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1.
Dokl Biochem Biophys ; 512(1): 300-318, 2023 Oct.
Article in English | MEDLINE | ID: mdl-38093135

ABSTRACT

Quinoline derivatives possess several therapeutic properties. Aim: studying the anticancer effect of 3-(4-methyl-2-oxo-2-H-quinoline-7-yloxy)-3-phenylacrylic acid's sodium solution on the Ehrlich ascites carcinoma (EAC). Median lethal dose (LD50) and dose response curve was determined for sodium salt solution of 3-(4-methyl-2-oxo-2-H-quinoline-7-yloxy)-3-phenylacrylic acid, then diving a group of one hundred Swiss albino mice, which are all females, into five groups: group 1: (negative control) where intraperitoneally injected with saline into mice for 10 successive days; group 2 (positive control), also namely (EAC-bearing group): where the EAC cells were intraperitoneally injected into mice (2.5 × 106 cells/mouse) only one time on the first day; group 3 which is defined as the (therapeutic group) where the Na+ salt of the synthetic compound was injected into the peritoneum of the mice (2.5 mg/kg) the very first day after the injection of the EAC, then the compound was injected every two days for a period of 10 days; group 4 which is the (preventive group) where the sodium salt of the synthetic compound (2.5 mg/kg) was injected in the peritoneum of the mice the day before the injection of the EAC, then the compound was successively injected every day for a period of ten days; and group 5 which is the (drug group) in which mice were repeatedly injected) in their peritoneum with the sodium salt of the synthetic compound (2.5 mg/kg on a daily basis over a period of ten days. On the eleventh day of the trial, EAC cells were harvested from each mouse in a heparinized saline, in addition to blood samples, liver and kidney tissues which are also collected. Molecular docking showed that compound's sodium salt was docked into (PDB: 2R7G) and (PDB: 2R3I), which are the retinoblastoma protein receptor and the cyclin D-1 receptor respectively. Compared to those in the positive control group, mice in both the therapeutic and preventive groups, has shown a significant decrease in MDA, cyclin D-1 levels in the tissues of both liver and kidney tissues, in addition to the serum ALT, AST, CK-MB, and LDH activities, and the serum urea and creatinine concentration. However, mice in the formerly mentioned groups, both therapeutic and preventive groups, have shown an increase in the serum albumin, total protein, retinoblastoma protein in both liver and kidney tissues as well as the total antioxidant capacity, when compared to mice in the positive control group. It is worth mentioning that histopathological findings have confirmed that. Sodium salt of 3-(4-methyl-2-oxo-2H-quinoline-7-yloxy)-3-phenylacrylic acid showed potential in vivo anticancer and antioxidant effects against Ehrlich ascites carcinoma cells; (EAC cells).


Subject(s)
Antineoplastic Agents , Carcinoma, Ehrlich Tumor , Quinolines , Female , Animals , Mice , Molecular Docking Simulation , Ascites/drug therapy , Retinoblastoma Protein/therapeutic use , Carcinoma, Ehrlich Tumor/drug therapy , Carcinoma, Ehrlich Tumor/pathology , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Antioxidants/therapeutic use , Quinolines/pharmacology , Quinolines/therapeutic use , Cyclin D
2.
Heliyon ; 9(3): e13869, 2023 Mar.
Article in English | MEDLINE | ID: mdl-36873464

