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1.
Plants (Basel) ; 13(7)2024 Mar 26.
Artículo en Inglés | MEDLINE | ID: mdl-38611489

RESUMEN

Orange Bombax ceiba (B. ceiba) is an indigenous plant, and its stamen is an important ingredient in traditional Lanna food. There are limitations in scientific reports on the effects of the biological activities of B. ceiba stamens on the male reproductive system. This study aims to investigate the phytochemical compounds of the orange B. ceiba stamen and its potential effect on the antioxidant properties and quality of cattle sperm treated with Fe. The orange BUE had the highest total phenolics, total tannins, total monomeric anthocyanins, and maximal antioxidant potential. The orange BAE had the highest concentration of total flavonoids. LC-QTOF/MS showed that the orange BUE contained the highest number of phytochemical compounds related to male reproductive enhancement. The orange BUE enhanced sperm motility, and both the orange BUE and the BAE enhanced sperm viability and normal sperm morphology via free radical scavenging. It might be suggested that B. ceiba stamens have benefits for sperm preservation, sperm quality, and increasing the economic value of local plants, and that they may be developed and used to guard against oxidative stress from cryodamage induced by frozen semen technology.

2.
Foods ; 13(4)2024 Feb 19.
Artículo en Inglés | MEDLINE | ID: mdl-38397604

RESUMEN

Alzheimer's disease (AD) is the most common neurodegenerative disease that results in memory impairment. Aegle marmelos (L.) Correa (AM) is used as a traditional medicine. AM leaves have the potential to inhibit acetylcholinesterase activity. This study used scopolamine to induce AD in rats. The aim of this study was to investigate the effects of AM leaf extract using this model. Motor and memory functions were tested by the motor activity and Morris water maze (MWM) tests, respectively. The density of the synaptophysin and dendritic spines in the CA1 were detected by immunofluorescence and Golgi impregnation, respectively. The hippocampal histology was reviewed by H&E staining. After the treatment, the latency times in the MWM tests of the AD groups reduced, while the motor activities showed no difference. The density of the synaptophysin of the AD groups increased after the treatments, and that of the dendritic spines also increased in all AD groups post-treatment. The hippocampal tissue also recovered. AM leaf extract can improve cognitive impairment in AD models by maintaining the presynaptic vesicle proteins and dendritic spines in a dose-dependent manner.

3.
Toxics ; 11(6)2023 May 25.
Artículo en Inglés | MEDLINE | ID: mdl-37368582

RESUMEN

Mancozeb (Mz) is one of the most widely used pesticides that has been reported to cause adverse human health risks. White Nelumbo nucifera (N. nucifera) petals have therapeutic properties to prevent toxicity. Hence, this study attempted to determine the effects of N. nucifera extract on hepatotoxicity and oxidative stress in mancozeb-treated rats. Seventy-two male rats were divided into nine groups and designed with a control; N. nucifera extract was administered at the doses of 0.55, 1.1, and 2.2 mg/kg bw/day, Mz was administered at 500 mg/kg bw/day, and the co-treatment groups (N. nucifera and Mz) were administered 0.55, 1.1, and 2.2 mg/kg bw/day of N. nucifera followed by administering Mz 500 mg/kg bw/day daily for 30 days. The results showed that all doses of N. nucifera extract did not induce hepatic toxicity and could suppress the toxicity of mancozeb by increasing body weight gain and decreasing relative liver weight, lobular inflammation, and total injury score. The combination treatment also decreased the molecular markers of oxidative stress (2-hydroxybutyric acid, 4-hydroxynonenal, l-tyrosine, pentosidine, and N6-carboxymethyllysine). Furthermore, the reduced glutathione and oxidized glutathione contents were adjusted close to the normal level. Therefore, N. nucifera extract is a natural antioxidant supplement that could decrease the toxicity of mancozeb and can be safely consumed.

