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1.
Plants (Basel) ; 10(4)2021 Mar 26.
Artigo em Inglês | MEDLINE | ID: mdl-33810509

RESUMO

Three specimens of H. officinalis subsp. aristatus were collected in three areas of the Abruzzo region (Italy) and subjected to macroscopic and microscopic observation to support their botanical identification. The essential oils (EOs) obtained from the aerial parts of the samples were characterized with the object to define their phytochemical and pharmaceutical biology profile. They highlight three different chemotypes, including one never seen in previous literature (CIV17-EO, distilled from sample harvested in 2017 at Civitaretenga), that showed a fingerprinting with the predominance of (-)-limonen-10-yl-acetate (67.9%). In 2017 European Food Safety Authority (EFSA) reported the genotoxicity of similar compounds, therefore, to dismiss any safety concern for the CIV17-EO use as flavouring substance, the Ames test was performed with no evidence of mutagenic activity. Safety of use coupled with chemical characterization of this new chemotype set the stage for a better standardization of H. officinalis EOs. The ethanolic extracts, on the other hand, with qualitatively similar chemical profiles in which caftaric, chlorogenic and rosmarinic acid were the main molecules, showed interesting antioxidant activity and a slight cytotoxicity towards the A549 cell line that could indicate a starting point for the evaluation of an additional preventive tool for maintaining health status.

2.
Foods ; 9(10)2020 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-33080917

RESUMO

Plant secondary metabolites possess chemopreventive and antineoplastic properties, but the lack of information about their exact mechanism of action in mammalian cells hinders the translation of these compounds in suitable therapies. In light of this, firstly, Origanum vulgare L. hydroalcoholic extract was chemically characterized by spectrophotometric and chromatographic analyses; then, the molecular bases underlying its antitumor activity on B16-F10 and A375 melanoma cells were investigated. Oregano extract induced oxidative stress and inhibited melanogenesis and tumor cell proliferation, triggering programmed cell death pathways (both apoptosis and necroptosis) through mitochondria and DNA damage. By contrast, oregano extract was safe on healthy tissues, revealing no cytotoxicity and mutagenicity on C2C12 myoblasts, considered as non-tumor proliferating cell model system, and on Salmonella strains, by the Ames test. All these data provide scientific evidence about the potential application of this food plant as an anticancer agent in in vivo studies and clinical trials.

3.
Plants (Basel) ; 9(9)2020 Aug 19.
Artigo em Inglês | MEDLINE | ID: mdl-32825034

RESUMO

The climate emergency and the risks to biodiversity that the planet is facing nowadays, have made the management of food resources increasingly complex but potentially interesting. According to FAO, one-third of the edible parts of food produced throughout the whole food supply chain gets lost or wasted globally every year. At the same time, demographic growth makes it necessary to change course toward sustainable economic development in order to satisfy market demands. The European Union supported the idea of a Circular Economy from 2015 and arranged annual Action Plans toward a greener, climate-neutral economy. Following the biorefinery concept, food waste becomes byproducts that can be recovered and exploited as high added-value materials for industrial applications. The use of sustainable extraction processes to manage food byproducts is a task that research has to support through the development of low environmental impact strategies. This review, therefore, aims to take stock of the possibilities of extracting molecules from food waste biomass following ecopharmacognostic approaches inspired by green chemistry guidelines. In particular, the use of innovative hybrid techniques to maximize yields and minimize the environmental impact of processes is reviewed, with a focus on bound phenolic extractions.

4.
Molecules ; 24(19)2019 Sep 20.
Artigo em Inglês | MEDLINE | ID: mdl-31546987

RESUMO

Both environmental and economic issues are increasingly pushing for the revalorization of agri-food by-products, including those arising from wine industry. Wastes produced from wine-making processes are important sources of biologically active compounds, mainly phenolic acids and flavonoids, which could be re-used for several applications, for example as additive surrogates or new ingredients in foodstuffs and/or pharmaceuticals. Therefore, the development of methods aimed at isolating, characterizing and quantifying molecules present in winery by-products acquires considerable importance in view of their re-utilization on a large scale. In this connection, this study demonstrated that high-performance thin-layer chromatography (HPTLC) and high-performance liquid chromatography with diode array detection (HPLC-DAD) can operate in synergy for the investigation of pomace and seed materials arising from both white and red cultivars of Vitis Vinifera. By virtue of fingerprint profiling, mass spectrometry (MS) interfacing and band comparison method, HPTLC enabled detection and identification of phenolic acids, non-anthocyanic flavonoids and anthocyanins. On the contrary, only anthocyanins could be identified by HPLC-DAD, and their subsequent quantification showed that malvidin-3-O-glucoside (oenin) was the most abundant one. In parallel, HPTLC has allowed to detect and quantify proanthocyanidins (PAC), showing that only catechin was present in the test samples. Both quantitative analytical methods were validated in terms of linearity, detection and quantification limits and precision.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Cromatografia em Camada Delgada/métodos , Vitis/química , Vinho , Antocianinas/análise , Flavonoides/análise , Glucosídeos/análise
5.
Sci Rep ; 9(1): 7199, 2019 05 10.
Artigo em Inglês | MEDLINE | ID: mdl-31076590

