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1.
Anticancer Agents Med Chem ; 21(11): 1460-1471, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33019940

RESUMEN

INTRODUCTION: Inflammation is a vital reaction of the natural immune system that protects against encroaching agents. However, uncontrolled inflammation can lead to complications. Trigonella foenumgraecum is traditionally used as an anti-inflammatory herb. OBJECTIVES: The current study was conducted to explore the antioxidant, anti-inflammatory, and antiangiogenic potentials of Trigonella foenum-graecum seeds oil. METHODS: Oil was extracted from seeds of Trigonella foenum-graecum by cold press method and labelled as TgSO. Phytochemical (GC-MS, Folin-Ciocalteu method) and metal analyses were conducted to evaluate the metalo-chemical profile of TgSO. In vitro antioxidant assays (2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis-3- ethylbenzothiazoline-6-sulfonic acid and ferric reducing antioxidant power) were performed to assess its antioxidant potential. In vitro antimicrobial activity was evaluated using agar disc diffusion method and the safety profile of TgSO was assessed in acute toxicological studies following OECD 425 guidelines. In vivo antiinflammatory activities of TgSO were assessed in carrageenan, serotonin, histamine, formalin, and cotton pelletinduced oedema models. Serum TNF-α, Superoxide Dismutase (SOD) and, Catalases (CAT) levels were assessed by ELISA kits. In vivo antiangiogenic activity of TgSO was screened in chick Chorioallantoic Membrane (CAM) assay. Histopathological studies using excised paws were conducted to observe the effects of TgSO treatment at the tissue level. In silico docking studies were conducted to screen the binding potentials of identified compounds with TNF-α. RESULTS: Extraction by cold press method yielded 16% of TgSO. Phytochemical analysis of TgSO through GCMS showed the presence of eugenol, dihydrocoumairn, heptadecanoic acid, tri- and tetradecanoic acid, and hexadecanoic acid, respectively. Total phenolic contents of TgSO were found to be 0.30±0.01mg/g gallic acid equivalent in Folin-Ciocalteu method. Metal analysis indicated the presence of different metals in TgSO. Findings of antioxidant models showed the moderate antioxidant potential of TgSO. Findings of antimicrobial assays showed that TgSO was active against bacterial (S. aureus, S. epidermidis) and fungal (C. albicans, and A. niger) strains. In vivo toxicity study data showed that TgSO was safe up to the dose of 5000 mg/kg. Data of oedema models showed a significant (p<0.05) reduction in oedema development in TgSO treated animals in both acute and chronic models. Histopathological evaluations of paws showed minimum tissue infiltration with inflammatory cells in TgSO-treated animals. Treatment with TgSO also significantly (p<0.05) down-regulated TNF-α in serum while levels of SOD and CAT were up-regulated. Findings of the CAM assay revealed the antiangiogenic activity of TgSO. Findings of in silico docking studies showed that identified phytoconstituents can bind with culprit cytokine (TNF-α). CONCLUSION: Data obtained from the current study conclude that TgSO has antioxidant, anti-inflammatory, and antiangiogenic effects that validate its traditional uses. Synergistic actions of different phytoconstituents are proposed to be responsible for the observed effects.


Asunto(s)
Inhibidores de la Angiogénesis/farmacología , Antibacterianos/farmacología , Antiinflamatorios/farmacología , Antifúngicos/farmacología , Granuloma/tratamiento farmacológico , Fitoquímicos/farmacología , Aceites de Plantas/farmacología , Inhibidores de la Angiogénesis/química , Inhibidores de la Angiogénesis/aislamiento & purificación , Animales , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antifúngicos/química , Antifúngicos/aislamiento & purificación , Aspergillus niger/efectos de los fármacos , Candida albicans/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Regulación hacia Abajo/efectos de los fármacos , Edema/inducido químicamente , Edema/tratamiento farmacológico , Femenino , Inflamación/tratamiento farmacológico , Masculino , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Neovascularización Patológica/tratamiento farmacológico , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Aceites de Plantas/química , Aceites de Plantas/aislamiento & purificación , Ratas , Semillas/química , Staphylococcus aureus/efectos de los fármacos , Staphylococcus epidermidis/efectos de los fármacos , Relación Estructura-Actividad , Trigonella/química , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores
2.
Curr Pharm Biotechnol ; 22(3): 423-432, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-32351177

RESUMEN

BACKGROUND: Paraphenylenediamine (PPD) is a highly toxic compound used for hair-dyeing worldwide. PPD self-poisoning had significantly increased in recent times with increased mortality rates. OBJECTIVE: This study aims to evaluate the toxic effects of PPD and the protective potential of its prospective antidote Virgin Coconut Oil (Cocos nucifera). METHODS: PPD was identified and validated by FT-IR and UV mass spectrometer. PPD toxicity was induced in-vivo by single intraperitoneal injection (40 mg/kg and 60 mg/kg). Single-injection of Virgin Coconut Oil (VCO) was administered in the presence of PPD at doses of 5 mg/kg and 10 mg/kg. Blood was analyzed for renal, hepatic and cardiac biomarkers. Relevant organs were collected, weighed and preserved for histopathological examination. Statistical analysis was carried out to note mortality rate, survival duration and serum biochemical parameter. Molecular docking studies were performed to assess attachment of PPD with histaminergic receptors. RESULTS: PPD injection achieved 100% mortality rate with short survival span, and disturbed hepatic, renal, and cardiac serum markers with marked histopathological changes. VCO notably decreased mortality rate, raised treatment time window with marked adjustment in hepatic, renal, and cardiac markers. Docking studies proved that PPD attaches robustly with histaminergic receptors. CONCLUSION: The study concludes that VCO possesses lifesaving protection against PPD toxicity and can be a suitable antidote.


Asunto(s)
Aceite de Coco/administración & dosificación , Cocos , Colorantes/toxicidad , Citoprotección/efectos de los fármacos , Fenilendiaminas/toxicidad , Animales , Aceite de Coco/química , Aceite de Coco/aislamiento & purificación , Citoprotección/fisiología , Femenino , Riñón/efectos de los fármacos , Riñón/patología , Hígado/efectos de los fármacos , Hígado/patología , Simulación del Acoplamiento Molecular/métodos , Estudios Prospectivos , Estructura Secundaria de Proteína , Ratas , Ratas Wistar , Espectroscopía Infrarroja por Transformada de Fourier/métodos
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