RESUMEN
Extreme environments Morrope and Bayovar Salt lagoons, several ecosystems and microhabitats remain unexplored, and little is known about the diversity of Actinobacteria. We suggest that the endemic bacteria present in this extreme environment is a source of active molecules with anticancer, antimicrobial, and antiparasitic properties. Using phenotypic and genotypic characterization techniques, including 16S rRNA sequencing, we identified these bacteria as members of the genera Streptomyces, Pseudonocardia, Staphylococcus, Bacillus, and Pseudomonas. Actinobacteria strains were found predominantly. Phylogenetic analysis revealed 13 Actinobacteria clusters of Streptomyces, the main genus. Three Streptomycetes, strains MW562814, MW562805, and MW562807 showed antiproliferative activities against three tumor cell lines: U251 glioma, MCF7 breast, and NCI-H460 lung (non-small cell type); and antibacterial activity against Staphylococcus aureus ATCC 6538, Escherichia coli ATCC 10536, and the multidrug resistant Acinetobacter baumannii AC-972. The antiproliferative activities (measured as total growth inhibition [TGI]) of Streptomyces sp. MW562807 were 0.57 µg/mL, for 0.61 µg/mL, and 0.80 µg/mL for glioma, lung non-small cell type, and breast cancer cell lines, respectively; the methanolic fraction of the crude extract showed a better antiproliferative activity and could inhibit the growth of (U251 (TGI = 38.3 µg/mL), OVCAR-03 (TGI = 62.1 µg/mL), and K562 (TGI = 81.5 µg/mL)) of nine tumor cells types and one nontumor cell type. Extreme enviroments, such as the Morrope and Bayovar Salt saloons are promising sources of new bacteria, whose compounds may be useful for treating various infectious diseases or even some types of cancer.
Asunto(s)
Actinobacteria , Filogenia , Antibacterianos , Pruebas de Sensibilidad Microbiana , ARN Ribosómico 16S , StreptomycesRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: The incidence of gastric mucosa lesions in the adult population has increased mainly due to the continued use of nonsteroidal anti-inflammatory drugs (NSAIDs). The cashew (Anacardium occidentale L.) is a tropical tree, cultivated in several countries, whose barks, leaves and pseudofruit (cashew apple) are popularly used in traditional medicine for the treatment of many diseases, including gastric ulcer. AIM: Our study evaluated the potential gastroprotective effect of the carotenoid and anacardic acids-enriched aqueous extract (CAE), prepared from cashew apple pomace, in the dose-repeated acetylsalicylic acid (ASA)-induced gastric lesions model in rats. MATERIAL AND METHODS: After randomly distribution into five group (G1 - G5, n = 8 animals/group), male Wistar rats were daily treated with ASA solution (200 mg/kg, 5 ml/kg, G2 - G5) or potable water (Satellite group, G1) during 14 days. From 8th to 14th experimental day, rats in G3 - G5 groups were orally treated with CAE (50, 100 and 500 mg/kg, 5 ml/kg, respectively). Body weight was measured on 0, 7th and 14th day. On the 14th experimental day, all surviving animals were euthanized for macroscopic evaluation of the inner organs and stomach removal. After weighting, each stomach was properly prepared for biochemical analysis [myeloperoxidase activity (MPO), reduced glutathione analysis (GSH), IL-1ß, CXCL2/MIP-2, TNF-α and IL-10 levels]. RESULTS: At the most efficient dose (100 mg/kg, p.o.), CAE-treated animals showed a slight improvement in the macroscopic aspect of gastric mucosa associated with significant (p < 0.05) reduced levels of IL-1ß, CXCL2/MIP-2, and MPO activity besides increased levels of GSH (partially), and IL-10 in stomach tissues. CONCLUSIONS: The present study demonstrated that the carotenoid and anacardic acids-enriched extract obtained from cashew apple pomace is a promising raw material for the development of herbal medicine and/or functional food supplements for the adjuvant treatment of NSAIDs-induced gastric ulcers.
Asunto(s)
Anacardium/química , Antiulcerosos/farmacología , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Úlcera Gástrica/prevención & control , Ácidos Anacárdicos/química , Ácidos Anacárdicos/aislamiento & purificación , Ácidos Anacárdicos/farmacología , Ácidos Anacárdicos/uso terapéutico , Animales , Antiinflamatorios no Esteroideos/toxicidad , Antiulcerosos/uso terapéutico , Aspirina/toxicidad , Carotenoides/química , Carotenoides/aislamiento & purificación , Carotenoides/farmacología , Carotenoides/uso terapéutico , Quimiocina CXCL2/metabolismo , Modelos Animales de Enfermedad , Mucosa Gástrica/efectos de los fármacos , Glutatión/metabolismo , Interleucina-10/metabolismo , Interleucina-1beta/metabolismo , Masculino , Peroxidasa/metabolismo , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Sustancias Protectoras/uso terapéutico , Ratas Wistar , Úlcera Gástrica/inducido químicamenteRESUMEN
Three undescribed germacranolide sesquiterpene lactones, named macrocephalides A-C, along with known steroids, triterpenes and flavonoids were isolated from the aerial parts of Campuloclinium macrocephalum. The structures of the undescribed compounds were elucidated with basis on their 1D and 2D-NMR, and HR-ESI-MS data. Their absolute configurations were assigned by comparison of experimental and calculated electronic circular dichroism (ECD) spectra. Additionally, macrocephalides A-C were evaluated for their in vitro cytotoxic activities against nine human cancer cell lines. Macrocephalides A and B exhibited moderate to potent cytotoxic activity, inhibiting 50% of cell growth (GI50) at concentrations ranging from 0.576 to 6.37 µM.
Asunto(s)
Asteraceae , Eupatorium , Sesquiterpenos , Línea Celular Tumoral , Humanos , Lactonas/farmacología , Estructura Molecular , Fitoquímicos , Sesquiterpenos/farmacologíaRESUMEN
INTRODUCTION: Osteonecrosis of the jaw is a condition associated with intraoral ulceration and bone necrosis induced by antiresorptive medications, such as zoledronic acid, a bisphosphonate. Previous data on Arrabidaea chica (H&B.) Verlot wound healing activity prompted the study reported herein on A. chica standardized hydro alcoholic extract in vitro cytoprotective activity data on epithelial and osteoblastic cells exposed to zoledronic acid (ZA). METHODS: Primary human gingival fibroblasts and murine pre-osteoblasts were treated with ZA 10 µM together with 5 or 10 µg.mL-1 A. chica extract for 24h and 48 h. At both times, cells were submitted to viability assay and caspase 3/7 activation evaluation. Statistical analysis used one-way ANOVA and p=0.05. RESULTS: In cell viability assay, a drastic damage effect of ZA appeared after 48 h in both epithelial (55.8%) and pre-osteoblastic cells (39.7%). When treated with ZA in combination with A. chica extract, cells showed higher viability values: 74.1%-82.3% for fibroblasts and 66% for pre-osteoblasts. Furthermore, the combined treatment presented lower caspase 3/7 activation in fibroblasts and pre-osteoblasts. CONCLUSION: At low concentrations, A. chica extract showed promising cytoprotective effects against ZA-induced damage actions; however, further in vitro and in vivo studies are required to establish the mechanism of action.