scholarly journals Anti-Cancer and Electrochemical Properties of Thiogenistein—New Biologically Active Compound

2021 ◽  
Vol 22 (16) ◽  
pp. 8783
Author(s):  
Elżbieta U. Stolarczyk ◽  
Weronika Strzempek ◽  
Marta Łaszcz ◽  
Andrzej Leś ◽  
Elżbieta Menaszek ◽  
...  
Keyword(s):  
Oxidation Reaction ◽  
Oxidation Mechanism ◽  
Gold Surface ◽  
Biologically Active ◽  
Self Assembled Monolayer ◽  
Molecular Mechanics Calculations ◽  
Normal Prostate ◽  
Prostate Epithelial Cells ◽  
Before And After

Pharmacological and nutraceutical effects of isoflavones, which include genistein (GE), are attributed to their antioxidant activity protecting cells against carcinogenesis. The knowledge of the oxidation mechanisms of an active substance is crucial to determine its pharmacological properties. The aim of the present work was to explain complex oxidation processes that have been simulated during voltammetric experiments for our new thiolated genistein analog (TGE) that formed the self-assembled monolayer (SAM) on the gold electrode. The thiol linker assured a strong interaction of sulfur nucleophiles with the gold surface. The research comprised of the study of TGE oxidative properties, IR-ATR, and MALDI-TOF measurements of SAM before and after electrochemical oxidation. TGE has been shown to be electrochemically active. It undergoes one irreversible oxidation reaction and one quasi-reversible oxidation reaction in PBS buffer at pH 7.4.. The oxidation of TGE results in electroactive products composed likely from TGE conjugates (e.g., trimers) as part of polymer. The electroactive centers of TGE and its oxidation mechanism were discussed using IR supported by quantum chemical and molecular mechanics calculations. Preliminary in-vitro studies indicate that TGE exhibits higher cytotoxic activity towards DU145 human prostate cancer cells and is safer for normal prostate epithelial cells (PNT2) than genistein itself.

An electrokinetic-combined electrochemical study of the glucose electro-oxidation reaction: effect of gold surface energy

RSC Advances ◽  
2016 ◽  
Vol 6 (19) ◽  
pp. 15630-15638 ◽  
Author(s):  
N. Arjona ◽  
G. Trejo ◽  
J. Ledesma-García ◽  
L. G. Arriaga ◽  
M. Guerra-Balcázar
Keyword(s):  
Surface Energy ◽  
Oxidation Reaction ◽  
Oxidation Mechanism ◽  
Gold Surface ◽  
Electrochemical Study ◽  
Gold Surfaces ◽  
Electro Oxidation ◽  
Effect Of Glucose

Electrokinetic analysis demonstrates the effect of glucose adsorption on gold surfaces in the glucose electro-oxidation mechanism.

scholarly journals Theoretical prediction and experimental measurement of the bile-pigment isomer pattern obtained from degradation of catalase haem

1986 ◽  
Vol 236 (1) ◽  
pp. 303-306 ◽  
Author(s):  
N J Brindle ◽  
A C T North ◽  
S B Brown
Keyword(s):  
Theoretical Prediction ◽  
Oxidation Reaction ◽  
Three Dimensional ◽  
Oxygen Molecule ◽  
Bile Pigment ◽  
Molecular Mechanics Calculations ◽  
Protein Moiety ◽  
Relative Accessibility

Degradation in vitro of the haem in catalase by a ‘coupled oxidation’ reaction yields products in which approx. 45% of the haem groups have been cleaved at the alpha-methene bridge, 55% at the beta-bridge and a trace at the delta-bridge. Molecular-mechanics calculations with the three-dimensional structural co-ordinates of catalase shows that these proportions of products can be accounted for by the relative accessibility of the four methene bridges to a haem-linked oxygen molecule, thus further confirming Brown's [(1976) Biochem. J. 159, 23-27] hypothesis that the first stage of haem catabolism in vivo is selective attack by haem-bound oxygen, with selectivity conferred by the surrounding protein moiety.

scholarly journals Germacranolides from Carpesium divaricatum: Some New Data on Cytotoxic and Anti-Inflammatory Activity

