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Rehab M Abdel Megeed, Dalia B Fayed, Amira Abood, Mai O Kadry
Although, fluconazole is widely used in clinical treatment as an antifungal drug, it recorded potential problems as resistance and intracellular accumulation. Female albino mice were injected with single ip dose of Candida albicans (1.5 × 106 CFU) . Three weeks post treatment with fluconazole and two novel synthesized compounds [(2-(4-(Pyridin-2-yl) aminosulfonylphenylamino)-6-(naphthalen-2-yl)-4-(pyridin-2-yl) pyridine-3carbonitrile) and (2-(4-(Pyrimidin-2-yl) aminosulfonylphenylamino)-6-(naphthalen-2-yl)-4-(pyridine-2-yl)pyridine-3-carbonitrile) (13b & 14b, respectively)] in both low and high doses (50 mg/kg & 200 mg/kg), liver function and vaginal inflammation were assessed...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Mahboob Alam, Mohammad Jane Alam, Shaista Azaz, Mehtab Parveen, Soonheum Park, Shabbir Ahmad
The quantum chemical study, spectroscopic characterization and biological activity of the pharmaceutically active 7-benzoyloxycoumarin (2) molecule have been presented. Potential energy surface (PES) scanning has been performed to search for the most stable molecular geometry of the present compound. The stable geometry in the ground state, IR, UV-Vis absorption and NMR (13 C, 1 H) spectra of the title compound were theoretically obtained and compared with the experimental one. Various theoretical molecular parameters like molecular energy, atomic charges, dipole moment, thermodynamic parameters, donor-acceptor natural bond orbital (NBO) hyperconjugative interaction energies, frontier molecular orbitals energies, HOMO-LUMO gap, molecular electrostatic potential, chemical reactivity descriptors, molecular polarizability and non-linear optical (NLO) properties are presented...
April 2018: Computational Biology and Chemistry
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Sajid Rashid, Qaiser Iqbal, Maryam Rozi, Saima Younis, Jamaluddin Mahar
Ten fused heterocyclic derivatives bearing the 2,6-di(subsituted phenyl)thiazolo[3,2-b]-1,2,4-triazoles as central rings were synthesized and structures of the compounds were established by analytical and spectral data using FTIR, EI-MS, (1)H NMR and (13)C NMR techniques. In vitro inhibitory activities of synthesized compounds on α-amylase, α-glucosidase and α-burylcholinesterase (α-BuChE) were evaluated using a purified enzyme assays. Compound 5c demonstrated strong and selective α-amylase inhibitory activity (IC50=1...
October 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Saeed Ahmad, Fariha Rashid Bhatti, Farhan Hameed Khaliq, Tehreem Younas, Asadullah Madni, Abida Latif
The present study demonstrates the biological study of Ficus carica fruit. Methanolic extract of plant fruit was prepared and evaporated under reduced pressure by rota vapor and n- hexane, Chloroform, ethyl acetate and n-butanol soluble fractions were prepared separately from crude methanolic extract. These fractions were then screened for acetyl cholinesterase, butryl cholinesterase and lipoxygenase activities. n-butanol soluble fraction showed significant antiacetylcholinesterase activity (78.55±0.76%) with IC50 of 55...
September 2016: Pakistan Journal of Pharmaceutical Sciences
Jacob K Akintunde, C Abigail Irechukwu
BACKGROUND: The antipsychotic, haloperidol, is extremely efficient in the treatment of schizophrenia but its application is constrained because of irreversible adverse drug reactions. Hence, in this study, we investigate the differential effects of black seed oil on cholinesterase [acetylcholinesterase (AChE) and butrylcholinesterase (BuChE), ectonucleotidase (5'-nucleotidase), lactate dehydrogenase (LDH) and monoamine oxidase (MAO)] activities and relevant markers of oxidative stress in the cerebrum of haloperidol-induced neuronal-damaged rats...
