8 research outputs found
Novel Gold(I) Thiolate Derivatives Synergistic with 5‑Fluorouracil as Potential Selective Anticancer Agents in Colon Cancer
New gold(I) thiolate
complexes have been synthesized and characterized, and their physicochemical
properties and anticancer activity have been tested. The coordination
of PTA derivatives provides optimal hydrophilicity/lipophilicity properties
to the complexes, which present high solution stability. Moreover,
the complexes show a high anticancer activity against Caco-2 cells,
comparable to that of auranofin, and a very low cytotoxic activity
against enterocyte-like differentiated cells. Their activity has been
shown to produce cell death by apoptosis and arrest of the cell cycle
because of interaction with the reductase enzymes and consequent reactive
oxygen species production. Some of these new complexes are also able
to decrease the necessary dose of 5-fluorouracil, a drug used for
the treatment of colon cancer, by a synergistic mechanism
<i>S</i>‑Propargylthiopyridine Phosphane Derivatives As Anticancer Agents: Characterization and Antitumor Activity
<i>S</i>-Propargylthiopyridine
phosphane gold(I) derivatives with
the water-soluble phosphanes PTA (1,3,5-triaza-7-phosphaadamantane),
DAPTA (3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane), and
TPPTS (sodium triphenylphosphane trisulfonate) are described and used
as metalloligands by coordination to copper(I). New heteronuclear
gold(I) and copper(I) complexes of the type [Au<sub>2</sub>Cu(CCCH<sub>2</sub>SC<sub>5</sub>H<sub>4</sub>N)<sub>2</sub>L<sub>2</sub>] (L
= PTA, DAPTA, PPh<sub>3</sub>, TPPTS) and [AuCu(CCCH<sub>2</sub>SC<sub>5</sub>H<sub>4</sub>N)(L)(PPh<sub>3</sub>)<sub>2</sub>]NO<sub>3</sub> (L = PTA, DAPTA) are reported. The X-ray crystal
structure of [Au(CCCH<sub>2</sub>SC<sub>5</sub>H<sub>4</sub>N)(PTA)] (<b>1</b>), which confirms the coordination
of the metallic center to the alkyne unit, displays a zigzag polymeric
chain with short gold–gold contacts of 3.2680(16) Å. Strong
antiproliferative effects are found for most of the new complexes
in human colon cancer cell lines (Caco-2, PD7, and TC7 clones), with
these effects being more pronounced than for the reference drugs cisplatin
and auranofin, especially for the heterodimetallic derivatives, which
are markedly more active than the corresponding mononuclear precursors.
Apoptosis-induced cell death is found for all compounds, as shown
by an annexin-V/propidium iodide double-staining assay
<i>Rosa canina</i> Extracts Have Antiproliferative and Antioxidant Effects on Caco-2 Human Colon Cancer - Fig 5
<p><b>Cell-cycle analysis after treatment with two concentrations</b> (a: 125 and b: 1000 mg/L) of Fr 1: total extract (1), Fr 2: vit. C (2), Fr 3: neutral polyphenols (3) and Fr 4: acid polyphenols or flavonoids (4) from rosehip (<i>Rosa canina</i> L) after 72 h. In control (C), the cells are without treatment. Cell cycle and DNA fragmentation were determined by propidium iodide staining. Percentages of G<sub>1</sub>, S and G<sub>2</sub>-phase are shown when possible. Experiments were performed in triplicate.</p
Chemical formula, concentration and total antioxidant capacity of the different extract fractions.
<p>Chemical formula, concentration and total antioxidant capacity of the different extract fractions.</p
Summary of PD7 and TC7 colon cancer cells treated with two concentrations (a: 125 and b: 1000 mg/L) of rosehip (<i>Rosa canina</i> L) fractions after 72 h.
