Abstract:
:The cholesteryl ester transfer protein (CETP), inhibition of which assists in maintaining a high level of high-density lipoprotein cholesterol in the blood, is a target for anti-atherosclerosis treatments. Orange monascus pigment was produced by a Monascus species in a 5 L jar fermenter and various derivative compounds were synthesised by incorporating 19 different L-amino acids into the orange pigment. Among them, the L-Thr and L-Tyr derivatives exhibited high inhibitory activities against the CETP reaction. The inhibitory activities of the L-Thr and L-Tyr derivatives increased in a dose-dependent manner, resulting in IC50 values of 1.0 and 2.3 μM, respectively. When CETP reactions in the presence of the derivatives were performed, the inhibition modes of the L-Thr and L-Tyr derivatives were non-competitive with inhibition constant (Ki) values of 2.7 and 4.3 μM, respectively.
journal_name
Nat Prod Resjournal_title
Natural product researchauthors
Jang H,Choe D,Shin CSdoi
10.1080/14786419.2014.905561subject
Has Abstractpub_date
2014-01-01 00:00:00pages
1427-31issue
18eissn
1478-6419issn
1478-6427journal_volume
28pub_type
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