August 2016: Therapeutic Advances in Drug Safety
G Zengin, N S Degirmenci, L Alpsoy, A Aktumsek
OBJECTIVE: The aim of this work was to investigate the cytotoxic, antioxidative, and enzyme inhibition effects of alizarin, quinizarin, and purpurin, which are anthraquinones (AQ). METHODS: Cytotoxic effects were evaluated with cell inhibition rate by 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide assay. Different chemical assays, including free radical scavenging activity (1,1-diphenyl-2-picrylhydrazyl and 2,2-azino-bis(3-ethylbenzothiazloine-6-sulfonic acid)), phosphomolybdenum and reducing power (ferric reducing antioxidant power and cupric ion reducing activity), were used to evaluate the antioxidant properties...
May 2016: Human & Experimental Toxicology
Halide Edip Temel, Tuncer Temel, Dondu Uskudar Cansu, Ayşegul Ozakyol
BACKGROUND: After 40 years since establishment of Child-Pugh staging, 14 years since establishment of MELD scoring system, and 25 years since establishment of King's College Criteria, there is still a search for more accurate systems for determination of prognosis in patients with acute liver failure--cirrhosis and prioritization for receipt of a liver transplant--prediction of post transplant mortality. Butrylcholinesterase is an enzyme which is synthesized in the liver. The aim of the study was to evaluate the clinical utility of butrylcholinesterase as a discriminatory and prognostic factor in chronic liver disease patients...
2015: Clinical Laboratory
Ismail Isik, Ismail Celik
The present study was aimed to investigate the effects of subacute and subchronic treatment of some plant growth regulators (PGRs), such as abscisic acid (ABA) and gibberellic acid (GA3), on neurological and immunological biomarkers in various tissues of rats. The activities of acetylcholinesterase (AChE) and butrylcholinesterase (BChE) were selected as biomarkers for neurotoxic biomarkers. Adenosine deaminase (ADA) and myeloperoxidase (MPO) were measured as indicators for immunotoxic investigation purpose...
December 2015: Toxicology and Industrial Health
Preet Anand, Baldev Singh
Alzheimer's disease (AD), a progressive neurodegenerative disorder, is characterized by the deficits in the cholinergic system and deposition of beta amyloid (Aβ) in the form of neurofibrillary tangles and amyloid plaques. Since the cholinergic system plays an important role in the regulation of learning and memory processes, it has been targetted for the design of anti-Alzheimer's drugs. Cholinesterase inhibitors enhance cholinergic transmission directly by inhibiting the enzyme acetylcholinesterase (AChE) which hydrolyses acetylcholine...
April 2013: Archives of Pharmacal Research
Nilüfer Orhan, Didem Deliorman Orhan, Mustafa Aslan, Murat Süküroğlu, Ilkay Erdogan Orhan
ETHNOPHARMACOLOGICAL RELEVANCE: Galium species have been reported to be used against epilepsy in traditional Turkish folk medicine. AIM OF STUDY: The present work was undertaken to evaluate the in vivo anticonvulsant and in vitro neuroprotective effects of Galium spurium L. and to determine the major constituents by UPLC-TOF-MS. MATERIALS AND METHODS: Anticonvulsant activity of the aerial parts of Galium spurium was investigated using pentylenetetrazole, picrotoxin, and maximal electroshock-induced seizure animal models...
May 7, 2012: Journal of Ethnopharmacology
I Erdogan Orhan, G Orhan, E Gurkas
Cholinesterase enzyme family consisting of acetylcholinesterase (AChE) and butrylcholinesterase (BChE) is important in pathogenesis of Alzheimer's disease (AD), explained by "cholinergic hypothesis". Accordingly, deficiency of the neuromediator called "acetylcholine" excessive amount of BChE has been well-described in the brains of AD patients. Consequently, cholinesterase inhibition has become one of the most-prescribed treatment strategies for AD. In fact, cholinesterase inhibitors have been also reported for their effectiveness in some other diseases including glaucoma, myasthenia gravies, as well as Down syndrome, lately...
September 2011: Mini Reviews in Medicinal Chemistry
Asuman Kan, Ilkay Orhan, Gulay Coksari, Bilge Sener
Neuroprotective effect of the ethyl acetate and ethanol extracts of the silks of four Zea mays L. varieties (var. intendata, var. indurata, var. everta and var. saccharata) was evaluated by acetylcholinesterase, butrylcholinesterase and tyrosinase inhibitions and by antioxidant activity tests against 2,2-diphenyl-1-picrylhydrazyl and superoxide as well as two iron-related antioxidant methods (iron-chelation capacity and ferric-reducing antioxidant power). Total phenol and flavonoid contents in the extracts were determined spectrophotometrically...
