Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experiment
Statin side effects are not a rare occurrence, in particular dyspeptic disorders, insomnia, headache, skin erythema, rash are often noted. All of this determines scientists to find new effective and low-toxic hypolipidemic agents. Various natural and synthetic xanthine derivatives have been recogniz...
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Zaporizhzhia State Medical and Pharmaceutical University
2021-06-01
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| Series: | Zaporožskij Medicinskij Žurnal |
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| Online Access: | http://zmj.zsmu.edu.ua/article/view/207465/232319 |
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| author | I. M. Bilai M. I. Romanenko D. H. Ivanchenko |
| author_facet | I. M. Bilai M. I. Romanenko D. H. Ivanchenko |
| author_sort | I. M. Bilai |
| collection | DOAJ |
| description | Statin side effects are not a rare occurrence, in particular dyspeptic disorders, insomnia, headache, skin erythema, rash are often noted. All of this determines scientists to find new effective and low-toxic hypolipidemic agents. Various natural and synthetic xanthine derivatives have been recognized as therapeutically potential compounds and reported to control various diseases. Therefore, the study of new xanthine derivatives and their hypolipidemic effects, which would have a significant therapeutic effect with minimal side effects, is relevant.
The aim of the study was to examine the effect of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on lipidogram parameters in experimental laboratory rats.
Materials and methods. The objects of the study were 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives. The experiments were performed in white laboratory Wistar rats weighing 180–220 g. Experimental modeling of hyperlipidemia – tween model: intraperitoneal administration of tween-80 at a dose of 200 mg/100 g body weight. The test compounds were administered orally, simultaneously with tween, at a dose of 1/10 of LD50 (previously calculated by Prozorovsky express method) for 6 days. The following indicators of lipidogram were determined: total cholesterol (TC), high-density lipoprotein cholesterol (HDL cholesterol), low-density lipoprotein cholesterol (LDL cholesterol), triglycerides (TG) and atherogenic index of plasma: TC – HDL cholesterol / HDL cholesterol. The experiments were carried out with respect to Bioethical rules and norms.
Results. The studies have shown data on the hypolipidemic activity of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkane acid derivatives. According to the conditional efficiency index Ʃ, which included the overall percentage of the following indicators – total cholesterol, low-density lipoprotein cholesterol and triglycerides, the leading compounds were 2439 (87.47 %), 6047 (82.30 %). The reference drug atorvastatin had a value of 82.98 %.
Conclusions. The major compound was 2439 identified among all compared to the control group. The prospect of further research is a more detailed study on the ability of xanthine derivatives to exhibit hypolipidemic effects and to influence oxidative stress in various hyperlipidemic models. |
| format | Article |
| id | doaj-art-bc4977dbd7d14cd39f2d509e508fa6b7 |
| institution | DOAJ |
| issn | 2306-4145 2310-1210 |
| language | English |
| publishDate | 2021-06-01 |
| publisher | Zaporizhzhia State Medical and Pharmaceutical University |
| record_format | Article |
| series | Zaporožskij Medicinskij Žurnal |
| spelling | doaj-art-bc4977dbd7d14cd39f2d509e508fa6b72025-08-20T03:23:18ZengZaporizhzhia State Medical and Pharmaceutical UniversityZaporožskij Medicinskij Žurnal2306-41452310-12102021-06-0123341141610.14739/2310-1210.2021.3.207465Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experimentI. M. Bilai0https://orcid.org/0000-0002-7574-4093M. I. Romanenko1https://orcid.org/0000-0003-4213-7841D. H. Ivanchenko2https://orcid.org/0000-0001-9858-2659Zaporizhzhia State Medical University, UkraineZaporizhzhia State Medical University, UkraineZaporizhzhia State Medical University, UkraineStatin side effects are not a rare occurrence, in particular dyspeptic disorders, insomnia, headache, skin erythema, rash are often noted. All of this determines scientists to find new effective and low-toxic hypolipidemic agents. Various natural and synthetic xanthine derivatives have been recognized as therapeutically potential compounds and reported to control various diseases. Therefore, the study of new xanthine derivatives and their hypolipidemic effects, which would have a significant therapeutic effect with minimal side effects, is relevant. The aim of the study was to examine the effect of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on lipidogram parameters in experimental laboratory rats. Materials and methods. The objects of the study were 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives. The experiments were performed in white laboratory Wistar rats weighing 180–220 g. Experimental modeling of hyperlipidemia – tween model: intraperitoneal administration of tween-80 at a dose of 200 mg/100 g body weight. The test compounds were administered orally, simultaneously with tween, at a dose of 1/10 of LD50 (previously calculated by Prozorovsky express method) for 6 days. The following indicators of lipidogram were determined: total cholesterol (TC), high-density lipoprotein cholesterol (HDL cholesterol), low-density lipoprotein cholesterol (LDL cholesterol), triglycerides (TG) and atherogenic index of plasma: TC – HDL cholesterol / HDL cholesterol. The experiments were carried out with respect to Bioethical rules and norms. Results. The studies have shown data on the hypolipidemic activity of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkane acid derivatives. According to the conditional efficiency index Ʃ, which included the overall percentage of the following indicators – total cholesterol, low-density lipoprotein cholesterol and triglycerides, the leading compounds were 2439 (87.47 %), 6047 (82.30 %). The reference drug atorvastatin had a value of 82.98 %. Conclusions. The major compound was 2439 identified among all compared to the control group. The prospect of further research is a more detailed study on the ability of xanthine derivatives to exhibit hypolipidemic effects and to influence oxidative stress in various hyperlipidemic models.http://zmj.zsmu.edu.ua/article/view/207465/232319xanthineshyperlipidemialipoproteins |
| spellingShingle | I. M. Bilai M. I. Romanenko D. H. Ivanchenko Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experiment Zaporožskij Medicinskij Žurnal xanthines hyperlipidemia lipoproteins |
| title | Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experiment |
| title_full | Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experiment |
| title_fullStr | Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experiment |
| title_full_unstemmed | Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experiment |
| title_short | Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experiment |
| title_sort | study on the influence of 7 β hydroxy γ aryloxypropylxanthinyl 8 thioalkanic acid derivatives on the lipid metabolism in experiment |
| topic | xanthines hyperlipidemia lipoproteins |
| url | http://zmj.zsmu.edu.ua/article/view/207465/232319 |
| work_keys_str_mv | AT imbilai studyontheinfluenceof7bhydroxygaryloxypropylxanthinyl8thioalkanicacidderivativesonthelipidmetabolisminexperiment AT miromanenko studyontheinfluenceof7bhydroxygaryloxypropylxanthinyl8thioalkanicacidderivativesonthelipidmetabolisminexperiment AT dhivanchenko studyontheinfluenceof7bhydroxygaryloxypropylxanthinyl8thioalkanicacidderivativesonthelipidmetabolisminexperiment |