Ehrlich Ascites Carcinoma Cell Line Research Articles

Synthesis of Silver Nanoparticles Using Camellia sinensis Leaf Extract: Promising Particles for the Treatment of Cancer and Diabetes.

Both diabetes and cancer pose significant threats to public health. To overcome these challenges, nanobiotechnology offers innovative solutions for the treatment of these diseases. However, the synthesis of nanoparticles can be complex, costly and environmentally toxic. Therefore, in this study, we successfully synthesized Camellia sinensis silver nanoparticles (CS-AgNPs) biologically from methanolic leaf extract of C. sinensis and as confirmed by the visual appearance which exhibited strong absorption at 456 nm in UV-visible spectroscopy. The fourier transform infrared spectroscopy (FTIR) analysis revealed that phytochemicals of C. sinensis were coated with AgNPs. Scanning electron microscopy (SEM) analysis showed the spherical shape of CS-AgNPs, with a size of 15.954 nm, while X-ray diffraction spectrometry (XRD) analysis detected a size of 20.32 nm. Thermogravimetric analysis (TGA) indicated the thermal stability of CS-AgNPs. The synthesized CS-AgNPs significantly inhibited the ehrlich ascites carcinoma (EAC) cell growth with 53.42±1.101 %. The EAC cell line induced mice exhibited increased level of the serum aspartate aminotransferase (AST), alanine transaminase (ALT), and alkaline phosphatase (ALP), however this elevated serum parameter significantly reduced and controlled by the treatment with CS-AgNPs. Moreover, in a streptozotocin-induced diabetic mice model, CS-AgNPs greatly reduced blood glucose, total cholesterol, triglyceride, low-density lipoprotein (LDL) and creatinine levels. These findings highlight that the synthesized CS-AgNPs have significant anticancer and antidiabetic activities that could be used as promising particles for the treatment of these major diseases. However, pre-clinical and clinical trial should be addressed before use this particles as therapeutics agents.

Pharmaceutical manifestation of Knoevenagel condensed metal (II) complexes through virtual, in vitro and in vivo assessments

Sulphur containing compounds possess a great deal of interest due to wide range of beneficial activities towards biotic species. This work also deals with the study of biological examination of newly synthesized sulphur containing Cu(II) and Zn(II) complexes derived from (E)-4-(phenylimino)-3-((E)-1-(phenylimino)ethyl)pent-2-ene-1-thiol Schiff bases. Moreover, the DNA nuclease efficiency of the synthesized metal complexes is studied by UV absorption studies, Fluorescence studies, Viscosity and CV titrations which confirm the intercalative mode of binding. Pharmacokinetic studies and drug like activity of these compounds are screened with the help of SWISS ADME online freeware. Their morphological nature is corroborated by various spectral techniques. Optimized geometry and biologically accessible nature of the synthesized compounds are investigated by Gaussian 09 W software. Interestingly, molecular docking studies are carried out against cancer DNA and 6J10 cancer cell. Anti–inflammatory and in vitro antioxidant activities have been studied to validate the theoretical prediction. Based on these preliminary pharmacological activities, the in vitro cytotoxicity and in vivo antitumor activities are examined using MCF-7, HeLa, Hep-2, HepG-2 and Ehrlich ascites carcinoma (EAC) cell lines. All the above examinations reveal that the nitro substituted transition metal complexes possess higher biological bustle. Communicated by Ramaswamy H. Sarma

Dual function of new Nd(III) and Gd(III) complexes for cytotoxic and optoelectronic fields: Synthesis, characterization, DFT calculations, and PVA composite films

New two lanthanide complexes of Neodymium (III) and Gadolinium (III) ions were prepared based on 2‐Cyano‐N′‐([4‐oxo‐4H‐chromen‐3‐yl]methylene) acetohydrazide as a chelating agent. The prepared Nd(III) and Gd(III) complexes were characterized via elemental analysis, molecular conductance, IR, and TGA. The obtained results showed the chelating agent behaves as tridentate via oxygen of γ pyrone and carbonyl groups and nitrogen of the azomethine group. The antitumor activity of isolated complexes was investigated against the Ehrlich Ascites Carcinoma cell line (E.A.C). The results of antitumor activity cleared that Gd(III) complex has higher activity than Nd(III) complex and moderate activity relative to cisplatin and 5‐Furacil. Besides, DFT calculations were estimated for prepared Nd(III) and Gd(III) complexes by the Gaussian program. Theoretical parameters were calculated. The energy gap values confirmed the higher activity of the Gd(III) complex over the other Nd(III) complex. In addition, the composite films of Nd(III) and Gd(III) complexes were prepared using the cast technique. The electrical and optical absorption properties of these polymer composites were analyzed.

