scholarly journals Characterization, Diversity, and Structure-Activity Relationship Study of Lipoamino Acids from Pantoea sp. and Synthetic Analogues

2019 ◽  
Vol 20 (5) ◽  
pp. 1083 ◽  
Author(s):  
Seindé Touré ◽  
Sandy Desrat ◽  
Léonie Pellissier ◽  
Pierre-Marie Allard ◽  
Jean-Luc Wolfender ◽  
...  
Keyword(s):  
Methicillin Resistant Staphylococcus Aureus ◽  
Inhibitory Concentration ◽  
Biological Evaluation ◽  
Comprehensive Analysis ◽  
Chain Fatty Acid ◽  
Long Chain Fatty Acid ◽  
Lipoamino Acids ◽  
Structure Activity ◽  
Relationship Study ◽  
Saturated Medium

A biological evaluation of a library of extracts from entomopathogen strains showed that Pantoea sp. extract has significant antimicrobial and insecticidal activities. Three hydroxyacyl-phenylalanine derivatives were isolated from this strain. Their structures were elucidated by a comprehensive analysis of their NMR and MS spectroscopic data. The antimicrobial and insecticidal potencies of these compounds were evaluated, and compound 3 showed 67% mortality against Aedes aegypti larvae at a concentration of 100 ppm, and a minimum inhibitory concentration (MIC) of 16 µg/mL against methicillin-resistant Staphylococcus aureus. Subsequently, hydroxyacyl-phenylalanine analogues were synthesized to better understand the structure-activity relationships within this class of compounds. Bioassays highlighted the antimicrobial potential of analogues containing saturated medium-chain fatty acids (12 or 14 carbons), whereas an unsaturated long-chain fatty acid (16 carbons) imparted larvicidal activity. Finally, using a molecular networking-based approach, several close analogues of the isolated and newly synthesized lipoamino acids were discovered in the Pantoea sp. extract.

Synthesis and structure–activity relationships of novel abietane diterpenoids with activity against Staphylococcus aureus

2019 ◽  
Vol 11 (24) ◽  
pp. 3109-3124
Author(s):  
Macarena Funes Chabán ◽  
Antonia I Antoniou ◽  
Catherine Karagianni ◽  
Dimitra Toumpa ◽  
Mariana Belén Joray ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Minimum Inhibitory Concentration ◽  
Toxic Effect ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Inhibitory Concentration ◽  
Dehydroabietic Acid ◽  
Target Cells ◽  
Structure Activity ◽  
Abietane Diterpenoids ◽  
Relationship Study

Aim: To find alternative compounds against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-susceptible S. aureus (MSSA), novel derivatives from dehydroabietic acid were synthesized. Methods & results: Compound 12 was the most effective against 15 MRSA and 11 MSSA with minimum inhibitory concentration values ranging from 3.9 to 15.6 μg/ml. Although less active than 12, compound 11, followed by 25 and 13, also exhibited anti-staphylococcal activity. Additional studies showed that compound 12 is devoid of toxic effect on non-target cells. A structure–activity relationship study revealed that an oxime at C-13 together with a hydroxyl at C-12 could play a key role in the activity. Conclusion: These structures, in particular compound 12, could arise as templates for the development of agents against MRSA and MSSA.

Antimicrobial activity of seven Piper species from Colombian coffee-growing Eco-region against multidrug resistant bacteria

2020 ◽  
Vol 3 (3) ◽  
pp. 33-37
Author(s):  
Oscar M Mosquera ◽  
◽  
Roman Y. Ramirez-Rueda ◽  
Aura M. Blandon ◽  
◽  
...  
Keyword(s):  
Methicillin Resistant Staphylococcus Aureus ◽  
Inhibitory Concentration ◽  
Methanolic Extract ◽  
Biological Activities ◽  
Multidrug Resistant ◽  
Inhibitory Effect ◽  
Biological Evaluation ◽  
Resistant Bacteria ◽  
Antibacterial Compounds ◽  
Layer Chromatography

Species of Piper genus are known for their numerous biological activities and their diverse phytochemical composition. The object of this work was to evaluate the antibacterial activity of extracts obtained from seven Piperaceae species. Broth microdilution technique was used for biological evaluation and some phytochemical nuclei present in the bioactive extracts were identified by thin layer chromatography and characterization reactions. Among the most important results, it is highlighted the inhibitory effect of the methanolic extract from Piper pesaresanum against Methicillin-resistant Staphylococcus aureus ATTC 43300, with minimum inhibitory concentration of 62.5 μg/mL. Additionally, secondary metabolites such as alkaloids, phenols and flavonoids were detected in this extract. In conclussion, the species P. pesaresanum showed high potential for bioguided search of antibacterial compounds against multidrug resistant S. aureus.

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