Means for treatment and prevention of poisoning with heavy-metal compounds

FIELD: medicine; veterinary.

SUBSTANCE: method describes the use of 2,4-diphenyl-7,8-benzo-5,6-dihydroselenochromen as a means of treatment and prevention of poisoning with heavy metal compounds.

EFFECT: higher resistance in animals and humans to poisoning with heavy-metal compounds.

8 tbl, 1 ex

 

The invention relates to the field of medicine and veterinary medicine and can be used as a means for the treatment and prevention of poisoning by heavy metals.

It is known the use of bis(benzoylmethyl)selenide (trade name - DAFS-25) General formula: (C6H5COCH2)2Se as a means for the treatment and prevention of diseases caused by deficiency of selenium in the body of farm animals and birds (see RF patent №2051681, IPC AC 33/04), and as a means for the treatment and prevention of infectious diseases and poisonings (see RF patent №2171110, IPC AC 33/04). This relatively low toxic, the preparation was tested for poisoning animals with mycotoxins.

Aryl-substituted 4H-selenopyran are among the least toxic organic compounds of selenium (LD50>700 mg/kg) and can be used as drugs with antimicrobial and antifirewall activity (see A.S. No. 1246566, IPC C07D 345/00).

Using 9-phenyl-s-octahydrophenanthrene (which structurally can be attributed to the condensed selenopyran) has a positive effect on animals, humans, and birds (see RF patent №2230523, IPC A61D 7/00; RF patent №2230524, IPC A61D 7/00; RF patent №2230525, IPC A61D 7/00; RF patent №2230526, IPC A61D 7/00).

It is established that at the moment only Selenite NAT the Oia reduces the severity of poisoning by arsenic compounds, cadmium, lead and others (see Hygiene criteria environment. 58. Selenium. - Geneva: world health organization. - 1989. - 270 C.). However, sodium Selenite has a relatively high toxicity (LD50=7-9 mg/kg) (see Worms D.K., Evdokimov, P.D., Wisher A.S., Drugs in veterinary medicine. The Handbook. / M.: Kolos, 1977, s). Therefore, the search among the selenium-containing organic compounds seems relevant.

The objective of this invention is to provide selectabase of the drug, which increases the resistance of animals and humans to poisoning by heavy metals.

Specified is achieved by introducing into the body of 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin.

This substance is easily obtained from the corresponding 1,5-diketone and zinc selenide under conditions of acid catalysis (see Fedotov O.V., the Shaft AB the Journal Chemistry of heterocyclic compounds". - 2006. No. 10. - S-1587). Found previously unknown property of 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin to reduce the severity of poisoning by heavy metals.

Investigated the ability of 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin to reduce the severity of poisoning by heavy metals, for example cadmium sulfate (CdSO4), cobalt chloride (CoCl2), nitrate mercury (Hg(NO3)2and Arsene is the sodium (Na 3AsO3). As object of research were taken outbred white mice in vivo with an average weight of 20 g (18-23 g)from which they were created 7 control groups and 4 experimental groups of ten animals each.

2,4-Diphenyl-7,8-benzo-5,6-dihydrohelenalin was introduced in the form of a solution of the oil from the calculation of 0.8 mg/kg (16 mg in 10 ml of olive oil). As salts of cobalt, cadmium, mercury and arsenic was administered dissolved in an appropriate volume of distilled water.

The blood of the mice was carried out on the biochemical analyzer Screen master PLUS. Biochemical analyzer Screen master PLUS - semi-automatic biochemical analyzer, determines the substrates, enzymes, electrolytes, hormones and some hematological parameters. Specifications: optical range - 6 filters; from 340 to 630 nm; linear range from 0,006 up to 2,500 opted Accuracy is 0.001 opted

Animals of the first control group orally was administered olive oil in the amount of 10 μl per day for 14 days.

Animals of the second control group orally injected with a solution of 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin (selenoprotein) in olive oil in the amount of 10 μl per day for 14 days. 10 µl of olive oil were 16 µg selenoprotein that for an animal weighing 20 g dose is 0.8 mg/kg of live weight (table 1, 3, 5, 7).

Animal is the third of the control group orally injected with a solution of 0.9 mg of sodium arsenite in 10 μl of distilled water, the animal weighing 20 g dose is 45 mg/kg of live weight. The death of experimental animals comes through 22-30 hours after introduction of the solution into the body.

