MCF-7 Human Cancer Cells Research Articles

Design, Synthesis and Anticancer Evaluation of 1,2,4-Oxadiazole Bearing Isoxazole-Pyrazole Derivatives

A novel library of 1,2,4-oxadiazole bearing isoxazole-pyrazole derivatives (13a-j) were designed, synthesized and evaluated for their anticancer activity towards MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer) and MDA MB-231 (breast cancer) human cancer cell lines by MTT assay. Here etoposide used as standard drug. Among them, five compounds (13b, 13c, 13d, 13h and 13i) were exhibited more potent activity. In which compound 13h was the most promising compound against all cell lines MCF-7, A549, DU-145 and MDA MB-231.

Synthesis and screening of anticancer potentials of some new terephthaldehyde-derived nitrone compounds

Purpose: To synthesize and screen some new nitrone compounds derived from terephthaldehyde for their anticancer potential.
 Methods: Six new compounds (H, p-Me,p-Br, p-Cl, o-Cl and m-Me) were synthesized via a condensation reaction between terephthaldehyde and a variety of aryl hydroxylamine compounds derived from nitrobenzene and its derivatives. The chemical structures of these compounds were identified using elemental CHN analysis and were elucidated using Fourier Transform infra-red (FT-IR), 1H-nuclear magnetic resonance (1H NMR), mass spectrometry (MS), and elemental analysis. The anticancer effects of the compounds were screened in vitro with respect to their cytotoxicity on MCF7 human cancer cells line. The IC50 values were obtained by MTT assay and their effects on apoptosis of MCF-7 cells were assessed using Acridine orange-ethidium bromide AO/EtBr staining method under a fluorescence microscope.
 Results: Only four compounds (2b, 2d, 2e, and 2f) inhibited more than 50 % of the growth of MCF-7 cells. The strongest anti-proliferation effect against MCF-7 cells was exhibited by 2f (m-Me), producing more apoptosis which increased membrane disruption and consistency of lysosome vacuoles; it also exhibited higher cytotoxic effects on human cancer cell lines (IC50 < 7.5) than the other synthesized compounds.
 Conclusion: The new nitrone compounds (2b, 2d, 2e, and 2f) synthesized from terephthaldehyde exhibit some anticancer properties, and so are potential anticancer agents.
 Keywords: Terephthaldehyde, Nitrone, Cytotoxicity, Anticancer, MCF-7 cells

MCF7 Human Breast Cancer Cells Engineered to Stably Overexpress DEPTOR via CRISPR/Cas9 to Reduce Anabolic Capacity

As a potent cellular inhibitor of both mTOR complexes, DEPTOR protein has the potential to dramatically alter the anabolic potential of many different cell types and conditions. Manipulation of DEPTOR protein content means that cellular anabolism can be more aggressively regulated at a single bottleneck of key cellular signaling pathways. This approach could be particularly advantageous in a number of disease states where anabolically aggressive behavior gives rise to specific pathology. To evaluate this concept, we developed a novel subset of the immortalized MCF7 human epithelial breast cancer cell line. By utilizing CRISPR/Cas9 to facilitate a targeted insertion of a constitutively active DEPTOR gene into the human AAVS1 genomic safe harbor site, we examined direct and indirect measures of cellular anabolism to determine the efficacy of abating the anabolic potential of this type of human cancer.MCF7 cells overexpressing DEPTOR (DEP) were generated by genome integration of a constitutively active DEPTOR gene via a homologous directed repair (HDR) based template following a double stranded break (DSB) at the human AAVS1 safe harbor site by Cas9 nuclease. A second group of cells were used as a control by treating them with a vector containing a red fluorescent protein (RFP) gene in lieu of the DEPTOR gene. Both vectors contain a separate promoter for green fluorescence protein (GFP) gene, and N‐acetyltransferase. Both groups of cells were subjected to 14 days of puromycin selection, and appropriate fluorophore presence was confirmed. Rates of protein synthesis were measured using deuterium heavy water stable isotope methods, and cellular anabolic signaling was assessed via immunoblotting.Twenty‐four hour rates of protein synthesis were significantly reduced in DEP compared to RFP (23.390 ± 2.26 vs. 37.314 ± 0.21 %/day, respectively; p=0.029), representing a 37.6% reduction. DEPTOR protein content was found to be significantly higher in the DEP group compared to RFP controls (9.593 ± 3.209 vs. 1 ± 0.552, respectively; p<0.001). Total (0.978 ± 0.202 vs 1 ± 0.162; p=0.841) and phosphorylated (0.65 ± 0.445 vs 1 ± 0.406; p=0.186) p70 S6 KinaseThr389 were not found to be different between DEP and RFP. The phosphorylated to total ratio of p70 S6 Kinase was lower in DEP vs RFP (0.619 ± 0.315 vs 0.978 ± 0.255, respectively; p=0.05). Interestingly, both total 4E‐BP1 (1.340 ± 0.107 vs 1 ± 0.102, p<0.001) and Thr 37/46 phosphorylation (2.106 ± 0.742 vs 1 ± 0.559, p=0.015) were significantly higher in the DEP vs RFP groups, respectively, but the phosphorylated to total ratios were not different between groups.These results indicate that DEPTOR overexpression dramatically impacts the anabolic activity of MCF7 human cancer cells, as shown by significant reductions in protein synthesis rates, as well as phosphorylation of the downstream mTORC1 target p70 S6 Kinase. Increases in phosphorylated and total 4E‐BP1 could be the result of long‐term inhibition of mTORC1 by DEPTOR protein, possibly indicating the need for evaluation of 4E‐BP1’s unique role in regulating transitions between Cap‐Dependent and Cap‐Independent mRNA translation.Support or Funding InformationFunding provided by the Sydney & JL Huffine’s Institute and the College of Education and Human Development.

Synthesis of Potent Cytotoxic Epidithiodiketopiperazines Designed for Derivatization.

We describe our design, synthesis, and chemical study of a set of functional epidithiodiketopiperazines (ETPs) and evaluation of their activity against five human cancer cell lines. Our structure–activity relationship-guided substitution of ETP alkaloids offers versatile derivatization while maintaining potent anticancer activity, offering exciting opportunity for their use as there are no examples of complex and potently anticancer (nM) ETPs being directly used as conjugatable probes or warheads. Our synthetic solutions to strategically designed ETPs with functional linkers required advances in stereoselective late-stage oxidation and thiolation chemistry in complex settings, including the application of novel reagents for dihydroxylation and cis-sulfidation of diketopiperazines. We demonstrate that complex ETPs equipped with a strategically substituted azide functional group are readily derivatized to the corresponding ETP-triazoles without compromising anticancer activity. Our chemical stability studies of ETPs along with cytotoxic evaluation of our designed ETPs against A549, DU 145, HeLa, HCT 116, and MCF7 human cancer cell lines provide insights into the impact of structural features on potency and chemical stability, informing future utility of ETPs in chemical and biological studies.

Antiproliferative Effects of Ocimum basilicum Methanolic Extract and Fractions, Oleanolic Acid and 3-epi-Ursolic Acid

Aims: The aim of the current study was to identify active compound(s) responsible for the antiproliferative effects of O. basilicum and explore their underlying mechanism/s. Background: Plants have been the source of medicines for the treatment of various diseases since ancient times. Ocimum basilicum (Sweet Basil, Bobai Tulsi) has been used in the folk medicine for the treatment of human liver, spleen and stomach cancers. Background: Plants have been the source of medicines for the treatment of various diseases since ancient times. Ocimum basilicum (Sweet Basil, Bobai Tulsi) has been used in the folk medicine for the treatment of human liver, spleen and stomach cancers. Objective: To emphasize the importance of O. basilicum as a potential novel non-toxic alternative to the conventional anticancer therapy. Method: O. basilicum (aerial parts) methanolic extract and fractions were screened against HT-144, MCF-7, NCI-H460 and SF-268 human cancer cell lines using sulforhodamine B assay. The more active Petroleum Ether Insoluble (PEI) fraction was fractionated into six sub-fractions (OB-1 to OB-6). Four pure compounds (3-O-methyl ursolic acid, oleanolic acid, 3-epi-ursolic acid and ursolic acid) were isolated from the more potent sub-fraction OB- 6. Triple channel immunofluorescence microscopy was employed to observe the effects of methanolic extract, PEI fraction, sub-fractions OB-5 and OB-6, 3-epi-ursolic acid and oleanolic acid on the cytoskeleton and nuclei of MCF-7 cells. Result: The methanolic extract and the PEI fraction exhibited selectively greater growth inhibition against MCF-7 cell line (TGI: 56 and 36.2 µg/ml, respectively). By using triple channel immunofluorescence microscopy, it was observed that the methanolic extract, PEI fraction, sub-fraction OB-5 and 3-epi-ursolic acid induced irregular mitotic spindle formation and slowing of mitotic progression in MCF-7 cells while sub-fraction OB-6 induced mitotic arrest in the prophase stage. F-actin aggregation was also visible in PEI fraction, subfraction OB-5 and 3-epi-ursolic acid treated MCF-7 cells. Conclusion: These results emphasize the importance of O. basilicum as a potential novel non-toxic alternative to the conventional anticancer therapy and suggest that it inhibits the growth of MCF-7 cancer cells via multiple mechanisms such as interaction with the microtubules and mitotic spindle apparatus, and F-actin aggregation.