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4644
Author(s):  
Natalia Kłeczek ◽  
Janusz Malarz ◽  
Barbara Gierlikowska ◽  
Łukasz Skalniak ◽  
Agnieszka Galanty ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Sesquiterpene Lactones ◽  
Inflammatory Activity ◽  
Human Neutrophils ◽  
Normal Prostate ◽  
Prostate Epithelial Cells ◽  
Tnf Α ◽  
P53 Status ◽  
Anti Inflammatory

Carpesium divaricatum Sieb. & Zucc., a traditional medicinal plant used as an inflammation-relieving remedy, is a rich source of terpenoids. At least 40 germacrane-type sesquiterpene lactones, representatives of four different structural groups, were isolated from the plant. Cytotoxicity against cancer cells in vitro is the most frequently described biological activity of the compounds. However, little is known about the selectivity of the cytotoxic effect. The anti-inflammatory activity of the germacranolides is also poorly documented. The objective of the present study was to assess the cytotoxic activity of selected C. divaricatum germacranolides-derivatives of 4,5,8,9-tetrahydroxy-3-oxo-germacran-6,12-olide towards cancer and normal cell lines (including cells of different p53 status). Moreover, to assess the anti-inflammatory effect of the compounds, the release of four proinflammatory cytokines/chemokines (IL-1β, IL-8, TNF-α and CCL2) by lipopolysaccharide-stimulated human neutrophils was measured by ELISA. The investigated sesquiterpene lactones demonstrated nonselective activity towards prostate cancer (Du145 and PC3) and normal prostate epithelial cells (PNT2) as well as against melanoma cells (A375 and HTB140) and keratinocytes (HaCaT). Cytotoxic activity against osteosarcoma cells was independent of their p53 status. In sub-cytotoxic concentrations (0.5–2.5 µM) the studied compounds significantly decreased cytokine/chemokine release by lipopolysaccharide-stimulated human leukocytes.

Effects of luteinizing hormone-releasing hormone (LRH) upon bioactive and immunoreactive serum LH in patients with Turner's syndrome before and after oestrogen treatment

1985 ◽  
Vol 109 (3) ◽  
pp. 304-308 ◽  
Author(s):  
Marco Francesco Celani ◽  
Vanna Montanini ◽  
Paolo Marrama
Keyword(s):  
Biologically Active ◽  
Delayed Response ◽  
Turner's Syndrome ◽  
Turner’S Syndrome ◽  
Oestrogen Treatment ◽  
Serum Lh ◽  
Before And After ◽  
The Mean ◽  
Ethinyl Oestradiol

Abstract. One daily dose of 0.05 mg ethinyl oestradiol was administered to 5 patients with Turner's syndrome (mean age ± sem = 16.4 ± 0.7 years) for 10 days. The effects of acute stimulation with luteinizing hormonereleasing hormone (LRH) (0.1 mg iv) on biologically active and immunoreactive LH were analysed before therapy and at the end of oestrogen treatment. Bioactive LH (BIO-LH) was measured by a sensitive and specific in vitro bioassay based upon testosterone production by mechanically dispersed mouse Leydig cell preparations. Immunoreactive LH (RIA-LH) was evaluated by a double antibody RIA method. Prior to oestrogen treatment, LRH induced a prompt rise in BIO-LH and RIA-LH levels, which reached peak values at 30 and 45 min, respectively. After oestrogen treatment, a delayed response (with peak values at 120 min) was observed for both BIO-LH and RIA-LH. Before oestrogen treatment, the mean bioactivity to immunoreactivity (B/I) ratio of LRH-stimulated LH showed a significant decrease from basal values (P < 0.05). In contrast, after ethinyl oestradiol administration the mean LH B/I ratio increased significantly from basal values in response to LRH (P < 0.05). The mean relative maximum response (Δ%) for BIO-LH was significantly higher (P < 0.05) in oestrogen-treated than in untreated patients, whereas the mean BIO-LH Δ area was significantly lower in the former group (P < 0.01). Similarly, oestrogens decreased significantly the mean RIA-LH Δ area (P < 0.05), whereas they did not affect significantly the mean RIA-LH Δ%. The results further emphasize that oestrogens may change the quality of circulating LH.

