EVALUATION OF ANTICANCER ACTIVITY OF CUCUMIS CALLOSUS AGAINST EHRLICH’S ASCITES CARCINOMA BEARING MICE

Objective: Our previous research isolated Cucurbitacin B (CuB) and ebenone leucopentaacetate (ELP) from methanolic fruit extract of Cucumis callosus (MFCC). The fruits of C. callosus (Rottl.) Cogn. (Family: Cucurbitaceae) plant have been traditionally used for antioxidant, anti-inflammatory, and antidiabetic actions. The objective of this research was to evaluate in vitro and in vivo anticancer effect of MFCC on Ehrlich Ascites Carcinoma (EAC) cell lines.Methods: In vitro anticancer assay of MFCC and standard drug, 5-fluorouracil (5-FU) was evaluated using Trypan blue and 3-(4, 5-dimethylthiazol-yl)-2, 5-diphenyl tetrazolium bromide methods. In vivo anticancer activity of MFCC and 5-FU was also performed after 24h of EAC cells (2×106cells/ mouse) inoculation based on toxicity study for 9 consecutive days. The activity of the extract was assessed by the study of tumor volume, tumor weight, viable and non-viable cell count, hematological parameters, and biochemical estimations.Results: The MFCC showed the direct antitumor effect on EAC cells in a dose-dependent manner with an IG50 value of 0.61 mg/ml. Furthermore, MFCC (350 mg/kg) exhibited significant (p<0.01) decrease in tumor volume, tumor weight, and viable cell count of EAC-treated mice. Hematological profile, biochemical estimation assay significantly (p<0.01) reverted to normal level in MFCC, and 5-FU treated mice.Conclusion: The anticancer activity of fruits of C callosus is may be either due to the presence of CuB or/and ELP as phytoconstituent and the activity is comparable to standard drug 5-FU.

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EVALUATION OF ANTICANCER ACTIVITY OF PARKINSONIA ACULEATA LEAVES EXTRACT ON EHRLICH’S ASCITES CARCINOMA-INDUCED MICE.

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v11i1.22404 ◽

2018 ◽

Vol 11 (1) ◽

pp. 390

Author(s):

Prameela Rani A ◽

Agarjuna Babu E ◽

Prem Madhur S ◽

Ravi Chandra Sekhara Reddy D ◽

Phani Kumar K

Keyword(s):

Cell Count ◽

Anticancer Activity ◽

Tumor Volume ◽

Hematological Parameters ◽

Ethanolic Extract ◽

Viable Cell ◽

Ehrlich Ascites Carcinoma ◽

Parkinsonia Aculeata ◽

Tumor Weight ◽

Ehrlich Ascites

Objective: The objective of the study was to investigate the anticancer activity of the ethanolic extract of Parkinsonia aculeata (EEPA) leaves. Methods: Anticancer activity of P. aculeata (EEPA) of leaf extract was evaluated in Swiss albino mice against Ehrlich ascites carcinoma (EAC) cell line at the doses of 200 and 400 mg/kg body weight orally. The extracts were administered for 14 consecutive days. 24 h of the last dose and 18 h of fasting, the mice were sacrificed, and the anticancer effect of EEPA was assessed by evaluating tumor volume, viable and nonviable tumor cell count, tumor weight, hematological parameters, and biochemical parameters of EAC bearing mice.Results: P. aculeata extracts showed a significant decrease in (p<0.01) tumor volume, viable cell count, tumor weight, and elevated the life span of EAC bearing mice. Hematological profile such as red blood cell, hemoglobin count reverted to normal level in EEPA treated mice. The extracts significantly (p<0.05) decreased the levels of lipid peroxidation and significantly (p<0.05) increased the levels of reduced glutathione, superoxide dismutase and catalase.Conclusion: The results showed that the EEPA was effective in inhibiting the tumor growth in ascitic models and that is comparable to 5-fluorouracil.

