scholarly journals Synthesis, Characterisation and In Vitro Anticancer Activity of Catalytically Active Indole-Based Half-Sandwich Complexes

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4540
Author(s):  
Joan J. Soldevila-Barreda ◽  
Kehinde B. Fawibe ◽  
Maria Azmanova ◽  
Laia Rafols ◽  
Anaïs Pitto-Barry ◽  
...  
Keyword(s):  
Sodium Formate ◽  
In Vitro Cytotoxicity ◽  
High Turnover ◽  
Normal Prostate ◽  
Prostate Cell ◽  
Ovarian Cancer Cell Lines ◽  
Catalytically Active ◽  
Half Sandwich ◽  
In Cells

The synthesis, characterisation and evaluation of the in vitro cytotoxicity of four indole-based half-sandwich metal complexes towards two ovarian cancer cell lines (A2780 and A2780cisR) and one normal prostate cell line (PNT2) are presented herein. Although capable of inducing catalytic oxidation of NADH and able to reduce NAD+ with high turnover frequencies, in cells and in the presence of sodium formate, these complexes also strongly interact with biomolecules such as glutathione. This work highlights that efficient out-of-cells catalytic activity might lead to higher reactivity towards biomolecules, thus inhibiting the in-cells catalytic processes.

scholarly journals Synthesis and Properties of CurNQ for the Theranostic Application in Ovarian Cancer Intervention

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4471
Author(s):  
Lara G. Freidus ◽  
Pradeep Kumar ◽  
Thashree Marimuthu ◽  
Priyamvada Pradeep ◽  
Viness Pillay ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cancer Detection ◽  
Ovarian Cancer Cell ◽  
In Vitro Cytotoxicity ◽  
Cancer Targeting ◽  
The Novel ◽  
Cytotoxicity Assays ◽  
Ovarian Cancer Cell Lines ◽  
Cancer Intervention

Synthesis of a novel theranostic molecule for targeted cancer intervention. A reaction between curcumin and lawsone was carried out to yield the novel curcumin naphthoquinone (CurNQ) molecule (2,2′-((((1E,3Z,6E)-3-hydroxy-5-oxohepta-1,3,6-triene-1,7-diyl) bis(2-methoxy-4,1-phenylene))bis(oxy))bis(naphthalene-1,4-dione). CurNQ’s structure was elucidated and was fully characterized. CurNQ was demonstrated to have pH specific solubility, its saturation solubility increased from 11.15 µM at pH 7.4 to 20.7 µM at pH 6.8. This pH responsivity allows for cancer targeting (Warburg effect). Moreover, CurNQ displayed intrinsic fluorescence, thus enabling imaging and detection applications. In vitro cytotoxicity assays demonstrated the chemotherapeutic properties of CurNQ as CurNQ reduced cell viability to below 50% in OVCAR-5 and SKOV3 ovarian cancer cell lines. CurNQ is a novel theranostic molecule for potential targeted cancer detection and treatment.

scholarly journals In Vitro Anti-Prostate Cancer Activity of Two Ebselen Analogues

2020 ◽  
Vol 13 (3) ◽  
pp. 47 ◽  
Author(s):  
Katarzyna B. Kaczor-Keller ◽  
Anna Pawlik ◽  
Jacek Scianowski ◽  
Agata Pacuła ◽  
Magdalena Obieziurska ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cancer Cell ◽  
Biological Activities ◽  
Cytotoxic Action ◽  
Organoselenium Compounds ◽  
M Cell ◽  
Normal Prostate ◽  
Prostate Cell ◽  
Anticancer Mechanism

