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1.
Phytomedicine ; 89: 153615, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34153878

RESUMEN

BACKGROUND: Inflammation and oxidative stress are common pathologies in a wide range of chronic diseases. Polysaccharides are known to exhibit antioxidant and anti-inflammatory potential and are suggested to possess immunomodulatory potential. PURPOSE: Herein, the immunomodulatory activity of a sulfated polysaccharide (PS) separated from a brown marine algae Turbinaria ornata is studied in LPS instigated systemic inflammation in experimental rats. STUDY DESIGN AND METHODS: Male SD rats are pretreated with different doses of PS (2.5, 5, 10 mg/kg bw) for a week followed by inducing systemic inflammation using LPS (10 mg/kg i.p.). Blood withdrawn after 8 h of LPS injection is subjected to hematological analysis (WBC, HCT, and PLT). After 24 h of LPS induction, cardiac tissue was isolated and subjected to biochemical, molecular, and histopathological analysis. Effect of PS pre-treatment (2.5, 5, 10 mg/kg bw) was checked by assessing serum parameters (AST, CK-MB, and γGT), antioxidant markers (LPO, GSH, SOD, Grx) and inflammatory markers (IL1ß, IL6, IL10, NFκB), followed by analyzing the iNOS, PI3k and Akt to identify the probable mode of action. RESULTS: Elevated levels of AST, CK-MB, and γGT in serum were significantly reduced on PS pretreatment. LPS significantly raised the LPO and Grx levels in heart tissue whereas, PS pre-treatment significantly reduced LPO and Grx levels. GSH and SOD levels were reduced upon LPS induction and were brought to near normal by HD of PS. PS also reduced the mRNA levels of IL6, Trx, and increased IL10 levels in the heart tissue substantiating its anti-inflammatory and antioxidant potency. Further, IL1ß, NFκB, iNOS, and pPI3k/pAkt expressions were significantly modulated by PS in the cardiac tissue substantiating the immunomodulatory effect. A trend of improvement in the inflammatory pathology was also observed in the heart tissue compared to LPS control, as confirmed by histopathology analysis. CONCLUSION: Altogether, this study concludes the immunomodulatory potential of PS from the marine macroalgae Turbinaria ornata significantly and prevents LPS induced systemic inflammation in the cardiac tissue presumably influenced by the glucopyranose and fucopyranose subunits in the polysaccharide.


Asunto(s)
Inmunomodulación , Inflamación/tratamiento farmacológico , Phaeophyceae , Polisacáridos , Animales , Lipopolisacáridos , Masculino , Estrés Oxidativo , Phaeophyceae/química , Polisacáridos/farmacología , Ratas , Ratas Sprague-Dawley , Sulfatos
2.
J Food Biochem ; 45(2): e13595, 2021 02.
Artículo en Inglés | MEDLINE | ID: mdl-33368458

RESUMEN

A sedentary lifestyle combined with the intake of high-calorie diet has been the paramount cause of metabolic syndrome (MS) which is now a serious concern of public health worldwide as it involves the coexistence of hypertension, hyperlipidemia, glucose intolerance, and obesity. Hence, identifying a suitable strategy to overcome the worldwide menace of MS is imperative. Macrotyloma uniflorum a lesser known legume is highly nutritious and notable for its ethano-medicinal potential. Herein, the influence of M. uniflorum in high-fat dietinduced metabolic changes in a rodent model of metabolic syndrome was evaluated. Serum levels of glucose, total cholesterol, triglycerides, VLDL-c, and bodyweight were decreased, whereas HDL-c was increased in M. uniflorum-treated MS rats. The protein expression (AMPK-α, PPAR-α, and PPAR-γ) and gene expression (leptin, adiponectin, resistin, UCP2, NF-κB, and IL-6) results are impressive to highlight that M. uniflorum modulates the pathological conditions of MS and proves to be cardioprotective. Furthermore, the histopathological analysis confirmed the pathological changes and substantiates the influence of M. uniflorum to overcome MS. The HPLC and GC (MS) profiling reveals the presence of an array of polyphenols such as rutin (694.61 µg/g), catechin (500.12 µg/g), epicatechin (158.10 µg/g), gallic acid (17.98 µg/g), ferulic acid (10.911 µg/g), daidzein (6.51 µg/g), and PUFA, respectively, which probably exhibits the therapeutic effect on MS and associated complications by modulating lipid metabolism and adipogenesis. PRACTICAL APPLICATIONS: Metabolic disorders like CVD and diabetes are leading cause of mortality and morbidity worldwide. With emerging issues on adverse effects of modern drugs, the emphasis on "Food is Medicine and Medicine as Food" has taken dramatic dimensions in the healthcare sector. Therefore, nutraceuticals are in great demand in the developed world off late. Legumes, are potent elements in a balanced diet next to cereals. Exploring the medicinal properties of legumes could bring a revolution in public health and nutraceutical industries. This study scientifically validated the phytochemicals in M. uniflorum for its functional potential in the management of Metabolic Syndrome (MS). This study would help the nutraceutical industries to develop functional foods using M. uniflorum seeds to make porridges and soups or nutraceutical supplements with the bioflavonoids isolated from M. uniflorum for the management of metabolic disorders by mitigating hyperlipidemia, oxidative stress, and inflammation.


