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The biochemical study of activity of serum cholinesterase in workers of industrial enterprise was carried out on the example of petrochemical industry. The indicators of average activity of enzyme and prevalence of indicators going beyond limits of reference values were analyzed depending on manufacturing-labor experience, profession and diseases established in workers. The main diseases, professional and labor experience groups were identified where activity of cholinesterase significantly changes. The impact of labor experience and profession on level of activity ofenzyme in blood serum is demonstrated.

Peganum Harmala L., Peganасеае widely distributed in Georgia. On the basis of chemical analysis of the composition of alkaloids it was found out that the plant contains quinazoline derivatives, among which dominats alkaloid d, 1 peganine: С11Н12NО2, m.p. 198-99ºC (СН3ОН). UV, λmax 275 (lgε 3,95). In IR-spectrum (KBr) 1625 cm- (-N=C) 3200-370 (OH)cm-1 . Mass- spectrum: М+ 171(100%). It was studied the dynamics of accumulation for total alkaloids and d, l - peganine: in the budding phase the amount of alkaloids was - 3,71%, d, l - peganine 0,07÷0,09%; in the phase of mass flowering the sum of alkaloids - 4,51% ,d, l - peganine - 0,1÷0,13%; in the phase of ripeness total alkaloids - 3.92%; d,l - peganine - 0,08÷0,1. The study of specific pharmacological activity showed that the d,l - peganine similar to peganine at a dose of 30 mg/kg causes a decrease in heart rate by 30÷40 beats/min, which is characteristic for anticholinesterases, in parallel with this, a decrease in cholinesterase activity in blood serum has been observed.

Changes in the activity of enzyme cholinesterase (ChE) have been experimentally investigated under the influence of amplitude-modulated super-high-frequency electromagnetic radiation (carrier frequency of 2.375 MHz; power flux density of 8 mW/cm2, 20 mW/cm2 and 50 mW/cm2; modulation frequency range 10 to 210 Hz; exposure time 5 min). The appearance of peaks of the cholinesterase increased relative activity, as well as the changes in the direction and intensity of the reaction associated with the modulation frequency and power flux are observed at equal power flux densities and exposure times.

The influence of cationic detergent cetyltrimethylammonium on the human blood cholinesterases activity (erythrocyte acetylcholinesterase and plasma butyrylcholinesterase) in reactions of hydrolysis of alpha-thionaphthylacetat and acetylthiocholine is studied. It is shown, that cetyltrimethylammonium is reversible effector for both cholinesterases. This compound competitively inhibited enzymatic hydrolysis of acetylthiocholine by both cholinesterases, and in the reactions of enzymatic hydrolysis alpha-thionaphthylacetat display as the synergistic activator--in experiments with butyrylcholinesterase, and as the reversible inhibitor--in experiments with acetylcholinesterase. Kinetic constants in reaction of acetylcholinesterase inhibition by cetyltrimethylammonium defined by means of different substrates--alpha-thionaphthylacetat and acetylthiocholin. They are close among themselves and amount (2.5 +/- 0.3) x 10(-5) and (2.8 +/- 0.3) x 10(-5) M, accordingly. Butyrylcholinesterase was more sensitive to influence of cetyltrimethylammonium. The kinetic constants defined for this enzyme by the effect of inhibition of acetylthiocholin hydrolysis or activation of alpha-thionaphthylatcetat hydrolysis, are also close among themselves and amount (3.9 +/- 0.4) x 10(-6) and (4.4 +/- 0.4) x 10(-6) M, accordingly.

