Effect of complex compounds of methyl derivatives of 5-hydroxyuracil with succinic acid on the antioxidant system and the morpho-functional state of the liver of old rats exposed to carbon tetrachloride

2017 ◽  
pp. 52-56 ◽  
Author(s):  
В.А. Мышкин ◽  
Д.А. Еникеев ◽  
И.Д. Габдрахманова ◽  
Д.В. Срубилин ◽  
А.Р. Гимадиева ◽  
...  
Keyword(s):  
Carbon Tetrachloride ◽  
Succinic Acid ◽  
Functional State ◽  
Antioxidant System ◽  
Free Radical Oxidation ◽  
Complex Compounds ◽  
Corrective Effect ◽  
Old Rats ◽  
Methyl Derivatives ◽  
Derivatives Of

Цель. Изучение влияния комплексных соединений - 5-гидрокси-1,3,6-триметилурацила с сукцинатом (1) и 5-гидрокси-3,6-диметилурацила с сукцинтом (2) - на процессы перекисного окисления липидов (ПОЛ), антиоксидантную систему (АОС) и морфофункциональное состояние печени старых крыс при токсикозе, вызванном тетрахлорметаном. Методы. Опыты выполнены на 50 белых беспородных крысах-самцах, массой более 400 г. Токсическое поражение печени вызывали введением 50%-ного масляного раствора тетрахлорметана (ТХМ) (2 г/кг, п/к) в течение 4 дней [6]. Одновременно вводили исследуемые препараты - соединения 1, 2 и референтный препарат силимарин (50 мг/кг, в/бр) 3 раза в сутки в течение первых 4 дней и в течение последующих 3 дней 1 раз в сутки. Через 7 дней от начала введений исследовали сыворотку крови и печень. Результаты. Комплексные соединения 1 и 2 ограничивали некрозогенное действие ТХМ частично сохраняли функционально-метаболическую активность за счет благоприятного влияния на ферменты (АсАТ, ЩФ), содержание общего билирубина и холестерина в крови, а также за счет частичной нормализации нарушенного равновесия ПОЛ/АОС. Комплексное соединение 5-гидрокси-1,3,6-триметилурацила с сукцинатом более эффективно, чем соединение 2, уменьшало интенсивность и распространенность дистрофических и некротических процессов у старых крыс и существенно ограничивало выраженность гепатотоксического действия ТХМ. Заключение. Защитное действие 5-гидрокси-1,3,6-триметилурацила с сукцинатом было связано с корригирующим влиянием на глутатионовую и ферментативную системы антиоксидантной защиты. The influence of two new complex compounds of methyl derivatives of 5-hydroxyuracil with succinic acid on the antioxidant system and morpho-functional state of the liver of old rats exposed to carbon tetrachloride has been studied experimentally. The aim was to study the influence of complex compounds - 5-hydroxy -1,3,6 - trimethyluracil succinate (1) and 5-hydroxy-3,6-dimethyluracil succinate (2) - on the processes of free radical oxidation, antioxidant system regulating these processes and morpho-functional state of the liver of old rats exposed to carbon tetrachloride. Results. Complex Compounds 1 and 2 used prophylactically in old rats ( 50 mg/kg three times/day х 4 intraperitoneally, then 50 mg/kg once/ per day x 3 intraperitoneally) have been shown to limit necrosogenic effects of TCR ( 2 g/kg/day><4 subcutaneously), to preserve partially functional - metabolic activity due to favorable effects on enzymes (AST, alkaline phosphatase), total blood bilirubin and cholesterol and also due to partial normalization of POL/AOS imbalance. According to most indicators, Compound 1 turns out to be more effective and comparable to the effect of the silymin hepatoprotector. Conclusion. The cCompound 1 reduced the intensity and prevalence of dystrophic and necrotic processes of cellular reactions of the liver tissues in old rats and limited significantly the severity of TCR hepatotoxicity due to a corrective effect on glutathione and enzymatic antioxidant defense system.

Effect of 1,3,6-trimethyl-5-hydroxyuracil succinate on the antioxidant system and free-radical processes in the liver of adult and old rats treated with carbon tetrachloride

2018 ◽  
pp. 55-59
Author(s):  
И.Д. Габдрахманова ◽  
В.А. Мышкин ◽  
Д.А. Еникеев ◽  
А.Р. Гимадиева
Keyword(s):  
Superoxide Dismutase ◽  
Free Radical ◽  
Carbon Tetrachloride ◽  
Antioxidant System ◽  
Complex Compound ◽  
Antiradical Activity ◽  
Conjugated Dienes ◽  
Experimental Animals ◽  
Old Rats ◽  
Radical Processes