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ANTI PROLIFERATIVE ACTIVITY OF CALAMUS ROTANG AS A SPOTLIGHT ON EHRLICH’S ASCITES CARCINOMA TREATED PERITONEAL AS WELL AS SOLID TUMOR MODEL

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2018v10i1.21449 ◽

2018 ◽

Vol 10 (1) ◽

pp. 85

Author(s):

Subeer Roy ◽

Diksha Kumari ◽

Mainak Chakraborty ◽

Pallab Kanti Haldar

Keyword(s):

Life Span ◽

Cell Count ◽

Anticancer Activity ◽

Solid Tumor ◽

Tumor Volume ◽

Hematological Parameters ◽

In Vitro Cytotoxicity ◽

Control Group

Objective: Methanol extract of Calamus rotang (MECR) root was appraised as a spotlight for the candidate of anticancer activity through the vehicle (Ehrlich Ascites Carcinoma) on Swiss albino mice.Methods: In vitro cytotoxicity assay has been accessed by trypan blue and MTT assay. In vivo anticancer activity was done using EAC cells (2 × 106) where in each groups mice were 6. After treatment with MECR at the lower dose of 200 and higher dose of 400 mg/kg respectively for 9 d, half of the mice of each group were sacrificed and the rest were kept to check prolongation of life span. The anticancer potential of MECR was evaluated by tumor volume, viable and nonviable tumor cell count, tumor weight, hematological parameters, biochemical estimations and Furthermore, tissue antioxidant parameters. Besides, solid tumor activity was also inspected.Results: In MECR treated groups (200 and 400 mg/kg) tumor volume, packed cell volume and viable cell count was significantly lessened as compared to that of the EAC control group. Life span, most reliable criteria for anticancer study, increased quite surprisingly by 50% and 100% in a dose dependant manner while compared to EAC control group. The hematological, biochemical and liver tissue antioxidant parameter are significantly (p<0.05) restored along with solid tumor case study (solid tumor volume) towards the normal level after treatment with MECR.Conclusion: From the above study it can be inferred that the MECR has impressive anticancer activity in dose dependent way.

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Antineoplastic Activities of MT81 and Its Structural Analogue in Ehrlich Ascites Carcinoma-Bearing Swiss Albino Mice

Oxidative Medicine and Cellular Longevity ◽

10.4161/oxim.3.1.10495 ◽

2010 ◽

Vol 3 (1) ◽

pp. 61-70 ◽

Cited By ~ 6

Author(s):

Sujata Maiti Choudhury ◽

Malaya Gupta ◽

Upal Kanti Majumder

Keyword(s):

Cell Count ◽

Tumor Volume ◽

Ehrlich Ascites Carcinoma ◽

Viable Tumor Cell ◽

Structural Analogue ◽

Mean Survival Time ◽

Ehrlich Ascites ◽

Eac Cells

Many fungal toxins exhibit in vitro and in vivo antineoplastic effects on various cancer cell types. Luteoskyrin, a hydroxyanthraquinone has been proved to be a potent inhibitor against Ehrlich ascites tumor cells. The comparative antitumor activity and antioxidant status of MT81 and its structural analogue [Acetic acid-MT81 (Aa-MT81)] having polyhydroxyanthraquinone structure were assessed against Ehrlich ascites carcinoma (EAC ) tumor in mice. The in vitro cytotoxicity was measured by the viability of EAC cells after direct treatment of the said compounds. In in vivo study, MT81 and its structural analogue were administered (i.p.) at the two different doses (5, 7 mg MT81; 8.93, 11.48 mg Aa-MT81/kg body weight) for 7 days after 24 hrs. of tumor inoculation. The activities were assessed using mean survival time (MST), increased life span (ILS), tumor volume, viable tumor cell count, peritoneal cell count, protein percentage and hematological parameters. Antioxidant status was determined by malondialdehyde (MDA) and reduced glutathione (GSH ) content, and by the activity of superoxide dismutase (SOD) and catalase (CA T). MT81 and its structural analogues increased the mean survival time, normal peritoneal cell count. They decreased the tumor volume, viable tumor cell count, hemoglobin percentage and packed cell volume. Differential counts of WBC, total counts of RBC & WBC that altered by EAC inoculation, were restored in a dose-dependent manner. Increased MDA and decreased GSH content and reduced activity of SOD, and catalase in EAC bearing mice were returned towards normal after the treatment of MT81 and its structural analogue. Being less toxic than parent toxin MT81, the structural analogue showed more prominent antineoplastic activities against EAC cells compared to MT81. At the same time, both compounds exhibit to some extent antioxidant potential for the EAC-bearing mice.