RESUMO

Proteasome inhibition represents an important anticancer strategy. Here, we studied the mechanisms at the basis of the pro-apoptotic activity of the standardized decoction of Hemidesmus indicus, a plant evoking a complex anticancer activity, and explored its inhibition of proteasome activity in human leukemia cells. Additionally, we preliminary tested the cytotoxicity of some H. indicus's phytochemicals on leukemia cells and their intestinal absorption on a human intestinal epithelium model consisting of a monolayer of differentiated Caco2 cells. We observed a potent antileukemic effect for H. indicus, imputable to the modulation of different critical targets at protein and mRNA levels and the reduction of the 26S proteasome expression. We found that some phytomarkers of H. indicus decoction passed through the enterocyte monolayer. Overall, our study supports the pharmacological potential of H. indicus, which can represent an interesting botanical drug in the oncological area.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Hemidesmus/química , Inibidores de Proteassoma/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Antineoplásicos Fitogênicos/química , Células CACO-2 , Diferenciação Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Absorção Intestinal , Células Jurkat , MicroRNAs/genética , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Complexo de Endopeptidases do Proteassoma/genética , Complexo de Endopeptidases do Proteassoma/metabolismo , Inibidores de Proteassoma/química
6.
J Ethnopharmacol ; 244: 111932, 2019 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-31128149

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Hedyosmum (family: Chloranthaceae) represents an interesting source of natural active compounds, and the 45 species of this genus are widespread in Central and South America and to a lesser extent Southeast Asia (southern China and western Malaysia). Several species are traditionally used in folk medicine. However, the data made available in recent years have not been organized and compared. AIM OF THIS REVIEW: The present study is a critical assessment of the state-of-the-art concerning the traditional uses, the phytochemistry and the pharmacology of species belonging to the genus Hedyosmum to suggest further research strategies and to facilitate the exploitation of the therapeutic potential of Hedyosmum species for the treatment of human disorders. MATERIALS AND METHODS: The present review consists of a systematic overview of scientific literature concerning the genus Hedyosmum published between 1965 and 2018. Moreover, an older text, dated from 1843, concerning the traditional uses of H. bonplandianum Kunth has also been considered. Several databases (Francis & Taylor, Google Scholar, PubMed, SciELO, SciFinder, Springer, Wiley, and The Plant List Database) have been used to perform this work. RESULTS: Sixteen species of the genus Hedyosmum have been mentioned as traditional remedies, and a large number of ethnomedicinal uses, including for the treatment of pain, depression, migraine, stomach-ache and ovary diseases, have been reported. Five species have been used as flavouring agents, tea substitutes or foods. Sesterterpenes, sesquiterpene lactones, monoterpenes, hydroxycinnamic acid derivatives, flavonoids, and neolignans have been reported as the most important compounds in these species. Studies concerning their biological activities have shown that members of the Hedyosmum genus possesses promising biological properties, such as analgesic, antinociceptive, antidepressant, anxiolytic, sedative, and hypnotic effects. Preliminary studies concerning the antibacterial, antioxidant, antiplasmodial, and antifungal activities of these plants as well as their cytotoxic activities against different tumour cell lines have been reported. Some active compounds from the Hedyosmum genus have been used as starting points for the innovative and bioinspired development of synthetic molecules. A critical assessment of these papers has been performed, and some conceptual and methodological problems have been identified regarding the materials and methods and the experimental design used in these studies, including a lack of ethnopharmacological research. CONCLUSIONS: The present review partially confirms the basis for some of the traditional uses of Hedyosmum species (mainly H. brasiliense) through preclinical studies that demonstrated their antinociceptive and neuroprotective effects. Due to promising preliminary results, further studies should be conducted on 13-hydroxy-8,9-dehydroshizukanolide and podoandin. Moreover, several essential oils (EOs) from this genus have been preliminarily investigated, and the cytotoxic and antibacterial activities of H. brasiliense and H. sprucei EOs certainly deserve further investigation. From the promising findings of the present analysis, we can affirm that this genus deserves further research from ethnopharmacological and toxicological perspectives.


Assuntos
Magnoliopsida , Preparações de Plantas/uso terapêutico , Animais , Etnofarmacologia , Humanos , Medicina Tradicional , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Fitoterapia , Preparações de Plantas/química , Preparações de Plantas/farmacologia
7.
Molecules ; 24(8)2019 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-31027274

RESUMO

The chemical composition and biological activity of essential oils isolated from the leaves of Siparuna aspera, Siparuna macrotepala, Piper leticianum, Piper augustum and the rhizome of Hedychium coronarium were evaluated. These species are used medicinally in different ways by the Amazonian communities that live near the Kutukú mountain range. Chemical studies revealed that the main components for the two Siparuna species were germacrene D, bicyclogermacrene, α-pinene, δ-cadinene, δ-elemene, α-copaene and ß-caryophyllene; for the two Piper species ß-caryophyllene, germacrene D, α-(E,E)-farnesene, ß-elemene, bicyclogermacrene, δ-cadinene and for H. coronarium 1,8-cineole, ß-pinene, α-pinene and α-terpineol. The antioxidant activity of all essential oils was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), photochemiluminescence (PCL) quantitative assays, and DPPH and ABTS bioautographic profiles, with different results for each of them. Antimicrobial activity studies were carried out on three yeasts, six Gram positive and four Gram negative bacteria, by means of the disc diffusion method. The essential oil of H. coronarium showed the most relevant results on L. grayi, K. oxytoca and S. mutans, P. augustum and P. leticianum on S. mutans. An antibacterial bioautographic test for H. coronarium was also carried out and highlighted the potential activity of terpinen-4-ol and 1,8-cineole.


Assuntos
Óleos Voláteis/análise , Zingiberaceae/química , Antibacterianos/análise , Antibacterianos/farmacologia , Monoterpenos Bicíclicos , Compostos Bicíclicos com Pontes/análise , Compostos Bicíclicos com Pontes/farmacologia , