scholarly journals Gold(I) Complexes with P-Donor Ligands and Their Biological Evaluation

Processes ◽  
2021 ◽  
Vol 9 (12) ◽  
pp. 2100
Author(s):  
Monika Richert ◽  
Renata Mikstacka ◽  
Mariusz Walczyk ◽  
Marcin Janusz Cieślak ◽  
Julia Kaźmierczak-Barańska ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Umbilical Vein ◽  
Biological Properties ◽  
Biological Evaluation ◽  
In Vitro Cytotoxicity ◽  
Myelogenous Leukemia ◽  
31P Nmr Spectroscopy ◽  
Cervix Carcinoma ◽  
Ovarian Carcinoma Cell Line

Gold(I) complexes with phosphine ligands—[Au(TrippyPhos)Cl] (1) (TrippyPhos = 1-[2-[bis(tert-butyl)phosphino]phenyl]-3,5-diphenyl-1H-pyrazole), [Au(BippyPhos)Cl]0.5CH2Cl2 (2) (BippyPhos = 5-(di-tert-butylphosphino)-1′, 3′, 5′-triphenyl-1′H-[1,4′]bipyrazole), and [Au(meCgPPh)Cl] (3) (meCgPPh = 1,3,5,7-tetramethyl-6-phenyl-2,4,8-trioxa-6-phosphaadamantane—were investigated as types of bioactive gold metallodrugs. Complexes (1)–(3) were characterized using IR, 1H, 13C, 31P NMR spectroscopy, elemental analysis and mass spectrometry (FAB-MS). Complexes of (1) and (2) exhibited substantial in vitro cytotoxicity (IC50 = 0.5–7.0 μM) against both the cisplatin-sensitive and -resistant variants of the A2780 human ovarian carcinoma cell line, as well as against the A549 human lung carcinoma, K562 chronic myelogenous leukemia, and HeLa (human cervix carcinoma) cells. However, among the compounds studied, complex (2) showed the most promising biological properties: the highest stability in biologically relevant media, selectivity towards cancer cells over the non-cancer cells (HUVEC, human umbilical vein endothelial cells), and the highest inhibitory effect on cytosolic NADPH-dependent reductases in A2780 and A2780cis cells among the gold complexes under analysis.

scholarly journals In vitro cytotoxicity assessment of ferulic, caffeic and p-coumaric acids on human renal cancer cells

2020 ◽  
Vol 17 (1) ◽  
pp. 1-12
Author(s):  
Rita Caparica ◽  
André Rolim Baby ◽  
Tânia Almeida ◽  
João Guilherme Costa
Keyword(s):  
Cancer Cells ◽  
Renal Cancer ◽  
Biological Effects ◽  
Biological Properties ◽  
In Vitro Cytotoxicity ◽  
Hydroxycinnamic Acids ◽  
Therapeutic Uses ◽  
Cytotoxicity Assessment ◽  
The Impact

Bioactive compounds from natural sources have been extensively studied as potential therapeutic agents, due to their chemical, structural, and biological properties. Among them, hydroxycinnamic acids emerge with a very interesting pharmacological potential to prevent and treat several diseases, including cancer. However, while some studies support their anticancer activity, other reports indicate otherwise. Since the impact of these compounds on renal cancer is not well established, further studies are needed to better understand their biological effects and their potential therapeutic uses in this cancer. In this work, the cytotoxicity of three hydroxycinnamic acids: ferulic, caffeic and p-coumaric acids, was evaluated on 786-O human renal cancer cells by MTT and CV assays. At concentrations up to 250 µM, none of the studied natural compounds showed cytotoxic effects to 786-O cell line. At higher concentrations (500 and 1000 µM), while ferulic acid also did not significantly influence the cell viability of 786-O cells, p-coumaric and caffeic acids decreased the renal cancer cells viability. Nevertheless, further studies on the biological activity of these compounds, using other methodologies, as well as using other cancer cell models, should be performed.

