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Inflammation is a complex response of the human organism and relates to the onset of various disorders including diabetes. The current research work aimed at investigating the anti-inflammatory and anti-diabetic effects of ferruginan, a compound isolated from Olea ferruginea. Its in vitro anti-inflammatory activity was determined by using the heat-induced hemolysis assay, while the anti-diabetic effect of the compound was studied by the yeast cell glucose uptake assay. Ferruginan exhibited a maximum of 71.82% inhibition of inflammation and also increased the uptake of glucose by yeast cells by up to 74.96% at the highest tested concentration (100 µM). Moreover, ferruginan inhibited α-amylase dose-dependently, by up to 75.45% at the same concentration. These results indicated that ferruginan possesses promising anti-inflammatory and anti-diabetic properties in vitro, even if at high concentrations. To provide preliminary hypotheses on the potentially multi-target mechanisms underlying such effects, docking analyses were performed on α-amylase and on various molecular targets involved in inflammation such as 5′-adenosine monophosphate-activated protein kinase (AMPK, PDB ID 3AQV), cyclooxygenase (COX-1, PDB ID 1EQG, and COX-2, 1CX2), and tumor necrosis factor alpha (TNF-α, PDB ID 2AZ5). The docking studies suggested that the compound may act on α-amylase, COX-2, and AMPK.