scholarly journals Synthesis and Evaluation of the Antitumor Activity of (E)-3-((2-(5-(4-chlorophenyl) thiazol-2-yl) hydrazono) methyl) benzene-1,2-diol “In vitro and In vivo Study”

2019 ◽  
pp. 1-16
Author(s):  
Faten Z. Mohamed ◽  
Mohamed S. Elghreeb ◽  
Moustafa S. Abdelhamid ◽  
Hazem A. Elbaz
Keyword(s):  
Antitumor Activity ◽  
Life Span ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cytotoxic Effect ◽  
Ehrlich Ascites Carcinoma ◽  
Ehrlich Ascites ◽  
Liver And Kidney

Background: Thiazole nucleus–containing compounds have an antitumor efficiency against various types of cancer. Purpose: The present study was designed to determine the cytotoxic effect of newly synthesized thiazole derivative (TD1) on human cancer cell lines, in addition to evaluate its antitumor activity against Ehrlich ascites carcinoma (EAC) in mice. Materials and Methods: TD1 was synthesized and investigated for its cytotoxic effect on HCT116 (colon cancer), HepG2 (liver cancer), PC3 (prostate cancer) and MCF7 (breast cancer). The effect of TD1 on cell viability, tumor volume, and percent of increase in life span (% ILS) in Ehrlich–bearing mice was studied. Hematological parameters, liver and kidney function tests were evaluated. The activity of superoxide dismutase (SOD) and catalase (CAT), as well as malondialdehyde (MDA) and reduced glutathione levels were determined in liver and kidney tissues. The expression of P53 in EAC was analyzed by flow cytometry. Results: TD1 demonstrated an inhibitory effect on both cancer cell lines in vitro and Ehrlich ascites cells in vivo. TD1 increased in life span of Ehrlich–bearing mice compared to control. Cell cycle and flow cytometric analysis revealed that TD1 directed Ehrlich cells toward apoptosis by increasing of P53 expression. Conclusion: It was concluded that TD1 have a potent antitumor activity against Ehrlich ascites carcinoma in mice beside a cytotoxic effect on MCF-7, PC3, HepG2 and HCT-116.

scholarly journals Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1838
Author(s):  
Naglaa M. Ahmed ◽  
Mahmoud M. Youns ◽  
Moustafa K. Soltan ◽  
Ahmed M. Said
Keyword(s):  
Molecular Modeling ◽  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Normal Cells

Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Compounds 1–4 showed broad spectrum cytotoxic activity against all these cancer cell lines compared to normal cells. Compound 4g showed potent antiproliferative activity against these cell lines (IC50 = 5.1, 5.02, and 6.6 μM, respectively) comparable to the standard treatment (5-FU and erlotinib). In addition, the most promising group of compounds was further evaluated for their in vivo antitumor efficacy against EAC tumor bearing mice. Notably, compound 4g showed the most potent in vivo antitumor activity. The most active compounds were evaluated for their EGFR inhibitory (range 53–79 %) activity. Compound 4g was found to be the most active compound against EGFR (IC50 = 0.25 µM) showing equipotency as the reference treatment (erlotinib). Molecular modeling study was performed on compound 4g revealed a proper binding of this compound inside the EGFR active site comparable to erlotinib. The data suggest that compound 4g could be used as a potential anticancer agent.

scholarly journals In vitro and in vivo evaluation of antitumor activity of methanolic extract of Argyreia nervosa leaves on Ehrlich ascites carcinoma

2015 ◽  
Vol 10 (2) ◽  
pp. 399
Author(s):  
Bhawna Sharma ◽  
Isha Dhamija ◽  
Sandeep Kumar ◽  
Hema Chaudhary
Keyword(s):  
Antitumor Activity ◽  
Solid Tumor ◽  
Methanolic Extract ◽  
Ehrlich Ascites Carcinoma ◽  
Ehrlich Ascites ◽  
Wide Range ◽  
Antioxidant Parameters ◽  
Argyreia Nervosa

<p>The herb of importance like <em>Argyreia nervosa</em> has shown wide range of pharmacological activities. Its methanolic extract of <em>A. nervosa</em> has been explored against Ehrlich ascites carcinoma (EAC) induced liquid and solid tumor in mice. Liquid and solid tumors were induced by intraperitoneal and subcutaneous transplantation of EAC cells in Balb/C mice. Significant and dose dependant results are observed when the mice are sacrificed on 15<sup>th</sup> day for estimation of tumor proliferation, hematological, biochemical and hepatic antioxidant parameters. Mean survival time (days) was increased to 36.5 from 20.5 extract treated mice. The extract also showed a decrease (p&lt;0.001) in body weight and percentage reduction in tumor volume respectively when it was evaluated in solid tumor induced mice for a period of 30 days.  From the result it was concluded that the extract has as a potent antitumor activity and that is comparable to 5-fluorouracil.</p><p> </p>

