Bioactive compounds from Octopus vulgaris ink extracts exerted anti-proliferative and anti-inflammatory effects in vitro

• Published in: Food and chemical toxicology 2021-05, Vol.151, p.112119, Article 112119
• Main Authors: Hernández-Zazueta, Martín S., Luzardo-Ocampo, Iván, García-Romo, Joel S., Noguera-Artiaga, Luis, Carbonell-Barrachina, Ángel A., Taboada-Antelo, Pablo, Campos-Vega, Rocío, Rosas-Burgos, Ema Carina, Burboa-Zazueta, María G., Ezquerra-Brauer, Josafat M., Burgos-Hernández, Armando
• Format: Article
• Language: English
• Subjects: Anti-proliferative effect; Colorrectal cancer; Cytokine modulation; Ink; Metabolomic analysis; Octopus (Octopus vulgaris)
• ISSN: 0278-6915; 1873-6351
• DOI: 10.1016/j.fct.2021.112119

Underutilized marine food products such as cephalopods’ ink could be sources of bioactive compounds providing health benefits. This study aimed to assess the anti-proliferative and anti-inflammatory effects from Octopus vulgaris ink extracts (hexane-, ethyl acetate-, dichloromethane- (DM), and water extracts) using human colorectal (HT-29/HCT116) and breast (MDA-MB-231) cancer cells, and LPS-challenged murine RAW 264.7 cells. Except by ethyl-acetate, all of the extracts exhibited anti-proliferative effects without being cytotoxic to ARPE-19 and RAW 264.7 cells. Among DM fractions (F1/F2/F3), DM-F2 showed the highest anti-proliferative effect (LC50 = 52.64 μg/mL), inducing pro-apoptotic morphological disruptions in HCT116 cells. On RAW 264.7 cells, DM-F2 displayed the lowest nitrites reduction and up-regulation of key-cytokines from the JAK-STAT, PI3K-Akt, and IL-17 pathways. Compared to control, DM-F2 increased IL-4 and decreased NF-κB fluorometric expression in peripheral blood mononuclear cells (PBMCs). Metabolomic analysis of DM-F2 highlighted hexadecanoic acid and 1-(15-methyl-1-oxohexadecyl)-pyrrolidine as the most important metabolites. These compounds also exhibited high in silico binding affinity (−4.6 to −5.8 kcal/mol) to IL-1α, IL-1β, and IL-2. Results suggested the joint immuno-modulatory and anti-proliferative effect derived from selected compounds of underutilized marine food products such as ink. This is the first report of such biological activities in extracts from O. vulgaris ink. [Display omitted] •The biological activity of O. vulgaris ink (OI) extracts was evaluated.•OI dichloromethane extract (DM) displayed the highest anti-proliferative effect.•A DM-fraction (DM-F2) showed the highest nitrite reduction on RAW 264.7 cells.•DM and DM-F2 metabolomic analysis underlined fatty acid biosynthetic pathways.•TLR4/NF-κB, JAK-STAT, and MAPK pathways were modulated by DM-F2.