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.

scholarly journals Hydrogen Peroxide Oxidation Reaction on a 4-Mercaptopyridine Self-Assembled Monolayer on Au(111) Metallized by Platinum Nanoislands

2021 ◽  
Author(s):  
Mathias Piescheck ◽  
Areeg Abdelrahman ◽  
Johannes M. Hermann ◽  
Heiko Müller ◽  
Timo Jacob ◽  
...  
Keyword(s):  
Hydrogen Peroxide ◽  
Oxidation Reaction ◽  
Structural Changes ◽  
Systematic Investigation ◽  
Peroxide Oxidation ◽  
Self Assembled Monolayer ◽  
Hydrogen Peroxide Oxidation ◽  
Before And After ◽  
Total Current Density ◽  
Self Assembled

AbstractA systematic investigation of the hydrogen peroxide oxidation reaction (HPOR) in phosphate buffer (pH = 7.3) on an Au(111) single crystal modified with a 4-mercaptopyridine self-assembled monolayer (SAM) has been conducted before and after metallization with Pt. While bare Au(111) shows considerable electrocatalytic activity towards the HPOR, the inhibition of the oxidation reaction after modification with the SAM implies that adsorbed 4-mercaptopyridine molecules do not catalyze the HPOR. However, SAM-modified Au(111) recovers catalytic activity for the HPOR already after a single metallization step fabricating Pt islands on-top. Hydrogen peroxide (HP) may then either react at the (non-metallic) Pt nanoislands or on reactivated Au sites, made accessible by structural changes of the SAM induced by the metallization. The shape of the voltammetric profiles for the HPOR on repeatedly metallized SAMs suggests that the contribution of Au to the total current density gradually diminishes with increasing Pt coverage while the contribution of the Pt islands increases. The electrochemical behavior is dominated by the Pt islands at a coverage of 0.5 ML obtained by three subsequent metallization steps. Graphical abstract

scholarly journals The role of IKK in constitutive activation of NF-κB transcription factor in prostate carcinoma cells

2002 ◽  
Vol 115 (1) ◽  
pp. 141-151 ◽  
Author(s):  
Alexander V. Gasparian ◽  
Ya Juan Yao ◽  
Dariusz Kowalczyk ◽  
Ludmila A. Lyakh ◽  
Apollon Karseladze ◽  
...  
Keyword(s):  
Cell Lines ◽  
Prostate Carcinoma ◽  
Dominant Negative ◽  
Kinase Assay ◽  
Normal Prostate ◽  
Constitutive Activation ◽  
Prostate Epithelial Cells ◽  
Induced Apoptosis ◽  
Androgen Independent

Rel/NF-κB transcription factors are implicated in the control of cell proliferation, apoptosis and transformation. The key to NF-κB regulation is the inhibitory IκB proteins. During response to diverse stimuli, IκBs are rapidly phosphorylated by IκB kinases (IKKs), ubiquitinated and undergo degradation. We have investigated the expression and function of NF-κB, IκB inhibitors and IKKs in normal prostate epithelial cells and prostate carcinoma (PC) cell lines LNCaP, MDA PCa 2b, DU145, PC3, and JCA1. We found that NF-κB was constitutively activated in human androgen-independent PC cell lines DU145, PC3, JCA1 as well as androgen-independent CL2 cells derived from LNCaP. In spite of a strong difference in constitutive κB binding, Western blot analysis did not reveal any significant variance in the expression of p50, p65, IκBs, IKKα, and IKKβ between primary prostate cells, androgen-dependent and androgen-independent PC cells. However, we found that in androgen-independent PC cells IκBα was heavily phosphorylated and displayed a faster turnover. Using an in vitro kinase assay we demonstrated constitutive activation of IKK in androgen-independent PC cell lines. Blockage of NF-κB activity in PC cells by dominant-negative IκBα resulted in increased constitutive and TNF-α-induced apoptosis. Our data suggest that increased IKK activation leads to the constitutive activation of NF-κB ‘survival signaling’ pathway in androgen-independent PC cells. This may be important for the support of their androgen-independent status and growth advantage.

scholarly journals Tunable cytotoxic aptamer–drug conjugates for the treatment of prostate cancer

2018 ◽  
Vol 115 (18) ◽  
pp. 4761-4766 ◽  
Author(s):  
Bethany Powell Gray ◽  
Linsley Kelly ◽  
Douglas P. Ahrens ◽  
Ashley P. Barry ◽  
Christina Kratschmer ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cancer Cells ◽  
Prostate Cancer Cells ◽  
Normal Prostate ◽  
New Class ◽  
Drug Conjugates ◽  
Prostate Epithelial Cells ◽  
Organ Tissue

