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Introduction
My research field is inorganic medicinal chemistry, my interests cover the following main topics:
- Metal-based drugs
- Metal trafficking in vitro (thermodynamic characterization of metal complexes in solution)
- Development of novel metal-chelating agents for theranostic purposes
- Development and characterization of iron-based drugs
- Organic, inorganic and metal-organic synthesis
- Inorganic Drug Delivery Systems (IDDS)
- Development of advanced NMR techniques for complex matrices
Publications
Publications (85)
Cancer is a leading cause of death worldwide, its genesis and progression are caused by homeostatic errors, and reactive oxygen species play a major role in promoting aberrant cancer homeostasis. In this scenario, curcumin could be an interesting candidate due to its versatile antioxidant, anti-inflammatory, anti-tumor, anti-HIV, and anti-infection...
Curcumin is known for its therapeutic properties; among these, antioxidant, anti-inflammatory and anti-cancer ones stand out. Besides, curcumin metal complexes have shown widespread application in medicine and can be exploited as lead structures for developing metal-based drugs. Unfortunately, curcumin is poorly bioavailable, mainly due to its inst...
Introduction
specific microbial communities are associated to host plants, influencing their phenotype and fitness. Despite the rising interest in plant microbiome, the role of microbial communities associated with perennial fruit plants remains overlooked.
Objectives
this work provides the first comprehensive description of the taxonomical and fu...
Unprotected exposure to solar UV is the main recognized cause of the spreading of skin cancer that has occurred in the last decades. Organic and inorganic UV filters are the main defense against UV exposure and have become ubiquitous in personal-care products, packaging, plastics, dyes, and many other sectors. UV filters still have some stability a...
Curcumin is a natural occurring molecule that has aroused much interest among researchers over the years due to its pleiotropic set of biological properties. In the nuclear medicine field, radiolabelled curcumin and curcumin derivatives have been studied as potential radiotracers for the early diagnosis of Alzheimer’s disease and cancer. In the pre...
Celebrating the “25th Anniversary of Molecules” with a Special Issue dedicated to “Recent Advances in Inorganic Chemistry” strengthens the renewed role that inorganic chemistry, one of the oldest chemistry divisions, has lately earned thanks to cutting-edge perspectives and interdisciplinary applications, eventually receiving the veneration and res...
The copper(II) complexes of general formula [Cu(GL)(Cl)] (1–3, G = OMe, H and NO2, respectively), bearing tridentate Schiff base ligands (GL−) and a chloride as a fourth labile one, are here reported. The Schiff bases derive from the monocondensation of ethylenediamine and substituted salicylaldehyde, where the electronic properties are modulated b...
Curcumin metal complexes showed widespread applications in medicine and can be exploited as a lead structure for developing new tracers for nuclear medicine application. Herein, the synthesis, chemical characterization and radiolabelling with gallium-68 and scandium-44 of two new targeting vectors based on curcumin scaffolds and linked to the chela...
Cadmium (Cd) and lead (Pb) are two toxic heavy metals (HMs) whose presence in soil is generally low. However, industrial and agricultural activities in recent years have significantly raised their levels, causing progressive accumulations in plant edible tissues, and stimulating research in this field. Studies on toxic metals are commonly focused o...
Colorectal cancer is the third most commonly occurring cancer in men and the second most commonly occurring cancer in women worldwide. We have recently reported that curcuminoid complexes labelled with gallium-68 have demonstrated preferential uptake in HT29 colorectal cancer and K562 lymphoma cell lines compared to normal human lymphocytes. In the...
Metastatic castration-resistant prostate cancer is commonly treated with chemotherapy, whose effect is less than satisfactory. This raised the need for novel agents for the treatment of prostate cancer. In the present study, five phthalimide-based curcumin derivatives were synthesized and completely characterized to assess improved stability, pharm...
Microwave-assisted extraction of organic compounds from vegetal matrixes is a relatively young ield of research. The exceptional results achievable at the laboratory scale by microwave assisted extraction, like shorter extraction times, lower average temperatures, reduction of organic solvents use, higher yields and selectivity, as well as energy a...
Several neurodegenerative diseases, like Alzheimer's (AD), are characterized by amyloid fibrillar deposition of misfolded proteins, and this feature can be exploited for both diagnosis and therapy design. In this paper, structural modifications of curcumin scaffold were examined in order to improve its bioavailability and stability in physiological...
A solid biostimulant (AA309) obtained through thermobaric hydrolysis applied on trimmings and shavings of bovine hides tanned with wet-blue technology was chemically characterized, and its effects in maize (Zea mays L.) were evaluated. AA309 contained 13.60% total nitrogen (N), mainly in organic forms (13.40%), and several amino acids, especially l...
