Maria Sinicropi - Academia.edu (original) (raw)
Papers by Maria Sinicropi
The synthesis and activity of 1,3-indandione derivatives as acetylcholinesterase (AChE) inhibitor... more The synthesis and activity of 1,3-indandione derivatives as acetylcholinesterase (AChE) inhibitors are reported. The synthetic key-step consists of the Knovenagel olefination between 1,3-indandione and a substituted (1-benzylpiperidin-4-yl)methanal followed by selective double bond reduction. AChE inhibitory activity was measured by a quick fluorimetric method. One of the new compounds showed a significant interaction with the enzyme. Molecular modelling studies were performed in order to propose the binding modes within the AChE gorge compared to the known inhibitor Donepezil.
Corrigendum to “Inhibition of human topoisomerase I and II and anti-proliferative effects on MCF-7 cells by new titanocene complexes” [Bioorg. Med. Chem. 23 (2015) 7302–7312]
Bioorganic & Medicinal Chemistry, 2015
Synthesis and x-ray analysis of the dirhodium (II, II) carboxylate complex Rh2 (O2CCH3) 4 (formH) 2 (form H= N, N'-di-p-tolylformamidine)
Inorganica Chimica …, 1994
... D. [14]. M. Nardelli. Comput. Chem. 7 (1983), p. 95 version locally modified. Abstract | PDF ... more ... D. [14]. M. Nardelli. Comput. Chem. 7 (1983), p. 95 version locally modified. Abstract | PDF (390 K) | View Record in Scopus | Cited By in Scopus (1365). [15]. DM Grove, G. van Koten, HJC Ubbels, K. Vrieze, LC Niemann and CH Stam. J. Chem. Soc., Dalton Trans. (1986), p. 717. ...
International Journal of Molecular Sciences
Resveratrol (3,5,4′-trihydroxystilbene; RSV) is a natural nonflavonoid polyphenol present in many... more Resveratrol (3,5,4′-trihydroxystilbene; RSV) is a natural nonflavonoid polyphenol present in many species of plants, particularly in grapes, blueberries, and peanuts. Several in vitro and in vivo studies have shown that in addition to antioxidant, anti-inflammatory, cardioprotective and neuroprotective actions, it exhibits antitumor properties. In mammalian models, RSV is extensively metabolized and rapidly eliminated and therefore it shows a poor bioavailability, in spite it of its lipophilic nature. During the past decade, in order to improve RSV low aqueous solubility, absorption, membrane transport, and its poor bioavailability, various methodological approaches and different synthetic derivatives have been developed. In this review, we will describe the strategies used to improve pharmacokinetic characteristics and then beneficial effects of RSV. These methodological approaches include RSV nanoencapsulation in lipid nanocarriers or liposomes, nanoemulsions, micelles, insertion ...
Journal of enzyme inhibition and medicinal chemistry, 2018
Synthetic or natural carbazole derivatives constitute an interesting class of heterocycles, which... more Synthetic or natural carbazole derivatives constitute an interesting class of heterocycles, which showed several pharmaceutical properties and occupied a promising place as antitumour tools in preclinical studies. They target several cellular key-points, e.g. DNA and Topoisomerases I and II. The most studied representative, i.e. Ellipticine, was introduced in the treatment of metastatic breast cancer. However, because of the onset of dramatic side effects, its use was almost dismissed. Many efforts were made in order to design and synthesise new carbazole derivatives with good activity and reduced side effects. The major goal of the present study was to synthesise a series of new N-thioalkylcarbazole derivatives with anti-proliferative effects. Two compounds, 5a and 5c, possess an interesting anti-proliferative activity against breast and uterine cancer cell lines without affecting non-tumoural cell lines viability. The most active compound (5c) induces cancer cells death triggering...
Molecules (Basel, Switzerland), Jan 30, 2018
Despite the progress achieved by anti-retroviral drug research in the last decades, the discovery... more Despite the progress achieved by anti-retroviral drug research in the last decades, the discovery of novel compounds endowed with selective antiviral activity and reduced side effects is still a necessity. At present, the most urgent requirement includes the improvement of HIV (Human Immunodeficiency Virus) prevention and sexual transmission and the development of new drugs to treat the chronic lifelong infection. Six chloro-1,4-dimethyl-9-carbazoles (,-,) have been prepared following opportunely modified known chemical procedures and tested in luciferase and β-galactosidase expressing CD4⁺, CXCR4⁺, CCR5⁺ TZM-bl cells. a preliminary biological investigation on the synthesized small series of chloro-1,4-dimethyl-9-carbazoles has been carried out. Among all tested compounds, a nitro-derivative () showed the most interesting profile representing a suitable lead for the development of novel anti-HIV drugs.
