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1.
Mar Drugs ; 17(5)2019 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-31091726

RESUMO

Retinoids are essential during early cardiovascular morphogenesis. However, recent studies showed their important role in cardiac remodeling in rats with hypertension and following myocardial infarction. The present study aimed to investigate the effect of zeaxanthin heneicosylate (ZH); a carotenoid ester isolated from Dunaliella salina microalgae, on cardiac dysfunction ensuing d-galactose injection in rats. Rats injected with d-GAL (200 mg/kg; I.P) for 8 weeks were orally treated with ZH (250 µg/kg) for 28 consecutive days. Results showed that d-GAL injection caused dramatic electrocardiographic changes as well as marked elevation in serum levels of homocysteine, creatinine kinase isoenzyme and lactate dehydrogenase. A reduction in the cardiac contents of glucose transporter-4 and superoxide dismutase along with the elevation of inducible nitric oxide synthetase and interleukin-6 was also noticed. Oral administration of ZH significantly improved the above mentioned cardiac aging manifestations; this was further emphasized through histopathological examinations. The effect of ZH is mediated through the interaction with retinoid receptor alpha (RAR-α) as evidenced through a significant elevation of RAR-α expression in cardiac tissue following the lead of an in silico molecular docking study. In conclusion, zeaxanthin heneicosylate isolated from D. salina ameliorated age-associated cardiac dysfunction in rats through the activation of retinoid receptors.


Assuntos
Clorofíceas/química , Expressão Gênica/efeitos dos fármacos , Cardiopatias/tratamento farmacológico , Receptor alfa de Ácido Retinoico/genética , Zeaxantinas/farmacologia , Zeaxantinas/uso terapêutico , Envelhecimento/efeitos dos fármacos , Animais , Galactose , Coração/efeitos dos fármacos , Cardiopatias/induzido quimicamente , Ratos , Ratos Wistar , Zeaxantinas/isolamento & purificação
2.
Adv Pharm Bull ; 8(3): 523-528, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30276150

RESUMO

Purpose: Aging is associated with hepatic morphological and physiological deterioration due to the accumulation of endogenous and exogenous free radicals and the resultant oxidative stress. The present study aims to investigate the effect of Haematococcus pluvialis microalgae on hepatic changes associated with D-galactose (D-Gal)-induced aging in rats. Methods: Aging was induced in rats by daily intraperitoneal injection of D-Gal (200 mg/kg/day) for eight consecutive weeks. D-Gal-injected rats were treated by astaxanthin (ATX)-rich H. pluvialis biomass, its carotenoid and polar fractions for two weeks. Twenty four hours after the last dose, blood samples were collected and the liver tissues were isolated for further biochemical and histopathological examinations. Results: D-Gal induced aging was associated with an elevation in serum liver function parameters, hepatic oxidative stress biomarkers viz., catalase (CAT), glutathione transferase (GST) and myeloperoxidase (MPO), as well as decreased expression of nuclear factor like-2 (Nrf2). Moreover, induction of aging exhibited an elevation of hepatic inflammatory cytokine; interleukin-6 (IL-6) and its modulator; nuclear factor Kappa B (NF-KB). However, treatment of D-Gal injected rats with ATX-rich H. pluvialis restored the serum liver function parameters as well as hepatic CAT, GST and MPO levels with an elevated expression of Nrf2. Treatment with ATX-rich H. pluvialis was also accompanied with a decrease in hepatic levels of NF-KB and IL-6. Histopathological examination emphasized all the previous results. Similarly, all trans-astaxanthin showed high affinity towards Nrf2 with -7.93 kcal/mol estimated free energy of binding as well as moderate affinities towards IL-6 and NF-KB through a docking study. Conclusion: ATX-rich H. pluvialis showed beneficial effects by ameliorating the hepatic changes associated with D-Gal induced aging in rats due to its modulatory role of the Nrf2/Keap pathway.

3.
Adv Pharm Bull ; 7(4): 655-660, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29399557

RESUMO

Purpose: the non-edible fruit parts of Casimiroa edulis Llave et were evaluated for their active constituents and their potential as antioxidants, anti-inflammatory and antitumor activity. Methods: Fruits peel (FP) and seeds kernel (SK) of Casimiroa edulis Llave et Lex. were extracted successively with hexane and then methanol. Fatty acids were prepared from hexane extracts and identified by GC. Total flavonoid, phenolic acids and tannins contents in methanol extracts were determined by UV spectrophotometer and identified by HPLC. Antioxidant, in-vitro anti-inflammatory activity and antitumor effect against Caco-2 cell line were determined. Results: GC analysis of hexane extracts showed that oleic acid (47.00%) was the major unsaturated fatty acids in both extracts while lignoceric acid (15.49%) is the most abundant saturated fatty acid in (FP). Total phenolic, flavonoid and tannin contents in (FP) & (SK) methanol extracts were; 37.5±1.5, 10.79±0.66 and 22.28±0.23 for (FP); 53.5±1.5mg/g, 14.44±0.32 mg/g; and 53.73±3.58 mg/g for (SK) respectively. HPLC analysis of methanol extract revealed that; the major phenolic compound was pyrogallol in (FP) and p-hydroxybenzoic acid in (SK), the major flavonoid was luteolin 6-arabinose-8-glucose in (FP) and acacetin in (SK). Conclusion: This study showed that non-edible parts of C. edulis fruit is a rich source of different phenolic compounds and fatty acids which has great antioxidant, anti-inflammatory and antitumor activities; that could be used as a natural source in pharmaceutical industry.

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