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.