RESUMEN
Chromatographic separation of fruits and flowers of the Thai medicinal plant, Miliusa velutina, resulted in the isolation of five new rare homogentisic acid derivatives, miliusanal (1) and miliusanones A-D (2-5), together with fifteen known secondary metabolites (6-20). Their structures were determined through the use of extensive spectroscopic data. The absolute configurations of homogentisic acid derivatives 2-7 were identified using NOESY data and a comparison of experimental and calculated ECD spectral data. Compounds 2, 3, 6, and 7 showed antimalarial activity with IC50 values in the range of 3.3-5.2⯵g/mL. Compound 6 also showed activity against Mycobacterium tuberculosis with an MIC value of 50⯵g/mL. Compounds 1-3, 6 and 7 exhibited cytotoxicity againt KB, MCF-7, NCI-H187 and Vero cell lines with IC50 values in the range of 5.8-40.4⯵g/mL. In addition, compounds 1, 2 and 6 showed moderate antibacterial activities against three Gram-positive bacteria (Bacillus cereus, Staphylococcus aureus, and Methicillin resistant S. aureus) with MICs in the range of 32-64⯵g/mL.
Asunto(s)
Annonaceae/química , Antibacterianos/farmacología , Antineoplásicos Fitogénicos/farmacología , Ácido Homogentísico/farmacología , Animales , Antibacterianos/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Chlorocebus aethiops , Flores/química , Frutas/química , Bacterias Grampositivas/efectos de los fármacos , Ácido Homogentísico/aislamiento & purificación , Humanos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Mycobacterium tuberculosis/efectos de los fármacos , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Tailandia , Células VeroRESUMEN
The use of probiotic bacteria to control bacterial infection in farmed fish is of clear practical interest. The aims of this study were to isolate and select a probiotic Bacillus sp. and to evaluate the effects of its supplementation on the growth and disease resistance of hybrid catfish. Bacillus siamensis strain B44v, selectively isolated from Thai pickled vegetables (Phak-dong), displayed a high potential as a probiotic in catfish culture. This bacterium produced a bacteriocin-like substance and exhibited a broad-spectrum antibacterial activity inhibiting both Gram-positive and Gram-negative bacteria, especially the fish pathogens Aeromonas hydrophila and Streptococcus agalactiae. The susceptibility to all 14 antibiotics tested implies its less possibility to be the antibiotic-resistant bacterium. Bacillus siamensis strain B44v possessed interesting adhesion properties, as shown by its high percentages of hydrophobicity (64.8%), auto-agglutination (73.8%), co-aggregation (67.2% with A. hydrophila FW52 and 63.5% with S. agalactiae F3S), and mucin binding (88.7%). The strain B44v survived simulated gastrointestinal conditions and produced protease and cellulase enzymes. Hybrid catfish (C. macrocephalus × C. gariepinus) were employed in the feed-trial experiments. Fish fed diet containing strain B44v (107 CFU/g feed) displayed not only no mortality but also growth improvement. At the end of the feed trial, fish were challenged by an intraperitoneal injection of Aeromonas hydrophila FW52. The Bacillus siamensis strain B44v fed fish survived (75.0%; p < 0.05) better than the controls (36.7%; p < 0.05) after a two week challenge. These collective results present for the first time the potential of Bacillus siamensis strain B44v for use as a bacterial probiotic in aquaculture.