4.
Foods ; 12(11)2023 May 28.
Artículo en Inglés | MEDLINE | ID: mdl-37297420

RESUMEN

Nelumbo nucifera Gaertn. (N. nucifera) tea is used as food and folk medicine to reduce toxicity in Southeast Asia. Mancozeb (Mz) is used for controlling fungi in agriculture and contains heavy metals. This study aimed to examine the effect of white N. nucifera petal tea on cognitive behavior, hippocampus histology, oxidative stress, and amino acid metabolism in rats poisoned with mancozeb. Seventy-two male Wistar rats were divided into nine groups (n = 8 in each). Y-maze spontaneous alternation test was used to assess cognitive behavior, and amino acid metabolism was investigated by nuclear magnetic resonance spectroscopy (1H-NMR) from blood. There was a significant increase in relative brain weight in the Mz co-administered with the highest dose (2.20 mg/kg bw) of white N. nucifera group. The levels of tryptophan, kynurenine, picolinic acid, and serotonin in blood showed a significant decrease in the Mz group and a significant increase in the Mz co-administered with low dose (0.55 mg/kg bw) of white N. nucifera group. However, there was no significant difference in cognitive behavior, hippocampus histology, oxidative stress, and corticosterone. This study demonstrated that a low dose of white N. nucifera petal tea has a neuroprotective effect against mancozeb.

5.
Trop Anim Health Prod ; 54(5): 308, 2022 Sep 17.
Artículo en Inglés | MEDLINE | ID: mdl-36114327

RESUMEN

Relatively, little is known about the corpus luteum (CL) function in early pregnancy after the successful treatment of luteal phase deficiency in repeat-breeder dairy cows when exposed to extreme environments under tropical climate. To investigate the influence of increased tissues of corpora lutea (CLs) by inducing secondary CL based on progesterone (P4) concentration and fertility in repeat-breeder dairy cows undergoing the fixed-time artificial insemination (FTAI) protocol, 32 cows were treated with gonadotropin releasing hormone (GnRH) on day 5 post-induction (experiment 1). In experiment 2, 213 cows were bred using the short-term FTAI protocol. On day 5 post-FTAI, cows were divided into two groups: treatment with (GnRH5-treated group) or without (GnRH5-untreated group) GnRH. The temperature-humidity index ranged from 77.3 to 82.8. Cows bearing two CLs had greater P4 concentrations than cows bearing only one CL on their ovaries (P < 0.05). Pregnancy rates were greater in GnRH5-treated group than the GnRH5-untreated group (P < 0.01). Moreover, repeat-breeder cows bearing two CLs had a greater likelihood of pregnancy (odds ratio = 20.86) than cows bearing only one CL on their ovaries (P < 0.01). Under heat stress condition, the results highlighted that increasing luteal tissues by creating secondary CL leads to enhanced peripheral P4 concentrations and improved pregnancy outcomes in repeat-breeder dairy cows.


Asunto(s)
Progesterona , Clima Tropical , Animales , Bovinos , Cuerpo Lúteo , Femenino , Fertilidad , Hormona Liberadora de Gonadotropina/farmacología , Respuesta al Choque Térmico , Embarazo , Progesterona/farmacología
6.
Biology (Basel) ; 11(4)2022 Mar 29.
Artículo en Inglés | MEDLINE | ID: mdl-35453722

