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1.
Fitoterapia ; 140: 104420, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31733344

RESUMEN

We report for the first time the isolation of 2-furyl(phenyl)methanol (5) from the chloroform extracts of the Atractylis gummifera roots. A. gummifera is a thistle belonging to the Asteraceae family that produces the ent-kaurane diterpenoid glycoside atractyloside (ATR). ATR (1) was isolated and chemically modified to obtain its aglycone atractyligenin (2) and the methylated derivatives ATR-OMe (3) and genine-OMe (4). The compounds 1-5 were structurally characterised and evaluated against the intracellular amastigote, cultured within macrophages, and the extracellular promastigote of Leishmania donovani, the protozoan parasite responsible for the highly infective disease visceral leishmaniasis, which is fatal if untreated. The 2-furyl(phenyl)methanol 5 exhibited notable activity against the promastigote.


Asunto(s)
Antiprotozoarios/farmacología , Atractylis/química , Leishmania donovani/efectos de los fármacos , Metanol/farmacología , Animales , Antiprotozoarios/aislamiento & purificación , Italia , Macrófagos/parasitología , Metanol/análogos & derivados , Metanol/aislamiento & purificación , Ratones Endogámicos BALB C , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales , Rizoma/química
2.
Food Funct ; 5(3): 517-20, 2014 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-24452710

RESUMEN

Bacopa monnieri (L., BM) is a traditional Ayurvedic medicinal herb recognised for its efficacy in relieving acute pain and inflammation, as related to selective inhibition of cyclo-oxygenase-2 (COX-2) enzyme and consequent reduction in COX-2-mediated prostanoid mediators. BM is also associated with cognitive enhancing (nootropic) activity including improving memory free recall, observed after prolonged intake (>3 months). It is likely that the time frame required to exert an effect in the brain reflects regulation by BM of chronic inflammation and oxidative stress associated with aging and chronic diseases, and other polypharmacological effects. We report down-regulation by BM of NO and TNF-α in stimulated RAW 246.7 macrophages and of IFN-γ in stimulated human blood cells. Furthermore, in human blood cells, IL-10 was slightly elevated indicating polarisation towards a regulatory T cell phenotype. These results provide further supportive evidence to justify the clinical evaluation of BM for managing diseases involving chronic systemic and brain inflammation driven by the innate immune system.


Asunto(s)
Antiinflamatorios/farmacología , Bacopa/química , Inmunidad Innata/efectos de los fármacos , Macrófagos/efectos de los fármacos , Extractos Vegetales/farmacología , Envejecimiento/efectos de los fármacos , Envejecimiento/inmunología , Animales , Células Sanguíneas/efectos de los fármacos , Células Sanguíneas/inmunología , Encéfalo/efectos de los fármacos , Encéfalo/inmunología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Humanos , Interleucina-10/inmunología , Macrófagos/inmunología , Ratones , Factor de Necrosis Tumoral alfa/inmunología
3.
Nutr Cancer ; 65(5): 746-64, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-23859043

RESUMEN

Numerous in vitro studies using solvent or aqueous extracts of raw dietary plant material have demonstrated modulation of colon cancer cell growth and apoptosis and effects on immune and nonimmune pathways of inflammation. We have developed a generic, 3-staged food-compatible process involving heating for conversion of dietary plants into food ingredients and report results on potential colon cancer-regulating properties of processed forms of Bay leaf (Laurus nobilis). In vitro studies demonstrated inhibition of cancer cell growth by processed Bay leaf products in HT-29, HCT-116, Caco-2, and SW-480 human cancer cell lines, which were accompanied by variable levels of elevated apoptosis. Bay leaf also exerted moderate inhibition of cycloxygenase 2 and 5 lipoxygenase enzymatic activity. In addition, these extracts significantly downregulated interferon-γ production in T helper Type 1-stimulated whole blood from healthy donors. Furthermore, size fractionation of the extracts revealed that antiproliferative and proapoptotic activities were associated with low mass (primarily polyphenolics and essential oils) and high mass (primarily proteins including polyphenol oxidase) chemical classes, respectively. Bay leaf exerted in vitro bioactivity that might be relevant to protecting against early events in sporadic colorectal cancer, with potential for further optimization of bioactivity by size-based fractionation.


Asunto(s)
Diferenciación Celular/efectos de los fármacos , Neoplasias Colorrectales/metabolismo , Laurus/química , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Araquidonato 5-Lipooxigenasa/metabolismo , Células CACO-2 , Supervivencia Celular/efectos de los fármacos , Ciclooxigenasa 2/metabolismo , Inhibidores Enzimáticos/farmacología , Células HCT116 , Células HT29 , Humanos , Interferón gamma/metabolismo , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta/química , Polifenoles/farmacología
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