Therapies that can eliminate both local and metastatic prostate tumor lesions while sparing normal organ tissue are desperately needed. With the goal of developing an improved drug-targeting strategy, we turned to a new class of targeted anticancer therapeutics: aptamers conjugated to highly toxic chemotherapeutics. Cell selection for aptamers with prostate cancer specificity yielded the E3 aptamer, which internalizes into prostate cancer cells without targeting normal prostate cells. Chemical conjugation of E3 to the drugs monomethyl auristatin E (MMAE) and monomethyl auristatin F (MMAF) yields a potent cytotoxic agent that efficiently kills prostate cancer cells in vitro but does not affect normal prostate epithelial cells. Importantly, the E3 aptamer targets tumors in vivo and treatment with the MMAF-E3 conjugate significantly inhibits prostate cancer growth in mice, demonstrating the in vivo utility of aptamer–drug conjugates. Additionally, we report the use of antidotes to block E3 aptamer–drug conjugate cytotoxicity, providing a safety switch in the unexpected event of normal cell killing in vivo.

Electron microscopic study of the membrane glycoproteins in the rat kidney after cisplatin treatment

1989 ◽  
Vol 47 ◽  
pp. 912-913
Author(s):  
S.K. Aggarwal
Keyword(s):  
Alkaline Phosphatase ◽  
Rat Kidney ◽  
Light And Electron Microscopy ◽  
Kidney Tissue ◽  
Membrane Glycoproteins ◽  
Electron Microscopic ◽  
Before And After ◽  
Interstrand Cross Links ◽  
Cross Links

The proposed primary mechanism of action of the anticancer drug cisplatin (Cis-DDP) is through its interaction with DNA, mostly through DNA intrastrand cross-links or DNA interstrand cross-links. DNA repair mechanisms can circumvent this arrest thus permitting replication and transcription to proceed. Various membrane transport enzymes have also been demonstrated to be effected by cisplatin. Glycoprotein alkaline phosphatase was looked at in the proximal tubule cells before and after cisplatin both in vivo and in vitro for its inactivation or its removal from the membrane using light and electron microscopy.Outbred male Swiss Webster (Crl: (WI) BR) rats weighing 150-250g were given ip injections of cisplatin (7mg/kg). Animals were killed on day 3 and day 5. Thick slices (20-50.um) of kidney tissue from treated and untreated animals were fixed in 1% buffered glutaraldehyde and 1% formaldehyde (0.05 M cacodylate buffer, pH 7.3) for 30 min at 4°C. Alkaline phosphatase activity and carbohydrates were demonstrated according to methods described earlier.

Structural integrity after cold storage of human epidermal model in hypothermosol: A correlative ultrastructural and fluorescent assay

1994 ◽  
Vol 52 ◽  
pp. 270-271
Author(s):  
Henry H. Eichelberger ◽  
John G. Baust ◽  
Robert G. Van Buskirk
Keyword(s):  
Cold Storage ◽  
Structural Integrity ◽  
Culture Media ◽  
Cell Structure ◽  
Natural State ◽  
Sodium Cacodylate ◽  
Ruthenium Tetroxide ◽  
Cacodylate Buffer ◽  
Before And After

For research in cell differentiation and in vitro toxicology it is essential to provide a natural state of cell structure as a benchmark for interpreting results. Hypothermosol (Cryomedical Sciences, Rockville, MD) has proven useful in insuring the viability of synthetic human epidermis during cold-storage and in maintaining the epidermis’ ability to continue to differentiate following warming.Human epidermal equivalent, EpiDerm (MatTek Corporation, Ashland, MA) consisting of fully differentiated stratified human epidermal cells were grown on a microporous membrane. EpiDerm samples were fixed before and after cold-storage (4°C) for 5 days in Hypothermosol or skin culture media (MatTek Corporation) and allowed to recover for 7 days at 37°C. EpiDerm samples were fixed 1 hour in 2.5% glutaraldehyde in sodium cacodylate buffer (pH 7.2). A secondary fixation with 0.2% ruthenium tetroxide (Polysciences, Inc., Warrington, PA) in sodium cacodylate was carried out for 3 hours at 4°C. Other samples were similarly fixed, but with 1% Osmium tetroxide in place of ruthenium tetroxide. Samples were dehydrated through a graded acetone series, infiltrated with Spurrs resin (Polysciences Inc.) and polymerized at 70°C.

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