RESUMEN

The antral follicle count (AFC) is a test in which the number of oocyte-containing follicles that are developing in both ovaries are visually counted. The count of these follicles strongly relates to the population of the growing follicle reserve on the ovaries. However, the importance of the main number of antral follicle populations (mAFC) in mono-ovulatory animal species has yet to be completely elucidated. Moreover, the investigation of the ovarian interrelationship with unilateral mAFC (main number of antral follicle populations appearing on only one side of the ovary) and bilateral mAFC (main number of antral follicle populations appearing in equivalent numbers on both sides of the ovary) and how understanding this interrelationship can offer possible indicators of ovarian response to hormonal induction have not yet been investigated in mono-ovulatory Bos indicus beef cows. The aim of this study is to investigate the different ovarian interrelationships of mAFC (unilateral and bilateral mAFC) at the time of exogenous hormonal stimulation on the total number of AFC (left and right ovaries) at the beginning of the hormonal protocol for ovarian stimulation and ovarian response at the completion of exogenous hormonal stimulation as well as their usefulness as possible biomarkers of successful hormonal stimulation in Bos indicus beef cattle. Beef cows (n = 104) with low total numbers of AFC (4.7 ± 2.4 follicles) were stimulated with a gonadotropin-releasing hormone-progesterone-prostaglandin F2α-based protocol. At the beginning of the hormonal protocol, ovarian ultrasound scans were performed to evaluate AFC from both ovaries of cows. Beef cows were divided into two groups, unilateral (n = 74) and bilateral mAFC (n = 30), according to the ovarian interrelationship. At the completion of the hormonal stimulation, ovarian ultrasound scans were performed to evaluate the dominant follicle (DF) and cows with DF > 8.5 mm in diameter emerging on their ovaries were defined as having experienced a response to hormonal stimuli. There was a difference of 19.1% between Bos indicus cows bearing unilateral mAFC that produced an increase in ovarian response (odds ratio = 2.717, p < 0.05) compared to the responsive rate of cows displaying bilateral mAFC (82.4% vs. 63.3%). In unilateral mAFC, cows bearing mAFC ipsilateral to the ovary of dominant follicle (DF) had a higher responsive rate than cows bearing mAFC contralateral to the DF ovary (50.0% vs. 32.4%, p < 0.05). In mAFC ipsilateral to the DF ovary, pregnancy rates were greatest in cows bearing mAFC and DF on the right ovary compared with cows bearing mAFC and DF on the left ovary (25.0% vs. 9.1%, p < 0.05). In primiparous and multiparous cows, unilateral mAFC occurs with a greater (p < 0.05) frequency than bilateral mAFC (69.0% and 72.0% vs. 31.0% and 28.0%, respectively). In unilateral mAFC, primiparous cows bearing mAFC ipsilateral to the DF ovary had a greater responsive rate than primiparous cows bearing mAFC contralateral to the DF ovary (55.0% vs. 20.0%, p < 0.05). In mAFC ipsilateral to the DF ovary, responsive and pregnancy rates were greatest (p < 0.05) in multiparous cows bearing mAFC and DF on the right ovary compared with multiparous cows bearing mAFC and DF on the left ovary (58.1% and 22.6% vs. 25.8% and 3.2%, respectively). Furthermore, there was a positive correlation between the mean diameter of AFC at the time of the exogenous hormonal trigger and the mean diameter of DF at the completion of hormonal synchronisation (p < 0.05). Our findings emphasise that the ovarian interrelationship with unilateral mAFC at the time of the hormonal trigger might be a promising biomarker for predicting success in ovarian response to hormonal stimulation of mono-ovulatory Bos indicus beef cows with low AFCs.

7.
Plants (Basel) ; 11(5)2022 Feb 26.
Artículo en Inglés | MEDLINE | ID: mdl-35270108

RESUMEN

The white Nelumbo nucifera petals aqueous extraction (NAE) was prominent in phytochemical content, antioxidant activity, and enhanced rat sperm viability induced by FeSO4, a heavy metal. Mancozeb (MZ) contains heavy metals and is widely used for fungal control in agriculture and industry. It induces oxidative stress and causes of spermatogenesis and reproductive organs' abnormalities in both humans and animals. The aims of the present study were to investigate the effects of white Nelumbo nucifera petals aqueous extraction (WNAE) on sperm quality in cattle sperm induced by MZ. Moreover, this study investigated phytochemical compounds by liquid chromatography-mass spectrometry. A protein profile related to sperm quality with SDS-page and sperm energy preservation for each treatment was determined. The results found nine phytochemical compounds, in which quercetin-3-O-arabinoglycoside was a major flavonoid that was found in the WNAE. MZ induced free radicals in cells, leading to LPO and protein oxidation, while decreasing sperm motility, sperm viability, acrosome integrity, and normal sperm morphology. The cattle sperm found four proteins related to sperm quality including MWs of 17, 31, 34, and 55 kDa. The WNAE effectively increased energy preservation, sperm motility, sperm viability, acrosome integrity, and normal sperm morphology. The WNAE enhanced sperm qualities by reducing oxidative stress. It might be suggested that WNAE has benefits for sperm preservation which may be used to guard against toxicity in animals or humans exposed to MZ contaminants.

8.
Animals (Basel) ; 12(3)2022 Jan 25.
Artículo en Inglés | MEDLINE | ID: mdl-35158616

RESUMEN

An investigation of vascularity of ovarian and uterine arteries after hormonal treatment for inactive ovaries using the short-term progesterone-based programme had not yet been explored in repeat-breeder crossbred dairy cows. To investigate the in vivo follicular and uterine arterial indices as an indicator of successful hormonal stimulation for inactive ovaries in repeat-breeder crossbred dairy cattle, 59 cows with inactive ovaries were induced with a 5-day progesterone-based protocol. At the completion of hormonal synchronisation, cows were divided into two groups according to the size of the largest follicle (LF) on their ovary: small (≤10.0 mm) and large (>10.0 mm) LFs. Vascularities of LF and uterine artery (UtA) were evaluated using a colour Doppler tool. Cows that presented with large LF had greater follicular and UtA vascular indices (p < 0.001) and pregnancy rate (p < 0.01) than cows bearing small LF on their ovary. There was a positive correlation (p < 0.001) between follicular size and LF and UtA vascular indices. Our findings highlighted that in vivo LF and UtA vascular indices at the completion of hormonal stimulation might be a promising indicator for predicting success in ovarian response to hormonal stimulation for inactive ovaries of infertile crossbred dairy cows.

9.
Plants (Basel) ; 10(10)2021 Sep 26.
Artículo en Inglés | MEDLINE | ID: mdl-34685828

RESUMEN

Moringa oleifera Lam. (M. oleifera) has been called the "miracle tree" due to its attributes for therapy in various diseases. However, M. oleifera studies on the male reproductive system have been limited. The aim of this study was a phytochemical screening and investigation of the effects of M. oleifera leaf tea on sexual behavior, reproductive function and antioxidant activities. Male rats were fed with M. oleifera leaf tea extract at doses of 0.55, 1.10 and 2.20 mg/kg or distilled water for 30 days. The result showed that M. oleifera leaf tea contained rich total phenols and flavonoids. The courtship behavior, seminiferous tubule diameter, epithelium height, epithelium area, type A spermatogonia, and spermatogonia efficiency were significantly increased in all treatment groups. The groups treated with 1.10 and 2.20 mg/kg increased the number of Sertoli cells. The total of spermatogenic cells increased in the group treated with 0.55 mg/kg. M. oleifera leaf tea scavenged DPPH radical, ABTS radical and H2O2, and inhibited LPO and AGEs formation. Due to M. oleifera leaf tea containing rich total phenols, flavonoids, and antioxidants, it could enhance sexual function and the male reproductive system.

10.
Plants (Basel) ; 10(7)2021 Jul 05.
Artículo en Inglés | MEDLINE | ID: mdl-34371577

RESUMEN

Sacred lotus (Nelumbo nucifera Gaertn.; N. nucifera) is a common ingredient in traditional medicine and Thai recipes. Its petal is an agricultural waste from stamen production. There are limitations in the used and pharmacological data of the petals resulting in more petals waste. The aims of this study were to investigate the phytochemical contents, antioxidant activity, and potential effects on sperm viability of aqueous (NAE) and ethanolic extracts (NEE) of both red and white N. nucifera petals. The white NAE had the highest total phenolics content, total tannins content and maximal antioxidant activity. The white NEE had the highest concentration of total flavonoids. Quercetin was a major flavonoid and was found in the aqueous extracts. Both red and white of NAE in the range of 0.22 to 1.76 mg/mL increased sperm viability. The white NAE was prominent in phytochemical content, antioxidant activity, and both red and white NAE effectively increased rat sperm viability in the in vitro model. The white NAE enhanced sperm viability by decreasing oxidative stress. It might be suggested that the N. nucifera petals have benefits for sperm viability health promotion and may increase the economic value of agricultural waste.

11.
Anim Reprod Sci ; 213: 106281, 2020 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-31987316

RESUMEN

The objectives were to evaluate effects of tropical seasons on thermal biology, preovulatory follicle (POF) diameter, POF and luteal vascularities, and estradiol (E2) and progesterone (P4) concentrations; and to determine the associations among the values for these variables during preovulatory and postovulatory periods in Thai native cows in tropical climates: cold, hot, and rainy seasons. Development and vascularity of the POF and corpora lutea (CL) were evaluated using color Doppler ultrasonography. The temperature-humidity index (THI) was greater when the preovulatory period occurred during the rainy season when compared with the occurrence during the hot and cold seasons of the year. Furthermore, POF diameter was less when the THI was greater. The THI was greater when the postovulatory period occurred during the rainy season when compared to the occurrence of the postovulatory period during the hot and cold seasons of the year. Furthermore, the CL vascularity and P4 concentration were less when the THI was greater. The THI was inversely correlated with CL vascularity and P4 concentrations. When the THI was greatest during the hot and rainy seasons of the year, there were the greatest negative effects on POF size, POF and CL blood flow, and concentrations of E2 and P4 during the preovulatory and postovulatory periods. While native Bos indicus are capable of adapting to tropical conditions, there are still negative effects, such as impaired POF and CL functions, when the THI induces heat stress.


Asunto(s)
Bovinos/fisiología , Cuerpo Lúteo/irrigación sanguínea , Folículo Ovárico/irrigación sanguínea , Folículo Ovárico/fisiología , Ovulación/fisiología , Temperatura , Animales , Femenino , Estaciones del Año , Clima Tropical
12.
Asian J Androl ; 9(6): 849-55, 2007 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-17968473

RESUMEN

AIM: To study the effects of Boesenbergia rotunda (Krachai) on sexual behaviour in male albino rats. METHODS: Thirty-two male Wistar rats were equally divided into four groups: experimental groups were gavaged with the ethanolic extract of the rhizome of B. rotunda at doses of 60, 120 and 240 mg/kg and a control group received distilled water, for 60 days. Sexual behaviour, reproductive organs, diameter of seminiferous tubule, epididymal sperm density, and androgenic hormones were evaluated. RESULTS: Within 30-min observation, there was no significant difference of courtship behaviour, mount frequency (MF), intromission frequency (IF), mount latency (ML), intromission latency (IL), copulatory efficiency or intercopulatory interval in male rats. In three 10-min intervals over a 30-min period, courtship behaviour and MF during the first 10-min were significantly higher than those in the second and third 10-min observation in all groups, whereas IF had no significant difference. All doses of B. rotunda extract significantly increased the relative testicular weight and the diameter of the seminiferous tubules. The dose of 60 mg/kg also significantly increased the relative weight of the seminal vesicle. Nevertheless, the sperm density, serum testosterone and androstenedione levels were not affected by the B. rotunda extract. CONCLUSION: B. rotunda does not affect sexual behaviour nor serum androgenic levels.


Asunto(s)
Extractos Vegetales/farmacología , Conducta Sexual Animal/efectos de los fármacos , Zingiberaceae , Androstenodiona/sangre , Animales , Relación Dosis-Respuesta a Droga , Femenino , Masculino , Ratas , Ratas Wistar , Túbulos Seminíferos/efectos de los fármacos , Túbulos Seminíferos/patología , Recuento de Espermatozoides , Testículo/efectos de los fármacos , Testículo/patología , Testosterona/sangre
13.
FEBS J ; 274(6): 1470-80, 2007 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-17489102

RESUMEN

The multidrug resistance-associated protein transporter ABCC1 (MRP1) is an integral plasma membrane protein involved in the multidrug resistance phenotype. It actively expels a number of cytotoxic molecules from cells. To gain insight into the modulation of the functional properties of this integral membrane protein by cholesterol, a main component of the lipid bilayer, we used multidrug-resistant GLC4/ADR cells, which overexpress MRP1. Upon altering the plasma membrane cholesterol content of these cells, membrane localization and the activity of MRP1 were analyzed. A detergent-free methodology was used to separate "light" and "heavy" plasma membrane fractions. Our data show that MRP1 was exclusively found in "light" fractions known as L0 phase membrane microdomains, together with 23% of gangliosides GM1 and 40% of caveolin-1. Depletion of the membrane cholesterol level to 40% by treatment with the cholesterol-chelating agent methyl-beta-cyclodextrin did not modify MRP1 activity, as evidenced either by the rate of efflux of pirarubicin or that of glutathione. Further cholesterol depletion below 40% yielded both a partial shift of MRP1 to the high-density fraction and a decrease of its functionality. Taken together, these data suggest that MRP1 functionality depends on its localization in cholesterol-rich membrane microdomains.


Asunto(s)
Resistencia a Múltiples Medicamentos , Resistencia a Antineoplásicos , Neoplasias Pulmonares/metabolismo , Proteínas Asociadas a Resistencia a Múltiples Medicamentos/metabolismo , Línea Celular Tumoral , Permeabilidad de la Membrana Celular , Colesterol/metabolismo , Humanos , Proteínas Asociadas a Resistencia a Múltiples Medicamentos/fisiología , Tensoactivos
14.
Artículo en Inglés | MEDLINE | ID: mdl-17547083

