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1.
Bull Exp Biol Med ; 169(1): 57-59, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-32488783

RESUMEN

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.


Asunto(s)
Fertilidad/efectos de los fármacos , Quinolinas/farmacología , Epitelio Seminífero/efectos de los fármacos , Urea/análogos & derivados , Animales , Animales no Consanguíneos , Bencimidazoles/farmacología , Citoprotección/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Masculino , Ratas , Epitelio Seminífero/fisiología , Espermatogénesis/efectos de los fármacos , Testículo/efectos de los fármacos , Urea/farmacología
2.
Biomed Khim ; 64(4): 334-343, 2018 Aug.
Artículo en Ruso | MEDLINE | ID: mdl-30135280

RESUMEN

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.


Asunto(s)
Insuficiencia Cardíaca/prevención & control , Mitocondrias Cardíacas/efectos de los fármacos , Miocitos Cardíacos/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Primula/química , Animales , Antioxidantes/metabolismo , Enfermedad Crónica , Modelos Animales de Enfermedad , Insuficiencia Cardíaca/metabolismo , Masculino , Mitocondrias Cardíacas/metabolismo , Miocitos Cardíacos/metabolismo , Consumo de Oxígeno/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Ratas
3.
Bull Exp Biol Med ; 159(5): 635-7, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26468030

RESUMEN

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.


Asunto(s)
Bencimidazoles/farmacología , Ciclo Estral/efectos de los fármacos , Fármacos para la Fertilidad Femenina/farmacología , Fertilización/efectos de los fármacos , Aptitud Genética/efectos de los fármacos , Conducta Sexual Animal/efectos de los fármacos , Animales , Animales no Consanguíneos , Ciclo Estral/fisiología , Femenino , Fertilización/fisiología , Mortalidad Fetal , Aptitud Genética/fisiología , Libido/efectos de los fármacos , Tamaño de la Camada/efectos de los fármacos , Tamaño de la Camada/fisiología , Masculino , Embarazo , Ratas , Conducta Sexual Animal/fisiología
4.
Bioorg Khim ; 40(3): 327-34, 2014.
Artículo en Ruso | MEDLINE | ID: mdl-25898740

RESUMEN

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.


Asunto(s)
Antihipertensivos/síntesis química , Hipertensión/tratamiento farmacológico , Uracilo/síntesis química , Animales , Antihipertensivos/química , Humanos , Hipertensión/patología , Isomerismo , Ratas , Relación Estructura-Actividad , Uracilo/química
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