Asunto(s)
Fabaceae , Síndrome Metabólico , Adipoquinas , Animales , Suplementos Dietéticos , Obesidad , Ratas
3.
Comb Chem High Throughput Screen ; 23(9): 931-938, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-31985369

RESUMEN

BACKGROUND: Inflammation and pain, mainly induced by the prostaglandins synthesized by the cyclooxygenase enzymes, may cause distress. To overcome this unpleasant stress in a safer manner, numerous natural molecules are proven for modulating the COX enzymes. Epicatechin and daidzein are two bioactive natural compounds present in horsegram, a legume known for its medicinal properties. OBJECTIVE: The present study aims at evaluating the potential of horsegram, and some of its bioactive molecules, to be used as an anti-inflammatory and analgesic agent mediated by the inhibition of COX enzymes, which can be recommended as a substitute for chemically synthesized NSAIDs. METHODS: The present work involved the quantification of epicatechin and daidzein present in horsegram seeds. The COX enzyme inhibitory nature of epicatechin and daidzein was tested using in silico docking analysis with Autodock software and was further confirmed by in vitro COX inhibitory biochemical assays. Furthermore, the anti-inflammatory and analgesic activities of the horsegram seeds were evaluated in animal experiments. RESULTS: Horsegram seeds contain 158.1 microgram/g and 6.51 microgram/g of epicatechin and daidzein respectively. The docking studies reveal that both the bioactive molecules exhibit better binding efficiency with COX-2 protein as compared to COX-1. Hence, in vitro COX-2 inhibitory assay was performed for epicatechin, daidzein and compared with known analgesic agent diclofenac which revealed a pronounced dose dependent inhibitory activity. Furthermore, the analgesic and anti-inflammatory activity of horsegram in experimental animals exhibited a dose dependent effect which might be due to the presence of the bioactive compounds such as epicatechin and daidzein. CONCLUSION: The results suggest that epicatechin and daidzein present in horsegram are potent cyclooxygenase inhibitors and thus would be helpful in the management of inflammation and pain.


Asunto(s)
Analgésicos/química , Antiinflamatorios/química , Inhibidores de la Ciclooxigenasa 2/química , Fabaceae/química , Flavonoides/química , Inflamación/tratamiento farmacológico , Dolor/tratamiento farmacológico , Extractos Vegetales/química , Prostaglandina-Endoperóxido Sintasas/metabolismo , Semillas/química , Analgésicos/farmacología , Animales , Antiinflamatorios/farmacología , Antiinflamatorios no Esteroideos/farmacología , Catequina/farmacología , Inhibidores de la Ciclooxigenasa 2/farmacología , Relación Dosis-Respuesta a Droga , Descubrimiento de Drogas , Humanos , Isoflavonas/farmacología , Masculino , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología , Unión Proteica , Ratas Sprague-Dawley , Relación Estructura-Actividad
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