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Hepatoprotective effect of Nobiletin against 5-fluorouracil induce hepatotoxicity
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5-florouracil is a widely used anticancer/anti-metabolite drug used to treat solid tumor like colon cancer, head and neck, rectum, stomach, pancreas and breast cancer; but, it can cause hepatotoxicity by induction of apoptosis through activation of caspases enzymes and oxidative stress. Nobiletin is a citrus fruit-derived flavonoid that possess significant biological activity, including anticancer, and anti-inflammatory. This study was design to investigate the effects of nobiletin against 5-florouracil-indcued hepatotoxicity in male rats through the measurement of selected -inflammatory, -apoptosis, and -oxidative stress markers. By use male Albino rats weighing 150-250gm around 28 animals; giving them tap water ad libitum and fed commercial pellets; and randomized into four groups (7animals/group) as following arrangement: Group I oral administered only corn oil for rats 1 ml for each kilogram for day by using of oral gavage for rat for 14 days. Group II: oral administered Nobiletin at dose 10 mg for each kilogram for each day (dissolved in corn oil) via oral gavage for 14 days. Group III: oral administered corn oil via oral gavage for 14 days after that single IP injection of 5-FU (150 mg/kg) on the day fourteenth (14). Group VI: Rats oral administered nobiletin dissolved in corn oil daily by oral gavage at a dose 10 mg/kg for each day for 14 days and a single IP injection of (150 mg/kg) 5-florouracil was given on day 14. All groups, seven animals of each group were sacrificed at day fifteenth (15); and, serum was collected to measure inflammatory and anti-inflammatory markers (interlukin-6 and interlukin-10) and liver function tests(ALT, LDH and AST); furthermore, liver tissue samples were collected to measure level of caspase-3, malondialdehyde and reduced form of glutathione, assessment of Hemeoxygenase-1 and NADPH quinone dehydrogenase-1 enzymes. In addition, histopathological study of the liver tissue of rats was perform to detect difference between architecture of liver cells in all rats’ groups. The protective effect of Nobiletin noted by decrease in apoptosis of hepatocytes by decreasing of caspase-3 and reduction on free radical through reduce in malondialdehyde level, also increase in Hemeoxygenase-1gene expression. Increase in NADPH quinone dehydrogenase-1 dehydrogenase enzyme. On histopath reduce in congestion and some inflammatory infiltration by using of nobiletin prior to give 5-florouracil.

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Study of the Protective Effects of Benfotiamine Against CCl4-Induced Hepatotoxicity in Rats
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Liver is considered as the first target for the toxic effects of toxins and other xenobiotics, and this can be attributed to its role as a site which receive all absorbed xenobiotics from the gastrointestinal tract and its role as a major site for biotransformation of xenobiotics. The present study was designed to evaluate the possible hepatoprotective effect of benfotiamine against CCl4-induced hepatotoxicity in rats. The study was conducted on 48 male albino rats; the animals were allocated into 8 groups (6 rats in each group) and treated as follow: 4 groups treated with oral doses of either normal saline, benfotiamine (100 mg/kg), thiamine (100 mg/kg), N-acetylcystein (400 mg/kg) only without induction of hepatic damage. Th

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Publication Date
Tue Feb 01 2022
Journal Name
Macromolecular Symposia
Synthesis of 5‐Fluorouracil–Naproxen Conjugates as a Mutual Prodrug for Targeting Cancer Tissues
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Abstract<p>A new 5‐fluorouracil–naproxen conjugate is synthesized as a mutual prodrug for targeting cancer tissues. The structure of the target compound and their intermediate are characterized by their melting point, IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR, and elemental microanalysis. The cytotoxic activity is preliminarily evaluated using nonsmall lung cancer CRL‐2049, human breast cancer CAL‐51, and one type of normal cell line; rat embryo fibroblast cell line. The synthesized compound shows a good cytotoxic effect at the cancer cell and no significant effect at rat embryo fibroblast cell line.</p>
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Publication Date
Sun Mar 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Design, Synthesis and Kinetic Study of Coumarin-Based Mutual Prodrug of 5-Fluorouracil and Dichloroacetic acid
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On the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in HCl buffer (pH 1.2) and in phosphate buffer (pH 7.4), as well as in vitro release study in human serum. The chemical structure of prodrug was confirmed by analyzing its FTIR, 1H NMR, 13C NMR and MS-ESI spectra. The results of in vitro kinetic study indicated that the prodrug was significantly stable in HCl and in phosphate buffers, and was hydrolyzed in human serum followed pseudo first order kinetics.

Keywords: Coumarin-bas

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Publication Date
Sun Dec 27 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and evaluation of B-cyclodextrin Based Nanosponges of 5- Fluorouracil by Using Ultrasound Assisted Method
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CD-nanosponges were prepared by crosslinking B-CD with diphenylcarbonate (DPC) using ultrasound assisted technique. 5-FU was incorporated with NS by freeze drying, and the phase solubility study, complexation efficiency (CE) entrapment efficiency were performed. Also, the particle morphology was studied using SEM and AFM. The in-vitro release of 5-FU from the prepared nanosponges was carried out in 0.1N HCl.

