title: Selective cholinesterase inhibition by lanostane triterpenes from fruiting bodies of Ganoderma lucidum.
abstract: Two new lanostane triterpenes, named methyl ganoderate A acetonide (1) and n-butyl ganoderate H (2), were isolated from the fruiting bodies of Ganoderma lucidum together with 16 known compounds (3-18). Extensive spectroscopic and chemical studies established the structures of these compounds as methyl 7β,15α-isopropylidenedioxy-3,11,23-trioxo-5α-lanost-8-en-26-oate (1) and n-butyl 12β-acetoxy-3β-hydroxy-7,11,15,23-tetraoxo-5α-lanost-8-en-26-oate (2). Because new compounds exhibiting specific anti-acetylcholinesterase activity are being sought as possible drug candidates for the treatment of Alzheimer's and related neurodegenerative diseases, compounds 1-18 were examined for their inhibitory activities against acetylcholinesterase and butyrylcholinesterase. All of the compounds exhibited moderate acetylcholinesterase-inhibitory activity, with IC(50) values ranging from 9.40 to 31.03μM. In contrast, none of the compounds except lucidadiol (13) and lucidenic acid N (14) exhibited butyrylcholinesterase-inhibitory activity at concentrations up to 200μM. These results indicate that these lanostane triterpenes are preferential inhibitors of acetylcholinesterase and may be suitable drug candidates.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
authors.forename: Iksoo
authors.initials: I
authors.lastname: Lee
authors.forename: Bora
authors.initials: B
authors.lastname: Ahn
authors.forename: Jaesue
authors.initials: J
authors.lastname: Choi
authors.forename: Masao
authors.initials: M
authors.lastname: Hattori
authors.forename: Byungsun
authors.initials: B
authors.lastname: Min
authors.forename: Kihwan
authors.initials: K
authors.lastname: Bae
mesh_terms: D002800:Cholinesterase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D020940:Reishi / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D002800:Cholinesterase Inhibitors; D014315:Triterpenes