Antiproliferative and antioxidant effects on breast cancer cells of oleuropein and its semisynthetic peracetylated derivatives

Bulotta, Stefania; Corradino, Rosanna; Celano, Marilena; D’Agostino, Massimo; Maiuolo, Jessica; Oliverio, Manuela; Procopio, Antonio; Iannone, Michelangelo; Rotiroti, Domenicantonio; Russo, Diego

doi:10.1016/j.foodchem.2011.02.025

Cited by 93 publications

(65 citation statements)

References 33 publications

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“…Recent reports [24] have suggested the potential improvements concerning the OLE effect by protecting the molecule through its peracetylation. In previous studies, we have shown that Ac-OLE has a stronger anti-proliferative effect than OLE in the experimental models of tumor cells in vitro [8,9] . Also in a very recent study, we demonstrate the beneficial effects of Ac-OLE at the same dose (20 mg/kg/day) in the prevention of hepatic steatosis, hyperinsulinemia and weight gain in mice fed with high fat cafeteria diet [25] .…”

Section: Discussionmentioning

confidence: 96%

“…Due to their health benefits, oleuropein, oleuropein derivatives, and seco-phenolic compounds are all considered to be important elements that make extra virgin olive oil a staple part of the Mediterranean diet. Also, the compounds include the ability to scavenge reactive oxygen species (ROS) [5][6][7] , to inhibit the proliferation of several tumor cell lines [5,[8][9][10][11] , and also to protect against cardiovascular diseases [3,[12][13][14][15] and metabolic disorders as Diabetes mellitus [16][17][18][19] . In addition, they are effective in experimental models of age-related disorders, such as neurodegenerative diseases [14,20,21] .…”

Section: Introductionmentioning

confidence: 99%

“…By using an innovative extractive method that employs renewable sources of primary matter and adopts sustainable synthetic strategies, we obtained OLE and some acetylated derivatives in good yields and very mild conditions [22,23] ; interestingly, the latter compounds have shown an improved capacity to permeate the molecular membrane, in addition to their 'drug likeness' [22] . Moreover, we have recently demonstrated that peracetylated oleuropein (Ac-OLE) possesses in vitro an antioxidant and a growth-inhibitory activity that is even stronger than OLE when acting against both breast and thyroid cancer cell lines [8,9] . While the absence of toxicity of oleuropein is well established [1,5,11] , very little is known about the in vivo effects of its peracetylated derivative.…”

Section: Introductionmentioning

confidence: 99%

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Safety evaluation of subchronic oral administration of Oleuropein and its semisynthetic peracetylated derivative

Russo¹

2016

JPP

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Olive leaf extracts are a natural source of phenolic compounds; this includes secoiridoid oleuropein (OLE), which has been widely investigated for its beneficial health effects. Previous in vitro studies have revealed antiproliferative and antioxidant activity in peracetylated oleuropein that is even stronger than oleuropein itself. The aim of the present study was to evaluate the effect of the subchronic administration of oleuropein, and for the first time, also evaluate its semisynthetic peracetylated derivative (peracetylated oleuropein, Ac-OLE). OLE and Ac-OLE were orally administered to male C57BL/6JOlaHsd mice at doses of 20 mg/kg/day for 15 weeks. In comparison to the control group, there were no treatment-related clinical signs of toxicity, nor were there any changes to note in body weight, food consumption, hematological and clinical chemistry parameters, or liver weight. Moreover, the histological examination of the liver, kidney, and lungs did not reveal any morphological alterations. These findings demonstrate that no adverse effects may be attributed to the subchronic oral administration of 20 mg/kg/day of Ac-OLE. However, additional experiments are necessary to clarify the action of the peracetylated compound in light of its therapeutic use.

