Human Breast Adenocarcinoma MCF-7 Cells Research Articles

Phytochemical profiling, cytotoxic, anti-migration, and anti-angiogenic potential of phenolic-rich fraction from Peganum harmala: in vitro and in ovo studies.

Peganum harmala has been extensively employed in Algerian traditional medicine practices. This study aimed to explore the impact of n-butanol (n-BuOH) extract sourced from Peganum harmala seeds on cell proliferation, cell migration, and angiogenesis inhibition. Cytotoxic potential of n-BuOH extract was evaluated using MTT (3-(4,5-dimethylthiazol-2-yl) 2,5 diphenyltetrazolium bromide) assay against human breast adenocarcinoma MCF-7 cells, cell migration was determined using scratch assay, and anti-angiogenic effect was evaluated through macroscopic and histological examinations conducted on chick embryo chorioallantoic membrane. Additionally, this research estimated the phytochemical profile of n-BuOH extract. Fifteen phenolic compounds were identified using Ultra-performance liquid chromatography UPLC-ESI-MS-MS analysis. In addition, the n-BuOH extract of P. harmala exhibited potent antioxidant and free radical scavenging properties. The n-BuOH extract showed potent cytotoxicity against MCF-7 cell with an IC50 value of 8.68 ± 1.58 μg/mL. Furthermore, n-BuOH extract significantly reduced migration. A strong anti-angiogenic activity was observed in the groups treated with n-BuOH extract in comparison to the negative control. Histological analysis confirmed the anti-angiogenic effect of the n-BuOH extract. This activity is probably a result of the synergistic effects produced by different polyphenolic classes.

In Vitro Antiviral and Anticancer Effects of Tanacetum sinaicum Essential Oil on Human Cervical and Breast Cancer.

Cervical cancer has been linked to human papillomavirus (HPV) types 16 and 18. Essential oils (EOs) are vital natural products of plants with various therapeutic and biological properties. The purpose of this study is to investigate and assess Tanacetum sinaicum essential oil's possible antiviral and anticancer properties, with a focus on its in vitro effects on human cervical cancer and human breast adenocarcinoma cell lines. Tanacetum sinaicum EO was extracted via hydrodistillation (HD) and characterized using gas chromatography-mass spectrometry (GC-MS). MTT assay was used to determine the cell viability of Hela (a human epithelial cervical cancer) and MCF-7 (human breast adenocarcinoma) cell lines. Quantitative real-time polymerase chain reaction (PCR) was utilized to assess the antiviral efficacy of EO against HPV-16 and 18, and anti-metastatic characteristics. The biological activity of EO was assessed using Autophage and Cell genotoxicity via the comet assay. EO is mostly composed of chrysanthenyl acetate, thujone, and verbenol. The cell viability was reduced after 24 hours of incubation at doses from 100 to 400 µg/ml. Concentrations of 800 to 3,200 µg/ml significantly inhibit cell growth. After a 24-hour incubation period, doses ranging from 100 to 400 µg/ml reduced cell viability from 62 to 72%. Concentrations of 800 to 3,200 µg/ml significantly suppress cell growth by over 95%. In MCF7 and HeLa cell lines, EO lowered virus copy numbers in a dose-dependent manner, with higher concentrations of the oil inhibiting virus replication more effectively. EO treatment increased the number of autophagosomes/autolysosomes and acidic vesicular organelles in both cell lines. On the HeLa and MCF7 cell lines, EO demonstrated antiproliferative and antimetastatic effects. The results demonstrated that EO had dose-dependent genotoxic effects on both cancer cell lines, as evidenced by DNA damage. Tanacetum sinaicum EO is a prospective source of natural bioactive compounds that can be employed in pharmaceutical and medicinal applications due to its antiviral, antiproliferative, anti-metastatic and genotoxic properties.

Sequential assembly of DNA nanoparticles inside cells enables lysosome interference and cell behavior regulation

The artificial manipulation of exogenous molecules in living cells is a promising means to regulate cellular behaviors. However, the spatiotemporal control of self-assembly within the complex intracellular environment remains grand challenge. Herein, we report a controlled sequential assembly of DNA nanoparticles in living cells, responding to acidic environment in lysosome, which enables lysosome interference and subsequently regulates a series of cellular behaviors. Two types of ultra-long DNA chains (DNA-chain-1 and 2) synthesized via rolling circle amplification were compressed by magnesium ion to two DNA nanoparticles (DNP-1 and 2), respectively. In the acidic environment of lysosomes, both DNP-1 and DNP-2 dissociated to DNA chains, and the DNA chains were subsequently assembled through base-pairing to form a hydrogel. This sequential assembly process consumed hydrogen ions within the lysosome, decreased lysosomal acidity, and thus altered the hydrolase activity and lysosomal membrane permeability. The interference of sequential assembly on lysosomes promoted cell movement in human breast adenocarcinoma MCF-7 cells, with 81.19% and 36.24% enhancement in cell migration and invasion capacity, respectively; the level of cellular autophagy was increased by 170.00%. Our study provides a new strategy for the sequential assembly of exogenous DNA materials in living cells.

