Characterization of Immunological Activities of Peanut Stilbenoids, Arachidin-1, Piceatannol, and Resveratrol on Lipopolysaccharide-Induced Inflammation of RAW 264.7 Macrophages

Abstract

Biological activities of peanut stilbenoids, mainly resveratrol and its derivatives, have attracted increased attention and interest because of peanut being a potent producer and a dietary channel to convey these polyphenols to the human body. As arachidin-1 and piceatannol are structurally close to resveratrol, it is worthy to investigate their immunological activities on inhibition of lipopolysaccharide (LPS)-induced production of PGE2 and NO and mediation of the related transcription factors (NF-kappaB and C/EBP) of RAW 264.7 macrophage cells. Productions of PGE2 and NO were inhibited by all the test stilbenoids in a dose-dependent manner while gene and protein expressions of COX-2 and iNOS were not inhibited. As shown by NF-kappaB-driven luciferase assay, LPS-induced NF-kappaB activities were also reduced by the stilbenoids. In further, when these stilbenoids were subjected to monitoring their inhibitory effectiveness on LPS-induced transcription factor expressions of C/EBPdelta and C/EBPbeta, only C/EBPdelta expressions were reduced. Thus, these stilbenoids were effective in inhibition of PGE2- or NO-mediated inflammation and NF-kappaB- or C/EBPdelta-mediated inflammatory gene expression. In comparison, the highest inhibitory activity on LPS-induced PGE2/NO production, C/EBPdelta gene expression, and NF-kappaB activation was piceatannol which was followed in order by arachidin-1 and resveratrol. The observed anti-inflammatory activities of these peanut stilbenoids are of merit in further consideration for nutraceutical applications.

In Vitro evaluation of the cytotoxic and anti-proliferative properties of resveratrol and several of its analogs

“…In this regard, RES has demonstrated pro-oxidant, genitourinary, immunotoxic, hepatotoxic and genotoxic properties [18][19][20][21][22][23]. PIC, a metabolite of RES, has been reported to induce apoptosis of transformed and primary lymphocytes [17] and to also exhibit cytotoxic actions towards macrophages in vitro [24]. TPS has been found to possess strong apoptosis-inducing properties in leukemia cell lines but not in normal hematopoietic stem cells [14].…”

Evaluation of Resveratrol and Piceatannol Cytotoxicity in Macrophages, T Cells, and Skin Cells

“…To this end, resveratrol is a potent inhibitor of reactive oxygen species produced by zymosanstimulated macrophages, monocytes, and neutrophils (24). Resveratrol and its analogs have also been found to inhibit the production of proinflammatory mediators such as prostaglandins and nitric oxide from stimulated macrophages exposed to endotoxin (25). Whereas these two studies demonstrate how macrophages stimulated with immunogens such as zymosan or endotoxins respond to resveratrol, the response of nonstimulated macrophages to a challenge with this polyphenol remains poorly defined.…”

Discovery of New Stilbene Antioxidants of the Bio-Elicited Peanut Sprout Powder (BPSP) and Longevity Extension of Mice Fed with BPSP-Supplemented Diets

“…Among the test stilbenoids shown in Figure 3, it is of importance to point out that arachidin-1 and arachidin-3 have exhibited considerably higher AOP and antiglycative activities than other stilbenes. As reported, arachidin-1 and arachidin-3 are major stilbenes of BPSP and bear potent antioxidant and anti-inflammatory activities have been demonstrated [8] [23]. In further, a broad spectrum of potent biological activities of arachidin-1 has been demonstrated [4] [28].…”

“…Biosynthesis of peanut stilbenes could be remarkably enhanced by subjecting kernels to germination and wound-stress elicitation [8]. The isolated peanut stilbenes, such as arachidin-1, have exhibited potent anti-inflammatory and anti-cancer along with anti-oxidant activities [8] [23] [24] [26]. In a recent report, arachidin-1 and resveratrol exhibit phytoestrogenic activities and modulate regulatory T cell functions responsible for successful aging of the aged ICR mice [28].…”