Synthesis and preliminary biological evaluation of gabactyzine, a benactyzine-GABA mutual prodrug, as an organophosphate antidote.

Organophosphates (OPs) are inhibitors of acetylcholinesterase and have deleterious effects on the central nervous system. Clinical manifestations of OP poisoning include convulsions, which represent an underlying toxic neuro-pathological process, leading to permanent neuronal damage. This neurotoxicity is mediated through the cholinergic, GABAergic and glutamatergic (NMDA) systems.

Analytical determination of bioactive compounds as an indication of fruit quality.

The aim of this investigation was to determine the bioactive compounds in kiwifruit as an indication of quality after extraction using methanol and ethyl acetate. Using FTIR and three-dimensional fluorescence spectroscopy and electrospray ionization/MS, the contents of polyphenols, flavonoids, flavanols, and tannins, and the level of the antioxidant activity by 2, 2-azino-bis (3-ethyl-benzothiazoline-6-sulfonic acid) diammonium salt, 1, 1-diphenyl-2-picrylhydrazyl, ferric-reducing/ antioxidant power, and cupric reducing antioxidant capacity assays were determined and compared. It was found that the methanol extracts of kiwifruit showed significantly higher amounts of bioactive acetate extracts.

The influence of raw and processed garlic and onions on plasma classical and non-classical atherosclerosis indices: investigations in vitro and in vivo.

Garlic and white and red varieties of onion were subjected to processing by a variety of culinary methods, and bioactive compounds then determined. For in vivo studies, 84 male Wistar rats were randomly divided into 14 diet groups, each of six rats, including two control groups (one with no supplementation and one with cholesterol supplementation only). During the 30-day trial, the basal diets of the other 12 groups were supplemented with 1% cholesterol and raw or processed vegetables.

Concentration of bioactive compounds in mussels Mytilus galloprovincialis as an indicator of pollution.

The polycyclic aromatic hydrocarbons (PAHs), polychlorinated biphenyls (PCBs) and organotins were analyzed in mussels Mytilus galloprovincialis from polluted and unpolluted sites from Mokpo Bay, Korea. The total PAH's concentrations (10(-3)mgkg(-1)) measured by GC-MS were in the range from 31+/-23 to 1+/-1. Among the eight PAHs the predominant ones were fluoranthene, phenanthrene and pyrene and accounted approximately 63% of the total PAHs.

Osmium tetroxide: a new kind of weapon.

OsO4 is a powerful oxidizer. It affects mainly the skin and mucous membranes. Although unsuitable for a large-scale terrorist attack, mainly due to its scarcity, it could be used in small-scale attacks.

Bromine--the red cloud approaching.

Bromine is a strong and prevalent irritating agent that can spread both as liquid and as fumes. It has a characteristic reddish-brown color. The mainstay of the medical management is supportive and symptomatic therapy that should be given as soon as possible to prevent further damage.

Biochemical characteristics of the herb mixture Prolipid as a plant food supplement and medicinal remedy.

Prolipid a known mixture of herbs is used as a plasma lipid lowering medicine. No side effects were registered. However, the bioactive substances of Prolipid were not investigated.

The nutritional and metabolic indices in rats fed cholesterol-containing diets supplemented with durian at different stages of ripening.

The aim of this investigation was to assess the nutritional and health properties of Mon Thong durian cultivar at different stages of ripening. The assessment was carried out in vitro and in vivo. The contents of dietary fibers, minerals and trace metals at different stages of ripening were comparable.

Bioactivity of beer and its influence on human metabolism.

Extracted total phenols, flavanols and flavonoids were measured in beer samples and their quality as antioxidants was measured by two modified antioxidant methods: the 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonate) radical cation (ABTS * +) and the beta-carotene-linoleate model system (beta-carotene). It was found that the antioxidant potential of beer was well correlated with flavanols and flavonoids and was slightly lower with total polyphenols (R2 values from 0.8203 to 0.

[Cyanides--treatment beneath the shade of terror].

Although the use of cyanides as warfare agents has not been documented since the Iran-Iraq war in the 1980s, there are rising fears of cyanide being used by terrorists. An Al-Qaeda terror plot to use cyanide gas in the London Underground was foiled in 2002. The threat of similar events becomes more imminent in light of the terror attacks in our country and worldwide, accompanied by statements and threats by fundamentalist leaders to employ chemical weapons.

Effect of ethylene treatment on kiwifruit bioactivity.

Unlabelled: The consumption of fruits and vegetables with high antioxidant activities leads to best healthful results. Therefore, in the present investigation we tried to find the peak of the kiwifruits antioxidant activity during the first 10 days of ethylene treatment (100 ppm at 20 degrees C). In order to receive the most reliable data five different antioxidant assays were used: ferric-reducing/antioxidant power (FRAP); cupric reducing antioxidant capacity (CUPRAC); trolox equivalent antioxidant capacity (TEAC); 1, 1-diphenyl-2-picrylhydrazyl radical (DPPH); and Folin-Ciocalteau.

