U937 Cancer Cell Research Articles

Synthesis and Preliminary Studies for In Vitro Biological Activity of Two New Water-Soluble Bis(thio)carbohydrazones and Their Copper(II) and Zinc(II) Complexes

Research in the field of metallodrugs is continually increasing. However, it is often limited by the poor solubility in water of the metal complexes. To try to overcome this problem, the two new ligands bis-(sodium 3-methoxy-5-sulfonate-salicylaldehyde)thiocarbohydrazone (bis-TCH, Na2H4L1) and bis-(sodium 3-methoxy-5-sulfonate-salicylaldehyde)carbohydrazone (bis-CH, Na2H4L2) were synthesized and characterized, both achieving high solubility in water. The speciation of the ligands and their coordinating behaviour towards the biologically relevant Cu(II) and Zn(II) ions were studied spectroscopically and potentiometrically, determining the pKas of the ligands and the formation constants of the complex species. The monometallic and bimetallic Cu(II) and Zn(II) complexes were isolated, and the single-crystal X-ray structure of [Cu2(NaHL1)(H2O)7].3.5H2O was discussed. Finally, preliminary studies of the in vitro cytotoxic properties of the new compounds were started on normal (Hs27) and cancer (U937) cell lines. bis-TCH was able to induce a growth inhibition effect between 40% and 45% in both cell lines; bis-CH did not produce a reduction in cell viability in Hs27 cells but revealed mild antiproliferative activity after 72 h of treatment in U937 cancer cells (GI50 = 46.5 ± 4.94 μg/mL). Coordination of the Cu(II) ions increased the toxicity of the compounds, while, in contrast, Zn(II) complexes were not cytotoxic.

Long-term exposure of human U87 glioblastoma cells to polyethylene microplastics: Investigating the potential cancer progression

Precancerous cells are present in all human bodies. Various environmental triggers can promote the development of cancer. Microplastics, an emerging concern, may potentially act as one such trigger, contributing to cancer initiation or progression. Studies have confirmed the presence of microplastics within the human body. This raises concerns about their potential toxicity and health risks. In the present study, we aimed to investigate the impact of polyethylene microplastics (PE-MPs) within the size range of 37–75 microns on glioblastoma cancer cells. Initially, we assessed the short-term effects of six different concentrations of PE-MPs (20 mg/mL, 10 mg/mL, 5 mg/mL, 2.5 mg/mL, 1.25 mg/mL, and 0.62 mg/mL) on the U87 glioblastoma cell line. The results demonstrated that PE-MPs exposure led to an increase in cell proliferation compared to the untreated control group. Based on these findings, we decided to further explore the long-term effects of PE-MPs on U87 cancer cells. To evaluate the long-term effects, U87 glioblastoma cells were continuously exposed to 0.005 g of PE-MPs over an extended period of 26 days. Chronic exposure to PE-MPs significantly increased the proliferative and migratory capacities of U87 cells compared to the unexposed control group. Furthermore, continuous PE-MPs exposure altered the behavior and morphological characteristics of U87 cells. These cells exhibited a propensity to aggregate and form colonies within the culture flask. The formation of spheroid structures was also observed in the PE-MPs-exposed cell population. The results of this research indicate that polyethylene microplastics can promote the progression of glioblastoma cancer.

Cancer Chemotherapeutic Effect of Vernonia Amygdalina Delile on Glioblastoma Brain Cancer Cell.

This study is targeted at assessing the chemotherapy factor of the ethanol extract of Vernonia amygdalina Delile (VAD). U87 glioblastoma cells were treated with extract and a fraction of Vernonia amygdalina Delile (VAD) was harvested from the herbarium. Cytotoxicity was evaluated to determine the IC50 through microscopic observation followed by an MTT assay. Subsequently, flow cytometry with a FACS type was employed to conduct cell cycle and apoptosis analyses. Annexin V/PI and PI markers were used to assess apoptosis and cell cycle progression. The ethanol extract and ethyl acetate fraction of VAD showed promising effects as cancer chemotherapy in glioblastoma cells. The IC50 values for the extract and fraction were notably low, at 37.65 µg/ml and 10.12 µg/ml, respectively, for U87 cells. Analysis of apoptosis using FACS revealed a more pronounced apoptotic effect of the 15 µg/ml fraction of VAD on both early and late apoptosis compared to the 75 µg/ml extract of VAD. Although some differences in cell cycle properties were observed, there were no significant differences in cell cycle analysis between the extract and fraction. These findings underscore the efficacy of VAD's ethanol extract and ethyl acetate fraction as chemotherapeutic agents against U87 cancer cells. The low IC50 values and significant induction of early apoptosis highlight the cytotoxic effects of these treatments on U87 cells.

