scholarly journals Synthesis and characterization of copper (II) octaazamacrocyclic complexes with glycine derivatives. In vitro antiproliferative and antimicrobial evaluation of Cu(II) and Co(II) analogous

2020 ◽  
Vol 85 (5) ◽  
pp. 637-649
Author(s):  
Branka Drazic ◽  
Mirjana Antonijevic-Nikolic ◽  
Zeljko Zizak ◽  
Sladjana Tanaskovic
Keyword(s):  
Cell Line ◽  
Magnetic Measurements ◽  
Macrocyclic Ligand ◽  
Chemical Properties ◽  
Cancer Cell Line ◽  
Myelogenous Leukemia ◽  
Boat Conformation ◽  
Human Embryonic Lung ◽  
Cell Line Hela

Two new complexes with the general formula [Cu2(L)tpmc] (ClO4)3?nH2O (tpmc = N,N?,N??,N???-tetrakis(2-pyridylmethyl)- -1,4,8,11-tetraazacyclotetradecane, L = N-methylglycine, n = 3; L = N,N- -dimethylglycine, n = 2) were isolated and their composition, some physical and chemical properties and geometries were proposed based on elemental analysis (C, H, N), conductometric and magnetic measurements and spectroscopic data (UV?Vis, FTIR). It is evident that the complexes are binuclear and an exo coordination mode of the macrocyclic ligand in the boat conformation was proposed. The co-ligands are coordinated as a bridge using both oxygen atoms of the OCO- group. The cytotoxic activity of Cu(II) complexes as well as their Co(II) analogs, the starting ligands and the free salts were tested against human cervix adenocarcinoma cell line (HeLa), human chronic myelogenous leukemia cells (K562), human breast cancer cell line (MDA-MB-453), and a non-cancerous cell line, human embryonic lung fibroblast (MRC-5). The IC50 values for the Cu(II) complexes were from 21.6?0.04 to 66.1?0.8, and for the Co(II) analogs were within the range from 8.8?0.74 to 15.40?1.52. All four complexes were tested for their antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and the yeast Candida albicans.

scholarly journals Co-Crystals of Resveratrol and Polydatin with L-Proline: Crystal Structures, Dissolution Properties, and In Vitro Cytotoxicities

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5722
Author(s):  
Yijie Lou ◽  
Kaxi Yu ◽  
Xiajun Wu ◽  
Zhaojun Wang ◽  
Yusheng Cui ◽  
...  
Keyword(s):  
Cell Line ◽  
Chemical Properties ◽  
Cancer Cell Line ◽  
Lung Cancer Cell Line ◽  
Hek 293 ◽  
Dissolution Properties ◽  
Diphenyltetrazolium Bromide ◽  
Water Ph ◽  
Physical And Chemical

Resveratrol (RSV) and polydatin (PD) have been widely used to treat several chronic diseases, such as atherosclerosis, pulmonary fibrosis, and diabetes, among several others. However, their low solubility hinders their further applications. In this work, we show that the solubility of PD can be boosted via its co-crystallization with L-proline (L-Pro). Two different phases of co-crystals, namely the RSV-L-Pro (RSV:L-Pro = 1:2) and PD-L-Pro (PD:L-Pro = 1: 3), have been prepared and characterized. As compared to the pristine RSV and PD, the solubility and dissolution rates of PD-L-Pro in water (pH 7.0) exhibited a 15.8% increase, whereas those of RSV-L-Pro exhibited a 13.8% decrease. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay of pristine RSV, PD, RSV-L-Pro, and PD-L-Pro against lung cancer cell line A549 and human embryonic kidney cell line HEK-293 indicated that both compounds showed obvious cytotoxicity against A549, but significantly reduced cytotoxicity against HEK-293, with PD/PD-L-Pro further exhibiting better biological safety than that of RSV/RSV-L-Pro. This work demonstrated that the readily available and biocompatible L-Pro can be a promising adjuvant to optimize the physical and chemical properties of RSV and PD to improve their pharmacokinetics.

scholarly journals A study of novel cobalt(II) octaazamacrocyclic complexes with aminocarboxylates or their derivatives