New insights for the use of quercetin analogs in cancer treatment
Future medicinal chemistry, Nov 1, 2017
Quercetin (Q1) is a flavonoid widely present in plants and endowed with several pharmacological p... more Quercetin (Q1) is a flavonoid widely present in plants and endowed with several pharmacological properties mostly due to its antioxidant potential. Q1 shows anticancer activity and could be useful in cancer prevention. On the other hand, Q1 is poorly soluble in water and unstable in physiological systems, and its bioavailability is very low. A small set of Q1 derivatives (Q2-Q9) has been synthesized following opportunely modified chemical procedures previously reported. Anticancer activity has been evaluated by MTT assay. Human Topoisomerases inhibition has been performed by direct enzymatic assays. Apoptosis has been evaluated by TUNEL assay. ROS production and scavenging activity have been determined by immunofluorescence. The anticancer profile of a small library of Q1 analogues, in which the OH groups were all or partially replaced with hydrophobic functional groups, has been evaluated. Two of the studied compounds demonstrated an interesting cytotoxic profile in two breast canc...
Novel Au and Ag carbene complexes exert anti-tumor effects triggering the ROS-dependent intrinsic apoptotic pathway
ChemMedChem, Dec 9, 2017
Cisplatin and other platinum-based drugs are well-known valid anticancer drugs. However, during t... more Cisplatin and other platinum-based drugs are well-known valid anticancer drugs. However, during the chemotherapy, the presence of numerous side effects and the onset of frequent phenomena of resistance pushes forward many research groups to devise new metal-based compounds holding improved anticancer properties and lower undesired effects. Amongst the variety of synthesized compounds, significant anti-proliferative effects were obtained employing organometallic compounds, particularly those based on silver or gold. With this in mind, we have synthesized four compounds, two silver- and two gold-complexes, with good inhibitory effects on the in vitro proliferation of breast and ovarian cancer cells models. The most active compound, i.e. AuL4, possess a 9-fold higher antitumor activity compared to cisplatin and induced dramatic morphological changes in HeLa cells. AuL4 induces PARP-1 cleavage, caspases 3/7 and 9 activation, mitochondria disruption, cytochrome c release in cancer cell c...
International Journal of Environmental Research and Public Health
Molecules, 2017
N-Palmitoyl-ethanolamine (PEA) is an anti-inflammatory component of egg yolk that is usually empl... more N-Palmitoyl-ethanolamine (PEA) is an anti-inflammatory component of egg yolk that is usually employed for the prevention of respiratory apparatus virus infection and then frequently used for its efficient anti-inflammatory and analgesic effects in experimental models of visceral, neuropathic, and inflammatory diseases. Nevertheless, data of its use in animal or human therapy are still scarce and further studies are needed. Herein, we report the biological evaluation of a small library of N-palmitoyl-ethanolamine analogues or derivatives, characterized by a protected acid function (either as palmitoyl amides or hexadecyl esters), useful to decrease their hydrolysis rate in vitro and prolong their biological activity. Two of these compounds-namely phenyl-carbamic acid hexadecyl ester (4) and 2-methyl-pentadecanoic acid (4-nitro-phenyl)-amide (5)-have shown good anti-inflammatory and antioxidant properties, without affecting the viability of J774A.1 macrophages. Finally, crystals suitable for X-ray analysis of compound 4 have been obtained, and its solved crystal structure is here reported. Our outcomes may be helpful for a rational drug design based on new PEA analogues/derivatives with improved biological properties.