Цель исследования: изучение влияния сукцината 1,3,6-триметил-5-гидроксиурацила на антиоксидантную систему и свободнорадикальные процессы в печени взрослых и старых крыс при воздействии тетрахлорметана. Методика. В эксперименте использованы половозрелые животные 12-месячного возраста со средней массой 250 г и старые животные 24-месячного возраста, средней массой 395 г по 30 особей в каждой возрастной группе. Токсическое поражение печени вызывали подкожным введением 50%-ного масляного раствора тетрахлорметана (ТХМ, 2 г/кг) в течение 4 сут. Одновременно с токсикантом опытным животным внутрибрюшинно вводили водный раствор коплексного соединения сукцинат-1,3,6-триметил-5-гидроксиурацила (2,5 мг/100 г) 3 раза в сут. в течение первых 4 сут. и в течение последующих 3 сут. 1 раз в сут. Контролем служили опытные животные, которым вводили физиологический раствор в том же объеме. Изучали окислительную модификацию белков, перекисное окисление липидов (по содержанию ТБК-реагирующих продуктов, уровню гидроперекисей липидов и содержанию диеновых конъюгатов). Состояние антиоксидантной системы оценивали по активности ферментов супероксиддисмутазы, каталазы и глутатионпероксидазы, определяемых биохимическими методами. Антирадикальную активность комплексного соединения и его составляющих субстанций исследовали в модельной системе «этилбензол-ледяная уксусная кислота» с вычислением константы К - скорости взаимодействия перекисных радикалов с молекулами изучаемого соединения в сравнении с эталонным антиоксидантом-ионолом с витамином Е. Результаты. Сукцинат + 1,3,6-триметил-5-гидрокси-урацила существенно снижает токсическое действие ТХМ на печень взрослых и старых крыс, устраняет дисбаланс в системах свободнорадикального окисления белков у старых крыс, статистически значимо улучшает показатели свободнорадикального окисления (СРО) липидов в печени взрослых и старых крыс: снижает уровень продуктов ПОЛ - гидроперекисей, диеновых конъюгатов, ТБК-реагирующих продуктов, а также улучшает работу антиоксидантной системы (АОС), повышая активность каталазы, супероксиддисмутазы и глутатионпероксидазы. Установлена высокая антирадикальная активность изучаемого препарата сопоставимая с активностью эталонного антиоксиданта ионола. Заключение. Сукцинат и его производные способны выступать как индивидуальные вещества с непосредственным антирадикальным механизмом действия, а не только как стимуляторы ферментативных систем антиоксидантной защиты. Aim. To study the effect of a complex compound, 1,3,6-trimethyl-5-hydroxyuracil succinate, on the antioxidant system and free radical processes induced by carbon tetrachloride in the liver of adult and old rats. Methods. The study used sexually mature animals aged 12 months and weighing 250 g and old animals aged 24 months weighing 395 g (total n= 60, 30 rats in each age group). Toxic damage of liver was induced by subcutaneous injections of a 50% oil solution of carbon tetrachloride (CTC) at 2 g/kg for 4 days. Together with the toxicant, experimental animals were injected with a water solution of a complex compound, succinate 1,3,6-trimethyl-5-hydroxyuracil, at a dose of 2.5 mg/100 g, i.p., 3 times per day for the first 4 days and once daily for the following 3 days. Experimental animals were used as controls, which were administered saline in the same volume. Oxidative modifications of proteins, lipid peroxidation (by levels of thiobarbituric acid reactive substances (TBARS), lipid hydroperoxides, and conjugated dienes) were studied. Condition of the antioxidant system was evaluated by activities of superoxide dismutase, catalase, and glutathione peroxidase using biochemical methods. Antiradical activity of the complex compound and its components was studied in a model system of ethylbenzene-glacial acetic acid; the K7 constant of the rate of peroxide radical interaction with molecules of the studied compound was compared with the reference antioxidant ionol with vitamin E. Results. Succinate +1.3.6-trimethyl-5-hydroxyuracil, considerably reduced TXM hepatotoxicity in adult and old rats; removed the disbalance in free radical systems of protein oxidation in old rats; significantly improved indexes of free-radical oxidation (FRO) of hepatic lipids in adult and old rats; decreased levels of LP products, hydroperoxides, conjugated dienes, and TBARS, and enhanced performance of the antioxidant system (AOS) by increasing activities of catalase, superoxide dismutase, and glutathione peroxidase. The study demonstrated a high antiradical activity of the study drug comparable with the activity of the reference antioxidant, ionol. Сonclusion. Succinate and its derivatives can perform as individual substances with a direct antiradical mechanism of action rather than as stimulators of enzymic systems of antioxidant defence.

Synthesis of Complex Compounds of Methyl Derivatives of 8-Quinolineselenol with Metals and Their Cytotoxic Activity.

