Cancer Cell Line Caco-2 Research Articles

Kinetic Ultrasound-Assisted Extraction as a Sustainable Approach for the Recovery of Phenolics Accumulated through UVA Treatment in Strawberry By-Products.

Ultrasound-assisted extraction (UAE) is an efficient and sustainable method for extracting bioactive compounds from agro-industrial by-products. Moreover, it has been reported that ultraviolet A (UVA) radiation can induce the biosynthesis and accumulation of bioactive phenolic compounds. This study optimized the efficiency of ultrasound-assisted extraction (UAE) for recovering ultraviolet A (UVA)-induced phenolic compounds in strawberry by-products (RF-N). The impact of three factors (solid-liquid ratio, ethanol concentration, and ultrasound power) on total phenolic compound (TPC) kinetics using Peleg's model was investigated. The developed model showed a suitable fit for both RF-N and strawberry by-products treated with UVA (RF-E). The optimal UAE conditions obtained were of a 1:30 ratio, 46% ethanol, and 100% ultrasound power, resulting in an average yield of 13 g total phenolics kg-1. The bioaccessibility of phenolic compounds during in-vitro digestion was 36.5%, with agrimoniin being the predominant compound. UAE combined with UVA treatment increased the bioactivity of RF extracts, displaying significant anti-proliferative effects on HT29 and Caco-2 cancer cell lines, as well as anti-inflammatory potential and cellular antioxidant activity. The ultrasound proved to be a sustainable and effective technique for extracting phenolic compounds from RF, contributing to the valorization of strawberry agro-industrial by-products, and maximizing their nutraceutical potential.

Targeted Drug Administration onto Cancer Cells Using Hyaluronic Acid-Quercetin-Conjugated Silver Nanoparticles.

Quercetin (QtN) displays low systemic bioavailability caused by poor water solubility and instability. Consequently, it exerts limited anticancer action in vivo. One solution to increase the anticancer efficacy of QtN is the use of appropriate functionalized nanocarriers that preferentially target and deliver the drug to the tumor location. Herein, a direct advanced method was designed to develop water-soluble hyaluronic acid (HA)-QtN-conjugated silver nanoparticles (AgNPs). HA-QtN reduced silver nitrate (AgNO3) while acting as a stabilizing agent to produce AgNPs. Further, HA-QtN#AgNPs served as an anchor for folate/folic acid (FA) conjugated with polyethylene glycol (PEG). The resulting PEG-FA-HA-QtN#AgNPs (further abbreviated as PF/HA-QtN#AgNPs) were characterized both in vitro and ex vivo. Physical characterizations included UV-visible (UV-Vis) spectroscopy, Fourier transform infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), particle size (PS) and zeta potential (ZP) measurements, and biopharmaceutical evaluations. The biopharmaceutical evaluations included analyses of the cytotoxic effects on the HeLa and Caco-2 cancer cell lines using the MTT assay; cellular drug intake into cancer cells using flow cytometry and confocal microscopy; and blood compatibility using an automatic hematology analyzer, a diode array spectrophotometer, and an enzyme-linked immunosorbent assay (ELISA). The prepared hybrid delivery nanosystem was hemocompatible and more oncocytotoxic than the free, pure QtN. Therefore, PF/HA-QtN#AgNPs represent a smart nano-based drug delivery system (NDDS) and could be a promising oncotherapeutic option if the data are validated in vivo.

Synthesis, anticancer activity, molecular docking and molecular dynamics studies of some pyrazole–chalcone hybrids

Four new hybrid compounds (H1–H4) bearing pyrazole (S1 and S2) and chalcone (P1 and P2) fragments were synthesized and characterized. Compounds were assayed for their ability to inhibit the proliferation of human lung (A549) and colon (Caco-2) cancer cell lines. Besides, toxicity against normal cells was determined using the human umbilical vein endothelial cells (HUVEC). In silico molecular docking, molecular dynamics (MD) simulation and absorption, distribution, metabolism, excretion, and toxicity (ADMET) studies were carried out to predict the binding modes, protein stability, drug-likeness and toxicity of the reported compounds. The in vitro anticancer activity of the tested compounds revealed dose-dependent cell-specific cytotoxicity. In silico studies revealed that the compounds have a good binding affinity, possess appropriate drug-likeness properties and have low toxicity profiles. Communicated by Ramaswamy H. Sarma

Anticancer Effect of Fluorouracil and Gum-Based Cerium Oxide Nanoparticles on Human Malignant Colon Carcinoma Cell Line (Caco2).

