Synthetic Resveratrol Derivatives and Their Biological Activities: A Review

Abstract

Resveratrol, a naturally derived stilbene that exists in various foods and beverages, has attracted extensive exploration due to its multiple biological activities, such as anticancer, antioxidant, cardiovascular protection, anti-inflammatory, antiviral, chemopreventive effect, neuroprotective effect, immunomodulation and so on. However, owing to its poor oral bioavailability, the application of resveratrol is greatly restricted. Because of that, a large amount of efforts had been made by researchers on designing its derivatives to obtain compounds with improved efficiency and low toxicity for developing more active drugs for clinical application. In this report, we review the current development of studying on resveratrol derivatives including their properties and activities. Additionally, this article also presents the synthetic routes of correlative resveratrol derivatives.

Resveratrol and inflammatory bowel disease

“…Hence, inhibition of oxidative stress and inflammation have been a focus of investigation of antioxidants, especially phytochemicals, in experimental therapies of IBD . Resveratrol ( trans ‐3,5,4′‐trihydroxy‐stilbene) has demonstrated antioxidative and anti‐inflammatory activity . A stilbene found in certain foods, including red wine, grapes, mulberries, peanuts, and many other fruits and plants, resveratrol has been shown to effectively reduce tissue MDA levels and MPO activity; increase SOD, GPx, and catalase (CAT) activities; and suppress the expression of tumor necrosis factor α (TNF‐α), interleukin (IL)‐8, interferon‐γ (IFN‐γ), and other inflammatory biomarkers in a murine model of UC .…”

Bile Acid Conjugates with Anticancer Activity: Most Recent Research

“…Cholic and deoxycholic acid amides were conjugated with a series of amino-substituted α-cyanostilbene derivatives, and their anticancer activity was evaluated against the human osteosarcoma (HOS) cancer cell line [51]. α-Cyanostilbenes are usually considered as resveratrol analogs, displaying good anticancer activity against a range of cancer cell line [56]. For the synthesis of hybrid compounds, α-cyanostilbenes were prepared with 80-85% overall yields by Knoevenagel condensation between 2-(4-nitrophenyl) acetonitrile and various aldehydes with catalityc amounts of piperidine, followed by reduction of the nitro group (Scheme 9).…”

Strategies to Improve Resveratrol Systemic and Topical Bioavailability: An Update

“…From a structural point of view, RSV prodrugs maintain the 3,5,4′-trihydroxystilbene skeleton in their structure and possess suitable promoiety on the phenolic hydroxyls (Figure 2) [64]. Differently, RSV analogs are derivatives obtained by structural modification on the trans -stilbene core, for example, modification of the double bond or of the benzene ring, phenyl ring substitutions with halogens or other substituents (Figure 2) [62,65,66,67]. Due to the tremendous amount of publications regarding the trans -RSV derivatives and the specific scope of this review, here we mainly focus on the description of RSV prodrugs and technological approaches involving RSV incorporation into different delivery systems.…”