Development and optimization of nanoparticles loaded with erucin, a dietary isothiocyanate isolated from Eruca sativa: Antioxidant and antiproliferative activities in ehrlich-ascites carcinoma cell line.

The study on Erucin (ER) has gained interest of nutraceutical and pharmaceutical industries because of its anti-cancer properties. Erucin is an isothiocyanate obtained from the seeds of Eruca sativa which possess certain drawbacks such as poor aqueous solubility and bioavailability. Therefore, the present study aimed at developing ER-cubosomes (CUB) by solvent evaporation technique followed by applying Central Composite Design to optimize ER loaded cubosomes. For this purpose, independent variables selected were Monoolein (MO) as lipid and Pluronic-84 (P-84) as a stabilizer whereas dependent variables were particle size, percentage of ER loading and percentage of its entrapment efficiency. The cubosomal nanocarriers exhibited particle size in the range of 26nm, entrapment efficiency of 99.12 ± 0.04% and drug loading of 3.96 ± 0.0001%. Furthermore, to investigate the antioxidant potential, we checked the effect of ER and ER-CUB by DNA nicking assay, DDPH assay and Phosphomolybdate assay, and results showed significant improvement in antioxidant potential for ER-CUB than ER. Similarly, ER-CUB showed enhanced anticancer activity with a marked reduction in IC50 value than ER in MTT assay. These results suggested that ER-CUB produced notable escalation in antioxidant potential and enhanced anticancer activity than ER.

Anticancer potential of Nymphaea nouchali Brum flowers against Ehrlich ascites carcinoma cell lines.

Nymphaea nouchali Brum is exotic and medicinal plant in India. The main of this study is to evaluate the anticancer properties of Nymphaea nouchali Brum flowers against Ehrlich ascites carcinoma (EAC)-induced Swiss albino mice. The anticancer properties of Nymphaea nouchali Brum dry and fresh methanol extracts was investigated using EAC in Swiss albino mice. After inoculation of EAC cells into mice, treatment with NNDM flower extract (200 and 400 mg/kg) and standard drug 5-Fluorouracil (20 mg/kg) was continued for 9 days. The evaluation of the effect of drug response was made by the study of tumor growth response including increase in lifespan, the study of hematological parameters, biochemical estimations, and antioxidant assay of liver tissue compared to EAC control. The viability of cancer cell lines (such as HeLa, MCF-7, and MDA-MB 231 cells) was evaluated by 3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide (MTT) assay. Therefore, from the results of the present study, it can be concluded that NNDM exhibited significant antitumor activity against EAC in Swiss albino mice. The effect of NNDM on viability of cancer cell lines (such as HeLa, MCF-7, and MDA-MB 231 cells) was evaluated by MTT assay, apoptosis in HeLa cell lines was evaluated by DNA laddering assay, HeLa cells treated with NNDM exhibited a characteristic "ladder" pattern after separation of the fragments by agarose gel electrophoresis and subsequent visualization, by ethidium bromide staining. NNDM exhibited a significant effect on cell viability. Based on results, it was concluded that NNDM exhibited cytotoxic effect on cancer cells and, from DNA laddering assay, it can be concluded that NNDM-induced apoptosis in EAC cells.

In-vivo Anticancer Activity of Root and Leaf extract of Jurinea dolomiaea Boiss (Asteraceae) against Ehrlichs Ascites Carcinoma (EAC) Cell Line

Cancer is a type of disease of uncontrolled growth cells. The currently available treatments are radiotherapy, chemotherapy, hormone therapy and surgery, in which all of them have side effects. Due to the adverse side effects, it is challenging to develop new drug for cancer treatment. Hence, the scientists are trying to seek the compounds from natural sources to treat cancer. Therefore, in this present investigation, root and leaf extracts of Jurinea dolomiaea Boiss has subjected to evaluate its anti-proliferative effect along with molecular signaling of apoptosis in Ehrlich ascites carcinoma (EAC) cell line. Jurinea dolomiaea root and leaf extracts exhibit a considerable scavenging activity in comparison to a standard antioxidant BHT. Moreover, root and leaf extracts were able to agglutinate 2% RBC of goat blood at minimum 12.5 g/mL and 50.0 g/mL concentration respectively. Cytotoxic activity was also found in root and leaf extract. In haemocytometic observation, the root and leaf extract exhibit about 62.54±2.41% and 53.96±2.34% cell growth inhibition respectively where as standard anticancer drug Bleomycin showed 79.43±1.92% growth inhibition. Morphological change under fluorescence microscope showed nuclear condensation and fragmentation which are the sign of apoptosis. Therefore, current results depict root extract of Jurinea dolomiaea Boiss have anti-proliferative activity against EAC cell line and can be a good source of anticancer agents to treat cancer.