2009 ◽  
Vol 74 (6) ◽  
pp. 629-640 ◽  
Author(s):  
Gordana Vuckovic ◽  
Sladjana Tanaskovic ◽  
Mirjana Antonijevic-Nikolic ◽  
Vukosava Zivkovic-Radovanovic ◽  
Gordana Gojgic-Cvijovic
Keyword(s):  
Magnetic Measurements ◽  
Macrocyclic Ligand ◽  
Chemical Properties ◽  
High Spin State ◽  
Mixed Ligand ◽  
Potential Range ◽  
Boat Conformation ◽  
Physical And Chemical Properties ◽  
Physical And Chemical ◽  
And Chemical Properties

Four new air-stable mixed-ligand Co(II) complexes having the general formula [Co2(Y)tpmc]Z3?q(H2O/CH3CN) (HY = N-methylglycine/N,N-dimethylglycine, Z = - 4BF , qH2O=4 or 3; HY=S-norvaline/S-valine Z=-ClO4 , qCH3CN = 0.5; qH2O = 0.5; tpmc = N,N',N'',N'''-tetrakis(2-pyridylmethyl)- -1,4,8,11-tetraazacyclotetradecane) were prepared. The composition, some physical and chemical properties and their tentative geometries were evaluated based on elemental analysis (C, H, N), conductometric and magnetic measurements, spectroscopic data (UV/Vis, IR) and cyclic voltammetry. The data were compared with earlier described analogous complexes containing the macrocyclic ligand and aliphatic aminocarboxylates. It is assumed that all complexes are binuclear with an exo coordination mode of the octaazamacrocyclic pendant ligand in the boat conformation. In addition, two -N-(CH2)2-N- portions of the cyclam ring within the tpmc ligand and Co(II) ions in the high-spin state are most probably bridged via oxygen atoms from the anion of the aminocarboxylate/derivatives, whereas nitrogen atoms rest uncoordinated. In all cases, a combined chelate-bridged coordination is proposed as the most probable. The complexes were electrochemically stable in the potential range -1.0 to 1.0 V. They were also preliminary assayed toward some microorganisms together with the ligands, starting simple salts and solvents as test substances. In some cases, certain antimicrobial activity of the complexes was detected.

scholarly journals Synthesis of 3-(2-(subsituted-(trifluoromethyl)phenylamino)acetyl)-2H-chromen-2-one derivatives as new anticancer agents

2022 ◽  
Vol 11 (1) ◽  
pp. 105-112 ◽  
Author(s):  
Anees Pangal ◽  
Yusufi Mujahid ◽  
Bajarang Desai ◽  
Javed A. Shaikh ◽  
Khursheed Ahmed
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Cervical Cancer Cell Line ◽  
Solvent Free Conditions ◽  
Cell Line Hela ◽  
Mcf 7

Under solvent free conditions and in presence of a base 3-(2-(subsituted-(trifluoromethyl)phenylamino)acetyl)-2H-chromen-2-one derivatives were synthesized by grinding technique. Structural investigations were carried out with IR studies, HRMS, 1HNMR and 13CNMR. The compounds were checked for their in vitro anticancer activities against three different human cancer cell lines viz human breast cancer cell line (MCF-7), human cervical cancer cell line (HeLa) and human oral squamous cell carcinoma (SCC-40) using SRB method. All the title compounds showed low toxicity towards non-malignant PBMC cells indicating their tumour selectivity. The compounds exhibited good in vitro anti-proliferative potency at lower concentrations against HeLa and MCF-7 cell lines and remain moderately active against SCC-40.

scholarly journals Toxicity and Antitumor Activity of a Thiophene–Acridine Hybrid

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 64 ◽  
Author(s):  
Thaís Lisboa ◽  
Daiana Silva ◽  
Sâmia Duarte ◽  
Rafael Ferreira ◽  
Camyla Andrade ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Leukemia Cell Line ◽  
Zebrafish Embryos ◽  
Cell Line Hela ◽  
Hct 116

