RESUMEN
Bioactive phytoconstituents have been increasingly investigated for their potential human health benefits. Corema album (L.) D. Don, an Ericaceae, reportedly has antioxidant, antimicrobial and anticancer properties. Aiming at enhancing its nutraceutical potential, we performed a spectrochemical analysis of hydroethanolic extracts from C. album leaves. We report on changes in the antioxidant activity of the extracts, as well as in the accumulation of key phytoconstituents (namely phenolic compounds), in female and male samples, throughout three harvesting seasons (February, July, and October). For each extract, the antioxidant activity was assessed by different spectrophotometric methods. Simultaneously, attenuated total reflectance Fourier transform mid-infrared spectroscopy (FTIR-ATR), and high-performance liquid chromatography - electrospray ionisation - quadrupole time-of-flight mass spectrometry (HPLC-ESI-Q-TOF-MS), were used to identify and monitor variations in the composition of phenolic compounds in the extracts. The main compounds identified were epicatechin, laricitrin-O-hexoside isomers, and myricetin-O-hexoside isomers. Significant differences were found in the composition and relative abundance of the compounds of interest, according to sex and season. Overall, a trend was observed whereby phenolic content and antioxidant activities were higher in males and increased between the earlier and the latest harvests. Based on these results, we may conclude that late summer or early autumn harvests are preferable when aiming at the highest yearly content of bioactive compounds. Additionally, it should be considered that extracts from male individuals typically display higher antioxidant activities. Ultimately, our understanding of C. album in the context of nutraceutical applications is benefited from the quantitative and qualitative portrait provided here, thus promoting its relevance as a source of bioactive compounds.
Asunto(s)
Antioxidantes , Ericaceae , Femenino , Masculino , Humanos , Antioxidantes/farmacología , Antioxidantes/química , Estaciones del Año , Extractos Vegetales/química , Cromatografía Líquida de Alta Presión/métodosRESUMEN
This study reports an evaluation of the biological properties of the edible berries from Corema album, an endemic shrub of the Portuguese coastline, aiming at its use as a nutraceutical. Different methanolic extracts were obtained from the pulp and seed of fresh berries: pulp extract, seed residue, and seed oil (extracted and characterized for the first time). For each of these, the antioxidant activity was assessed, by different methods, as well as the antimicrobial ability. Overall, the seeds were shown to be the most nutraceutical part of the berry since they showed higher antioxidant activity, while the pulp extract displayed a significant antimicrobial capacity against several clinically relevant bacterial strains. Furthermore, the extracts were fully characterized by complementary infrared and Raman spectroscopy, revealing the presence of phenolic acids, polysaccharides, sugars, and triterpenoids in the pulp, high content of unsaturated fatty acids in the seed oil, and significant amounts of phenolics and carotenoids in the seed residue. These results pave the way for a reliable correlation between chemical composition and biological activity, in edible fruit samples.
RESUMEN
Tamarillo (tree tomato) is a subtropical tree that produces edible fruits with health-beneficial properties, since it contains several components with potential therapeutic and chemoprotective activity. The present work reports the first complete vibrational study (Raman and infrared) of this edible fruit. This approach allowed us to determine where the most relevant nutraceutical compounds are located in the fruit, as well as their relative amounts. Particular vibrational signatures were obtained for each part of the fruit, reporting different components for the epicarp (outer and inner sections), the pulp and the seeds, especially regarding the content in phenolic compounds, unsaturated fatty acids/esters and polymeric chains from the cuticular wax. Valuable information, at the molecular level was gathered regarding the nutricional value of tamarillo's fruit, for its different fractions. This is expected to pave the way for its introduction as a promising nutraceutical, based on the potential therapeutic properties of its main components.
Asunto(s)
Suplementos Dietéticos , Frutas , Fenoles , Frutas/química , Fenoles/análisis , VibraciónRESUMEN
This study aimed at the development of improved drugs against human osteosarcoma, which is the most common primary bone tumor in children and teenagers with a low prognosis. New insights into the impact of an unconventional Pd(II) anticancer agent on human osteosarcoma cells were obtained by synchrotron radiation-Fourier transform infrared microspectroscopy and quasi-elastic neutron scattering (QENS) experiments from its effect on the cellular metabolism to its influence on intracellular water, which can be regarded as a potential secondary pharmacological target. Specific infrared biomarkers of drug action were identified, enabling a molecular-level description of variations in cellular biochemistry upon drug exposure. The main changes were detected in the protein and lipid cellular components, namely, in the ratio of unsaturated-to-saturated fatty acids. QENS revealed reduced water mobility within the cytoplasm for drug-treated cells, coupled to a disruption of the hydration layers of biomolecules. Additionally, the chemical and dynamical profiles of osteosarcoma cells were compared to those of metastatic breast cancer cells, revealing distinct dissimilarities that may influence drug activity.
Asunto(s)
Antineoplásicos/farmacología , Ácidos Grasos/metabolismo , Difracción de Neutrones , Osteosarcoma/tratamiento farmacológico , Paladio/farmacología , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Sincrotrones/instrumentación , Neoplasias Óseas/tratamiento farmacológico , Neoplasias Óseas/metabolismo , Neoplasias Óseas/patología , Cisplatino/farmacología , Femenino , Humanos , Osteosarcoma/metabolismo , Osteosarcoma/patología , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Neoplasias de la Mama Triple Negativas/metabolismo , Neoplasias de la Mama Triple Negativas/patología , Células Tumorales CultivadasRESUMEN
We have previously showed that platinum drugs up-regulate SSAT and SMO and down-regulate ODC and SAMDC in the polyamine pathway. Several studies including our own established that platinum drugs combined with polyamine analog DENSPM produces synergistic increase in SSAT activity with polyamine depletion. Since polyamine pathway is an important therapeutic target, we investigated whether agents containing both platinum and polyamines have similar effects on the polyamine pathway. Two complexes i) Pt-spermine with two cisplatin molecules linked to a spermine in the center and ii) Pd-spermine with similar structure i, but Pd (II) substituted for Pt (II) were analyzed with respect to their effect on the expression of genes in polyamine pathway, SSAT and SMO protein expression, SSAT activity and polyamine pools. Pt-, Pd-spermine complexes induced significant down-regulation of SMO, arginase 2 and NRF-2, with no change in SSAT, while cisplatin as a single agent or in combination with DENSPM induced significant up-regulation of SSAT and SMO. The SSAT activity was not induced by either Pt- or Pd-spermine in A2780 cells; SMO protein levels were significantly elevated compared to the no-drug control and to a similar extent as cisplatin/DENSPM. The Pd-spm treatment induced a fall in putrescine levels to 33%, spermidine to 62% and spermine to 72% while Pt-spm did not induce such a decline. Comparative cytotoxicity studies in A2780 cells indicated the potency to be cisplatin> Pd-Spm>Pt-Spm. Although both complexes exhibit a lower potency, the degree of resistance itself is much lower for Pt-spermine and Pd-spermine in that order (2.5 and 7.5, respectively) compared to cisplatin ( approximately 12) as tested in cisplatin resistant A2780/CP cells. These studies suggest that Pd (II)-polyamine complexes may constitute a promising group of inorganic compounds for further studies in the development of novel chemotherapy/adjuvant chemotherapy strategies.