Synthesis and antiproliferative activity of new hybrids bearing neocryptolepine, acridine and α-aminophosphonate scaffolds

Synthesis of novel α-aminophosphonate hybrids 8a–f was accomplished by the reaction of 11-phenoxy-4-formylneocryptolepine 3, aminoalkylamino acridines 6a–f and diphenyl phosphite 7 in the presence of lithium perchlorate as Lewis acid catalyst in methanol. The starting aldehyde 3 was obtained by reaction of 11-chloroneocryptolpine 1 with 4-hydroxybenzaldehyde 2 in the presence of potassium carbonate in DMF, whereas 9-aminoalkylamino acridines 6a–f were synthesized by reaction of 9-chloroacridine 4 with appropriate diamines 5a–f. The structure of all synthesized hybrids was confirmed by spectroscopic methods and showed spectra in consistence with the expected structures. The antiproliferative activity of all synthesized hybrids was evaluated against HCT-116, MCF-7, HepG2 and A549 human cancer cell lines. The screened results proved that most of the reported compounds are potent, especially hybrid 8a, which displayed the highest activity against MCF-7, HepG2 and A549 cancer cell lines with IC50 8.2, 23.1 and 19.4 µM, respectively. This activity is significantly higher than the standard drug doxorubicin. Moreover, hybrid 8f showed most potent activity against HCT-116 cancer cell line with IC50 2.4 µM higher than the reference drug doxorubicin (IC50:10.90 µM).

Structure activity relationship analysis of antiproliferative cyclic C5-curcuminoids without DNA binding: Design, synthesis, lipophilicity and biological activity

The chemical susceptibility of the β-diketone linker between the two aromatic rings in the structure of curcumin to hydrolysis and metabolism has made it crucial to investigate structurally modified analogs of curcumin without such shortcomings. The synthesis of twenty cyclic C5-curcuminoids is described in this study in order to gain more insight into their anticancer structure-activity relationship (SAR). The design of their synthesis included four different cyclanones and five substituted aromatic aldehydes to form four, five-membered subgroups. These model compounds were evaluated in vitro for antiproliferative activity in an XTT cell viability assay against MCF-7 human non-invasive breast adenocarcinoma cancer cells and Jurkat human T lymphocyte leukemia cells in five different concentrations (10 nM, 100 nM, 1 μM, 10 μM and 20 μM). The majority of the compounds investigated have shown remarkable cytotoxicity with IC50 values in the range of 120 nM and 2 μM with very high relative toxicity values to curcumin. The SAR conclusions are drawn and summarized. A method was developed and applied in a TLC based experimental logP measurement, which is new for such C5-curcuminoids. The logP data and structural modifications have shown a strong correlation. The correlation of these experimental logP and the corresponding IC50 values of the model-compounds were calculated according to the Pearson and Kendall correlation coefficient and showed weak concordance. The physicochemical behaviors of the majority of these compounds are in good accordance with Lipinski’s rule. The most promising compound is 7a, which is the most active (IC50 = 0.12–0.32 μM), most potent (80 times of curcumin) with the lowest lipophilicity (experimental logP = 3.22) which is important also from a pharmacokinetic point of view. The analysis of experimental logP and computed ClogP values have revealed good agreement. These cyclic C5-curcuminoids in contrast to curcumin do not bind to natural DNA based on their CD spectra.

