Glycolipids from Sargassum filipendula, a Natural Alternative for Overcoming ABC Transporter-Mediated MDR in Cancer.

Chemotherapy is a widely used strategy to treat cancer, a disease that causes millions of deaths each year. However, its efficacy is reduced by the overexpression of ABC transporters, which are proteins that expel the drugs used in chemotherapy and involved in the multidrug resistance (MDR). Glycolipids have been identified as potential inhibitors of ABC transporters. Algae of the genus Sargassum contain high levels of glycolipids, making them a promising therapeutic alternative against the MDR phenotype. Sargassum filipendula glycolipids were obtained by exhaustive maceration with chloroform/methanol, purified by column and thin layer chromatography, and then characterized by FTIR, NMR, and LC-MS. Cell viability by PI labeling and inhibition of ABC transporters were analyzed by flow cytometry. Assessment of resistance reversal was determined by MTT assay. Ten sulfoquinovosylglycerol-type compounds were found, and six of them are reported for the first time. In particular, moiety 4 (GL-4) showed strong and moderate inhibitory activity against ABCC1 and ABCB1 transporters respectively. Treatment of GL-4 in combination with the antineoplastic drug vincristine sensitized Lucena-1 cell model to drug and reversed the MDR phenotype. This is the first report of glycolipids isolated from S. filipendula capable of inhibiting ABC transporters and thus overcoming acquired drug resistance.

Sargassum filipendula, a Source of Bioactive Compounds with Antioxidant and Matrix Metalloproteinases Inhibition Activities In Vitro with Potential Dermocosmetic Application.

The antioxidant and the potential inhibitory capacity of matrix metalloproteinases of the phlorotannin-type polyphenolic and fucoidan-type polysaccharides extracts obtained from the macroalga S. filipendula were evaluated. Through chromatographic and spectroscopic techniques, the corresponding chemical structure of compounds present in the extracts was determined. Antioxidant capacity was evaluated using the methyl linoleate model for the inhibition of lipid peroxidation, and the free radical scavenging capacity was assessed using DPPH, ABTS, •OH, O2•- methods. The matrix metalloproteinase inhibition potential was measured by collagenase and elastase inhibition tests, using epigallocatechin gallate as a positive control. The extracts exhibited a high scavenging capacity of radical species evaluated and inhibition of diene conjugate formation and thiobarbituric acid reactive substances. The results showed that the crude extracts presented dose-dependent collagenase and elastase inhibition, with IC50 values between 0.04 and 1.61 mg/mL. The structure of the residues of the polysaccharide was identified mainly as (1→3)-sulfated (1→3) α-l-fucopyranose at carbon 4 and residues of ß-d-glucopyranose, α-d-Mannopyranose, and ß-d-Galactopyranose, while in the polyphenol extract the presence of phloroglucinol was identified and the presence of eckol, bifuhalol, and trifuhalol was suggested. Our results allow us to infer that S. filipendula is a potential source of bioactive ingredients with antioxidant and anti-aging activity.

Anticancer and Antioxidant Activity of Water-Soluble Polysaccharides from Ganoderma aff. australe against Human Osteosarcoma Cells.

Wild mushrooms have gained great importance for being a source of biologically active compounds. In this work, we evaluate the anticancer and antioxidant activity of a water-soluble crude polysaccharide extract isolated from the fruiting bodies of the Ganoderma aff. australe (GACP). This mushroom was collected in San Mateo (Boyacá, Colombia) and identified based on macroscopic and microscopic characterization. GACP was characterized by UV-Vis spectroscopy, Fourier-transform infrared spectroscopy, high-performance liquid chromatography-diode array detector, and nuclear magnetic resonance. The antiradical and antioxidant activity were evaluated by different methods and its anticancer activity was verified in the osteosarcoma MG-63 human cell line. Chemical and spectroscopic analysis indicated that GACP consisted of ß-D-Glcp-(1→, →3)-ß-D-Glcp-(1→ and α-D-Glcp-(1→ residues. The results of the biological activity showed that GACP exhibited high antioxidant activity in the different methods and models studied. Moreover, the results showed that GACP impaired cell viability (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay) and cell proliferation (clonogenic assay) in a dose-response manner on MG-63 cells. The findings of this work promote the use of mushroom-derived compounds as anticancer and antioxidant agents for potential use in the pharmaceutical and food industries.

Lentinula edodes, a Novel Source of Polysaccharides with Antioxidant Power.

The fruiting bodies of edible mushrooms represent an important source of biologically active polysaccharides. In this study, Lentinula edodes crude polysaccharides (LECP) were extracted in hot water, and their antioxidant and antiradical activities were investigated. The antioxidant activity of LECP was investigated against reactive species such as 1,1'-diphenyl-2-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid, hydroxyl and superoxide anion radicals, reducing power with EC50 values of 0.51, 0.52, 2.19, 3.59 and 1.73 mg/mL, respectively. Likewise, LECP inhibited the lipid peroxidation induced in methyl linoleate through the formation of conjugated diene hydroperoxide and malondialdehyde. The main sugar composition of LECP includes mannose, galactose, glucose, fucose and glucuronic acid. Characterization by Fourier transform infrared spectroscopy and nuclear magnetic resonance determined that LECP was made up of α and ß glycosidic bonds with a backbone of α-D-Glc, →6)-ß-D-Glcp-(1→, →6)-α-D-Galp-(1→ and ß-D-Manp-(1→ residues. The results showed that LECP can scavenge all reactive species tested in a concentration-dependent manner and with a protective effect in the initial and final stages of lipid peroxidation. The natural antioxidant activity of the LECP that was investigated strengthens the high medicinal and nutritional value of this mushroom.