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EVALUATION OF ANTICANCER ACTIVITY OF PARKINSONIA ACULEATA LEAVES EXTRACT ON EHRLICH’S ASCITES CARCINOMA-INDUCED MICE.

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i1.22404 ◽

2018 ◽

Vol 11 (1) ◽

pp. 390

Author(s):

Prameela Rani A ◽

Agarjuna Babu E ◽

Prem Madhur S ◽

Ravi Chandra Sekhara Reddy D ◽

Phani Kumar K

Keyword(s):

Cell Count ◽

Anticancer Activity ◽

Tumor Volume ◽

Hematological Parameters ◽

Ethanolic Extract ◽

Viable Cell ◽

Ehrlich Ascites Carcinoma ◽

Parkinsonia Aculeata ◽

Tumor Weight ◽

Ehrlich Ascites

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Synthesis, In Silico and In Vivo Evaluation of Novel 1, 3, 4-Thiadiazole Analogues as Novel Anticancer Agents

Letters in Drug Design & Discovery ◽

10.2174/1570180816666190710145939 ◽

2020 ◽

Vol 17 (4) ◽

pp. 434-444 ◽

Cited By ~ 1

Author(s):

Swathi Krishna ◽

Byran Gowramma ◽

Manal Mohammed ◽

Rajagopal Kalirajan ◽

Lakshman Kaviarasan ◽

...

Keyword(s):

Vero Cell ◽

Anticancer Activity ◽

Cell Lines ◽

Binding Interaction ◽

Standard Drug ◽

Discovery Studio ◽

Vero Cell Lines ◽

Mcf 7

Background: 1,3,4-thiadiazole is a lead molécule which is versatile for a wide variety of biological activities and in continuation of our interest in establishing some novel heterocyclic compounds for antitumor activity. Objective: The objective of the study was to synthesize series of 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine derivative and evaluated for their possible in vitro and in vivo anticancer activity. Methods: The synthesis of 2-aminonaphthoxy-1,3,4-thiadiazole and 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine as intermediates were carried out by cyclization method. A mixture of thiosemicarbazide and naphthoxyacetic acid/piperonylic acid and phosphoryl chloride were subjected to cyclization with phosphorous oxychloride to obtain compound 3. Further compounds 1 and 3 were reacted with different aromatic aldehydes in methanol to form compounds 2a-e and 4a-e. The compounds 2a-e and 4a-e were characterized for the melting points, IR, Proton NMR and Mass spectra. The compounds were further evaluated for their anticancer activity. The docking study was performed using Discovery studio 4.1 (Accelrys) software against DNA-binding domain of STAT3. The compounds were analyzed for the ligand-protein binding interaction(s) by molecular docking into the active site of STAT3β using the CDOCKER protocol of Discovery studio (v4.1). Results: The title compounds were screened for in vitro anticancer on human breastadenocarcinoma cells (MCF-7 and Vero). Compounds 4c, 4d and 2d against MCF 7 and 4d against Vero cell lines were found to be the most active dérivatives with IC50 values of 1.03, 2.81 and 3.45 µg/ml against MCF 7 and 31.81 µg/ml against Vero cell lines, respectively. Conclusion: From the in vivo anticancer studies, it was concluded that the synthesized compounds 4c and 4d displayed anticancer activity comparable to the standard drug, while the rest of the compounds demonstrated mild potency for anticancer studies.

