ABSTRACT
We investigated the secondary metabolites present in Penicillium janthinellum MPT-25, an endophytic fungus isolated from Taxus wallichiana var. chinensis (Pilger) Florin. Chemical characterization of the solid cultured extract resulted in the isolation of 11 compounds, including eight previously undescribed metabolites: a thiazolo[5,4-b]pyridine alkaloid, janthinedine A (1), and seven ar-bisabol sesquiterpenes, janthinepenes A-G (2-8). Their structures were elucidated by a combination of extensive spectroscopic methods, including single-crystal X-ray diffraction and ECD spectra. The antimicrobial activities of these compounds were evaluated against seven agricultural pathogenic fungi and eight clinically drug-resistant bacteria.
ABSTRACT
A new chromone analog (1) and a new pyrrole alkaloid (2), together with four known compounds, were isolated from the endophytic fungus Penicillium sclerotiorum MPT-250 obtained from the stems of Taxus wallichiana var. chinensis (Pilger) Florin. The structural elucidation of these metabolites was performed by high-resolution mass spectrometry and NMR spectroscopy. Compounds 1 and 5 exhibited significant antibacterial activity against carbapenems-resistant Pseudomonas aeruginosa and multidrug-resistant Enterococcus faecium with an minimum inhibitory concentration (MIC) value of 3.13 µg/ml respectively.
ABSTRACT
Three new hydroxyphenylacetic acid derivatives, stachylines E-G (1-3), and a new alkaloid, mortieridinone (4), along with six known compounds (5-10), were isolated from endophytic fungus Mortierella sp. in Epimedium acuminatum Franch. Their structures were determined by their spectroscopic analyses and by comparison with the literature data. Compounds 7 and 10 showed selective antibacterial activity against tested multidrug-resistant bacteria with minimum inhibitory concentration (MIC) values ranging from 25 to 3.13â µg/mL.
Subject(s)
Alkaloids/pharmacology , Anti-Bacterial Agents/pharmacology , Epimedium/microbiology , Mortierella/chemistry , Phenylacetates/pharmacology , Alkaloids/chemistry , Alkaloids/isolation & purification , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Drug Resistance, Multiple, Bacterial/drug effects , Enterococcus faecium/drug effects , Microbial Sensitivity Tests , Molecular Structure , Phenylacetates/chemistry , Phenylacetates/isolation & purification , Staphylococcus aureus/drug effectsABSTRACT
With unique advantages, the small-molecule anticancer drugs have recently gained growing attention. Particular strategies, exemplified by high-throughput screening, fragment-based drug discovery, virtual screening and knowledge-based design, have been developed to identify active compounds. However, such screens generally rely on sophisticated and expensive instrumentations. Herein, we developed a simple spheroids 3D culture system to enable direct screening of small molecules with reliable results. Using this system, we screened 27 fungal natural products and three fungal crude extracts for their inhibitory effects on cancer cell growth, and invasion. We identified that the compound M23 (epitajixanthone hydrate, a derivative of prenylxanthone) and the crude extracts (MPT-191) from the fungi Taxus chinensis showed potential anticancer activity. The effect of epitajixanthone hydrate on cancer cell growth and invasion were further confirmed by the assays of cells viability, trans-well migration and invasion, colony formation and cells reattachment. Overall, Epitajixanthone hydrate was identified as an effective inhibitor of cancer cell growth and invasion by our simple and fast screening platform.