The animals of the fourth control group orally injected with a solution of 0.9 mg of sodium arsenite (Na3AsO3in 10 µl distillirovannoi water for animal weighing 20 g dose is 45 mg/kg of live weight. After 20 hours after injection of the solution into mice were decapitation and selection of blood for analysis (table 1, 2).

Animals of the fifth control group orally injected with a solution of cobalt chloride (CoCl2) in an amount of 20 μl, with a dose of 200 mg/kg. the Operation was performed within 7 days, 7 days, 2 hours after the introduction of the toxicant produced decapitation. During decapitate collected the blood with subsequent clinical and laboratory study. The autopsy revealed that the internal organs are in a presumptive norm (table 3, 4).

Animals of the sixth control group orally injected nitrate mercury (Hg(NO3)2) in an amount of 10 μl, with a dose of 140 mg/kg of the Substance was administered for 7 days, 7 days, 2 hours after the introduction of the toxicant produced decapitation. During calitatii collected the blood with subsequent clinical and laboratory study. The autopsy showed profuse bleeding in the lungs, heart and liver (ABL, 6).

Animals seventh control group orally injected sulfate cadmium (CdSO4) in an amount of 10 μl, with a dose of 200 mg/kg of the Substance was administered for 7 days, 7 days, 2 hours after the introduction of the toxicant produced decapitation. During decapitate collected the blood with subsequent clinical and laboratory study. At autopsy observed bleeding in the lungs and heart (table 7, 8).

Animals of the first experimental group was administered 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin in the amount of 0.8 mg/kg over 1 hour was introduced Na3AsO3with a dose of 45 mg/kg, Four animals died after 20-30 hours. For the other animals were observed for 7 days and then spent the decapitation. During decapitate collected the blood with subsequent clinical and laboratory study. The results are shown in tables 1 and 2.

Table 1

The results of biochemical blood tests during the experiment with sodium arsenite
Biochemical pok lcontrolNa3AsO3selenoproteinNa3AsO3+selenoprotein
Glucose, mmol/l5±0,75 11,55±2,05p<0,023.98±0,63p<0,057,14±0,34p<0,01
LDH, u/l1117±1342109±151p<0,00120000±5144p<0,011720±158p<0,02
Lactate, u/l0,27±0,022,25±0,43p<0,00112,96±2,53p<0,00111,88±2,32p<0,001
Alkaline phosphatase, u/l102±10154±14p<0,02105±10p<0,05298±37,8p<0,001
AST, u/l90±3,6190±34p<0,02360±53,9p<0,001780±140p<0,001
Urea, mmol/l7,51±0,375,3±0,84p<0,057,3±0,36p<0,058,71±0,39p<0,05
Creatinine, g/l152±13,7115±10p<0,0175±for 9.64p<0,001125±12p<0,001
Albumin, g/l40±2,834,3±2,680±7,5p<0,00138±2,7p<0,001
Acting protein, g/l58±6,3872±1,9p<0,05105±16,9p<0,02156±29p<0,01
AST - aspartate aminotransferase

LDH - lactate dehydrogenase

Alkaline phosphatase alkaline phosphatase

p - significance level

Table 2

The results of the weighing of the internal organs, in grams
Bodies (g)NormaNa3AsO3Na3AsO3+selenoprotein
Intestine3,24±0,483,79±0,38p<0,024,67±0,39p<0,05
Liver1,92±0,231,57±0,19p<0,021,8±0,23p<0,01
Kidney0,44±0,040,54±0,03p<0,010,49±0,04p<0,05
Heart0,12±0,010,15±0,01p<0,010,16±0,01p<0,02
Light0,24#x000B1; 0,030,28±0,03p<0,0010,26±0,03p<0,01
Pancreas0,32±0,060,05±0,02p<0,010,13±0,02p<0,01

According biochemical parameters of blood of 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin has expressed no antitoxic effect against drug arsenic (activity indicator of liver enzymes remain high). However, mortality in the application of sodium arsenite in the control group was 100%, and there was a significant decrease in the weight of liver and pancreas. The application of 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin leads to complete restoration of liver mass and partial weight recovery of the pancreas and largely eliminates the mortality of animals.