Matrix Protein of Vesicular Stomatitis Virus Targets the Mitochondria, Reprograms Glucose Metabolism, and Sensitizes to 2-Deoxyglucose in Glioblastoma.

A potential therapeutic approach for cancer treatment is target oxidative phosphorylation and glycolysis simultaneously. The matrix protein of vesicular stomatitis virus (VSV MP) can target the surface of mitochondria, causing morphological changes that may be associated with mitochondrial dysfunction and oxidative phosphorylation inhibition. Previous research has shown that mitochondrial abnormalities can direct glucose metabolism toward glycolysis. Thus, after treatment with VSV MP, glycolysis inhibition is necessary to completely block glucose metabolism and eradicate cancer. Here, to inhibit glycolysis, the 2-deoxy-D-glucose (2-DG), a synthetic glucose analog was used to combine with VSV MP to treat cancer. This study aims to determine how VSV MP affects the glucose bioenergetic metabolism of cancer cells and to evaluate the synergistic effect of 2-DG when combined with VSV. Our results indicated that in U87 and C6 glioblastoma cell lines, VSV MP caused mitochondrial membrane potential loss, cytochrome c release, and glucose bioenergetics metabolism reprogramming. When combined with 2-DG, VSV MP synergistically aggravated cell viability, apoptosis, and G2/M phase arrest. Meanwhile, the combination therapy exacerbated ATP depletion, activated AMPK, and inhibited mammalian target of rapamycin signaling pathways. In addition, 2-DG treatment alone induced autophagy in glioblastoma cells; however, VSV MP inhibited the autophagy induced by 2-DG in combined treatment and finally contributed to the enhanced cytotoxic effect of the combination strategy in U87 and C6 cancer cells. In the orthotopic U87 glioblastoma model and subcutaneous C6 glioblastoma model, the combined treatment led to significant tumor regression and prolonged survival. A potent therapeutic approach for treating glioblastoma may be found in the combination of VSV MP and glycolytic inhibitors.

Chemical characterization and pharmacological properties of polysaccharides from Allium roseum leaves: In vitro and in vivo assays

Allium roseum is amongst the most important wild medicinal plants. It is known for its diverse biological properties, including antioxidant, antibacterial and antidiabetic activities. In this work, the polysaccharides (PARLs) were ultrasonically extracted from Allium roesum leaves then purified and analyzed by several techniques. Chemical composition and GC–MS analysis showed that the obtained polysaccharides were composed mainly of glucose (40.20 %), mannose (25.30 %), fructose (10.60 %) and galacturonic acid (15.11 %). Moreover, PARLs exhibited a potent antioxidant effect with higher capacities up to 69.61 % and 71.72 % for DPPH and ABTS free radicals, respectively. Furthermore, PARLs significantly modulated inflammatory response by reducing TNF-α, IL-6, and IL-8 pro-inflammatory mediators and promoting the anti-inflammatory IL-10 mediator in LPS stimulated THP-1 derived macrophages. The in-vivo tests proved that the extract was able to decrease carrageenan-induced rat paw swelling by around 68.15 % after 4 h of treatment. PARLs, significantly reduced the growth of U87 (glioblastoma) and IGROV-1 cancer cells with IC50 values of about 4.27 and 7.89 mg/mL respectively. This research clearly shows that Allium roseum polysaccharides can be used as natural antioxidants with anti-inflammatory and anticancer properties.

Basic Fibroblast Growth Factor Accumulation in Culture Medium Masks the Direct Antitumor Effect of Anti-VEGF Agent Bevacizumab.

