Diazinon Toxicokinetics, Tissue Distribution and Anticholinesterase Activity in the Rat

The toxicokinetics, tissue distribution, and anticholinesteruse (antiChE ) activity of diazinon were investigated in the rat. Plasma concentrations most adequately fitted a two-compartment open model after iv administration of 10 mg/kg and a one-compartment model after oral administration of 80 mg/kg. Diazinon elimination half-life following iv and oral dosing was 4.70 and 2.86 h, respectively. The oral bioavailabllity was found to be low (35.5%). Hepatic extraction ratios after iv administration of 5 or 10 mg

STUDIES ON THE RELATIONSHIP BETWEEN THE MO REACTIVITY INDICES AND REVERSIBLE ANTICHOLINESTERASE ACTIVITY OF CUIXINGNING

Reversible anticholinesterase (anti-ChE)agents can inhibit the function of acetylcholinesterase (AChE)temporarily and have been used in the treatment of glaucoma and myasthenia gravis, and recently used as analeptic for anesthesia, to improve the efficiency of learning and memory impairment.

Phytochemical profile and ABTS cation radical scavenging,cupric reducing antioxidant capacity and anticholinesterase activities of endemic Ballota nigra L.subsp.anatolica P.H.Davis from Turkey

Objective:To evaluate the chemical compositions and biological activities of an endemic Ballota nigra L.subsp.anatolica P.H.Davis.Methods:Essential oil and fatty acid composition were determined by GC/MS analysis.ABTS cation radical decolourisation and cupric reducing antioxidant capacity assays were carried out to indicate the antioxidant activity.The anticholinesterase potential of the extracts were determined by Ellman method.Results:The major compounds in the fatty acid composition of the petroleum ether extract were identified as palmitic(36.0%)and linoleic acids(14.3%).The major components of essential oil were 1-hexacosanol(26.7%),germacrene-D(9.3%)and caryophyllene oxide(9.3%).The water extract indicated higher ABTS cation radical scavenging activity than α-tocopherol and BHT,at 100μg/mL.The acetone extract showed 71.58 and 44.71%inhibitory activity against butyrylcholinesterase and acetylcholinesterase enzyme at 200μg/mL,respectively.Conclusions:The water and acetone extracts of Ballota nigra subsp.anatolica can be investigated in terms of both phytochemical and biological aspects to find natural active compounds.

Synthesis and anticholinesterase activity of a novel series of acetazolamide condensed 1,4-dihydropyridines

A novel Acetazolamide condensed 1,4-dihydropyridines was set up by treating of N-(5-acetamido-1,3,4-thiadiazol-2-ylsulfonyl)-3-oxobutanamide with an aryl aldehyde and 25-30%alkali with sight amount of barium nitrate as a catalyst.Confirmation of the synthetic structure of the titled compounds(4-16)was substantiated by thin-layer chromatography(TLC),IR,^(1)H NMR,^(13)C NMR,Mass spectra(MS)and elemental analysis(C,H,and N)were finished.The titled compounds were assessed for anticholinesterase activity against acetylcholinesterase and butyl cholinesterase enzymes.The titled compound produced weak,moderate,or high anticholinesterase activity.Particularly,compound 8 demonstrated the best anticholinesterase activity of all the 1,4-dihydropyridines,with an IC_(50) estimation of 0.08μM and 2.9μM.

Analysis of chemical composition and bioactive property evaluation of Indian propolis

Objective:To analyze the chemical composition and to evaluate the bioactive potential of hydroalocoholic extract of propolis.Methods:Ethanol extract of propolis was analyzed by GCMS,HPTLC and HPLC methods and in vitro antioxidant,anticholinesterase and cytotoxicity assay were performed.Remits:GC-MS analysis revealed the presence of fatty acids,alcohols, and quercetin.Quercetin was identified and quantified by HPTLC and HPLC methods.Dose dependent DPPH and hydroxyl radical scavenging activity of hydroalcoholic extract of propolis was calculated as 16.20 and 34.33 μg/mL respectively.Inhibition of lipid peroxidation was significant and the IC_(50) value was calculated as 55.56 μg/mL.Anticholinesterase activity was less observed.The cytotoxic activity against both breast(MCF-7) and lung cancer(A543) cell lines were significant and the IC_(50)value was calculated as 10 and 13 μg/mL respectively.Conclusions: These findings showed that bioactive compounds present in propolis will alleviate many diseases and can be used for better human health.