ABSTRACT

Background: Cancer is leading to premature deaths across the globe. Therapeutic approaches are still being developed to enhance the survival of cancer patients. In our previous study, extracts from four Togolese plants, namely, Cochlospermum planchonii (CP), Piliostigma thonningii (PT), Paullinia pinnata (PP), and Securidaca longipedunculata (SL), actually used in traditional medicine for cancer treatment, showed beneficial health effects against oxidative stress, inflammation, and angiogenesis. Purpose: In the present study, we aimed to investigate the cytotoxicity and antitumor activities of these four plant extracts. Material and methods: Breast, lung, cervical, and liver cancer cell lines were exposed to the extracts, and viability was assessed using the Sulforhodamine B method. P. pinnata and S. longipedunculata with significant cytotoxicity were selected for in vivo tests. The acute oral toxicity of these extracts was assessed using BALB/c mice. The antitumor activity was evaluated using the EAC tumor bearing mice model, wherein mice were orally treated with extracts at different concentrations for 14 days. The standard drug was cisplatin (3.5 mg/kg, i.p), single dose. Results: Cytotoxicity tests revealed that SL, PP, and CP extracts have more than 50% cytotoxicity at 150 µg/mL. The acute oral toxicity of PP and SL at 2000 mg/kg did not show any toxic signs. At therapeutic doses of 100 mg/kg, 200 mg/kg and 400 mg/kg of PP and 40 mg/kg, 80 mg/kg, and 160 mg/kg of SL, extracts showed beneficial health effects by modulating several biological parameters. SL extract significantly reduced tumor volume (P < 0.001), cell viability, and normalized hematological parameters. SL also demonstrated a strong anti-inflammatory activity similar to the standard drug. The SL extract also revealed a significant increase of the life span of treated mice. PP extract reduced the tumor volume and significantly improved the values of endogenous antioxidants. Both PP and SL extracts also exerted significant anti-angiogenic potency. Conclusion: The study indicated that polytherapy would be a panacea for the efficient use of medicinal plant extracts against cancer. This approach will make it possible to act simultaneously on several biological parameters. Molecular studies of both extracts targeting key cancer genes in several cancer cells are currently underway.

3.
Clin Exp Pharmacol Physiol ; 49(1): 145-174, 2022 01.
Article in English | MEDLINE | ID: mdl-34536310

ABSTRACT

Nowadays, quinoline scaffold is among the most vital construction compounds for the development of new drugs. The purpose of this research is to evaluate the anti-cancer activity of sodium salt of ethyl (E)-2-cyano-3-(7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-yl)-3-(4-hydroxyphenyl) acrylate against Ehrlich ascites carcinoma (EAC) cells residing in female mice's peritoneal cavity. The docking study exhibited a favourable interaction between the compound and the receptors 1MOY and 3KJF of osteopontin and caspase 3, respectively. The compound's sodium salt showed potential antioxidant and anti-cancer effects against Ehrlich ascites carcinoma (EAC) cells in vivo. Herein, the results elucidated that treatment with the compound's sodium salt exerted significant chemopreventive and chemotherapeutic effects, which reduced both EAC cell volume and count. Our results revealed that treatment with the sodium salt of the compound demonstrated a remarkable in vivo apoptotic effect through elevation of the expression of caspase 3 and reduction of osteopontin levels. Histopathological examination confirmed that the compound's sodium salt improved liver and kidney tissues without any apparent adverse effects.


Subject(s)
Antineoplastic Agents/therapeutic use , Carcinoma, Ehrlich Tumor/drug therapy , Quinolones/therapeutic use , Animals , Antineoplastic Agents/pharmacology , Antioxidants/pharmacology , Antioxidants/therapeutic use , Dose-Response Relationship, Drug , Female , Lethal Dose 50 , Mice , Molecular Docking Simulation , Molecular Structure , Quinolones/pharmacology
4.
J Ethnopharmacol ; 278: 114297, 2021 Oct 05.
Article in English | MEDLINE | ID: mdl-34118341

