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1.
Toxicol Res (Camb) ; 10(4): 761-770, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34484667

RESUMO

Alcoholism has been linked to problems with male reproductive function. The combined effects of alcohol, cannabis, and tobacco were compared in this study. A total of 35 rats were assigned randomly into seven groups A-G: animals in A were administered distilled water. Animals in B-G were either administered alcohol orally (30 ml 40% alcohol) or exposed to smoke from ignited tobacco (exposure to smoke from 0.7 g tobacco for 5 min) or cannabis (exposure to smoke from 0.7 g tobacco and cannabis for 5 min): B (orally administered alcohol), C (exposed to the smoke from tobacco), D (exposed to smoke from cannabis), E (treated with alcohol and exposed to smoke from tobacco), F (treated with alcohol and exposed to smoke from cannabis), G (treated with alcohol and exposed to smokes from tobacco and cannabis). Assays were carried on the testicular homogenate after a 14-day treatment. There was a significant increase in activity of alkaline phosphatase (P ≤ 0.05), concentrations of cholesterol, glutathione reductase, and malondialdehyde in treated rats by the co-administration of alcohol with cannabis and tobacco compared with the control group. The combined treatment also caused degeneration and morphological distortions of testicular cells. The biochemical and histoarchitectural change was due to oxidative damage attributable to the synergistic effects. The high binding energy of tetrahydrocannabinol ligand to prostate acid phosphatase may be a prediction that the ligand can have an inhibitory effect on the function of enzymes in the prostate.

2.
Biomed Pharmacother ; 132: 110863, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33113424

RESUMO

PURPOSE: Benign prostatic hyperplasia (BPH) is a urological disease characterized by proliferation of the stromal and epithelial cells of the prostate of older men. Ketogenic diet (KD) is a high fat, moderate protein and low carbohydrate diet which acts on metabolic systems through hormonal modulation and simulation amongst other mechanisms. This study investigated the effect of KD consumption in Testosterone Propionate (TP) induced BPH. MATERIALS AND METHODS: Twenty-Five male rats were divided into five groups of five animals each; control and KD group were administered distilled water and KD respectively, while the remaining groups were given 30 mg/kg body weight of TP subcutaneously once daily for 28 days. Thereafter, the three groups, TP, TP + Finasteride, TP + KD were administered standard rat chow, finasteride (0.1 mg/kg) and KD respectively, for 42 days prior to sacrificing the rats and their serum and prostate glands obtained for analysis. RESULTS: Triglyceride, Total cholesterol, HMG CoA reductase, Follicle Stimulating Hormone, Luteinizing Hormones, Testosterone, Prostate Specific Antigen (PSA) concentration and Malondialdehyde levels were significantly increased (p ≤ 0.05) while superoxide dismutase, catalase and glutathione peroxidase activities were significantly (p ≤ 0.05) reduced in the TP group. These changes were reversed significantly (p ≤ 0.05) in the finasteride and KD treatment groups. The diet also caused significant (p ≤ 0.05) decrease in prostate weight and stromal glandular tissue. CONCLUSION: This study suggests that ketogenic diet consumption ameliorated prostatic hyperplasia in the rats and may be considered as an affordable and non-invasive management option for benign prostatic hyperplasia in men.


Assuntos
Dieta Cetogênica , Próstata , Propionato de Testosterona , Animais , Antioxidantes/metabolismo , Biomarcadores/sangue , Modelos Animais de Doenças , Hormônios/sangue , Lipídeos/sangue , Masculino , Malondialdeído/sangue , Próstata/metabolismo , Próstata/patologia , Antígeno Prostático Específico/sangue , Hiperplasia Prostática/sangue , Hiperplasia Prostática/induzido quimicamente , Hiperplasia Prostática/metabolismo , Hiperplasia Prostática/patologia , Ratos Wistar , Fatores de Tempo
3.
Parasitol Res ; 119(6): 1925-1941, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32279093

RESUMO

Toxoplasmosis is a common parasitic disease caused by Toxoplasma gondii. Limitations of available treatments motivate the search for better therapies for toxoplasmosis. In this study, we synthesized a series of new imidazole derivatives: bis-imidazoles (compounds 1-8), phenyl-substituted 1H-imidazoles (compounds 9-19), and thiopene-imidazoles (compounds 20-26). All these compounds were assessed for in vitro potential to restrict the growth of T. gondii. To explore the structure-activity relationships, molecular analyses and bioactivity prediction studies were performed using a standard molecular model. The in vitro results, in combination with the predictive model, revealed that the imidazole derivatives have excellent selectivity activity against T. gondii versus the host cells. Of the 26 compounds screened, five imidazole derivatives (compounds 10, 11, 18, 20, and 21) shared a specific structural moiety and exhibited significantly high selectivity (> 1176 to > 27,666) towards the parasite versus the host cells. These imidazole derivatives are potential candidates for further studies. We show evidence that supports the antiparasitic action of the imidazole derivatives. The findings are promising in that they reinforce the prospects of imidazole derivatives as alternative and effective antiparasitic therapy as well as providing evidence for a probable biological mechanism.