Evaluation of Cisplatin Combined with Ondansetron in Ehrlich Ascites Carcinoma in Vitro and in Vivo

2000 ◽  
Vol 86 (2) ◽  
pp. 153-156 ◽  
Author(s):  
Osama Ahmed Badary ◽  
Sahar Moustafa Sharaby ◽  
Sanaa Abd El-Baky Kenawy ◽  
Ezz El-Deen El-Denshary ◽  
Farid Mohamed Ahmed Hamada
Keyword(s):  
Antitumor Activity ◽  
Ehrlich Ascites Carcinoma ◽  
Host Tissue ◽  
Nausea And Vomiting ◽  
Single Treatment ◽  
Blood Cell Count ◽  
Ehrlich Ascites ◽  
Eac Cells

Aims and background Nausea and vomiting occur in the majority of patients receiving cisplatin (CDDP) chemotherapy. Ondansetron, a new 5-HT3 receptor antagonist, has been used effectively to control CDDP-induced nausea and vomiting. This study examined the potential of ondansetron to interfere with CDDP antitumor activity and toxicity in Ehrlich ascites carcinoma (EAC). Methods The influence of ondansetron on CDDP cytotoxicity was evaluated using EAC cells in culture. In addition, the influence of ondansetron pretreatment on CDDP-induced antitumor activity and host tissue toxicity was studied in EAC-bearing mice. Results Ondansetron (0.25 μM) enhanced CDDP (0–32 μM) cytotoxicity against EAC cells in vitro. In EAC-bearing mice ondansetron (0.2 mg/kg, ip) administered 1 h before CDDP (7 mg/kg, ip) did not modify the antitumor activity of CDDP. CDDP (7 mg/kg, ip) single treatment induced significant increases in blood urea nitrogen (2-fold) and serum creatinine (2.5-fold) and significant decreases in hematocrit (25%) and white blood cell count (39%) compared to saline treatment. Mice receiving ondansetron 1 h before CDDP showed no significant enhancement of CDDP-induced nephrotoxicity or myelosuppression compared to those pretreated with saline receiving the same dose of CDDP. Conclusions This study suggests that the use of ondansetron to control CDDP-induced nausea and vomiting does not affect CDDP antitumor efficacy.

scholarly journals Biochemical Studies of (5-P-chlorophenyl -2-benzo 5, 6-coumarin-3-yelthylidene aminothiazole) as Antitumor Agent

2019 ◽  
pp. 1-16
Author(s):  
Faten Z. Mohamed ◽  
Mohamed S. Elghreeb ◽  
Moustafa S. Abdelhamid ◽  
Hazem A. Elbaz
Keyword(s):  
Antitumor Activity ◽  
Cell Count ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
Biological Activities ◽  
Control Cell ◽  
P53 Expression ◽  
Thiazole Derivative ◽  
Ehrlich Ascites

Heterocyclic compounds have a large spectrum of biological activities including antitumor activity. The present study describes the cytotoxic effect of newly synthesized thiazole derivative (TD2) that can prove effective antitumor activity on both in vivo and in vitro studies. Objective: the essential objective of this research is to prove the cytotoxic effect of newly synthesized thiazole derivative (TD2) up on EAC bearing mice and many kinds of human cell lines. Materials and Methods: Antitumor activity of TD2 was examined on EAC in Swiss albino Mice at dose of 2.5 mg/kg. TD2 was injected for 10 following days after transplantation of tumor. After one day of last dose and 18 hours of fasting, 7 Mice were sacrificed and the remaining was kept to evaluate ILS %. Antitumor activity of TD2 was assessed by inspecting tumor volume, tumor weight, viable cell count and nonviable cell count, hematological, biochemical and antioxidant parameters of mice. Results: TD2 demonstrated an inhibitory effect on both cancer cell lines in vitro and Ehrlich ascites cells in vivo.TD2 increased in life span of Ehrlich–bearing mice compared to control. Cell cycle and flow cytometric analysis revealed that TD2 directed Ehrlich cells toward apoptosis by increasing of P53 expression. Conclusion: It was concluded that TD2 have a potent antitumor activity against Ehrlich ascites carcinoma in mice beside a cytotoxic effect on MCF-7, PC3, HepG2 and HCT-116.