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Tabebuia pallida (Lindl.) Miers (T. pallida) is a well-known native Caribbean medicinal plant. The leaves and barks of T. pallida are used as traditional medicine in the form of herbal or medicinal tea to manage cancer, fever, and pain. Moreover, extracts from the leaves of T. pallida showed anticancer activity. However, the chemical profile and mechanism of anticancer activity of T. pallida leaves (TPL), stem bark (TPSB), root bark (TPRB) and flowers (TPF) remain unexplored. AIM OF THE STUDY: The present study was designed to explore the regulation of apoptosis by T. pallida using Ehrlich Ascites Carcinoma (EAC) cultured cells and an EAC mouse model. LC-ESI-MS/MS was used for compositional analysis of T. pallida extracts. MATERIALS AND METHODS: Dried and powdered TPL, TPSB, TPRB and TPF were extracted with 80% methanol. Using cultured EAC cells and EAC-bearing mice with and without these extracts, anticancer activities were studied by assessing cytotoxicity and tumor cell growth inhibition, changes in life span of mice, and hematological and biochemical parameters. Apoptosis was analyzed by microscopy and expression of selected apoptosis-related genes (Bcl-2, Bcl-xL, NFκ-B, PARP-1, p53, Bax, caspase-3 and -8) using RT-PCR. LC-ESI-MS analysis was performed to identify the major compounds from active extracts. Computer aided analyses was undertaken to sort out the best-fit phytoconstituent of total ten isolated compounds of this plant for antioxidant and anticancer activity. RESULTS: In EAC mice compared with untreated controls, the TPL extract exhibited the highest cancer cell toxicity with significant tumor cell growth inhibition (p < 0.001), reduced ascites by body weight (p < 0.01), increased the life span (p < 0.001), normalized blood parameters (RBC/WBC counts), and increased the levels of superoxide dismutase and catalase. TPL-treated EAC cells showed increased apoptotic characteristics of membrane blebbing, chromatin condensation and nuclear fragmentation, and caspase-3 activation, compared with untreated EAC cells. Moreover, annexin V-FITC and propidium iodide signals were greatly enhanced in response to TPL treatment, indicating apoptosis induction. Pro- and anti-apoptotic signaling after TPL treatment demonstrated up-regulated p53, Bax and PARP-1, and down-regulated NFκ-B, Bcl-2 and Bcl-xL expression, suggesting that TPL shifts the balance of pro- and anti-apoptotic genes towards cell death. LC-ESI-MS data of TPL showed a mixture of glycosides, lapachol, and quercetin antioxidant and its derivatives that were significantly linked to cancer cell targets. The compound, pelargonidin-3-O-glucoside was found to be most effective in computer aided models. CONCLUSIONS: In conclusion, the TPL extract of T. pallida possesses significant anticancer activity. The tumor suppressive mechanism is due to apoptosis induced by activation of antioxidant enzymes and caspases and mediated by a change in the balance of pro- and anti-apoptotic genes that promotes cell death.


Subject(s)
Antineoplastic Agents/therapeutic use , Apoptosis/drug effects , Carcinoma/drug therapy , Phytotherapy , Plant Extracts/pharmacology , Plant Leaves/chemistry , Animals , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/adverse effects , Antineoplastic Agents/chemistry , Caspase 3/genetics , Caspase 3/metabolism , Caspase 8/genetics , Caspase 8/metabolism , Cell Line, Tumor , Cell Survival/drug effects , Dose-Response Relationship, Drug , Gene Expression Regulation, Neoplastic/drug effects , Humans , Male , Mice , Neoplasms, Experimental , Plant Extracts/administration & dosage , Plant Extracts/adverse effects , Plant Extracts/chemistry
5.
Anticancer Agents Med Chem ; 21(6): 782-792, 2021.
Article in English | MEDLINE | ID: mdl-32781964

ABSTRACT

BACKGROUND: Syzygium cumini is one of the evidence-based traditional medicinal plant used in the treatment of various ailments. OBJECTIVES: Herein, the antioxidant property and anticancer property of Syzygium cumini against Ehrlich Ascites Carcinoma (EAC) cells were examined to find effective chemotherapeutics. METHODS: In vitro assays, and phytochemical and chromatographic analyses were used to determine antioxidant properties and chemical constituents of Syzygium cummini Bark Methanolic Extract (SCBME). Functional assays were used to measure the anticancer activity of SCBME. Fluorescence microscopy and RT-PCR were used to examine morphological and molecular changes of EAC cells followed by SCBME treatment. RESULTS: Phytochemical and GC-MS analyses confirmed the presence of compounds with antioxidant and anticancer activities. Accordingly, we have noted a strong antioxidant activity of SCBME with an IC50 value of ~10µg/ml. Importantly, SCBME exerted a dose-dependent anticancer activity with significant inhibition of EAC cell growth (71.08±3.53%; p<0.001), reduction of tumor burden (69.50%; p<0.01) and increase of life span (73.13%; p<0.001) of EAC-bearing mice at 75mg/kg/day. Besides, SCBME restored the blood toxicity towards normal in EAC-bearing mice (p<0.05). DISCUSSION: SCBME treated EAC cells showed apoptotic features under a fluorescence microscope and fragmented DNA in DNA laddering assay. Moreover, up-regulation of the tumor suppressor p53 and pro-apoptotic Bax and down-regulation of NF-κB and anti-apoptotic Bcl-2 genes implied induction of apoptosis followed by SCBME treatment. CONCLUSION: The antiproliferative activity of SCBME against EAC cells is likely due to apoptosis, mediated by regulation of p53 and NF-κB signaling. Thus, SCBME can be considered as a useful resource in cancer chemotherapy.