Recent Advances in Curcumin Nanocarriers for the Treatment of Different Types of Cancer with Special Emphasis on In Vitro Cytotoxicity and Cellular Uptake Studies

2020 ◽  
Vol 10 (5) ◽  
pp. 577-590
Author(s):  
Jai B. Sharma ◽  
Shailendra Bhatt ◽  
Asmita Sharma ◽  
Manish Kumar
Keyword(s):  
Cancer Cells ◽  
Cellular Uptake ◽  
Anticancer Agents ◽  
Targeted Delivery ◽  
In Vitro Cytotoxicity ◽  
Curcumin Nanoparticles ◽  
Cytotoxicity Studies ◽  
Delivery Technique ◽  
Different Types

Background: The potential use of nanocarriers is being explored rapidly for the targeted delivery of anticancer agents. Curcumin is a natural polyphenolic compound obtained from rhizomes of turmeric, belongs to family Zingiberaceae. It possesses chemopreventive and chemotherapeutic activity with low toxicity in almost all types of cancer. The low solubility and bioavailability of curcumin make it unable to use for the clinical purpose. The necessity of an effective strategy to overcome the limitations of curcumin is responsible for the development of its nanocarriers. Objective: This study is aimed to review the role of curcumin nanocarriers for the treatment of cancer with special emphasis on cellular uptake and in vitro cytotoxicity studies. In addition to this, the effect of various ligand conjugated curcumin nanoparticles on different types of cancer was also studied. Methods: A systematic review was conducted by extensively surfing the PubMed, science direct and other portals to get the latest update on recent development in nanocarriers of curcumin. Results: The current data from recent studies showed that nanocarriers of curcumin resulted in the targeted delivery, higher efficacy, enhanced bioavailability and lower toxicity. The curcumin nanoparticles showed significant inhibitory effects on cancer cells as compared to free curcumin. Conclusion: It can be concluded that bioavailability of curcumin and its cytotoxic effect to cancer cells can be enhanced by the development of curcumin based nanocarriers and it was found to be a potential drug delivery technique for the treatment of cancer.

A novel class of ruthenium-based photosensitizers effectively kills in vitro cancer cells and in vivo tumors

2015 ◽  
Vol 14 (11) ◽  
pp. 2014-2023 ◽  
Author(s):  
Jamie Fong ◽  
Kamola Kasimova ◽  
Yaxal Arenas ◽  
Pavel Kaspler ◽  
Savo Lazic ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Biological Properties

The photo-physical and photo-biological properties of two small (<2 kDa), novel Ru(ii) photosensitizers (PSs) referred to as TLD1411 and TLD1433 are presented.

Oxovanadium(IV) complexes with tetradentate thiosemicarbazones. Synthesis, characterization, anticancer enzyme inhibition and in vitro cytotoxicity on breast cancer cells

Polyhedron ◽  
2021 ◽  
Vol 202 ◽  
pp. 115192
Author(s):  
Onur Ertik ◽  
Ferdane Danışman Kalındemirtaş ◽  
Büşra Kaya ◽  
Refiye Yanardag ◽  
Serap Erdem Kuruca ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Enzyme Inhibition ◽  
Breast Cancer Cells ◽  
In Vitro Cytotoxicity

scholarly journals In Vitro Characterization of Magnetic Resonance Imaging Contrast Agents for Molecular Imaging.

Blood ◽  
2006 ◽  
Vol 108 (11) ◽  
pp. 3944-3944
Author(s):  
Zhi Yu ◽  
Michael Grafe ◽  
Heike Meyborg ◽  
Eckart Fleck ◽  
Yangqiu Li
Keyword(s):  
Endothelial Cells ◽  
Molecular Imaging ◽  
Cellular Uptake ◽  
Umbilical Vein ◽  
Biological Properties ◽  
Blue Staining ◽  
Iron Core ◽  
Coated Particles ◽  
Coated Particle

