Human Cervical Cancer HeLa Cells Research Articles

Evaluation of Cell Cycle-Dependent Migration Activity after X-ray Exposure: A Radiobiological Approach for Optimization of Radiotherapy with Cell Cycle-Targeting Agents.

Radiotherapy with cell cycle-specific anticancer agents has become an important option in the control of both primary tumors and metastases. Here, we used image analysis algorithms that enable quick segmentation and tracking to describe a radiobiological approach for the optimized selection of cell cycle-targeting anticancer drugs for radiotherapy. We confirmed cell cycle-synchronization using human cervical cancer HeLa cells expressing a fluorescent ubiquitination-based cell cycle indicator (FUCCI) as a cell cycle-monitoring probe. Cells synchronized in the G1 and G2 phases were irradiated with X rays at 0.5-2 Gy. Each cell was identified using Cellpose, a deep learning-based algorithm for cellular segmentation, and the velocity and direction of migration were analyzed using the TrackMate plugin in Fiji ImageJ. G1 phase synchronized cells showed a dose-dependent decrease in velocity after irradiation, while G2 cells tended to increase their velocity. The migration pattern of all cells appeared to be a random walk model, regardless of the exposure dose. In addition, we used cisplatin to arrest the cell cycle. HeLa-FUCCI cells arrested at the G2 phase via cisplatin treatment showed enhanced cell migration after X-ray exposure. These results indicated that anticancer agents that arrest the cell cycle of cancer cells in a specific phase may enhance cell migration after radiotherapy. Our approach, using cellular segmentation and tracking algorithms, could enhance the radiobiological assessment of cell cycle-specific migration after irradiation to aid in optimizing radiotherapy using cell cycle-targeting agents.

Antheraea proylei J. Sericin Induces Apoptosis in a Caspase-Dependent Manner in A549 and HeLa Cells.

To investigate the anticancer activity of sericin preparation from cocoons of A. proylei. In spite of much progress in cancer, the global cancer burden is still significant and increasing. Sericin, an adhesive protein of silk cocoons, has been shown to be a potential protein in various biomedical applications, including cancer therapeutics. The present study evaluates the anticancer property of sericin from cocoons of Antheraea proylei J (SAP) against human lung cancer (A549) and cervical cancer (HeLa) cell lines. This is the first report of anti-cancer activity of the non-mulberry silkworm A. proylei J. Establish the antiproliferative potential of SAP. 2. Identify the molecular mechanism of cell death induced by SAP on two different cell lines. SAP was prepared from cocoons of A. proylei J. by the process of the degumming method. Cytotoxicity activity was assessed by MTT assay, and genotoxicity activity was assessed by comet assay. Cleavage of caspase and PARP proteins and phosphorylation of MAPK pathway members were analysed by Western blotting. Cell cycle analysis was done by flow cytometer. SAP causes cytotoxicity to A549 and HeLa cell lines with the IC50 values 3.8 and 3.9 µg/µl respectively. SAP induces apoptosis in a dose-dependent manner through caspase-3 and p38, MAPK pathways in A549 and HeLa cells. Moreover, in A549 and HeLa cells, SAP induces cell cycle arrest at the S phase in a dose-dependent manner. The difference in the molecular mechanisms of apoptosis induced by SAP in A549 and HeLa cell lines may be due to the difference in the genotypes of the cancer cell lines. However, further investigation is warranted. The overall results of the present study envisage the possibility of using SAP as an anti-tumorigenic agent.

Hypoxia-activated prodrug combining site-specific chemotherapy and light-driven photothermal therapy