The antitumor effects of thiophene and acridine compounds have been described; however, the clinical usefulness of these compounds is limited due to the risk of high toxicity and drug resistance. The strategy of molecular hybridization presents the opportunity to develop new drugs which may display better target affinity and less serious side effects. Herein, 2-((6-Chloro-2-methoxy-acridin-9-yl)amino)-5,6,7,8-tetrahydro-4H-cyclohepta[b]-thiophene-3-carbonitrile (ACS03), a hybrid thiophene–acridine compound with antileishmanial activity, was tested for toxicity and antitumor activity. The toxicity was evaluated in vitro (on HaCat and peripheral blood mononuclear cells) and in vivo (zebrafish embryos and acute toxicity in mice). Antitumor activity was also assessed in vitro in HCT-116 (human colon carcinoma cell line), K562 (chronic myeloid leukemic cell line), HL-60 (human promyelocytic leukemia cell line), HeLa (human cervical cancer cell line), and MCF-7 (breast cancer cell line) and in vivo (Ehrlich ascites carcinoma model). ACS03 exhibited selectivity toward HCT-116 cells (Half maximal inhibitory concentration, IC50 = 23.11 ± 1.03 µM). In zebrafish embryos, ACS03 induced an increase in lactate dehydrogenase, glutathione S-transferase, and acetylcholinesterase activities. The LD50 (lethal dose 50%) value in mice was estimated to be higher than 5000 mg/kg (intraperitoneally). In vivo, ACS03 (12.5 mg/kg) induced a significant reduction in tumor volume and cell viability. In vivo antitumor activity was associated with the nitric oxide cytotoxic effect. In conclusion, significant antitumor activity and weak toxicity were recorded for this hybrid compound, characterizing it as a potential anticancer compound.

scholarly journals The enzyme subunit SubA of Shiga toxin-producing E. coli strains demonstrates comparable intracellular transport and cytotoxic activity as the holotoxin SubAB in HeLa and HCT116 cells in vitro

2021 ◽  
Vol 95 (3) ◽  
pp. 975-983
Author(s):  
Katharina Sessler ◽  
Panagiotis Papatheodorou ◽  
Fanny Wondany ◽  
Maike Krause ◽  
Sabrina Noettger ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Shiga Toxin ◽  
Intracellular Transport ◽  
Molecular Mechanisms ◽  
Cancer Cell Line ◽  
Epithelial Cell Line ◽  
Human Colon Cancer ◽  
Cell Line Hela

AbstractThe subtilase cytotoxin (SubAB) is secreted by certain Shiga toxin-producing Escherichia coli (STEC) strains and is composed of the enzymatically active subunit SubA and the pentameric binding/transport subunit SubB. We previously demonstrated that SubA (10 µg/ml), in the absence of SubB, binds and intoxicates the human cervix cancer-derived epithelial cell line HeLa. However, the cellular and molecular mechanisms underlying the cytotoxic activity of SubA in the absence of SubB remained unclear. In the present study, the cytotoxic effects mediated by SubA alone were investigated in more detail in HeLa cells and the human colon cancer cell line HCT116. We found that in the absence of SubB, SubA (10 µg/ml) is internalized into the endoplasmic reticulum (ER), where it cleaves the chaperone GRP78, an already known substrate for SubA after its canonical uptake into cells via SubB. The autonomous cellular uptake of SubA and subsequent cleavage of GRP78 in cells is prevented by treatment of cells with 10 µM brefeldin A, which inhibits the transport of protein toxins into the ER. In addition, by analyzing the SubA mutant SubAΔC344, we identified the C-terminal SEEL motif as an ER-targeting signal. Conclusively, our results strongly suggest that SubA alone shares the same intracellular transport route and cytotoxic activity as the SubAB holotoxin.

New Platinum (II) Ternary Complexes of Formamidine and Pyrophosphate: Synthesis, Characterization and DFT Calculations and In vitro Cytotoxicity

2020 ◽  
Vol 23 (7) ◽  
pp. 611-623
Author(s):  
Ahmed A. Soliman ◽  
Fawzy A. Attaby ◽  
Othman I. Alajrawy ◽  
Azza A.A. Abou-hussein ◽  
Wolfgang Linert
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Theoretical Calculations ◽  
Thermal Analyses ◽  
Cancer Cell Line ◽  
Cellular Growth ◽  
Planar Geometry ◽  
Square Planar ◽  
Vis Spectroscopy

Aim and Objective: Platinum (II) and platinum (IV) of pyrophosphate complexes have been prepared and characterized to discover their potential as antitumor drugs. This study was conducted to prepare and characterize new ternary platinum (II) complexes with formamidine and pyrophosphate as an antitumor candidate. Materials and Methods: The complexes have been characterized by mass, infrared, UV-Vis. spectroscopy, elemental analysis, magnetic susceptibility, thermal analyses, and theoretical calculations. They have been tested for their cytotoxicity, which was carried out using the fastcolorimetric assay for cellular growth and survival against MCF-7 (breast cancer cell line), HCT- 116 (colon carcinoma cell line), and HepG-2 (hepatocellular cancer cell line). Results: All complexes are diamagnetic, and the electronic spectral data displayed the bands due to square planar Pt(II) complexes. The optimized complexes structures (1-4) indicated a distorted square planar geometry where O-Pt-O and N-Pt-N bond angles were 82.04°-96.44°, respectively. Conclusion: The complexes showed noticeable cytotoxicity and are considered as promising antitumor candidates for further applications.