Role of Calabrian Black Rice in Metabolic Syndrome: in vitro Evaluation of Oryza Sativa L. Indica biological properties
Current Nutrition & Food Science, 2017
Metabolic Syndrome is becoming more common and it is characterized by an excess intake of energy,... more Metabolic Syndrome is becoming more common and it is characterized by an excess intake of energy, readily available carbohydrates and fats that result in postprandial hyperglycemia and hyperlipidemia. In the treatment of Metabolic Syndrome, a diet characterized by functional food, high fiber intake and low glycemic index is recommended. The aim of this research was to study, in vitro, the beneficial and biological properties of black rice cultivated in Sibari plain, a particular area of the region of Calabria, and verify if the climatic conditions of this area influence the composition of this pigmented rice. The antioxidant activity was investigated by performing the DPPH radical scavenging assay, while the free phenolic content of CBR extract was measured by Folin Ciocalteu’s assay and the obtained results were expressed as mg of gallic acid equivalent/mg of extract. In order to establish the anti-inflammatory effect of CBR extract, its reactivity towards nitric oxide (NO) was evaluated, while, its anti-hypertensive activity was studied by determining the ACE activity inhibition. CBR extract also suppresses pancreatic lipase activity with an IC50 value of 34.3 μg/ml and it decreases cellular lipid accumulation by about 60%. Finally, its hypoglycemic effect was evaluated by measuring the inhibiting activity towards α-glucosidase and α-amylase enzymes. The obtained results demonstrate that this kind of black rice owns different beneficial properties, which make it a functional food that could improve metabolic disorders of MS.
Drug delivery, 2017
Sericin is a natural protein that has been used in biomedical and pharmaceutical fields as raw ma... more Sericin is a natural protein that has been used in biomedical and pharmaceutical fields as raw material for polypeptide-based drug delivery systems (DDSs). In this paper, it has been employed as pharmaceutical biopolymer for the production of sunitinib-polypeptide conjugate. The synthesis has been carried out by simple click reaction in water, using the redox couple l-ascorbic acid/hydrogen peroxide as a free radical grafting initiator. The bioconjugate molecular weight (50 kDa < Mw < 75 kDa) was obtained by SDS-PAGE, while the spectroscopic characteristics have been studied in order to reveal the presence of grafted sunitinib. In both FT-IR and UV/Vis spectra, signals corresponding to sunitinib functional groups have been identified. Since sunitinib is an anticancer drug characterized by low bioavailability and low permeability, the bioconjugation aimed at their enhancement. In vitro studies demonstrated that bioavailability has been increased to almost 74%, compared with com...
Molecules, 2017
The quest for alternative drugs with respect to the well-known cis-platin and its derivatives, wh... more The quest for alternative drugs with respect to the well-known cis-platin and its derivatives, which are still used in more than 50% of the treatment regimens for patients suffering from cancer, is highly needed. In this context, organometallic compounds, which are defined as metal complexes containing at least one direct covalent metal-carbon bond, have recently been found to be promising anticancer drug candidates. A series of new metallocene complexes with scandium, yttrium, and neodymium have been prepared and characterized. Some of these compounds show a very interesting anti-proliferative activity in triple negative breast cancer cell line (MDA.MB231) and the non-hormone sensitive prostate cancer cell line (DU145). Moreover, the interaction of some of them with biological membranes, evaluated using liposomes as bio-membrane mimetic model systems, seems to be relevant. The biological activity of these compounds, particularly those based on yttrium, already effective at low concentrations on both cancer cell lines, should be taken into account with regard to new therapeutic approaches in anticancer therapy.
Old Drug Scaffold, New Activity: Thalidomide Correlated Compounds Exerting Different Effects on Breast Cancer Cell Growth and Progression
ChemMedChem, 2017
Thalidomide was first used for relief of morning sickness in pregnant women and then withdrawn fr... more Thalidomide was first used for relief of morning sickness in pregnant women and then withdrawn from the market because of its dramatic effects on normal fetal development. Over the last decades, it has been used successfully for the treatment of several pathologies, including cancer. Many analogues with improved activity have been synthesized and tested. Herein we report some effects on the growth and progression of MCF-7 and MDA-MB-231 breast cancer cells by a small series of thalidomide-correlated compounds, which are very effective at inducing cancer cell death by triggering TNFα-mediated apoptosis. The most active compounds are able to drastically reduce the migration of breast cancer cells by regulation of the two major proteins involved in epithelial-mesenchymal transition (EMT): vimentin and E-cadherin. Moreover, these compounds diminish the intracellular biosynthesis of vascular endothelial growth factor (VEGF), which is primarily involved in the promotion of angiogenesis, sustaining tumor progression. The multiple features of these compounds that act on various key points of the tumorigenesis process make them good candidates for preclinical studies.
