Anti-inflammatory effect of lipophilic grape seed proanthocyanidin in RAW 264.7 cells and a zebrafish model

• Published in: Journal of functional foods 2020-12, Vol.75, p.104217, Article 104217
• Main Authors: Zhang, Linli, Chen, Jun, Liao, Hejing, Li, Changhong, Chen, Mingshun
• Format: Article
• Language: English
• Subjects: Anti-inflammatory; Lipophilic grape seed proanthocyanidin; RAW 264.7 cells; Zebrafish
• ISSN: 1756-4646; 2214-9414
• DOI: 10.1016/j.jff.2020.104217

[Display omitted] •LGSP suppress the production of NO and pro-inflammatory cytokines in macrophages.•LGSP inhibit the activation of MAPKs and NF-κB signaling pathways.•LGSP reduce the recruitment of neutrophils at the amputation site in zebrafish.•LGSP present better anti-inflammatory effect than GSP in vitro and in vivo. Grape seed proanthocyanidin (GSP), a major polyphenol in grape seed, has several remarkable physiological activities beneficial to human health. However, the hydrophilicity of GSP hampers its cellular absorption and thus limits the bio-efficiency in vivo. In order to enhance the lipophilicity of GSP for improved bio-efficiency, lipophilic grape seed proanthocyanidin (LGSP) was synthesized by enzymatic esterification of GSP. The anti-inflammatory activity of LGSP was evaluated in lipopolysaccharides-stimulated RAW 264.7 cells in vitro and a zebrafish tail-amputated model in vivo. LGSP exhibited strong inhibitory effects on the production of NO and pro-inflammatory cytokines TNF-α, IL-6 and IL-1β in RAW 264.7 cells. Further mechanistic studies showed that LGSP achieved the aforementioned effects by inhibiting the activation of MAPKs and NF-κB signaling pathways. In the zebrafish model, LGSP effectively suppressed the aggregation of neutrophils. Our findings suggest that LGSP may be effective as a complementary agent for the prevention/treatment of inflammation-mediated diseases.