The direct antitumor effect of bevacizumab (BEV) has long been debated. Evidence of the direct antitumor activities of drugs are mainly obtained from in vitro experiments, which are greatly affected by experimental conditions. In this study, we evaluated the effect of BEV-containing medium renewal on the results of in vitro cytotoxicity experiments in A549 and U251 cancer cells. We observed starkly different results between the experiments with and without BEV-containing medium renewal. Specifically, BEV inhibited the tumor cell growth in the timely replacement with a BEV-containing medium but promoted tumor cell growth without medium renewal. Meanwhile, compared with the control, a significant basic fibroblast growth factor (bFGF) accumulation in the supernatant was observed in the group without medium renewal but none in that with replaced medium. Furthermore, bFGF neutralization partially reversed the pro-proliferative effect of BEV in the medium non-renewed group, while exogenous bFGF attenuated the tumor cell growth inhibition of BEV in the medium-renewed group. Our data explain the controversy over the direct antitumor effect of BEV in different studies from the perspective of the compensatory autocrine cytokines in tumor cells.

The Effects of ABT-199 and Dihydroartemisinin Combination on Cell Growth and Apoptosis in Human U937 and KG-1 Cancer Cells.

Change in the balance of Bcl-2 family proteins is one of the main reasons for resistance of tumor cells to ABT-199. In this study, the effect of dihydroartemisinin on cell growth, apoptosis and sensitivity of the AML cells to ABT-199 was investigated. Cell proliferation and survival were assessed by trypan blue staining and MTT assay, respectively. Cell apoptosis was measured by Hoechst 33342 staining and caspase-3 activity assay. The expression levels of Bcl-2, Mcl-1 and Bax mRNA were tested by qRT-PCR. Our data showed that combination therapy significantly reduced the IC50 value and synergistically decreased the AML cell survival and growth compared with dihydroartemisinin or ABT-199 alone. Treatment with each of ABT-199 or dihydroartemisinin alone clearly enhanced the Bax mRNA expression and inhibited the expression of Mcl-1 and Bcl-2 mRNA. Inhibition of Mcl-1 mRNA by dihydroartemisinin was associated with enhancement of apoptosis induced by ABT-199 in AML cells. In conclusion, dihydroartemisinin not only triggers the intrinsic pathway of apoptosis, but also can increase the sensitivity of the AML cells to ABT-199 via suppression of Mcl-1 expression.

Precise Construction of Dual-Promising Anticancer Drugs Associated with Gold Nanomaterials on Glioma Cancer Cells.

Multiple chemodrugs with nanotechnology have proven to be an effective cancer treatment technique. When taken combined, cabazitaxel (CTX) and cisplatin (PT) have more excellent cytotoxic effects than drugs used alone in the chemotherapy of several different cancers. However, several severe side effects are associated with using these chemotherapy drugs in cancer patients. Gold nanomaterials (AuNMs) are promising as drug carriers because of their small diameter, easy surface modifications, good biocompatibility, and strong cell penetration. This work aimed to determine the CTX and PT encapsulated with AuNMs against human glioma U87 cancer cells. The fabrication of the AuNMs achieved a negative surface charge, polydispersity index, and the mean sizes. The combined cytotoxic effect of CTX and PT bound to AuNMs was greater than that of either drug alone when tested on U87 cells. The half inhibitory concentration (IC50) values for free PT were 54.7 μg/mL (at 24 h) and 4.8 g μg/mL (at 72 h). Results acquired from the MTT assay show cell growth decreases time- and concentration-dependent AuNMs, free CTX, free PT, and AuNMs@CTX/PT-induced cytotoxicity and, ultimately, the cell death of U87 cells via apoptosis. The biochemical apoptosis staining techniques investigated the cells' morphological changes of the cells (acridine orange and ethidium bromide (AO-EB) and nuclear staining (DAPI) techniques). The AO-EB and nuclear staining results reveal that the NPs effectively killed cancer cells. Furthermore, the flow cytometry analysis examined the mode of cell death. Therefore, AuNMs@CTX/PT has excellent potential in the cancer therapy of different cancer cells.

