Development of lipase inhibitors from various derivatives of monascus pigment produced by Monascus fermentation

Derivatives of monascus pigment having high lipase-inhibitory activities were developed and characterized. Various derivatives of monascus pigment were produced during Monascus fermentation with added l-, d-amino acids. From them, compounds having high inhibitory activities against a porcine pancreatic lipase were selected. Monascus pigments produced with aromatic and non-polar aliphatic l-, d-amino acids revealed strong inhibitory activities against the lipase. l-Trp and d-Tyr derivatives showed especially low IC₅₀ values of 61.2 and 103 μM, respectively. Further structure modifications of pigment derivatives were made with amino acid esters and dipeptides for enhanced inhibitory activity. l-Leu-OEt and l-Tyr-OEt derivatives made via further structure modifications showed high lipase-inhibitory activities with IC₅₀ values of 12.2 and 13.8 μM, respectively. The l-Leu-OEt derivative exhibited some specificity against porcine pancreatic lipase but not exhibit high activities against other digestive enzymes. Some compounds were developed from modification of monascus pigment followed by lipase-inhibitory activity tests.