The development of a highly effective and low toxic drug is very beneficial for precise cancer therapy. Herein, taking advantage of the hypoxic nature of tumors, we carefully designed and synthesized the first hypoxia-activated single-molecule prodrug BDP-CPT-NO2 for fluorescence imaging-guided chemo-photothermal dual-mode therapy. The prodrug contains the chemotherapeutic drug camptothecin (CPT) and a boron dipyrromethene (BDP)-based photothermal agent, which are connected through a nitroreductase (NTR)-responsive linker (a nitro unit), and shows no fluorescence and extremely low cytotoxicity under normoxia. However, the nitro in the prodrug could be reduced to amino by exogenous NTR with nicotinamide adenine dinucleotide (NADH) in PBS buffer solution and endogenous NTR in hypoxic cancer cells, which is followed by a self-immolative reaction that leads to the release of CPT and BDP-COOH. This process is accompanied by significantly enhanced BDP and CPT fluorescence, which are due to NTR-induced ester-to-carboxylate conversion and fluorescence resonance energy transfer (FRET) interruption, respectively. Concomitantly, BDP-CPT-NO2 displays powerful combined chemo-PTT therapeutic efficacy, as evidenced in human cervical cancer HeLa and human liver cancer HepG2 cells, as well as in mice bearing H22 tumors. This study provides a promising strategy for effective and selective cancer treatment by hypoxia-activated prodrugs caged within organic photothermal agents.

Retraction: Celastrol inhibit the proliferation, invasion and migration of human cervical HeLa cancer cells through down-regulation of MMP-2 and MMP-9.

Zhang J, Wang R, Cheng L, Xu H. Celastrol inhibit the proliferation, invasion and migration of human cervical HeLa cancer cells through down-regulation of MMP-2 and MMP-9. J Cell Mol Med. 2021;25:5335-5338. doi: 10.1111/jcmm.16488 The above article, published online on 4 May 2021 in Wiley Online Library (wileyonlinelibrary.com), has been retracted by agreement between the journal Editor-in-Chief, Stefan N. Constantinescu, and the Foundation for Cellular and Molecular Medicine/John Wiley & Sons Ltd. Following publication, concerns were raised by third parties that portions of Figure1 are identical to Figure1 presented in another article (1) from a different author group and covering a different research topic. Further investigation confirmed these concerns and revealed additional duplication in Figures1 and 2, overlapping with Figures1 and 3 in (1). The authors of both articles were approached for an explanation but the authors of this article did not respond. The authors of (1) were unable to provide any underlying data. The retraction has been agreed because of concerns regarding the integrity of the research presented given that the figures were duplicated. (1) Shi X, Luo X, Chen T, etal. Naringenin inhibits migration, invasion, induces apoptosis in human lung cancer cells and arrests tumour progression invitro. J Cell Mol Med. 2021;25:2563-2571. doi: 10.1111/jcmm.16226.

Retraction: Naringenin inhibits migration, invasion, induces apoptosis in human lung cancer cells and arrests tumour progression invitro.

Shi X, Luo X, Chen T, Guo W, Liang C, Tang S, Mo J. Naringenin inhibits migration, invasion, induces apoptosis in human lung cancer cells and arrests tumour progression invitro. J Cell Mol Med. 2021; 25: 2563-2571. https://doi.org/10.1111/jcmm.16226 The above article, published online on 1 February 2021 in Wiley Online Library (wileyonlinelibrary.com), has been retracted by agreement between the journal Editor-in-Chief, Stefan N. Constantinescu, and the Foundation for Cellular and Molecular Medicine/John Wiley & Sons Ltd. Following publication, concerns were raised by third parties that portions of Figure1 are identical to Figure1 in another article (1) from a different author group and covering a different research topic. Further investigation confirmed these concerns and revealed additional duplication in Figures1 and 3, overlapping with Figures1 and 2 in (1). The authors of both articles were approached for an explanation but were unable to address the concerns raised. The authors of (1) did not respond, and the authors of this article were unable to provide any underlying data. The retraction has been agreed because of concerns regarding the integrity of the research presented given that the figures were duplicated. (1) Zhang J, Wang R, Cheng L, Xu H. Celastrol inhibit the proliferation, invasion and migration of human cervical HeLa cancer cells through down-regulation of MMP-2 and MMP-9. J Cell Mol Med. 2021; 25: 5335-5338. https://doi.org/10.1111/jcmm.16488.

Parkin Enhances Gefitinib-induced Anoikis in HeLa Cervical Cancer Cells.