Alternating electric fields can improve chemotherapy treatment efficacy in blood cancer cell U937 (non-adherent cells)

BackgroundRecent achievements in cancer therapy are the use of alternating electrical fields at intermediate frequencies (100–300 kHz) and low intensities (1–3 V/cm), which specifically target cell proliferation while affecting different cellular activities depending on the frequency used.MethodsIn this article, we examine the effect of electric fields on spherical suspended cells and propose the combination of Daunorubicin, a chemotherapy agent widely used in the treatment of acute myeloid leukemia, with electric field exposure. U937 cells were subjected to an electric field with a frequency of 200 kHz and an intensity of 0.75 V/cm, or to a combination of Daunorubicin and electric field exposure, resulting in a significant reduction in cell proliferation. Furthermore, the application of an electric field to U937 cells increased Daunorubicin uptake.ResultsApoptosis and DNA damage were induced by the electric field or in conjunction with Daunorubicin. Notably, normal cells exposed to an electric field did not show significant damage, indicating a selective effect on dividing cancer cells (U937). Moreover, the electric field affects the U937 cell line either alone or in combination with Daunorubicin. This effect may be due to increased membrane permeability.ConclusionsOur findings suggest that the use of electric fields at intermediate frequencies and low intensities, either alone or in combination with Daunorubicin, has potential as a selective anti-cancer therapy for dividing cancer cells, particularly in the treatment of acute myeloid leukemia. Further research is needed to fully understand the underlying mechanisms and to optimize the use of this therapy.

Synthesis, Structural Modification, and Bioactivity Evaluation of Substituted Acridones as Potent Microtubule Affinity-Regulating Kinase 4 Inhibitors.

Acridones present numerous pharmacological activities, including inhibition of microtubule affinity-regulating kinase 4 (MARK4) kinase activity. To investigate structure-activity relationships and develop potent MARK4 inhibitors, derivatives of 2-methylacridone were synthesized and tested for their activity against MARK4 kinase. Selective substitutions at the nitrogen atom were accomplished by treating 2-methylacridone with alkyl halides in the presence of K2CO3. In addition, amidation of acridone acetic acid 11 with piperazine or tryptophan methyl ester followed by derivatization with various amines gave a series of new acridone derivatives. Among the tested compounds, six were identified as possessing high inhibitory activity against MARK4. The molecular modeling studies showed that the derivatives bearing piperazine or tryptophan bind well to the ATP-binding site of MARK4. The antiproliferative activity of six active compounds was evaluated against HeLa and U87MG cancer cells. Tryptophan derivatives 23a, 23b, and 23c showed significant cytotoxicity against both cell lines with EC50 values ranging from 2.13 to 4.22 μM, while derivatives bearing piperazine were found to be not cytotoxic. Additionally, compound 23a decreased the proliferation of human MDA-MB-435 and U251 cancer cells in the low micromolar range; however, it also affects the non-cancerous HGF cells. Due to their high binding affinity against MARK4, the synthesized compounds could be potential agents to target MARK4 against cancer and tauopathies.

Dynamic contrast enhanced (DCE) MRI estimation of vascular parameters using knowledge-based adaptive models

We introduce and validate four adaptive models (AMs) to perform a physiologically based Nested-Model-Selection (NMS) estimation of such microvascular parameters as forward volumetric transfer constant, Ktrans, plasma volume fraction, vp, and extravascular, extracellular space, ve, directly from Dynamic Contrast-Enhanced (DCE) MRI raw information without the need for an Arterial-Input Function (AIF). In sixty-six immune-compromised-RNU rats implanted with human U-251 cancer cells, DCE-MRI studies estimated pharmacokinetic (PK) parameters using a group-averaged radiological AIF and an extended Patlak-based NMS paradigm. One-hundred-ninety features extracted from raw DCE-MRI information were used to construct and validate (nested-cross-validation, NCV) four AMs for estimation of model-based regions and their three PK parameters. An NMS-based a priori knowledge was used to fine-tune the AMs to improve their performance. Compared to the conventional analysis, AMs produced stable maps of vascular parameters and nested-model regions less impacted by AIF-dispersion. The performance (Correlation coefficient and Adjusted R-squared for NCV test cohorts) of the AMs were: 0.914/0.834, 0.825/0.720, 0.938/0.880, and 0.890/0.792 for predictions of nested model regions, vp, Ktrans, and ve, respectively. This study demonstrates an application of AMs that quickens and improves DCE-MRI based quantification of microvasculature properties of tumors and normal tissues relative to conventional approaches.

