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.
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
|The quantitative content of the biochemical parameters|
|G, mmol/l||B, g/l||LDH, U/l||M, mmol/l||U, U/l||Alat, U/l||K, mmol/l||X, mmol/l|
|Control (olive oil)||6,9±0,2||40±3||2009±7||44,6±0,8||369±4||24±3||54±3||1,43±0,3|
|The sodium arsenite (group 4)||2,81±0,3||70±3||6520±23||8,7±0,7||113±3||26±0,2||52±4||1,45±0,3|
|4H-selenopyran + sodium arsenite (7)||4,46±0,3||68±3||6360±23||4,0±0,7||74±3||22±0,2||40±4||1,24±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.
The results of the weighing of the internal organs of mice in grams.
|Control (olive oil)||0,39±0,03||0.14±0,02||0,24±0,02||0,23±0,02||1,38±0,12||0,10±0,01|
|The sodium arsenite (group 4)||0,18±0,02||0,12±0,01||0,23±0,02||0,22±0,01||0,88±0,10||0,02±0,01|
|4H-selenopyran + sodium arsenite (group 5)||0,24±0,03||0,13±0,02||0,21±0,03||0,26±0,03||1,26±0,11||0,17±0,02|
|4H-selenopyran (14 days) + arsenite (7)||0,25±0,03||0,14±0,02||0,22±0,03||0,21±0,02||1,27±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.
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to biologically active substances displaying perspective using medicine, veterinary science, cosmetics and dairy industry. Agent comprises polyoxyarylene ester and hydroquinone in their ratio from 83:17 to 5:95, respectively. Agent comprises 2-(1-oxy-4-hydroxyphenylene)benzoquinone or 4-hydroxyphenylene-2,4-dioxybenzene as a polyoxyarylene ester. Method for preparing agent involves mixing polyoxyarylene ester with hydroquinone and wearing the prepared mixture up to formation of the uniform mass. Invention provides creature of a novel agent of the broad spectrum of effect, namely: antioxidant, antihypoxic, antitumor, radioprotective, immunostimulating and biocide effects.
EFFECT: valuable properties of agent.
7 cl, 20 tbl, 16 ex
SUBSTANCE: claimed adsorbent contains spherical activated carbon having size diameter of 0.01-1 mm, specific surface determined in accordance to Langmuir equation of 1000 m2/g or more, ratio of diffraction intensities R of 1.4 or more (R is determined as R = (I15-I35)/(I24-I35) (1), wherein I15 is diffraction intensity at diffraction angle (2θ) of X-ray diffraction is 15°C; I35 is diffraction intensity at diffraction angle (2θ) of X-ray diffraction is 35°C; I24 is diffraction intensity at diffraction angle (2θ) of X-ray diffraction is 24°C), and pore volume having diameter of 7.5-15000 nm is less than 0.25 mg/ml. In another embodiment claimed adsorbent contains abovementioned spherical activated carbon with modified surface. Also disclosed are pharmaceutical composition and method for prevention or treatment of kidney or liver diseases containing said adsorbent.
EFFECT: new adsorbent for peroral administration.
20 cl, 5 ex, 2 tbl, 12 dwg
FIELD: organic chemistry, medicine, hepatology.
SUBSTANCE: invention relates to using 2-methylthiopyrimido[4,5-b]indole of the formula (1): showing melting point at 243°C (with decomposition) and value LD50 > 1000 mg/kg used in liver protection from poisoning with carbon tetrachloride. Proposed compound exceeds activity of the "Essentiale" as a comparison preparation.
EFFECT: valuable medicinal property of compound, enhanced effectiveness.
FIELD: pharmaceutical industry.
SUBSTANCE: claimed adsorbent contains spherical active carbon, obtained from thermosetting resin as carbon source, having particle size of 0.001-1 mm, specific surface determined by Langmuir adsorption equation of 1000 m2/g or more and pore volume of 7.5-15000 nm in diameter less than 0.25 ml/g. Also disclosed is adsorbent being similar to abovementioned one, wherein total content of acidic groups is 0.40-1.00 meq/g; total content of basic groups is 0.4-1.1 meq/g. Pharmaceutical compositions contain said adsorbents and pharmaceutically acceptable carriers and recipients. Agents of present invention are useful in treatment of kidney or liver diseases or disorders associated with uremic substance by administration of said adsorbents.
EFFECT: products of increased selectivity.
21 cl, 5 ex, 2 tbl, 11 dwg
FIELD: chemical and pharmacological industry.
SUBSTANCE: invention relates to encapsulated form of Acyzol containing Acyzol and pharmaceutically acceptable fillers in specific component ratio.
EFFECT: encapsulated mass with high technological characteristics, high biological availability and effectiveness of Acyzol component.
5 tbl, 3 dwg
FIELD: veterinary science.
