Cationic first-row transition metal saccharinate complexes with tris(2-pyridylmethyl)amine: synthesis, structures and anticancer studies.

A series of new cationic first-row transition metal complexes of [Mn(sac)(HO)(tpma)](sac)·HO (Mn), [(μ-O){FeCl(tpma)}](sac)·3HO (Fe), [Co(sac)(HO)(tpma)](sac)·HO (Co), [Ni(HO)(tpma)](sac)·2HO (Ni), [Cu(sac)(tpma)](sac) (Cu) and [Zn(sac)(HO)(tpma)](sac) (Zn), where sac = saccharinate and tpma = tris(2-pyridylmethyl)amine, were synthesized and structurally characterized by elemental analysis, UV-Vis, IR, ESI-MS, NMR, X-ray diffraction and conductivity measurements. The cytotoxic activity of the metal complexes was evaluated against lung carcinoma (A549), breast adenocarcinoma (MCF7), colon (HT29), and normal BEAS-2B cell lines. Mn and Fe displayed potent cytotoxic activity in all cell lines with IC values between 1.

Fabrication of a Dual-Drug-Loaded Smart Niosome-g-Chitosan Polymeric Platform for Lung Cancer Treatment.

Changes in weather conditions and lifestyle lead to an annual increase in the amount of lung cancer, and therefore it is one of the three most common types of cancer, making it important to find an appropriate treatment method. This research aims to introduce a new smart nano-drug delivery system with antibacterial and anticancer capabilities that could be applied for the treatment of lung cancer. It is composed of a niosomal carrier containing curcumin as an anticancer drug and is coated with a chitosan polymeric shell, alongside Rose Bengal (RB) as a photosensitizer with an antibacterial feature.

Review on Methods, High-throughput Screening Techniques, and Cell Culture Based Assays for SARS-CoV-2.

The COVID-19 outbreak caused by the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) continues to have high incidence and mortality rate globally. To meet the increasingly growing demand for new therapeutic drugs and vaccines, researchers are developing different diagnostic techniques focused on screening new drugs in clinical use, developing an antibody targeting a SARS-CoV-2 receptor, or interrupting infection/replication mechanisms of SARS-CoV-2. Although many prestigious research publications are addressing this subject, there is no open access platform where all experimental techniques for COVID-19 research can be seen as a whole.

The neutralization effect of montelukast on SARS-CoV-2 is shown by multiscale in silico simulations and combined in vitro studies.

Small molecule inhibitors have previously been investigated in different studies as possible therapeutics in the treatment of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). In the current drug repurposing study, we identified the leukotriene (D4) receptor antagonist montelukast as a novel agent that simultaneously targets two important drug targets of SARS-CoV-2. We initially demonstrated the dual inhibition profile of montelukast through multiscale molecular modeling studies.

Palladium (II) complex and thalidomide intercept angiogenic signaling via targeting FAK/Src and Erk/Akt/PLCγ dependent autophagy pathways in human umbilical vein endothelial cells.

The current study assessed the effects of the thalidomide and palladium (II) saccharinate complex of terpyridine on the suppression of angiogenesis-mediated cell proliferation. The viability was assessed after treatment with palladium (II) complex (1.56-100 μM) and thalidomide (0.

Synergistic interactions between resveratrol and doxorubicin inhibit angiogenesis both in vitro and in vivo.

Resveratrol is a polyphenolic compound which is found in many nutrients including grapes, peanuts, raspberries, and apples. Anti-proliferative, anti-angiogenic and apoptotic effects of resveratrol have been shown on various cancer cells. Doxorubicin is considered as one of the most effective anticancer agents and reveals its antitumor activity by induction of apoptosis and inhibition of angiogenesis.

Palladium (II) Complex Enhances ROS-Dependent Apoptotic Effects via Autophagy Inhibition and Disruption of Multiple Signaling Pathways in Colorectal Cancer Cells.

Background: Inhibition of autophagy is reported to be a therapeutically effective strategy in overcoming resistance that is a deadly outcome in cancer. One of the most common reasons for chemo-resistance to treatment is the patients with tumors exhibiting a KRAS mutation, which occurs in approximately 40% of colorectal cancer patients.

Objective: Hence, we assessed whether a Palladium (Pd)(II) complex is a promising anticancer complex, compared to 5-fluorouracil in KRAS wt HT-29 and KRAS mutant HCT-15 cells.

New manganese(II), iron(II), cobalt(II), nickel(II) and copper(II) saccharinate complexes of 2,6-bis(2-benzimidazolyl)pyridine as potential anticancer agents.