scholarly journals Anticancer Potential of Aqueous Ethanol Seed Extract ofZiziphus mauritianaagainst Cancer Cell Lines and Ehrlich Ascites Carcinoma

2011 ◽  
Vol 2011 ◽  
pp. 1-11 ◽  
Author(s):  
Tulika Mishra ◽  
Madhu Khullar ◽  
Aruna Bhatia
Keyword(s):  
Cell Lines ◽  
Ehrlich Ascites Carcinoma ◽  
Seed Extract ◽  
Ziziphus Mauritiana ◽  
Dependent Manner ◽  
Swiss Albino Mice ◽  
Ehrlich Ascites ◽  
Albino Mice

Ziziphus mauritiana(Lamk.) is a fruit tree that has folkloric implications against many ailments and diseases. In the present study, anticancer potential of seed extract ofZiziphus mauritiana in vitroagainst different cell lines (HL-60, Molt-4, HeLa, and normal cell line HGF) by MTT assay as well asin vivoagainst Ehrich ascites carcinoma bearing Swiss albino mice was investigated. The extract was found to markedly inhibit the proliferation of HL-60 cells. Annexin and PI binding of treated HL-60 cells indicated apoptosis induction by extract in a dose-dependent manner. The cell cycle analysis revealed a prominent increase in sub Go population at concentration of 20 μg/ml and above. Agarose gel electrophoresis confirmed DNA fragmentation in HL-60 cells after 3 h incubation with extract. The extract also exhibited potent anticancer potentialin vivo. Treatment of Ehrlich ascites carcinoma bearing Swiss albino mice with varied doses (100–800 mg/kg b.wt.) of plant extract significantly reduced tumor volume and viable tumor cell count and improved haemoglobin content, RBC count, mean survival time, tumor inhibition, and percentage life span. The enhanced antioxidant status in extract-treated animals was evident from decline in levels of lipid peroxidation and increased levels of glutathione, catalase, and superoxide dismutase.

scholarly journals Biogenic silver nanoparticles induce apoptosis in Ehrlich ascites carcinoma

2020 ◽  
Vol 7 (11) ◽  
pp. 4100-4113
Author(s):  
Hamed A. Abosharaf ◽  
Mohammed Salah ◽  
Thoria Diab ◽  
Motonari Tsubaki ◽  
Tarek M. Mohamed
Keyword(s):  
Silver Nanoparticles ◽  
Mouse Model ◽  
Combined Treatment ◽  
Ehrlich Ascites Carcinoma ◽  
Ehrlich Ascites ◽  
Liver And Kidney ◽  
Mango Leaves ◽  
Eac Cells

Introduction: Plant-mediated synthesis of silver nanoparticles (AgNPs) is accounted as an ecofriendly process. The present study was conducted to estimate the potency of biogenic AgNPs against Ehrlich ascites carcinoma (EAC) cells in vitro and EAC-bearing mice in vivo. Methods: AgNPs were prepared using mango leaves extract and characterized by X-ray diffraction (XRD), scanning electron microscope (SEM), and transmission electron microscopy (TEM). Ehrlich ascites carcinoma (EAC) mouse model was established by intraperitoneal injection of 1 x 106 EAC cells. Biogenic AgNPs- alone or combined with Doxorubicin (DOX)- was administered intraperitoneally day by day for two weeks. Results: Biologically synthesized AgNPs showed a cytotoxic effect against cultured EAC cells but with less toxicity toward normal cells compared to DOX, which had strong cytotoxicity against both cells. Biogenic AgNPs alone or combined with DOX triggered the cytotoxicity against the EAC-bearing mouse model via decreasing body weight, tumor volume, and the number of viable tumor cells. The combined treatment (AgNPs-DOX) ameliorated the drastic effect induced by injection of EAC cells through improving liver and kidney functions compared to those treated with DOX alone. In addition, the combined treatment showed an elevation in the expression of Bax and caspase-3, and a reduction in the expression of Bcl-2 protein in the EAC cells. Furthermore, this combined treatment effectively arrested the cell cycle at the G0/G1 phase. Moreover, the combined treatment with AgNPs-DOX caused a significant reduction in the activity of ornithine decarboxylase (ODC). Conclusion: These findings suggest that biogenic AgNPs could be useful in developing a potent combination therapy against different types of cancers.

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