<p>In control, the cells are without treatment.</p
<i>trans</i>-Thionate Derivatives of Pt(II) and Pd(II) with Water-Soluble Phosphane PTA and DAPTA Ligands: Antiproliferative Activity against Human Ovarian Cancer Cell Lines
A series
of PTA and DAPTA platinum(II) and palladium(II) thionate
complexes of the type <i>trans</i>-[M(SN)<sub>2</sub>P<sub>2</sub>] were prepared from the reaction of <i>cis</i>-[MCl<sub>2</sub>P<sub>2</sub>] [M = Pt, Pd; P = PTA (1,3,5-triaza-7-phosphaadamantane),
DAPTA (3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane)] with
the <i>in situ</i> generated sodium salts of the heterocyclic
thiones <i>S</i>-<i>m</i>-methylpyrimidine-2-thione, <i>S</i>-4,6-dimethylpyrimidine-2-thione, <i>S</i>-4,6-dihydroxypyrimidine-2-thione,
benzothiazole-2-thione, benzoxazole-2-thione, <i>S</i>-1,3,4,-thiadiazole-2-thione, <i>S</i>-4,5-<i>H</i>-thiazolan-2-thione, and <i>S</i>-pyrimidine-4(1<i>H</i>)-one-2-thione. The X-ray
structures of six of the compounds confirm the <i>trans</i> disposition and, only in the case of [Pd<sub>2</sub>Cl<sub>2</sub>(<i>S</i>-pyrimidine-4(1<i>H</i>)-one-2-thionate)<sub>2</sub>(PTA)<sub>2</sub>], a dinuclear structure with a Pd–Pd
distance of 3.0265(14)Å was observed. <i>In vitro</i> cytotoxicities against human ovarian cancer cell lines A2780 and
A2780cisR were evaluated for ten complexes showing a high inhibition
of cellular growth with a comparable inhibitory potency (IC<sub>50</sub>) against A2780 cells to that of cisplatin. Notably, the compounds
also show significant (up to 7-fold higher) activity in cisplatin-resistant
A2780cisR cell lines
<i>trans</i>-Thionate Derivatives of Pt(II) and Pd(II) with Water-Soluble Phosphane PTA and DAPTA Ligands: Antiproliferative Activity against Human Ovarian Cancer Cell Lines
A series
of PTA and DAPTA platinum(II) and palladium(II) thionate
complexes of the type <i>trans</i>-[M(SN)<sub>2</sub>P<sub>2</sub>] were prepared from the reaction of <i>cis</i>-[MCl<sub>2</sub>P<sub>2</sub>] [M = Pt, Pd; P = PTA (1,3,5-triaza-7-phosphaadamantane),
DAPTA (3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane)] with
the <i>in situ</i> generated sodium salts of the heterocyclic
thiones <i>S</i>-<i>m</i>-methylpyrimidine-2-thione, <i>S</i>-4,6-dimethylpyrimidine-2-thione, <i>S</i>-4,6-dihydroxypyrimidine-2-thione,
benzothiazole-2-thione, benzoxazole-2-thione, <i>S</i>-1,3,4,-thiadiazole-2-thione, <i>S</i>-4,5-<i>H</i>-thiazolan-2-thione, and <i>S</i>-pyrimidine-4(1<i>H</i>)-one-2-thione. The X-ray
structures of six of the compounds confirm the <i>trans</i> disposition and, only in the case of [Pd<sub>2</sub>Cl<sub>2</sub>(<i>S</i>-pyrimidine-4(1<i>H</i>)-one-2-thionate)<sub>2</sub>(PTA)<sub>2</sub>], a dinuclear structure with a Pd–Pd
distance of 3.0265(14)Å was observed. <i>In vitro</i> cytotoxicities against human ovarian cancer cell lines A2780 and
A2780cisR were evaluated for ten complexes showing a high inhibition
of cellular growth with a comparable inhibitory potency (IC<sub>50</sub>) against A2780 cells to that of cisplatin. Notably, the compounds
also show significant (up to 7-fold higher) activity in cisplatin-resistant
A2780cisR cell lines
Computational Modeling and Inelastic Neutron Scattering Contributions to the Study of Methyl-silica Xerogels: A Combined Theoretical and Experimental Analysis
In
amorphous materials, such as xerogels, the properties are the
key to most of their applications. Therefore, it is of great importance
to get insight into the xerogel structure. In order to achieve a better
understanding of structure formation in methyl-silica xerogels and
thus be able to better influence the properties of these materials,
we have chosen the molecular approach to model the hybrid–xerogel
structure using the density functional theory. A theoretical cage
model for hybrid xerogels was performed from the PBEPBE/6-31G(d,p)
method. The model could explain the presence of ordered domains in
the structure. A comprehensive listing of all IR and <sup>29</sup>Si NMR assignments is provided. The effects in the structure of the
organic functional groups incorporated on the host structure network
are investigated using inelastic neutron scattering spectroscopy (INS).
The combination of experiments and modeling permitted an analysis
of the INS studies, including unique INS assignments, contributing
to the understanding of the skeletal SiO<sub>2</sub> network of silica
xerogels and so to obtain information about the structure of this
material