ChemInform ◽  
2006 ◽  
Vol 37 (35) ◽  
Author(s):  
E. Lukevics ◽  
I. Shestakova ◽  
I. Domracheva ◽  
A. Nesterova ◽  
J. Ashaks ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Complex Compounds ◽  
Methyl Derivatives ◽  
Derivatives Of

Synthesis of complex compounds of methyl derivatives of 8-quinolineselenol with metals and their cytotoxic activity

2006 ◽  
Vol 42 (1) ◽  
pp. 53-59 ◽  
Author(s):  
E. Lukevics ◽  
I. Shestakova ◽  
I. Domracheva ◽  
A. Nesterova ◽  
J. Ashaks ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Complex Compounds ◽  
Methyl Derivatives ◽  
Derivatives Of

Synthesis of precursors of C4 and C5 cumulenones

1984 ◽  
Vol 37 (12) ◽  
pp. 2509 ◽  
Author(s):  
RFC Brown ◽  
KJ Coulston ◽  
FW Eastwood ◽  
BM Gatehouse ◽  
LW Guddatt ◽  
...  
Keyword(s):  
Carbon Dioxide ◽  
Carbon Tetrachloride ◽  
Titanium Tetrachloride ◽  
X Ray ◽  
Endo Isomer ◽  
X Ray Crystallography ◽  
Methyl Derivatives ◽  
Derivatives Of

Bicyclo[2.2.l]hept-5-en-2-one was condensed with 2,2-dimethyl-1,3-dioxan-4,6-dione in the presence of titanium tetrachloride/pyridine to yield 5-(bicyclo[2.2.1]hept-5'-en-2'-ylidene)-2,2-dimethyl-1,3- dioxan-4,6-dione (6a) which on pyrolysis at 520-560�/0.01 mm gave acetone, carbon dioxide, cyclopentadiene and butatrienone. In the same way 5-(7'-oxabicyclo[2.2.1]hept-5'-en-2'-ylidene)-2,2- dimethyl-1,3-dioxan-4,6-dione (6b) was prepared from 7-oxabicyclo[2.2.1]hept-5-en-2-one and on pyrolysis at 570�/0.01 mm it gave acetone, carbon dioxide, furan and butatrienone. Alkylation of 2-trimethylsiloxybicyclo[2.2.1]hepta-2,5 with phenylthiomethyl chloride with titanium tetrachloride as catalyst followed by condensation with 2,2-dimethyl-1,3-dioxan-4,6-dione gave an endo/exo mixture of 5-(3'-phenylthiomethylbicyclo[2.2.1]hept-5'-en-2'-ylidene)-2,2-dimethy 1-1,3-dioxan- 4,6-dione. The structure of the endo isomer was established by X-ray crystallography. Oxidation of the phenylthiomethyl compound with m-chloroperbenzoic acid yielded the sulfoxide which was converted by boiling in carbon tetrachloride into 5-(3'-methylenebicyclo[2.2.l]hept-5'-en-2'-ylidene)- 2,2-dimethyl-1,3-dioxan-4,6-dione (8). Preliminary studies on the fragmentation of compound (8) have shown that at 450�/0.01 mm it is converted into acetone, carbon dioxide and products showing ketene absorption at 2140 cm-1. The formation of pentatetraenone has not been established with certainty. The 3'-phenylsulfonylmethyl, phenylselenyl and methyl derivatives of (6a) are also described.

Physical Properties of TCNQ Salts with N-Methyl Derivatives of Pyridine

1982 ◽  
Vol 85 (1) ◽  
pp. 257-263 ◽  
Author(s):  
A. Graja ◽  
M. Przybylski ◽  
B. Butka ◽  
R. Swietlik
Keyword(s):  
Physical Properties ◽  
Methyl Derivatives ◽  
Derivatives Of

Methyl derivatives of furan

1974 ◽  
Vol 39 (11) ◽  
pp. 3109-3116 ◽  
Author(s):  
J. Šrogl ◽  
M. Janda ◽  
I. Stibor ◽  
V. Skála ◽  
P. Trška ◽  
...  
Keyword(s):  
Methyl Derivatives ◽  
Derivatives Of

Preliminary Note on Dietthio and Diethylsulphone derivatives of Succinic Acid

1897 ◽  
Vol 21 ◽  
pp. 156-159
Author(s):  
Crum Brown ◽  
R. Fairbairn
Keyword(s):  
Succinic Acid ◽  
Calcium Chloride ◽  
Boiling Point ◽  
Carbonic Acid ◽  
Steam Bath ◽  
Sodium Bromide ◽  
Absolute Alcohol ◽  
Preliminary Note ◽  
Aqueous Layer ◽  
Derivatives Of

Sodium mercaptide and dibromosuccinic ether, in the proportion of two molecules of the former to one of the latter, were dissolved separately in absolute alcohol, and slowly mixed. A considerable evolution of heat took place, while sodium bromide separated out. The flask was then digested for some hours on the steam-bath. The alcohol was subsequently distilled off, and the residue, on cooling, was treated with water. An oil separated out. This oil was collected by means of a separating funnel, and the aqueous layer several times extracted with ether. The oil and the ethereal extracts were added together and dried over calcium chloride. Next morning the ether was distilled off at the ordinary pressure. The remainder was distilled in vacuo. Between 50° and 60° a few drops came over, which proved to be ethyldisulphide.The remainder came over between 150° and 170°.This latter fraction was redistilled, and a portion of it used for analysis. The boiling point at 20 mm. pressure was 160°.Combustion of dietthiosuccinic ether.Weight of substance taken = ·2477 gram.Weight of carbonic acid obtained = ·4476 gram.Weight of water obtained = ·1702 gram.

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