Sesquiterpene Furan Compound CJ-01, a Novel Chitin Synthase 2 Inhibitor from Chloranthus japonicus SIEB.

Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Korea.
Biological & Pharmaceutical Bulletin (Impact Factor: 1.83). 06/2008; 31(5):1041-4. DOI: 10.1248/bpb.31.1041
Source: PubMed


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.

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    • "Given the importance of AMPK in metabolic disorders [8,14], we conducted a systematical analysis for AMPK activation in HepG2 cells treated with natural compounds isolated from Chloranthusjaponicus. Chloranthusjaponicus (Chloranthaceae) is widely used in traditional Chinese medicine for the treatment of traumatic injuries, rheumatic arthralgia, bone fractures, pulmonary tuberculosis, and neurasthenia [28,29]. The main chemical components of this plant are sesquiterpenoid dimers and trimers [30–32]. "
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