Potential Role of Natural Antioxidant Products in Oncological Diseases

Nutrition has a significant effect and a crucial role in disease prevention. Low consumption of fruit and vegetables and a sedentary lifestyle are closely related with the onset and development of many types of cancer. Recently, nutraceuticals have gained much attention in cancer research due to their pleiotropic effects and relatively non-toxic behavior. In fact, although in the past there have been conflicting results on the role of some antioxidant compounds as allies against cancer, numerous recent clinical studies highlight the efficacy of dietary phytochemicals in the prevention and treatment of cancer. However, further investigation is necessary to gain a deeper understanding of the potential anticancer capacities of dietary phytochemicals as well as the mechanisms of their action. Therefore, this review examined the current literature on the key properties of the bioactive components present in the diet, such as carotenoids, polyphenols, and antioxidant compounds, as well as their use in cancer therapy. The review focused on potential chemopreventive properties, evaluating their synergistic effects with anticancer drugs and, consequently, the side effects associated with current cancer treatments

. Evaluation of the antioxidant and antiproliferative potential properties of phytocomplexes extracted from Mediterranean area fruits

Breast and cervical cancer represents the first and the second cause of death for women worldwide1,2. Therefore, new advanced chemotherapies applications are very urgently needed this cancer. High attention has been paid to natural compounds in fruits and vegetables with potential nutraceutical properties. In this regard, dietary polyphenols have been widely demonstrated to be able to not only reduce oxidative and inflammatory stress, but also decrease proliferation of cancer cells. However, the biological activity of various food plants has not yet been studied. This work aims to characterize the nutraceutical potential of four fruits such as, Malpighia emarginata (MEE), Arbutus unedo (AUE), Goji berries (LBE), Annona cherimola (ACE). For this reason, our study focused on the evaluation of antioxidant potential and antiproliferative activity of polyphenol extracts on cervical cancer (HeLa) and breast cancer (MCF-7) cell line

Synthesis and cytotoxic activity evaluation of 2,3-thiazolidin-4-one derivatives on human breast cancer cell lines

It is well known that resveratrol (RSV) displayed cancer-preventing and anticancer properties but its clinical application is limited because of a low bioavailability and a rapid clearance from the circulation. Aim of this work was to synthesize pharmacologically active resveratrol analogs with an enhanced structural rigidity and bioavailability. In particular, we have synthesized a library of 2,3-thiazolidin-4-one derivatives in which a thiazolidinone nucleus connects two aromatic rings. Some of these compounds showed strong inhibitory effects on breast cancer cell growth. Our results indicate that some of thiazolidin-based resveratrol derivatives may become a new potent alternative tool for the treatment of human breast cancer

Targeting the CaMKII/ERK Interaction in the Heart Prevents Cardiac Hypertrophy

AIMS: Activation of Ca2+/Calmodulin protein kinase II (CaMKII) is an important step in signaling of cardiac hypertrophy. The molecular mechanisms by which CaMKII integrates with other pathways in the heart are incompletely understood. We hypothesize that CaMKII association with extracellular regulated kinase (ERK), promotes cardiac hypertrophy through ERK nuclear localization. METHODS AND RESULTS: In H9C2 cardiomyoblasts, the selective CaMKII peptide inhibitor AntCaNtide, its penetratin conjugated minimal inhibitory sequence analog tat-CN17β, and the MEK/ERK inhibitor UO126 all reduce phenylephrine (PE)-mediated ERK and CaMKII activation and their interaction. Moreover, AntCaNtide or tat-CN17β pretreatment prevented PE induced CaMKII and ERK nuclear accumulation in H9C2s and reduced the hypertrophy responses. To determine the role of CaMKII in cardiac hypertrophy in vivo, spontaneously hypertensive rats were subjected to intramyocardial injections of AntCaNtide or tat-CN17β. Left ventricular hypertrophy was evaluated weekly for 3 weeks by cardiac ultrasounds. We observed that the treatment with CaMKII inhibitors induced similar but significant reduction of cardiac size, left ventricular mass, and thickness of cardiac wall. The treatment with CaMKII inhibitors caused a significant reduction of CaMKII and ERK phosphorylation levels and their nuclear localization in the heart. CONCLUSION: These results indicate that CaMKII and ERK interact to promote activation in hypertrophy; the inhibition of CaMKII-ERK interaction offers a novel therapeutic approach to limit cardiac hypertrophy

An efficient approach for monosulfide bridge formation in solid-phase peptide synthesis

An efficient approach for the synthesis of cyclic peptides containing unnatural thioether side-chain bridges, based on the use of (2S)-9-fluorenylmethyl-2-[(tert-butoxycarbonyl)amino]-4-iodobutanoate and its homologue 5-iodopentanoate, is reported. The synthesis was performed by a tandem combination of solidphase peptide synthesis and microwave-assisted cyclization strateg

A new efficient synthetic methodology for tetrahydroisoquinoline and tetrahydro--carboline derivatives using the Pictet-Spengler reaction

A new solution-phase methodology microwave-assisted for improving the Pictet-Spengler reaction in the synthesis of the tetrahydroisoquinoline and β-carboline derivatives has been reported. This methodology was applied to obtain a small library of tetrahydroisoquinoline and β-carboline derivatives using L-Dopa, dopamine, and tryptophan, as well as a variety of commercially available aldehydes as starting material. The use of such nonconventional reaction conditions reveals several features like a short reaction time compared to conventional eating, ease of isolation of the products after work-up, and improvement of the yields. This new one-pot protocol would be an ideal and rapid method to synthesize compounds in a combinatorial context