Gefitinib exhibits anticancer activity against cervical cancer cells via anoikis, a type of apoptosis induced by cell detachment from the extracellular matrix. Previous studies have reported that Parkin expression affects the efficacy of anticancer drugs. However, the impact of Parkin expression on the therapeutic effects of gefitinib in human cervical cancer remains unclear. Thus, this study aimed to evaluate whether Parkin over-expression improves the therapeutic effects of gefitinib against HeLa cervical cancer cells. Cell viability and apoptotic death of HeLa cells were measured by trypan blue dye exclusion assay and flow cytometry. Cell detachment, adhesion, spreading, and cell-cell interaction were observed by inverted microscopy. Alteration of adhesion-related molecules was evaluated by confocal microscopy and western blot assay. Parkin expression potentiated gefitinib-induced cell detachment by affecting the organization of the actin cytoskeleton. In addition, Parkin expression induced a further reduction in the reattachment of and interaction between detached cells. The therapeutic efficacy of low-dose gefitinib combined with Parkin expression was equivalent to that of high-dose gefitinib alone. Parkin expression promotes gefitinib-induced anoikis, consequently increasing the efficacy of gefitinib against HeLa human cervical cancer cells. Based on our results, we propose that Parkin can be used to increase the anti-cancer effect of gefitinib on cervical cancer cells.

Evaluation of the Antiproliferative Potential of Yellow Jaboticaba (Myrciaria glazioviana) Extracts Against Human Cervical Cancer (HeLa cells line) and the Analysis of Their Chemical Composition by HPLC-HRESIMS.

Cervical cancer is a specific type of cancer that affects women around the world, with an incidence of 604 thousand new cases per year and 341 thousand deaths. There is a high demand for new effective antineoplastic drugs with few side effects. In this sense, recent research highlights the potential of compounds of natural origin in treating and preventing different types of cancer. Myrciaria glazioviana is a Brazilian native species belonging to the Myrtaceae family, which has previously described biological activities such as antimicrobial, anti-inflammatory, and antioxidant properties. This study aims to evaluate the anticancer activity of the dichloromethane extract (MGD) and ethyl acetate extract (MGA) of M. glazioviana leaves against human cervical cancer cell line (HeLa), as well as to identify their bioactive compounds. Using HPLC-HRESIMS technique, ten compounds were characterized in both samples: quinic acid, ellagic acid, Tri-O-methyl ellagic acid, two derivatives of Tetra-O-methyl flavellagic acid, quercetrin, Di-O-methyl ellagic acid, and three derivatives of pentamethyl coruleoellagic acid. Through MTT assays using HeLa cells and NIH/3T3 cells, it was observed that MGD and MGA were selective against tumor cells, with IC50 values of 24.31 and 12.62 μg/mL, respectively. The samples induced the tumor cell death by apoptosis, as evidenced by the activation of caspases 3/7, cell shrinkage, and pyknotic nuclei. Both samples were also able to inhibit the migration of HeLa cells after 24 hours of treatment, indicating a potential antimetastatic effect. Therefore, the present research highlights the antiproliferative and antimigratory potential of this species against HeLa cells.

Redox-Responsive Gold Nanoparticles Coated with Hyaluronic Acid and Folic Acid for Application in Targeting Anticancer Therapy.

Methotrexate (MTX) has poor water solubility and low bioavailability, and cancer cells can become resistant to it, which limits its safe delivery to tumor sites and reduces its clinical efficacy. Herein, we developed novel redox-responsive hybrid nanoparticles (NPs) from hyaluronic acid (HA) and 3-mercaptopropionic acid (MPA)-coated gold NPs (gold@MPA NPs), which were further conjugated with folic acid (FA). The design of FA-HA-ss-gold NPs aimed at enhancing cellular uptake specifically in cancer cells using an active FA/HA dual targeting strategy for enhanced tumor eradication. MTX was successfully encapsulated into FA-HA-ss-gold NPs, with drug encapsulation efficiency (EE) as high as >98.7%. The physicochemical properties of the NPs were investigated in terms of size, surface charges, wavelength reflectance, and chemical bonds. MTX was released in a sustained manner in glutathione (GSH). The cellular uptake experiments showed effective uptake of FA-HA-ss-gold over HA-ss-gold NPs in the deep tumor. Moreover, the release studies provided strong evidence that FA-HA-ss-gold NPs serve as GSH-responsive carriers. In vitro, anti-tumor activity tests showed that FA-HA-ss-gold/MTX NPs exhibited significantly higher cytotoxic activity against both human cervical cancer (HeLa) cells and breast cancer (BT-20) cells compared to gold only and HA-ss-gold/MTX NPs while being safe for human embryonic kidney (HEK-293) cells. Therefore, this present study suggests that FA-HA-ss-gold NPs are promising active targeting hybrid nanocarriers that are stable, controllable, biocompatible, biodegradable, and with enhanced cancer cell targetability for the safe delivery of hydrophobic anticancer drugs.

