrol [42], and producing nano-formulations to improve its transport across the plasma membrane [43]. Considering its rapid metabolism, in the present study, trans-resveratrol was injected intracerebroventricularly in rats to allow its delivery close to potential target for neuroprotection in ICH.