The Aim: To study the efficiency of enteral nutritional support and its impact on clinical-laboratorial markers of hepatocellular failure of the patients with Child-Pue's hepatic cirrhosis type B suffering from trafologic impairment. MATERIAL AND RESEARCH METHODS: 61 patients with Child-Pue's hepatic cirrhosis type B suffering from trafologic impairment took part in the randomized prospective study. The control group (31 patients) got the conventional treatment with lactulose, beta-blocker, spironolactone on the basis of 1.2 g/kg protein weight and 30 kcal/kg body weight per day. There were 30 patients in the second group (the principal one) and in addition to conventional treatment they got the multisubstrate nutritional cocktail of dietary fibers on the basis of 0.3 g/kg protein weight, 7.5 g fibers per day and 10 kcal/kg body weight during 30 days. To evaluate the efficiency of the treatment we analyzed the clinical presentation and the intensity of blood cholinesterase. The stage of hepatic encephalopathy was defined with the affinity numbers test of Retainer. The parameters under study were checked before the treatment, 30 days and 60 days later after the treatment began., Results: It was found out during the prospective randomized study that the patients under nutritional support showed the positive clinical dynamics (asthenia and hepatic encephalopathy retrogression and the accurate increase of blood cholinesterase from 4365.4 +/- 1028.6 ME up to 5502.7 +/- 1142.6 ME (p < 0.05)., Conclusion: Nutritional support of the patients with Child-Pue's hepatic cirrhosis type B suffering from trafologic impairment is effective and has an accurate impact upon clinical-laboratorial markers of hepatocellular failure.

Aim: To determine the role of acetylcholine (AC), serotonine (5-HT) and cytokines in progression and complications of chronic alcohol pancreatitis (CAP)., Material and Methods: 50 CAP patients were examined in the exacerbation, remission and complications of CAP (48 males, 2 females) aged 30-50 years. Control group consisted of 15 healthy subjects. IL-1beta, IL-6, IL-8, IFN-gamma, TNF-alpha, IL-4 were studied with enzyme immunoassay, 5-HT--with Ch. Sadovanquivad method, AC and activity of cholinesterase (CE) in the blood--by the method of Sh. Hestrin. Pancreatic tissue fibrosis was assessed according to computer tomography findings., Results: Patients with CAP in exacerbation had significant rise of proinflammatory, anti-inflammatory cytokines, AC and 5-HT. In a complicated course of CAP there is a pronounced rise in TNFalpha in normal level of IL-4. CAP patients with destructive changes in the pancreas showed significant rise in the level of AC and 5-HT and lowering of cytokines. CE activity in complicated course of CAP is low this indicating protein-synthetic insufficiency in CAP patients., Conclusion: In CAP the action of 5-HT and AC aims at maintenance of secretory activity of the pancreas. In inflammation participation of neuromediators decreases. Stimulation of pancreatic secretory activity switched to autonomic regulation which is prognostically unfavourable.

The biochemical parameters of hepatobiliary system functions were studied in patients with opisthorchiasis and concomitant diseases, such as chronic viral hepatitis concurrent with chronic opisthorchiasis, as well as Ixodes tick-borne borreliosis in the presence of the same invasion. Although the magnitude ofbiochemical changes is not great in chronic opisthorchiasis or chronic viral hepatitis, the concomitance of these two diseases were ascertained to result in pronounced abnormalities, by demonstrating the exhaustion of spare capacities of the hepatobiliary system in parasitic invasion (or viral infection). When opisthorchiasis was concurrent with Ixodes tickborne borreliosis, some parameters under study differed from those in the groups of patients with monoinfections. Variance analysis showed that chronic opisthorchiasis had a great impact on carbohydrate and lipid metabolisms (glucose and cholesterol levels). The findings suggest that the formation of stable host-parasite relationships in chronic opisthorchiasis alters human metabolic processes and their compensatory capabilities.

The examination of the activity of serum amilase and cholinesterase in the blood from subjects who had died of heroin poisoning showed significant elevation of such activity. These findings allow experts to use the activity of the above enzymes as effective markers in detection of narcotic drugs in cadaveric blood, opiate narcotics, in particular.

The impact of the buffer capacity and of buffer nature on the effective activity of enzymes was demonstrated by the example of blood choline esterase (CE). The enzyme activity, when determined in vitro, is inversely related with a size of the buffer capacity. The substitution of sodium for potassium entails a changed activity in the phosphate buffers, e.g. in case of CE--by 30%, which essentially surpasses the influence of pH within a range of 7.0-8.0. A possible mechanism of the observed phenomenon is under consideration.

