Fourteen eremophilane sesquiterpenoids (-), including nine new congeners, septoreremophilanes A-I (-), together with three known sesquiterpenes (-), two known tetralone derivatives (, ), and two known cholesterol analogues (, ), were isolated from the endophytic fungus . Compounds - and belong to the family of the highly oxygenated eremophilane sesquiterpenoids with a 6/6/5 tricyclic system and bearing a hemiacetal moiety. The inhibitions of all metabolites against eight bacteria were estimated , and nine new metabolites (-) were tested for antineuroinflammatory activity. Notably, the effects of against pv. and against displayed potent inhibitory, with the MIC values of 6.25 and 6.25 M, respectively. Further, scanning electron microscopy analyses indicated that and were to change the outer configuration of bacterial cells, respectively, and the investigations demonstrated that and may act as potential structure templates for the development of the agrochemical bactericides. Additionally, compound displayed potent inhibition of NO generation in lipopolysaccharide-induced BV-2 microglial cells (IC = 12.0 ± 0.32 M), and the conceivable anti-inflammatory mechanisms implicated were also investigated by molecular docking. Thus, the bioactive metabolites of the strain may serve as a novel resource to be developed.
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http://dx.doi.org/10.1021/acs.jafc.1c04131 | DOI Listing |
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