scholarly journals 8-Hydroxyquinoline Glycoconjugates: Modifications in the Linker Structure and Their Effect on the Cytotoxicity of the Obtained Compounds

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4181 ◽  
Author(s):  
Monika Krawczyk ◽  
Gabriela Pastuch-Gawołek ◽  
Aleksandra Pluta ◽  
Karol Erfurt ◽  
Adrian Domiński ◽  
...  
Keyword(s):  
Cancer Progression ◽  
Cytotoxic Effect ◽  
Copper Ions ◽  
Nitrogen Heterocycles ◽  
Anti Cancer ◽  
Hct 116 ◽  
Complexing Properties ◽  
Sugar Derivatives ◽  
Derivatives Of ◽  
Mcf 7

Small molecule nitrogen heterocycles are very important structures, widely used in the design of potential pharmaceuticals. Particularly, derivatives of 8-hydroxyquinoline (8-HQ) are successfully used to design promising anti-cancer agents. Conjugating 8-HQ derivatives with sugar derivatives, molecules with better bioavailability, selectivity, and solubility are obtained. In this study, 8-HQ derivatives were functionalized at the 8-OH position and connected with sugar derivatives (D-glucose or D-galactose) substituted with different groups at the anomeric position, using copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition (CuAAC). Glycoconjugates were tested for inhibition of the proliferation of cancer cell lines (HCT 116 and MCF-7) and inhibition of β-1,4-galactosyltransferase activity, which overexpression is associated with cancer progression. All glycoconjugates in protected form have a cytotoxic effect on cancer cells in the tested concentration range. The presence of additional amide groups in the linker structure improves the activity of glycoconjugates, probably due to the ability to chelate metal ions present in many types of cancers. The study of metal complexing properties confirmed that the obtained glycoconjugates are capable of chelating copper ions, which increases their anti-cancer potential.

Synthesis, spectral, molecular modeling, biological and antitumor studies of new nifuroxazide complexes

2021 ◽  
Vol 11 (7) ◽  
pp. 1071-1083
Author(s):  
Eid H. Alosaimi ◽  
Walaa H. El-Shwiniy ◽  
Saad M. Alshahrani ◽  
Ayman A. O. Younes ◽  
Mostafa Y. Nassar ◽  
...  
Keyword(s):  
Bacterial Species ◽  
Thermal Analyses ◽  
Molar Conductance ◽  
Cancer Drug ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Anti Cancer ◽  
Hct 116 ◽  
Mcf 7

Series of Zr(IV), Ce(IV) and U(VI) complexes were synthesized with nifuroxazide ligand. Design and formulae of the complexes suggested in the light of analytical, spectral, magnetic and thermal analyses (1HNMR, IR, UV-Vis). The calculated values of molar conductance mean that, all isolated complexes were electrolytes. The data revealed the complexes formation and suggested that nifuroxazide binds as a bidentate at NO sites with metal ions. The kinetic parameters evaluated using Coats Redfern (CR) and Horowitz-Metzeger (HM) methods. The thermodynamic data reflect the thermal stability for all complexes. The calculated bond length and force constant values for UO2 bond are 1.741 Å and 459.409 Nm−1. The research investigations were related to quantum chemical calculations conducted at the theory level of DFT/B3LYP/LANL2DZ. The nifuroxazide, inorganic salts and their metal complexes were assayed against different bacterial species as well as the in vitro growth inhibitory activity against human breast carcinoma (MCF-7) and HCT-116 cell lines. Zr(IV) complex was found to have the highest activity against all the tested organisms and a powerful anti-cancer drug.

Sulfamic and succinic acid derivatives of 25-OH-PPD and their activities to MCF-7, A-549, HCT-116, and BGC-823 cell lines

2017 ◽  
Vol 27 (4) ◽  
pp. 1076-1080 ◽  
Author(s):  
Wu-Xi Zhou ◽  
Jia-Qing Cao ◽  
Xu-De Wang ◽  
Jun-Hui Guo ◽  
Yu-Qing Zhao
Keyword(s):  
Succinic Acid ◽  
Cell Lines ◽  
Hct 116 ◽  
Derivatives Of ◽  
Mcf 7

scholarly journals The Nuclease from Gram-Negative Bacteria Serratia Marcescens is Weakly Cytotoxic at Therapeutic Doses

2020 ◽  
Vol 5 (2) ◽  
pp. 1-8
Author(s):  
Maria Filimonova
Keyword(s):  
Cytotoxic Effect ◽  
Culture Medium ◽  
Normal Skin ◽  
Biochemical Properties ◽  
Gram Negative Bacteria ◽  
Physical Chemical ◽  
Human Cell Cultures ◽  
Hct 116 ◽  
Therapeutic Doses ◽  
Mcf 7