Design, Cytotoxicity, and Tumor Targeted Drug Delivery of 5Fluorouracil Encapsulated in pH-Sensitive Co-polymers GG-g-P (HEMA) Conjugate Riboflavin Thin-Film

The study finds the design, cytotoxicity, and tumor-targeted drug delivery of 5Fluorouracil encapsulated in pH-sensitive guar gum grafted polymer. Cancer targeting 5FU loaded GG grafted p(HEMA) conjugated riboflavin thin-film (GG-g-P(HEMA)-RF) was successfully fabricated from guar gum, 2-hydroxy ethyl methacrylate, and riboflavin targeting agents using N, N-methylene bis acrylamide as a crosslinking agent in the presence of tetramethylethylenediamminne (TEMED) initiator Ammonium persulfate act as a catalyst. FT-IR and XRD spectroscopy techniques were used to analyze the structural features of the GG-g-P(HEMA)-RF. The results of SEM revealed that the carrier is of uniform rod shape, with a low porosity index and outstanding performance in phrases of 5FU encapsulation and extended-release ability. Targeted drug delivery strategies have received special attention from the scientific world due to advantages such as more effective therapy and reduction of side effects. Cytotoxicity effects of 5FU loaded GG-g-P(HEMA)-RF against Ehrlich Ascites Carcinoma (EAC) cells in vitro were investigated at different concentrations (0, 25, 50, 100, and 150 μg/mL) using trypan blue exclusion assay. The MTT cytotoxic assay investigated cell viability against EAC experimental models and implied the excellent biocompatibility of the carrier. The results revealed the anti-proliferative effect along with molecular signaling of apoptosis and generated reactive oxygen species (ROS) in Ehrlich Ascites Carcinoma cell lines. The morphological changes of apoptosis were evident in EAC cells and were observed using optical microscopy after staining. DPPH free radical scavenging assay was carried out to determine the radical scavenging activity of the 5FU loaded and unloaded GG-g-P(HEMA)-RF. The 5FU loaded GG-g-P(HEMA)-RF with DNA interaction was examined by electronic and spectroscopic fluorescence methods.

Network pharmacology and in vitro testing of Theobroma cacao extract's antioxidative activity and its effects on cancer cell survival.

Theobroma cacao L. is a commercially important food/beverage and is used as traditional medicine worldwide against a variety of ailments. In the present study, computational biology approaches were implemented to elucidate the possible role of cocoa in cancer therapy. Bioactives of cocoa were retrieved from the PubChem database and queried for targets involved in cancer pathogenesis using BindingDB (similarity index ≥0.7). Later, the protein-protein interactions network was investigated using STRING and compound-protein via Cytoscape. In addition, intermolecular interactions were investigated via molecular docking. Also, the stability of the representative complex Hirsutrin-epidermal growth factor receptor (EGFR) complex was explored using molecular dynamics simulations. Crude extract metabolite profile was carried out by LC-MS. Further, anti-oxidant and cytotoxicity studies were performed in Chinese hamster ovary (normal) and Ehrlich ascites carcinoma (cancer) cell lines. Herein, the gene set enrichment and network analysis revealed 34 bioactives in cocoa targeting 50 proteins regulating 21 pathways involved in cancer and oxidative stress in humans. EGFR scored the highest edge count amongst 50 targets modulating 21 key pathways. Hence, it was selected as a promising anticancer target in this study. Structural refinement of EGFR was performed via all-atom molecular dynamics simulations in explicit solvent. A complex EGFR-Hirsutrin showed the least binding energy (-7.2 kcal/mol) and conserved non-bonded contacts with binding pocket residues. A stable complex formation of EGFR-Hirsutrin was observed during 100 ns MD simulation. In vitro studies corroborated antioxidant activity for cocoa extract and showed a significantly higher cytotoxic effect on cancer cells compared to normal cells. Our study virtually predicts anti-cancer activity for cocoa affected by hirsutrin inhibiting EGFR. Further wet-lab studies are needed to establish cocoa extract against cancer and oxidative stress.