Comparison of antiproliferative effects of amlodipine and nebivolol against MCF-7 cells: An in vitro study

Background: Breast cancer (BC) has become the most common cancer among women in India. Both amlodipine, belonging to calcium channel blockers, and nebivolol, belonging to the beta blockers class have proven anticancer mechanisms. However, the effect has not been compared between these drugs till now. Aim and Objectives: The present study aims to compare the antiproliferation effects of amlodipine and nebivolol against human breast adenocarcinoma MCF-7 cells. Materials and Methods: Cell viability assay was used to screen the antiproliferation effects of the study drug molecules in MCF-7 cell cultures. The IC50 values were derived graphically by plotting the cell viability against drug concentration. Results: Both amlodipine and nebivolol exhibited dose-dependent cytotoxicity against BC cells. The IC50 of amlodipine was 166.6 μg/mL and nebivolol was 114.6 μg/mL. Conclusion: In this study, nebivolol showed potent cytotoxicity compared to amlodipine. This inference may provide further insights into future drug research.

Differences in nonoxidative sulfur metabolism between normal human breast MCF-12A and adenocarcinoma MCF-7 cell lines

Recent studies have revealed the role of endogenous hydrogen sulfide (H2S) in the development of breast cancer. The capacity of cells to generate H2S and the activity and expression of the main enzymes (cystathionine beta synthase; CBS, cystathionase γ-lyase; CGL, 3-mercaptopyruvate sulfurtransferase; MPST and thiosulfate sulfurtransferase; TST) involved in H2S metabolism were analyzed using an in vitro model of a non-tumourigenic breast cell line (MCF-12A) and a human breast adenocarcinoma cell line (MCF-7). In both cell lines, MPST, CGL, and TST expression was confirmed at the mRNA (RT-PCR) and the protein (Western Blot) level, while CBS expression was detected only in MCF-7 cells. Elevated levels of GSH, sulfane sulfur and increased CBS and TST activity were presented in the MCF-7 compared to the MCF-12A cells. It appears that cysteine might be mainly a substrate for GSH synthesis in breast adenocarcinoma. Increased capacity of the cells to generate H2S was shown for MCF-12A compared to MCF-7 cell line. Results suggest an important function of CBS in H2S metabolism in breast adenocarcinoma. The presented work may contribute to further research on new therapeutic possibilities for breast cancer - one of the most frequently diagnosed types of cancer among women.

Dual-targeted delivery system using hollow silica nanoparticles with H+-triggered bubble generating characteristic coated with hyaluronic acid and AS1411 for cancer therapy

Objective Herein, a dual-targeting delivery system using mesoporous silica nanoparticles with hollow structures (HMSNs) was developed for the specific delivery of epirubicin (EPI) to cancer cells and introducing a H+-triggered bubble generating nanosystem (BGNS). HMSNs containing EPI are covered by hyaluronic acid (HA) shell and AS1411 aptamer to create the BGNS-EPI-HA-Apt complex, which is highly selective against CD44 marker and nucleolin overexpressed on the surface of tumor cells. Methods MTT assay compared the cytotoxicity of different treatments in CHO (Chinese hamster ovary) cells as well as 4T1 (murine mammary carcinoma) and MCF-7 (human breast adenocarcinoma) cells. The internalization of Epi was assessed by flow cytometry along with fluorescence imaging. In vivo studies were conducted on BALB/c mice bearing a tumor from 4T1 cell line where monitoring included measuring tumor volume, mouse weight changes over time alongside mortality rate; accumulation levels for Epi within organs were also measured during this process. Results The collected data illustrated that BGNS-EPI-HA-Apt complex controlled the release of EPI in a sustained method. Afterward, receptor-mediated internalization via nucleolin and CD44 was verified in 4T1 and MCF-7 cells using fluorescence microscopy assay and flow cytometry analysis. The results of tumor inhibitory effect study exhibited that BGNS-EPI-HA-Apt complex decreased off-target effect and improved on-target effects because of its targeting ability. Conclusion The data acquired substantiates that HA-surface modified HMSNs functionalized with aptamers possess significant potential as a focused platform for efficient transportation of anticancer agents to neoplastic tissues.