New mononuclear complexes [Mn(NO)(sac)(HO)(bzimpy)]·2DMF (Mn), [Fe(sac)(HO)(bzimpy)]·2HO (Fe), [Co(bzimpy)](sac)·2HO (Co), [Ni(bzimpy)](sac)·HO·i-PrOH (Ni) and [Cu(sac)(bzimpy)]·3DMF (Cu) (sac = saccharinate and bzimpy = 2,6-bis(2-benzimidazolyl)pyridine) were synthesized and structurally characterized by elemental analysis, UV-Vis, IR, ESI-MS and X-ray diffraction. The anticancer activity of the metal complexes against A549 (lung), MCF-7 (breast), HT29 (colon) cancer cells and MCF10A (normal human breast epithelial) cells was tested and compared with those of cisplatin and bzimpy. The complexes displayed potent cytotoxic activity especially in MCF-7 and A549 cell lines, but they were practically inactive against the normal cells.

Correction: Zn(ii), Cd(ii) and Hg(ii) saccharinate complexes with 2,6-bis(2-benzimidazolyl)pyridine as promising anticancer agents in breast and lung cancer cell lines via ROS-induced apoptosis.

Correction for 'Zn(ii), Cd(ii) and Hg(ii) saccharinate complexes with 2,6-bis(2-benzimidazolyl)pyridine as promising anticancer agents in breast and lung cancer cell lines via ROS-induced apoptosis' by Ceyda Icsel et al., Dalton Trans., 2020, 49, 7842-7851, DOI: .

A promising therapeutic combination for metastatic prostate cancer: Chloroquine as autophagy inhibitor and palladium(II) barbiturate complex.

Autophagy is a catabolic process for cells that can provide energy sources and allows cancer cells to evade cell death. Therefore, studies on the combination of autophagy inhibitors with drugs are increasing as a new treatment modality in cancer. Previously, we reported the anti-tumor activity of a Palladium (Pd)(II) complex against different types of cancer in vitro and in vivo.

Zn(ii), Cd(ii) and Hg(ii) saccharinate complexes with 2,6-bis(2-benzimidazolyl)pyridine as promising anticancer agents in breast and lung cancer cell lines via ROS-induced apoptosis.

New Zn(ii), Cd(ii) and Hg(ii) complexes of saccharinate (sac) and 2,6-bis(2-benzimidazolyl)pyridine (bzimpy), [Zn(bzimpy)2](sac)2·2H2O (Zn), [Cd(sac)2(bzimpy)] (Cd) and [Hg(sac)2(bzimpy)] (Hg), were prepared and fully characterized by spectroscopic methods and X-ray crystallography. In vitro anticancer screening in A549 (lung), MCF-7 (breast) and HT29 (colon) cell lines showed that Zn was highly cytotoxic against A549 and MCF-7 cells with IC50 values of 1.74 ± 0.

Induction of autophagy enhances apoptotic cell death via epidermal growth factor receptor inhibition by canertinib in cervical cancer cells.

Background: It has been known epidermal growth factor receptor (EGFR) frequently overexpressed in cervical cancer. High levels of EGFR expression in their tumors leads to a poor prognosis and inhibition frequently induces autophagy in cancer cells. This study aimed to investigate whether EGFR inhibition by canertinib induces autophagy and this induction influence the effect of Palladium (Pd) (II) complex and 5-fluorouracil (5-FU) especially in nontoxic doses.

Bioassay-guided isolation of cytotoxic compounds from Chrysophthalmum montanum (DC.) Boiss.

Bioassay-guided isolation of the 80% methanol extract of the aerial parts of Chrysophthalmum montanum (DC.) Boiss. (Asteraceae) led to the isolation of four known guaianolide-type sesquiterpene lactones, 6α-acetoxy-4α-hydroxy-1βH-guaia-9.

Chloroquine Used in Combination with Chemotherapy Synergistically Suppresses Growth and Angiogenesis and .

Background: The inhibition of autophagy using pharmacological inhibitors such as chloroquine may be an effective strategy to overcome chemotherapy or resistance to anti-angiogenic therapy.

Materials And Methods: The cytotoxic effect of doxorubicin (0.1-1 μM), chloroquine (0.

Structures and biochemical evaluation of silver(I) 5,5-diethylbarbiturate complexes with bis(diphenylphosphino)alkanes as potential antimicrobial and anticancer agents.

New silver(I) 5,5-diethylbarbiturate (barb) complexes with a series of bis(diphenylphosphino)alkanes such as 1,1-bis(diphenylphosphino)methane (dppm), 1,2-bis(diphenylphosphino)ethane (dppe), 1,3-bis(diphenylphosphino)propane (dppp) and 1,4-bis(diphenylphosphino)butane (dppb) were synthesized and characterized. [Ag(barb)(μ-dppm)] (1), [Ag(barb)(μ-dppe)(DMSO)] (2) and [Ag(barb)(μ-dppp)] (3) were binuclear, while [Ag(barb)(μ-dppb)] (4) was a coordination polymer. 1-4 effectively bind to the G/C rich region of the major groove of DNA and interact with BSA via hydrophobic interactions in accordance with molecular docking studies.