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In vivo Anticancer Activity on Ehrlich Ascites Carcinoma (EAC) Cells and in vitro Antimicrobial Activity of Psidium guajava Bark Extracts

Bangladesh Journal of Microbiology ◽

10.3329/bjm.v35i1.39808 ◽

2019 ◽

Vol 35 (1) ◽

pp. 79-81

Author(s):

Md Jakir Hossain ◽

Shashwata Biswas ◽

Mohammad Shahriar ◽

Sohidul Islam ◽

Chowdhury Rafiqul Ahsan

Keyword(s):

Antimicrobial Activity ◽

Anticancer Activity ◽

Methanol Extract ◽

Ehrlich Ascites Carcinoma ◽

Psidium Guajava ◽

Negative Control ◽

Ehrlich Ascites ◽

Eac Cells

This study was performed to evaluate the in vivo anticancer activity against ehrlich ascites carcinoma (EAC) cells and in vitro antimicrobial activity of Psidium guajava bark extracts. By soxhlet apparatus, the P. guajava bark extracts were obtained using four solvents (n-hexane, petroleum benzene, chloroform, and methanol) according to their increasing solubility. In case of in vivo anticancer activity of the sample extracts, mice were seeded with approximately 1x105 ehrlich ascites carcinoma (EAC) cells. After seven days of consecutive treatment, the negative and positive control groups (n=8 each group) showed an average EAC cell count of 2.4x108 and 1.8x108 respectively, and the experimental groups showed the cell count of 2.2x 108, 2.1x108, 1.9x108, and 1.41x108 when mice received h-hexane, petroleum benzene, chloroform, and methanol extract respectively. Experimental group that received methanol extract showed percent increase of life span (% ILS) of 33.3 when compared with the negative control. However, treatment in a cyclic manner of the mice showed % ILS of 52.15 for experimental group when compared negative control. In antimicrobial activity experiment, an intermediate zone of sensitivity of the crude methanol extract was found against Escherichia coli, Shigella flexneri, and Staphylococcus aureus when compared with amoxicillin. All these results indicated the anticancer activity and antimicrobial activity of the methanol extract of P. guajava barks on different experimental models. Bangladesh J Microbiol, Volume 35 Number 1 June 2018, pp 79-81

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EVALUATION OF IN VIVO ANTICANCER AND IMMUNOSTIMULATORY ACTIVITY OF FLOWERS OF MIMOSA PUDICA LINN. (FABACEAE)

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i7.18514 ◽

2017 ◽

Vol 10 (7) ◽

pp. 266 ◽

Cited By ~ 1

Author(s):

Debaprotim Dasgupta ◽

Suvakanta Dash

Keyword(s):

Anticancer Activity ◽

Tumor Volume ◽

Neutrophil Adhesion ◽

Mimosa Pudica ◽

Immunostimulatory Activity ◽

Tumor Weight ◽

Carbon Clearance ◽

Isolated Compound ◽

Dose Dependent

Objective: To investigate the in vivo anticancer and immunostimulatory activity of dichloromethane (DCM) extract of flowers of Mimosa pudica and its isolated compound 11β hydroxy-3 methoxy 1,2 dehydro crinane.Methods: The anticancer activity was performed on Ehrlich ascites carcinoma (EAC) cell line in Swiss albino mice. The activity was assessed by evaluating tumor volume, viable and nonviable tumor cell count, tumor weight, hematological, and histopathological parameters of EAC-bearing animals. The immunostimulatory activity was performed through carbon clearance, delayed type hypersensitivity (DTH), neutrophil adhesion and humoral antibody (HA) titer methods.Results: At the dose of 500 and 1000 mg/kg/day p.o for the extracts and 2.5 mg/kg/day p.o. for the isolated compound, significantly decrease the tumor volume (3.46±0.135 ml, 2.25±0.153 ml, and 1.84±0.012), increased the life span (59.32%, 76.39%, and 82.43%) and significantly (p<0.05) decreased tumor weight as compared with control. Hematological profiles were found to be nearly normal level in extract treated mice compared with tumor bearing control mice. The immunostimulatory activity was also found to be effective in the above dosage regimen. The results revealed that animals treated with above doses show a significant increase in the rate of carbon clearance from blood, increase in HA titer value, increase in neutrophil adhesion and significant (p<0.05) increase in mean paw edema in DTH reactions in dose-dependent manner.Conclusion: The results demonstrated that the extract is possessing dose-dependent anticancer activity and immunostimulatory activity attributed to the presence of crinane alkaloid.