Abstract The aim of this work was to evaluate the biological properties of one citrate-coated and two different dextran-coated paramagnetic particles with comparable size (iron core 4–10 nm). Endothelial cells from humans and mice as well as human macrophages were incubated for different time intervals with different particle suspensions. The cellular uptake was semi-quantitatively measured using the Prussian blue staining and, in addition, by cellular iron content. Furthermore the effect of known inhibitors of endocytosis was evaluated. In addition, it was evaluated whether linking of monoclonal antibodies to dextran-coated particles can make them bind specifically to certain cell surface structures. The results showed that the bEnd.3 cell line, human umbilical vein endothelial cells (HUVECs) and THP-1/macrophage cell lines internalize paramagnetic particles. The ranking of cellular uptake was: VSOP &gt; CMD-coated particles &gt;&gt; CLIO. The carboxydextran-coated SPIO uptake by endothelial cells is reduced by colchicine (50%). Conversely, cytochalasin B down-regulates the endocytosis of citrate-coated particle. Our data imply that the major mechanism of uptake would be pinocytosis for the VSOP and phagocytosis for the carboxydextran-coated particle CMD. The different surface coating can influence not only the quantity of the internalization, but also the pathway of internalization. CLIO linked to CD40 antibodies or to CD62E antibodies bound significantly better than IgG-linked CLIO. This was true especially for the anti-CD40-CLIO constructs where fluorescence increased two fold. Comparable results were observed with anti-CD62E-CLIO constructs; however, increase in fluorescence was higher than with CD40 binding; it increased on 3.9-fold (median) and 4.5-fold (mean). In conclusions, the binding of antibody-conjugated CLIO to the antigen-expressing cells was specific, with an affinity similar to that of the free antibody. Thus, it seems feasible to use antibody linked SPIOs for molecular imaging.

scholarly journals Development, Characterization and In Vitro Evaluation of Paclitaxel and Anastrozole Co-Loaded Liposome

Processes ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 1110
Author(s):  
Minh Thanh Vu ◽  
Dinh Tien Dung Nguyen ◽  
Ngoc Hoi Nguyen ◽  
Van Thu Le ◽  
The Nam Dao ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Combination Therapy ◽  
Cancer Treatment ◽  
Cancer Cells ◽  
Breast Cancer Treatment ◽  
In Vitro Cytotoxicity ◽  
Cytotoxicity Studies ◽  
Combined Drugs

Paclitaxel (PTX) and anastrozole (ANA) have been frequently applied in breast cancer treatment. PTX is well-known for its anti-proliferative effect meanwhile ANA has just been discovered to act as an estrogen receptor α (ERα) ligand. The combination therapy of PTX and ANA is expected to improve treating efficiency, as ANA would act as a ligand binding with the ERα gene expressed in breast cancer cells and thereafter PTX would inhibit the division and cause death to those cancer cells. In this study, liposome-based nanocarriers (LP) were developed for co-encapsulation of PTX and ANA to improve the efficacy of the combined drugs in an Estrogen receptor-responsive breast cancer study. PTX-ANA co-loaded LP was prepared using thin lipid film hydration method and was characterized for morphology, size, zeta potential, drug encapsulation and in vitro drug release. In addition, cell proliferation (WST assay) and IN Cell Analyzer were used for in vitro cytotoxicity studies on a human breast cancer cell line (MCF-7). Results showed that the prepared LP and PTX-ANA-LP had spherical vesicles, with a mean particle size of 170.1 ± 13.5 nm and 189.0 ± 22.1 nm, respectively. Controlled and sustained releases were achieved at 72 h for both of the loaded drugs. The in vitro cytotoxicity study found that the combined drugs showed higher toxicity than each single drug separately. These results suggested a new approach to breast cancer treatment, consisting of the combination therapy of PTX and ANA in liposomes based on ER response.

scholarly journals Biomimetic gradient scaffold of collagen–hydroxyapatite for osteochondral regeneration

2020 ◽  
Vol 11 ◽  
pp. 204173141989606 ◽  
Author(s):  
Cristian Parisi ◽  
Luca Salvatore ◽  
Lorenzo Veschini ◽  
Maria Paola Serra ◽  
Carl Hobbs ◽  
...  
Keyword(s):  
Biological Properties ◽  
Biological Evaluation ◽  
Mechanical Tests ◽  
Host Cells ◽  
Smooth Transition ◽  
Treatment Modalities ◽  
Chemical Compositions ◽  
Osteochondral Defects