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine

2020 ◽  
Vol 17 (2) ◽  
pp. 151-159
Author(s):  
Tran Nguyen Minh An ◽  
Pham Thai Phuong ◽  
Nguyen Minh Quang ◽  
Nguyen Van Son ◽  
Nguyen Van Cuong ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Thiazole Derivatives ◽  
Ligand Interaction ◽  
Ic50 Value ◽  
Mcf 7

: A series of novel 1,3-thiazole derivatives (5a-i) with a modified phenothiazine moiety were synthesized and tested against cancer cell line MCF-7 for their cytotoxicity. Most of them (5a-i) were less cytotoxic or had no activity against MCF-7 cancer cell line. Material and Methods: The IC50 value of compound (4) was 33.84 μM. The compounds (5a-i) were also evaluated for antimicrobial activities, but no significant activity was observed. The antioxidant activity was conducted for target compounds (5a-i). The IC50 value of compound (5b) was 0.151mM. Results: The total amount of energy, ACE (atomic contact energy), energy of receptor (PDB: 5G5J), and ligand interaction of structure (4) were found to be 22.448 Kcal.mol-1 , -247.68, and -91.91 Kcal.mol-1, respectively. The structure (4) is well binded with the receptor because the values of binding energy, steric energy, and the number of hydrogen bondings are -91.91, 22.448 kcal.mol-1, and 2, respectively. It shows that structure (4) has good cytotoxicity with MCF-7 in vitro. Conclusion: The increasing of docking ability of structures (5a-i) with the receptor is presented in increasing order as (5f)>(5e)>(5g)>(5a)>(5b)>(5d)>(5c)>(5i)>(5h). The structure bearing substitution as thiosemicarbazone (4), nitrogen heterocyclic (5f), halogen (5e), and azide (5g) showed good cytotoxicity activity in vitro.

Design, Synthesis, Molecular Docking, and Anticancer Evaluation of Pyrazole Linked Pyrazoline Derivatives with Carbothioamide Tail as EGFR Kinase Inhibitors

2020 ◽  
Vol 21 (1) ◽  
pp. 42-60
Author(s):  
Farah Nawaz ◽  
Ozair Alam ◽  
Ahmad Perwez ◽  
Moshahid A. Rizvi ◽  
Mohd. Javed Naim ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Kinase Assay ◽  
Cervix Uteri ◽  
Egfr Kinase

Background: The Epidermal Growth Factor Receptor (known as EGFR) induces cell differentiation and proliferation upon activation through the binding of its ligands. Since EGFR is thought to be involved in the development of cancer, the identification of new target inhibitors is the most viable approach, which recently gained momentum as a potential anticancer therapy. Objective: To assess various pyrazole linked pyrazoline derivatives with carbothioamide for EGFR kinase inhibitory as well as anti-proliferative activity against human cancer cell lines viz. A549 (non-small cell lung tumor), MCF-7 (breast cancer cell line), SiHa (cancerous tissues of the cervix uteri), and HCT-116 (colon cancer cell line). Methods: In vitro EGFR kinase assay, in vitro MTT assay, Lactate dehydrogenase release, nuclear staining (DAPI), and flow cytometry cell analysis. Results: Compounds 6h and 6j inhibited EGFR kinase at concentrations of 1.66μM and 1.9μM, respectively. Furthermore, compounds 6h and 6j showed the most potent anti-proliferative results against the A549 KRAS mutation cell line (IC50 = 9.3 & 10.2μM). Through DAPI staining and phase contrast microscopy, it was established that compounds 6h and 6j also induced apoptotic activity in A549 cells. This activity was further confirmed by FACS using Annexin-V-FITC and Propidium Iodide (PI) labeling. Molecular docking studies performed on 6h and 6j suggested that the compounds can bind to the hinge region of ATP binding site of EGFR tyrosine kinase in a similar pose as that of the standard drug gefitinib. Conclusion: The potential anticancer activity of compounds 6h and 6j was confirmed and need further exploration in cancer cell lines of different tissue origin and signaling pathways, as well as in animal models of cancer development.

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