We studied fluorescence of 9-amino-1,2,3,4-tetrahydroacridine hydrochloride (tacrine) in the presence of serum cholinesterase. Quenching of tacrine fluorescence dependent on cholinesterase activity has been revealed. A quenching mechanism is proposed; it includes formation of a complex and charge transfer mediated by excited tacrine molecule as well as indole of tryptophan residue from the periphery of cholinesterase active site.

A response of a complex of biochemical parameters of hepatic function to therapeutic exposures was studied at different stages of development of Opisthorchis invasion. The activity of AST, ALT, GGT, GGT, AP, AM, and CE and the concentration of bilirubin, cholesterol, and glucose in the sera from 232 patients with acute or chronic opisthorchiasis were studied. Their study was conducted in several steps: before treatment, after a course of pathogenetic therapy, 1-3 days after antihelminthic therapy with bilthricide and azinox, in early (following 1-3 months) and late (following more than 6 months) residual periods. Pathogenetic therapy was found to alleviate an acute inflammatory process in the liver, but without eliminating cholestasis completely. Antihelminthic therapy improved the results of hepatic tests in different periods after treatment for acute or chronic opisthorchiasis in relation to the rate of compensation of structural lesions. By and large, after pathogenetic and antihelminthic therapy for opisthorchiasis the parameters characterizing the cytolytic syndrome became more rapidly than those that reflect the biliary system. However, there was no complete recovery of impaired hepatic and pancreatic functions throughout the follow-up.

The main biochemical indices of hepatic functions (the activities of alanine aminotransferase, aspartate aminotransferase, gamma-glutamyl transferase, alkaline phosphatase, alpha-amylase, choline esterase and the concentrations of total bilirubin, cholesterol, and glucose) were studied in the sera of 256 patients with chronic opisthorchiasis. It was found that with diseases manifested in different clinical forms (cholangitis, cholecystitis, cholangiocholecystitis, cholangiohepatitis, cholecystitis in combination with pancreatitis), most study indices are within the normal ranges, but significantly differ from the means in a group of apparently healthy individuals. The findings suggest that such clinical forms of opisthorchiais as cholangiocholecystitis and cholangiohepatitis are characterized by manifestations of cytolysis and cholestasis, as cholecystitis is manifested by cytolysis, as cholecystitis in combination with pancreatitis, by cholestasis, and as cholangitis, by cholestasis and hepatic cell insufficiency. It is possible that further studies will provide evidence for how to correct detected disorders during pathogenetic therapy.

Influence of dietary supplement Tinrostim-C on cholinesterase (ChE) activity and serum lipids peroxidation (LP) in patients whose work connects with emotional stress was examined. Activity of ChE was measured by Ellman calorimetric method (with acetylthiocholin as substrate), LP--by fluorimetric method with malone dialdehyde. Tinrostim-C was given three times a day in 0.5 g. On the 10th day of taking the preparation an activity of serum ChE increased 23.5% higher and had been staying higher during the whole period of observation. In vitro experiments showed an activating effect of Tinrostim-C and piracetam for serum ChE. The level of LP being initially higher was decreasing to values close to normal and had been staying at decreased level during the whole period of observation.

The influence of tritium oxide injected peritoneally of the range of activity of 5.5 MBq/g to 111 MBq/g versus gamma-radiation of 137Cs with decreasing dose rate in biochemical parameters of blood in rats was compared. It was shown that relative biological effectiveness of tritium oxide was higher than that for metabolism and it was equal to 1.5 in average.

Concentrations of the products of peroxide oxidation of lipids (POL), indices of the system of antioxidant defence (SAD), and the activity of 13 diagnostically significant organic/tissue specific enzymes (DSE) were determined in blood serum of cosmonauts who had participated in short (5-9 days, n = 8), long (125-179 days, N = 15), and superlong (241-366 days, n = 5) missions. To feature an interrelation of the indices under study, the canonical correlation analysis of a set of POL and SAP parameters and DSE activity was performed. Compared with pre-flight values, changes in the POL and SAP parameters were significant in serum only after the long-duration missions. Signs of POL activation were noted following the superlong missions. After the long-duration missions increased was the activity (mainly, within the norm) of DSEs, specific for the organs and tissues functioning of which is stressed in the period of post-flight readaptation (skeletal muscles, myocardium, liver). After the superlong missions, the DSE activity either remained essentially unchanged or decreased. In all the tested groups, highly reliable correlations between POL, SAP, and the DSE activity, traditionally applied in clinical diagnostics, were observed. These advocate for the use of POL and SAP indices in medical diagnostics and prognosis of cosmonauts' health.