Subject(s)
Antineoplastic Agents, Phytogenic/chemistry , Antioxidants/chemistry , Carcinoma, Ehrlich Tumor/drug therapy , Plant Bark/chemistry , Plant Extracts/chemistry , Syzygium/chemistry , Animals , Antineoplastic Agents, Phytogenic/pharmacology , Antioxidants/pharmacology , Apoptosis/drug effects , DNA Fragmentation/drug effects , Disease Models, Animal , Dose-Response Relationship, Drug , Gas Chromatography-Mass Spectrometry , Gene Expression Regulation/drug effects , Humans , Male , Methanol/chemistry , Mice , NF-kappa B/genetics , NF-kappa B/metabolism , Plant Extracts/pharmacology , Plants, Medicinal , Proto-Oncogene Proteins c-bcl-2/genetics , Proto-Oncogene Proteins c-bcl-2/metabolism , Solvents/chemistry , Tumor Suppressor Protein p53/genetics , Tumor Suppressor Protein p53/metabolism , bcl-2-Associated X Protein/genetics , bcl-2-Associated X Protein/metabolism
6.
BMC Complement Altern Med ; 16: 211, 2016 Jul 12.
Article in English | MEDLINE | ID: mdl-27405609

ABSTRACT

BACKGROUND: Ricinus communis (Euphorbiaceae) has previously been reported to possess analgesic, antihistamine, antioxidant and anti-inflammatory activities. This study was designed for isolation, characterization and evaluation of antibacterial and anti-proliferative activities of R. communis seed protein. METHODS: The concentration and molecular weight of R. communis seed protein were estimated by SDS-PAGE and spectrophotometric analysis, respectively. Lectin activity was evaluated by hemagglutination assay on mice blood. In vitro susceptibility of four human pathogenic bacteria including Escherichia coli, Pseudomonas aeruginosa, Enterobacter aerogenes and Staphylococcus aureus was detected using disk diffusion assay, and minimum inhibitory concentration (MIC) value was determined using micro-dilution method. A total of twenty four Swiss albino mice containing Ehrlich's ascites carcinoma (EAC) cells were treated with the crude protein of R. communis at 50 and 100 µg/ml/d/mouse for 6 days. Growth inhibitory activity of R. communis seed protein on EAC cells was determined by haemocytometer counting using trypan blue dye and DAPI (4΄,6-diamidino-2-phenylindole) staining was used to assess apoptotic cells. RESULTS: The protein concentration of six R. communis (castor) varieties ranged between 21-35 mg/ml and molecular weight between 14-200 kDa. Castor protein agglutinated mice blood at 3.125 µg/wall. The seed protein shows considerable antimicrobial activity against E. coli, P. aeruginosa and S. aureus, exhibiting MIC values of 250, 125 and 62.5 µg/ml, respectively. Administration of seed protein led to 54 % growth inhibition of EAC cells at 100 µg/ml. DAPI staining indicates marked features of apoptosis including condensation of cytoplasm, nuclear fragmentation and aggregation of apoptotic bodies etc. CONCLUSION: Our study suggests that the lectin rich R. communis seed protein has strong antibacterial and anticancer activities.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antineoplastic Agents/pharmacology , Cell Proliferation/drug effects , Plant Extracts/pharmacology , Ricinus communis/chemistry , Seeds/chemistry , Animals , Anti-Bacterial Agents/chemistry , Antineoplastic Agents/chemistry , Apoptosis/drug effects , Bangladesh , Mice , Microbial Sensitivity Tests , Neoplasms, Experimental , Plant Extracts/chemistry , Plant Proteins/chemistry , Plant Proteins/pharmacology
7.
BMC Complement Altern Med ; 16: 157, 2016 May 31.
Article in English | MEDLINE | ID: mdl-27246877