Sodium hydroxide mediated alumina nanoparticles from waste aluminum foil sheets – Biological impact and photo-catalytic efficacy on commercial dyes

Herein, we reported a one-pot facile synthesis of alumina nanoparticles using waste aluminum foil sheet and sodium hydroxide by a simple solution method. The synthesized alumina nanoparticles were examined by UV Visible, X-Ray diffraction studies (XRD), Scanning Electron Microscope (SEM), and Energy Dispersive Analysis by X-rays (EDAX) to determine their size, shape, chemical nature and crystal structure. The average size of the alumina nanoparticles was found to be 50–70 nm. Besides the photocatalytic activity of alumina nanoparticles on two different commercial dyes, viz., MG and MB dyes were evaluated under UV light and naturally available daylight sources. The dye degradation percentages of MG dye under daylight irradiation are ∼17.7% and ∼94.8% under UV light irradiation, ∼14.8% and 90.1% for pure dye and alumina nanoparticles respectively. The percentage of degradation of MB dye in the presence of pure dye, alumina nanoparticles under daylight irradiation, and UV light irradiation are ∼19.6%, ∼92.6%, and ∼6%, 87.2% respectively. These results strongly authenticate the enhanced Photocatalytic activity due to efficient charge separation originating in the alumina nanoparticles. The alumina NPs exhibited an effective antibacterial activity against gram-positive and gram-negative bacteria and also showed an inhibition against human MCF-7 cancer cells, indicating its efficiency in the field of biomedical research.

Anti-bacterial/fungal and anti-cancer performance of green synthesized Ag nanoparticles using summer savory extract

Nowadays, the expansion of nanoparticles as antimicrobial and anticancer agents is one of the most exciting methods for cancer therapy and microbial diseases that can vanquish the problems of drug resistance. In this research, the biosynthesis of silver nanoparticles (AgNPs) was stated using Summer Savory extract. Moreover, these AgNPs by UV-Vis spectroscopy, FTIR, XRD, FESEM, EDX, PSA, and zeta potential analysis were characterized, and by antimicrobial and anti-cancerous performance was evaluated. The maximum absorption peak at 472 nm by UV-Visible spectra confirmed the formation of Ag nanoparticles. The results obtained by FT-IR determined the presence of organic compounds such as amines, alkenes, alcohols, phenols, which performed significant roles in the fixating of these nanoparticles. The results obtained from FESEM, EDX, PSA, and Zeta Potential Analysis revealed that synthesized AgNPs had a hexagonal structure with a size ranging from 10 to 100 nm. The antimicrobial properties of the synthesized AgNPs were examined by Minimum Inhibitory Concentration, Minimum Bactericidal Concentration, and Minimum Fungal Concentration against five microbial strains included Klebsiella pneumonia, Escherichia coli, Enterococcus faecalis, Staphylococcus aureus, and Saccharomyces cerevisiae. The results demonstrated that biosynthesized AgNPs had the most antimicrobial activity, especially against E. Coli. The anti-cancerous results of these nanoparticles through MTT assay demonstrated exceptional anticancer effects against K-562 and MCF-7 human cancer cell lines with IC50 values 50 and 200 µg/ml, respectively.

Synthesis and cytotoxic effect of a few N-heteroaryl enamino amides and dihydropyrimidinethiones on AGS and MCF-7 human cancer cell lines.

Background and purpose:Cancer prevalence has increased in the last century posing psychological, social, and economic consequences. Chemotherapy uses chemical molecules to control cancer. New studies have shown that dihydropyrimidinethione (DHPMT) derivatives have the potential of being developed into anticancer agents.Experimental approach:New derivatives of DHPMTs and a few acyclic bioisosters were synthesized via Biginelli reaction and assessed for their toxicity against gastric (AGS) and breast cancer (MCF-7) cell lines through MTT method.Findings / Results:Chemical structures of all synthesized N-heteroaryl enamino amides and DHPMTs were confirmed by spectroscopic methods. Result of biological assessment exhibited that none of the tested agents was more cytotoxic than cis-platin against AGS and MCF-7 cell lines and compound 2b was the most cytotoxic agent against AGS (IC50 41.10 μM) and MCF-7 (IC50 75.69 μM). Cytotoxic data were mostly correlated with the number of H-bond donors within gastric and breast cancer cells.Conclusion and implications:It was realized that DHPMTs were able to inhibit the growth of cancer cells much better than acyclic enamino amides and moreover; N-(4-methylbenzothiazol-2-yl) DHPMT derivative (2b) supposed possible interaction with a poor electron site of target due to the lipophilic nature of benzothiazole ring and also less electron rich nature than isoxazole. Similar scenario was observed with acyclic enamino amides in which incorporation of sulfur and nitrogen containing heterocycles doubled the cytotoxic effects. Results of the present contribution might assist in extending the scope of DHPMTs as privileged medicinal scaffolds.