The plasma activity of gamma-glutamyl transferase (GGT) and cholinesterase (CE) was assayed in 79 patients with opisthorchiasis in its active and chronic periods, as well in different periods after anthelminthic therapy with biltricide and azinox. The mean values of CE activity did not significantly differ between the groups of the examinees. The probability of decreased CE synthesis in the residual period was significantly greater in the treatment of chronic than acute opisthorchiasis. The maximum activity of GGT was found in acute opisthorchiasis, its values were also significantly higher than the control ones and remained unchanged within a year after anthelminthic therapy. Possible causes of delayed normalization of enzymatic activity following the treatment of chronic versus acute opisthorchiasis are discussed in the paper.

The data of long-standing research allowed to establish correlation between oxygen consumption different at various age and catecholamine (CA) content and acetylcholinesterase (AChE) activity in blood. Early postnatal age is characterised by adrenergic indexes of homeostasis manifesting in high CA content and AChE activity in blood and high quantities of consumed oxygen. After complete realisation of antigravitation reactions cholinergic indexes of homeostasis are revealed in the organism. They appear as essential decrease of AChE activity and CA content in blood and reduction of oxygen consumption. As a result negentropy tendencies of organism development increase and hence the adaptive and working capacities of the organism enhance. In the old age because of the decrease of skeletal musculature mass repeated and essential decrease of oxygen consumption takes place and it is due to the decrease of AChE activity in blood and the increase rather than decrease of CA content in blood. The organism converts to hypobiotic state with entropy tendencies of protracted and prolonged collapse.

Significant difference in catalytic properties of partially purified cholinesterases from blood serum of pigeon and hen was shown by photometric method using Ellman's reagent. From eight studied thioesters, pigeon cholinesterase hydrolysed with the highest rate butyrylthiocholine but hen cholinesterase--propionylthiocholine. The enzymatic hydrolysis obeyed Michaelis-Menten equation only at low concentration of substrates up to 0.15-0.5 mM. High concentration of substrates activated hen cholinesterase, but inhibited pigeon cholinesterase.

In reaction of hydrolysis of choline and thiocholine esters of carbonic acids at 25 degrees C, cholinesterase activity of the blood serum from the fish A. ballerus has been studied by modified Ellman's method and potentiometric titration method. The activity is maximal in pH region 7.5-9.0 and is not inhibited by high concentration of substrates. Michaelis constants and maximal rates for the enzyme reactions were determined. Butyrylcholine and butyrylthiocholine were hydrolyzed with the highest rates by the serum. Some of the organophosphorus inhibitors (diisopropylfluorphosphate and DDVF) inhibit cholinesterase activity of the blood serum significantly faster, whereas some of the carbamates (aminostygmin, eserine, etc.) inhibit it significantly slower than typical butyrylcholinesterase from horse blood serum and typical acetylcholinesterase of human erythrocytes. Besides, with respect to the sensitivity to inhibitors and some other properties, fish blood serum cholinesterase differs from other known cholinesterases.

Inhalation exposure to kuscide changed the function of the CNS, microcirculation, blood cholinesterase activity. Kuscide concentration 40 mg/m3 is toxic for rats, 4 mg/m3 is threshold, and 0.4 mg/m3 is nonactual. MAC of kuscide for working environment is 0.5 mg/m3.