Biopolymeric self-assembled nanoparticles for enhanced antibacterial activity of Ag-based compounds
International Journal of Pharmaceutics, 2016
Microbial infections still remain one of the main issues for human health. The rapid development ... more Microbial infections still remain one of the main issues for human health. The rapid development of resistance towards the most common antimicrobial drugs in bacteria represents today a challenge in the infections management. In the present work we have investigated the antibacterial activity of a group of compounds, namely silver N-heterocyclic carbene complexes, against a broad spectrum of bacteria. For the most promising compound, a biopolymeric nanocarrier has been developed, in order to potentiate the metal complex activity against both Gram +ve and Gram -ve. The polymeric nanovehicle is based on dextran, modified with oleic acid residues, that confer amphiphilic properties to the polysaccharide. We have characterized the obtained biomaterial and studied its ability to self-assemble into nanoparticles in aqueous environment. Next, the transdermal diffusion analyses have been carried out to evaluate the ability of the polymeric particles to penetrate tissues. Thanks to the strategy adopted, we have fabricated an antibacterial system to which K. pneumoniae and E. coli are the most sensitive.
Environmental contamination has exposed humans to various metal agents, including mercury. It has... more Environmental contamination has exposed humans to various metal agents, including mercury. It has been determined that mercury is not only harmful to the health of vulnerable populations such as pregnant women and children, but is also toxic to ordinary adults in various ways. For many years, mercury was used in a wide variety of human activities. Nowadays, the exposure to this metal from both natural and artificial sources is significantly increasing. Recent studies suggest that chronic exposure, even to low concentration levels of mercury, can cause cardiovascular, reproductive and developmental toxicity, neurotoxicity, nephrotoxicity, immunotoxicity, and carcinogenicity. Possible biological effects of mercury, including the relationship between mercury toxicity and diseases of the cardiovascular system, such as hypertension, coronary heart disease and myocardial infarction, are being studied. As heart rhythm and function are under autonomic nervous system control, it has been hyp...
A Review on Mercury Toxicity in Food
Food Toxicology, 2016
Synthesis, characterization and cytotoxic activity on breast cancer cells of new half-titanocene derivatives
Bioorganic Medicinal Chemistry Letters, Mar 26, 2013
Resveratrol and Its Analogs As Antitumoral Agents For Breast Cancer Treatment
Mini reviews in medicinal chemistry, 2016
Resveratrol (3,5,4'-tri-hydroxystilbene) (RSV), a naturally occurring phytoalexin, readily av... more Resveratrol (3,5,4'-tri-hydroxystilbene) (RSV), a naturally occurring phytoalexin, readily available in the diet, has gained interest as a non-toxic agent capable of displaying cancer-preventing and anti-cancer properties. Several studies, using both in vitro and in vivo models, have illustrated RSV capacity to modulate a multitude of signaling pathways associated with cellular growth and division, apoptosis, angiogenesis, invasion and metastasis. However, its clinical application is limited because of a low oral bioavailability with high adsorption but rapid metabolism and low tissue concentrations. Several chemical modifications to the backbone structure have been made for the purpose of improving pharmacokinetic parameters. One promising strategy involves the introduction of methoxylic or hydroxylic groups on the phenylic rings of RSV. Moreover, by replacing the alkene linker between the two aromatic rings with a heterocyclic system rigid analogs such as 2,3- thiazolidin-4-on...
Engineered Polymer-Based Nanomaterials for Diagnostic, Therapeutic and Theranostic Applications
Mini-Reviews in Medicinal Chemistry, 2015
Nanomedicine can be defined as the medical application of molecular nanotechnology and it plays a... more Nanomedicine can be defined as the medical application of molecular nanotechnology and it plays a key role and pharmaceutical research and development, especially related to cancer prevention, monitoring, diagnosis and treatment. In this context, nanomaterials are attracting significant research interest due to their abilities to stay in the blood for long time, accumulate in pathological sites including tumors or inflammatory areas via the enhanced permeability and retention (EPR) effect, and facilitate targeted delivery of specific therapeutic agents. In the last decades, considerable attention was attracted by the development of nano-sized carriers, based on natural or synthetic polymers, able to provide the controlled release of anticancer drugs in the aim to overcome the drawbacks associated to the conventional chemotherapy. Furthermore, when loaded with imaging agents, this kind of systems offers the opportunity to exploit optical or magnetic resonance imaging (MRI) in cancer diagnosis. Polymeric materials are characterized by several functionalities where both therapeutic and imaging components, and also targeting moieties, can be attached for simultaneous targeted therapy and imaging providing innovative platforms defined as theranostic agents with a great potential in monitoring and treatment of cancer.