ABSTRACT

BACKGROUND: Amaranthus (Amaranthaceae) has previously been reported to possess different bioactive phytochemicals including phenols, tannins and flavonoids. The current study was designed to evaluate the antioxidant, anti-proliferative and antimicrobial activity of stem and seed extracts of Amaranthus lividus (AL) and Amaranthus hybridus (AH), respectively. METHODS: Antioxidant activity of methanol extract was assessed by DPPH radical scavenging assay. Determination of lectin activity of Amaranthus extract was carried out using hemagglutination assay on mouse blood. A total of thirty six Swiss albino mice containing Ehrlich's ascites carcinoma (EAC) cells were treated with AL and AH extract at 25, 50 and 100 µg/ml/day/mouse for six days. Growth inhibitory activity was determined by haemocytometer counting of EAC cells using trypan blue dye and DAPI (4΄,6-diamidino-2-phenylindole) staining was used to assess apoptotic cells. Gene amplification study was conducted to observe the expression pattern of p53, Bax, Bcl-2 and caspase-3 mRNA using PCR (polymer chain reaction) technique. In vitro susceptibility of five pathogenic bacteria including Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Salmonella typhi and Staphylococcus aureus was detected using disk diffusion assay. RESULTS: The radical scavenging assay indicated that AH and AL possesses potent antioxidant potential, exhibiting IC50 value of 28 ± 1.5 and 93 ± 3.23 µg/ml, respectively. Hemagglutination assay revealed that AH and AL agglutinated mice blood at 1.565 and 3.125 µg/wall, respectively. Administration of AH and AL extract led to 45 and 43 % growth inhibition of EAC cells, respectively at 100 µg/ml with marked features of apoptosis including cell shrinkage, condensation of cytoplasm and aggregation of apoptotic bodies etc. Up-regulation of p53, Bax and caspase-3 and down-regulation of Bcl-2 mRNA in Amaranthus treated mice indicated mitochondria mediated apoptosis of EAC cells in comparison with control. None of the bacterial species showed susceptibility to the extract of both the Amaranthus species. CONCLUSION: Our current findings suggest that both of the Amaranthus species have strong antioxidant, lectin and anti-proliferative activity on EAC cells. The current anticancer potential was observed due mainly to the mitochondria mediated apoptosis of EAC cells.


Subject(s)
Amaranthus/chemistry , Anti-Infective Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Antioxidants/pharmacology , Plant Extracts/pharmacology , Animals , Bangladesh , Biphenyl Compounds , Carcinoma, Ehrlich Tumor , Drug Screening Assays, Antitumor , Female , Indoles/metabolism , Mice , Microbial Sensitivity Tests , Picrates , Vegetables/chemistry
8.
Phytother Res ; 29(4): 573-81, 2015 Apr.
Article in English | MEDLINE | ID: mdl-25583285

ABSTRACT

Anticancer activities of p-menth-1-ene-4,7-diol (EC-1) isolated from Eucalyptus camaldulensis Dhnh. were studied on Ehrlich ascites carcinoma (EAC) cells by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay. Anticancer activities also analyzed in EAC-bearing mice by assessment of cancer growth inhibition, changes in cancer volume, changes in life span, and hematological parameters. Apoptosis was analyzed by fluorescence microscope, DNA fragmentation assay, and flow cytometry. The expression of apoptosis-related genes, Bcl-2, Bcl-X, PARP-1, p53, and Bax, were analyzed using polymerase chain reaction (PCR). EC-1 significantly inhibited proliferation of EAC cells in vivo and restored the altered hematological parameters of EAC-bearing mice. Cytological observation by fluorescence microscope showed apoptosis of EAC cells upon treatment with EC-1. Also, DNA fragmentation assay revealed EAC cells' apoptosis following EC-1 treatment. Increased mRNA expressions of p53 and Bax genes and negative expressions of Bcl-2 and Bcl-X were observed in cells treated with EC-1. These findings confirmed the induction of apoptosis by EC-1. In addition, MTT assay showed dose-dependent anticancer activity of EC-1 against EAC cell. Cell cycle analysis revealed that EC-1 treatment caused suppression of EAC cells at S phase. To conclude, EC-1 is a novel anticancer compound and showed antiproliferative and apoptotic activities in cellular and mice models.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Carcinoma, Ehrlich Tumor/drug therapy , Cell Cycle/drug effects , Eucalyptus/chemistry , Terpenes/pharmacology , Animals , Carcinoma, Ehrlich Tumor/pathology , Cell Proliferation , DNA Fragmentation , Male , Mice , Plant Bark/chemistry
9.
Asian Pac J Trop Biomed ; 4(Suppl 1): S284-92, 2014 May.
Article in English | MEDLINE | ID: mdl-25183099