The nuclease from S.marcescens heads a family of homological nonspecific nucleases. Its cultivation features, structure, mechanism of action, some physical, chemical and biochemical properties are well studied. It is presented by two isoforms, differing by N-terminal fragment and some properties. The nuclease demonstrated a cancer suppressing effect in mice. It is a key component of the anti-rabies composition which increases survival of the infected mice. It is similar by its efficiency to Pulmozyme® that is used for airway cleansing during the treatment of pulmonary diseases. The aim of the study was to analyze a cytotoxic effect of S. marcescens nuclease and its separate isoforms at different concentrations. To determine the cytotoxicity we used MTT assay and human cell cultures of colorectal cancer -HCT 116, breast cancer MCF-7 and normal skin fibroblasts. Results show that the nuclease demonstrates a weak cytotoxic effect at the amounts of 0.2 – 25 µg per 1 ml of the cell culture medium that is close to its therapeutic doses. This effect is not connected with the loss of the enzymatic activity. The isoforms are similar by their IC50.

scholarly journals Synthesis, Characterization, and Cytotoxicity of Binuclear Cooper(II)-Complexes with some S-Alkenyl Derivatives of Thiosalicyclic Acid

2017 ◽  
Vol 18 (1) ◽  
pp. 13-18 ◽  
Author(s):  
Dusan Lj. Tomovic ◽  
Andriana M. Bukonjic ◽  
Aleksandar Kocovic ◽  
Milos V. Nikolic ◽  
Marina Z. Mijajlovic ◽  
...  
Keyword(s):  
Cytotoxic Effect ◽  
Magnetic Measurements ◽  
Human Colon ◽  
Carcinoma Cells ◽  
Thiosalicylic Acid ◽  
Colon Carcinoma Cells ◽  
Human Colon Carcinoma ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Derivatives Of

Abstract New complexes of copper(II) with S-alkenyl derivatives of thiosalicylic acid (alkenyl = propenyl-(L1), isobutenyl-(L2)) have been synthesized and characterized by microanalysis, infrared spectra, magnetic measurements, and by NMR spectra. The cytotoxic activity of two newly synthesized precursor S-alkenyl derivatives of thiosalicylic acid were tested using an MTT colorimetric technique on HCT-116 human colon carcinoma cells. The cytotoxic effect of the copper(II)- complexes were higher compared to the cytotoxicity of the corresponding ligand (for concentrations from 31.25 to 250 μM). Copper(II)-complexes showed a slightly lower cytotoxicity compared to cisplatin. Complexes of copper(II) with S-alkenyl derivatives of thiosalicylic acid (at concentrations from 250 to 1000 μM) had a cytotoxic effect on HCT-116 cells compared to cisplatin.

scholarly journals Incorporation of Sulfonamide Moiety into Biguanide Scaffold Results in Apoptosis Induction and Cell Cycle Arrest in MCF-7 Breast Cancer Cells

2021 ◽  
Vol 22 (11) ◽  
pp. 5642
Author(s):  
Magdalena Markowicz-Piasecka ◽  
Karol Sadowski ◽  
Johanna Huttunen ◽  
Joanna Sikora ◽  
Kristiina M. Huttunen
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cell Growth ◽  
Cellular Uptake ◽  
Apoptosis Induction ◽  
Cell Growth Inhibition ◽  
Cycle Arrest ◽  
Anti Cancer ◽  
Derivatives Of ◽  
Mcf 7

Metformin, apart from its glucose-lowering properties, has also been found to demonstrate anti-cancer properties. Anti-cancer efficacy of metformin depends on its uptake in cancer cells, which is mediated by plasma membrane monoamine transporters (PMAT) and organic cation transporters (OCTs). This study presents an analysis of transporter mediated cellular uptake of ten sulfonamide-based derivatives of metformin in two breast cancer cell lines (MCF-7 and MDA-MB-231). Effects of these compounds on cancer cell growth inhibition were also determined. All examined sulfonamide-based analogues of metformin were characterized by greater cellular uptake in both MCF-7 and MDA-MB-231 cells, and stronger cytotoxic properties than those of metformin. Effective intracellular transport of the examined compounds in MCF-7 cells was accompanied by high cytotoxic activity. For instance, compound 2 with meta-methyl group in the benzene ring inhibited MCF-7 growth at micromolar range (IC50 = 87.7 ± 1.18 µmol/L). Further studies showed that cytotoxicity of sulfonamide-based derivatives of metformin partially results from their ability to induce apoptosis in MCF-7 and MDA-MB-231 cells and arrest cell cycle in the G0/G1 phase. In addition, these compounds were found to inhibit cellular migration in wound healing assay. Importantly, the tested biguanides are more effective in MCF-7 cells at relatively lower concentrations than in MDA-MB-231 cells, which proves that the effectiveness of transporter-mediated accumulation in MCF-7 cells is related to biological effects, including MCF-7 cell growth inhibition, apoptosis induction and cell cycle arrest. In summary, this study supports the hypothesis that effective transporter-mediated cellular uptake of a chemical molecule determines its cytotoxic properties. These results warrant a further investigation of biguanides as putative anti-cancer agents.

