ABSTRACT
Actinomycetes are known to produce numerous secondary bioactive metabolites of pharmaceutical interest. The purpose of this study was to isolate, characterize, and investigate the antibacterial, antifungal, and anticancer activities of metabolites produced by Actinobacteria isolated from the rhizosphere of Paullinia cupana. The Actinobacteria was identified as Streptomyces hygroscopicus ACTMS-9H. Based on a bioguided study, the methanolic biomass extract obtained from submerged cultivation had the most potent antibacterial, antifungal, and cytotoxic activities. This extract was partitioned with n-hexane, ethyl acetate, and 2-butanol. Elaiophylin was isolated from the methanolic biomass extract, and its molecular formula was determined (C54H88O18) based on 1H and 13C NMR, IR and MS analyses. The 2-butanol phase was fractionated into four fractions (EB1, EB2A, EB2B, and EB3M). Chemical prospecting indicated the presence of alkaloids, saponins, and reducing sugars in the methanolic extract and 2-butanol phase. The elaiophylin displayed anticancer activity in HEp-2 and HL-60 cells with an IC50 of 1 µg/mL. The EB1 fraction was selectively toxic to HL-60 cells with IC50 of 9 ng/mL. Bioautography showed that the EB1 fraction contained an alkaloid with antibacterial and antifungal activities (MIC values ≤1.9 and <3.9 µg/mL, respectively). In conclusion, the EB1 fraction and elaiophylin of S. hygroscopicus have potent antimicrobial, antifungal, and anticancer activities.
Subject(s)
Anti-Infective Agents/isolation & purification , Antineoplastic Agents/isolation & purification , Biological Products/isolation & purification , Soil Microbiology , Streptomyces/isolation & purification , Streptomyces/physiology , Anti-Infective Agents/chemistry , Antineoplastic Agents/chemistry , Bacteria/drug effects , Biological Products/chemistry , Brazil , Cell Line, Tumor , Cell Survival/drug effects , Fungi/drug effects , Humans , Inhibitory Concentration 50 , Microbial Sensitivity Tests , Paullinia/growth & development , Rhizosphere , Spectrum Analysis , Streptomyces/chemistry , Streptomyces/metabolismABSTRACT
Lippia alba (Mill.) N.E. Brown (Verbenaceae) is commonly used in the Brazilian folk medicine to the treatment of gastric illnesses, diarrhea, fever, asthma, and as a tranquilizer. This work evaluated the antimicrobial activity of ethyl acetate, methanol and aqueous extracts from the roots of the L. alba using plates-holes diffusion assay and the phytochemical profile. The results obtained showed that the ethyl acetate and methanol extracts presented antimicrobial activity against Staphylococcus aureus (ATCC 6538P), Staphylococcus aureus (ATCC 6538) and Klebsiella pneumonia (ATCC 10031). Terpenoids, phenylpropanoids and sugars were detected in the phytochemical analysis.
Lippia alba (Mill.) N.E. Brown (Verbenaceae) é geralmente usada na medicina popular brasileira para o tratamento de doenças gástricas, febre, asma e como tranqüilizante. Este trabalho avaliou a atividade antimicrobiana dos extratos acetato de etila, metanol e aquoso das raízes de L. alba usando métodos de difusão em poços e o perfil fitoquímico. Os resultados obtidos mostraram que os extratos acetato de etila e metanol apresentaram atividade antimicrobiana contra Staphylococcus aureus (ATCC 6538P), Staphylococcus aureus (ATCC 6538) e Klebsiella pneumonia (ATCC 10031). Terpenóides, fenilpropanóides e açúcares foram detectados na análise fitoquímica.