Antcamphorols A-K, Cytotoxic and ROS Scavenging Triterpenoids from Antrodia camphorata.

Antrodia camphorata is a rare and valuable medicinal mushroom. In this work, 11 new triterpenoids, namely, antcamphorols A-K (1-11), together with 10 known triterpenoids, 12-21, were isolated from dish-cultured A. camphorata. Compound 1 is an unprecedented C31 lanostane-type triterpenoid featuring a methyl group at C-15 and a C-21-O-C-24 tetrahydropyran ring at C-17. Compounds 2-11 are ergostane-type triterpenoids, and they include two pairs of norergostanes 2-5. The structures of the new compounds were identified by NMR, 2D NMR, and HRESIMS data analyses. The absolute configurations of 1 and 6 were defined by X-ray diffraction data, and the absolute configuration at C-25 of 4 was determined by the modified Mosher's method. Compounds 7, 9, 10, 16, and 19 showed significant ROS scavenging activities (63.9-70.5% at 20 μM) in high-glucose-induced HUVECs. Compounds 3 and 8 exhibited moderate cytotoxic activities against U251 (IC50, 9.2 μM) and MCF-7 (IC50, 8.1 μM) human cancer cell lines, respectively.

Anticancer, Antiproliferative and Lactate Dehydrogenase Enzyme Activities of Different Parts of Acorn (Quercus coccifera L.) against A549, MCF-7 and HeLa Human Cancer Cells

Bu çalışmada, Meşe palamudunun (Q. coccifera) dış-kabuk, külah ve iç kısmından elde edilen özütlerin; A549, MCF-7, HeLa kanser hücreleri ve kanserli olmayan HUVEC hücrelerine karşı potansiyel antikanser, antiproliferatif ve nekrotik kapasiteleri araştırılmıştır. Analizler sonucunda, meşe palamudunun farklı kısımlarından elde edilen ekstrelerin en düşük konsantrasyonda dahi antikanser ve antiproliferatif etkiye sahip oldukları ortaya konulmuştur. Palamut meyvesinin külah kısmından elde edilen etanol özütleri, 5.04±0.02 ile 18.04±0.16 µg/mL arasında değişen IC50 değerleriyle, diğer kısımlarından elde edilen özütlerden daha yüksek antikanser aktivite göstermiştir. En yüksek oranda sitotoksik aktivite MCF-7 hücrelerine karşı gözlenirken; en düşük sitotoksik aktivite ise A549 hücrelerinde gözlenmiştir. Antikanser ve antiproliferatif aktivite sonuçlarının aksine, en yüksek LDH aktivitesi HeLa hücrelerinde belirlenmiştir. MTT ve tripan mavisi analiz sonuçlarıyla uyumlu olarak, en yüksek LDH salınım kapasitesi külah kısmından elde etanol özütlerinde saptanmıştır. Bu çalışma; meşe palamudunun, kanser hücrelerinde hücre büyümesini konsantrasyon ve zamana bağlı olarak engelleme potansiyeline sahip olduğunu ortaya koyan, özgün bir çalışmadır.

Design and synthesis of newer 1,3,4-oxadiazole and 1,2,4-triazole based Topsentin analogues as anti-proliferative agent targeting tubulin

A set of two series of 1,3,4-oxadiazole (11a-n) and 1,2,4-Triazole (12a, c, e, g, h, j-n) based topsentin analogues were prepared by replacing imizadole moiety of topsentin through a multistep synthesis starting from indole. All the compounds synthesized were submitted for single dose (10 µM) screening against a NCI panel of 60-human cancer cell lines. Among all cancer cell lines, colon (HCC-2998) and Breast (MCF-7, T-47D) cancer cell lines were found to be more susceptible for this class of compounds. Among the compounds tested, compounds 11a, 11d, 11f, 12e and 12h, were exhibited good anti-proliferative activity against various cancer cell lines. Compounds 11d, 12e and 12h demonstrated better activity with IC50 2.42 µM, 3.06 µM, and 3.30 µM respectively against MCF-7 human cancer cell line than that of the standard drug doxorubicin IC50 6.31 µM. Furthermore, 11d induced cell cycle arrest at G0/G1 phase and also disrupted mitochondrial membrane potential with reducing cell migration potential of MCF-7 cells in dose dependent manner. In vitro microtubule polymerization assays found that compound 11d disrupt tubulin dynamics by inhibiting tubulin polymerization with IC50 3.89 μM compared with standard nocodazole (IC50 2.49 μM). In silico docking studies represented that 11d was binding at colchicine binding site of β-tubulin. Compound 11d emerged as lead molecule from the library of compounds tested and this may serve as a template for further drug discovery.