Animals of the second experimental group oral was administered 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin (0.8 mg/kg), and after 1 hour was introduced CoCl2(200 mg/kg). The operation was conducted within 7 days, 7 days, 2 hours after the introduction of the toxicant produced decapitation. During decapitate collected the blood with subsequent clinical and laboratory study. The autopsy revealed that the internal organs are estimated norm of the Results are shown in tables 3 and 4.

Table 3

The results of biochemical blood tests during the experiment with cobalt chloride
Biochemical pok lcontrolCoCl2selenoproteinCoCl2+selenoprotein
Glucose, mmol/l5±0,757.78±0,49p<0,013.98±0,63p<0,058.22±0,48p<0,01
LDH, u/l1117±1343740±716p<0,0120000±5144p<0,0118000±3616p<0,001
Lactate, u/l0,27±0,020,81±0,14p<0,0112,96±2,53p<0,0017,56±1,21p<0,001
Alkaline phosphatase, u/l102±10306±42p<0,001105±10 p<0,05170±and 19.4p<0,01
AST, u/l90±3,6160±27,7p<0,05360±53,9p<0,001270±49,8p<0,01
Urea, mmol/l7,51±0,371,1±0,52p<0,0017,3±0,36p<0,057,1±0,34p<0,05
Creatinine, g/l152±13,755±44p<0,0575±for 9.64p<0,00175±9,65p<0,001
Albumin, g/l40±2,864±4,82p<0,00180±7,5p<0,00176±9,6p<0,01
Acting protein, g/l58±6,38148±26,5p<0,01105±16,9p<0,02100±10,1 p<0,01
Table 4

The results of the weighing of the internal organs, in grams
Bodies (g)NormaCoCl2CoCl2+selenoprotein
Intestine3,24±0,484,19±0,43p<0,0014,22±0,06p<0,05
Liver1,92±0,232,10±0,22p<0,021,77±0,22p<0,05
Kidney0,44±0,040,65±0,04p<0,010,38±0,03p<0,05
Heart0,12±0,010,16±0,01p<0,020,16±0,01p<0,01
Light0,24±0,030,34±0,03p<0,05 0,27±0,03p<0,02
Pancreas0,32±0,060,06±0,02p<0,010,15±0,02p<0,02

As a result of application of the drug is recovered, the mass of the kidneys, lungs and pancreas. The mass of all other organs is relatively normal.

Animals of the third experimental group oral was administered 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin (0.8 mg/kg), and after an hour of Hg(NO3)2(140 mg/kg). Substances were administered for 7 days, 7 days, 2 hours after the introduction of the toxicant produced decapitation. During decapitate collected the blood with subsequent clinical and laboratory study. In the absence of such noted profuse bleeding in the lungs, heart and liver. In the case of the use selenological connection hemorrhage is absent. The research results are summarized in tables 5 and 6.

Table 5

The results of biochemical blood tests during the experiment with nitrate of mercury
Biochemical pok lcontrol Hg(NO3)2selenoproteinHg(NO3)2+selenoprotein
Glucose, mmol/l5±0,758.85±1,15p<0,023.98±0,63p<0,055,11±0,75p<0,001
LDH, u/l1117±134481±18p<0,00120000±5144p<0,011849±260p<0,05
Lactate, u/l0,27±0,0271,98±12p<0,00112,96±2,53p<0,0014,58±0,9p<0,001
Alkaline phosphatase, u/l102±10304±44p<0,001105±10p<0,05312±43,5p<0,001
AST, u/l90±3,6120±12p<0,05360±53,9p<0,001170±17p<0,001
Urea, mmol/l7,51±0,372,18±0,46p<0,0017,3±0,36p<0,054,92±0,61p<0,01
Creatinine, g/l152±13,775±22p&t; 0,0275±for 9.64p<0,001110±6,6p<0,01
Albumin, g/l40±2,876±9,6p<0,0180±7,5p<0,00181±9,9p<0,01
Acting protein, g/l58±6,3882±compared to 8.26p<0,05105±16,9p<0,0298±12p<0,02