We investigated whether co-incubation of 5-FU and gum-based cerium oxide nanoparticles (CeO2 NPs) would improve half-maximal inhibitory concentration (IC50) and apoptosis in the Caco-2 cancer cell line Materials and Methods: In this experimental study, we synthesized Ceo-2-XG by the nano perception method. X-ray diffraction (XRD), field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), dynamic light scattering (DLS) and vibrating sample magnetometer (VSM) techniques were employed to characterize the synthesized nanoparticles. The Caco-2 cancer cells were cultured and treated with Ceo-2- XG and 5-FU. Cytotoxicity analysis was carried out using MTT assay on Caco-2 cancer cells. CXCR1, CXCR2, CXCL8, BAX, BCL-2, P53, CASPASE-3, CASPASE-8 and CASPASE-9 gene expression changes were assessed by quantitative reverse-transcriptase polymerase chain reaction (qRT-PCR). The Caco-2 cancer cell mortality mechanism was analyzed using Annexin V-FITC/PI flow cytometry. Using the inverted microscope morphology changes of the Caco-2 cancer cells was observed. With a sample size of roughly 11 nm, TEM analysis revealed spherical structures. Interestingly, after 72 hours, 400 μg/ml nanoparticles significantly lowered the 50 of 5-FU from 101 to 71 μg/ml (P<000.1). Furthermore, qRT-PCR analysis showed that BCL-2, CXCR1, CXCR2 and CXCR8 expressions were significantly decreased in the 5-FU and Ceo-2-XG nanoparticles co-incubated group, compared to the 5-FU alone (P<0.001). Notably, gene expressions of BAX, P53, CASPASE-3, CASPASE-8 and CASPASE-9 were significantly higher in the 5-FU and Ceo- 2-XG nanoparticles co-incubated group, compared to the 5-FU alone (P<0.001). The findings revealed that dead cells owing to apoptosis were more than two times higher in 5-FU and Ceo-2-XG nanoparticles cancer cells than in 5-FU alone treated cancer cells. Co-incubation of 5-FU and Ceo-2-XG nanoparticles significantly increased apoptosis in the Caco-2 cancer cells. The antiproliferative activity of co-incubated 5-FU and Ceo-2-XG nanoparticles on Caco-2 cancer cells was substantially higher than that of 5-FU alone.

Effect of combination treatment of protocatechuic acid with 5-fluorouracil and oxaliplatin on colon cancer Caco-2 cell line

Among the most common antitumor drugs used in the treatment of colon cancer are 5-fluorouracil and oxaliplatin (5-FU and OXA). However, both these drugs have many side effects, and hence there is a need for new treatment\approach to reduce the side effects aas well as drug concentration. In this context, here, we investigated the effect of addition of protocatechuic acid (PCA) onto either monotherapies or combination therapies of 5-FU and OXA on the human colon cancer (Caco-2) cell line. In addition, we did evaluate the synergistic effect of PCA with 5-FU and OXA. Further, we determined the suppressive effects of different doses of PCA alone or in combination with 5-FU/OXA on cell proliferation after 24 and 48 hours. We identified a suppressive effect of PCA on cell viability at 48 h starting from the dose of 50 µM Matrix metalloproteinase-2 (MMP-2) and MMP-9 gene expression levels and apoptotic effects showed significant increases and decreases depending on the dose and time applied in the experimental groups. The highest synergistic activity was seen at 2:1 concentration of 5-FU+ PCA. Our findings indicate the presence of the cytotoxic and apoptotic effects of PCA in Caco-2 cells at 48 h, increasing with a dose- and time-dependent manner.