The synthesis and activity of 1,3-indandione derivatives as acetylcholinesterase (AChE) inhibitor... more The synthesis and activity of 1,3-indandione derivatives as acetylcholinesterase (AChE) inhibitors are reported. The synthetic key-step consists of the Knovenagel olefination between 1,3-indandione and a substituted (1-benzylpiperidin-4-yl)methanal followed by selective double bond reduction. AChE inhibitory activity was measured by a quick fluorimetric method. One of the new compounds showed a significant interaction with the enzyme. Molecular modelling studies were performed in order to propose the binding modes within the AChE gorge compared to the known inhibitor Donepezil.
Corrigendum to “Inhibition of human topoisomerase I and II and anti-proliferative effects on MCF-7 cells by new titanocene complexes” [Bioorg. Med. Chem. 23 (2015) 7302–7312]
Bioorganic & Medicinal Chemistry, 2015
Synthesis and x-ray analysis of the dirhodium (II, II) carboxylate complex Rh2 (O2CCH3) 4 (formH) 2 (form H= N, N'-di-p-tolylformamidine)
Inorganica Chimica …, 1994
... D. [14]. M. Nardelli. Comput. Chem. 7 (1983), p. 95 version locally modified. Abstract | PDF ... more ... D. [14]. M. Nardelli. Comput. Chem. 7 (1983), p. 95 version locally modified. Abstract | PDF (390 K) | View Record in Scopus | Cited By in Scopus (1365). [15]. DM Grove, G. van Koten, HJC Ubbels, K. Vrieze, LC Niemann and CH Stam. J. Chem. Soc., Dalton Trans. (1986), p. 717. ...
International Journal of Molecular Sciences
Resveratrol (3,5,4′-trihydroxystilbene; RSV) is a natural nonflavonoid polyphenol present in many... more Resveratrol (3,5,4′-trihydroxystilbene; RSV) is a natural nonflavonoid polyphenol present in many species of plants, particularly in grapes, blueberries, and peanuts. Several in vitro and in vivo studies have shown that in addition to antioxidant, anti-inflammatory, cardioprotective and neuroprotective actions, it exhibits antitumor properties. In mammalian models, RSV is extensively metabolized and rapidly eliminated and therefore it shows a poor bioavailability, in spite it of its lipophilic nature. During the past decade, in order to improve RSV low aqueous solubility, absorption, membrane transport, and its poor bioavailability, various methodological approaches and different synthetic derivatives have been developed. In this review, we will describe the strategies used to improve pharmacokinetic characteristics and then beneficial effects of RSV. These methodological approaches include RSV nanoencapsulation in lipid nanocarriers or liposomes, nanoemulsions, micelles, insertion ...
Journal of enzyme inhibition and medicinal chemistry, 2018
Synthetic or natural carbazole derivatives constitute an interesting class of heterocycles, which... more Synthetic or natural carbazole derivatives constitute an interesting class of heterocycles, which showed several pharmaceutical properties and occupied a promising place as antitumour tools in preclinical studies. They target several cellular key-points, e.g. DNA and Topoisomerases I and II. The most studied representative, i.e. Ellipticine, was introduced in the treatment of metastatic breast cancer. However, because of the onset of dramatic side effects, its use was almost dismissed. Many efforts were made in order to design and synthesise new carbazole derivatives with good activity and reduced side effects. The major goal of the present study was to synthesise a series of new N-thioalkylcarbazole derivatives with anti-proliferative effects. Two compounds, 5a and 5c, possess an interesting anti-proliferative activity against breast and uterine cancer cell lines without affecting non-tumoural cell lines viability. The most active compound (5c) induces cancer cells death triggering...
Molecules (Basel, Switzerland), Jan 30, 2018
Despite the progress achieved by anti-retroviral drug research in the last decades, the discovery... more Despite the progress achieved by anti-retroviral drug research in the last decades, the discovery of novel compounds endowed with selective antiviral activity and reduced side effects is still a necessity. At present, the most urgent requirement includes the improvement of HIV (Human Immunodeficiency Virus) prevention and sexual transmission and the development of new drugs to treat the chronic lifelong infection. Six chloro-1,4-dimethyl-9-carbazoles (,-,) have been prepared following opportunely modified known chemical procedures and tested in luciferase and β-galactosidase expressing CD4⁺, CXCR4⁺, CCR5⁺ TZM-bl cells. a preliminary biological investigation on the synthesized small series of chloro-1,4-dimethyl-9-carbazoles has been carried out. Among all tested compounds, a nitro-derivative () showed the most interesting profile representing a suitable lead for the development of novel anti-HIV drugs.