Alterations in S6K1 isoforms expression induce Epithelial to Mesenchymal Transition and Estrogen Receptor 1 Silencing in human breast adenocarcinoma MCF-7 cells

Alterations in S6K1 isoforms expression induce Epithelial to Mesenchymal Transition and Estrogen Receptor 1 Silencing in human breast adenocarcinoma MCF-7 cells

Systematic Minigene-Based Splicing Analysis and Tentative Clinical Classification of 52 CHEK2 Splice-Site Variants.

Disrupted pre-mRNA splicing is a frequent deleterious mechanism in hereditary cancer. We aimed to functionally analyze candidate spliceogenic variants of the breast cancer susceptibility gene CHEK2 by splicing reporter minigenes. A total of 128 CHEK2 splice-site variants identified in the Breast Cancer After Diagnostic Gene Sequencing (BRIDGES) project (https://cordis.europa.eu/project/id/634935) were analyzed with MaxEntScan and subsetted to 52 variants predicted to impact splicing. Three CHEK2 minigenes, which span all 15 exons, were constructed and validated. The 52 selected variants were then genetically engineered into the minigenes and assayed in MCF-7 (human breast adenocarcinoma) cells. Of 52 variants, 46 (88.5%) impaired splicing. Some of them led to complex splicing patterns with up to 11 different transcripts. Thirty-four variants induced splicing anomalies without any trace or negligible amounts of the full-length transcript. A total of 89 different transcripts were annotated, which derived from different events: single- or multi-exon skipping, alternative site-usage, mutually exclusive exon inclusion, intron retention or combinations of the abovementioned events. Fifty-nine transcripts were predicted to introduce premature termination codons, 7 kept the original open-reading frame, 5 removed the translation start codon, 6 affected the 5'UTR (Untranslated Region), and 2 included missense variations. Analysis of variant c.684-2A > G revealed the activation of a non-canonical TG-acceptor site and exon 6 sequences critical for its recognition. Incorporation of minigene read-outs into an ACMG/AMP (American College of Medical Genetics and Genomics/Association for Molecular Pathology)-based classification scheme allowed us to classify 32 CHEK2 variants (27 pathogenic/likely pathogenic and 5 likely benign). However, 20 variants (38%) remained of uncertain significance, reflecting in part the complex splicing patterns of this gene.

Deciphering the anticancer, anti-inflammatory and antioxidant potential of Ti nanoparticles fabricated using Zingiber officinale

Rapid and sustainable green technology was implemented in the current study to fabricated Ti nanoparticles. The vegetable ginger with the scientific name Zingiber officinale was employed as a biological source in the fabrication process of nanoparticles. The optical, structural, morphological, and particle size of the fabricated Ti nanoparticles were characterized with the help of UV–visible absorption spectrum, FTIR (Fourier Transform Infrared) spectrum, SEM (Scanning Electron Microscope) analysis, DLS (Dynamic Light Scattering) technique and XRD (X-ray powder diffraction) crystallography technique. The presence of spherical-shaped Ti nanoparticles with an average particle size of 93 nm was confirmed based on these characterization techniques. The anti-cancer properties of the Z. officinale mediated Ti nanoparticles were analyzed through MTT assay against cell lines MCF-7 (Human breast adenocarcinoma cell line) and concentration-dependent anti-cancer properties were observed. The anti-inflammatory capacity of the Z. officinale mediated Ti nanoparticles were examined through protein denaturation and nitric oxide scavenging assay. The antioxidant capacity of the Z. officinale mediated Ti nanoparticles were examined through DPPH assay, hydrogen peroxide radical scavenging assay, hydroxyl radical scavenging assay, and FRAP (Ferric Reducing Antioxidant Power) analysis. The fabricated Ti nanoparticles exhibited anti-inflammatory and antioxidant capacity in a concentration-dependent pattern.