A complex of enzymatic tests, characterizing the liver function and cellular cytolysis in patients with acute myocardial infarction of various severities (without complications and with various types of complications and outcomes) was used in examinations over the first week of the disease. Significant changes in five of the seven tested enzymes were found: aspartate aminotransferase, glutamate dehydrogenase, sorbitol dehydrogenase, cholinesterase, alanine aminotransferase, the degree and incidence of changes in their activities being the lowest in the patients with acute myocardial infarction without complications, higher in those with this condition with isolated complications, still higher in those with combined complications and a favorable outcome, and the highest in those with combined complications and a lethal outcome. Secondary hepatopathy in patients with acute myocardial infarction augments as the complications develop, particularly in arrhythmia, disordered conductivity, and combined complications. Measurements of glutamate dehydrogenase and sorbitol dehydrogenase are recommended starting from the first day of the disease, of cholinesterase from the third day of the disease for a dynamic monitoring of the liver status in order to timely detect and correct hepatopathy and assess the status of patients with complicated acute myocardial infarction.

On the grounds of physiological and hygienic studies comparative estimation of working conditions and functional state of workers' organisms is presented with regard to technologies used in hothouses. It was established that in assessment of professionally conditioned hazard not only the level of chemical substances (pesticides content in the air of working zone, quantities of preparations in skin wash-outs) but also the total duration of contact with xenobiotics matter. Complex of methods including detection of possible specific pesticide influence and tests reflecting general state of the body is suggested for use in clinical and hygienic investigations. Personal professional registers containing data on duration of work with toxic substances are recommended.

Female rats injected with organophosphate inhibitor of acetylcholinesterase chlorophose at doses of 10 mg/kg and 360 mg/kg showed less considerable decrease in blood acetylcholinesterase activity than did male animals. Females compared with males also demonstrated less expressed clinical symptoms of poisoning (salivation, convulsion) after injection of chlorophose at dose of 360 mg/kg. The value of LD50 in female rats was 860 mg/kg, whereas the comparable value in male animals was 700 mg/kg. Following the injection of atropine at doses of 0.1, 0.3, 0.6 mg/100 g female rats showed 2-3 fold increases in basal adrenal and plasma corticosterone levels, but significant decreases in stress-induced corticosterone levels. As for males, the basal and stress-induced values of corticosterone were not significantly affected by atropine administration. These results suggest that functional reserves of cholinergic system and responsiveness of the hypothalamic-pituitary-adrenal axis to cholinergic influence are greater in females than in males. It is concluded that cholinergic status is significantly higher in female rats than in male ones.

The pharmacological properties of a new drug approved in the USSR for the treatment of cholinolytics poisonings are described. The drug is as active as physostigmine. However, its action is longer. Aminostigmine exhibits marked central effects, which forms the basis for its use for elimination of brain dysfunctions caused by choline blockers.

Blood from the cat donor was perfused into the haemodynamically isolated cat brain. The changes of the vascular resistance and their capacity during the pharmacological activity of the endogenic cholinergic mechanism on the introduction of phosphacol into the bloodstream were investigated. Research has shown that the reduction of the activity of cholinergics leads to a decrease in pressure in the arteries of the brain and to an increase of the intercellular fluid absorption, caused by the neurogenic cholinergic influences. The possibility of a mediator realisation of the cholinergic influences on the brain vessels is discussed.

Examination was performed of 48 chronic sufferers with persistent hepatitis (PH), 70 with active hepatitis (AH) and 179 with hepatic cirrhosis (HC) by activity of cholinesterase (CE). Lowering of total CE activity proportional to hepatic cellular insufficiency was seen in decompensated HC and chronic AN. CE isoforms (7 in healthy subjects) furnished additional information about its activity. Marked hepatic cell insufficiency in HC patients warrants disappearance of 3-4 CE isoforms. The presence of only one or two of them suggests a lethal outcome. In chronic AN four or less CE isoforms predict development of HC.

Female mongrel albino rats were administered orally carbophos in a dose of 10 mg/kg (1/100 of LD50) on the 11th, 13th, 15th and 17th days of pregnancy. The antenatal administration of carbophos was shown to produce combined disturbances of the postnatal development of the mongrel albino rats manifesting themselves in changes of the maturation of sensomotor reflexes, cholinesterase activity, increased addiction both to carbophos and ethanol.