Commercial Wheat and Oat Flour Derived Fluorescent Carbon Quantum Dots through Sustainable Hydrothermal Synthesis and Their Biological Activities

AbstractIn this study, we utilized processed edible commercial wheat and oat flours to synthesize highly fluorescent carbon dots using green hydrothermal synthesis. The as‐synthesized carbon quantum dots (CQDs) were characterized using UV‐vis spectrophotometry, photoluminescence spectrophotometry, high‐resolution transmission electron microscopy, and Fourier transform infrared spectroscopy. The synthesized wheat‐CQDs (W‐CQDs) and oat‐CQDs (O‐CQDs) had monodispersed spherical shapes with average sizes of 3–8 and 5–10 nm, respectively, and exhibited strong fluorescence intensity and excitation‐dependent photoluminescence. The W‐CQDs and O‐CQDs were highly dispersed in aqueous solutions and exhibited bright green and blue fluorescence, respectively, under UV light (λex=380 and 370 nm). Both CQDs contained abundant functional groups, including amino, hydroxyl, and carboxyl groups, which may play a major role in biological applications. The W‐CQDs and O‐CQDs showed good free‐radical scavenging capacity in the 2,2‐diphenylpicrylhydrazyl (DPPH) and H2O2 assays. The anti‐inflammatory activities of W‐CQDs and O‐CQDs were more effective than that of the standard, with EC50 values of 1.8 and 1.3 mg/mL, respectively, in the protein denaturation assay. Additionally, the CQDs exhibited low cytotoxicity toward NIH3T3 fibroblast and human HeLa cervical cancer cells when treated with a 5‐mg/mL concentration. Therefore, green‐synthesized W‐CQDs and O‐CQDs are easily available, less cytotoxic, and applicable to therapeutic and cell nanocarrier purposes.

Dictyostelium Differentiation-Inducing Factor 1 Promotes Glucose Uptake via Direct Inhibition of Mitochondrial Malate Dehydrogenase in Mouse 3T3-L1 Cells.

Differentiation-inducing factor 1 (DIF-1), found in Dictyostelium discoideum, has antiproliferative and glucose-uptake-promoting activities in mammalian cells. DIF-1 is a potential lead for the development of antitumor and/or antiobesity/antidiabetes drugs, but the mechanisms underlying its actions have not been fully elucidated. In this study, we searched for target molecules of DIF-1 that mediate the actions of DIF-1 in mammalian cells by identifying DIF-1-binding proteins in human cervical cancer HeLa cells and mouse 3T3-L1 fibroblast cells using affinity chromatography and liquid chromatography-tandem mass spectrometry and found mitochondrial malate dehydrogenase (MDH2) to be a DIF-1-binding protein in both cell lines. Since DIF-1 has been shown to directly inhibit MDH2 activity, we compared the effects of DIF-1 and the MDH2 inhibitor LW6 on the growth of HeLa and 3T3-L1 cells and on glucose uptake in confluent 3T3-L1 cells in vitro. In both HeLa and 3T3-L1 cells, DIF-1 at 10-40 μM dose-dependently suppressed growth, whereas LW6 at 20 μM, but not at 2-10 μM, significantly suppressed growth in these cells. In confluent 3T3-L1 cells, DIF-1 at 10-40 μM significantly promoted glucose uptake, with the strongest effect at 20 μM DIF-1, whereas LW6 at 2-20 μM significantly promoted glucose uptake, with the strongest effect at 10 μM LW6. Western blot analyses showed that LW6 (10 μM) and DIF-1 (20 μM) phosphorylated and, thus, activated AMP kinase in 3T3-L1 cells. Our results suggest that MDH2 inhibition can suppress cell growth and promote glucose uptake in the cells, but appears to promote glucose uptake more strongly than it suppresses cell growth. Thus, DIF-1 may promote glucose uptake, at least in part, via direct inhibition of MDH2 and a subsequent activation of AMP kinase in 3T3-L1 cells.