Osteochondral defects remain a major clinical challenge mainly due to the combined damage to the articular cartilage and the underlying bone, and the interface between the two tissues having very different properties. Current treatment modalities have several limitations and drawbacks, with limited capacity of restoration; however, tissue engineering shows promise in improving the clinical outcomes of osteochondral defects. In this study, a novel gradient scaffold has been fabricated, implementing a gradient structure in the design to mimic the anatomical, biological and physicochemical properties of bone and cartilage as closely as possible. Compared with the commonly studied multi-layer scaffolds, the gradient scaffold has the potential to induce a smooth transition between cartilage and bone and avoid any instability at the interface, mimicking the natural structure of the osteochondral tissue. The scaffold comprises a collagen matrix with a gradient distribution of low-crystalline hydroxyapatite particles. Physicochemical analyses confirmed phase and chemical compositions of the gradient scaffold and the distribution of the mineral phase along the gradient scaffold. Mechanical tests confirmed the gradient of stiffness throughout the scaffold, according to its mineral content. The gradient scaffold exhibited good biological performances both in vitro and in vivo. Biological evaluation of the scaffold, in combination with human bone-marrow–derived mesenchymal stem cells, demonstrated that the gradient of composition and stiffness preferentially increased cell proliferation in different sub-regions of the scaffold, according to their high chondrogenic or osteogenic characteristics. The in vivo biocompatibility of the gradient scaffold was confirmed by its subcutaneous implantation in rats. The gradient scaffold was significantly colonised by host cells and minimal foreign body reaction was observed. The scaffold’s favourable chemical, physical and biological properties demonstrated that it has good potential as an engineered osteochondral analogue for the regeneration of damaged tissue.

scholarly journals Silica-Coated Europium-Doped Gadolinium Oxide Nanorods for Dual-Modal Imaging of Cancer Cells

NANO ◽  
2017 ◽  
Vol 12 (06) ◽  
pp. 1750073 ◽  
Author(s):  
T. Gayathri ◽  
R. Arun Kumar ◽  
B. S. Panigrahi ◽  
B. Devanand
Keyword(s):  
Cancer Cells ◽  
Synthesis Method ◽  
Life Time ◽  
Gadolinium Oxide ◽  
In Vitro Cytotoxicity ◽  
Precipitation Method ◽  
Osteosarcoma Cell ◽  
Oxide Nanorods ◽  
Prepared Nanorods

Dual-modal imaging of cancer cells is possible with the silica-coated europium-doped gadolinium oxide nanorods due to their magnetic and luminescent properties. In the synthesized nanorods, europium ions serve as ‘luminescent centers’ facilitating optical imaging and gadolinium oxide acts as the contrast agent for magnetic resonance imaging (MRI). This article reports the synthesis method of the europium-doped gadolinium oxide (Eu:Gd2O[Formula: see text] nanorods by the co-precipitation method. The prepared nanorods are further coated with silica to improve its biocompatibility. From the x-ray diffraction (XRD) data, the crystallinity was found to decrease due to the amorphous nature of the silica. Transmission electron microscopy (TEM) studies show that Eu:Gd2O3 nanorods with a length of [Formula: see text][Formula: see text]600[Formula: see text]nm and diameter of [Formula: see text][Formula: see text]40[Formula: see text]nm were formed. Silica was coated uniformly with the thickness of [Formula: see text][Formula: see text]15[Formula: see text]nm. Fourier transform infrared spectroscopy (FTIR) confirms the presence of silica in the prepared nanorods. Emission at 611[Formula: see text]nm due the presence of Eu[Formula: see text] ions was observed. The life time of uncoated and silica-coated nanorods was calculated to be 1.1[Formula: see text]ms and 0.9[Formula: see text]ms, respectively. In vitro cytotoxicity of the synthesized nanorods in MG63 (human osteosarcoma cell line) was assessed by MTT assay. In vitro MRI studies reveal that the prepared nanorods can be used for T1 contrast enhancement.

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