Cardiac toxicity can occur during the therapy with several cytotoxic drugs, including 5- Fluorouracil (5- FU). It is an antimetabolite that acts during the S phase of the cell cycle and is activated by thymidine phosphorylase into fluorodeoxyuridylate (5 fluoro 2'deoxyuridine 5'monophosphate, 5-FdUMP) that inhibits thymidylate synthase, thus preventing DNA synthesis that leads to imbalanced cell growth and ultimately cell death. It is still a widely used anticancer drug, since 1957. The present study aimed to evaluate the possible cardio-protective effects of ethanolic artichoke extract (Cynara scolymus L.) against 5-fluorouracil (5-FU) induced cardio-toxicity in rats by evaluating serum levels of Alanine aminotransferase, aspartate aminotransferase and creatine kinase enzymes. Methods: Twenty -four female albino rats were randomly divided into 4 groups each group with 6 rats. Group I: (negative control) received oral daily dose of dimethyl sulfoxide (DMSO) (2 ml/kg /day) for 10 successive days. Group II: (positive control) received oral daily dose of DMSO (2 ml/kg /day) for 10 successive days and subsequently administered single dose of 5-FU (150 mg/kg) by intraperitoneal injection on 8th day in association with DMSO. Groups III: received oral daily dose of ethanolic artichoke extract (200 mg/kg/day) for 10 successive days. Groups IV: received oral daily dose of ethanolic artichoke extract (200 mg/kg/day) for 10 successive days with subsequently administered single intraperitoneal dose of 5-FU (150 mg/kg) on 8th day in association with ethanolic extract. Results: Treatment of ethanolic artichoke extract prior 5-FU intoxication significantly attenuate the increase of serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) and creatine kinase (CK) enzymes activities caused by 5-FU-induced cardio-toxicity in rats. Conclusions: Results of the present finding suggest that the ethanolic artichoke extract may be an effective modulator in mitigating 5-FU induced cardiac toxicity in rats.
Keywords: Ethanolic artichoke extract, 5-Fluorouracil, Cardio-protection, AST, ALT and CK.
Sildenafil, tadalafil, and vardenafil are phosphodiesterase type 5 enzyme (PDE-5) inhibitors used for the treatment of male erectile dysfunction. This present study aims to investigate 55 herbal products indicated for men’s sexual health from the Malaysian market for adulteration of PDE-5 inhibitors and analogues. The screening and identification of 20 PDE-5 inhibitors and analogues in herbal products of various forms (powder, capsules, tablets, and pastels) were conducted using gas chromatography–electron impact-mass spectrometer (GC-EI-MS). The analysis has shown that 19 herbal products were adulterated with PDE-5 inhibitors and analogues. Unique ion fragmentations and the presence of molecular
... Show MoreAsthma is chronic inflammatory disease affecting 5% of world population. Characterized by eosinophilic type2 inflammation. FKBP51 immunophilin, important modular protein of glucocorticoid receptor (GR). We aimed to evaluate immunocytochemical localization of GR and FKBP51 in induced sputum cells by using immunocytochemical method and immunofluorescent ant-FKBP51 and anti –GR antibody and estimation of IgE and Type 2 inflammatory cytokine IL-5,IL-13 by ELISA technique.GR in the sputum show non-significant decrease of cytoplasmic distribution of the patient groups and highly significant increase in steroid treated patients and non-significant increase in nuclear distribution in non-steroid, FKBP51 nuclear localization show non-significant i
... Show MoreNowadays, the use of natural bio-products in pharmaceuticals is gaining popularity as safe alternatives to chemicals and synthetic drugs. Algal products are offering a pure, healthy and sustainable choice for pharmaceutical applications. Algae are photosynthetic microorganisms that can survive in different environmental conditions. Algae have many outstanding properties that make them excellent candidate for use in therapeutics. Algae grow in fresh and marine waters and produce in their cells a wide range of biologically active chemical compounds. These bioactive compounds are offering a great source of highly economic bio-products. The prese
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This study was designed to show the inhibitory effect of different concentrations of alcoholic extract of Borage officinalis on the Monoamine oxidase (MAO) and Acetylcholinesterase (AChE) enzymes in human serum. The results obtained from the study exhibited that alcoholic extract of Borage officinalis caused inhibition to enzymes activity with all concentrations of the extract. The results also showed that when the concentration of the extract was (0.001 mg/ml), the percentage of inhibition was (4.3% with MAO and 15.2% with AChE) and this percentage increases until reaching up to (74.7% with MAO and 84.18% with AChE) when the concentration of the extract was (0.1 mg/ml). From the kinetic parameters, studies found that alcoholic extract o
... Show MoreCurcumin is a yellow pigment produced from the rhizomes of the Curcuma longa plant and a primary chemo preventive component of turmeric is used as a spice and food coloring ingredient. Curcumin has a large number of pharmacological activities, such as anticancer, anti-diabetic, antioxidant, anti-infectious, and anti-inflammatory properties.Investigation of the geno-protective effect of curcumin on methotrexate induces chromosomal aberrations of spleen and bone marrow cells. In this study, 32 mice were used and divided into four groups (eight mice at each group) as follows: Group1 (negative control): Dimethyl sulfoxide was given intraperitoneally to mice every day for ten days.Group2 (positive control): Mice were received a single do
... Show MoreBackground: Decalcification of surface enamel adjacent to fixed orthodontic appliances, in the form of white spot lesions, is a wide spread and familiar well-known side effect of orthodontic treatment. The present study was carried out to evaluate the effect of enamel protective agent (Clinpro white varnish) on shear and tensile bond strength of Dentaurum orthodontic stainless steel brackets by using 3M Unitek and Ormco as orthodontic adhesive agents. Materials and methods: Sixty-four extracted human upper first premolar teeth were selected and randomly divided into two groups with 32 teeth each, representing the shear and tensile bond strength testing groups. Then according to the type of bonding adhesive and the addition of Clinpro before
... Show MoreSmall molecules drug conjugate mutual prodrug design (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended for targeting folate receptor , along with greater conservation of component until reaching the target tumor tissue . The designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were processed forward successfully by multistep reaction procedures , and by Thin Layer Chromatography (TLC) for
... Show MoreThe purpose of this research work is to synthesize conjugates of NSAIDs (ibuprofen, and naproxen) with sulfadiazine as possible mutual prodrugs to overcome the local gastric irritation of NSAIDs with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo bond that undergo reduction only by colonic bacterial azoreductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
Prednisolone (SAID) was conjugated with ibuprofen (NSAID) through an amino acid (glycine) as a spacer arm to synthesize the following compound:
Prednisolone – glycine – ibuprofen.
The method employed consists of converting the carboxylic acid function of (R,S) – ibuprofen – glycine to the highly reactive acid chloride and subsequent reaction with the C21 hydroxyl group of prednisolone. This reactive intermediate was found to react as well with the C17 tertiary hydroxyl group of the steroid to form three compounds and eight diastereomers. These results were confirmed by T.L.C, and the desired compound was separated by column chromatograph
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