Synthesis, cytotoxicity, antioxidant activity and molecular modeling of new NSAIDs-EBS derivatives

Two series of NSAIDs-EBS derivatives (5a-j and 9a-i) based on the hybridization of nonsteroidal anti-inflammatory drugs (NSAIDs) skeleton and Ebselen moiety were synthesized. Their cytotoxicity was evaluated against five types of human cancer cell lines, BGC-823 (human gastric cancer cell line), SW480 (human colon adenocarcinoma cells), MCF-7 (human breast adenocarcinoma cells), HeLa (human cervical cancer cells), A549 (human lung carcinoma cells). Moreover, the most active compound 5j showed IC50 values below 3 μM in all cancer cell lines and with remarkable anticancer activity against MCF-7 (1.5 μM) and HeLa (1.7 μM). The redox properties of the NSAIDs-EBS derivatives prepared herein were conducted by 2, 2-didiphenyl-1-picrylhydrazyl (DPPH), bleomycin dependent DNA damage and glutathione peroxidase (GPx)-like assays. Finally, TrxR1 inhibition activity assay and molecular docking study revealed NSAIDs-EBS derivatives could serve as potential TrxR1 inhibitor.

Chemical composition and in vitro cytotoxicity of Cyclotrichium niveum essential oil against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cells

The current study is aimed to investigate the essential oil yields, chemical compositions and in vitro cytotoxic activities of Cyclotrichium niveum (Boiss.) Manden et Scheng. C. niveum is an endemic species of Turkiye, generally used as a spice in local cuisine and traditional medicine. The plant material was collected from Yeşilyurt province of Malatya in August. Hydrodistillation yielded 1.41% (g/g) essential oil. The majority of the essential oil was dominated by oxygenated monoterpenes mainly pulegone (56.83%) and isomenthone (29.06%). Cytotoxicity tests of C. niveum essential oil on MCF-7 (human breast adenocarcinoma cells) and A549 (human lung adenocarcinoma alveolar basal epithelial cells) cell lines represented promising results. IC50 values on MCF-7 and A549 were found to be 31.68 μg/mL and 66.70 μg/mL respectively. In the current work, we have shown for the first time that C. niveum essential oil has cytotoxic properties in the cancer cell lines tested.

Evaluation of the Anticancer Activity of Calcium Ions Introduced into Human Breast Adenocarcinoma Cells MCF-7/WT and MCF-7/DOX by Electroporation.

Breast cancer ranks among the top three most common malignant neoplasms in Poland. The use of calcium ion-assisted electroporation is an alternative approach to the classic treatment of this disease. The studies conducted in recent years confirm the effectiveness of electroporation with calcium ions. Electroporation is a method that uses short electrical pulses to create transitional pores in the cell membrane to allow the penetration of certain drugs. The aim of this study was to investigate the antitumor effects of electroporation alone and calcium ion-assisted electroporation on human mammary adenocarcinoma cells that are sensitive (MCF-7/WT) and resistant to doxorubicin (MCF-7/DOX). The cell viability was assessed using independent tests: MTT and SRB. The type of cell death after the applied therapy was determined by TUNEL and flow cytometry (FACS) methods. The expression of Cav3.1 and Cav3.2 proteins of T-type voltage-gated calcium channels was assessed by immunocytochemistry, and changes in the morphology of CaEP-treated cells were visualized using a holotomographic microscope. The obtained results confirmed the effectiveness of the investigated therapeutic method. The results of the work constitute a good basis for planning research at the in vivo level and in the future to develop a more effective and safer method of breast cancer treatment for patients.

Label-Free Imaging of Cell Apoptosis by a Light-Addressable Electrochemical Sensor.

Label-free electrochemical visualization of cancer cell apoptosis is essential for cancer therapies. In this work, we proposed a noninvasive imaging method using a light-addressable electrochemical sensor (LAES) for label-free imaging of drug-induced tumor cell apoptosis. The dynamic AC photocurrent changes on MCF-7 human breast adenocarcinoma cells after inducing by tamoxifen were imaged. And the reasons for photocurrent changes on the cells were explored by monitoring the changes in the ζ potentials of cells and Faradic impedance. The results demonstrated that the AC photocurrent on apoptotic MCF-7 cells increased, and the apoptosis degree of each cell was heterogeneous. Moreover, the AC photocurrent increase was attributed to the increased cell membrane permeability and the increased gap between the cell basal surface and the substrate caused by cell apoptosis. This study provides a brand new approach for label-free visualizing cell apoptosis heterogeneity, which has great potential in apoptosis-associated drug screening or drug efficacy evaluation.

