Development of inhibitors against lipase and alpha-glucosidase from derivatives of monascus pigment.
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.
Kim
Jong Hoon
JH
Department of Biotechnology, College of Engineering, Yonsei University, Seoul, South Korea.
Kim
Hyun Jung
HJ
Park
Hae Woong
HW
Youn
Sung Hun
SH
Choi
Duck-Young
DY
Shin
Chul Soo
CS
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*
D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D010860:Pigments, Biological; C028544:cyclohexylalanine; D010649:Phenylalanine; D009646:Norleucine; D008049:Lipase; D010396:Penicillamine