ABSTRACT

OBJECTIVE: To find out the effective anticancer drugs from bacterial products, petroleum ether extract of Corynebacterium xerosis. METHODS: Antiproliferative activity of the metabolite has been measured by monitoring the parameters like tumor weight measurement, tumor cell growth inhibition in mice and survival time of tumor bearing mice, etc. Hepatoprotective effect of the metabolites was determined by observing biochemical, hematological parameters. RESULTS: It has been found that the petroleum ether extract bacterial metabolite significantly decrease cell growth (78.58%; P<0.01), tumor weight (36.04 %; P<0.01) and increase the life span of tumor bearing mice (69.23%; P<0.01) at dose 100 mg/kg (i.p.) in comparison to those of untreated Ehrlich ascites carcinoma (EAC) bearing mice. The metabolite also alters the depleted hematological parameters like red blood cell, white blood cell, hemoglobin (Hb%), etc. towards normal in tumor bearing mice. Metabolite show no adverse effect on liver functions regarding blood glucose, serum alkaline phosphatases, glutamic pyruvic transaminase, glutamic oxaloacetic transaminase activity and serum billirubin, etc. in normal mice. Histopathological observation of these mice organ does not show any toxic effect on cellular structure. But in the case of EAC bearing untreated mice these hematological and biochemical parameters deteriorate extremely with time whereas petroleum ether extract bacterial metabolite receiving EAC bearing mice nullified the toxicity induced by EAC cells. CONCLUSION: Study results reveal that metabolite possesses significant antiproliferative and hepatoprotective effect against EAC cells.

10.
Chem Biol Interact ; 222: 44-9, 2014 Oct 05.
Article in English | MEDLINE | ID: mdl-25168848

ABSTRACT

Photodynamic therapy (PDT) is emerging as a promising non-invasive treatment for cancers. It involves three key components; a photosensitizer, light and tissue oxygen. Even though several photosensitizers have been investigated for their use in PDT, they have several disadvantages and hence the search for more effective sensitizers has become important in recent years. The dye selected in our study - symmetrical diiodinated benzothiazolium squaraine (SQDI) - is one of the newly developed photosensitizers. The study aimed to evaluate the in vitro cytotoxicity of the dye on Ehrlich's Ascites Carcinoma (EAC) cells and to assess the in vivo toxicity on Swiss Albino mice. The EAC cells were maintained in the peritoneum of mice and used to study the dark toxicity and phototoxicity by Trypan blue dye exclusion method, estimation of Reactive Oxygen Species (ROS), caspase activity and levels of thiobarbituric acid reactive substances (TBARS). The in vitro studies revealed that the dye induces toxicity in the presence of light and mediates cell death. The in vivo part of the study, which dealt with the toxicity evaluation in the body of Swiss Albino mice, was done by analyzing the parameters like serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), lactate dehydrogenase (LDH), creatine kinase (CK) and alkaline phosphatase (ALP). No significant change was observed in the above mentioned parameters in the dye administered group when compared to control. Altogether, this experiment indicates that the SQDI selected for our study may be used as an efficient photosensitizer for PDT applications and does not elicit acute toxicity to normal tissues in the absence of light.


Subject(s)
Benzothiazoles/pharmacology , Cyclobutanes/pharmacology , Phenols/pharmacology , Photochemotherapy/methods , Photosensitizing Agents/pharmacology , Alanine Transaminase/blood , Alkaline Phosphatase/blood , Animals , Aspartate Aminotransferases/blood , Benzothiazoles/chemistry , Benzothiazoles/toxicity , Carcinoma, Ehrlich Tumor/drug therapy , Carcinoma, Ehrlich Tumor/metabolism , Caspase 3/metabolism , Cell Line, Tumor , Creatine Kinase/blood , Cyclobutanes/chemistry , Cyclobutanes/toxicity , L-Lactate Dehydrogenase/blood , Male , Mice , Phenols/chemistry , Phenols/toxicity , Photosensitizing Agents/chemistry , Photosensitizing Agents/toxicity , Reactive Oxygen Species/metabolism , Thiobarbituric Acid Reactive Substances/metabolism
11.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-672851