Antioxidant activity and Cytotoxic evaluation of Phytofabricated Silver Nanoparticles of Fig (Ficus mollis Vahl)

The present study aimed to evaluate Antioxidant and Cytotoxic activity of phytofabricated silver nanoparticles (FmF-AgNPs) derived from Figs of Ficus mollis. This green synthesized FmF-AgNPs were tested for antioxidant activity with DPPH assay and cytotoxicity activity against MCF-7 (Human breast adenocarcinoma cell lines) with MTT assay at various concentrations. The data obtained demonstrated that FmF-AgNPs posses both antioxidant activity and cytotoxicity activity which is dosage-dependent. In conclusion, results obtained revealed the potent therapeutic value of phytofabricated silver nanoparticles (FmF-AgNPs) can act as potent antioxidant and anticancer agent.

High Efficacy on the Death of Breast Cancer Cells Using SPMHT with Magnetite Cyclodextrins Nanobioconjugates.

In this study, we present the experimental results obtained in vitro on the human breast adenocarcinoma cell line (MCF-7) by applying superparamagnetic hyperthermia (SPMHT) using novel Fe3O4-PAA-(HP-γ-CDs) (PAA is polyacrylic acid and HP-γ-CDs is hydroxypropyl gamma-cyclodextrins) nanobioconjugates previously obtained by us. In the in vitro SPMHT experiments, we used concentrations of 1, 5 and 10 mg/mL of Fe3O4 ferrimagnetic nanoparticles from Fe3O4-PAA-(HP-γ-CDs) nanobioconjugates suspended in culture media containing 1 × 105 MCF-7 human breast adenocarcinoma cells. The harmonic alternating magnetic field used in the in vitro experiments that did not affect cell viability was found to be optimal in the range of 160-378 Gs and at a frequency of 312.2 kHz. The appropriate duration of the therapy was 30 min. After applying SPMHT with these nanobioconjugates under the above conditions, MCF-7 cancer cells died out in a very high percentage, of until 95.11%. Moreover, we studied the field up to which magnetic hyperthermia can be safely applied without cellular toxicity, and found a new upper biological limit H × f ~9.5 × 109 A/m⋅Hz (H is the amplitude and f is the frequency of the alternating magnetic field) to safely apply the magnetic field in vitro in the case of MCF-7 cells; the value was twice as high compared to the currently known value. This is a major advantage for magnetic hyperthermia in vitro and in vivo, because it allows one to achieve a therapy temperature of 43 °C safely in a much shorter time without affecting healthy cells. At the same time, using the new biological limit for a magnetic field, the concentration of magnetic nanoparticles in magnetic hyperthermia can be greatly reduced, obtaining the same hyperthermic effect, while at the same time, reducing cellular toxicity. This new limit of the magnetic field was tested by us in vitro with very good results, without the cell viability decreasing below ~90%.

Correlative Fluorescent Scanning Probe Nanotomography Used to Study the Intracellular Distribution of Doxorubicin in MCF-7 Human Breast Adenocarcinoma Cells

Developing technologies for efficient targeted drug delivery for oncotherapy requires new methods to analyze the features of micro- and nanoscale distributions of antitumor drugs in cells and tissues. A new approach to three-dimensional analysis of the intracellular distribution of cytostatics was developed using fluorescence scanning optical-probe nanotomography. A correlative analysis of the nanostructure and distribution of injected doxorubicin in MCF-7 human breast adenocarcinoma cells revealed the features of drug penetration and accumulation in the cell. The technology is based on the principles of scanning optical probe nanotomography and is applicable to studying the distribution patterns of various fluorescent or fluorescence-labelled substances in cells and tissues.

Reduction-sensitive flower-like magnetomicelles based on PCL-ss-PEG-ss-PCL triblock copolymer as anti-cancer drug delivery system

Introducing an intelligent pharmaceutical nanocarrier for targeted drug release and reducing the side effects of chemotherapy is the main goal of many researchers. In this area, we synthesized amphiphilic triblock copolymer PCL-ss-PEG-ss-PCL consisting of cystamine as a reduction sensitive linkage. The aqueous self-assembly of triblock copolymer in the presence of magnetic iron oxide nanoparticles (Fe3O4) and doxorubicin (DOX) led to the formation of reduction-sensitive flower like magnetomicelle containing DOX and Fe3O4. The innovative design based on intelligent flower like structure led to high drug loading content, reduce drug release in physiologic condition, fast degradation at targeted site and burst release of more content of drug at earlier time. The DOX loading content was about 19% and DOX- loaded magnetomicelles (D-LMM) showed more triggered release under redox conditions at pH = 5. The efficiency of D-LMM was compared with non-reduction sensitive control group (CD-LMM), free DOX and commercial product of liposomal DOX (LD) in vitro. The D-LMM showed significant improvement in cellular uptake and toxicity behavior on human breast adenocarcinoma MCF-7 cells in comparison to commercial LD and also displayed better results in the cytotoxicity and apoptosis/necrosis assays in comparison to CD-LMM.