Dose-dependent influence of commercial garlic (Allium sativum) on rats fed cholesterol-containing diet.

The aim of this investigation was to evaluate the dose-dependent influence of commercial garlic on rats fed cholesterol-containing diets. It was found that commercial garlic contains high concentrations of dietary fibers, microelements, and total polyphenols, and its total antioxidant capacity as determined by two independent assays [1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS)] was similar to that of the original garlic samples. Wistar rats (35) were randomly divided into five diet groups, named control, Chol, Garlic500, Garlic750, and Garlic1000.

Red grapefruit positively influences serum triglyceride level in patients suffering from coronary atherosclerosis: studies in vitro and in humans.

The contents of the bioactive compounds in red and blond grapefruits and their influence on humans suffering from hypertriglyceridemia were studied. It was found that red grapefruit has a higher content of bioactive compounds and a higher antioxidant potential than blond grapefruit, determined by oxygen radical scavenging capacity, 1,1-diphenyl-2-picrylhydrazyl, carotenoid bleaching, and Folin-Ciocalteu assays. Fifty-seven hyperlipidemic patients, ages 39-72 years, after coronary bypass surgery, recruited from the Institute's pool of volunteers, were randomly divided into three equal in number (19) groups: two experimental (red and blond groups) and one control group (CG).

[Political poisoning with dioxins--a weapon of chemical "disgracefulness"].

The recent attempt to poison Ukrainian President, Viktor Yuschenko with dioxins, raised public concern regarding this toxic chemical. In industrial countries, there is a constitutive exposure of humans to dioxin compounds, which are formed as by-products in manufacturing processes of various chlorinated organic chemicals and in waste incinerators. Dioxins are extremely stable in the environment and have a low turnover rate in the body--sometimes they are detected years after the original exposure.

Pharmacologic prophylaxis against nerve agent poisoning.

Nerve agent poisoning is characterized by the rapid progression of toxic signs, including hypersecretions, tremor, convulsions and profound brain damage. In the political arena of today's world, the threat of nerve agent use against military troops has prompted armies to search for prophylactic protection. The two main strategies for prophylaxis include biological scavengers that can bind or cleave nerve agents before they react with acetylcholinesterase, and antidotes as prophylactic treatment.

Adverse reaction to atropine and the treatment of organophosphate intoxication.

Atropine is the drug of choice for treatment of organophosphate nerve agent and insecticide intoxication and has been used for this indication for several decades. Adverse reactions to atropine may occur, and are of two types: toxic and allergic. Toxic reaction, the most common form, results from the anti-muscarinic effects of the drug.

Bretazenil, a benzodiazepine receptor partial agonist, as an adjunct in the prophylactic treatment of OP poisoning.

Benzodiazepines, mainly diazepam, are commonly used as anticonvulsants in the treatment of organophosphate casualties. Although very effective, diazepam usually is not used in prophylactic treatments because of its adverse effects on task performance and its abuse liability. Benzodiazepine (BZ) partial agonists are unique in that they are able to occupy all the population of a given receptor without eliciting the maximal physiological response.

Catalytic antibodies: generation, nature, and possible role as chemical warfare scavengers.

Nearly three decades have passed since the idea was proposed that antibodies may provide catalytic activity as enzymes. Since then the term "catalytic antibodies" has gained more and more popularity. Numerous antibodies enhancing the rate of reactions have been described.

Creatine kinase activity decrease with short-term freezing.

Freezing of serum samples at -30 degrees C without protective agents is the simplest and least expensive method of storage in serum banks. We investigated the stability of creatine kinase (CK) in human sera after freezer storage under such conditions for 24 h (n = 30) or for 2 or 4 weeks (n = 99). CK activity was measured in fresh sera and compared to matched thawed sera after freezer storage at the designated time intervals.

The effect of substituted aminoalkylaminoanthraquinones on eukaryotic cells.

Nine aminoalkylaminoanthraquinones (I-IX) were evaluated for their cytotoxic potency against normal and malignant mammalian cells. The 1.8-di-(aminopropylamino) derivative (VIII) exhibited significant activity against several tumor cell systems and had some selectivity.

Zwitterionic analogues of cimetidine as H2 receptor antagonists.

A series of analogues of the H2 receptor histamine antagonist cimetidine have been synthesized in which the dipolar cyanoguanidine group has been replaced by a number of zwitterionic moieties. Although none of the compounds is more effective than cimetidine in blocking histamine-stimulated tachycardia on the isolated guinea pig atrium, the activities of most of the compounds possessing rigid dipoles can be accounted for on the basis of dipole orientation relative to the common side chain and by considering the active species in each case to be the zwitterion. These findings are in general agreement with those found for analogues having conjugated groups as dipoles.