Biocompatible polysaccharide fabricated graphene oxide nanoparticles: A versatile nanodrug carrier to deliver κ- carrageenan against cancer cells

A graphene oxide mediated hybrid nano system for pH stimuli-responsive and in vitro drug delivery targeted for cancer was described in this study. Graphene oxide (GO) functionalized Chitosan (CS) mediated nanocarrier capped with xyloglucan (XG) was fabricated with and without Kappa carrageenan (κ-C) from red seaweed, Kappaphycus alverzii, as an active drug. FTIR, EDAX, XPS, XRD, SEM and HR-TEM studies were carried out for GO-CS-XG nanocarrier loaded with and without active drugs to understand the physicochemical properties. XPS (C1s, N1s and O1s) confirmed the fabrications of XG and functionalization of GO by CS via the binding energies at 284.2 eV, 399.4 eV and 531.3 eV, respectively. The amount of drug loaded in vitro was 0.422 mg/mL. The GO-CS-XG nanocarrier showed a cumulative drug release of 77 % at acidic pH 5.3. In contrast to physiological conditions, the release rate of κ-C from the GO-CS-XG nanocarrier was considerably higher in the acidic condition. Thus, a pH stimuli-responsive anticancer drug release was successfully achieved with the GO-CS-XG-κ-C nanocarrier system for the first time. The drug release mechanism was carried out using various kinetic models that showed a mixed release behavior depending on concentration and diffusion/swelling mechanism. The best-fitting model which supports our release mechanism are zero order, first order and Higuchi models. GO-CS-XG and κ-C loaded nanocarrier biocompatibility were determined by in vitro hemolysis and membrane stabilization studies. MCF-7 and U937 cancer cell lines were used to study the cytotoxicity of the nanocarrier by MTT assay, which indicates excellent cytocompatibility. These findings support the versatile use of a green renewable biocompatible GO-CS-XG nanocarrier as targeted drug delivery and potential anticancer agent for therapeutic purposes.

Fabrication and Characterization of Ag-Graphene Nanocomposites and Investigation of Their Cytotoxic, Antifungal and Photocatalytic Potential.

In the present study, we aimed to synthesize (Ag)1-x(GNPs)x nanocomposites in variable ratios (25% GNPs-Ag, 50% GNPs-Ag, and 75% GNPs-Ag) via an ex situ approach to investigate the incremental effects of GNPs (graphene nanoparticles) on AgNPs (silver nanoparticles). The prepared nanocomposites were successfully characterized using different microscopic and spectroscopic techniques, including X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, ultraviolet spectroscopy, and Raman spectroscopic analysis. For the evaluation of morphological aspects, shape, and percentage elemental composition, SEM and EDX analyses were employed. The bioactivities of the synthesized nanocomposites were briefly investigated. The antifungal activity of (Ag)1-x(GNPs)x nanocomposites was reported to be 25% for AgNPs and 66.25% using 50% GNPs-Ag against Alternaria alternata. The synthesized nanocomposites were further evaluated for cytotoxic potential against U87 cancer cell lines with improved results (for pure AgNPs IC50: ~150 µg/mL, for 50% GNPs-Ag IC50: ~12.5 µg/mL). The photocatalytic properties of the nanocomposites were determined against the toxic dye Congo red, and the percentage degradation was recorded as 38.35% for AgNPs and 98.7% for 50% GNPs-Ag. Hence, from the results, it is concluded that silver nanoparticles with carbon derivatives (graphene) have strong anticancer and antifungal properties. Dye degradation strongly confirmed the photocatalytic potential of Ag-graphene nanocomposites in the removal of toxicity present in organic water pollutants.

Cellular Response of Cancer to Music: Mirror, Mirror, on the Wall, Which is the Most Effective of Them All?

Aim: Cancer is one of the most common health problems in the world. Music is a therapy method that creates positive changes in human behavior. This study aims to examine the effects of Turkish and Western classical music on MCF-7, SKOV-3, PC-3, U87, and COLO741 cancer cell lines. Material and Methods: Group 1: No sound, Group 2: Turkish classical music (ney), Group 3: Western classical music (piano), and Group 4: Western classical music (violin). After listening to the cancer cells for 40 min, the audio files were interrupted for 1h, and then music was played for another 40 min. The effect of music on the proliferation of cancer cells was determined by WST-1 cell viability analysis. Statistical analyzes were performed with the SPSS program. Results: There was no statistically significant difference between the groups that were applied music once in only the MCF-7 breast cancer cells and the control group (p>0.05). A statistically significant decrease was detected in cell viability when the control group and the other groups that were applied to music twice were compared (p<0.05). For other cancer cell lines except (please the SKOV-3 ovarian cancer cells, it was determined that music application once also caused a statistically significant decrease in cell viability (p<0.05). Conclusion: We determined that classical music effectively reduced and suppressed the number of cancer cells. According to the data, Turkish and Western classical music can be used to support the treatment in of cancer patients.