Antioxidant, Cytotoxicity, and Anti-inflammation Activities of Phenanthroline Adducts of Zn(II) and Ni(II) bis(N-alkyl-N-phenyldithiocarbamate)

In this study, 4,7-diphenyl-1,10-phenanthroline adducts of Ni(II) and Zn(II) of N-methyl or ethyl-N-phenyldithiocarbamate were synthesized and the final adducts were represented as [Zn(L1)2L3], [Zn(L2)2L3], [Ni(L1)2L3], [Ni(L2)2L3] (where L1 = methyl, L2 = ethyl, L3 = bathophenanthroline) and characterized using various spectroscopic techniques and elemental analysis. Both the FT-IR and NMR analysis suggest that all the adducts possessed six coordination geometry by the metal atom centres upon the emergence of a new M-N bond. This was shown by the changes observed in the peaks and chemical shifts of the adducts in comparison to the parent complexes. The cytotoxicity, antioxidant, and anti-inflammatory properties were evaluated using different assays to ascertain their biological properties. In all the assays, no noticeable trend was observed between the adducts of similar ligands and metals. Nevertheless, in the antioxidant assays, a good to moderate activity was observed, especially in the DPPH assay, which gave the best radical scavenging properties. Additionally, the estimated IC50 values of 0.011 and 14.76 µM were calculated for the cytotoxicity in the human cervical cancer (HeLa) cell line for both [Zn(L1)2L3] and [Ni(L2)2L3] adducts, respectively, in comparison to 5-Flurouracil (17.48 µM). On the other hand, very low cytotoxicity was found for most of the adducts in the embryonic kidney 293 (HEK 293) cell lines, especially for [Zn(L1)2L3], demonstrating its superior amongst the other adduct and the standard drug. Moreover, the adducts exhibited good to moderate anti-inflammatory properties compared to diclofenac, a controlled drug. These findings thus suggest that the adducts, particularly [Zn(L1)2L3], hold promise as potential anticancer agents and warrant further evaluation through clinical trials.

Treatment affects load to failure and microdamage accumulation in healthy and osteolytic rat vertebrae

Bone turnover and microdamage are impacted by the presence of skeletal metastases which can contribute to increased fracture risk. Treatments for metastatic disease may further impact bone quality. This exploratory study aimed to establish an initial understanding of microdamage accumulation and load to failure in healthy and osteolytic rat vertebrae following focal and systemic cancer treatment (docetaxel (DTX), stereotactic body radiotherapy (SBRT), or zoledronic acid (ZA)). Osteolytic spine metastases were developed in 6-week-old athymic female rats via intracardiac injection of HeLa human cervical cancer cells (day 0). Additional rats served as healthy controls. Rats were either untreated, received SBRT to the T10-L6 vertebrae on day 14 (15 Gy, two fractions), DTX on day 7 or 14, or ZA on day 7. Rats were euthanized on day 21. Tumor burden was assessed with bioluminescence images acquired on day 14 and 21, histology of the excised T11 and L5 vertebrae, and ex-vivo μCT images of the T13-L4. Microstructural parameters (bone volume/total volume, trabecular number, spacing, thickness, and bone mineral density) were measured from L2 vertebrae. Load to failure was measured with axial compressive loading of the L1-L3 motion segments. Microdamage accumulation was labeled in T13 vertebrae with BaSO4 staining and was visualized with high resolution μCT imaging. Microdamage volume fraction was defined as the ratio of BaSO4 to bone volume. DTX administered on day 7 reduced tumor growth significantly (p < 0.05). Microdamage accumulation was found to be increased by the presence of metastases but was reduced by all treatments with ZA showing the largest improvement in HeLa cell injected rats. Load to failure was decreased in untreated and SBRT HeLa cell injected rats compared to healthy controls (p < 0.01). There was a moderate negative correlation between load to failure and microdamage volume fraction in vertebrae from rats injected with HeLa cells (R = −0.35, p = 0.031). Strong correlations were also found between microstructural parameters and load to failure and microdamage accumulation. Several factors, including the presence of osteolytic lesions and use of cancer therapies, influence microdamage accumulation and load to failure in rat vertebrae. Understanding the impact of these treatments on fracture risk of metastatic vertebrae is important to improve management of patients with spinal metastases.