SUBSTANCE: in case of dioxine intoxication animals should be prescribed with dimephosphon at the dosage of about 50-150 mg/kg body weight daily for 10-30 d. The innovation provides decreased embryonic lethality in animals.
EFFECT: higher efficiency of therapy.
3 ex, 1 tbl
FIELD: medicine, toxicology.
SUBSTANCE: invention proposes applying 15% aqueous solution of 1-methyl-5-[2'-(benzyldimethylammonio)ethyl]carbamoyl pyridinium-2-aldoxime dichloride that exceeds the 15% solution of dipiroxime (TMB-4, trimedoxime bromide) used in native medicinal practice by the curative effectiveness. Invention can be used in urgent treatment of acute poisoning with organophosphorus poisonous substances eliciting neuroparalytic effect.
EFFECT: enhanced effectiveness, valuable medicinal properties of agent.
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
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: medicine, virology, biochemistry.
SUBSTANCE: invention relates to a method for treatment or prophylaxis of infections caused by a related virus in animal, such as SIV, FIV or AIDS, and to using some inhibitors of cyclooxygenase isoform-2 (COX-2) by this designation. Preferable COX-2 inhibitors are L-745337, rofecoxibe, NS398, SC58125, etodolac, meloxicam, celecoxib, DuP-697, DFU, tricyclic MF, valdecoxib, paraoxib-sodium, etoricoxib or nimesulide relating to nonsteroid anti-inflammatory drugs. They improve immune functions of T-cells, reduce or eliminate the immunodeficient state.
EFFECT: improved method of prophylaxis, valuable medicinal properties of drugs.
24 cl, 18 dwg, 6 tbl, 7 ex
FIELD: organic chemistry, pharmacy.
SUBSTANCE: invention relates to novel compounds of the formula (I): their pharmaceutically acceptable salts or solvates, or stereoisomers possessing properties of agonists of β2-adrenoreceptors, to pharmaceutical composition based on thereof, using the claimed compounds in manufacturing a medicinal agent, and to a method for modulation of β2-adrenergic receptors. In the formula (I) each among R1-R5 is chosen independently from group comprising hydrogen atom, (C1-C4)-alkyl and Ra wherein alkyl is substituted optionally with substituted chosen from Rb; or R4 and R5 are combined to form group of the formula: -NRdC(=O)C(Rd)=C(Rd)-; R6, R7 and R8 represent hydrogen atom; R9 represents (C1-C4)-alkyl; R10 represents hydrogen atom or (C1-C4)-alkyl; each among R11, R12 and R13 is chosen independently from group including hydrogen atom, (C1-C4)-alkyl, vinyl, cyclohexyl, phenyl, halogen atom, -CO2Rd, -ORd, -S(O)mRd, -N(NRdRe)Rd or -S(O)2NRdRe, 5-6-membered monocyclic heteroaryl comprising 1 or 2 heteroatoms chosen from nitrogen (N), sulfur (S) atoms, 9-membered bicyclic heteroaryl comprising N as a heteroatom and 5-membered heterocycle comprising N as a heteroatom; or R11 and R12 in common with atoms to which they are bound form 6- or 7-membered heterocyclic ring comprising oxygen (O) atom as a heteroatom and wherein for R11-R13 each phenyl or heteroaryl is substituted optionally with 1 or 2 substitutes chosen independently from Rc, and each heterocyclyl is substituted optionally with 1 or 2 substitutes chosen from Rb and Rc; alkyl is substituted optionally with substitute chosen from Rb, and vinyl is substituted optionally with substitute chosen from Rm; w = 0, 1, 2, 3 or 4. Values Ra, Rb, Rc, Rd, Rm and m are given in the invention claim.
EFFECT: improved method for modulation, valuable medicinal properties of compounds and pharmaceutical composition.
22 cl, 225 ex
FIELD: medicine, phytotherapy, pharmacy.
SUBSTANCE: invention relates to using Ginkgo biloba extracts comprising 20-30% of flavone glycosides, 2.5-4.5% of mainly gynkgolides A, B, C and J, 2-4% of bilobalide, less 10% of proanthocyanidines and less 10 ppm of compounds of alkylphenol type. Also, the invention relates to using the Ginkgo biloba extract of type Egb 761® for preparing a medicinal agent designated for prophylaxis and treatment of sarcopenia. Proposed extracts reduce age-dependent loss of muscle mass and increase the ratio of a muscle mass to the total body mass.
EFFECT: valuable medicinal properties of extracts.
5 cl, 1 tbl, 2 ex
FIELD: medicine, oncology, pharmacology, pharmacy.
SUBSTANCE: invention relates to methods and medicinal formulations used in antitumor treatment and enhancing oral biological availability of taxanes. Method involves administration of taxane in combination with agent enhancing biological availability of taxane in oral administration in subject wherein concentrations of taxane attain levels of therapeutic activity in subject. Ketoconazol representing inhibitor of cytochrome P-450 is used as agent enhancing oral biological availability of taxane. Invention provides enhancing bioavailability of taxane in its oral administration in subject in subtherapeutic doses that results to decreasing toxicity of treatment.
