title: Sesquiterpene furan compound CJ-01, a novel chitin synthase 2 inhibitor from Chloranthus japonicus SIEB.
abstract: A novel sesquiterpene furan compound CJ-01 was isolated from the methanol extract of the whole plant of Chloranthus japonicus SIEB. by monitoring the inhibitory activity of chitin synthase 2 from Saccharomyces cerevisiae. Based on spectroscopic analysis, the structure of compound CJ-01 was determined as 3,4,8a-trimethyl-4a,7,8,8a-tetrahydro-4a-naphto[2,3-b]furan-9-one. The compound inhibited chitin synthase 2 of Saccharomyces cerevisiae in a dose-dependent manner with an IC50 of 39.6 microg/ml, whereas it exhibited no inhibitory activities against chitin synthase 1 and 3 of S. cerevisiae up to 280 microg/ml. CJ-01 has 1.7-fold stronger inhibitory activity than polyoxin D (IC50=70 microg/ml), a well-known chitin synthase inhibitor. These results indicate that the compound is a specific inhibitor of chitin synthase 2 from S. cerevisiae. In addition, CJ-01 showed antifungal activities against various human and phytopathogenic fungi. Therefore, the compound might be an interesting lead to develop effective antifungal agents.
authors.affiliation: Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Korea.
authors.forename: Nam Hui
authors.initials: NH
authors.lastname: Yim
authors.forename: Eui Il
authors.initials: EI
authors.lastname: Hwang
authors.forename: Bong Sik
authors.initials: BS
authors.lastname: Yun
authors.forename: Ki Duk
authors.initials: KD
authors.lastname: Park
authors.forename: Jae Sun
authors.initials: JS
authors.lastname: Moon
authors.forename: Sang Han
authors.initials: SH
authors.lastname: Lee
authors.forename: Nack Do
authors.initials: ND
authors.lastname: Sung
authors.forename: Sung Uk
authors.initials: SU
authors.lastname: Kim
mesh_terms: D000818:Animals; D002687:Chitin Synthase / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005658:Fungi / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008566:Membranes / Q000187:drug effects / Q000201:enzymology; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D009181:Mycoses / Q000382:microbiology; D010944:Plants / Q000737:chemistry*; D012441:Saccharomyces cerevisiae / Q000187:drug effects / Q000201:enzymology; D012717:Sesquiterpenes / Q000494:pharmacology*
chemical_list: C529590:CJ-01 compound; D004791:Enzyme Inhibitors; D012717:Sesquiterpenes; D002687:Chitin Synthase; C400821:chitin synthase 2