Table 6

The results of the weighing of the internal organs, in grams
Bodies(g)NormaHg(NO3) 2Hg(NO3)2+selenoprotein
Intestine3,24±0,48of 4.38±0,33p<0,015,03±0,29p<0,001
Liver1,92±0,231,85±0,23p<0,012,25±0,2p<0,02
Kidney0,44±0,040,53±0,02p<0,050,62±0,07p<0,05
Heart0,12±0,010,15±0,01p<0,050,17±0,02p<0,05
Light 0,24±0,030,26±0,03p<0,0010,22±0,03p<0,05
Pancreas0,32±0,060,06±0,01p<0,0010,14±0,04p<0,05

The activity of AST - corresponds to the norm. However, given the toxic effects of mercury salts on mice, it can be assumed that the normal activity of AST - a consequence of the inhibitory effect of mercury salts on the enzyme. This is confirmed by increased activity of AST in the presence selenological compounds, as well as with the joint use of mercury salts and selenoprotein. When the biochemical analysis of blood of mice treated with selenoprotein found negligible toxic effects of selenium in the liver of mice, resulting in increased enzyme activity of serum alkaline phosphatase and AST.

In a joint feeding mice a salt of mercury and selenoorganicheskikh the connection is detected by the normalization of biochemical parameters of blood serum.

As a result of application of the drug is recovered, the mass of the pancreas. The mass of all other organs is relatively normal.

The animals of the fourth experimental group oral was administered 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin (0.8 mg/kg), which after an hour CdSO 4(200 mg/kg). Substances were administered for 7 days, 7 days, 2 hours after the introduction of the toxicant produced decapitation. During decapitate collected the blood with subsequent clinical and laboratory study. At autopsy observed bleeding in the lungs and heart. In the case of the use selenological connection hemorrhage is absent. The research results are summarized in tables 7 and 8.

Table 7

The results of biochemical blood tests during the experiment with cadmium sulfate
Biochemical pok lcontrolCdSO4selenoproteinselenoprotein+CdSO4
Glucose, mmol/l5±0,759.54±0,75p<0,013.98±0,63p<0,055.95±0,63p<0,05
LDH, u/l1117±1344018±134p<0,0120000±5144p<0,0119516±3830R< 0,001
Lactate, u/l0,27±0,0265,0±0,02p<0,00112,96±2,53p<0,00111,13±2,22p<0,001
Alkaline phosphatase, u/l102±10430±10p<0,01105±10p<0,05128±2p<0,05
AST, u/l90±3,6290±3,6p<0,001360±53,9p<0,001210±39,8p<0,02
Urea, mmol/l7,51±0,371,03±0,37p<0,0017,3±0,36p<0,057,4±0,37p<0,02
Creatinine, g/l152±13,7*75±14p<0,00175±for 9.64p<0,00163±11,4p<0,001
Albumin, g/l 40±2,849±2,8p<0,00180±7,5p<0,00172±7,5p<0,01
Acting protein, g/l58±6,38112±6,4p<0,05105±16,9p<0,0278±4,3p<0,05
Table 8

The results of the weighing of the internal organs, in grams
Bodies (g)NormaCdSO4CdSO4+selenoprotein
Intestine3,24±0,483,38±0,48p<0,054,08±0,45p<0,001
Liver1,92±0,231,35±0,14p<0,051,92±0,23p<0,01
Kidney0,44±0,040,37±0,04p<0,0010,49± 0,04p<0,02
Heart0,12±0,010,12±0,01p<0,010,10±0,01p<0,01
Light0,24±0,030,24±0,03p<0,020,28±0,03p<0,02
Pancreas0,32±0,060,04±0,01p<0,010,09±0.01p<0,001

As a result of application of the drug is recovered, the mass of the kidneys, liver and pancreas. The mass of all other organs is relatively normal.

Thus, it is shown that application of 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin advisable in case of poisoning by salts of heavy metals.

The application of 2,4-diphenyl-7,8-benzo-5,6-dihydrohelenalin as a means for the treatment and prevention of poisoning by heavy metals.



 

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14 cl, 58 ex

FIELD: medicine.