Novel metal complexes with pyrano[3,2‐c]quinoline‐3‐carboxaldehyde: Synthesis, spectroscopic, molecular modeling, QSAR, antimicrobial, and antitumor studies

Reaction of 6‐ethyl‐4‐hydroxy‐2,5‐dioxo‐5,6‐dihydro‐2H‐pyrano[3,2‐c]quinoline‐3‐carboxaldehyde (HL) with some metal ions, namely, manganese (II), cobalt (II), nickel (II), zinc (II), cadmium (II), chromium (III), iron (III), cerium (III), oxovanadium (IV), and dioxouranium (VI), yielded a new series of metal complexes; with the general formula, [MHnLAm(H2O)x]Xy·zH2O, n = 0–1, A = NO3− or OAc−, m = 0–2, X = NO3− or SO42−, y = 0–1, and z = 0–3. The metal complexes were characterized by elemental analysis, molar conductance, magnetic moment, thermal analysis, and spectroscopic studies. The HL ligand coordinated with metal ions as monobasic or neutral bidentate via OO donor sites of aldehyde –O and phenolic –OH producing metal complexes with tetrahedral, octahedral, and pentagonal bipyramidal geometries. On the bases of PM3 level, molecular orbital calculations were performed for metal complexes using HyperChem 7.52 program, and the results were correlated with the experimental data. The biological activity of chelating agent and its metal complexes was screened towards Staphylococcus aureus and Bacillus subtilis as Gram‐positive bacteria; Salmonella typhimurium and Escherichia coli as Gram‐negative bacteria, as well as Candida albicans (yeast) and Aspergillus fumigatus (fungus). The antitumor activity of the HL ligand and its metal complexes was tested against Ehrlich Ascites Carcinoma cell line (EAC), which revealed promising IC50 values, comparable with that of cisplatin. Additional QSAR models were developed to predict the biodistribution of a smaller set of metal complexes and the calculated data correlated with antitumor results.

Extracts of Tagetes erecta exhibit potential cytotoxic and antitumor activity that could be employed as a promising therapeutic agent against cancer: A study involving in vitro and in vivo approach

Background and purposeGlobally, the burden of cancer is increasing consistently. Modern cancer therapies include lots of toxicity in the non-targeted organs reducing the life expectancy of the patients. Therefore, the development of safer alternative medicines with less toxicity and high efficacy is of immense importance. The present study was designed to evaluate the anticancer activity of a medicinal plant, “Tagetes erecta L.” (TE), in established cancer cell lines in vitro and in animal models in vivo. MethodsGC–MS analysis was performed to reveal the bioactive compounds present in the leaves of TE. To evaluate the antitumor potential of aqueous extract of TE (AETE), EAC (Ehrlich ascites carcinoma) induced solid tumor model was prepared in Swiss albino mice. The effect of AETE on body weight (BW), tumor weight (TW), and tumor volume (TV) was assessed in control and tumor-bearing animals. Further, the survival of the experimental animals was also monitored to assess the effect of AETE on life span. To determine the cytotoxicity induced by AETE, trypan blue dye exclusion assay, MTT assay, and LDH release assay was performed in EAC and HEp-2 cell lines by in vitro methods. Further, cell cycle assay and apoptosis assay was employed to ascertain the AETE-induced cytotoxicity is due to apoptosis or not. In addition, we have done a mitochondrial membrane potential assay using a flow cytometer to understand the mechanism of apoptosis. ResultsGC–MS analysis revealed the presence of hexadecanoic acid, Linolenic acid, Quinic acid, 2,3- dihydro benzofuran (Coumaran), and β-stigmasterol as major bioactive compounds in TE leaves. Results in animal studies showed that AETE treatment potentially reduced the TW and TV and increased the life span in EAC-induced tumor-bearing animals. Side effect analysis was also done in normal Swiss albino mice that confirmed the lack of toxicity of AETE. Studies in cancer cell lines indicated dose and time-dependent cytotoxicity in HEp-2 and EAC cells. Flow cytometric analysis established significant induction of apoptosis in EAC cells without arresting the cell cycle. In addition, AETE treatment led to a significant increase in cells with depolarised mitochondrial membrane potential. ConclusionThe present study indicated that AETE potentially inhibits tumor progression without disturbing normal body physiology. Thus, we conclude that AETE can be used as a potential therapeutic agent against cancer.

Deciphering the molecular pathways of apoptosis using purified fractions from leaf extract of Basella alba through studying the regulation of apoptosis related genes.