Study on the Active Components and Inhibiting Effect of Melastoma dodecandrum Lour. on Human Cervical Cancer Cells Based on Spectrum–Effect Relationship Analysis

Background The ethnic drug Melastoma dodecandrum Lour. (MDL) is an important medicinal plant with potential antitumor properties, which have been proposed as promising anticancer agents, but the material basis for its therapeutic effect is still unclear and lacks in-depth research. Methods In this study, the in vitro antitumor effects of different MDL extracts in different gynecological tumor cells were investigated by CCK-8 assay. The active components of 21 batches of MDL samples collected from different product areas and markets were determined and compared by the UPLC method. On this basis, the data was processed with the fingerprint similarity software, and the correlation between MDL fingerprint and antihuman cervical cancer activity was further analyzed by a multivariate statistical method. Results Five kinds of MDL extracts, including the aqueous extract, the crude polysaccharide, the total polyphenol, the ethyl acetate fraction of the aqueous extract and 50% ethanol extract, had inhibitory effects on human cervical cancer HeLa and SiHa cells, among which total polyphenols of MDL showed stronger inhibition effect on human cervical cancer cells. In addition, the fingerprint of the total polyphenols of MDL had sixteen common peaks, and six common peaks were checked by using diode array and UV spectra, among which peak 1 (gallic acid), peak 4 (protocatechuic acid), peak 12 (unknown), and peak 15 (ellagic acid) were negatively correlated with the IC50 value of the SiHa cells, and all variable importance values were greater than 1. Conclusion Our data demonstrated that the main active components of MDL inhibiting human cervical cancer SiHa cells may be the synergistic effect of gallic acid, protocatechuic acid and ellagic acid, and the further spectrum-effect relationship analysis provides an important reference and basis for the quality control and the development of new anticervical cancer drug of MDL.

Bioactive O^N^O^ Schiff base appended homoleptic titanium(iv) complexes: DFT, BSA/CT-DNA interactions, molecular docking and antitumor activity against HeLa and A549 cell lines.

Five new homoleptic derivatives of titanium(iv) have been developed and characterized by physicochemical techniques. Metal complexes, TiH2L1 [(C38H26N6O4)Ti], TiH2L2 [(C38H24F2N6O4)Ti], TiH2L3 [(C38H24Cl2N6O4)Ti], TiH2L4 [(C38H24Br2N6O4)Ti] and TiH2L5 [(C38H24N8O8)Ti], were obtained by treating Ti(OPri)4 with appropriate ONO ligands (H2L1-H2L5) in anhydrous THF as solvent. The electronic structures and properties of titanium(iv) complexes (TiH2L1-TiH2L5) and ligands (H2L1-H2L5) were examined by DFT studies. The stability of all synthesized derivatives was assessed by a UV-visible technique using 10% DMSO, GSH medium and n-octanol/water systems. The binding interactions of BSA and CT-DNA with respective titanium(iv) complexes were successfully evaluated by employing UV-visible absorption, fluorescence, circular dichroism (CD) techniques and docking studies. The in vitro cytotoxicity of TiH2L2, TiH2L3 and TiH2L4 complexes was assessed against HeLa (human epithelioid cervical cancer cells) and A549 (lung carcinoma) cell lines. The IC50 values of TiH2L2, TiH2L3 and TiH2L4 were observed to be 28.8, 14.7 and 31.2 μg mL-1 for the HeLa cell line and 38.2, 32.9 and 67.78 μg mL-1 for A549 cells, respectively. Complex TiH2L3 exhibited remarkably induced cell cycle arrest in the G1 phase and 77.99% ROS production selectivity in the HeLa cell line.