The metal complexing ability in solution of four substituted curcumin (CUR)-derived ligands K3T, originated by the insertion of a –CH2CH2COOtBu branch on the central atom of the diketonic moiety of CUR and related derivatives with variable meta and para substituents (OH, OMe, H, OCOCH3) on the peripheral aromatic rings, is examined. These molecules...
Thanks to the ability to suppress the proliferation and to kill tumour cells, several studies have shown the anti-cancer effects of curcumin (CUR) and its derivatives, i.e. diacetylcurcumin (DAC) and bis-dehydroxycurcumin (bDHC). This study is focused onto the development of curcuminoid complexes with gallium-68 employed as potential new radio-labe...
Bis-dehydroxycurcumin tert-butyl ester (K2T23) is a derivative of the natural spice curcumin. Curcumin is widely studied for its multiple therapeutic properties, including photosensitized cytotoxicity. However, the full exploitation of curcumin phototoxic potential is hindered by the extreme instability of its excited state, caused by very efficien...
Microwave-assisted extraction was applied to Juglans regia L. fresh male flowers and unripe walnut seeds to evaluate the total phenolic contents of the extracts as well as the percentage of water-soluble polyphenols. The research was planned using the Design of Experiments technique to investigate the role on the extraction efficiency of different...
Curcumin derivatives labelled with fluorine-18 or technetium-99m have recently shown their potential as diagnostic tools for Alzheimer's disease. Nevertheless, no study by exploiting the labelling with gallium-68 has been performed so far, in spite of its suitable properties (positron emitter, generator produced radionuclide). Herein, an evaluation...
Curcumin and its derivatives have attracted great interest in the prevention and treatment of Alzheimer's disease (AD), thanks both to the ability to hinder the formation of amyloid-beta (Aβ) aggregates and the ability to bind Cu (II) ion. In this article, we explore the ability of curcumin derivatives of K2T series to affect amyloid Aβ1-40 aggrega...
In this paper, we report the study of the loading and the release of curcuminoids by bioactive glasses (BG) and mesoporous bioactive glasses (MBG). Through a detailed spectroscopic study, it was possible to determine the amount and the type of molecules released in water and in simulated body fluid (SBF). In particular, curcumin and K2T21 show a go...
Natural compounds represent an extremely wide category to be exploited, in order to develop new pharmaceutical strategies. In this framework, the number of in vitro, in vivo and clinical trials investigating the therapeutic potential of curcumin is exponentially increasing, due to its antioxidant, anti-inflammatory and anticancer properties. The po...
Among relevant metal ions in biological systems, zinc and iron play a key role as active partners of the catalytic machinery. In particular, the inhibition of metal enzymes that are involved in physiological and pathological processes has been deeply investigated for the rational design of selective and efficient drugs based on chelators. Since imi...
Appendix S1 ATR/FTIR spectra Gaussian curve fitting.
Figure S1 Histograms of HA (upper) and FA (lower) of the ATR/FTIR peak areas processed by using Gaussian curve fitting.
In alpine environments, colonies of snow vole (Chionomys nivalis Martins) cause strong pedoturbation, which may affect humification process and soil organic matter (SOM) cycling, with repercussions on the hormone-like activity of organics. We investigated the effect of snow vole pedoturbation on the chemical and spectroscopic features of soil organ...
Screen-printed electrode (SPE) modified with carbon black nanoparticles (CB) has been tested as a new platform for the stable deposition of caffeic acid (CFA) on the electrode surface. The electrochemical performance from varying the amount of CFA/CB composite has been tested with respect to NADH determination. The electrocatalytic activity of CFA/...
The litter decomposition process depends on the litter chemical composition, especially the ratio between more labile compounds, cellulose, and the recalcitrant lignin and waxes. Their determination is crucial to predict the process, though lignin measurement presents some limitations due to drawbacks of the different methods. Thermal analysis has...
Abstract
In alpine environments, colonies of snow vole (Chionomys nivalis Martins)
cause strong pedoturbation, which may affect humification process and soil
organic matter (SOM) cycling, with repercussions on the hormone-like activity
of organics. We investigated the effect of snow vole pedoturbation on the
chemical and spectroscopic features of s...
Curcumin (CUR) and curcuminoids complexes labeled with fluorine-18 or technetium-99m have recently shown their potential as diagnostic tools for Alzheimer's disease. Gallium-68 is a positron-emitting, generator-produced radionuclide, and its properties can be exploited in situ in medical facilities without a cyclotron. Moreover, CUR showed a higher...