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In Vitro and in Vivo Evaluation of Paclitaxel-induced Release of Apoptotic Biomarker ccCK18 to Guide Treatment Optimization in Ovarian Cancer

10.21203/rs.3.rs-61635/v1 ◽

2020 ◽

Author(s):

Elien De Thaye ◽

Koen Van de Vijver ◽

Jo Van Dorpe ◽

An Vermeulen ◽

Jan Van Bocxlaer ◽

...

Keyword(s):

Ovarian Cancer ◽

Cell Count ◽

Cell Lines ◽

Drug Exposure ◽

Tumor Volume ◽

Apoptotic Cell ◽

Treatment Needs ◽

Treatment Optimization

Abstract Background: Cytokeratins hold potential as biomarkers due to their epithelial specificity, abundance and cleavage by caspases during apoptosis. We evaluated paclitaxel-induced circulating caspase-cleaved (cc) cytokeratin 18 (CK18) as potential apoptotic cell-death marker to guide treatment optimization in ovarian cancer.Methods: Six ovarian cancer cell lines (SK-OV-3, SK-OV-3lucIP1, Caov-3, NIH:OVCAR-3, PA-1 and PM-LGSOC-01) were exposed in vitro to paclitaxel (PTX, 0 to 1000 nM) for 24h. Extracellular levels of ccCK18 were measured until 5 days after drug exposure. Cell count and ccCK18 release data were analyzed using a phase-nonspecific pharmacodynamic model implemented in NONMEM®. PA-1 and SK-OV-3lucIP1 xenografted female SCID/Beige mice received a placebo or single dose of 50 mg/kg PTX intraperitoneally. Response to PTX was evaluated in vivo using tumor volume and released ccCK18 levels. Results: In vitro, the correlation between cell count and released ccCK18 levels was present in all cell lines (Spearman’s rank correlation coefficient > 0.64). Tumor volume and ccCK18 longitudinal dynamics were markedly different for controls and PTX-treated PA-1 xenografts with changes in ccCK18 release preceding changes in tumor volume. For SK-OV-3lucIP1 xenografts, no differences were found between controls and PTX-treated mice. Conclusions: An association between PTX-induced ccCK18 release and cell count was demonstrated in vitro. The in vivo study supported the presence of an early-apoptotic peak in ccCK18 levels compared to a later observed effect on tumor volume in PTX-sensitive xenografts. Given the heterogeneous character of ovarian cancer, application and implementation of ccCK18 in a clinical setting to optimize or personalize cancer treatment needs further refinement.

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1,3,4-Thiadiazolo (3,2-Α) Pyrimidine-6-Carbonitrile Scaffold as PARP1 Inhibitors.

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520621666201216095018 ◽

2020 ◽

Vol 21 ◽

Author(s):

Elizabeth Eldhose ◽

Kaviarasan Lakshmanan ◽

Praveen T. Krishnamurthy ◽

Kalirajan Rajagopal ◽

Manal Mohammed ◽

...

Keyword(s):