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Section: Discussionmentioning

confidence: 96%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Safety evaluation of subchronic oral administration of Oleuropein and its semisynthetic peracetylated derivative

Russo¹

2016

JPP

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“…Moreover, it has been shown that HT inhibits proliferation of human MCF-7 breast cancer cells (Siriani et al, 2010;Bulotta et al 2011;Bouallagui et al, 2011a), human HT29 colon carcinoma cells (Guichard et al, 2006), human M14 melanoma cells (D'Angelo et al, 2005) and human PC3 prostate cells (Quiles et al, 2002).…”

Section: Anticancer Activitymentioning

confidence: 99%

Biological Properties of Hydroxytyrosol and Its Derivatives

Fernandez‐Bolanos¹,

López²,

López-García³

et al. 2012

Olive Oil - Constituents, Quality, Health Properties and Bioconversions

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“…Hydroxytyrosol has the capacity to scavenge peroxyl radicals, which inhibits the oxidation of low-density lipoproteins (LDL), and carries cholesterol (LDL-C), a fundamental stage in the emergence of atherosclerosis and other cardiovascular diseases (Vázquez-Velasco et al 2011). Moreover, this compound may produce a proapoptotic effect intervening in the expression of genes related to the tumor cell propagation of promyelocytes (HL60 cells) (Fabiani et al 2011), as well as the inhibition of the development of some carcinogenic human cells (Bouallagui et al, 2011;Bulotta et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Comparison between different liquid-liquid and solid phase methods of extraction prior to the identification of the phenolic fraction present in olive oil washing wastewater from the two-phase olive oil extraction system

2017

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SUMMARY:Phenolic compounds from olive mill wastewater (OMW), are characterized by a strong antioxidant activity. At the same time, they represent an environmental problem because they are difficult to degrade. The purpose of this work was to identify these biologically active compounds in the OMW from two-phase olive oil production in order to convert a polluting residue into a source of natural antioxidants. After optimizing the extraction process of phenolic compounds using liquid-liquid extraction (LLE) and solid phase extraction (SPE) methods, it was determined that the most appropriate sequence comprised a previous centrifugation to remove the lipid fraction, followed by liquid extraction with ethyl acetate or SPE. The most important compounds identified in olive oil washing wastewater (OOWW) were tyrosol, hydroxytyrosol and succinic acid; whereas the ones in the wastewater derived from the washing of the olives (OWW) were cresol, catechol, 4-methylcatechol, hydrocinnamic acid and p-hydroxy-hydrocinnamic acid. KEYWORDS: Antioxidants; Ethyl acetate; Extraction; Hydroxytyrosol; Olive oil wastewater; PolyphenolsRESUMEN: Comparación entre métodos de extracción líquido-líquido y en fase sólida previos a la identificación de la fracción fenólica presente en las aguas residuales procedentes del lavado del aceite de oliva obtenido mediante el sistema de extracción de aceite de oliva en dos fases. Los compuestos fenólicos presentes en las aguas residuales de la industria oleícola (OMW) se caracterizan por una gran actividad antioxidante. Por otra parte, suponen un problema medioambiental debido a que son difíciles de degradar. El objetivo de este trabajo fue la identificación de estos compuestos biológicamente activos que se encuentran en las OMW generadas del proceso de obtención del aceite de oliva por el sistema de dos fases, para así convertir un residuo contaminante en una fuente de antioxidantes naturales. Tras optimizar el proceso de extracción de los compuestos fenólicos utilizando extracción líquido-líquido (LLE) y extracción en fase sólida (SPE), se obtuvo que la secuencia más apropiada comprendió una centrifugación previa para eliminar la fracción lipídica, seguida de una extracción líquida con acetato de etilo o una SPE. Los compuestos más importantes identificados en las aguas residuales del lavado del aceite de oliva (OOWW) fueron tirosol, hidroxitirosol y el ácido succínico, mientras que los de las aguas residuales derivadas del lavado de las aceitunas (OWW) fueron cresol, catecol, 4-metilcatecol, ácido hidrocinámico y ácido p-hidroxi-hidrocinámico.

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Antiproliferative and antioxidant effects on breast cancer cells of oleuropein and its semisynthetic peracetylated derivatives

Cited by 93 publications

References 33 publications

Safety evaluation of subchronic oral administration of Oleuropein and its semisynthetic peracetylated derivative

Safety evaluation of subchronic oral administration of Oleuropein and its semisynthetic peracetylated derivative

Biological Properties of Hydroxytyrosol and Its Derivatives

Comparison between different liquid-liquid and solid phase methods of extraction prior to the identification of the phenolic fraction present in olive oil washing wastewater from the two-phase olive oil extraction system

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