Sesquiterpene furan compound CJ-01, a novel chitin synthase 2 inhibitor from Chloranthus japonicus SIEB.
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.
Yim
Nam Hui
NH
Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Korea.
Hwang
Eui Il
EI
Yun
Bong Sik
BS
Park
Ki Duk
KD
Moon
Jae Sun
JS
Lee
Sang Han
SH
Sung
Nack Do
ND
Kim
Sung Uk
SU
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*
C529590:CJ-01 compound; D004791:Enzyme Inhibitors; D012717:Sesquiterpenes; D002687:Chitin Synthase; C400821:chitin synthase 2