Synthesis and characterization of biocompatible hydrogel based on hydroxyethyl cellulose-g-poly(hydroxyethyl methacrylate)

A novel polymeric hydrogel composed of hydroxyethyl cellulose-g-poly(2-hydroxyethyl methacrylate) was prepared via graft polymerization of hydroxyethyl methacrylate on the surface of hydroxyethyl cellulose. N,Nʹ-Methylenebisacrylamide was used as a cross-linker. In this work, we changed the ratio of hydroxyethyl cellulose to the monomer, while the potassium persulfate and the cross-liker were used in amounts proportional to the wt% of both the matrix and monomer. The copolymers formation was confirmed by infrared spectroscopy and X-ray diffraction pattern, while the changes in the surface morphology of the hydrogel were examined by scanning electron microscopy. The increase in the monomer ratio gradually improved the thermal stability of the resultant hydrogels. Finally, the cytotoxicity of the new polymeric hydrogels was evaluated using HCT-116, HepG2, MCF-7 human cancer cell lines and RPE-1 normal cell line. The cytotoxicity studies showed that the hydrogels were selectively toxic against the tested human cancer cell lines in a dose-dependent manner, whereas their cytotoxic activity was significantly reduced when they incubated with human RPE-1 normal cell lines, suggesting their possible utility in the formulation of anticancer drugs.

A New Optical Biflavonoid, (2″R)-2″,3″-Dihydrorobustaflavone 7,4′-Dimethyl Ether, and Other Constituents from Selaginella trichoclada Alsto

A new optical biflavonoid, (2” R)-2″,3″-dihydrorobustaflavone 7,4′-dimethyl ether (1), and 6 known compounds (2-7) were isolated for the first time from the 70% ethanol extract of Selaginella trichoclada Alsto. The structures of the compounds were confirmed by extensive spectroscopic data analyses. Racemic compound 1 was separated by chiral-phase high-performance liquid chromatography, and the absolute configurations of (±)-1 were defined by circular dichroism spectroscopic data. Compound 1 exhibited moderate cytotoxicity against MCF-7, A549, and HepG2 human cancer cell lines.

Facile green synthesis and characterization of Crataegus microphylla extract-capped silver nanoparticles (CME@Ag-NPs) and its potential antibacterial and anticancer activities against AGS and MCF-7 human cancer cells

A facile, fast and inexpensive method to preparation of silver nanoparticles (CME@Ag-NPs) with very favorable efficiency in biological assay has been expanded utilizing Crataegus microphylla fruit extract as reducing agent. Some parameters such as pH, time, AgNO3 concentration and temperature on the biological assay efficiency and morphological characteristics of CME@Ag-NPs were investigated to reach optimum condition. FT-IR, XRD, TEM, DLS, FESEM, EDS and UV/Vis analysis were used to investigate the properties of the as-synthesized CME@Ag-NPs. Regular, homogeneous and spherical-like morphology of CME@Ag-NPs with a mean particle size of 30–50 nm was obtained from FESEM and TEM images. The antibacterial activity of CME@Ag-NPs was explored on Acinetobacter baumannii, Staphylococcus aureus, Enterococcus, Pseudomonas, Escherichia coli, Klebsiella and Proteus mirabilis bacteria by MIC and MBC test. Investigation of the antibacterial activity showed that as-obtained nanoparticles have significant activity against Proteus mirabilis (MIC value of 3.5 μg/ml and MBC value of 7 μg/ml) than other bacterial strains. Further, antibacterial activity of CME@Ag-NPs was determined against multidrug-resistant. Interestingly, as-synthesized silver nanoparticles displayed considerable antibacterial activity against all the test strains. In vitro cytotoxicity of nanoparticles on MCF-7 and AGS cell lines was assayed in different concentration of CME@Ag-NPs and doxorubicin as positive control. As the results show, CME@Ag-NPs is excellent effective in inhibiting the growth of MCF-7 and AGS cell lines.