Design, Synthesis and In Vitro Anti-Cancer Evaluation of Novel Derivatives of 2-(2-Methyl-1,5-diaryl-1H-pyrrol-3-yl)-2-oxo-N-(pyridin-3- yl)acetamide

2020 ◽  
Vol 16 (3) ◽  
pp. 340-349
Author(s):  
Ebrahim S. Moghadam ◽  
Farhad Saravani ◽  
Ernest Hamel ◽  
Zahra Shahsavari ◽  
Mohsen Alipour ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Peripheral Neuropathy ◽  
Cell Line ◽  
Normal Cell ◽  
Caspase 3 ◽  
Annexin V ◽  
Normal Cell Line ◽  
Anti Cancer ◽  
Mcf 7

Objective: Several anti-tubulin agents were introduced for the cancer treatment so far. Despite successes in the treatment of cancer, these agents cause toxic side effects, including peripheral neuropathy. Comparing anti-tubulin agents, indibulin seemed to cause minimal peripheral neuropathy, but its poor aqueous solubility and other potential clinical problems have led to its remaining in a preclinical stage. Methods: Herein, indibulin analogues were synthesized and evaluated for their in vitro anti-cancer activity using MTT assay (on the MCF-7, T47-D, MDA-MB231 and NIH-3T3 cell lines), annexin V/PI staining assay, cell cycle analysis, anti-tubulin assay and caspase 3/7 activation assay. Results: One of the compounds, 4a, showed good anti-proliferative activity against MCF-7 cells (IC50: 7.5 μM) and low toxicity on a normal cell line (IC50 > 100 μM). All of the tested compounds showed lower cytotoxicity on normal cell line in comparison to reference compound, indibulin. In the annexin V/PI staining assay, induction of apoptosis in the MCF-7 cell line was observed. Cell cycle analysis illustrated an increasing proportion of cells in the sub-G-1 phase, consistent with an increasing proportion of apoptotic cells. No increase in G2/M cells was observed, consistent with the absence of anti-tubulin activity. A caspase 3/7 assay protocol showed that apoptosis induction by more potent compounds was due to activation of caspase 3. Conclusion: Newly synthesized compounds exerted acceptable anticancer activity and further investigation of current scaffold would be beneficial.

Derivatives of Deoxypodophyllotoxin Induce Apoptosis Through Bcl-2/Bax Proteins Expression

2020 ◽  
Vol 20 ◽  
Author(s):  
Ya-Nan Li ◽  
Ni Ning ◽  
Lei Song ◽  
Yun Geng ◽  
Jun-Ting Fan ◽  
...  
Keyword(s):  
Annexin V ◽  
Mtt Method ◽  
Anthriscus Sylvestris ◽  
Anti Tumor Activity ◽  
Derivatives Of ◽  
Toxicity In Vitro ◽  
Ht 29 ◽  
Mcf 7

Background: Deoxypodophyllotoxin, isolated from theTraditional Chinese Medicine Anthriscus sylvestris, is well-known because of its significant antitumor activity with strong toxicity in vitro and in vivo. Objective: In this article, we synthesized a series of deoxypodophyllotoxin derivatives, and evaluated their antitumor effectiveness.Methods:The anti tumor activity of deoxypodophyllotoxin derivatives was investigated by the MTT method. Apoptosis percentage was measured by flow cytometer analysis using Annexin-V-FITC. Results: The derivatives revealed obvious cytotoxicity in the MTT assay by decreasing the number of late cancer cells. The decrease of Bcl-2/Bax could be observed in MCF-7, HepG2, HT-29 andMG-63 using Annexin V-FITC. The ratio of Bcl-2/Bax in the administration group was decreased, which was determined by the ELISA kit. Conclusion: The derivatives of deoxypodophyllotoxin could induce apoptosis in tumor cell lines by influencing Bcl-2/Bax.

Novel Findings of Anti-cancer Property of Propofol

2018 ◽  
Vol 18 (2) ◽  
pp. 156-165 ◽  
Author(s):  
Jiaqiang Wang ◽  
Chien-shan Cheng ◽  
Yan Lu ◽  
Xiaowei Ding ◽  
Minmin Zhu ◽  
...  
Keyword(s):  
General Anesthesia ◽  
Cancer Progression ◽  
Molecular Mechanisms ◽  
Intravenous Anesthetic ◽  
The Past ◽  
Anti Cancer ◽  
Underlying Mechanisms ◽  
Recent Attention

Background: Propofol, a widely used intravenous anesthetic agent, is traditionally applied for sedation and general anesthesia. Explanation: Recent attention has been drawn to explore the effect and mechanisms of propofol against cancer progression in vitro and in vivo. Specifically, the proliferation-inhibiting and apoptosis-inducing properties of propofol in cancer have been studied. However, the underlying mechanisms remain unclear. Conclusion: This review focused on the findings within the past ten years and aimed to provide a general overview of propofol's malignance-modulating properties and the potential molecular mechanisms.

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