title: Development of inhibitors against lipase and alpha-glucosidase from derivatives of monascus pigment.
abstract: New derivatives of monascus pigment were produced during Monascus fermentation by the addition of unnatural amino acids, and the inhibitory activities of the derivatives against diet-related lipase and alpha-glucosidase were tested. Derivatives with penicillamine (H-Pen), cyclohexylalanine (H-Cha), butylglycine (L-t-Bg), and norleucine (H-Nle) showed relatively high inhibitory activities against lipase. The H-Pen derivative exhibited the highest inhibitory activity, with an IC(50) (50% inhibition) value of 24.0 microM. The four derivatives all showed noncompetitive inhibition patterns against lipase. The inhibition constant (K(i)) of the H-Pen derivative was estimated to be 20.7 microM. The H-Pen derivative also exhibited a relatively high inhibitory activity against alpha-glucosidase, with an IC(50) value of 50.9 microM. The inhibition pattern of the H-Pen derivative against alpha-glucosidase appeared to be of a mixed type. The inhibition constants K(i) and were estimated to be 25.9, and 98.9 microM, respectively.
authors.affiliation: Department of Biotechnology, College of Engineering, Yonsei University, Seoul, South Korea.
authors.forename: Jong Hoon
authors.initials: JH
authors.lastname: Kim
authors.forename: Hyun Jung
authors.initials: HJ
authors.lastname: Kim
authors.forename: Hae Woong
authors.initials: HW
authors.lastname: Park
authors.forename: Sung Hun
authors.initials: SH
authors.lastname: Youn
authors.forename: Duck-Young
authors.initials: DY
authors.lastname: Choi
authors.forename: Chul Soo
authors.initials: CS
authors.lastname: Shin
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors; D020128:Inhibitory Concentration 50; D008049:Lipase / Q000037:antagonists & inhibitors*; D032741:Monascus / Q000737:chemistry / Q000378:metabolism*; D009646:Norleucine / Q000378:metabolism; D010396:Penicillamine / Q000378:metabolism; D010649:Phenylalanine / Q000031:analogs & derivatives / Q000378:metabolism; D010860:Pigments, Biological / Q000737:chemistry / Q000302:isolation & purification / Q000502:physiology*
chemical_list: D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D010860:Pigments, Biological; C028544:cyclohexylalanine; D010649:Phenylalanine; D009646:Norleucine; D008049:Lipase; D010396:Penicillamine