Two doses of butyphos (1/10 and 1/50 LD50) were administered into rats within 6 months. Content of DNA was distinctly decreased in liver and kidney tissues within the first 2 weeks of the pesticide administration. Then DNA synthesis was increased 2-fold in liver tissue and remained high during all the 6 months of intoxication. Protein synthesis was increased in liver tissue within 3 months of the administration and remained elevated up to the end of experiment. High rate of protein synthesis, found in kidney and spleen tissues at the initial steps, was markedly decreased within 6 months. Content of DNA and RNA was decreased in the tissues studied within 1 month of the intoxication and restored within 3 months, while it remained at considerably lower level in liver and spleen tissues as compared with control values. Cholinesterase activity was lowered by 90% in blood within 11 weeks with the subsequent increase; but in the experimental group intoxicated with butyphos at 1/10 LD50 the enzymatic activity constituted only 60% of control values within 6 months. Histological study showed development of necrodystrophy in liver tissue and of fibroplastic glomerulonephritis in kidney. The deteriorating effect of butyphos on cellular genome functions appears to relate not only to its cytotoxicity but also to the cancerogenic and mutagenic properties of the pesticide.

Studies have been made of the effect of several organophosphorus inhibitors, R1(R2)P(O) . SCH2CH2SR and R1(R2)P(O)SCH2CH2SRR . -O4SCH3 (or -I), which differ by the structure of split (R, P) and phosphoryl (R1, R2) parts of the molecule, on cholinesterase (ChE) from the brain of the fly Delia brassicae, acetylcholinesterase (AChE) of the bovine erythrocytes and butyrylcholinesterase (BuChE) from the blood serum of the horse. For fly ChE, higher values of a constant (kII) of the inhibition rate (at pH 7.5 and temperature 25 degrees C) were obtained both with thiophosphates and with thiophosphonates. This finding reveals higher reactivity of the active centre of this enzyme, as well as significantly lower selectivity of the latter to the structure of organophosphorus inhibitors. The data obtained suggest the existence of differences in the size of hydrophobic regions of anionic and esterase parts of the active centre in ChE of the fly and AChE of mammals, as well as the existence of some similarity between ChE of the fly and BuChE.

As many as 94 women of reproductive and climacteric age were subjected to clinical and laboratory studies. Women of reproductive age demonstrated abnormalities of menstrual function of the type of ovulatory and anovulatory hemorrhages. The group over 40 years manifested an early onset of menopause. Alcoholism standing was from 2 to 15 years. Study of the neurohumoral characteristics in women suffering from alcoholism during abstinence revealed a considerable lowering of serotonin content in the blood as compared with normals. The content of acetylcholine, the activity of genuine and false blood cholinesterase were increased in women suffering from alcoholism, pointing to excitation in the cholinergic system. During abstinence, women of reproductive and climacteric age suffering from alcoholism demonstrated discrepancy in the activity of the neuromediator systems.

Functional activity of the mediation cholinergic system (MChS) was studied in experiment in animals as well as in patients after appendectomy, gastric resection for ulcer disease of the stomach and duodenum, cholecystectomy. Clear changes of biochemical characteristics were established in the system of neurohumoral regulation during the first day of the development of functional intestinal obstruction. In later terms of development of the disease the progressing disturbance of balance in the MChS was responsible for the decompensated state of the organism and suppression of the motor function of the intestine. Drugs such as Desoxypeganin hydrochloride and Primperan must be included in curative measures.

Ethyl acetate was studied as an atmosphere contaminant in an enclosed environment. A 90-day continuous experiment on 160 white rats and 120 white mice with three concentrations of the compound (43, 10 and 2 mg/m3) was carried out. Ethyl acetate used in the first two concentrations caused functional disturbances in the state of animals and morphological changes in their viscera. Ethyl acetate at a concentration of 2 mg/m3 was ineffective. The data obtained allow recommendations of permissible concentrations of ethyl acetate vapours in an enclosed atmosphere in relation to a different time of man's exposure.