Apoptosis plays a pivotal role in the exclusion of abnormal cells without any ruin of surrounding healthy cells. Generally, it occurs through an orderly and autonomously process which is controlled by proper function of various genes. Therefore, the current experiments detect the expression level/pattern of those genes to confirm the involvement of extrinsic and intrinsic pathway using Basella alba leaf (BAL). Several fractions after gel filtration chromatography of BAL extract have been pooled to evaluates its apoptosis induction potentiality on Ehrlich's Ascites Carcinoma (EAC) cells through conducting a number of bio-assays such as cell growth inhibition assay, fluorescence and optical microscopy, DNA fragmentation assay and gene expression analysis etc. The pooled fractions of BAL showed 12-56% inhibitory effect on EAC cell line at the concentration range of 25-400μg/ml that was determined by MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay. They also exhibited excellent cell growth inhibition at in vivo and in vitro condition when treated with 10, 20 and 40mg/kg day. After administration of six consequent days, significant morphological features of apoptosis were observed in EAC cells under both fluorescence and optical microscope which was further supported by DNA fragmentation assay. The polymerase chain reaction amplification of bax, bcl-2(B-cell lymphoma 2), p53, tumor necrosis factor-α, Fas, NF-kβ(Nuclear factor-Kappa-B), PARP-1(Poly (ADP-ribose) polymerase), Cyt-c cas-8, cas-9 and cas-3 revealed that the experimental sample able to induce apoptosis in both extrinsic and intrinsic pathways through altering the gene expression. The current findings suggest that sample from BAL occupy wonderful competence to induce cell apoptosis and become an ideal resource for cancer treatment.

Antitumour activity of Annona muricata L. leaf methanol extracts against Ehrlich Ascites Carcinoma and Dalton’s Lymphoma Ascites mediated tumours in Swiss albino mice

ABSTRACT The use of plants as a source of sedative or treatment for cancer is reasonably widespread worldwide. Annona muricata Linn exhibits a vast array of medicinal and ethno-pharmaceutical benefits, attributed by different plant parts. The activity of this plant is regarded to the bio-production of secondary metabolites like alkaloids, phenols, flavonoids, and most unique group of compounds, namely, annonaceous acetogenins. Whilst this plant is gaining popularity as an anticancer treating plant, this study was undertaken to verify the plausible anticancer effect of leaf methanol extracts of A. muricata (LEAM). Acute toxicity study was carried to obtain safe dose in mice models using haematological, biochemical, and histological evaluations in Swiss albino mice. In-vitro cytotoxicity towards Dalton’s Lymphoma Ascites (DLA) and Ehrlich Ascites Carcinoma (EAC) cell lines were determined by trypan blue exclusion method. In-vivo antitumour activity of LEAM (100, 200, and 500mg/kg b.wt.) was evaluated using DLA induced solid carcinoma and EAC induced ascites carcinoma models and its comparison with standard drug Cisplatin. Acute toxicity studies did not exhibit significant variations in treated mice suggesting diminutive side effects of LEAM. Statistical analysis revealed the IC50 values for DLA and EAC cell lines as 85.56 ± 5.28 and 68.07 ± 7.39 µg/mL, respectively, indicating better cytotoxic activity against EAC than DLA cells. LEAM decreased the tumour burden in dose-dependent manner. In comparison, with different concentrations tested, treatment with LEAM (200 mg/kg b.wt. and 500 mg/kg b.wt.) significantly reduced the solid tumour volume development by 58.11% and 65.70%, respectively. While lifespan was prolonged up to 51.43% in 500 mg/kg b.wt. LEAM treated ascites tumour-induced mice. This study thus indicates that LEAM possesses potent cytotoxic and antineoplastic activity and calls for more methodical safety assessments and other end-points of anti-tumourigenesis. Abbreviations: LEAM: Leaf methanol extract of Annona muricata; DLA: Dalton’s Lymphoma Ascites; EAC: Ehrlich Ascites Carcinoma; IC50 : Half maximal inhibitory concentration; CPCSEA: Committee for the Purpose of Control Supervision of Experiments on Animal; IAEC: Institutional Animal Ethics Committee; ARRIVE: Animal Research: Reporting In-vivo Experiments; DMSO: Dimethyl sulphoxide; LD50 : Lethal Dose, 50%; SD: Standard Deviation; Hb: Haemoglobin; RBC: Red blood cells; WBC: White blood cells; HCT: Hematocrit; MCV: Mean cell volume; MCH: Mean cell haemoglobin; MCHC: Mean cell haemoglobin concentration; SALP: Serum alkaline phosphatase; SGPT: Serum glutamic pyruvic transaminase; SGOT: Serum glutamic oxaloacetic transaminase; ATP: Adenosine triphosphate; EGFR: Epidermal Growth Factor Receptor

Antitumor activity of Albizia lebbeck L. against Ehrlich ascites carcinoma in vivo and HeLa and A549 cell lines in vitro.

