scholarly journals The Cytotoxic Activity of Diiron Bis-Cyclopentadienyl Complexes with Bridging C3-Ligands

2021 ◽  
Vol 11 (10) ◽  
pp. 4351
Author(s):  
Simona Braccini ◽  
Giacomo Provinciali ◽  
Lorenzo Biancalana ◽  
Guido Pampaloni ◽  
Federica Chiellini ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Ovarian Cancer Cell Line ◽  
Iron Oxidation ◽  
Aqueous Media ◽  
Cancer Cell Line ◽  
Resistant Cell ◽  
In Vitro Cytotoxicity ◽  
Resistant Cell Line

Diiron bis-cyclopentadienyl bis-carbonyl cationic complexes with a bridging vinyliminium ligand, [Fe2Cp2(CO)(μ-CO){μ-η1:η3-C3(R′)C2HC1NMe(R″)}]CF3SO3 (R = Xyl = 2,6-C6H3Me2, R′ = Ph, R″ = H, 2a; R = Xyl, R′ = R″ = Me, 2b; R = R′ = Me, R″ = H, 2c; R = Me, R′ = 2-naphthyl, R″ = H, 2d; R = Me, R′ = R″ = Ph, 2e), are easily available from commercial chemicals, robust in aqueous media and exert a variable in vitro cytotoxicity against cancer cell lines depending on the nature of the substituents on the vinyliminium ligand. The anticancer activity is, at least in part, associated to fragmentation reactions, leading to iron oxidation and active neutral and well-defined monoiron species. We report an innovative synthetic procedure for the preparation of 2a,c,d, and a facile method to access the monoiron derivative of 2a, i.e., [FeCp(CO){C1(NMeXyl)C2HC3(Ph)C(O)}] (3a). According to IC50 analyses at different times of incubation of the complexes, 3a is significantly faster in inhibiting cell viability compared to its diiron precursor 2a. The neutral complexes [Fe2Cp2(CO)(μ-CO){μ-k1N:k1C:k1C-C3(R′)C2(Se)C1(NMe2)C4(CO2Y)C5(CO2Y)}] (R′ = Y = Me, 4a; R′ = Pr, Y = tBu, 4b; R′ = Y = Et, 4c) are obtained via the two-step modification of the vinyliminium moiety and comprise a bridging selenophene-decorated alkylidene ligand. The antiproliferative activity exhibited by 4a-c is moderate but comparable on the ovarian cancer cell line A2780 and the corresponding cisplatin resistant cell line, A2780cisR. Complexes 4a-c in aqueous solutions undergo progressive release of the alkylidene ligand as a functionalized selenophene, this process being slower in cell culture medium. Since the released selenophenes SeC1{C(O)R′}C2(NMe2)C3(CO2Y)C4(CO2Y) (R′ = Y = Me, 5a; R′ = Pr, Y = tBu, 5b) are substantially not cytotoxic, it is presumable that the activity of 4a-c is largely ascribable to the {Fe2Cp2(CO)2} scaffold.

scholarly journals Synthesis, Spectral Characterization, and In Vitro Cytotoxicity of Some Fe(III) Complexes Bearing Unsymmetrical Salen-Type Ligands Derived from 2-Hydroxynaphthaldehyde and Substituted Salicylaldehydes

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Quang Trung Nguyen ◽  
Phuong Nam Pham Thi ◽  
Nguyen Van Tuyen
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Tumor Cell Line ◽  
In Vitro Cytotoxicity ◽  
Ionization Mass ◽  
Hek 293 ◽  
Human Cancer Cell Lines

Six Fe(III) complexes bearing unsymmetrical salen-type ligands derived from 2-hydroxynaphthaldehyde and substituted salicylaldehydes were synthesized by coordinating the unsymmetrical salen-type ligands with FeCl3.6H2O. The synthetic complexes were characterized by electrospray ionization mass spectra (ESI-MS), effective magnetic moments (μeff), and infrared (IR) and ultraviolet-visible (UV-Vis) spectra. The spectroscopic data are in good agreement with the suggested molecular formulae of the complexes. Their cyclic voltammetric studies in acetonitrile solutions showed that the Fe(III)/Fe(II) reduction processes are electrochemically irreversible. The in vitro cytotoxicity of the obtained complexes was screened on human cancer cell lines KB (a subline of Hela tumor cell line) and HepG2 (a human liver cancer cell line) and a normal human cell line HEK-293 (Human Embryonic Kidney cell line). The results showed that the synthetic Fe(III) complexes are highly cytotoxic and quite selective. The synthetic complexes bearing unsymmetrical salen-type ligands with different substituted groups in the salicyl ring indicate different cytotoxicity.

scholarly journals Cytotoxicity of Standardized Curcuminoids Mixture against Epithelial Ovarian Cancer Cell Line SKOV-3

2020 ◽  
Vol 88 (1) ◽  
pp. 11 ◽  
Author(s):  
Heba Almosa ◽  
Mihal Alqriqri ◽  
Iuliana Denetiu ◽  
Mohammed A. Baghdadi ◽  
Mohammed Alkhaled ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Ovarian Cancer Cell ◽  
Ovarian Cancer Cell Line ◽  
Cancer Cell Line ◽  
Reversed Phase ◽  
Potential Contribution ◽  
Dependent Manner

