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1.
Heliyon ; 4(10): e00834, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-30302412

RESUMEN

Blueberry ash (Elaeocarpus reticulatus Sm.) fruit has potential for human nutrition, but there is limited information on this fruit. This preliminary study aimed to characterise blueberry ash fruit and examine the influence of extraction solvents on its phytochemical and antioxidant properties. Blueberry ash fruit is dark blue in colour and is a stone fruit of small size (7 mm) and light weight (0.2 g). However, it has a high portion of flesh (60% of fruit weight), which is edible and can be a potential source of phytochemicals. Water, ethanol, acetonitrile, acetone, and their combination were tested for extraction of phytochemicals from flesh of this fruit. Water or absolute organic solvent was ineffective for extraction of phenolic compounds from this fruit, but mixtures of water and organic solvents were more effective, and 50% acetone was the most suitable extraction solvent. Extraction with 50% acetone, this fruit was found to contain high levels of total phenolic content, flavonoids, proanthocyanidins, and anthocyanins (104 mg GAE/g, 155 mg RUE/g, 78 mg CE/g, and 119 mg CGE/g, respectively). In addition, this fruit was found to possess potent antioxidant properties. Therefore, this fruit should be further studied for identification of its phenolic compounds and further tested for their biological properties.

2.
Pancreas ; 47(6): 690-707, 2018 07.
Artículo en Inglés | MEDLINE | ID: mdl-29894418

RESUMEN

Pancreatic cancer (PC) is one of the most devastating human cancers, and despite the significant advances in the current therapeutic options, the overall survival rate for PC has remained static for the past 50 years. Plant-derived bioactive compounds play a vital role in cancer therapeutics by providing new lead compounds for future drug development. Therefore, the isolation, characterization, and identification of new bioactive compounds for the prevention and treatment of cancer continue to be an important aspect of natural product research. Many in vitro and in vivo studies published in the last few decades have established strong links between the phytochemical profile of eucalypts and anticancer activity. However, only a small number of these reports have attempted to demonstrate a relationship between the biological activity of eucalypt extracts and PC. This review focuses on potential anti-PC effects of an array of bioactive compounds present in various species of eucalypts. It also highlights the necessity for further in vitro and in vivo studies to develop a complete understanding of the potential this group of plants has for the development of potent and specific chemotherapeutic drugs for PC.


Asunto(s)
Antineoplásicos Fitogénicos/uso terapéutico , Productos Biológicos/uso terapéutico , Eucalyptus/química , Neoplasias Pancreáticas/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Australia , Productos Biológicos/química , Eucalyptus/clasificación , Humanos , Estructura Molecular , Fitoterapia/métodos , Especificidad de la Especie
3.
Biomed Pharmacother ; 105: 449-460, 2018 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29879629

RESUMEN

New therapeutic strategies such as the development of novel drugs and combinatorial therapies with existing chemotherapeutic agents are urgently needed to improve the clinical prognosis of pancreatic cancer. We have previously reported the antiproliferative properties of aqueous crude Eucalyptus microcorys extract against pancreatic cancer cell lines. In this study, bioassay-guided fractionation of the aqueous crude E. microcorys extract using RP-HPLC and subsequent assessment of the resultant fractions (F1-F5) for their antioxidant activity and cytotoxicity against pancreatic cancer cell lines were performed. The molecular mechanisms associated with the cytotoxicity was characterised by studying the effects of the most potent fraction-1 (F1) on apoptosis and cell cycle profiles as well as its phytochemical constituents by LC-ESI/MS/MS. F1 displayed significantly greater antioxidant activity in three different assays (p < 0.05). Moreover, F1 exhibited significantly greater antiproliferative activity (IC50 = 93.11 ±â€¯3.43 µg/mL) against MIA PaCa-2 cells compared to the other four fractions (p < 0.05). F1 induced apoptosis by regulating key apoptotic proteins- Bcl-2, Bak, Bax, cleaved PARP, procaspase-3 and cleaved caspase-3 in MIA PaCa-2 cells, suggesting the involvement of intrinsic mitochondrial apoptotic pathway and arrested cells at G2/M phase. A combination of gemcitabine and F1 exerted a greater effect on apoptosis and cell cycle arrest than F1 or gemcitabine alone (p < 0.05). LC-ESI/MS/MS revealed the tentative identities of phytochemicals present in F1 and their similarities with the phenolic compounds previously reported in Eucalyptus with antipancreatic cancer activity. Our study shows that the polyphenol and antioxidant-rich fraction of E. microcorys extract is a promising candidate for developing mono or combination therapies against pancreatic cancer.