Modulation of Transcription Profile Induced by Antiproliferative Thiosemicarbazone Metal Complexes in U937 Cancer Cells.

Since the discovery of cisplatin, the search for metal-based compounds with therapeutic potential has been a challenge for the scientific community. In this landscape, thiosemicarbazones and their metal derivatives represent a good starting point for the development of anticancer agents with high selectivity and low toxicity. Here, we focused on the action mechanism of three metal thiosemicarbazones [Ni(tcitr)2], [Pt(tcitr)2], and [Cu(tcitr)2], derived from citronellal. The complexes were already synthesized, characterized, and screened for their antiproliferative activity against different cancer cells and for genotoxic/mutagenic potential. In this work, we deepened the understanding of their molecular action mechanism using an in vitro model of a leukemia cell line (U937) and an approach of transcriptional expression profile analysis. U937 cells showed a significant sensitivity to the tested molecules. To better understand DNA damage induced by our complexes, the modulation of a panel of genes involved in the DNA damage response pathway was evaluated. We analyzed whether our compounds affected cell cycle progression to determine a possible correlation between proliferation inhibition and cell cycle arrest. Our results demonstrate that metal complexes target different cellular processes and could be promising candidates in the design of antiproliferative thiosemicarbazones, although their overall molecular mechanism is still to be understood.

Cyclometalated C^N diphosphine ruthenium catalysts for Oppenauer-type oxidation/transfer hydrogenation reactions and cytotoxic activity

The neutral ruthenium cyclometalated complexes [Ru(C^N)(η2-OAc)(dppb)] proven to be efficient catalysts in Oppenauer-type oxidation and transfer hydrogenation reactions with TOF up to 14 300 h−1 and show cytotoxic activity against U87 cancer cells.

Green synthesis of Zn nanoparticles and in situ hybridized with BSA nanoparticles for Baicalein targeted delivery mediated with glutamate receptors to U87‐MG cancer cell lines

Glioblastoma multiforme (GBM) is the most aggressive malignant tumor of the brain. It has different glutamate receptor types. So, these receptors can be a suitable target for GBM treatment. The current study investigated the anticancer effects of bovine serum albumin (BSA)‐Baicalein @Zn‐Glu nanostructure mediated‐GluRs in human glioblastoma U87 cells. BSA‐Ba@Zn‐Glu hybrid nanoparticles (NPs) were set and considered transporters for Baicalein (Ba) active compound delivery. BSA‐Ba@Zn‐Glu NPs were synthesized by a single‐step reduction process. The successful production was confirmed through transmission electron microscopy (TEM), dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FT‐IR), and hemolysis test. The cytotoxic efficacy and apoptosis rate of the nanostructures on U87 glioblastoma cells were investigated by 3‐(4,5‐dimethylthialzol‐a‐yl)‐2,5 diphenyltetrazolium bromide (MTT) and flow cytometry assays, respectively. The synthesized BSA‐Ba@Zn‐Glu nanostructures with a diameter of 142.40 ± 1.91 to 177.10 ± 1.87 nm and zeta potential of −10.57 ± 0.71 to −35.77 ± 0.60 mV are suitable for extravasation into tumor cells. The drug release from the BSA‐Ba@Zn NPs showed controlled and pH‐dependent behavior. In vitro results indicated that the BSA‐Ba@Zn‐Glu NPs significantly reduce cell viability and promote apoptosis of U87 cancer cells. It revealed the cytotoxic effect of the Baicalein and an increase in cellular uptake of nanoparticles by Glu receptors. Zn NPs were synthesized based on a green synthesis method. BSA NPs were used as a nano‐platform for Glu conjugation and Ba drug delivery. BSA‐Ba@Zn‐Glu NPs induce cytotoxicity and apoptosis in human brain cancer cells (U87) in a dose‐dependent manner. Finally, this nanostructure could be served in targeted drug delivery in vivo studies and applied along with other strategies such as X‐ray irradiation as combinational therapies in future studies.