ABSTRACT

Objective: To find out the effective anticancer drugs from bacterial products, petroleum ether extract of Corynebacterium xerosis.Methods:parameters like tumor weight measurement, tumor cell growth inhibition in mice and survival time of tumor bearing mice, etc. Hepatoprotective effect of the metabolites was determined by observing biochemical, hematological parameters.Results:It has been found that the petroleum ether extract bacterial metabolite significantly Antiproliferative activity of the metabolite has been measured by monitoring the decrease cell growth (78.58%; P<0.01), tumor weight (36.04 %; P<0.01) and increase the life span of tumor bearing mice (69.23%; P<0.01) at dose 100 mg/kg (i.p.) in comparison to those of untreated Ehrlich ascites carcinoma (EAC) bearing mice. The metabolite also alters the depleted hematological parameters like red blood cell, white blood cell, hemoglobin (Hb%), etc. towards normal in tumor bearing mice. Metabolite show no adverse effect on liver functions regarding blood glucose, serum alkaline phosphatases, glutamic pyruvic transaminase, glutamic oxaloacetic transaminase activity and serum billirubin, etc. in normal mice. Histopathological observation of these mice organ does not show any toxic effect on cellular structure. But in the case of EAC bearing untreated mice these hematological and biochemical parameters deteriorate extremely with time whereas petroleum ether extract bacterial metabolite receiving EAC bearing mice nullified the toxicity induced by EAC cells.Conclusion:Study results reveal that metabolite possesses significant antiproliferative and hepatoprotective effect against EAC cells.

12.
Article in English | WPRIM (Western Pacific) | ID: wpr-343265

ABSTRACT

<p><b>OBJECTIVE</b>To find out the effective anticancer drugs from bacterial products, petroleum ether extract of Corynebacterium xerosis.</p><p><b>METHODS</b>Antiproliferative activity of the metabolite has been measured by monitoring the parameters like tumor weight measurement, tumor cell growth inhibition in mice and survival time of tumor bearing mice, etc. Hepatoprotective effect of the metabolites was determined by observing biochemical, hematological parameters.</p><p><b>RESULTS</b>It has been found that the petroleum ether extract bacterial metabolite significantly decrease cell growth (78.58%; P<0.01), tumor weight (36.04 %; P<0.01) and increase the life span of tumor bearing mice (69.23%; P<0.01) at dose 100 mg/kg (i.p.) in comparison to those of untreated Ehrlich ascites carcinoma (EAC) bearing mice. The metabolite also alters the depleted hematological parameters like red blood cell, white blood cell, hemoglobin (Hb%), etc. towards normal in tumor bearing mice. Metabolite show no adverse effect on liver functions regarding blood glucose, serum alkaline phosphatases, glutamic pyruvic transaminase, glutamic oxaloacetic transaminase activity and serum billirubin, etc. in normal mice. Histopathological observation of these mice organ does not show any toxic effect on cellular structure. But in the case of EAC bearing untreated mice these hematological and biochemical parameters deteriorate extremely with time whereas petroleum ether extract bacterial metabolite receiving EAC bearing mice nullified the toxicity induced by EAC cells.</p><p><b>CONCLUSION</b>Study results reveal that metabolite possesses significant antiproliferative and hepatoprotective effect against EAC cells.</p>

13.
Indian J Pharm Sci ; 75(5): 515-22, 2013 Sep.
Article in English | MEDLINE | ID: mdl-24403651

ABSTRACT

Melothria heterophylla (Lour.) Cogn., (family-Cucurbitaceae) popularly known as kundari, has been shown to exhibit antioxidant effects. The main objective was to isolate active constituents of the plant extract. In this study, the ability of M. heterophylla to induce apoptosis was studied in Ehrlich ascites carcinoma cells. Treatment of the Ehrlich ascites carcinoma cells with a variety of concentrations of the ethanol extracts of M. heterophylla and gallic acid (100-1000 µM), to determine the sequences of events marked by apoptosis, assayed by the spectrofluorometric method. Gallic acid and rutin were isolated from plant extract which were quantified by high-performance liquid chromatography. Our results indicate that ethanol extracts of M. heterophylla and gallic acid-induced apoptotic cell death in a dose dependent manner could be due to the generation of reactive oxygen species, especially H2O2, which is confirmed by caspase 3 activation. Treatment of Ehrlich ascites carcinoma bearing Swiss albino mice with varied doses (200 and 400 mg/kg, b.w.) of plant extract significantly reduced tumor volume and viable tumor cell count and improved hemoglobin content, RBC count, mean survival time, tumor inhibition, and percentage life span. The enhanced antioxidant status in extract-treated animals were evident from the decline in the levels of lipid peroxidation and increased levels of glutathione, catalase, and superoxide dismutase. The data suggest that M. heterophylla exerts anticancer activity, valuable for application in food and drug products.

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