RESUMEN
The soybean-derived protease inhibitor, Bowman-Birk inhibitor (BBI), is currently showing great promise as a novel cancer chemopreventive agent. In contrast to the wealth of research conducted on this compound, the anticancer effects of protease inhibitors isolated from other leguminous sources have received limited attention. In the current study, 7 protease inhibitor concentrates (PICs) were isolated from various leguminous sources (including soybean) and characterized. The effects of PICs on the proliferation of breast and prostate cancer cells were investigated in vitro. Chickpea PIC significantly inhibited the viability of MDA-MB-231 breast cancer and PC-3 and LNCaP prostate cancer cells at all concentrations tested (25-400 µg/ml). In addition, kidney bean (200, 400 µg/ml), soybean (50, 100 µg/ml), and mungbean (100, 200 µg/ml) PICs inhibited LNCaP cell viability. These findings suggest that leguminous PICs may possess similar anticancer properties to that of soybean BBI and deserve further study as possible chemopreventive agents.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Cicer/metabolismo , Descubrimiento de Drogas , Proteínas de Plantas/farmacología , Neoplasias de la Próstata/tratamiento farmacológico , Inhibidores de Proteasas/farmacología , Antineoplásicos Fitogénicos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Quimotripsina/antagonistas & inhibidores , Fabaceae/metabolismo , Femenino , Humanos , Masculino , Peso Molecular , Concentración Osmolar , Péptidos/química , Péptidos/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Proteínas de Plantas/química , Inhibidores de Proteasas/química , Inhibidores de Serina Proteinasa/química , Inhibidores de Serina Proteinasa/farmacologíaRESUMEN
The importance of honey for medicinal purposes is well documented in some of the world's oldest literature. Honey is well known and studied for its antimicrobial properties. The medicinal properties in honey originate from the floral source used by bees. Manuka honey is a dark monofloral honey rich in phenolic content, and currently it is gaining much attention for its antimicrobial activity. Researchers have found that honey is effective against a wide range of pathogens. The antibacterial potency of Manuka honey was found to be related to the Unique Manuka Factor (UMF) rating, which is correlated with the methylglyoxal and total phenols content. It is reported that different types of Manuka honey have differing effects and Gram-negative bacteria are more resistant than Gram-positive bacteria. Bacterial resistance to honey as antimicrobial agent has yet to be identified, possibly due to the presence of a complex mixture of methylglyoxal and other components. Honey is also reported to alter a bacterium's shape and size through septal ring alteration, which affects cell morphology and growth. Research has shown that Manuka honey of different UMF values has medicinal properties of interest and it can be beneficial when used as a combination treatment with other antimicrobial agents.
RESUMEN
Cucurbitaceae are one of most widely used plant species for human food but lesser known members have not been examined for bioactive components. The purpose of this study was to evaluate the antioxidant and genoprotective activities from three cucurbitaceae seeds extracts and to identify phenolic components by LC-ESIMS/MS analysis. From the results, the yield of seeds extract was 20-41% (w/w) and samples had 16-40% total phenols as gallic acid equivalents (GAE). Compared with methanol solvent, using acidified methanol led to increased extraction yield by 1.4 to 10-fold, higher phenolic content (149.5 ± 1.2 to 396.4 ± 1.9 mg GAE/g), higher DPPH radical quenching and enhanced genoprotective activity using the pBR322 plasmid assay. LC-ESI-MS/MS analysis led to identification of 14-17 components, based on authentic standards and comparison with literature reports, as mainly phenolic acids and esters, flavonol glycosides. This may be the first mass spectrometric profiling of polyphenol components from cucurbitaceae seeds.
Asunto(s)
Antimutagênicos/análisis , Antioxidantes/análisis , Cucurbitaceae/química , Fenoles/análisis , Extractos Vegetales/química , Semillas/química , Cromatografía Liquida , Daño del ADN/efectos de los fármacos , Flavonoles/análisis , Humanos , Extractos Vegetales/farmacología , Polifenoles/análisis , Espectrometría de Masas en TándemRESUMEN
The ferric reducing antioxidant power (FRAP) assay was recently adapted to a microplate format. However, microplate-based FRAP (mFRAP) assays are affected by sample volume and composition. This work describes a calibration process for mFRAP assays which yields data free of volume effects. From the results, the molar absorptivity (ε) for the mFRAP assay was 141,698 M(-1) cm(-1) for gallic acid, 49,328 M(-1) cm(-1) for ascorbic acid, and 21,606 M(-1) cm(-1) for ammonium ferrous sulphate. The significance of ε (M(-1) cm(-1)) is discussed in relation to mFRAP assay sensitivity, minimum detectable concentration, and the dimensionless FRAP-value. Gallic acid showed 6.6 mol of Fe(2+) equivalents compared to 2.3 mol of Fe(+2) equivalents for ascorbic acid. Application of the mFRAP assay to Manuka honey samples (rated 5+, 10+, 15+, and 18+ Unique Manuka Factor; UMF) showed that FRAP values (0.54-0.76 mmol Fe(2+) per 100g honey) were strongly correlated with UMF ratings (R(2)=0.977) and total phenols content (R(2) = 0.982)whilst the UMF rating was correlated with the total phenols (R(2) = 0.999). In conclusion, mFRAP assay results were successfully standardised to yield data corresponding to 1-cm spectrophotometer which is useful for quality assurance purposes. The antioxidant capacity of Manuka honey was found to be directly related to the UMF rating.