Selective synthesis of A-ring Е-arylidene derivatives from β-sitosterol and their activity

A series of 24-ethylcholest-4-ene-3,6-dione 2E-arylidene-derivatives has been synthesized by a Claisen-Schmidt reaction from a natural phytosterol β-sitosterol with yields of 80–85%. The structure of the obtained compounds was confirmed by NMR spectroscopy, including two-dimensional correlation experiments. The synthesized compounds were evaluated for their in vitro cytotoxicity and α-glucosidase inhibitory activity. It was established that compound 3 with pyridin-3-ylmethylene moiety exhibited a selective cytotoxic effect against the U251 cancer cell line with 99.31% inhibition of cancer cell growth. Compounds with pyridin-4-ylmethylene 4 and furan-2-ylmethylene-5 fragments were the most active inhibitors of α-glucosidase with IC50 64.00 and 38.95 µM, being 3- and 5-times more active than acarbose. Binding mode to α-glucosidase and ADMET characteristics for the lead molecule 5 were proposed computationally. To sum up, an efficient approach to the derivatives with promising antidiabetic activity based on available natural product β-sitosterol is suggested.

Phenylthiol-BODIPY-based supramolecular metallacycles for synergistic tumor chemo-photodynamic therapy

The development of more effective tumor therapy remains challenging and has received widespread attention. In the past decade, there has been growing interest in synergistic tumor therapy based on supramolecular coordination complexes. Herein, we describe two triangular metallacycles (1 and 2) constructed by the formation of pyridyl boron dipyrromethene (BODIPY)-platinum coordination. Metallacycle 2 had considerable tumor penetration, as evidenced by the phenylthiol-BODIPY ligand imparting red fluorescent emission at ∼660 nm, enabling bioimaging, and transport visualization within the tumor. Based on the therapeutic efficacy of the platinum(II) acceptor and high singlet oxygen (1O2) generation ability of BODIPY, 2 was successfully incorporated into nanoparticles and applied in chemo-photodynamic tumor therapy against malignant human glioma U87 cells, showing excellent synergistic therapeutic efficacy. A half-maximal inhibitory concentration of 0.35 μM was measured for 2 against U87 cancer cells invitro. In vivo experiments indicated that 2 displayed precise tumor targeting ability and good biocompatibility, along with strong antitumor effects. This work provides a promising approach for treating solid tumors by synergistic chemo-photodynamic therapy of supramolecular coordination complexes.

Ag@Ag2MoO4 decorated polyoxomolybdate/C3N4 nanostructures as highly efficient photocatalysts for the wastewater treatment and cancer cells killing under visible light

• Facile fabrication of Ag/Ag 2 MoO 4 /POM/C 3 N 4 plasmonic photocatalyst. • Anazolene Sodium dye solution is efficiently removed over the photocatalyst. • U251 cancer cells are drastically killed over the photocatalyst powder. • The photocatalytic pathways are well described based on ESR results and reaction conditions. Organic contaminants and biomedical wastes from industrial and academic activities have significantly affected the life quality of human being and organisms of the ecosystem. Photocatalytic materials have been prominent candidates to treat the above-mentioned hazards during the past decades. The novel Ag@Ag 2 MoO 4 /polyoxomolybdate/C 3 N 4 nanostructure was successfully fabricated by a combined pyrolysis-coprecipitation method at room temperature. The materials were characterized using a multi-technique approach to analyze the morphology and physicochemical properties. Based on the DRS analysis results, the final photocatalyst, Ag/Ag 2 MoO 4 /POM/C 3 N 4 , had a bandgap of 2.68 eV, suitable for absorbing the photons in the visible region. PL analysis results also confirmed the more efficient charge separation over Ag/Ag 2 MoO 4 /POM/C 3 N 4 compared to the pristine carbon nitride. Photocatalytic performance of the materials was evaluated for the removal of Anazolene Sodium dye compound and the treatment of biomedical waste, U251 cancer cells samples, which are extensively released to the environment as the result of academic activities. ESR technique was served to clarify the mechanism of the reaction. The results of the photocatalytic tests well supported the suitability of the photocatalysts for purifying the organic and biological wastes as two types of remarkable hazards in the ecosystem.