New insights for the use of quercetin analogs in cancer treatment
Future medicinal chemistry, Nov 1, 2017
Quercetin (Q1) is a flavonoid widely present in plants and endowed with several pharmacological p... more Quercetin (Q1) is a flavonoid widely present in plants and endowed with several pharmacological properties mostly due to its antioxidant potential. Q1 shows anticancer activity and could be useful in cancer prevention. On the other hand, Q1 is poorly soluble in water and unstable in physiological systems, and its bioavailability is very low. A small set of Q1 derivatives (Q2-Q9) has been synthesized following opportunely modified chemical procedures previously reported. Anticancer activity has been evaluated by MTT assay. Human Topoisomerases inhibition has been performed by direct enzymatic assays. Apoptosis has been evaluated by TUNEL assay. ROS production and scavenging activity have been determined by immunofluorescence. The anticancer profile of a small library of Q1 analogues, in which the OH groups were all or partially replaced with hydrophobic functional groups, has been evaluated. Two of the studied compounds demonstrated an interesting cytotoxic profile in two breast canc...
Novel Au and Ag carbene complexes exert anti-tumor effects triggering the ROS-dependent intrinsic apoptotic pathway
ChemMedChem, Dec 9, 2017
Cisplatin and other platinum-based drugs are well-known valid anticancer drugs. However, during t... more Cisplatin and other platinum-based drugs are well-known valid anticancer drugs. However, during the chemotherapy, the presence of numerous side effects and the onset of frequent phenomena of resistance pushes forward many research groups to devise new metal-based compounds holding improved anticancer properties and lower undesired effects. Amongst the variety of synthesized compounds, significant anti-proliferative effects were obtained employing organometallic compounds, particularly those based on silver or gold. With this in mind, we have synthesized four compounds, two silver- and two gold-complexes, with good inhibitory effects on the in vitro proliferation of breast and ovarian cancer cells models. The most active compound, i.e. AuL4, possess a 9-fold higher antitumor activity compared to cisplatin and induced dramatic morphological changes in HeLa cells. AuL4 induces PARP-1 cleavage, caspases 3/7 and 9 activation, mitochondria disruption, cytochrome c release in cancer cell c...
International Journal of Environmental Research and Public Health
Molecules, 2017
N-Palmitoyl-ethanolamine (PEA) is an anti-inflammatory component of egg yolk that is usually empl... more N-Palmitoyl-ethanolamine (PEA) is an anti-inflammatory component of egg yolk that is usually employed for the prevention of respiratory apparatus virus infection and then frequently used for its efficient anti-inflammatory and analgesic effects in experimental models of visceral, neuropathic, and inflammatory diseases. Nevertheless, data of its use in animal or human therapy are still scarce and further studies are needed. Herein, we report the biological evaluation of a small library of N-palmitoyl-ethanolamine analogues or derivatives, characterized by a protected acid function (either as palmitoyl amides or hexadecyl esters), useful to decrease their hydrolysis rate in vitro and prolong their biological activity. Two of these compounds-namely phenyl-carbamic acid hexadecyl ester (4) and 2-methyl-pentadecanoic acid (4-nitro-phenyl)-amide (5)-have shown good anti-inflammatory and antioxidant properties, without affecting the viability of J774A.1 macrophages. Finally, crystals suitable for X-ray analysis of compound 4 have been obtained, and its solved crystal structure is here reported. Our outcomes may be helpful for a rational drug design based on new PEA analogues/derivatives with improved biological properties.