Anticancer Activity ◽

In Silico ◽

Biological Activities ◽

Docking Study ◽

Binding Mode ◽

Oral Toxicity ◽

Standard Drug ◽

In Silico Docking

Background: 1,3,4-thiadiazolo pyrimidine is a lead molécule which is versatile for a wide variety of biological activities and in continuation of our interest in establishing some novel heterocyclic compounds for antitumor activity. Objective: The objective of the study was to synthesize series of 5-amino-7-(substituted aldehyde)-2[(naphthalene-2-yloxy)methyl] - [1,3,4]thiadiazolo-[3,2-α]-pyrimidine-6- carbonitrile derivative and evaluated for their possible in vitro and in vivo anticancer activity. Methods: Herein we report the synthetic scheme which was followed for the preparation of a series of title compounds B1- B9 is outlined in the scheme 1. The intermediate 5-[(naphthalen-2- yloxy)methyl]-1,3,4-thiadiazolo-2-amine was prepared by heating 2-naphthoxyacetic acid and thiosemicarbazide in presence of phosphoryl chloride at a temperature of 65 - 750C. The obtained compound reacted with malononitrile and appropriate amount of aromatic and heteroaromatic aldehydes in refluxing ethanol yielded 5-amino-7-(substituted aldehyde)-2[(naphthalene-2-yloxy)methyl] -[1,3,4]thiadiazolo-[3,2-α]-pyrimidine-6- carbonitrile derivatives (B1 – B9). The purity of synthesized compounds ensured by various spectral analysis. Results: In in-silico molecular docking studies compounds B3 and B9 show binding affinity like known PARP1 inhibitor olaparib. The cellular evaluation indicates that the anticancer activity of compounds B1, B3, B9 is significant when compared to standard drug (olaparib) against MDA-MB-232 cell line and compounds B3, B6, B7 are most active against MCF-7 cell lines. The most active compound B3 was subjected to acute oral toxicity studies by OECD 423 guidelines and in-vivo anti-cancer studies were carried out using DMBA induced model. Conclusion: The in-silico docking study of the newly synthesized compounds were performed, the results showed good binding mode in the active site of PARP1 enzyme. In-silico ADME properties of synthesized compounds were also studied and showed good drug like properties.

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Neferine induces mitochondrial dysfunction to exert anti-proliferative and anti-invasive activities on retinoblastoma

Experimental Biology and Medicine ◽

10.1177/1535370220928933 ◽

2020 ◽

Vol 245 (15) ◽

pp. 1385-1394

Author(s):

Jing Wang ◽

Yanmin Dong ◽

Qiuming Li

Keyword(s):

Tumor Volume ◽

Significant Inhibition ◽

Control Group ◽

High Dose ◽

Tumor Weight ◽

New Treatment ◽

Xenotransplantation Model

Retinoblastoma is common primary intraocular malignancy of infants and childhood. Neferine is a major bisbenzylisoquinoline alkaloid derived from the lotus plumule in Nelumbo nucifera. This study evaluated the mitigation role of Neferine on retinoblastoma in vitro and in vivo. Xenotransplantation model was established by injecting WERI-Rb-1 cells subcutaneously. Upon induction of retinoblastoma , mice were intraperitoneally injected with Neferine (0, 0.5, 1, 2 mg/kg) or ethanol every 3 days for 30 days. Tumor weight and tumor volume were measured every three days and compared between four groups. Then, mice were sacrificed and immunohistochemical examination was performed to compare Ki67, VEGF content between groups. WERI-Rb-1 cells were used for in vitro experiments and the anti-angiogenic role of Neferine was assessed by analyzing nodes/HPF number. In WERI-Rb-1 xenotransplantation model, compared with control group, 1 mg/kg Neferine treatment significantly inhibited tumor weight (0.39 ± 0.04 g vs. 0.25 ± 0.03 g, P< 0.05) and tumor volume (2163 ± 165 mm3 vs. 1276 ± 108 mm3, P< 0.05) after 30 days. Compared with ethanol-injected mice, 2 μM Neferine treatment significantly enhanced apoptosis rate (2.1 ± 0.6% vs. 14.6 ± 2.6%, P< 0.05), accompany downregulation of Ki67 (0.09 ± 0.02% vs. 0.01 ± 0.004%, P< 0.05) and VEGF (0.28 ± 0.04% vs. 0.05 ± 0.03%, P< 0.05) expression. Additionally, 2 μM Neferine treatment significantly decreased JC-1 red/green percentage. High-dose Neferine could decrease retinoblastoma angiogenesis in association with a significant inhibition on tumor growth and invasion. These findings suggested that Neferine could be a new treatment or adjuvant against retinoblastoma.

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