Novel lactone compounds from Mortierella verticillata that induce the human low density lipoprotein receptor gene: fermentation, isolation, structural elucidation and biological activities.
Among methods of controlling hypercholesterolemia and hyperlipidemia is the direct stimulation of hepatic low density lipoprotein (LDL) receptors. Two novel lactone compounds, CJ-12,950 and CJ-13,357, containing and unusual oxime moiety, were isolated from a zygomycete Mortierella verticillata. These lactones are potent inducers of the LDL receptor gene in vitro, that enhanced LDL receptor expression in human hepatocytes 2-fold at 100 nM.
Dekker
K A
KA
Central Research Division, Pfizer Pharmaceuticals Inc., Aichi, Japan.
Aiello
R J
RJ
Hirai
H
H
Inagaki
T
T
Sakakibara
T
T
Suzuki
Y
Y
Thompson
J F
JF
Yamauchi
Y
Y
Kojima
N
N
D018929:Cell Culture Techniques; D005285:Fermentation; D005786:Gene Expression Regulation; D006801:Humans; D007783:Lactones / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D018942:Macrolides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D009090:Mucorales / Q000737:chemistry* / Q000378:metabolism; D011973:Receptors, LDL / Q000235:genetics*
C111272:CJ-12950; C111273:CJ-13357; D007783:Lactones; D018942:Macrolides; D011973:Receptors, LDL