Synthesis, structures and biomolecular interactions of new silver(i) 5,5-diethylbarbiturate complexes of monophosphines targeting Gram-positive bacteria and breast cancer cells.

A series of new silver(i) 5,5-diethylbarbiturate (barb) complexes with the formulas [Ag(μ-barb)(PPh)] (1), [Ag(barb)(PPhCy)] (2), [Ag(barb)(PPhCy)] (3) and [Ag(barb)(PCy)] (4) (PPh = triphenylphosphine, PPhCy = diphenylcyclohexylphosphine, PPhCy = dicyclohexylphenylphosphine and PCy = tricyclohexylphosphine) were synthesized and fully characterized by elemental analysis, IR, NMR, ESI-MS and X-ray crystallography. All the complexes display a significant affinity towards DNA with a groove binding mode and also strongly bind to BSA via hydrophobic interactions. Lipophilicity increases from 1 to 4 with an increasing number of Cy groups in the phosphine ligands.

Enhanced cytotoxic activity of doxorubicin through the inhibition of autophagy in triple negative breast cancer cell line.

Background: The outcome of triple negative breast cancer is still poor and requires improvement with better therapy options. Autophagy has recently been shown to play a role in anticancer drug resistance. Therefore, we investigated if the effectiveness of doxorubicin was augmented by the inhibition of autophagy.

Anti-angiogenic effect of a Palladium(II)-Saccharinate Complex of Terpyridine in vitro and in vivo.

Anti-angiogenic activity of palladium (Pd)(II)-based complexes is unknown despite their quite powerful anticancer activity. This study was therefore carried out to evaluate both in vivo anti-angiogenic effect and in vitro cytotoxic activity of a Pd(II)-based complex. ([Pd(sac)(terpy)](sac)·4HO(sac=saccharinate and terpy=2,2':6',2″-terpyridine)) on HUVEC cells.

Different DNA immobilization strategies for the interaction of anticancer drug irinotecan with DNA based on electrochemical DNA biosensors.

The interaction of anticancer drug irinotecan (CPT-11) which is the inhibitor of the Topoisomerase I enzyme, with fish sperm double stranded deoxyribonucleic acid (dsDNA) and synthetic short oligonucleotides were studied electrochemically based on the oxidation signals of guanine and CPT-11 by using differential pulse voltammetry (DPV) and cyclic voltammetry (CV) at pencil graphite electrode (PGE). In this work, three types of methods such as adsorption, covalent attachment and electrostatic binding were used for the immobilization of DNA onto the PGE surface. It is found that an effective modification method for DNA on the electrode surface is very important because it shows an effect on the drug and DNA interaction.

The influence of Microgynon and Diane-35, two sub-fifty ovulation inhibitors, on voice function in women.

The early days of oral contraceptives showed some evidence that these medications may have caused undesirable side effects on the voice, mainly in terms of virilization. In a random study carried out at the university hospitals of Jena and Berlin (Charité), two more recent drugs were tested in this regard, one containing cyproterone acetate (Diane-35) and the other one levonorgestrel (Microgynon), both from Schering. Ninety-one patients took part in extensive clinical and instrumental phoniatric investigations of voice function over a period of one year.

Multicentred, phase III clinical trial of norethisterone enanthate 50 mg plus estradiol valerate 5 mg as a monthly injectable contraceptive; final three-year report.

Norethisterone enanthate (NET-EN) 50 mg combined with estradiol valerate (EV) 5 mg was studied as a once-a-month injectable contraceptive with regard to effectiveness, cycle control, adverse events and acceptability. In eight Family Planning Centres from five Latin American countries, 931 fertile women were followed-up for a period of 36 months, providing a total of 15,787 woman-months of experience. Only one pregnancy occurred: in the first treated month a few days before the second injection (failure rate 0.

A multicentred, two-year, phase III clinical trial of norethisterone enanthate 50 mg plus estradiol valerate 5 mg as a monthly injectable contraceptive.

Norethisterone enanthate (NET-EN) 50 mg combined with estradiol valerate (EV) 5 mg was studied as a once-a-month injectable contraceptive with regard to effectiveness, cycle control, adverse events and acceptability. In eight Family Planning Centres from 5 Latin American countries, 652 fertile women were followed-up for a period of 24 months, providing a total of 10,689 woman-months of experience. Only 1 pregnancy occurred, in the first treated month a few days before the second injection (failure rate 0.

Ovulation inhibitors containing cyproterone acetate or desogestrel in the treatment of hyperandrogenic symptoms.

An open, randomized, multicenter study was carried out to compare two oral contraceptives as regards their therapeutic efficacy in androgenization symptoms such as acne, seborrhea and hirsutism in women. The preparations used were the combination of 2 mg cyproterone acetate (CPA) with 0.035 mg ethinyl estradiol (EE) (Diane 35, Schering AG, Berlin-West) and 0.