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1.
Bull Exp Biol Med ; 169(1): 57-59, 2020 May.
Article in English | MEDLINE | ID: mdl-32488783

ABSTRACT

The effects of a new derivative of benzimidazole (K-134) in doses of 5 and 50 mg/kg on the spermatogenesis and fertilizing ability of spermatozoa were studied on male rats. It was found that 2-month course treatment with the studied substance enhances the producing ability of the spermatogenic epithelium and improves fertilizing ability of spermatozoa.


Subject(s)
Fertility/drug effects , Quinolines/pharmacology , Seminiferous Epithelium/drug effects , Urea/analogs & derivatives , Animals , Animals, Outbred Strains , Benzimidazoles/pharmacology , Cytoprotection/drug effects , Dose-Response Relationship, Drug , Male , Rats , Seminiferous Epithelium/physiology , Spermatogenesis/drug effects , Testis/drug effects , Urea/pharmacology
2.
Biomed Khim ; 64(4): 334-343, 2018 Aug.
Article in Russian | MEDLINE | ID: mdl-30135280

ABSTRACT

Experimental chronic heart failure (CHF), caused by administration of L-isoproterenol (2.5 mg/kg twice a day intraperitoneally for 21 days), promotes uncoupling of respiration and oxidative phosphorylation. The rate of mitochondrial oxygen consumption in the metabolic state V3 by Chance in animals with CHF decreased by 53.3% (p<0.05) with malate using (as an oxidation substrate feeding сomplex I of the electron transport chain (ETC)), by 70.6% (p<0.05) with succinate using (сomplex II substrate) and by 63.6% (p<0.05) when malate and succinate were added simultaneously. The respiratory control ratio significantly decreased 2.3 times for сomplex I, 2.5 for сomplex II, and 2.6 times for the simultaneous operation of two respiratory chain complexes in mitochondria of CHF rats compared to intact animals. Mitochondrial dysfunction in experimental CHF is evidently due to the development of oxidative stress. It was revealed that the content of malonic dialdehyde (MDA) in the group of rats with experimental CHF was higher by 54.7% (p<0.05), as compared with intact animals. The activity of superoxide dismutase (SOD) and catalase was lower by 17.5% (p<0.05), and by 18.4%, respectively than in the intact group. The dense extract from herba of Primula veris L. (DEHPV) 30 mg/kg limits the development of mitochondrial dysfunction in rats with experimental CHF, as evidenced by an increase in the role of V3 respiration for the first and second respiratory chain complexes in 1.7 (p<0.05) and 2.0 times (p<0.05), respectively, the ratio of respiratory control (RCR) - 1.7 times (p<0.05) for сomplex I and 2 times (p<0.05) for сomplex II compared with the negative control. The concentration of MDA was by 15.7% (p<0.05), lower and the activity of SOD was by 56.3% (p<0.05) higher.


Subject(s)
Heart Failure/prevention & control , Mitochondria, Heart/drug effects , Myocytes, Cardiac/drug effects , Oxidative Stress/drug effects , Plant Extracts/pharmacology , Primula/chemistry , Animals , Antioxidants/metabolism , Chronic Disease , Disease Models, Animal , Heart Failure/metabolism , Male , Mitochondria, Heart/metabolism , Myocytes, Cardiac/metabolism , Oxygen Consumption/drug effects , Plant Extracts/isolation & purification , Rats
3.
Bull Exp Biol Med ; 159(5): 635-7, 2015 Sep.
Article in English | MEDLINE | ID: mdl-26468030

ABSTRACT

The effects of a new thietanylbenzimidazole derivative (K-134) on estrous cycles, conception processes, and sexual behavior of female rats were studied. Two-week oral treatment with K-134 in doses of 5 and 50 mg/kg shortened the estrus phase and prolonged proestrus. Changes in sexual behavior were presented by activation of receptive sexual motivations without affecting proceptive motivations. The pregnancy and fertility indexes in experimental females after mating with intact males increased and pre- and postimplantation embryonic death decreased.


Subject(s)
Benzimidazoles/pharmacology , Estrous Cycle/drug effects , Fertility Agents, Female/pharmacology , Fertilization/drug effects , Genetic Fitness/drug effects , Sexual Behavior, Animal/drug effects , Animals , Animals, Outbred Strains , Estrous Cycle/physiology , Female , Fertilization/physiology , Fetal Mortality , Genetic Fitness/physiology , Libido/drug effects , Litter Size/drug effects , Litter Size/physiology , Male , Pregnancy , Rats , Sexual Behavior, Animal/physiology
4.
Bioorg Khim ; 40(3): 327-34, 2014.
Article in Russian | MEDLINE | ID: mdl-25898740

ABSTRACT

Using reaction of hydrazide 2-[6-methyl-1-(thiethane3-yl)uracil-3-yl]acetic acid with arylaldehydes and acetophenone derivatives were obtained acylhydrazones, which exist in DMSO solution as a mixture of two stereoisomers of a E(C=N)-isomer for due to hindered internal rotation around the hydrazide bond. It was revealed that the synthesized compounds exhibit antihypertensive activity.


Subject(s)
Antihypertensive Agents/chemical synthesis , Hypertension/drug therapy , Uracil/chemical synthesis , Animals , Antihypertensive Agents/chemistry , Humans , Hypertension/pathology , Isomerism , Rats , Structure-Activity Relationship , Uracil/chemistry
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