SUBSTANCE: the present innovation deals with describing the efficient quantity of, at least, one heterocyclic compound of formula (I) or its salts, moreover, the compound of formula (I) should be chosen out of (i) the compounds of formula (III) or their salts, in which Z, Z' indicate O, X indicates S (thiazolidine dionic group), G indicates O or S; at least, one out of R2 and R3 indicates CF3, OR0 or COOR0, where R0 indicates H or saturated linear or branched C1-C20-alkyl and, preferably, C10-C10-alkyl, (ii) compounds (VI) or their salts: in which Z, Z' and G independently indicate O or S, at least, one out of R2 and R3 indicates hydrogen, CN, CF3, NO2, OR0, COOR0 or saturated linear or branched C1-C20-alkyl and, preferably, C1-C10-alkyl, possibly substituted OR0, where R0 indicates H or saturated linear or branched C1-C20-alkyl and, preferably, C1-C10-alkyl, (iii) compounds (VII) or their salts in which Z, Z' and G independently indicate O or S; R indicates saturated linear or branched C1-C10-alkyl; at least, one out of R2 and R3 indicates saturated linear or branched C1-C20-alkyl and, preferably, C1-C10-alkyl, NO2, OR0, where R0 indicates H or saturated linear or branched C1-C20-alkyl and, preferably, C1-C10-alkyl. The compounds in question reveal improved action upon stimulation of keratin fibers growth, particularly, human keratin fibers, that prevents their falling down and increases their density.

EFFECT: higher efficiency.

31 cl, 13 ex, 6 tbl

FIELD: organic chemistry, toxicology.

SUBSTANCE: invention describes a method for using 2,4,6-triphenyl-4H-selenopyrane as an agent for treatment and prophylaxis of poisoning with arsenic compounds. Sodium arsenite was used as a toxicant. Using the claimed preparation reduces lethality of animals up to 40-60% (100% in control group). Also, significant improving blood indices and visceral organs of animals occurred, i. e. the severity degree of poisoning was decreased.

EFFECT: enhanced effectiveness of agent.

2 tbl

FIELD: veterinary science, veterinary pharmacology.

SUBSTANCE: the present innovation deals with applying 3-O-acetyl-4"-O-isovaleryl-tylosine or its pharmacologically acceptable acidic-additive salt as an active agent for obtaining the desired veterinary preparation for treating and preventing Lawsonia-induced infections in swine, particularly, in case when this veterinary preparation is being a fodder additive or drinking water additive. It has been, also, suggested to apply veterinary medicinal preparation for treating and preventing Lawsonia-induced infections in swine that contains as active ingredients in the mixture of 3-O-acetyl-4"-O-isovaleryl-tylosine or its pharmacologically acceptable acidic-additive salt and tetracycline, at weight ratio ranged 1:5 up to 1:10 in which, particularly, tetracycline is being either chlorotetracycline or oxytetracycline.

EFFECT: higher efficiency of therapy and prophylaxis.

4 cl, 6 ex, 10 tbl

FIELD: medicine.

SUBSTANCE: the suggested compositions include taxol as a factor to inhibit the development of blood vessels and a pharmaceutically acceptable carrier. Also, it has been described the method of embolization of blood vessel dealing with the supply of therapeutically efficient quantity of the above-mentioned composition into the vessel mentioned. According to the innovation in question these compositions are nontoxic, thrombogenic, they don't change their form or physical properties during storage period before their application, they reveal no clotting signs at formation of large-sized particles in solution and after injection, they lead to slow release of the factor that inhibits the development of blood vessels.

EFFECT: higher efficiency.

18 cl, 22 dwg, 19 ex, 3 tbl

FIELD: organic chemistry, natural compounds, medicine, oncology.

SUBSTANCE: invention represents new saponin mixtures used for inhibition of initiation and activation of mammalian epithelial cell in pre-malignant or malignant state, for stimulation of apoptosis of mammalian malignant cell, prophylaxis of anomalous proliferation of mammalian epithelial cell, for treatment of inflammatory and regulation of angiogenesis in mammal. These mixtures are isolated form plants of species Acacia victoriae. Also, invention relates to methods for their applying. These compounds can comprise triterpene component, such as acacic or oleanolic acid to which oligosaccharides and monoterpenoid components are joined. Mixtures and compounds elicit properties associated with regulation of apoptosis and cytotoxicity of cells and strong anti-tumor effect with respect to different tumor cells.

EFFECT: valuable medicinal properties of compositions.

43 cl, 53 tbl, 50 dwg, 44 ex

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