The aim of the present research was to study the effects of an ethanolic extract of Salvia sagittata Ruiz & Pav (SSEE), an endemic Ecuadorian plant traditionally used to treat inflammation and different intestinal affections, on primary cultures of porcine aortic endothelial cells (pAECs). pAECs were cultured in the presence of different concentrations (1-200 μg/mL) of SSEE for 24 h, and cytotoxicity was evaluated by the MTT assay. SSEE did not negatively affect cellular viability at any concentration tested. Cell cycle was analyzed and no significant change was observed. Then, the anti-inflammatory effects of SSEE on pAECs were analyzed using a lipopolysaccharide (LPS) as the inflammatory stimulus. Different markers involved in the inflammatory process, such as cytokines and protective molecules, were evaluated by real-time quantitative PCR and Western blot. SSEE showed the ability to restore pAEC physiological conditions reducing interleukin-6 and increasing Heme Oxygenase-1 protein levels. The phytochemical composition of SSEE was also evaluated via HPLC-DAD and spectrophotometric assays. The presence of different phenolic acids and flavonoids was revealed, with rosmarinic acid as the most abundant component. SSEE possesses an interesting antioxidant activity, as assessed through both the Oxygen Radical Absorbance Capacity (ORAC) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays. In conclusion, results suggest that SSEE is endowed with an in vitro anti-inflammatory effect. This represents the initial step in finding a possible scientific support for the traditional therapeutic use of this plant.
An essential oil was distilled with 0.25% yield from fresh flowers of Dalea mutisii Kunth, a native species mainly growing in the Andean region of Ecuador. A total of 50 compounds were identified, and most of them were quantified. The chemical composition was characterized by the prevalence of monoterpene hydrocarbons (>90%). Major components were α-pinene (42.9%), β-pinene (15.1%), β-phellandrene (12.6%), myrcene (6.7%), and (Z)-β-ocimene (5.4%). The essential oil was then submitted to enantioselective analysis, with a 2,3-diethyl-6-tert-butyldimethylsilyl-β-cyclodextrin-based capillary column. An enantiomeric excess was measured for (1R,5R)-(+)-α-pinene (91.6%), (1R,5R)-(+)-β-pinene (15.2%), (R)-(−)-α-phellandrene (4.8%), and (R)-(−)-β-phellandrene (88.8%), whereas (R)-(+)-limonene was enantiomerically pure. A gas chromatography–olfactometry (GC–O) analysis was additionally carried out on this pleasantly fragrant essential oil, following an aroma extract dilution analysis (AEDA) approach. Main odorants were α-pinene, β-pinene, α-phellandrene, and (Z)-β-ocimene, with dilution factors (FD) of 8, 4, 2, and 2, respectively.
Oreocallis grandiflora (Lam.) R. Br. is an Ecuadorian species belonging to the Proteaceae family, commonly known as cucharillo (Loja and Zamora provinces), cucharilla (Sierra region), gañal (Bolívar province), and algil (Chimborazo province). Its leaves and flowers, collected during blooming, are traditionally used for oral administration to treat liver diseases, vaginal bleeding, and ovary/uterus inflammation and as digestive, diuretic, and hypoglycemic remedy. Related literature does not report any scientific evidences regarding the chemical composition of the used parts of this species (leaves and flowers), while few indications are reported about the healthy properties of their preparations. Based on these premises, the present research was performed with the objectives to fill the gaps of the chemical and biological knowledge about this species, enriching the knowledge related to the plant biodiversity of Amazonian Ecuador and to the ethnobotanical tradition of Andean communities. Chemical and biological investigation (in vitro antioxidant and anti-inflammatory activity) of flower and leaf hydroalcoholic extracts shed a light on the functional metabolites putatively involved in healthy properties of the O. grandiflora traditional preparations. The chemical fingerprinting achieved by HPTLC and 1HNMR analyses showed the presence of flavonoids, subsequently quantitatively estimated by AlCl3 complexation assay and HPLC-DAD. Silica gel chromatography allowed the isolation of the main compounds of the flower extract: quercetin 3-O-β-glucuronide and myricetin 3-O-β-glucuronide. RP-HPLC-DAD-MS analyses showed the presence of quercetin 3-O-rutinoside and isorhamnetin 3-O-rutinoside, in addition to the above-mentioned molecules, in the leaf extract. Regarding the antioxidant (DPPH test, a radical scavenging assay) and anti-inflammatory (WST-1 assay, an oxidative burst test) activities, leaf extract showed the most promising results when compared to the positive controls. The same extract, however, exhibited a higher cytotoxicity compared to the flower extract, indicating the latter preparation as the most interesting anti-inflammatory crude drug.
Natural products are one of the main sources for developing new drugs. The alkaloids obtained from the plant family Amaryllidaceae have interesting structures and biological activities, such as acetylcholinesterase inhibition potential, which is one of the mechanisms used for the palliative treatment of Alzheimer’s disease symptoms. Herein we report the alkaloidal profile of bulbs and leaves extracts of Crinum × amabile collected in Ecuador and their in vitro inhibitory activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. Using Gas Chromatography coupled to Mass Spectrometry (GC-MS), we identified 12 Amaryllidaceae alkaloids out of 19 compounds detected in this species. The extracts from bulbs and leaves showed great inhibitory activity against AChE and BuChE, highlighting the potential of Amaryllidaceae family in the search of bioactive molecules.