Topoisomerases-IIα (TOP2A) enzyme is essential for cell viability due to its fundamental role in DNA metabolism and in chromatin organization during interphase and mitosis. TOP2A expression is finely regulated at the transcriptional level through the binding of the CCAAT-transcription factor NF-Y to its promoter. Overexpression and/or amplification...
Theoretical calculations employing DFT at the B3LYP/6-311G++** level are used to investigate the tautomeric equilibrium in curcumin derivatives. The solvent effect is evaluated using the CPCM continuum solvation method. The results are compared with experimental data obtained from the X-ray crystal structure of and UV-vis data. The KE tautomer is m...
The activation of autophagy has been extensively described as a pro-survival strategy, which helps to keep cells alive following deprivation of nutrients/growth factors and other stressful cellular conditions. In addition to cytoprotective effects, autophagy can accompany cell death. Autophagic vacuoles can be observed before or during cell death,...
A. Percentages of 4n phospho-Ser10H3 positive HCT116 cells (black bars) counted out of a total number of 4n cells (grey bars) after DMSO, Curcumin and bDHC treatments for 16 and 24 hours. B. Scanning Electron Microscopy images of control and bDHC-treated HCT116 cells. Scale bar: 5 µm. C. Left panel: Distribution of LOVO cells into the different pha...
A. Quantification of the expression levels of γH2AX, p53 and p21 versus actin in HCT116 cells co-treated with ZVAD or incubated with DMSO and bDHC alone (Western blots shown in Fig. 3A). B. Cytoplasmic (left panel) and mitochondrial/nuclear Cytochrome C levels following time-dependent administration of bDHC. Adriamycin (ADR) was used as positive co...
Left panel: Western blot analysis of LC3 expression in HCT116 cells treated with DMSO, bDHC and C3-bDHC for 24 hours. Right panel: PI/FACS cell cycle analysis of HCT116 cells following incubation with DMSO and C3-bDHC for 24 hours. Values are means of three independent experiments −/+ SD.
(TIF)
A. Ratio of LC3-II/LC3-I expression levels normalized to actin following DMSO and time dependent exposure of HCT116 cells to bDHC. B. LC3-II/LC3-I ratio in DMSO and bDHC cells co-treated with ZVAD or Wortmannin (WORT) versus DMSO. C. LC3-II/LC3-I ratio in Beclin1 (BCN1) and ATG7 inactivated cells following DMSO or bDHC administration. D. Ratio of L...
A. Left panel: Western blot analysis of LC3 expression following 24 and 48 hours of bDHC exposure in HF cells. Right panel indicates the levels of LC3-II versus actin following time-dependent exposure to bDHC. Values are means of three independent experiments. B. Upper left panels: LC3 expression levels in HCT116/E6 compared to HCT116 cells. Upper...
Bis-dehydroxycurcumin carboxylic acid (K2A23) is a synthetic curcuminoid designed to exhibit enhanced water solubility and photosensitizing potential with respect to natural curcumin. In this work, the tendency of the compound to form intra- and intermolecular hydrogen bonds in the ground state is studied by UV-visible absorption and by nuclear mag...
New smart materials based on phospho-silicate bioactive sol-gel glasses have been developed. To meet the ever-increasing demand for performing bio-materials, the surface features of the glasses have been tailored to achieve optimal behaviour in different applications (drug delivery, enzymes activity, chemo-signalling probe, stimuli-sensitive agents...
RNA binding proteins belonging to the TIS11/TTP gene family regulate the stability of multiple targets. Their inactivation or deregulated expression has recently been related to cancer, and it has been suggested that they are capable of displaying tumor suppressor activities. Here we describe three new targets of ZFP36 (PIM-1, PIM-3 and XIAP) and s...
Soil organic matter (SOM) is an important factor influencing aggregate stability. Interactions between SOM and soil structure are widely studied, although the subtle relationship between SOM content, pore size distribution and aggregate stability is not fully known. Here we investigate such a relationship by means of a long-term experiment establis...
New curcumin analogues (ester and acid series) were synthesized with the aim to improve the chemical stability in physiological conditions and potential anticancer activity. Cytotoxicity against different tumorigenic cell lines (human ovarian carcinoma cells -2008, A2780, C13*, and A2780/CP, and human colon carcinoma cells HCT116 and LoVo) was test...
The novel β-diketo compound (3-acetyl-4-oxopentanoic acid) OPAA is here synthesized and completely characterized in the solid state by means of X-ray crystallography and in solution by potentiometry and 1H and 13C NMR spectroscopy. In the solid state, OPAA exhibits the di-keto (DK) structure, however, in solution, we can observe a strong solvent de...