Algae Metabolites as an Alternative in Prevention and Treatment of Skin Problems Associated with Solar Radiation and Conventional Photo-protection

Abstract The histological structure and biochemistry of the skin is affected by solar radiation having adverse effects ranging from sunburns, premature aging that includes wrinkles, spots, dryness, and loss of collagen to cancer development. The skin has defense mechanisms to prevent damage caused by radiation, but when radiation exposure is excessive these mechanisms are not strong enough to protect the skin. The use of sunscreen is the most common practice of photo- protection. The active ingredients of these cosmetic protective formulations are generally from synthetic origin and have presented several drawbacks at the level of photo-stability, systemic absorption and can generate contact and photo-contact dermatitis. This review illustrates skin solar radiation problems, common sunscreen ingredients limitation and mentions how algae can be an alternative according to studies that have evaluated the photo-protective potential of extracts and compounds isolated by different techniques.

Effect of isoespintanol isolated from Oxandra cf. xylopioides against DNA damage of human lymphocytes.

Synthetic antioxidants are used in the food and pharmaceutical industry, however, there is concern about their safety; this has prompted the search for new antioxidants that are effective, safe and act at low concentrations. The objective of this study is to evaluate the oxygen radical scavenging capacity and clastogenic effect of the Isoespintanol /2-isopropyl-3,6-dimethyl-5-methylphenol) in DNA of human lymphocyte compared with the BHA (Butylated hydroxyanisole). The oxygen radical scavenging ability was evaluated by methods ORACFL and ORACPGR, genotoxicity was determined by comet assay and data analysis was performed using ANOVA and Duncan test. The results show that the oxygen radical scavenging capacity of the BHA is higher than Isoespintanol, however according to the reactivity concept proposed by Lopez-Alarcon and Lissi, the Isoespintanol it is more reactive than BHA. Furthermore, according to some studies, BHA presented adverse effects on the health of consumers. Comet assay results revealed that at concentrations between 3 and 1620 µM the Isoespintanol don't show clastogenic effects on DNA. In conclusion, the antioxidant capacity for the BHA is higher than Isoespintanol, but considering reactivity concepts proposed by López-Alarcon and Lissi, the Isoespintanol is faster to neutralize radicals that the BHA, furthermore, according to the National Institute of Health "BHA" is a human carcinogen.

In vitro UV absorption properties and radical scavenging capacity of Morella parvifolia (Benth. ) Parra-Os. extracts

The goal of this research was to identify major compounds of the aerial parts of M. parvifolia (Benth.) Parra-Os., that could enhance its possible application as additive in dermocosmetic products, as well as evaluate the antioxidant properties. The extracts agreed with the broad-spectrum UVB/UVA absorption detected and could act as broad-spectrum sunscreens, covering the UVA and UVB range. Methanolic extracts showed an important antiradical capacity (0.46 and 0.47 g/µmol DPPH), TPC (37.58 and 51.41mg GAE/g DS) and TAC (1.12 and 3.31 mg C3GE/g DS) in fruits and leaves, respectively. M. parvifolia could be considered as a prospective source of natural UV-radiation absorbers with antioxidant capacity. Although the results have clearly demonstrated the potential photoprotection capacity, more studies are needed to enhance its application as an additive in pharmaceutical and medicinal formulations.

Correlación del contenido de fenoles y antocianinas con la capacidad antioxidante Syzygium cumini (L. ) Skeels, (jambolan) / Phenol and anthocyanin content and correlation with the antioxidant capacity of Syzygium cumini (L.) Skeels, (jambolan)

Introducción: la especie Syzygium cumini (L.) Skeels, (jambolam), sin. Eugenia jambolana L, es una planta rica en metabolitos secundarios con un elevado potencial biológico, medicinal, entre otros y que pueden estar asociados con las propiedades terapéuticas reportadas para S. cumini. Objetivo: comparar capacidad antioxidante de extractos del fruto, pulpa y semilla de S. cumini, con respecto al contenido de polifenoles y antocianinas. Métodos: fruto, pulpa y semillas S. cumini deshidratados y macerados se sometieron a extracción sólido-líquido; el contenido de fenoles se evaluó por el método de Folin-Ciocalteu, el de antocianinas por el método de diferencial de pH y el potencial antioxidante in vitro se evaluó con base en los métodos del radical estable 1,1-difenil­2-picrilhidracil, el radical catión 2,2´-azino-bis(3-etilbenzotiazolin-6-sulphonic ácido) y poder antioxidante de reducción del ion férrico. Resultados: el contenido de fenoles obtenidos tanto en los extractos metanólicos como etanólicos fue muy similar en fruto y pulpa, mientras que en las semillas se observó un incremento hasta 5 veces con respecto a la pulpa, presentó correlación con el efecto de protección antioxidante entre los extractos evaluados. Conclusiones: la elevada presencia de fenoles determinada en todos los extractos afectó de manera positiva la capacidad protectora contra radicales libres, y los frutos de S. cumini, podrían ser considerados como una fuente potencial de compuestos biaoctivos con aplicaciones terapéuticas(AU)

