CS264505B1 - Xanthine reductase inhibiting agent - Google Patents
Xanthine reductase inhibiting agent Download PDFInfo
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- CS264505B1 CS264505B1 CS841902A CS190284A CS264505B1 CS 264505 B1 CS264505 B1 CS 264505B1 CS 841902 A CS841902 A CS 841902A CS 190284 A CS190284 A CS 190284A CS 264505 B1 CS264505 B1 CS 264505B1
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- xanthine
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- reductase inhibiting
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Abstract
Prostředek inhibující xanthin-reduktázy je tvořen sloučeninou kyseliny N-acetyl-p-aminosalicylové vzorce coox ■OH o. NHCOCH3 kde X je anorganický nebo organický kation. Prostředek může být využit v lékařské diagnostice, onkologii a biotechnologii a v genovém inženýrství.The xanthine reductase inhibiting agent is formed by the compound N-acetyl-p-aminosalicylic acid of the formula coox ■OH o. NHCOCH3 where X is an inorganic or organic cation. The agent can be used in medical diagnostics, oncology and biotechnology and in genetic engineering.
Description
Vynález se týká prostředku inhibujícího xanthinreduktázy.The present invention relates to a xanthine reductase inhibitor composition.
Xanthin-O2-reduktáza (známá též pod starším názvem xanthin-oxidáza) se vyskytuje ve sliznici lidského střeva a v lidských játrech. Metoda stanovení její aktivity je popsána v knize Jakoby W. B. (ed.): Enzyme Purification and Related Techniques, vol. 22, p. 150—152, Academie Press New York and London 1971.Xanthin-O 2 -reductase (also known as the xanthine oxidase) occurs in the human mucosa and the human liver. A method of determining its activity is described in Jakoby WB (ed.): Enzyme Purification and Related Techniques, vol. 22, pp. 150-152, Academic Press New York and London 1971.
Sodná sůl kyseliny N-acetyl-para-aminosalicylové získala státní registraci SSSR No. 388 281 (chemické sloučeniny s biologickým účinkem).N-Acetyl-para-aminosalicylic acid sodium salt obtained US State Registration No. 388 281 (chemical compounds with biological activity).
Jak vyplývá z následujícího příkladu, použití sloučeniny vzorceAs follows from the following example, the use of a compound of formula
COONaCOONa
NHCOCH3 je založeno na objevení její nové vlastnosti, a to jejího inhibičního účinku na xantin-reduktázy, při současné její netoxičnosti. Podstatou vynálezu je prostředek inhibující xanthin-reduktázu, který je tvořen sloučeninou vzorce coox é?°H kde X je anorganický nebo organický kation.NHCOCH3 is based on the discovery of its new property, its xanthine reductase inhibitory activity, while at the same time being non-toxic. The present invention is directed to a xanthine reductase inhibiting composition comprising a compound of the formula coox 6 wherein H is an inorganic or organic cation.
Vynález může být využit v lékařské diagnostice a v onkologii. Rovněž je perspektivní v oblasti biotechnologie a genovém inženýrství.The invention can be used in medical diagnostics and oncology. It is also promising in the field of biotechnology and genetic engineering.
Prostředek podle vynálezu se objasňuje v dále uvedeném příkladu:The composition according to the invention is illustrated in the following example:
U sodné soli kyseliny N-acetyl-para-aminosalicylové byl autory vynálezu objeven inhibující účinek na xanthin reduktázy. Ke stanovení byla užita standardní metodika Ústavu pro biologické zkoušení chemických sloučenin SSSR.The sodium salt of N-acetyl-para-aminosalicylic acid has been found to inhibit xanthine reductase. The standard methodology of the Institute for Biological Testing of Chemical Compounds of the USSR was used for the determination.
50% inhibice xanthin-O2 reduktázy je působena 0,8.10-4M roztokem sodné soli N-acetyl-para-aminosalicylové. 50% inhibice (I50) xanthin-DChFIF-reduktázy je dosahováno 0,8.10~4 roztokem sodné soli kyseliny N-acetyl-para-aminosalicylové (Vědecko-výzkumný ústav pro biologické zkoušení chemických sloučenin).50% inhibition of xanthine-O 2 reductase is caused by a 0.8.10 -4 M solution of N-acetyl-para-aminosalicyl sodium. 50% inhibition (I 50) xanthine DChFIF reductase is achieved 0,8.10 -4 solution of sodium salt of N-acetyl-para-aminosalicylic acid (Scientific-Research Institute for Biological testing of chemical compounds).
Přitom je Na-sůl kyseliny N-acetyl-para-aminosalicylové netoxická, o čemž svědčí následující údaje. Akutní toxicita sloučeniny ve fysiologickém roztoku byla testována intravenosně na myších — je nižší než 0,5 g/kg tělesné hmotnosti. Chronická toxicita byla testována perorálně na krysách při denních dávkách 0,5 g/kg tělesné hmotnosti podávaných po dobu 10 dnů a při denních dávkách 1 g/kg tělesné hmotnosti podávaných po dobu 10 dnů. Proti kontrolní skupině, jak v případě samic, tak v případě samců, nebyly zjištěny rozdíly, což svědčí o netoxičnosti i při vysokých denních dávkách opakovaně podávaných.The Na-salt of N-acetyl-para-aminosalicylic acid is non-toxic, as evidenced by the following data. The acute toxicity of the compound in saline was tested intravenously in mice - less than 0.5 g / kg body weight. Chronic toxicity was tested orally in rats at daily doses of 0.5 g / kg body weight administered for 10 days and at daily doses of 1 g / kg body weight administered for 10 days. There were no differences in the control group, both in females and males, suggesting non-toxicity even at high daily doses repeatedly.
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CS841902A CS264505B1 (en) | 1984-03-16 | 1984-03-16 | Xanthine reductase inhibiting agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CS841902A CS264505B1 (en) | 1984-03-16 | 1984-03-16 | Xanthine reductase inhibiting agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CS190284A1 CS190284A1 (en) | 1988-09-16 |
| CS264505B1 true CS264505B1 (en) | 1989-08-14 |
Family
ID=5354527
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CS841902A CS264505B1 (en) | 1984-03-16 | 1984-03-16 | Xanthine reductase inhibiting agent |
Country Status (1)
| Country | Link |
|---|---|
| CS (1) | CS264505B1 (en) |
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1984
- 1984-03-16 CS CS841902A patent/CS264505B1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CS190284A1 (en) | 1988-09-16 |
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