February 2012: International Journal of Food Sciences and Nutrition
Saeedan Begum, M Iqbal Choudhary, Khalid M Khan
Fourteen N,N'-diaryl unsymmetrically substituted thioureas were synthesised and their cytotoxic (in vitro), phytotoxic (in vitro), acetylcholinesterase and butrylcholinesterase activities were determined. Thiourea 16 exhibited high, and 1 and 3 showed significant phytotoxic activity. Thioureas 1, 3, 4, 6 and 10 showed significant activity and 2, 6 and 7 indicated moderate cytotoxic activities. Compound 12 exhibited butrylcholinesterase activity higher than a standard reference.
2009: Natural Product Research
Iti Bansal, C K Waghmare, T Anand, A K Gupta, B K Bhattacharya
A time-course study was carried out to measure the acetylcholinesterase (AChE) gene expression in the brain of female rats exposed to different doses of sarin and physostigmine. Short-term effects were studied with an acute single subcutaneous dose (s.c.) of 80 microg kg(-1) (0.5 x LD(50)) sarin. Cortex and cerebellum showed a significant decline in AChE mRNA expression at 2.5, 24 and 72 h. Biochemical studies showed that plasma butrylcholinesterase (BChE) and brain AChE activities were significantly decreased at 2...
July 2009: Journal of Applied Toxicology: JAT
Karen Fildes, Lee B Astheimer, Paul Story, William A Buttemer, Michael J Hooper
Huge aggregations of flightless locust nymphs pose a serious threat to agriculture when they reach plague proportions but provide a very visible and nutritious resource for native birds. Locust outbreaks occur in spring and summer months in semiarid regions of Australia. Fenitrothion, an organophosphate pesticide, is sprayed aerially to control locust plagues. To evaluate fenitrothion exposure in birds attending locust outbreaks, we measured total plasma cholinesterase (ChE), butrylcholinesterase (BChE), and acetylcholinesterase (AChE) activities in four avian species captured pre- and postfenitrothion application and ChE reactivation in birds caught postspray only...
November 2006: Environmental Toxicology and Chemistry
L Bartorelli, C Giraldi, M Saccardo, S Cammarata, G Bottini, A M Fasanaro, A Trequattrini et al.
OBJECTIVE: Cholinesterase (ChE) inhibitors are the only medications approved for the treatment of Alzheimer's disease (AD). The features of ChE inhibitors differ considerably. In addition to acetylcholinesterase (AChE) inhibition, rivastigmine also inhibits butrylcholinesterase (BuChE), providing dual AChE and BuChE inhibition. An observational study was performed to determine the response in routine clinical practice to switching AD patients to rivastigmine from a selective AChE inhibitor when that treatment no longer delivered a satisfactory clinical response...
November 2005: Current Medical Research and Opinion
Gulberk Ucar, Nesrin Gokhan, Akgul Yesilada, A Altan Bilgin
Twelve 1-N-substituted thiocarbamoyl-3-phenyl-5-thienyl-2-pyrazoline derivatives were synthesized and their biological interactions with human plasma and erythrocyte acetylcholinesterase (AChE) and butrylcholinesterase (BuChE) enzymes were assessed. Compounds 3i-3l of newly synthesized N-substituted pyrazolines, which were presented as selective and irreversible MAO-B inhibitors in our previous report, were found to inhibit human erythrocyte and plasma AChE activities selectively and non-competitively suggesting that these compounds may interact with a region close to the peripheral site of the enzyme molecule which could shift the proper positioning of the catalytic center...
July 15, 2005: Neuroscience Letters
S W Moore, G Johnson
The association between the congenital absence of colonic ganglion cells and an increased acetylcholinesterase (AChE) expression in the affected tissue is of diagnostic importance in Hirschsprung's disease (HSCR). Investigation of AChE's function in development may also help unravel some of the complex pathophysiology in HSCR. Normal nerves do not stain for AChE, but increased AChE expression is associated with the hypertrophied extrinsic nerve fibres of the aganglionic segment in HSCR. Although a high degree of histochemical diagnostic accuracy exists, results are not always uniform, and false positives and false negatives are reported...
April 2005: Pediatric Surgery International
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