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.
"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]. "
[Show abstract][Hide abstract] ABSTRACT: This study is the first to demonstrate that shizukaol D, a natural compound isolated from Chloranthusjaponicus, can activate AMP- activated protein kinase (AMPK), a key sensor and regulator of intracellular energy metabolism, leading to a decrease in triglyceride and cholesterol levels in HepG2 cells. Furthermore, we found that shizukaol D induces mitochondrial dysfunction by depolarizing the mitochondrial membrane and suppressing energy production, which may result in AMPK activation. Our results provide a possible link between mitochondrial dysfunction and AMPK activation and suggest that shizukaol D might be used to treat metabolic syndrome.
PLoS ONE 08/2013; 8(8):e73527. DOI:10.1371/journal.pone.0073527 · 3.23 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: The incidence and prevalence of serious mycoses continues to be a public health problem. Despite aggressive treatment with new or more established licensed antifungal agents, these infections are an important cause of morbidity and mortality, especially in immunocompromised patients.
To critically review the literature regarding important new developments in the field of antifungal therapy both in the English and Spanish versions.
The search of the literature focused on different antifungal targets or mechanisms of action as well as new agents or strategies that could improve antifungal therapy.
The review produced a huge amount of information on the use of virulent factors such as growth, filamentation, pathogen tissue clearance, among others, as putative targets of antifungal activity. More recently, the chemical-genetic relationships for licensed agents as well as for other compounds have been provided by the identification of the genes related to the mechanism of action.
Although the antifungal activity of numerous compounds has been examined, most of them are at the in vitro or animal models of efficacy stages. Therefore, further investigation should be carried out to realize the true clinical utility of these compounds.
Revista Iberoamericana de Micología 04/2009; 26(1):15-22. DOI:10.1016/S1130-1406(09)70004-X · 1.06 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: An antifungal compound was isolated from methanol extracts of stems and roots of Chloranthus henryi Hemsl. using ethyl acetate extraction and various chromatographic techniques. On the basis of spectroscopic analyses including mass and various NMR, the structure of the compound was identified as a dimeric sesquiterpene, CHE-23C. The compound showed potent antifungal activities (MICs = 1-32 microg/mL) in vitro against various phytopathogenic fungi such as Alternaria kikuchiana , Botrytis cinerea , Colletotrichum lagenarium , Magnaporthe grisea , Pythium ultimum , and Phytophthora infestans . In particular, it exhibited 91 and 100% disease-control activity in vivo against tomato late blight (P. infestans) and wheat leaf rust ( Puccinia recondita ) at concentrations of 33 and 100 microg/mL, respectively. The disease-control activity of this compound was stronger than that of the commercially available fungicide chlorothalonil, but weaker than that of dimethomorph. Therefore, the compound might serve as an interesting lead to develop effective antifungal agents.
Journal of Agricultural and Food Chemistry 08/2009; 57(13):5750-5. DOI:10.1021/jf900674y · 2.91 Impact Factor
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