Asunto(s)
Apoptosis , Puntos de Control del Ciclo Celular , Eucalyptus/química , Neoplasias Pancreáticas/patología , Extractos Vegetales/química , Hojas de la Planta/química , Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Proteínas Reguladoras de la Apoptosis/metabolismo , Ciclo Celular/efectos de los fármacos , Puntos de Control del Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Cromatografía de Fase Inversa , Humanos
4.
In Vitro Cell Dev Biol Anim ; 53(7): 604-615, 2017 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-28452004

RESUMEN

In spite of the recent advancements in oncology, the overall survival rate for pancreatic cancer has not improved over the last five decades. Eucalypts have been linked with cytotoxic and anticancer properties in various studies; however, there is very little scientific evidence that supports the direct role of eucalypts in the treatment of pancreatic cancer. This study assessed the anticancer properties of aqueous and ethanolic extracts of four Eucalyptus species using an MTT assay. The most promising extracts were further evaluated using a CCK-8 assay. Apoptotic studies were performed using a caspase 3/7 assay in MIA PaCa-2 cells. The aqueous extract of Eucalyptus microcorys leaf and the ethanolic extract of Eucalyptus microcorys fruit inhibited the growth of glioblastoma, neuroblastoma, lung and pancreatic cancer cells by more than 80% at 100 µg/mL. The E. microcorys and Eucalyptus saligna extracts showed lower GI50 values than the ethanolic Eucalyptus robusta extract in MIA PaCa-2 cells. Aqueous E. microcorys leaf and fruit extracts at 100 µg/mL exerted significantly higher cell growth inhibition in MIA PaCa-2 cells than other extracts (p < 0.05). Statistically similar IC50 values (p > 0.05) were observed in aqueous E. microcorys leaf (86.05 ± 4.75 µg/mL) and fruit (64.66 ± 15.97 µg/mL) and ethanolic E. microcorys leaf (79.30 ± 29.45 µg/mL) extracts in MIA PaCa-2 cells using the CCK-8 assay. Caspase 3/7-mediated apoptosis and morphological changes of cells were also witnessed in MIA PaCa-2 cells after 24 h of treatment with the extracts. This study highlighted the significance of E. microcorys as an important source of phytochemicals with efficacy against pancreatic cancer cells. Further studies are warranted to purify and structurally identify individual compounds and elucidate their mechanisms of action for the development of more potent and specific chemotherapeutic agents for pancreatic cancer.


Asunto(s)
Antineoplásicos/farmacología , Eucalyptus/química , Extractos Vegetales/farmacología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Forma de la Célula/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Desoxicitidina/análogos & derivados , Desoxicitidina/farmacología , Humanos , Concentración 50 Inhibidora , Gemcitabina
5.
Chem Biodivers ; 14(3)2017 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-27935659

