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A phytoalexin polyphenolic chemical, resveratrol, can be found in a variety of foods, including cereals, peanuts, grapes, strawberries, and raspberries. It is also known that resveratrol protects the body against cardiovascular diseases as well as various types of cancer. In addition to these health issues, resveratrol is currently the subject of research since it helps treat and prevent a number of illnesses. More clinical research is needed to validate resveratrol's potential as a therapeutic agent, despite the plethora of in vitro and in vivo evidence to support this. When the literature data are evaluated, the fact that resveratrol has a therapeutic effect in these studies, but it is known to be subject to rapid metabolism despite its low bioavailability and oral absorption of approximately 75%, has directed the studies to resveratrol derivatives, especially piceatannol. Based on recent studies, 4 types of resveratrol derivatives were assessed in this work: hydroxylated compounds, methoxylated compounds, glycosides, and oligomers. Because of their advantageous bioactivities, methoxylated, hydroxylated, and halogenated derivatives have drawn the most interest among these classes. However, as a result of these studies, more studies should be conducted to better understand whether resveratrol derivatives can be recommended as therapeutic agents. [ABSTRACT FROM AUTHOR]

Resveratrol (1), a naturally occurring stilbene compound, has been suggested as a potential whitening agent with strong inhibitory activity on melanin synthesis. However, the use of resveratrol in cosmetics has been limited due to its chemical instability and poor bioavailability. Therefore, resveratrol derivatives were prepared to improve bioavailability and anti-melanogenesis activity. Nine resveratrol derivatives including five alkyl ether derivatives with C2H5, C4H9, C5H11, C6H13, and C8H17 (2a-2e) and four ester derivatives with CH3, CH=C(CH3)2, CH(C2H5)C4H9, C7H15 (3a-3d) were newly synthesized and their effect on melanin synthesis were assessed. All the synthetic derivatives efficiently reduced the melanin content in α-MSH stimulated B16F10 melanoma cells. Further investigation showed that the inhibitory effect of 2a on melanin synthesis was achieved not by the inhibition of tyrosinase activity but by the inhibition of melanogenic enzyme expressions such as tyrosinase and tyrosinase-related protein (TRP)-1. Our synthetic resveratrol derivatives have more lipophilic properties than resveratrol by the addition of alkyl or acyl chains to free hydroxyl moiety of resveratrol; thus, they are expected to show better bioavailability in skin application. Therefore, we suggest that our synthetic resveratrol derivatives might be promising candidates for better practical application to skin-whitening cosmetics. [ABSTRACT FROM AUTHOR]

Resveratrol (3,5,4′-trihydroxystilbene; RSV) is a natural nonflavonoid polyphenol present in many species of plants, particularly in grapes, blueberries, and peanuts. Several in vitro and in vivo studies have shown that in addition to antioxidant, anti-inflammatory, cardioprotective and neuroprotective actions, it exhibits antitumor properties. In mammalian models, RSV is extensively metabolized and rapidly eliminated and therefore it shows a poor bioavailability, in spite it of its lipophilic nature. During the past decade, in order to improve RSV low aqueous solubility, absorption, membrane transport, and its poor bioavailability, various methodological approaches and different synthetic derivatives have been developed. In this review, we will describe the strategies used to improve pharmacokinetic characteristics and then beneficial effects of RSV. These methodological approaches include RSV nanoencapsulation in lipid nanocarriers or liposomes, nanoemulsions, micelles, insertion into polymeric particles, solid dispersions, and nanocrystals. Moreover, the biological results obtained on several synthetic derivatives containing different substituents, such as methoxylic, hydroxylic groups, or halogens on the RSV aromatic rings, will be described. Results reported in the literature are encouraging but require additional in vivo studies, to support clinical applications. [ABSTRACT FROM AUTHOR]