The aim of the present study was to explore the antitumor activity of the ethanolic extract of Albizia lebbeck L. pods against Ehrlich ascites carcinoma (EAC) in Swiss albino mice and its cytotoxic effect against HeLa and A549 cell lines in vitro. Antitumor activity of ethanolic extract of A. lebbeck L. (ALEE) pods was evaluated in Swiss albino mice against EAC cell lines at the doses of 200 and 400 mg/kg body weight which were given by intraperitoneal route of administration and was compared with 5-fluorouracil (5-FU), the reference standard. The extract and 5-FU were administered for 14 consecutive days. After 24 h of the last dose and 18 h of fasting, the mice were sacrificed and the antitumor effect of ALEE was assessed by evaluating tumor volume, viable and nonviable tumor cell count, increase in life span, and hematological parameters of EAC-bearing hosts.In vitro cytotoxicity has been assessed using (2,3-bis[2-Methoxy-4-nitro-5sulfophenyl]-2H-tetrazolium-5-carboxyanilide inner salt assay method and was compared with cisplatin, the reference standard. ALEE showed direct cytotoxicity on EAC cells in a dose-dependent manner. ALEE exhibited a significant (P < 0.001) decrease in the body weight, tumor volume, viable cell count, tumor weight, and elevated the life span of EAC tumor-bearing mice. Hematological profile such as red blood cell, hemoglobin, white blood cell, and platelet count was reverted to the normal level in ALEE-treated mice. The results showed that the ethanolic extract of A. lebbeck L. has a powerful antitumor activity because it was effective in significantly inhibiting the tumor growth in both in vivo and in vitro cancer cell lines.

Binary and ternary copper(II) complexes with 6-ethyl-4-hydroxy-2,5-dioxo-5,6-dihydro-2H-pyrano[3,2-c]quinoline-3-carboxaldehyde: Synthesis, spectral, thermal, molecular modeling, antimicrobial and antitumor studies

6-Ethyl-4-hydroxy-2,5-dioxo-5,6-dihydro-2H-pyrano[3,2-c]quinoline-3-carboxaldehyde (HL) was synthesized as a ligand and subject to chelate with Cu(II) ion of different anions (AcO–, NO3–, SO42–ClO4–, Cl– and Br–) in presence and absence of auxiliary ligands (L′); N,O-donor; or N,N-donor such as 8-hydroxyquinoline, 1,10-phenanthroline and 2,2′-bipyridyl. The obtained results revealed that the ligand behaves as a neutral/monoanionic bidentate, forming chelates with molar ratio 1:1, (M:L). The metal complexes were fully characterized by analytical and spectral techniques in addition to thermal, magnetic susceptibility and conductivity measurements. The metal complexes displayed square planar and octahedral geometrical arrangements depending on the nature of the anion. The ligand and its complexes were screened for their antimicrobial activity against Gram–positive bacteria which are Staphylococcus aureus and Bacillus subtilis, Gram–negative bacteria which are E. coli and S. typhimurium, yeast (Candida albicans) and fungus (Aspergillus fumigatus). The antitumor activity of the HL ligand and its Cu(II) complexes were examined against Ehrlich Ascites Carcinoma cell line (EAC) from ascetic fluid of the female Swiss albino mice. To explore the most probable structure and the nature of bonding of HL ligand to metal ions; semi-emperical (PM3) calculations were achieved in gas phase. All theoretically possible structural data of the free ligand (HL) and its complexes have been correlated with the experimental data to explore the most probable structure.

Synthesis of Ag/Cu and Cu/Zn bimetallic nanoparticles using toddy palm: Investigations of their antitumor, antioxidant and antibacterial activities

Abstract In the current study, green synthesis of bimetallic Ag/Cu and Cu/Zn bimetallic nanoparticles were carried out using toddy and were characterized. The formed Ag/Cu bimetallic nanoparticles were brown in colour while the formed Cu/Zn nanoparticles were green. Simultaneous synthesis of bimetallic nanoparticles in a single pot was investigated using toddy and the formed nanoparticles were evaluated for their antitumor and antibacterial activities. The nanoparticles were investigated for their antibacterial activity against Alcaligenes faecalis, Staphylococcus aureus, Citrobacter freundii, Klebsiella pneumoniae and Clostridium perfringens while the antitumor activity was done against Nasopharyngeal cancer (KB) cells and Ehrlich ascites carcinoma (EAC) cell lines. This is the first report on the green synthesis of these bimetallic nanoparticles using Toddy palm. The significance of the results in the light of existing literature is discussed in the present study.