Assuntos
Antiparasitários/química , Antiparasitários/farmacologia , Imidazóis/química , Imidazóis/farmacologia , Toxoplasma/efeitos dos fármacos , Animais , Células Cultivadas , Humanos , Imidazóis/síntese química , Modelos Moleculares , Relação Estrutura-Atividade , Toxoplasmose/parasitologia
4.
J Integr Med ; 15(1): 64-76, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28088261

RESUMO

OBJECTIVE: The leaves of Parquetina nigrescens have been claimed in folk medicine to be useful for managing sexual dysfunction, but there is inadequate scientific evidence for this claim. This investigation was conducted to assess the effects of aqueous leaf extract of Parquetina nigrescens (AEPN) in rats induced with sexual dysfunction. METHODS: Male rats were allocated into various groups after being induced into sexual dysfunction with paroxetine hydrochloride. The groups were treated with distilled water, PowMaxM (reference drug), and the AEPN at 20, 40 and 80 mg/kg body weight (BW) respectively for 7 d. Frequencies of mount (MF), intromission (IF), ejaculation (EF), as well as latencies of mount (ML), intromission (IL) and post-ejaculatory interval (PEI) were progressively monitored with receptive female rats on days 1, 3 and 7. The precentage of mounted, intromitted, and ejaculated rats, intromission ratio (IR), copulatory efficiency (CE) and intercopulatory interval (ICI) were also computed. Standard methods were employed to determine the levels of serum luteinizing and follicle stimulating hormones (LH and FSH), testosterone, nitric oxide (NO) and the activity of phosphodiesterase V (PDE5). RESULTS: The plant contained alkaloids, saponins, flavonoids, cardiac glycosides, steroids, tannins, phlobatannins, cardenolides, phenolics, anthraquinones and triterpenes with alkaloids (2.32 mg/g) occurring in greatest quantity while flavonoids, anthraquinones and cardenolides (0.01 mg/g, each) were the least. All the 20 standard amino acids were detected in the plant leaf, with the lowest concentration being 0.30 mg/g for methionine and the highest being 2.12 mg/g for cysteine. Furthermore, P. nigrescens leaves contained Na, K, Fe, Mg, Zn, Ca, Cu, Mn, P, Pb, Cd, Ni, Cr, and Co, with Fe present in the highest and Co the lowest concentrations. Paroxetine significantly (P<0.05) reduced MF, IF, EF, percentage mounted , intromitted, ejaculated, IR, CE, serum testosterone, LH, FSH and NO, while ML, IL, PEI, IF and PDE5 were significantly (P<0.05) increased and/or prolonged. The AEPN significantly reversed these paroxetine-treatment-related alterations with most profound activity at the highest dose of 80 mg/kg BW, similar to that of the PowMaxM-treated animals. CONCLUSION: The AEPN restored both the physical and biochemical indices of male sexual activity/competence via changes in reproductive hormones, NO and PDE5 activity. The pro-sexual activity, attributed to a myriad of mineral, amino acid and secondary metabolite constituents, was best at 80 mg/kg BW of AEPN.


Assuntos
Apocynaceae/química , Compostos Fitoquímicos/uso terapêutico , Fitoterapia , Extratos Vegetais/uso terapêutico , Comportamento Sexual Animal/efeitos dos fármacos , Disfunções Sexuais Fisiológicas/tratamento farmacológico , Animais , Copulação/efeitos dos fármacos , Nucleotídeo Cíclico Fosfodiesterase do Tipo 5/metabolismo , Ejaculação/efeitos dos fármacos , Feminino , Hormônio Foliculoestimulante/sangue , Hormônio Luteinizante/sangue , Masculino , Óxido Nítrico/sangue , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Ratos Wistar , Disfunções Sexuais Fisiológicas/metabolismo , Disfunções Sexuais Fisiológicas/fisiopatologia , Testosterona/sangue
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