Objective: The aim of this research was to evaluate the photoprotective effect of Oreocallis grandiflora hydroalcoholic extract (OGHE) against ultraviolet (UV)B-induced cell death model on a strain of Escherichia coli (ATCC 25922) and to determine the sun protection factor (SPF) using the equation proposed by Mansur.Methods: OGHE was obtained from leaves of O. grandiflora, following a standardized methodology. In short, O. grandiflora leaves were extracted with ethanol 70% v/v and defatted with n-hexane, hydroalcoholic fraction was concentrated under controlled conditions through rotary evaporator, and finally, the residue was freeze drying to obtain OGHE. The photoprotective effect was carried out using in vitro UVB-induced cell death model on a strain of E. coli (ATCC 25922), like a first approach to study its potential application on cosmetics. Results and Conclusions:From results, O. grandiflora is an important resource to produce new cosmetic products. However, the safety of OGHE is necessary to a rational development in that sense. OGHE shows advantages in relation to conventional active compounds of commercial sunscreens used in this research (2-ethylhexyl 4-methoxycinnamate and 2-ethylhexyl 4-(dimethylamino)benzoate) at the concentration of 2 mg/mL, on survivor time (with OGHE until 120 min), range of inactivation of E. coli caused by UVB (OGHE K value minor against to positive controls), and high SPF (13.56±0.21).
Parmelina tiliacea es una especie de liquen de Ecuador que ha sido poco estudiada en relación a sus potenciales aplicaciones. La investigación se llevó a cabo con el objetivo de establecer la actividad antiinflamatoria y citotóxica de P. tiliacea, mediante un método celular in vitro basado en el uso de una sal de tetrazolio solu- ble (WST-1) sobre neutrófilos aislados. Las moléculas de atranorina y dilactona del ácido pulvínico fueron aisladas del liquen P. tiliacea mediante métodos cromatográficos (cromatografía flash en columna y TLC). Los compuestos fueron identificados con la ayuda de estudios espectroscópicos (UV e IR), cromatográficos (TLC) y pruebas de identificación específicas para compuestos liquénicos usando reactivos químicos establecidos para este tipo de moléculas. Los resultados de actividad citotóxica mostraron una reducción de la viabilidad celular hasta un 15 – 20% a una concentración de 200 μg/mL de ambos compuestos identificados. A la misma concentración de 200 μg/mL, la actividad antiinflamatoria de atranorina, dilactona del ácido pulvínico y ácido acetilsalicílico (control positivo) fueron 75.92±0.73%, 73.65±0.44% y 83.77±0.47%, respectivamente. Este estudio constituye la base para investigaciones posteriores sobre líquenes en el Ecuador.
La variedad climática y la ubicación territorial del Ecuador favorece la diversidad biológica en el país. Sin embargo, debido a la presencia de gran número de flora y fauna por kilómetro cuadrado, la mayor parte no se encuentra estudiada, y a pesar de no contar con argumento científico para el uso de algunas especies vegetales, la población utiliza muchas de éstas para diferentes patologías, por lo que se realizó el estudio farmacológico de seis especies del género Passiflora de la provincia de Chimborazo – Ecuador, empleadas tradicionalmente para tratar el nerviosismo. Para la identificación se llevó a cabo un perfil de cromatografía en capa fina de cada especie, de los que se pudieron determinar cantidades considerables de moléculas con agrupamiento de tipo flavónico y cuantificación de los flavonoides totales. De las especies estudiadas P. manicata se destacó por su elevado contenido de flavonoides totales usando el método de cloruro de aluminio para derivatizar los compuestos de interés y poder evaluarlos mediante espectrofotometría UV-visible. Mientras que para la actividad farmacológica se llevó a cabo in vivo mediante el modelo de laberinto en cruz elevado. De los resultados obtenidos se ha logrado determinar que al menos dos de las seis especies tienen actividad ansiolítica significativa a las dosis de 25 y 50 mg/kg de extracto hidroalcohólico, siendo P. mixta y P. edulis las especies vegetales que en su composición presentarían constituyentes bioactivos para tal efecto.
Dos productos naturales, aceites esenciales de Cannabis sativa (cannabis) y Baccharis latifolia (chilca), fueron empleados como ingredientes antinflamatorios en un ungüento de aplicación tópica. Para medir la eficacia, las diversas fórmulas diseñadas a base de estos dos aceites esenciales fueron evaluadas in vivo, mediante el método de inducción del edema subplantar en ratas, como control positivo se empleó una formulación de venta libre con ingrediente activo diclofenaco al 1 %. La evaluación química de los dos aceites presentó para el aceite de chilca los siguientes componentes principales: ligulóxido 14.02 %, andro encecalinol 9.84 %, kesano 7.53 %, limoneno 5.6 % y Z-cadin-4-en-7-ol con el 5.03 %; mientras que en el aceite esencial de cannabis las moléculas más abundantes fueron: E-cariofileno 27.91 %, mirceno 21,19 %, α-pineno 8.05 %, α-humuleno 8.03 %, limoneno 7.18 %, terpinoleno 7.12 % y β-pineno 4.68 %. Los resultados de la investigación señalan que aquellas fórmulas con mezclas de los dos aceites esenciales en la formulación al 1 %, son las que poseen la mayor actividad antiinflamatoria, desde el punto de vista estadístico la significancia es alta en relación al control positivo en aquellas cuya composición de aceites es la siguiente: aceite esencial de cannabis 75 % y aceite de chilca 25 %, y aceite esencial de cannabis 50 % y aceite de chilca 50 %. El resto de las formulaciones presentan actividad, pero esta es similar a la de la fórmula comercial usada como control. De los resultados encontrados se puede proponer a ambos productos naturales como antinflamatorios, y prever el diseño y comercialización de medicamentos farmacéuticos tópicos usando a estos dos aceites esenciales.
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