Scientific research has been underway for decades in order to develop an effective anticancer drug, and it has become crucial to find a novel and effective chemotherapeutics in the case of prostate cancer treatment. Ebselen derivatives have been shown to possess a variety of biological activities, including cytostatic and cytotoxic action against tumor cells. In this study, the cytotoxic effect and anticancer mechanism of action of two organoselenium compounds— (N-allyl-1,2-benzisoselenazol-3(2H)-one (N-allyl-BS) and N-(3-methylbutyl)-1,2-benzisoselenazol-3(2H)-one) (N-(3-mb)-BS)—were investigated on two phenotypically different prostate cancer cell lines DU 145 and PC-3. The influence of analyzed compounds on the viability parameter was also assessed on normal prostate cell line PNT1A. The results showed that both organoselenium compounds (OSCs) efficiently inhibited cancer cell proliferation, whereas normal PNT1A cells were less sensitive to the analazyed ebselen analouges. Both OSCs induced G2/M cell cycle arrest and prompted cell death through apoptosis. The detection of cleaved Poly (ADP-ribose) Polymerase (PARP) confirmed this. In addition, N-allyl-BS and N-(3-m)-b-BS increased the level of reactive oxygen species (ROS) formation, however only N-allyl-BS induced DNA damage. Based on our data, we assume that OSCs’ anticancer action can be associated with oxidative stress induction and inactivation of the Akt- dependent signalling pathway. In conclusion, our data demonstrate that ebselen derivatives showed strong cytotoxic efficiency towards prostate cancer cells and may be elucidated as a novel, potent anticancer agent.

In vitro Cytotoxicity of Half-Sandwich Platinum Group Metal Complexes of a Cationic Alkylated Phosphaadamantane Ligand

2016 ◽  
Vol 2016 (8) ◽  
pp. 1267-1273 ◽  
Author(s):  
Andrew R. Burgoyne ◽  
Catherine H. Kaschula ◽  
M. Iqbal Parker ◽  
Gregory S. Smith
Keyword(s):  
Metal Complexes ◽  
Platinum Group Metal ◽  
In Vitro Cytotoxicity ◽  
Group Metal ◽  
Platinum Group ◽  
Half Sandwich

Comparison of human normal and neoplastic prostate epithelial cells by TEM and quantitative image analysis and morphometry (QIAM)

1994 ◽  
Vol 52 ◽  
pp. 86-87
Author(s):  
J. T. Gau ◽  
M. L. Grove ◽  
S. Strom ◽  
R. Orsini ◽  
K. C. Song ◽  
...  
Keyword(s):  
Epithelial Cells ◽  
Membrane Trafficking ◽  
Growth Regulation ◽  
Cellular Growth ◽  
Cell Trafficking ◽  
Normal Prostate ◽  
Prostate Cell ◽  
Prostate Epithelial Cells

Prostate cancer is the most common tumor in men in the U.S.A. The regulation of growth control in normal prostate cells and its contribution to tumor progression is a subject of intense investigation.Recently our group developed culture techniques that allowed us to study normal and neoplastic human prostate epithelial cells from human prostatectomy specimens. Since quantitative evaluation of intracellular compartments will be critical to defining the role of membrane trafficking in the growth regulation, we used TEM and QIAM to characterize normal and neoplastic prostate epithelial cells invivo, as well as in vitro. This work will serve as a baseline to subsequent studies using perturbants of cell trafficking and conditions ;hat promote or block cellular growth, to investigate the role of growth factors and stromal/epithelial nteraction in prostate growth regulation.Normal and neoplastic tissues were sampled for ultrastructural examination from grid mapped radical prostatectomy specimens that were processed for whole mounts. The SV40 immortalized "normal" prostate cell line (P69) was provided by Dr. Strom.

USP2a is an oncogenic isopeptidase and a potential target in prostate cancer

2006 ◽  
Vol 24 (18_suppl) ◽  
pp. 14522-14522
Author(s):  
C. Priolo ◽  
D. Tang ◽  
M. Brahmandam ◽  
B. Benassi ◽  
E. Sicinska ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Nude Mice ◽  
Fatty Acid Synthase ◽  
Chemotherapeutic Agents ◽  
Human Prostate ◽  
Wild Type ◽  
Normal Prostate ◽  
Prostate Cell