Low-dimensional compounds containing bioactive ligands. Part XXI: Crystal structures, cytotoxic, antimicrobial activities and BSA binding of zinc complexes with 5-chloro-7-nitro-8-hydroxyquinoline

Four new zinc(II) complexes containing molecules of 5-chloro-7-nitro-8-hydroxyquinoline (HClNQ), NH2(CH3)2[Zn(ClNQ)3]·DMF (1), K[Zn(ClNQ)3]·2DMF (2), {Na[Zn(ClNQ)(SO4)(H2O)]}n (3) and [Zn(ClNQ)2(H2O)2] (4), were prepared and characterized by IR and NMR spectroscopy, elemental analysis and single crystal X-ray analysis. Ionic complexes 1 and 2 have similar structures, in which Zn(II) atoms are coordinated by three chelate molecules of ClNQ via oxygen and nitrogen donor atoms forming rare fac isomers. The negative charge of the complex anions is balanced by uncoordinated NH2(CH3)2+ (1) and K+ cations (2). Complex 3 has a polymeric structure in which Zn(II) atom is penta-coordinated by one chelate molecule of ClNQ, one molecule of water and a pair of crystallographically equivalent sulfato ligands, which interconnect adjacent zinc atoms to form a zig-zag chain. The negative charge of the chain is balanced by sodium cations. In a molecular complex 4, equatorial plane is occupied by two chelate ClNQ molecules with nitrogen and oxygen atoms of the two ligands in an infrequent cis-arrangement and axial positions of a distorted octahedron occupy two aqua ligands. HClNQ and complexes 1, 3 and 4 were tested for their antiproliferative activity against HeLa, A549, MCF-7, MDA-MB-231, HCT-116 and Caco-2 cancer cell lines and their selectivity was verified using Cos-7 non-cancerous cell line. The results showed that the complexes exhibited poor nonselective antiproliferative activity. Antibacterial activity of HClNQ and complexes 1, 3 and 4 were tested, too. RIZD (relative inhibition zone diameter) and MIC (minimal inhibitory concentration) showed that complexes 1, 4 and HClNQ inhibited gram-positive bacteria S. aureus. Against gram-negative bacteria E. coli, only HClNQ and 1 were effective in tested concentration. Finally, BSA binding activity of complexes 1 – 4 was investigated by fluorescence quenching measurements.

Evaluation of probiotic bacteria effect on expression of VDR, IL3 and NOD2 genes in Caco-2 cell line

Probiotics are live and beneficial microorganisms that are known as a factor for prevention of infectious diseases and cancer. In this study, the effects of cytotoxicity of Lactobacillus plantarum extract on the colon cancer cell line (Caco-2) as well as the expression of VDR, IL3 and NOD2 genes were investigated.The supernatant of L. plantarum culture was collected. Then, the effects of cytotoxicity and fluidity of bacteria and Supernatant on Caco-2 cancer cell line were investigated using MTT method. Also, the expression of VDR, IL3 and NOD2 gene was evaluated using Real-Time PCR. Data were analyzed using one-way ANOVA. Investigation of the inhibitory effect of L. plantarum culture supernatant on Caco-2 cells and gene expression at different concentrations showed that 100 μL/mL for VDR, IL3 and NOD2 had the highest increase in gene expression significantly after 48 hours. The MTT test showed the highest lethality at a concentration of 100 μL/mL. Gene expression at 100 μL/mL increased significantly at 24, 48 and 72 h for VDR, 48 h for IL3 and 72 h for NOD2 compared to the control group (P &lt;0.05). L. plantarum can be used to develop a new treatment strategy with high efficacy, low side effects, biologically safe and lower cost. Based on this, it is suggested to investigate the treatment and prevention of colon cancer using L. plantarum.

GC/MS Analysis, Cytotoxicity, and Antiviral Activities of Annona glabra Hexane Extract Supported by In Silico Study.