Intestinal pseudo-obstruction:An uncommon condition with heterogeneous etiology and unpredictable outcome

Intestinal pseudo-obstruction (IPO) either acute or chronic is a condition including features of intestinal ileus in absence of mechanical obstruction. Our paper presents such a rare case of idiopathic IPO in a 53-year-old male patient with recurrent episodes of pseudo-obstruction, which were successfully resolved by anticholinesterase agents, motilin agonists or colonic decompression. However, the patient finally underwent total colectomy. Huge colonic dilatation was identified intraoperatorily, while histology showed a neuropathic variant of chronic intestinal pseudo-obstruction. Etiologic mechanisms and current therapeutic methods are reviewed in this paper, which concludes that IPO is a condition in which conservative treatment usually fails. Total colectomy with ileoanal pouch may be the only solution in these situations.

Biological activities of the Ornithogalum orthophyllum and its in silico ADMET profile

Background:The bulbs and aerial parts of Ornithogalum are used in Turkey both as food and to treat various ailments,and some of its medical applications are well known.However,the biological activities of Ornithogalum orthophyllum have not yet been investigated.The objective of this study was to examine the antioxidant,urease and cholinesterase enzyme inhibition,and cytotoxic activities of different extracts obtained from the bulb and aerial parts of the O.orthophyllum plant.In addition,the absorption,distribution,metabolism,excretion,and toxicity properties of some phenolic compounds in plants were examined in silico.Methods:The antioxidant activity of the extracts obtained from the aerial parts of O.orthophyllum was investigated using the 2,2-diphenyl-1-picrylhydrazyl,2,2-azinobis(3-ethylbenzothiazoline-6-sulphonic acid),ferric reducing antioxidant power,and cupric reducing antioxidant capacity methods.Urease and cholinesterase enzyme inhibition were determined by using the indophenol and Ellman methods,respectively.The cytotoxic activity of the extracts was measured using a test based on the luminometric readings of the adenosine triphosphate levels of the cells.pkCSM,a free online web server(http://structure.bioc.cam.ac.uk/pkcsm)was used to predict the properties of the compounds analyzed.Results:The methanol extract of the aerial parts of O.orthophyllum was observed to have strong antioxidant and acetylcholinesterase enzyme inhibition potential.The petroleum ether extract of the aerial parts showed the highest anti-urease activity.The chloroform extract of the aerial parts exhibited the highest cytotoxic effect against A431 human epidermoid carcinoma cells.The absorption percentages of protocatechuic acid,p-hydroxybenzoic acid,vanillic acid,and p-coumaric acid compounds from the small intestine were between 71.17%and 93.49%,which were quite high.All the compounds were predicted to be unable to penetrate the central nervous system due to their inability to cross the blood-brain barrier.Not all compounds analyzed were predicted to have mutagenic,hepatotoxic,or minnow toxicity effects.Conclusion:The extracts obtained from the aerial parts of O.orthophyllum have strong biological activity and contain compounds that are well-absorbed and do not have mutagenic,hepatotoxic,or minnow toxicity effects,suggesting that they can be used as natural medicinal and nutritional sources in the future.

Hormetic response of cholinesterase from Daphnia magna in chronic exposure to triazophos and chlorpyrifos

In vivo activity of cholinesterase （ChE） in Daphnia magna was measured at different time points during 21-day exposure to triazophos and chlorpyrifos ranging from 0.05 to 2.50 μg/L and 0.01 to 2.00 μg/L, respectively. For exposure to triazophos, ChE was induced up to 176.5% at 1.5 μg/L and day 10 when measured by acetylthiocholine （ATCh）, whereas it was induced up to 174.2% at 0.5 μg/L and day 10 when measured by butyrylthiocholine （BTCb）. For exposure to chlorpyrifos, ChE was induced up to 134.0% and 160.5% when measured by ATCh and BTCh, respectively, with both maximal inductions detected at 0.1 Ixg/L and day 8. Obvious induction in terms of ChE activity was also detected in daphnia removed from exposures 24 hr after their birth and kept in a recovery culture for 21 days. Results indicated that the enzyme displayed symptoms of hormesis, a characteristic featured by conversion from low-dose stimulation to high-dose inhibition. In spite of that, no promotion in terms of reproduction rate and body size was detected at any tested concentrations regardless of whether the daphnia were collected at end of the 21-day exposure or at end of a 21-day recovery culture. This suggested that induction of ChE caused by anticholinesterases had nothing to do with the prosperity of the daphnia population.