Role of Calabrian Black Rice in Metabolic Syndrome: in vitro Evaluation of Oryza Sativa L. Indica biological properties
Current Nutrition & Food Science, 2017
Metabolic Syndrome is becoming more common and it is characterized by an excess intake of energy,... more Metabolic Syndrome is becoming more common and it is characterized by an excess intake of energy, readily available carbohydrates and fats that result in postprandial hyperglycemia and hyperlipidemia. In the treatment of Metabolic Syndrome, a diet characterized by functional food, high fiber intake and low glycemic index is recommended. The aim of this research was to study, in vitro, the beneficial and biological properties of black rice cultivated in Sibari plain, a particular area of the region of Calabria, and verify if the climatic conditions of this area influence the composition of this pigmented rice. The antioxidant activity was investigated by performing the DPPH radical scavenging assay, while the free phenolic content of CBR extract was measured by Folin Ciocalteu’s assay and the obtained results were expressed as mg of gallic acid equivalent/mg of extract. In order to establish the anti-inflammatory effect of CBR extract, its reactivity towards nitric oxide (NO) was evaluated, while, its anti-hypertensive activity was studied by determining the ACE activity inhibition. CBR extract also suppresses pancreatic lipase activity with an IC50 value of 34.3 μg/ml and it decreases cellular lipid accumulation by about 60%. Finally, its hypoglycemic effect was evaluated by measuring the inhibiting activity towards α-glucosidase and α-amylase enzymes. The obtained results demonstrate that this kind of black rice owns different beneficial properties, which make it a functional food that could improve metabolic disorders of MS.
Drug delivery, 2017
Sericin is a natural protein that has been used in biomedical and pharmaceutical fields as raw ma... more Sericin is a natural protein that has been used in biomedical and pharmaceutical fields as raw material for polypeptide-based drug delivery systems (DDSs). In this paper, it has been employed as pharmaceutical biopolymer for the production of sunitinib-polypeptide conjugate. The synthesis has been carried out by simple click reaction in water, using the redox couple l-ascorbic acid/hydrogen peroxide as a free radical grafting initiator. The bioconjugate molecular weight (50 kDa < Mw < 75 kDa) was obtained by SDS-PAGE, while the spectroscopic characteristics have been studied in order to reveal the presence of grafted sunitinib. In both FT-IR and UV/Vis spectra, signals corresponding to sunitinib functional groups have been identified. Since sunitinib is an anticancer drug characterized by low bioavailability and low permeability, the bioconjugation aimed at their enhancement. In vitro studies demonstrated that bioavailability has been increased to almost 74%, compared with com...
Molecules, 2017
The quest for alternative drugs with respect to the well-known cis-platin and its derivatives, wh... more The quest for alternative drugs with respect to the well-known cis-platin and its derivatives, which are still used in more than 50% of the treatment regimens for patients suffering from cancer, is highly needed. In this context, organometallic compounds, which are defined as metal complexes containing at least one direct covalent metal-carbon bond, have recently been found to be promising anticancer drug candidates. A series of new metallocene complexes with scandium, yttrium, and neodymium have been prepared and characterized. Some of these compounds show a very interesting anti-proliferative activity in triple negative breast cancer cell line (MDA.MB231) and the non-hormone sensitive prostate cancer cell line (DU145). Moreover, the interaction of some of them with biological membranes, evaluated using liposomes as bio-membrane mimetic model systems, seems to be relevant. The biological activity of these compounds, particularly those based on yttrium, already effective at low concentrations on both cancer cell lines, should be taken into account with regard to new therapeutic approaches in anticancer therapy.
Old Drug Scaffold, New Activity: Thalidomide Correlated Compounds Exerting Different Effects on Breast Cancer Cell Growth and Progression
ChemMedChem, 2017
Thalidomide was first used for relief of morning sickness in pregnant women and then withdrawn fr... more Thalidomide was first used for relief of morning sickness in pregnant women and then withdrawn from the market because of its dramatic effects on normal fetal development. Over the last decades, it has been used successfully for the treatment of several pathologies, including cancer. Many analogues with improved activity have been synthesized and tested. Herein we report some effects on the growth and progression of MCF-7 and MDA-MB-231 breast cancer cells by a small series of thalidomide-correlated compounds, which are very effective at inducing cancer cell death by triggering TNFα-mediated apoptosis. The most active compounds are able to drastically reduce the migration of breast cancer cells by regulation of the two major proteins involved in epithelial-mesenchymal transition (EMT): vimentin and E-cadherin. Moreover, these compounds diminish the intracellular biosynthesis of vascular endothelial growth factor (VEGF), which is primarily involved in the promotion of angiogenesis, sustaining tumor progression. The multiple features of these compounds that act on various key points of the tumorigenesis process make them good candidates for preclinical studies.