Annona glabra Linn is employed in conventional medicine to treat a number of human disorders, including cancer and viruses. In the present investigation, the significant phytochemical components of Annona glabra hexane extract were identified using gas chromatography-mass spectrometry (GC-MS) analysis. Three major compounds were identified in the hexane extract: tritriacontane (30.23%), 13, 17-dimethyl-tritriacontane (22.44%), and limonene (18.97%). MTT assay was used to assess the cytotoxicity of the extract on six human cancer cell lines including liver (HepG-2), pancreas (PANC-1), lung (A-549), breast (MCF-7, HTB-22), prostate (PC-3), and colon (CACO-2, ATB-37). The extract exhibited significant cytotoxic activity against both CACO-2 and A-549 cancer cell lines (IC50 = 47 ± 0.74 μg/mL and 56.82 ± 0.92 μg/mL) in comparison with doxorubicin (IC50 = 31.91 ± 0.81 μg/mL and 23.39 ± 0.43 μg/mL) and of SI of 3.8 and 3.1, respectively. It also induced moderate-to-weak activities against the other cancerous cell lines: PC-3, PANC-1, MCF-7, and HepG-2 (IC50 = 81.86 ± 3.26, 57.34 ± 0.77, 80.31 ± 4.13, and 57.01 ± 0.85 μg/mL) in comparison to doxorubicin (IC50 = 32.9 ± 1.74, 19.07 ± 0.2, 15.48 ± 0.84 and 5.4 ± 0.22 μg/mL, respectively) and SI of 2.2, 3.1, 2.2, and 3.1, respectively. In vitro anti-HSV1 (Herpes simplex 1 virus) and HAV (Hepatitis A virus) activity was evaluated using MTT colorimetric assay with three different protocols to test protective, anti-replicative, and anti-infective antiviral activities, and three separate replications of each experiment were conducted. The plant extract showed promising protective and virucidal activity against HSV1 with no significant difference with acyclovir (79.55 ± 1.67 vs. 68.44 ± 7.62 and 70.91 ± 7.02 vs. 83.76 ± 5.67), while it showed mild protective antiviral activity against HAV (48.08 ±3.46) with no significant difference vs. acyclovir (36.89 ± 6.61). The selected main compounds were examined for their bioactivity through in silico molecular docking, which exhibited that limonene could possess the strongest antiviral properties. These findings support Annona glabra's conventional use, which is an effective source of antiviral and anticancer substances that could be used in pharmaceuticals.

Low-Dimensional Compounds Containing Bioactive Ligands. Part XX: Crystal Structures, Cytotoxic, Antimicrobial Activities and DNA/BSA Binding of Oligonuclear Zinc Complexes with Halogen Derivatives of 8-Hydroxyquinoline

Two tetranuclear [Zn4Cl2(ClQ)6]·2DMF (1) and [Zn4Cl2(ClQ)6(H2O)2]·4DMF (2), as well as three dinuclear [Zn2(ClQ)3(HClQ)3]I3 (3), [Zn2(dClQ)2(H2O)6(SO4)] (4) and [Zn2(dBrQ)2(H2O)6(SO4)] (5), complexes (HClQ = 5-chloro-8-hydroxyquinoline, HdClQ = 5,7-dichloro-8-hydroxyquinoline and HdBrQ = 5,7-dibromo-8-hydroxyquinoline) were prepared as possible anticancer or antimicrobial agents and characterized by IR spectroscopy, elemental analysis and single crystal X-ray structure analysis. The stability of the complexes in solution was verified by NMR spectroscopy. Antiproliferative activity and selectivity of the prepared complexes were studied using in vitro MTT assay against the HeLa, A549, MCF-7, MDA-MB-231, HCT116 and Caco-2 cancer cell lines and on the Cos-7 non-cancerous cell line. The most sensitive to the tested complexes was Caco-2 cell line. Among the tested complexes, complex 3 showed the highest cytotoxicity against all cell lines. Unfortunately, all complexes showed only poor selectivity to normal cells, except for complex 5, which showed a certain level of selectivity. Antibacterial potential was observed for complex 5 only. Moreover, the DNA/BSA binding potential of complexes 1–3 was investigated by UV-vis and fluorescence spectroscopic methods.

Discovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities

New quinoline-pyridine hybrids were designed and synthesised as PIM-1/2 kinase inhibitors. Compounds 5b, 5c, 6e, 13a, 13c, and 14a showed in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines. In addition, 6e, 13a, and 13c significantly induced apoptosis with percentage more than 66%. Moreover, 6e, 13a, and 13c significantly induced caspase 3/7 activation in HepG-2 cell line. Furthermore, 5c, 6e, and 14a showed potent in-vitro PIM-1 kinase inhibitory activity. While, 5b showed potent in-vitro PIM-2 kinase inhibitory activity. Kinetic studies using Lineweaver–Burk double-reciprocal plot indicated that 5b, 5c, 6e, and 14a behaved as competitive inhibitors while 13a behaved as both competitive and non-competitive inhibitor of PIM-1 kinase enzyme. Molecular docking studies indicated that, in-silico affinity came in coherence with the observed in-vitro inhibitory activities against PIM-1/2 kinases.

Preparation and Characterization of Capsaicin Encapsulated Polymeric Micelles and Studies of Synergism with Nicotinic Acids as Potential Anticancer Nanomedicines.

Capsaicin micelles were prepared by the direct dissolution using the amphiphilic copolymer Pluronic P123 and advanced for substantially novel submicro-nanocytotoxicity. Superior cytotoxicity of capsaicin loaded nanomicelles vs. both the raw capsaicin and reference cisplatin in pancreatic PANC1, breast MCF7, colorectal resistant CACO2, skin A375, lung A549 and prostate PC3 cancer cell lines were delineated. Nicotinic acid (NA) derivative 39 (2-Amino IsoNA) had antiinflammatory potential but consistently lacked antiproliferation in MCF7, PANC1 and CACO2. Besides NA derivatives 8 (5-MethylNA) and 44 (6-AminoNA) exhibited lack of antiinflammation but had comparable antitumorigenesis potency to cisplatin in PANC1 cells. Though capsaicin loaded nanomicelles exerted pronounced antiinflammation (with IC50 value of 510 nM vs. Indomethacin's) in lipopolysacchride-induced inflammation of RAW247.6 macrophages; they lacked DPPH scavenging propensities. Free capsaicin proved more efficacious vs. its loaded nanocarriers to chemosensitize cytotoxicity of combinations with NAs 1(6-Hexyloxy Nicotinic Acid), 5(6-OctyloxyNA), 8(5-MethylNA), 12(6-Thien-2yl-NA), 13(5,6-DichloroNA) and 44(6-AminoNA) in CACO2, PANC1 and prostate PC3. Capsaicin loaded nanomicelles proved more efficacious vs. free capsaicin to chemo-sensitize antiproliferation of cotreatments with NA derivatives, 1, 5, 8, 12, 13 and 44 (in skin A375), 1, 5, 8 and 12 (in breast MCF7), and 1, 5, 12 and 44 (in lung A549).

Cytoxic Effect Levels Of Sheep Whey Protein in Colorectal Adenocarcinoma Cell Line (Caco-2)

Abstract Objective: It was aimed to determine the antitumor and antiproliferative activity of whey protein (whey) obtained from sheep colostrum isolation on colorectal cancer cells (Caco-2). Method: Colostrum was separated into fractions as whey proteins using the isoelectric point. Before cell culture was studied, whey protein was sterilized by a membrane filter. Antitumoral activity levels of different concentrations of lyophilized proteins were measured by MTT viability test on cells and IC50 values were determined. Results: Sheep whey proteins were incubated with Caco-2 cells for 24, 48 and 72 hours with serial dilutions starting with 3200 µg/ml and decreasing. When incubated with sheep whey Caco-2 cells, cell viability: 66.34% at 24 h; IC50 value of 8.414 µg/ml; IC50 value of 46.61% at 48 h was 5,838 µg/ml; The IC50 value of 4.61% at 72 h was found to be 4,741 µg/ml. Conclusion: It was concluded that whey proteins obtained from sheep colostrum isolation have apoptotic and anticarcinogenic effects on Caco-2 cancer cell line and significantly inhibit the growth of tumor cells. We think that the results of this study will lead to studies to be carried out in vitro.