In the Italian oenological industry, the regular practice used to naturally increase the colour of red wines consists in blending them with a wine very rich in anthocyanins, namely Rossissimo. In the Asian market, on the other hand, anthocyanins extracted by black rice are frequently used as correctors for wine colour. This practice does not produc...
In this study, using DRIFT and HR MAS NMR, we analyzed the humic substances isolated from a soil treated, over 40 years, with different organic, mineral and organic plus mineral treatments and cultivated with maize as the main crop. As expected, the structure of humic substances was very complex but by combining both techniques (DRIFT and HR MAS NM...
In the present study, we investigate the structures of glucosylated curcumin derivatives with DFT at B3LYP/6-31G* level. A conformational analysis is performed in order to determine the conformational minimum (GS) and rotational transition state (TS) of curcumin derivatives and then their electronic features are evaluated. HOMO and LUMO frontier or...
Curcumin, an active ingredient in the traditional Ayurvedic herbal remedy [Curcuma longa L.], is nowadays also employed in western medicine for its pleiotropic activities, ranging from anticancer to its free radical scavenger ability. These features are related to curcumin's function as a metal chelator, especially being selective for hard Lewis ac...
Although acid soils are common in forest ecosystems, and there is documented evidence of pH influencing transformations of organic matter in soil, there are surprisingly few studies on the influence of soil pH on the chemical structure of physically fractionated soil organic matter (SOM). The aim of this study was to characterize the influence of p...
The 16-kDa diheme cytochrome c from the bacterium Shewanella baltica OS155 (Sb-DHC) was cloned and expressed in Escherichia coli and investigated through UV-vis, magnetic circular dichroism, and (1)H NMR spectroscopies and protein voltammetry. The model structure was obtained by means of comparative modeling using the X-ray structure of Rhodobacter...
Glycosylated water-soluble curcuminoids (C1–C3, first scheme of this article) differing in the 3,3′-ring substituents (–OH, –OCH3 and H) equilibrate between the di-keto and the keto–enol forms. The former are well observable in the absorption spectra in water, but their emissions are always negligible. The keto–enol forms of C1–C3 exhibit a broad r...
Curcumin, a phenolic compound from the plant Curcuma longa L., has shown a wide-spectrum of chemopreventive, antioxidant and antitumor properties. Although its promising chemotherapeutic activity, preclinical and clinical studies highlight Curcumin limited therapeutic application due to its instability in physiological conditions. To improve its st...
Turmeric extracts, among which curcumin and bis-demethoxycurcumin, are by far known for their therapeutic activities. In this study we propose easy and low cost synthetic pathways in order to obtain glucosyl-curcuminoids, safe and water soluble potential drugs and dyes, which may be implied in different fields ranging from pharmacology to food chem...
New curcumin derivatives are synthesized in order to improve chemical properties of curcumin. The aromatic ring glycosylation of curcumin provides more water-soluble compounds with a greater kinetic stability which is a fundamental feature for drug bioavailability. The glycosylation reaction is quite simple, low cost, with high yield and minimum wa...
The Fe(3+) chelating ability of some curcumin glucosyl derivatives (Glc-H; Glc-OH; Glc-OCH(3)) is tested by means of UV and NMR study. The pK(a) values of the ligands and the overall stability constants of Fe(3+) and Ga(3+) complexes are evaluated from UV spectra. The only metal binding site of the ligand is the beta-diketo moiety in the keto-enoli...
The main target of this study is a high-level computational analysis of Curcumin, employing DFT approach with two different sets of basis functions (B3LYP/6-31G∗ and B3LYP/6-311G∗∗). Accurate quantum mechanical studies, both in vacuum and in methanol medium, are carried out with the aim to analyze the conformational equilibria, to find the most sta...
A simple synthetic pathway to obtain glycosilated beta-diketo derivatives is proposed. These compounds show a good iron(III) affinity therefore we may suggest the use of their Fe(3+)-complexes as oral iron supplements in the treatment of anaemia. The glycosilated compounds (6-GlcH, 6-GlcOH and 6-GlcOCH(3)) are characterized by means of spectroscopi...
The purpose of the present study is to investigate, by means of thermogravimetric analysis (TG) and differential thermal analysis (DTA), diffuse reflectance infrared Fourier transform (DRIFT) and 2D nuclear magnetic resonance (NMR) spectroscopies, the structural features of the humic-like fraction (HLF) from olive pulp (OP), its effluents originate...