Biopolymeric self-assembled nanoparticles for enhanced antibacterial activity of Ag-based compounds
International Journal of Pharmaceutics, 2016
Microbial infections still remain one of the main issues for human health. The rapid development ... more Microbial infections still remain one of the main issues for human health. The rapid development of resistance towards the most common antimicrobial drugs in bacteria represents today a challenge in the infections management. In the present work we have investigated the antibacterial activity of a group of compounds, namely silver N-heterocyclic carbene complexes, against a broad spectrum of bacteria. For the most promising compound, a biopolymeric nanocarrier has been developed, in order to potentiate the metal complex activity against both Gram +ve and Gram -ve. The polymeric nanovehicle is based on dextran, modified with oleic acid residues, that confer amphiphilic properties to the polysaccharide. We have characterized the obtained biomaterial and studied its ability to self-assemble into nanoparticles in aqueous environment. Next, the transdermal diffusion analyses have been carried out to evaluate the ability of the polymeric particles to penetrate tissues. Thanks to the strategy adopted, we have fabricated an antibacterial system to which K. pneumoniae and E. coli are the most sensitive.
Environmental contamination has exposed humans to various metal agents, including mercury. It has... more Environmental contamination has exposed humans to various metal agents, including mercury. It has been determined that mercury is not only harmful to the health of vulnerable populations such as pregnant women and children, but is also toxic to ordinary adults in various ways. For many years, mercury was used in a wide variety of human activities. Nowadays, the exposure to this metal from both natural and artificial sources is significantly increasing. Recent studies suggest that chronic exposure, even to low concentration levels of mercury, can cause cardiovascular, reproductive and developmental toxicity, neurotoxicity, nephrotoxicity, immunotoxicity, and carcinogenicity. Possible biological effects of mercury, including the relationship between mercury toxicity and diseases of the cardiovascular system, such as hypertension, coronary heart disease and myocardial infarction, are being studied. As heart rhythm and function are under autonomic nervous system control, it has been hyp...
A Review on Mercury Toxicity in Food
Food Toxicology, 2016
Synthesis, characterization and cytotoxic activity on breast cancer cells of new half-titanocene derivatives
Bioorganic Medicinal Chemistry Letters, Mar 26, 2013
Resveratrol and Its Analogs As Antitumoral Agents For Breast Cancer Treatment
Mini reviews in medicinal chemistry, 2016
Resveratrol (3,5,4'-tri-hydroxystilbene) (RSV), a naturally occurring phytoalexin, readily av... more Resveratrol (3,5,4'-tri-hydroxystilbene) (RSV), a naturally occurring phytoalexin, readily available in the diet, has gained interest as a non-toxic agent capable of displaying cancer-preventing and anti-cancer properties. Several studies, using both in vitro and in vivo models, have illustrated RSV capacity to modulate a multitude of signaling pathways associated with cellular growth and division, apoptosis, angiogenesis, invasion and metastasis. However, its clinical application is limited because of a low oral bioavailability with high adsorption but rapid metabolism and low tissue concentrations. Several chemical modifications to the backbone structure have been made for the purpose of improving pharmacokinetic parameters. One promising strategy involves the introduction of methoxylic or hydroxylic groups on the phenylic rings of RSV. Moreover, by replacing the alkene linker between the two aromatic rings with a heterocyclic system rigid analogs such as 2,3- thiazolidin-4-on...
Engineered Polymer-Based Nanomaterials for Diagnostic, Therapeutic and Theranostic Applications
Mini-Reviews in Medicinal Chemistry, 2015
Nanomedicine can be defined as the medical application of molecular nanotechnology and it plays a... more Nanomedicine can be defined as the medical application of molecular nanotechnology and it plays a key role and pharmaceutical research and development, especially related to cancer prevention, monitoring, diagnosis and treatment. In this context, nanomaterials are attracting significant research interest due to their abilities to stay in the blood for long time, accumulate in pathological sites including tumors or inflammatory areas via the enhanced permeability and retention (EPR) effect, and facilitate targeted delivery of specific therapeutic agents. In the last decades, considerable attention was attracted by the development of nano-sized carriers, based on natural or synthetic polymers, able to provide the controlled release of anticancer drugs in the aim to overcome the drawbacks associated to the conventional chemotherapy. Furthermore, when loaded with imaging agents, this kind of systems offers the opportunity to exploit optical or magnetic resonance imaging (MRI) in cancer diagnosis. Polymeric materials are characterized by several functionalities where both therapeutic and imaging components, and also targeting moieties, can be attached for simultaneous targeted therapy and imaging providing innovative platforms defined as theranostic agents with a great potential in monitoring and treatment of cancer.