14522 Background: De-ubiquitinating enzymes (isopeptidases) remove ubiquitin side chains prior to degradation by the proteosome thus stabilizing their protein targets. We have identified a novel androgen regulated isopeptidase, USP2a, and demonstrated that it binds and prolongs the half-life of fatty acid synthase (FAS), a key enzyme in lipid metabolism of tumor cells. Methods: We determined whether USP2a has oncogenic properties in vitro and in vivo. Wild-type and catalytically inactive USP2a were introduced in immortalized normal prostate epithelial cells (AR-iPrECs). Clonogenicity assays and apoptosis induction by chemotherapeutic agents were performed on these cells. Anti-USP2a siRNA were transfected in normal and transformed (LNCaP, DU145 and PC-3) prostate cell lines. Oncogenicity in vivo was shown by s.c. injection of NIH3T3-USP2a cells in nude mice. Furthermore, USP2a mRNA expression and gene microarrays were tested in 52 human prostate adenocarcinomas. Results: Wild-type USP2a overexpression in AR-iPrEC cells resulted in a significant increase in number and size of colonies compared to those obtained in parental cells. Growth in soft agar was significantly enhanced as well. Silencing of USP2a in LNCAP and DU145 cells resulted in a strong apoptotic effect, evaluated by FACS analysis and cleaved-PARP expression. The role of this isopeptidase in apoptosis regulation was confirmed on AR-iPrEC-USP2a cells, that showed resistance to apoptosis induced by cisplatin and taxol. Importantly, USP2a overexpression was able to transform NIH3T3 cells, generating greater than or equal to 0.5 cm subcutaneous tumors in 12/12 nude mice within 3 weeks, while none of the negative controls grew. USP2a mRNA was overexpressed in 39% of human prostate cancers, showing 1.6–104 (median 5.48) fold induction relative to normal tissues by qRT-PCR. Gene expression profiling of the same tumors revealed specific signatures in USP2a-overexpressing tumors. Conclusions: Our results demonstrate that USP2a behaves as an oncogene in vitro and in vivo and is overexpressed in organ-confined prostate cancer. These data strongly suggest that this isopeptidase is a potential drug target in prostate cancer. [Table: see text]

A half-sandwich TaV dichlorido complex containing an O,N,O′-tridentate Schiff base ligand: synthesis, crystal structure and in vitro cytotoxicity

2019 ◽  
Vol 75 (3) ◽  
pp. 248-254 ◽  
Author(s):  
Zdeněk Trávníček ◽  
Pavel Štarha ◽  
Michal Čajan ◽  
Zdeněk Dvořák
Keyword(s):  
Crystal Structure ◽  
Schiff Base ◽  
Density Functional ◽  
In Vitro Cytotoxicity ◽  
X Ray Diffraction ◽  
Ovarian Carcinoma Cell Line ◽  
Functional Theory ◽  
Human Ovarian Carcinoma ◽  
Half Sandwich

A new electroneutral half-sandwich tantalum(V) dichlorido complex containing pentamethylcyclopentadienyl (Cp*) and the double-deprotonated version of the Schiff base 2-ethoxy-6-{(E)-[(2-hydroxyphenyl)imino]methyl}phenol (H2 L) as ligands, namely cis-dichlorido(2-ethoxy-6-{(E)-[(2-oxidophenyl)imino]methyl}phenolato-κ3 O,N,O′)(η5-pentamethylcyclopentadienyl)tantalum(V), [Ta(C10H15)(C15H13NO3)Cl2] or [Ta(η5-Cp*)(L)Cl2], has been prepared and thoroughly characterized by elemental analysis, IR and NMR spectroscopy, mass spectrometry, density functional theory (DFT) calculations and single-crystal X-ray diffraction. The molecular structure revealed that the TaV centre is coordinated by a η5-Cp* ligand, two monodentate chlorido ligands and one O,N,O′-tridentate L 2− ligand. The crystal structure is stabilized by C—H...C, C—H...Cl and C...C intermolecular interactions. Moreover, the complex shows notable in vitro cytotoxicity against the A2780 human ovarian carcinoma cell line, with IC50 = 14.4 µM, which is higher than that of the conventional platinum-based anticancer drug cisplatin (IC50 = 20.1 µM).

Half-sandwich Ru(η6-p-cymene) complexes featuring pyrazole appended ligands: Synthesis, DNA binding and in vitro cytotoxicity

2019 ◽  
Vol 194 ◽  
pp. 74-84 ◽  
Author(s):  
Yen-Chung Huang ◽  
Jebiti Haribabu ◽  
Ching-Ming Chien ◽  
Gopal Sabapathi ◽  
Chon-Kit Chou ◽  
...  
Keyword(s):  
Dna Binding ◽  
In Vitro Cytotoxicity ◽  
Half Sandwich
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