5-FU nanosponges particle size was in the nano size. The optimum formula showed a particle size of (405.46±30) nm, with a polydispersity index (PDI) (0.328±0.002) and a negative zeta potential (-18.75±1.8). Also the drug entrapment efficiency varied with the CD: DPC molar ratio from 15.6 % to 30%. The SEM an

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Study of Iraqi Spinach Leaves (Phytochemical and Protective Effects Against methotrexate-Induced hepatotoxicity in rats)
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Spinach, Spinacia oleracea L is a popular vegetable belonging to the family Chenopodiaceae. This study was concerned with extraction of compounds in Iraqi spinach leaves, preliminary phytochemical evaluation, identification of two biological important flavonols, quercetin and kaempferol in spinach leaves and evaluation of the protective effect of aqueous spinach extract on methotrexate (MTX) induced hepatotoxicity in rats. The percentage yield of extraction procedure, identification of spinach by chemical tests and identification of flavonols by thin layer chromatography (TLC) and High performance liquid chromatography (HPLC) were fully described in this study. The results indicate that the percentage of quarce

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Publication Date
Tue Oct 27 2015
Journal Name
International Journal Of Pharmacy And Pharmaceutical Sciences
EVALUATION OF CHEMOPREVENTIVE RESPONSE OF PENTOXIPHYLLINE AND SILDENAFIL INCOLORECTAL CARCINOMA EXPERIMENTALLY INDUCEDIN RATS: COMPARATIVE STUDYWITH 5-FLUOROURACIL
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Objective: This study was designed to investigate some possible therapeutic mechanisms of pentoxifylline and sildenafil in the treatment of colorectal carcinoma induced by 1, 2 dimethylhydrazines in rats. Methods: Rats were allocated into seven groups, negative control, colon cancer induced by 1,2,dimethylhydrazine, 5-fluorouracil (5-FU) (50 mg/kg)-treated, pentoxifylline (PTX) (50 mg/kg)-treated, sildenafil (0.7 mg/kg)-treated groups; the two other groups set as colon cancer induced group treated with PTX (50 mg/kg) plus 5-FU(50 mg/kg) and sildenafil (0.7 mg/kg) plus 5-FU (50 mg/kg), respectively. Results: Biochemical results revealed significant elevation of serum carcinoembryonic antigen (CEA) levels, carbohydrate19-9 antigen (CA19-9) as

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Publication Date
Tue Jul 08 2014
Journal Name
African Journal Of Traditional, Complementary And Alternative Medicines
Hepatoprotective Effect Of &lt;i&gt;Cymbopogon Citratus&lt;/i&gt; Aqueous Extract Against Hydrogen Peroxide-Induced Liver Injury In Male Rats
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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Effect of some induce chemical and biological agents against (Tilletia tritici (Bjerk) and T.laevis (Kühn) causal agents of wheat Common bunt disease
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This study was conducted to evaluate the efficiency of some chemicals and biological agents to induce systemic resistance (ISR) against to wheat common bunt disease caused by the two species of fungus Tilletia tritici (Bjerk.) Wint (T. caries (Dac.) Tul.) and T. laevis Kuhn (T. foetida (Wall.) Liro. Trails in the efforts to find an alternative, safe and environmentally friendly means to control the disease. Results of this study which carried out during two consecutive seasons for the years 2012 - 2013 and 2013 - 2014 at two different environmental locations. Seed treatment by (SA 100 and 200 mg/L, 500 ?–aminobutyric acid (BABA) and 1000 mg/L, Effective Microorganisms (EM1) 40 and 150 ml/kg seeds) have led to high significant redu

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of 5-Fluorouracil Derivatives as Possible Mutual Prodrugs with Meloxicam and Ibuprofen for Targeting Cancer Tissues
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In the present study, five derivatives have been designed to be synthesized as possible mutual prodrugs for 5-Fluorouracil (5-FU) and non steroidal anti-inflammatory drugs (NSAIDs) to selectively deliver the drugs into the cancer cells. The synthesis of the target compounds were accomplished following multistep reaction procedures, the chemical reaction followed up and the purity of the products were checked by TLC. The structure of the final compounds and their intermediates were confirmed by their melting points, infrared spectroscopy and elemental microanalysis, the hydrolysis of compound III was studied using HPLC technique. According to the results mentioned above, compounds (I−V) can be good candidates as possible mutual prod

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Publication Date
Fri Dec 27 2024
Journal Name
The Iraqi Journal Of Veterinary Medicine
Evaluating the Hepatoprotective Potential of Ginger Ethanolic Extract Against Lambda-Cyhalothrin-Induced Toxicity in Male Rats
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Ginger (Zingiber officinale Rosc.) is a traditional plant that is widely used as a spice or folk medicine. Lambda-cyhalothrin (LCT) is a synthetic pyrethroid that is widely used to control insecticide. The present study aimed to evaluate the potential protective effect of ginger ethanolic extract (GEE) on liver toxicity experimentally induced by LCT in albino rats. The experiment involved thirty adult male rats (‎Rattus norvegicus)‎, randomly ‎allocated to ‎one of three groups (n=10/group: control group, administered distilled water orally for 12 weeks‎; ‎LCT-treated group, received 5.43 mg/kg BW ‎(1/15 LD50‎ dose calculated in this study as 81.5 mg/kg BW) orally, for 12 weeks;‎ LCT-‎GEE-treated group, received t

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