EFFECT: improved and valuable medicinal properties of drug.
33 cl, 42 dwg, 10 tbl, 12 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel anthranilic acid amides with a by-side heteroarylsulfonyl chain. Invention describes compounds of the formula (I): wherein R1 means compounds of formulae: or wherein A means -CnH2n- wherein n = 0, 1, 2, 3, 4 or 5; D means a bond or -O-; E means -CmH2m- wherein m = 0, 1, 2, 3, 4 or 5; R8 means hydrogen atom, alkyl with 1, 2, 3 or 4 carbon atoms or -CpH2p-R14 wherein p = 1, 2, 3, 4 or 5; R14 means phenyl or heteroaryl wherein phenyl and heteroaryl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting fluorine (F), chlorine (Cl), bromine (Br) and iodine (J) atom, alkyl with 1, 2, 3 or 4 carbon atoms; R9 means hydrogen atom or alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms; R10 means hydrogen atom, alkyl with 1, 2, 3 or 4 carbon toms, phenyl, naphthyl or heteroaryl wherein phenyl, naphthyl and heteroaryl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms; R11 means cycloalkyl with 3, 4, 5 or 6 carbon atoms, phenyl, furyl, pyridyl, pyrazinyl wherein phenyl, furyl, pyridyl, pyrazinyl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms, alkoxy-group with 1, 2, 3 or 4 carbon atoms; R12 means alkyl with 1, 2, 3 or 4 carbon atoms, alkynyl with 1, 2, 3 or 4 carbon atoms, cycloalkyl with 3, 4, 5 or 6 carbon atoms, phenyl or heteroaryl; R13 means -CpH2p-R14 wherein p = 0, 1, 2, 3, 4 or 5; R15 means cycloalkyl with 3, 4, 5, 6, 7 or 8 carbon atoms; R2 means hydrogen atom; R3 means heteroaryl wherein heteroaryl is unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms; R4, R5, R6 and R7 mean independently of one another hydrogen atom, F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms, alkoxy-group with 1, 2, 3 or 4 carbon atoms, and their pharmaceutically acceptable salts also. Also, invention describes pharmaceutical composition containing compounds of the formula (I) possessing the effect blocking Kv1.5-channel. Proposed compounds can be used in treatment and prophylaxis of diseases mediated by K+-channel.
EFFECT: valuable medicinal property of compounds and pharmaceutical composition.
20 cl, 4 tbl, 70 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to a composition used in solubilization of paclitaxel. The composition comprises the following components, wt.-%: monoolein, 40-89.99 (or 40-64.7 as variants); oil, 10-59.99 (or 25-49.7 as variants), and paclitaxel, 0.3-4 (or 0.01-10 as variants), and to a method for preparing such composition. Paclitaxel-containing compositions don't comprise potentially toxic surface-active substances, show stability for prolonged time and possess high mucoadhesive capacity and high bioavailability.
EFFECT: valuable medicinal and pharmaceutical properties of composition.
22 cl, 5 tbl, 3 dwg, 19 ex
FIELD: organic chemistry, medicine, oncology, pharmacy.
SUBSTANCE: invention relates to novel C-2'-methylated derivatives of paclitaxel of the formula (I): wherein R represents trifluoromethyl group, phenyl, 2-furyl, 2-thienyl; R1 represents tert.-butoxycarbonyl or benzoyl group; R2 represents hydroxy-group; R3 means hydrogen atom or in common with R2 forms residue of cyclic carbonate of the formula: under condition that when R3 means hydrogen atom then R is not phenyl. Also, invention relates to a pharmaceutical composition based on thereof and using for preparing medicinal agents possessing an antitumor activity. Invention provides preparing novel derivatives of paclitaxel that possess antitumor activity.
EFFECT: valuable medicinal property of derivatives and pharmaceutical composition.
4 cl, 1 tbl, 6 ex
FIELD: medicine, in particular methods (variants) for prophylaxis and treatment of disorders associated with abnormal lipid carbohydrate metabolism or circulatory disturbances associated therewith in mammalian.
SUBSTANCE: claimed methods includes administration of pioglytazone or pharmaceutically acceptable salt thereof in combination with at least one member selected from group containing alpha-glucosidase inhibitor, aldose reductase inhibitor, biguanide, statin derivative, squalene, fibrate compound, enhancer of low density lipoprotein catabolism and inhibitor of angiotensine converting enzyme to mammalian. Alternatively method includes administration of pioglytazone or pharmaceutically acceptable salt thereof in combination with enhancer of insulin secretion and/or insulin preparation.
EFFECT: synergic effect in relation to lowering of glucose levels in blood, body mass losses, with decreased amount of side effects.
13 cl, 8 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