Induction of choline acetyltransferase activity in cholinergic neurons by stolonidiol: structure-activity relationship.
The effect of stolonidiol (1), a bioactive marine diterpenoid from the Japanese soft coral Clavularia sp., on choline acetyltransferase (ChAT) activity was examined using cultured cholinergic neurons. Stolonidiol (1) showed potent ChAT inducible activity in primary cultured basal forebrain cells and clonal septal SN49 cells, suggesting that it may act as a potent neurotrophic factor-like agent on the cholinergic nervous system. Further expansion of the structure-activity relationship to include stolonidiol (1) and its derivatives demonstrated that the exo-methylene group and the epoxide group are essential for ChAT-inducing activity. Stolonidiol (1) showed the highest activity among the test samples.
Yabe
T
T
Oriental Medicine Research Center, The Kitasato Institute, Minato-ku, Tokyo 108-8642, Japan.
Yamada
H
H
Shimomura
M
M
Miyaoka
H
H
Yamada
Y
Y
D000818:Animals; D002478:Cells, Cultured; D002795:Choline O-Acetyltransferase / Q000096:biosynthesis* / Q000235:genetics; D003063:Cnidaria / Q000737:chemistry*; D004224:Diterpenes / Q000737:chemistry / Q000494:pharmacology*; D004790:Enzyme Induction; D009474:Neurons / Q000201:enzymology*; D010275:Parasympathetic Nervous System / Q000166:cytology / Q000201:enzymology*; D051381:Rats; D020133:Reverse Transcriptase Polymerase Chain Reaction; D013329:Structure-Activity Relationship
D004224:Diterpenes; C409602:stolonidiol; D002795:Choline O-Acetyltransferase