RESUMEN

Kaempferia parviflora Wall. Ex. Baker (Krachaidum) has long been used among Thai men for sexual enhancement. The aim of this study was to determine the effect of K. parviflora ethanolic extract on the sexual behavior of male rats and its toxicity. The experiment was divided into three groups of rats given K. parviflora extract at doses of 60, 120, and 240 mg/kg BW for 60 days, whilst a control group received distilled water at 1 ml/day per oral. The results showed that all groups of male rats had significantly higher courtship behavior during the first 10-minute period of observation than in the 2nd and 3rd 10-minute periods, except those receiving the highest dose of K. parviflora. They revealed the same amount of courtship behavior throughout a whole 30-minute period, which was significantly lower than the control group. There was no significant difference between treated and control groups in other sexual behaviors; mount frequency (MF), intromission frequency (IF), mount latency (ML), or intromission latency (IL). Toxicological study revealed no significant difference of hemoglobin, WBC or differential cell count. All dosages had no effect on kidney and liver function, according to the normal values of blood urea nitrogen (BUN), creatinine (Crea), aspartate aminotransferase (AST) and alanine aminotransferase (ALT). Nevertheless, the histopathological study showed a morphological change in the liver. It was concluded that K. parviflora extract at 240 mg/kg BW reduced the time in the first 10 mintues of rat courtship behavior and the use of high and chronic doses of K. parviflora in humans should be considered inadvisable.


Asunto(s)
Extractos Vegetales/toxicidad , Conducta Sexual Animal/efectos de los fármacos , Zingiberaceae/toxicidad , Animales , Masculino , Medicina Tradicional , Ratas , Tailandia , Pruebas de Toxicidad
15.
J Med Chem ; 48(23): 7426-36, 2005 Nov 17.
Artículo en Inglés | MEDLINE | ID: mdl-16279802

RESUMEN

On the basis of the present knowledge of the substrate recognition site of ABC transporter proteins and inspired by the structures of verapamil and pervilleine A, a new class of Pgp-mediated multidrug resistance (MDR) reverters has been designed and synthesized. The new compounds are flexible molecules carrying one or two basic nitrogen atoms flanked, at properly modulated distance, by two aromatic moieties. Most of the molecules studied possess MDR inhibitory activity on anthracycline-resistant erythroleukemia K 562 cells, showing a potency that is higher than that of the reference compound verapamil and, in a few cases (7, 12, 13,17, 20, 22, 28), is in the high nanomolar range. These compounds may be useful leads to develop new MDR reverting agents. In fact, the chemical structure of the class is fairly simple and can be implemented in a variety of ways that will allow the synthesis of new compounds that might be useful leads for the development of drugs to control Pgp-dependent MDR.


Asunto(s)
Antracenos/síntesis química , Benzoatos/síntesis química , Resistencia a Múltiples Medicamentos/efectos de los fármacos , Resistencia a Antineoplásicos/efectos de los fármacos , Piperazinas/síntesis química , Tropanos/química , Verapamilo/química , Aminas/síntesis química , Aminas/química , Aminas/farmacología , Antracenos/química , Antracenos/farmacología , Antraciclinas/farmacología , Antineoplásicos/farmacología , Benzoatos/química , Benzoatos/farmacología , Técnicas Químicas Combinatorias , Humanos , Células K562 , Piperazinas/química , Piperazinas/farmacología , Relación Estructura-Actividad , Verapamilo/farmacología
16.
Bioorg Med Chem ; 13(4): 985-98, 2005 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-15670906

RESUMEN

A series of compounds with a diphenylmethyl cyclohexyl skeleton, loosely related to verapamil, has been synthesized and tested as MDR modulators on anthracycline-resistant erythroleukemia K 562 cells. Their residual cardiovascular action (negative inotropic and chronotropic activity as well as vasorelaxant activity) was evaluated on guinea-pig isolated atria preparations and on guinea-pig aortic strip preparations. Most compounds of the series possess a good MDR-reverting activity together with a low cardiovascular action. Among them, compounds 3a1, 7a, and 8a are more potent than verapamil as MDR reverters and lack any cardiovascular action; they can represent useful leads for the development of new safe MDR reversing drugs.


Asunto(s)
Ciclohexilaminas/farmacología , Resistencia a Múltiples Medicamentos/efectos de los fármacos , Animales , Aorta/efectos de los fármacos , Aorta/fisiología , Ciclohexilaminas/química , Femenino , Cobayas , Atrios Cardíacos/efectos de los fármacos , Humanos , Técnicas In Vitro , Células K562 , Espectroscopía de Resonancia Magnética , Espectrometría de Masas
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