The first peptide derivatives of dioxybiphenyl-bridged spiro cyclotriphosphazenes: In vitro cytotoxicity activities and DNA damage studies

In this study, we aimed to synthesize new peptide-substituted cyclotriphosphazenes from a series of tyrosine-based peptides and dioxyphenyl-substituted spirocyclotriphosphazenes, and to evaluate their in vitro cytotoxicity and genotoxicity activities. Genotoxicity studies were conducted to understand whether the cytotoxic compounds cause cell death through DNA damage. The structures of the novel series of phosphazenes were characterized by FT-IR, elemental analysis, MS, 1D (31P, 1H, and 13C-APT NMR), and 2D (HETCOR) NMR spectroscopic techniques. In vitro cytotoxic activities were carried out against human breast (MCF-7), ovarian (A2780), prostate (PC-3), colon (Caco-2) cancer cell lines and human normal epithelial cell line (MCF-10A) at different concentrations by using an MTT assay. The compounds showed considerable reductions in cell viability against all human cancer cell lines. Especially, the compounds exhibited notable effects in A2780 cell lines (p < 0.05). The IC50 values of the compounds in the A2780 cell line were calculated to be 1.914 µM for TG, 20.21 µM for TV, 20.45 µM for TA, 4.643 µM for TP, 5.615 µM for BTG, 1.047 µM for BTV, 27.02 µM for BTA, 0.7734 µM for BTP, 21.5 µM for DTG, 1.65 µM for DTV, 2.89 µM for DTA and 4.599 µM for DTP. DNA damage studies of the compounds were conducted by the comet assay method using tail length, tail density, olive tail moment, head length, and head density parameters, and the results showed that the cell death occurred through DNA damage mechanism. In a nutshell, these compounds show promising cytotoxic effects and can be considered powerful candidate molecules for pharmaceutical applications.

Biological Evaluation of Azide Derivative as Antibacterial and Anticancer Agents

Azides are significant compounds because of their biological effects on bacteria, viruses, fungi, and cancer. The antibacterial and anticancer properties of azide derivatives have been demonstrated in several microbial strains and cancer cell lines. The most significant microorganisms in command of hospital-acquired nosocomial infections include Acinetobacter baumannii (A. baumannii), Methicillin-resistant Staphylococcus aureus (MRSA), Candida albicans (C. albicans), and Candida dubliniensis (C. dubliniensis). These infections have become resistant to a variety of antibiotics. These resistant infections are frequently seen in cancer patients. Novel drug-active compounds are thus required that have both antibacterial and anticancer activity. This study examined previously synthesized 1-azido-5,6,7-trimethoxy-2,3-dihydro-1H-indene (4) for its antibacterial and anticancer activities. Antimicrobial activity was assessed using the disc diffusion technique, and minimum inhibitory concentration values were computed for zone formation in the examined pathogens. The study's findings indicate that while azide derivatives did not exhibit any effect against other pathogens, they suppressed bacterial growth with a zone diameter of 10 mm against A. baumannii. The MIC values of azide derivative against A. baumannii were 3.90 µg/ml. WST-8 analysis in Caco-2 cancer and healthy fibroblast cell line was used to determine the anticancer study. As a result of this analysis, the IC50 value was calculated to be 2.99 µM. There is little anticancer activity. A very low toxic effect of the azide compound on fibroblast cells was also observed. These findings suggest that this azide derivative may be tested as a potential antibacterial and anticancer agent.

Low-Dimensional Compounds Containing Bioactive Ligands. Part XIX: Crystal Structures and Biological Properties of Copper Complexes with Halogen and Nitro Derivatives of 8-Hydroxyquinoline