Anticancer Potential of Michelia champaca Linn. Bark Against Ehrlich Ascites Carcinoma (EAC) Cells in Swiss Albino Mice

Background: Adverse side effects of currently available therapies against cancer, leads scientists to find effective compounds from natural sources. Objective: In the present study, stem-bark of Mycelia champaca is subjected to evaluate its antiproliferative effect against Ehrlich Ascites Carcinoma (EAC) cells. To date, the anti-proliferative effects of M. champaca bark extract against EAC cell line has not been reported elsewhere. Therefore, we intended to investigate the anti-proliferative potential of M. champaca bark extract against EAC cells in vivo. Methods: In vivo anticancer activity was evaluated against EAC cells bearing Swiss albino mice by monitoring parameters such as tumor cell proliferation, tumor weight measurement, and survival time, etc. The mechanism of EAC killing was examined by observation of cell morphology and analysis the expression of certain cancer-related genes. In vitro antioxidant potentiality was determined in terms of several common antioxidant assays. In addition, total phenolic and flavonoids contents were measured to ensure the presence of phytochemicals. Results: M. champaca bark extract showed strong antioxidant activities which were found to be strongly correlated (P&lt;0.001) with phenolics and flavonoids contents. Furthermore, it was found that bark extract decreased tumor cell proliferation (77.46%; P&lt;0.01), tumor weight (42.13%; P&lt;0.001) and increased life span of tumor-bearing mice (71.97%; P&lt;0.01) at the dose of 250mg/kg (intraperitoneal; i.p.). M. champaca bark also altered the depleted hematological parameters such as red blood cell, white blood cell, hemoglobin (Hb%) towards normal in tumor bearing mice. In addition, upregulation of p53, Bax and downregulation of Bcl-2 followed by treatment indicated M. champaca bark could induce apoptosis of EAC cells. Conclusion: These results indicated that MEMCB possesses significant cytotoxic activities against EAC cells and has a strong in vitro antioxidant capacity. Therefore, the bark of M. champaca could be considered as a potential resource of anti-cancer agents, which might be used to formulate effective anticancer drugs.

Impact of graphene oxide nano sheets loaded with chemotherapeutic drug on tumor cells

Graphene oxide (GO) nanosheet is a drug delivery system due to its structural properties, which can be augmented in presence of folic acid (FA). This study aimed to compare the efficacy of GO as a passive (GO/DOX) and active (GO/FA/DOX) forms for delivering doxorubicin (DOX). These two forms of conjugates were characterized before and after loading of DOX to confirm the conjugation as well as their properties including size and thermal stability. Using Ehrlich ascites carcinoma (EAC) cell line, the antitumor effect was evaluated by MTT assay in vitro and cell count; tumor cell cycle and apoptosis were evaluated by flow cytometry in vivo. The results showed that the loading percentages of DOX onto GO (GO/DOX) and GO/FA/DOX were 91% and 83%, respectively. TEM, FT-IR, and TGA confirmed the nano size, physical conjugation by shifted groups, and thermal stability. In vitro, the conjugates induced similar decrease of EAC cell viability, but still lower than those of free DOX. Treatment of EAC-bearing mice with GO/DOX or GO/FA/DOX forms induced significant decreases of the total numbers of EAC cells by 79% and 97%, respectively, as compared with free DOX (97%). DOX, GO/DOX, and GO/FA/DOX induced cell cycle arrest at G0, G1, and S phase, respectively. These conjugates also induced significant apoptosis with different profiles on viable, early, and late apoptotic EAC cells. In conclusion, loading DOX on GO nanosheet activated with FA can induce antitumor effect similar to those of free DOX but with different mechanisms.

Study of the Radiosensitizing and Radioprotective Efficacy of Bromelain (a Pineapple Extract): In Vitro and In Vivo

This study hypothesizes that, bromelain (BL) acts as radiosensitizer of tumor cells and that it protects normal cells from radiation effects. In vitro and in vivo studies have been carried out to prove that assumption. In vitro MTT cell proliferation assay has shown that the irradiated Ehrlich ascites carcinoma (EAC) cell line could be sensitized by BL pretreatment. In vivo: animals were randomly divided into 5 groups, Group 1: control (PBS i.p for 10 days), Group 2: Ehrlich solid tumor (EST) bearing mice, Group 3: EST + γ-radiation (fractionated dose, 1 Gy × 5), Group 4: EST + BL (6 mg/kg, i.p), daily for 10 days, Group 5: EST + BL for 10 days followed by γ-irradiation (1 Gy × 5). The size and weight of tumors in gamma-irradiated EST bearing mice treated with BL decreased significantly with a significant amelioration in the histopathological examination. Besides, BL mitigated the effect of γ-irradiation on the liver relative gene expression of poly ADP ribose polymerase-1 (PARP1), nuclear factor kappa activated B cells (NF-κB), and peroxisome proliferator-activated receptor α (PPAR-α), and it restored liver function via amelioration of paraoxonase1 (PON1) activity, reactive oxygen species (ROS) content, lipid peroxidation (LPO) and serum aspartate transaminase (AST), alanine transaminase (ALT), and albumin (ALB). It is concluded that BL can be considered as a radio-sensitizer and radio-protector, suggesting a possible role in reducing radiation exposure dose during radiotherapy.