Introduction: Syzygium cumini (L.) Skeels, (jambolam), sin. Eugenia jambolana L, is considered as a source of secondary metabolites with a biological and medicinal potential and these can be associated with its therapeutics properties. Objetive: to correlated the content of polyphenols and anthocyanins with antioxidant capacity in ethanolic and methanolic extracts of S. cumini. Methods: dehydrated and powered fruits, pulp and seeds of S. cumini was subjected to solid-liquid extraction. Total phenolis content was determined by Folin-Cicoulteau method, anthocyanin content was determined by the pH differential method and the potential antioxidant was evaluated using 1,1-difenil­2-picrilhidracil radical stable, 2,2´-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical cation and ferric reducing/antioxidant power tests. Results: all extracts showed an important correlation between total phenolis content and antioxidant capacity values, however, in the seed total phenolis content was almost 5 times higher than that obtained in fruit and pulp. Conclusions: all extracts exhibited a considerable antioxidant potential against free radical, and S. cumini could be used as an alternative source of natural bioactive compounds with application in therapeutic research area(AU)

Estudio de la capacidad antioxidante in vitro de Phaseolus vulgaris L. (frijol) mediante extracción asistida por microondas / Study of in vitro antioxidant capacity of Phaseolus vulgaris L. (frijol) by microwave assisted extraction

Introducción: Phaseolus vulgaris L. (frijol) es una fuente nutricional importante en Colombia, que aporta un gran contenido de sustancias bioactivas con potencial benéfico para la salud, tales como polifenoles, entre otras, que contribuyen de manera sinérgica con sus propiedades terapéuticas, y que pueden tener un efecto positivo contra algunas patologías. Objetivos: evaluar el método de extracción asistido por microondas como método alternativo para estudiar la capacidad antioxidante in vitro en ocho variedades de P. vulgaris L. cultivadas en Colombia. Métodos: semillas sin piel de P. vulgaris, deshidratadas y maceradas se sometieron a extracción asistida por microondas y extracción sólido-líquido; el contenido de fenoles se evaluó por el método de Folin-Ciocalteu y el potencial antioxidante in vitro se evaluó con base en los métodos del radical estable catión radical difenil-picrilhidrazilo y el radical catión 2,2´-azino-bis(ácido 3-etilbenzotiazolin-6-sulfunico). Resultados: el método de extracción asistido por microondas realizada en horno microondas convencional fue más eficiente respecto a la convencional ya que disminuyó la cantidad de solvente, de muestra empleada y los tiempos de extracción. Los extractos obtenidos por extracción asistida por microondas en horno microndas convencional presentaron un contenido de fenoles entre 29,36 y 60,61 g EAG/L, mientras que el método extracción sólido-líquido, estuvo entre 32,75 y 113,27 g EAG/L. El efecto anti-radicalario fue similar entre los extractos evaluados. Conclusiones: todos los extractos presentaron buena capacidad protectora contra radicales libres, y la técnica de extracción asistida por microondas en horno microndas convencional puede ser usada como método alterno para una valoración rápida, eficiente y eficaz del contenido de sustancias bioactivas en diferentes matrices, se presentó mínimas diferencias entre los resultados obtenidos, comparados con las metodologías de extracción asistida por microondas establecidas antes(AU)

Introduction: Phaseolus vulgaris L. is a representative crop of nutrient and economic importance in Colombia. Additionally, P. vulgaris is considered as a natural source of bioactives compounds, such as polyphenols, which have been associated with valuable effects on health. Objetives: to evaluate the microwave extraction assisted technique as an alternative methodology to study the antioxidant capacity of eight varieties of P. vulgaris cultivated in Colombia. Methods: dehydrated and powered seeds of P. vulgaris was subjected to microwave assisted extraction and solid-liquid extraction and. Total phenolis content was determined by Folin-Cicoulteau method and the potential antioxidant was evaluated using diphenyl-picrylhydrazyl radical stable and 2,2-Azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical cation assays. Results: microwave assisted extraction-Household microwave oven technique was more efficient and versatile than SLE method. The extracts obtained microwave assisted extraction-Household microwave oven methodology showed polyphenol content ranged between entre 29,36 and 60,61 g EGA/L, but SLE was over 32,75 and 113,27 g EAG/L. Conclusions: all extracts showed a considerable antioxidant potential against free radical, and microwave assisted extraction-Household microwave oven method could be used as an alternative method for fast, efficient and effective evaluation of the content of polyphenol in various matrices, with minimal differences comparing to established microwave assisted extraction techniques(AU)