2,4,6-triphenyl-4h-selenipyrane as agent in treatment and prophylaxis of poisoning with arsenic compounds

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

 

I. Scope of application.

As a means for the treatment and prevention of poisoning by arsenic compounds.

II. The prior art.

A known method of using bis(benzoylmethyl)selenide (trade name - DAFS-25) the 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 [RF Patent №2051681, B. I. - 1996. No. 1], and as a means for the treatment and prevention of infectious diseases and poisonings [RF Patent №2171110, B. I. - 2001. No. 21]. Relatively low toxic drug (LD50=385 mg/kg) was tested in case of poisoning of animals by mycotoxins.

It is known that the use of sodium Selenite is able to reduce the severity of poisoning by arsenic, cadmium, lead and other [Hygienic criteria environment. 58. Selenium. - Geneva: world health organization. - 1989. - 270 S.]. However, it should be noted that sodium Selenite has a relatively high toxicity (LD50=7-9 mg/kg) [Worms D.K., Evdokimov, P.D., Wisher A.S. Drugs in veterinary medicine. The Handbook. / M.: Kolos, 1977, s].

It is known that aryl-substituted 4H-selenopyran are among the least toxic organic compounds of selenium (LD50>700 mg/kg), and can be the used as drugs possessing antimicrobial and antifirewall activity [Autospid. The USSR №1246566, B. I. - 1998. No. 10].

III. The essence of the invention.

The purpose of this invention is to find a drug that increases the resistance of animals and humans to poisoning by arsenic compounds.

Specified is achieved by introducing into the body of 2,4,6-triphenyl-4H-selenopyran, which is easily obtained from the corresponding 1,5-diketones and zinc selenide under conditions of acid catalysis [the Shaft B. I., Knots M.A., Filimonov A., Kharchenko VG Journal of General chemistry. - 1999. - T, issue 1. - P.84-85].

To study the ability of 2,4,6-triphenyl-4H-selenopyran to reduce the severity of poisoning by arsenic compounds (for example sodium arsenite) as the object of research were taken outbred white mice in vivo with an average weight of 20 g (19-22 g)from which they were created 3 control group and 5 experimental groups of ten animals each.

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 2,4,6-triphenyl-4H-selenopyran in olive oil in the amount of 10 μl per day for 14 days. 10 µl of olive oil were 16 µg 4H-selenopyran that for an animal weighing 20 g dose is 0.8 mg/kg of live weight.

The stomach is passed to a third 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 at 24-28 hours after injection of a solution into the body.

The animals of the fourth 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. After 20 hours after injection of the solution into mice were decapitation and selection of blood for analysis.

Animals of the fifth experimental group oral was administered sodium arsenite at concentrations of 45 mg/kg, and then, after 1 hour of the experiment, oral was administered 2,4,6-triphenyl-4H-selenopyran at a dose of 0.8 mg/kg after 24 to 28 hours 6 experimental animals died, the rest is monitored for 7 days. After a specified period the condition of the animals corresponded to the norm.

Animal sixth experimental group oral was administered for 14 days preparation 4H-selenopyran 10 μl per day. On day 14, after 1 hour after drug administration, animals were introduced a lethal dose of sodium arsenite. Through 26-28 hours killed four mouse, other individuals through 2 days regained their former state of health.

Animals seventh experimental group oral was administered for 14 days preparation 4H-selenopyran 10 μl per day. On day 14, after 1 hour after drug administration, animals bylawmen a lethal dose of sodium arsenite. After 20 hours were decapitation and selection of blood for analysis.

To compare the results by changing the concentration of certain biochemical parameters of blood held clinical-laboratory investigation of blood. The results of the study are presented in table 1.

The blood of the mice was carried out on the biochemical analyzer Screen master PLUS. Biochemical analyzer Screen master PLUS - semi-automatic biochemical analyzer. Specifies 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

Control (4N-selenopyran)
Table 1.
The quantitative content of the biochemical parameters
G, mmol/lB, g/lLDH, U/lM, mmol/lU, U/lAlat, U/lK, mmol/lX, mmol/l
Control (olive oil)6,9±0,240±32009±744,6±0,8369±424±354±31,43±0,3
9,4866341444,622162272,58
The sodium arsenite (group 4)2,81±0,370±36520±238,7±0,7113±326±0,252±41,45±0,3
4H-selenopyran + sodium arsenite (7)4,46±0,368±36360±234,0±0,774±322±0,240±41,24±0,3

* here and below, abbreviations used
1. D - glucose;
2. B - total protein;
3. LDH - lactate dehydrogenase;
4. M - urea;
5. S - alkaline phosphatase;
6. Alt - alanine Aminotransferase;
7. To - creatinine;
8. X - cholesterol.

To compare the results to change the state of internal organs in experimental and control groups spent the morbid anatomy investigated the E. The results of the study are presented in table 2.

Table 2.2.

The results of the weighing of the internal organs of mice in grams.
easyheartkidneykidneyliverpancreas
Control (olive oil)0,39±0,030.14±0,020,24±0,020,23±0,021,38±0,120,10±0,01
Control (4N-selenopyran)0,33±0,030,13±0,010,24±0,020,25±0,021,39±0,130,14±0,02
The sodium arsenite (group 4)0,18±0,020,12±0,010,23±0,020,22±0,010,88±0,100,02±0,01
4H-selenopyran + sodium arsenite (group 5)0,24±0,030,13±0,020,21±0,030,26±0,031,26±0,110,17±0,02
4H-selenopyran (14 days) + arsenite (7)0,25±0,030,14±0,020,22±0,030,21±0,021,27±0,13

On the basis of the conducted research it can be concluded that using the introduction of 2,4,6-triphenyl-4H-selenopyran can reduce the severity of poisoning by sodium arsenite.

The use of 2,4,6-triphenyl-4H-selenopyran as a means for the treatment and prevention of poisoning by arsenic compounds.



 

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