P-Terphenyl and Diphenyl Ether Derivatives from the Marine-Derived Fungus Aspergillus candidus HM5-4.

Two undescribed p-terphenyl derivatives, asperterphenylcins A-B (1-2), and two undescribed diphenyl ether derivatives, asperdiphenylcins A-B (3-4), together with three previously described p-terphenyl derivatives-4″-deoxyterprenin (5), terphenyllin (6), and 3″-hydroxyterphenyllin (7)-were obtained from the solid-rice culture of the marine-derived fungus Aspergillus candidus HM5-4, which was isolated from sponges from the South China Sea. Their structures were elucidated by HRESIMS data and NMR spectroscopic analysis. Compound 1 showed a strong inhibitory effect on Neoscytalidium dimidiatum, with an inhibition circle diameter of 31.67 ± 2.36 mm at a concentration of 10.0 µg/disc. Compounds 5 and 7 displayed cytotoxic activity against human chronic myeloid leukemia cells (K562), human liver cancer cells (BEL-7402), human gastric cancer cells (SGC-7901), human non-small cell lung cancer cells (A549) and human HeLa cervical cancer cells, with IC50 values ranging from 3.32 to 60.36 µM, respectively. Compounds 2, 6 and 7 showed potent inhibitory activity against α-glucosidase, with IC50 values of 1.26 ± 0.19, 2.16 ± 0.44 and 13.22 ± 0.55 µM, respectively.

Andrographolide coordinated ruthenium(II) arene complexes: Synthesis, spectral characterization, antioxidant assays, in vitro cytotoxicity, and apoptosis investigation

Two new ruthenium(II)-complexes, [Ru(Ang)((benzene)Cl2] (RuB-Ang) and [Ru(Ang)((p-cymene)Cl2] (RuC-Ang), were synthesized using andrographolide (Ang) as a ligand with [RuCl2(arene)]2 (arene = benzene or p-cymene) and characterized by various spectroscopic techniques. These techniques ascertained the formation of the complexes. An assessment of the antioxidant activity of the compounds indicated better scavenging activity against ABTS•+, DPPH•, O2−, NO• and OH− radicals. The cytotoxic activities of RuB-Ang and RuC-Ang have been evaluated against A549 (human lung) and HeLa (human cervical) cancer cell lines. The complexes exhibited superior anticancer activity to cisplatin and was non-toxic towards human umbilical vein endothelial (HUVEC) cells. The morphological changes of the HeLa and A549 cells with the complexes have been studied by AO-EB and DAPI staining methods. The cytotoxic nature of the compounds was RuC-Ang > RuB-Ang > cisplatin > ligand.

New Pd(II) complexes containing hydrazinyl oxazolyl coumarin derivatives: synthesis, spectral characterization and anti-cancer studies

Abstract New palladium(II) complexes containing coumarin derivatives such as (E)-3(2-(2-(1-(2-oxo-2H-chromen-3-yl)ethylidene)hydrazinyl)oxazol-4-yl)-2H-chromen-2-one (HL 1 ), (E)-7-hydroxy-3(2-(2-(1-(2-oxo-2H-chromen-3-yl)ethylidene)hydrazinyl)oxazol-4-yl)-2H-chromen-2-one (HL 2 ) were successfully designed and synthesized from the reaction of K2[PdCl4] with ligands HL 1&amp;2 with in Methanol medium. The ligands and complexes were characterized by various analytical and spectral techniques such as FT-IR, UV–Vis, 1H NMR and 13C NMR spectral techniques. From the spectral data we confirmed that the ligands neutrally coordinated with Pd(II) ion via their lactone oxygen, azomethine nitrogen and oxazolyl ring nitrogen atoms. The electrolytic nature of the complexes was confirmed by using conductivity experiments. Further anticancer activity of the compounds has examined with HeLa (human cervical cancer) cells along with the cisplatin as positive control and the obtained results revealed that the complexes possess significant anticancer activity and non-toxic towards HUVEC (human umbilical vein endothelial) cells.