Synthesis of Thiazole Linked Imidazo[2,1-b]Thiazoles as Anticancer Agents

Based on the search for new heterocyclic drugs suitable as anticancer agents and our knowledge of the efficacy of thiazol and imidazothiazole derivatives as anticancer drugs, we have created four new series of thiazolylimidazothiazole derivatives from the reaction of each of imidazothiazole-thiosemicabazone and imidazothiazole-thicarbohydrazone derivatives with acetyl-hydrazonoyl chlorides and ester-hydrazonoyl chlorides in dioxane/drops of Et3N. The structure of the four novel series of thiazolylimidazothiazoles was characterized by physical and spectroscopic tools. In addition, all the newly synthesized derivatives were examined in vitro for their activity against HCT-116 and MCF-7 human cancer cells using the MTT assay to evaluate their pharmaceutical importance. The encouraging potent results observed from anticancer elusidation studies on the newly prepared thiazolylimidazothiazole derivatives make the design and synthesis of novel series of these systems and studying of their pharmaceutical importance an active zone for more and more investigations.

Chemical Composition and Biological Activity of Salicornia fruticosa L.

Abstract Plants have been used as a source of traditional medicine to treat many diseases and conditions for many years. They considered as excellent source of phytochemicals which showed antioxidant and anticancer activities. The aim of the present study is to investigate the chemical composition and to determine the anticancer activity of Salicornia fruticosa (Chenopodiaceae) methanolic extract. S. fruticosa proved to be a source of isorhamnetin and its glycosides and showed anticancer activities. Seven major flavonoids were isolated and identified from the cytotoxic methanolic extract. The isolated compounds were identified, as quercetin 3',4'-dimethyl ether (1), isorhamnetin (2), isorhamnetin 3-O-rhamnoside (3), isorhamnetin 3-O-glucoside (4), isorhamnetin 3-O-rutinoside (5), isorhamnetin 3-O-neohesperidoside (6), isorhamnetin 3-O-rhamnosyl(1-2)arabinoside (7), by chromatographic analysis, chemical and spectroscopic tools (acid hydrolysis, UV, 1H and 13C NMR). Compounds 1 and 3-7 were isolated for the first time from the plant under investigation. The evaluation of cytotoxic activity of the methanolic extract against HCT-116, HepG2, A549 and MCF-7 human cancer cells, by MTT assay, revealed the higher potency of S. Fruticosa extract with IC50 [2.6. 10.9, 37.9, 5.4 (g/ml)] respectively, comparable to that of doxorubicin. The obtained results suggested that the investigated plant could be used for future development of naturally occurring anticancer agent. Subclinical and clinical trials on polar fractions of S. fruticosa are mandatory to pave the way for its use in treatment of cancer diseases (HCT-116, HepG2, A549 and MCF-7).

Bioactive triterpenoid saponins from the tubers of Hemsleya amabilis Diels

Five new cucurbitane-type triterpenoid saponins Xuedanosides A-E (1–5) were isolated from the medicinal plant Hemsleya amabilis Diels by silica gel column, octadecylsilyl (ODS) column, and pre-HPLC techniques. Their structures were determined by spectroscopic analysis and examined alongside existing data from prior studies. Separated compounds were evaluated for their cytotoxic activity in HeLa, HCT-8, MCF-7 and HepG2 human cancer cell lines, and compounds 1 and 2 showed significant effects against HeLa cells with IC50 values of 3.21 and 8.57 μM, respectively.

Synthesis and Cytotoxic Activity of New 1,3,4-Thiadiazole Thioglycosides and 1,2,3-Triazolyl-1,3,4-Thiadiazole N-glycosides.

New 1,3,4-thiadiazole thioglycosides linked to substituted arylidine systems were synthesized via glycosylation of the prepared 1,3,4-thiadiazole thiol compounds. Click strategy was also used for the synthesis of new 1,3,4-thiadiazole and 1,2,3-triazole hybrid glycosides by reaction of the acetylenic derivatives with different glycosyl azids followed by deacetylation process. The cytotoxic activities of the prepared compounds were studied against HCT-116 (human colorectal carcinoma) and MCF-7 (human breast adenocarcinoma) cell lines using the MTT assay. The results showed that the key thiadiazolethione compounds 2 and 3, the triazole glycosides linked to p-methoxyarylidine derivatives 14 and 15 in addition to the free hydroxyl glycoside 20 were found potent in activity comparable to the reference drug doxorubicin against MCF-7 human cancer cells. The acetylenic derivative 2 and glycoside 20 were also found highly active against HCT-116 cell lines.