IN VITRO CYTOTOXICITY ACTIVITY OF METHANOLIC LEAF AND FRUIT EXTRACT OF ZANTHOXYLUM OVALIFOLIUM WIGHT AGAINST DALTON’S LYMPHOMA ASCITES AND EHRLICH ASCITES CARCINOMA CANCER CELL LINES

Objectives: The objective of the present study, the methanolic leaf and fruit extraction of Zanthoxylum ovalifolium, was examined for in vitro cytotoxicity using trypan blue dye exclusion technique.&#x0D; Methodology: In vitro cytotoxicity activity of methanolic leaf and fruit extracts of Z. ovalifolium. Against Dalton’s lymphoma ascites (DLA) and Ehrlich ascites carcinoma (EAC) cell lines evaluated using trypan blue exclusion method. Non-viable cell absorbs blue color of trypan blue while viable cell does not absorb the dye. The percentage of total number of viable and non-viable cells is calculated using % viability=(live cell count/total cell count)×100.&#x0D; Results: Cytotoxicity activity of methanolic leaf and fruit extract against chosen tumor cell line at different concentrations of 10, 20, 50,100, and 200 μg/ml, respectively. The result confirmed that the fruit extract at 200 showed less toxic effect against DLA and EAC cell line showed 72% and 75% of inhibition growth of cell line and the most potent 80% and 82% of cell death were found in leaf extract against the chosen tumor cell line. The present study indicates that both leaf and fruit extract of Z. ovalifolium were appreciable antitumor activity against DLA and EAC cell lines may be due to the presence of phytochemicals such as flavonoids and alkaloids present in the plant.&#x0D; Conclusion: Zanthoxylum ovalifolium wight fruit and leaf methanolic extracts showed satisfying result of cytotoxicity activity against DLA and EAC cell line. Hence, Z.ovalifolium could be suggested as an important source of anticancer agent for pharmacological industries.

GREEN SYNTHESIS OF PYRAZOLO [3,4]-PYRIMIDINE-THIONES USING IONIC LIQUID 2-METHYL-IMIDAZOLIUM-OXALATE AS POTENT EHRLICH ASCITES CARCINOMA RECEPTOR ANTAGONISTS

Objective: Pyrazolopyrimidines are heterocyclic molecules containing nitrogen as the main composition, and hence, they exhibit pharmacological efficacy. They are analogs of purines so that possessing wide applications in the field of medicinal chemistry. The main objective of this study is to synthesize different derivatives of pyrazole-pyrimidine classes by adopting simple methodology as well as by employing green chemistry. The purpose of the synthesis of these molecules is to study the antitumor activity against Ehrlich ascites carcinoma (EAC) cell lines.&#x0D; Methods: After literature studies, it makes us to involve in the research of synthetic organic chemistry, especially to synthesize new compounds of pyrazolopyrimidines. We are reported solvent-free synthesis of pyrazolo [3,4-d]-pyrimidine-thiones through ethyl acetoacetate, hydrazine hydrate, thiourea, and different benzaldehydes. An ionic liquid 2-methyl-imidazolium-oxalate catalyzed the reactions under ultrasonication bath. Both conventional and ultrasonic methods were employed and comparison studies have been made. It was found that ultrasonic method completed the reaction quicker than the conventional method. All the synthesized compounds were confirmed their structures by 1HNMR, Fourier transform infrared, 13C-NMR, and elemental analysis spectra. The compounds were tested for in vitro anticancer activity against EAC cell lines. Most compounds revealed significant anticancer activity relative to doxorubicin as a positive control with inhibitory concentration (IC50) values.&#x0D; Results: Ultrasonication method is a simple method under which all the reactions were completed at faster time (&lt;7 min) compared to the convention method. Among eight molecules, 8a and 8d completed the reactions at a faster rate. We reported IC50 values of all the molecules, in which 8e and 8g were exhibited excellent potency against EAC cell lines at different concentrations .&#x0D; Conclusions: Ultrasonication method is an excellent method for the organic synthesis. We are herein reported that under this method, all the reactions are completed within 7 min. Hence, it is superior method than the conventional method. All synthesized molecules have shown good inhibitor potency against EAC cell lines. Among them, two molecules 8e and 8g have shown excellent inhibitor potency.