Arisugacins C and D, novel acetylcholinesterase inhibitors and their related novel metabolites produced by Penicilium sp. FO-4259-11.
The mutant of Penicillium sp. FO-4259, an arisugacins A and B producing strain, was found to produce a series of metabolites, designated arisugacins C, D, E, F, G and H, which were structurally related to arisugacins A and B. These compounds were isolated from the culture broth and the physico-chemical and biological properties were examined. The IC50 values of arisugacins C and D against acetylcholinesterase (AChE) were 2.5 microM and 3.5 microM, respectively. However arisugacins E, F, G and H did not inhibit AChE at 100 microM. Though they showed only weak or no activity against AChE compared with arisugacins A and B, they may be useful for the study of the structure-activity relationship.
Otoguro
K
K
Research Center for Biological Function, The Kitasato Institute, Tokyo, Japan.
Shiomi
K
K
Yamaguchi
Y
Y
Arai
N
N
Sunazuka
T
T
Masuma
R
R
Iwai
Y
Y
Omura
S
S
D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000302:isolation & purification* / Q000378:metabolism; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D010407:Penicillium; D011714:Pyrans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D011714:Pyrans; C095353:arisugacin; C040405:territrem B