In vitro activity of various Kenyan tea extracts against HeLa human cervical cancer cell line and molecular docking of tea catechins on high-risk HPV16E6 protein

Tea (Camellia sinensis) has been revealed to possess potential anticancer properties attributed to its catechin content. This study aimed to investigate the growth-inhibitory effects of various tea extracts on the HeLa cell line and molecular docking analysis of catechins on Human papillomavirus16 oncoprotein 6 (HPV16E6). Different catechins content in black, green, and purple tea were determined by using High-performance liquid chromatography (HPLC); molecular docking of four main catechins on HPV16E6 and in vitro antiproliferative activity and cell apoptosis assay were carried out. Molecular docking results suggested that the tea catechins have the potential to bind to the HPV16 E6 oncoprotein involved in cervical cancer development. The antiproliferative assay results indicated that purple tea had the highest inhibitory activity at both 24 h and 48 h, with IC50 values of 121.1 ± 3.25 μg/mL and 100.1 ± 3.76 μg/mL respectively, followed by green tea with 168.9 ± 12.59 μg/mL and 124.7 ± 3.53 μg/mL IC50 while black tea showed the least effectiveness with IC50 of 221 ± 19.35 μg/mL and 159.6 ± 2.33 μg/mL. DNA fragmentation, a characteristic of apoptosis, was observed in cells treated with the tea extracts. All three tea extracts demonstrated potential anti-cervical cancer activity bIy inhibiting cell proliferation and inducing apoptosis. The tea catechins showed promising interactions with the HPV16 E6 oncoprotein.

Mixed ligand Ni(II) complexes containing 2-chloroquinoline-3-carboxaldehyde-4(N)-substituted thiosemicarbazones and 2,2′-bipyridine: Synthesis, spectral characterization and in-vitro cytotoxicity

Ni(II) complexes (NiL1-NiL4) of 2-chloroquinoline-3-carboxaldehyde-4(N)-substituted thiosemicarbazones and 2,2′-bipyridine ligands were prepared and characterized by various spectroscopic techniques such as Fourier Transform Infrared (FT-IR), Ultraviolet–visible (UV–vis), 1H NMR and mass spectroscopy. The binding of the ligands to the nickel ion was through their azomethine nitrogen and thiolate sulfur atoms. The redox properties of the complexes were analyzed by cyclic voltammetry. The binding affinity of the complexes with CT-DNA (Calf Thymus DNA) and BSA (Bovine Serum Albumin) was studied using absorption and emission methods. The complex NiL3 exhibited better binding activity with high binding constant value with both DNA and BSA. Antiproliferative ability of the Ni(II) complexes (NiL1-NiL4) was explored against human cervical cancer cells HeLa and human normal embryonic kidney cells HEK. The morphological changes induced by the Ni(II) complexes on HeLa cells were analyzed by AO-EB and DAPI staining assays. The results obtained from the cytotoxicity studies showed the better cytotoxicity of the complex NiL3 towards inhibiting the growth of HeLa cells, whereas non toxic nature of the complexes was proved with HEK cells.

Synthesis, Evaluation of anticancer and antimicrobial activities of some Schiff bases derivatives

In this research, compound [1,2-Bis-(4-amino-5-mercapto-4H-[1,2,4]triazol-3-yl)-ethane-1,2-diol] was used as starting material for synthesis different Schiff's Bases compounds. The fusion of tartaric acid with thiocarbohydrazide produce the compound (C1), the Schiff's bases (C2-C4) were created through the condensation of substances (C1) with different substituted benzaldehydes in presence of glacial acetic acid as catalyst. Thin layer chromatography (TLC) was used to confirm the compounds' purity, and spectroscopic methods were used to infer the compounds' structures (FTIR) and magnetic nuclear resonance spectroscopy (1H-NMR and 13C-NMR). The agar well diffusion method was used to test synthesized compounds for their antibacterial activity against K. pneumonia and S. aureus, and the findings were inconsistent. Target substances were tested for their ability to kill human breast cancer at concentrations of 50 and 100 g/mL. Human muscle tissue HC normal cell line, human cervical cancer Hela cell line, and HePG2 cell line. The results showed that the chemicals had potential cytotoxic activity against the Hela cell line, particularly compound (C4), which had the greatest inhibition at doses of 100 mg/mL among the examined substances&#x0D;