Six new copper(II) complexes were prepared: [Cu(ClBrQ)2] (1a, 1b), [Cu(ClBrQ)2]·1/2 diox (2) (diox = 1,4-dioxane), [Cu(BrQ)2] (3), [Cu(dNQ)2] (4), [Cu(dNQ)2(DMF)2] (5) and [Cu(ClNQ)2] (6), where HClBrQ is 5-chloro-7-bromo-8-hydroxyquinoline, HBrQ is 7-bromo-8-hydroxyquinoline, HClNQ is 5-chloro-7-nitro-8-hydroxyquinoline and HdNQ is 5,7-dinitro-8-hydroxyquinoline. Prepared compounds were characterised by infrared spectroscopy, elemental analysis and by X-ray structural analysis. Structural analysis revealed that all complexes are molecular. Square planar coordination of copper atoms in [Cu(XQ)2] (XQ = ClBrQ (1a, 1b), BrQ (3) and ClNQ (6)) and tetragonal bipyramidal coordination in [Cu(dNQ)2(DMF)2] (5) complexes were observed. In these four complexes, bidentate chelate coordination of XQ ligands via oxygen and nitrogen atoms was found. Hydrogen bonds stabilizing the structure were observed in [Cu(dNQ)2(DMF)2] (5) and [Cu(ClNQ)2] (6), no other nonbonding interactions were noticed in all five structures. The stability of the complexes in DMSO and DMSO/water was evaluated by UV-Vis spectroscopy. Cytotoxic activity of the complexes and ligands was tested against MCF-7, MDA-MB-231, HCT116, CaCo2, HeLa, A549 and Jurkat cancer cell lines. The selectivity of the complexes was verified on a noncancerous Cos-7 cell line. Antiproliferative activity of the prepared complexes was very low in comparison with cisplatin, except complex 3; however, its activity was not selective and was similar to the activity of its ligand HBrQ. Antibacterial potential was observed only with ligand HClNQ. Radical scavenging experiments revealed relatively high antioxidant activity of complex 3 against ABTS radical.

Analysis of bioactive compounds using LC-ESI-MS/MS, cytotoxic, antimicrobial effects, and enzyme activities from Cyclotrichium origanifolium.

Cyclotrichium origanifolium is a medicinal plant belonging to the Lamiaceae family. In this study, phenolic content analysis, antimicrobial effects, and cytotoxic effects of extracts of C. origanifolium were investigated. In the extracts, phenolic compound analysis by the liquid chromatography-electrospray ionization-tandem mass spectrometry method, antimicrobial effect by the minimum inhibition concentration method, and cytotoxic effect on human dermal fibroblasts (HDF), glioblastoma cell (U87), ovarian adenocarcinoma cell (Skov-3), and human colorectal adenocarcinoma cell (CaCo-2) cancer cell lines were investigated. Cytotoxicity analyses were performed by the MTT method. In addition, the GST and AChE enzyme activities of the extracts were also measured. Around 18 compounds were detected in both the methanol and ethanol extract. It was found that the best antimicrobial effect on Gram-negative Pseudomonas aeruginosa was on methanol extract, while the ethanol extract was on Candida albicans fungus (respectively, 2.50 mg/ml, 5.0μg/ml). A 500 μg/ml of methanol extract has been shown to have cytotoxic activity high effect on HDF cells. GST and AChE activity were found to decrease in a concentration-dependent manner.

Sodium borohydride mediated synthesis of nano-sized silver particles: Their characterization, anti-microbial and cytotoxicity studies

This work reports the one-step, fast, easy, simple and economical process for the synthesis of nano-sized and stable silver particles. AgNPs were synthesized at six (0.02 M, 0.04 M, 0.06 M, 0.08 M, 0.10 M and 1.00 M) different concentrations of metal precursor and reducing agent. Sodium borohydride was used as both reducing and stabilizing agent. Characterization studies revealed that all the silver nanoparticles (AgNPs) synthesized were in the range of 10 nm–50 nm, spherical shaped, crystalline nature and with high negative surface charge (−30 mV to −47 mV). Among the AgNPs evaluated for their anti-microbial activity through well diffusion method against Escherichia coli (Gram negative bacteria), Bacillus subtilis (Gram positive bacteria) and Candida albicans (fungi), AgNPs-1.00 showed maximum zone of inhibition with 11.5 mm, 18.5 mm and 10 mm at highest test concentration (100 mg/L), respectively. Cytotoxicity of the AgNPs was determined against MCF-7, PVA1 and Caco-2 cancer cell lines through standard MTT assay. AgNPs-0.08 showed highest mortality% with 90% and 80% against MCF-7 and PVA1 at maximum test concentration (100 mg/L), respectively. However, none of the AgNPs showed toxicity towards Caco-2 cancer cell line. Therefore, AgNPs can be used as anti-microbial agents in the biomedical applications.