RESUMEN

While the pharmacological and toxicological properties of eucalypts are well known in indigenous Australian medicinal practice, investigations of the bioactivity of eucalypt extracts against high mortality diseases such as pancreatic cancer in Western medicine have to date been limited, particularly amongst the genera Corymbia and Angophora. Four Angophora and Corymbia species were evaluated for their phytochemical profile and efficacy against both primary and secondary pancreatic cancer cell lines. The aqueous leaf extract of Angophora hispida exhibited statistically higher total phenolic content (107.85 ± 1.46 mg of gallic acid equiv. per g) and total flavonoid content (57.96 ± 1.93 mg rutin equiv. per g) and antioxidant capacity compared to the other tested eucalypts (P < 0.05). Both A. hispida and A. floribunda aqueous extracts showed statistically similar saponin contents. Angophora floribunda extract exerted significantly greater cell growth inhibition of 77.91 ± 4.93% followed by A. hispida with 62.04 ± 7.47% (P < 0.05) at 100 µg/ml in MIA PaCa-2 cells with IC50 values of 75.58 and 87.28 µg/ml, respectively. More studies are required to isolate and identify the bioactive compounds from these two Angophora species and to determine their mode of action against pancreatic malignancies.


Asunto(s)
Myrtaceae/química , Fitoquímicos/química , Fitoquímicos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/química , Australia , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Humanos , Myrtaceae/metabolismo , Neoplasias Pancreáticas/metabolismo , Neoplasias Pancreáticas/patología , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/química , Hojas de la Planta/química , Hojas de la Planta/metabolismo , Saponinas/análisis
6.
Chem Biodivers ; 12(6): 907-24, 2015 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-26080737

RESUMEN

The genus Eucalyptus (Myrtaceae) is mainly native to Australia; however, some species are now distributed globally. Eucalyptus has been used in indigenous Australian medicines for the treatment of a range of aliments including colds, flu, fever, muscular aches, sores, internal pains, and inflammation. Eucalyptus oils containing volatile compounds have been widely used in the pharmaceutical and cosmetics industries for a multitude of purposes. In addition, Eucalyptus extracts containing nonvolatile compounds are also an important source of key bioactive compounds, and several studies have linked Eucalyptus extracts with anticancer properties. With the increasing research interest in Eucalyptus and its health properties, this review briefly outlines the botanical features of Eucalyptus, discusses its traditional use as medicine, and comprehensively reviews its phytochemical and anticancer properties and, finally, proposes trends for future studies.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Eucalyptus/química , Fitoquímicos/química , Extractos Vegetales/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Proliferación Celular/efectos de los fármacos , Humanos , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación
7.
Antioxidants (Basel) ; 4(4): 647-61, 2015 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-26783950

RESUMEN

Euphorbia tirucalli is a succulent shrub or small tree that is native to the African continent, however, it is widely cultivated across the globe due to its use in traditional medicines to treat ailments, ranging from scorpion stings to HIV. Recent studies have identified compounds present in the latex of the plant, including a range of bi- and triterpenoids that exhibit bioactivity, including anticancer activity. This study aimed to optimize water extraction conditions for high-yield total phenolic content recovery, to prepare methanol and aqueous extracts from the aerial sections of the plant, and to test the phytochemical, antioxidant, and anti-cancer properties of these extracts. Water extraction of total phenolic compounds (TPC) was optimized across a range of parameters including temperature, extraction time, and plant mass-to-solvent ratio. The water extract of the E. tirucalli powder was found to contain TPC of 34.01 mg GAE (gallic acid equivalents)/g, which was approximately half that of the methanol extract (77.33 mg GAE/g). The results of antioxidant assays showed a uniform trend, with the methanol extract's antioxidant reducing activity exceeding that of water extracts, typically by a factor of 2:1. Regression analysis of the antioxidant assays showed the strongest correlation between extract TPC and antioxidant activity for the ABTS (2,2-azino-bis(3-ethyl-benzothiazoline-6-sulfonic acid) and DPPH (2,2-diphenyl-1-picrylhydrazyl) methods. The methanol extract also showed greater growth inhibition capacity towards the MiaPaCa-2 pancreatic cancer cell line. These data suggest that further investigations are required to confirm the source of activity within the E. tirucalli leaf and stems for potential use in the nutraceutical and pharmaceutical industries.

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