INVESTIGATION OF THE INTRACELLULAR DISTRIBUTION OF DOXORUBICIN IN MCF-7 HUMAN BREAST ADENOCARCINOMA CELLS BY THE METHOD OF CORRELATIVE SCANNING FLUORESCENT PROBE NANOTOMOGRAPHY

The development of technologies for effective targeted drug delivery for oncotherapy requires the elaboration of new methods to analyze the features of micro- and nanoscale distributions of antitumor drugs in cells and tissues. This paper presents a new approach to three-dimensional analysis of intracellular distribution of cytostatics using fluorescence scanning optical-probe nanotomography technology. Correlative analysis of nanostructure and distribution of injected doxorubicin in studied MCF-7 human breast adenocarcinoma cells made it possible to reveal the features of drug penetration and accumulation in cells. The developed technology based on the principles of scanning optical probe nanotomography is applicable to study the distribution patterns of various fluorescent or fluorescence-labelled substances in cells and tissues.

New Apoptosis Inducers Containing Anti-inflammatory Drugs and Pnictogen Derivatives: A New Strategy in the Development of Mitochondrial Targeting Chemotherapeutics.

{[Ag8(Mef)8(μ2-S,O-DMSO)2(μ2-O-DMSO)2(O-DMSO)8]·2(H2O)} (1), [Ag(Mef)(tpP)2] (2), [Ag(Mef)(tpAs)3] (3), and {2 [Ag(Mef)(tpSb)3] (DMSO)} (4) were obtained by the conjugation of mefenamic acid (MefH), a nonsteroidal anti-inflammatory drug (NSAID), with a mitochondriotropic derivative of pnictogen tpE (tp = triphenyl group; E = P, As, and Sb) through silver(I). Their hydrophilicity was adjusted by their dispersion into sodium lauryl sulfate (SLS), forming SLS@1-4. 1-4 and SLS@1-4 were characterized by their spectral data and X-ray crystallography. They inhibit the proliferation of human breast adenocarcinoma cells MCF-7 (hormone-dependent (HD)) and MDA-MB-231 (hormone-independent (HI)). X-ray fluorescence reveals the Ag cellular uptake. The in vitro and in vivo nongenotoxicity was confirmed with micronucleus (MN), Artemia salina, and Allium cepa assays. Their mechanism of action was studied by cell morphology, DNA fragmentation, acridine orange/ethidium bromide (AO/EB) staining, cell cycle arrest, mitochondrial membrane permeabilization tests, DNA binding affinity, and LOX inhibitory activity and was rationalized by regression analysis.

Synthesis, structural and spectral characteristics of novel n,π-chelate complexes of Pd(II) and Pt(II) with N-allylthioureas and their influence on the growth of spheroids cells MCF-7 and GGT activity

Four mononuclear n,π-chelate complexes [M(HL1,2)Cl2] (M = Pd2+, Pt2+) have been obtained by the reactions of PdCl2 or K2[PtCl4] with N,N-diethyl-N'-(2-propenyl)thiourea (HL1) or N-cyclohexyl-N'-(2-propenyl)thiourea (HL2) in the presence of HCl. According to X-ray diffraction study, the molecules of HL1,2 are coordinated in a bidentate manner with the formation of six-membered chelate metallocycles in a twist-boat conformation. The diagonal arrangement of “soft-hard” donor atoms (S–M−Cl, C–M−Cl) in the coordination sphere leads to the Pearson's effect of “molecular antisymbiosis in the trans effect” that causes the formation of complexes with an M:L ratio of 1:1. However, interaction in the ratio 1:2, 1:3 is also possible in the solution under the conditions of monodentate coordination of HL1 and HL2. All compounds were investigated by IR, UV–vis and NMR spectra. The 1H/13C NMR study showed that this method is reliable for establishing the formation of a π-coordinating bond. The similarity of the synthesized complexes structure with cisplatin implies the same mechanism of their antitumor action. Thus, it was investigated their effect on the growth and biochemical characteristics of human breast adenocarcinoma cells MCF-7 (grown in three-dimensional culture as spheroids) and the activity of the enzyme gamma-glutamyl transpeptidase (GGT). The results showed that all studied π-complexes are more active compared to cisplatin, and they exhibit pronounced anti-metastatic and pro-apoptotic activity, which one is caused by their inhibitory effect.