TRIM28 Is a Novel Regulator of CD133 Expression Associated with Cancer Stem Cell Phenotype.

CD133 is an extensively studied marker of the most malignant tumor cell population, designated as cancer stem cells (CSCs). However, the function of this glycoprotein and its involvement in cell regulatory cascades are still poorly understood. Here we show a positive correlation between the level of CD133 plasma membrane expression and the proliferative activity of cells of the Caco-2, HT-29, and HUH7 cancer cell lines. Despite a substantial difference in the proliferative activities of cell populations with different levels of CD133 expression, transcriptomic and proteomic profiling revealed only minor distinctions between them. Nonetheless, a further in silico assessment of the differentially expressed transcripts and proteins revealed 16 proteins that could be involved in the regulation of CD133 expression; these were assigned ranks reflecting the apparent extent of their involvement. Among them, the TRIM28 transcription factor had the highest rank. The prominent role of TRIM28 in CD133 expression modulation was confirmed experimentally in the Caco2 cell line clones: the knockout, though not the knockdown, of the TRIM28 gene downregulated CD133. These results for the first time highlight an important role of the TRIM28 transcription factor in the regulation of CD133-associated cancer cell heterogeneity.

Potential Apoptotic Activities of Hylocereus undatus Peel and Pulp Extracts in MCF-7 and Caco-2 Cancer Cell Lines.

There is a huge demand for novel anticancer agents with fewer side effects compared to current therapies. Pitaya, or dragon fruit, is a reservoir of potent anticancer compounds. This research aimed to analyze the phytochemical components of Hylocereus undatus pulp and peel extracts using LC-MS and GC-MS, and to investigate the in vitro effects of both extracts against cancer (breast, MCF-7, and colon, Caco-2) and normal (lung; WI-38 and breast; MCF-10A) cell proliferation using the MTT assay. The apoptosis potential of the anticancer effects was also evaluated using flow cytometry, RT-PCR, and Western blot. The total phenolic and flavonoid contents in the peel extract were significantly higher than those in the pulp extract. Compared to the flavonoid and phenolic acid standards, the LC-MS analysis revealed the presence of nine compounds, which were represented as 84.32 and 5.29 µg/g of the flavonoids and 686.11 and 148.72 µg/g of the phenolic acids in the peel and pulp extracts, respectively. Among the identified compounds, chlorogenic acid, caffeic acid, ferulic acid, and rutin were found at the highest concentration in both plant extracts. Both extracts displayed cytotoxic activity against MCF-7 and Caco-2 cancer cells after 48 h of treatment at IC50 values ranging from 14 to 53 μg/mL with high selective indices against normal WI-38 and MCF-10A cell lines. The increase in apoptosis was revealed by the overexpression of p53, BAX, and caspase-9 and the downregulation of antiapoptotic Bcl-2 mRNA and protein expressions. The results indicate that H. undatus extracts can be a plant source for cancer therapy.

Determination of Anti Tumors Level of Caseın in Human Adenokarsinom Cell

Introduction: In this study, it was aimed to investigate the cytotoxicity and antitumoral activity of casein proteins obtained from bovine milk on colorectal cancer cells (Caco-2). Methods: Milk were fractionated as casein proteins. Antitumor activity levels of different concentrations of lyophilized proteins were measured by MTT viability test on cells and IC50 values were determined. Conclusion: Serial dilutions of casein proteins in milk, starting with 3.200 µg/ml and decreasing, were incubated with Caco-2 cells for 24, 48 and 72 hours. When incubated with bovine casein Caco-2 cells, cell viability: IC50 value found in the 24 hour run 9.172 µg/ml 69.21% at 3.200 µg/ml; IC50 at 48 hours was 8.927 cell viability; 58.5%; The IC50 value at 72 hours was 8.043 µg/ml, and cell viability was found to be 51.91%. It was concluded that bovine casein proteins have limited antiproliferative and anticarcinogenic effects on Caco-2 cancer cell lines.