Herbal medicine has been in use for centuries for a wide variety of ailments; however, the efficacy of its therapeutic agents in modern medicine is currently being studied. Curcuminoids are an example of natural agents, widely used due to their potential contribution in the prevention and treatment of cancer. In this study, the three main compounds of curcuminoids—curcumin, desmethoxycurcumin, and bisdesmethoxycurcumin—were determined by reversed-phase high performance liquid chromatography (HPLC) to quantify total content in a mixture. Subsequently, the effect of the three curcuminoids, employed as one sample, was evaluated, to study the proliferation, apoptosis, cell cycle, and migration of the human ovarian cancer cell line SKOV-3. The results reveal that curcuminoids inhibit the proliferation of SKOV-3 cells with concentration- and time-dependent mechanisms. The morphological analysis of the treated SKOV-3 cells showed a typical apoptotic phenotype—cell shrinkage and membrane blebbing in a dose-dependent manner. In addition, flow cytometry demonstrated an increase in apoptosis with an IC50 of 30 µM curcuminoids. The migration of SKOV-3 cells was also inhibited, reflected by a decrease in wound area. Furthermore, the curcuminoids were found to have no stimulation effect on the expression of cytokines TNF-α and IL-10. These results suggest that a curcuminoid mixture can effectively suppress epithelial cancer cell growth in vitro by inducing cellular changes and apoptosis.

scholarly journals IN VITRO CYTOTOXIC ACTIVITY OF SECOISOLARICIRESINOL DIGLUCOSIDE ON HT-29, PA-1 CELL LINES, AND α-AMYLASE INHIBITORY ACTIVITY

2019 ◽  
pp. 168-173
Author(s):  
GUNABHUSHANA DADDALA ◽  
SWAROOPARANI A
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Ovarian Cancer Cell Line ◽  
Cancer Cell Line ◽  
Secoisolariciresinol Diglucoside ◽  
Human Colon Cancer ◽  
Ht 29

Objective: The present study was conducted to evaluate the in vitro cytotoxic activity and α- amylase inhibitory activity of secoisolariciresinol diglucoside (SDG). Methods: The cytotoxic activity was conducted on HT-29 (human colon cancer cell line) and PA-1 (human ovarian cancer cell line) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay and the α- amylase inhibitory activity using acarbose as a standard. Both the tests were evaluated at different concentrations, 3.125–100 μg/ml and 50–2000 μg correspondingly and the concentration required for a 50% inhibition of viability (IC50) was determined graphically. The effect of the samples on the proliferation of HT-29 and PA-1 was expressed as the percentage cell viability. Results: SDG exhibited a considerable dose- and time-dependent inhibition on both HT-29 and PA-1 and also observed a concentration-dependent α-amylase inhibitory activity that leads in reduction of starch hydrolysis and hence eventually to lowered glucose levels. Conclusion: The present in vitro study concluded that SDG can be a potent anticancer and moderate hyperglycemic component.

scholarly journals Dispirooxindoles Based on 2-Selenoxo-Imidazolidin-4-Ones: Synthesis, Cytotoxicity and ROS Generation Ability

2021 ◽  
Vol 22 (5) ◽  
pp. 2613
Author(s):  
Vladimir K. Novotortsev ◽  
Maxim E. Kukushkin ◽  
Viktor A. Tafeenko ◽  
Dmitry A. Skvortsov ◽  
Marina A. Kalinina ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Selectivity Index ◽  
Azomethine Ylides ◽  
Ros Generation ◽  
Cytotoxic Action ◽  
Diphenyl Tetrazolium Bromide

A regio- and diastereoselective synthesis of two types of dispiro derivatives of 2-selenoxoimidazolidin-4-ones, differing in the position of the nitrogen atom in the central pyrrolidine ring of the spiro-fused system—namely, 2-selenoxodispiro[imidazolidine-4,3′-pyrrolidine-2′,3″-indoline]-2″,5-diones (5a-h) and 2-senenoxodispiro[imidazolidine-4,3′-pyrrolidine-4′,3″-indoline]-2″,5-diones (6a-m)—were developed based on a 1,3-dipolar cycloaddition of azomethine ylides generated from isatin and sarcosine or formaldehyde and sarcosine to 5-arylidene or 5-indolidene-2-selenoxo-tetrahydro-4H-imidazole-4-ones. Selenium-containing dispiro indolinones generally exhibit cytotoxic activity near to the activity of the corresponding oxygen and sulfur-containing derivatives. Compounds 5b, 5c, and 5e demonstrated considerable in vitro cytotoxicity in the 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide (MTT) test (concentration of compounds that caused 50% death of cells (CC50) 7.6–8.7 μM) against the A549 cancer cell line with the VA13/A549 selectivity index 5.2–6.9 and compound 6e—against the MCF7 cancer cell line (CC50 20.6 μM, HEK293T/A549 selectivity index 1.6); some compounds (5 and 6) increased the level of intracellular reactive oxygen species (ROS) in the experiment on A549 and PC3 cells using platinized carbon nanoelectrode. The tests for p53 activation for compounds 5 and 6 on the transcriptional reporter suggest that the investigated compounds can only have an indirect p53-dependent mechanism of action. For the compounds 5b, 6b, and 6l, the ROS generation may be one of the significant mechanisms of their cytotoxic action.

In Vitro: Cytotoxicity, Apoptosis and Ameliorative Potential of Lawsonia inermis Extract in Human Lung, Colon and Liver Cancer Cell Line

2020 ◽  
Vol 38 (8-9) ◽  
pp. 476-485
Author(s):  
Sharmeen Ishteyaque ◽  
Anjali Mishra ◽  
Sangeeta Mohapatra ◽  
Aparna Singh ◽  
Rabi S. Bhatta ◽  
...  
Keyword(s):  
Liver Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Human Lung ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Liver Cancer Cell ◽  
Lawsonia Inermis ◽  
Liver Cancer Cell Line
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