physostigmine/rak

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Modulation of immune functions in polymorphonuclear neutrophils induced by physostigmine, but not neostigmine, independent of cholinergic neurons.

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BACKGROUND Cholinesterase inhibitors (Ch-I) improve survival in experimental sepsis consistent with activation of the cholinergic-anti-inflammatory-pathway. So far, less is known about whether Ch-I have a direct immunomodulatory effect on immune cells (polymorphonuclear neutrophils, PMN) in the

A phase I trial of spirohydantoin mustard (NSC 172112) in patients with advanced cancer.

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Spirohydantoin mustard (spiromustine, NSC 172112) is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors. The rationale was to combine the reactive moiety of an active antitumor agent with the hydantoin part of the molecule,

UHPLC/GC-qTOF-MS metabolomics, MTT assay, and molecular docking studies reveal physostigmine as a new anticancer agent from the ethyl acetate and butanol fractions of Kigelia africana (Lam.) Benth. fruit extracts

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Kigelia africana plant is widely used as an herbal remedy in preventing the onset and the treatment of cancer-related infections. With the surge in the research interest of the plant, the specific chemical compound or metabolite that confer its anticancer properties has not been adequately

Cholinergic toxic syndrome by the anticancer drug irinotecan: acetylcholinesterase does not play a major role.

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BACKGROUND The anticancer drug irinotecan induces cholinergic side effects that are currently ascribed to the blockade of acetylcholinesterase. This study investigated (1) the pattern of acetylcholinesterase activity in patients receiving treatment with irinotecan and (2) the relationship between

Improved methodology for intracellular enzyme reaction and inhibition kinetics by flow cytometry.

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Flow cytoenzymology is the determination of enzyme activities or concentrations in single intact cells. Using the flow cytometer built and designed in our laboratory and recent modifications to hardware and software, we have developed an improved dynamic flow cytoenzymological procedure for the

Human arylacetamide deacetylase is a principal enzyme in flutamide hydrolysis.

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Flutamide, an antiandrogen drug, is widely used for the treatment of prostate cancer. The initial metabolic pathways of flutamide are hydroxylation and hydrolysis. It was recently reported that the hydrolyzed product, 4-nitro-3-(trifluoromethyl)phenylamine (FLU-1), is further metabolized to

Central anticholinergic syndrome vs. idiosyncratic reaction triggered by a small IV dose of atropine.

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A 58-year-old male was scheduled to undergo radical gastrectomy for cancer under general anesthesia. The patient developed agitation and irregular breathing after receiving a single dose of atropine (0.5 mg) to treat bradycardia immediately prior to induction of anesthesia. Within 5 min after the

Treatment of opioid-induced delirium with acetylcholinesterase inhibitors: a case report.

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A 55-year-old woman with advanced ovarian cancer and severe pain developed hypoactive delirium after an increase in her opioid dosage. Myoclonus and delirium improved dramatically with the intravenous injection of the acetylcholinesterase inhibitor physostigmine, and this improvement was maintained

A pediatric phase I and pharmacokinetic study of spirohydantoin mustard.

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A pediatric Phase I and pharmacokinetic study of the lipophilic alkylating agent spirohydantoin mustard (SHM) was conducted in 23 patients. The dose-limiting toxicity of SHM was neurological with disorientation, delirium, or hallucinations occurring in 9 of 23 patients. These symptoms were partially

Natural products as probes for new drug target identification.

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One traditional aspect of natural products in medical research has been their use in the identification and investigation of the physiological/pathological role of receptors and enzymes as possible targets for drug design programmes. Classical examples of this function of natural products in drug

[Anti-inflammatory effect of acetylcholine on lipopolysaccharide induced inflammatory response of alveolar macrophages].

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OBJECTIVE To observe the effect of acetylcholine (ACh) on lipopolysaccharide (LPS) induced inflammatory model of rat alveolar macrophages, and to observe the effect of the acetylcholinesterase inhibitor physostigmine (Phy) on the anti-inflammatory effect of ACh. METHODS The rat alveolar macrophages

Composition and cytotoxic and antioxidant activities of the oil of Piper aequale Vahl.

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BACKGROUND Piper aequale Vahl is a small shrub that grows in the shadow of large trees in the Carajás National Forest, Municipality of Parauapebas, Para state, Brazil. The local people have used the plant against rheumatism and inflammation. METHODS The essential oil of the aerial parts was

Senile dementia of the Alzheimer type.

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The prevalence of severe dementia in the United States is about 1.3 million cases, of which at least 50 to 60% are of the Alzheimer type. Severe dementia of the Alzheimer type is found rarely in a clearly dominant pattern, although often one or more relatives are affected. Down's syndrome in adults

Corticosterone primes the neuroinflammatory response to Gulf War Illness-relevant organophosphates independently of acetylcholinesterase inhibition.

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Gulf War Illness (GWI) is a chronic multi-symptom disorder affecting veterans of the 1991 Gulf War. Among the symptoms of GWI are those associated with sickness behavior, observations suggestive of underlying neuroinflammation. We have shown that exposure of mice to the stress hormone,

Pharmacologic cholinesterase inhibition improves survival in experimental sepsis.

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OBJECTIVE Lethal sepsis occurs when an excessive inflammatory response evolves that cannot be controlled by physiologic anti-inflammatory mechanisms, such as the recently described cholinergic anti-inflammatory pathway. Here we studied whether the cholinergic anti-inflammatory pathway can be

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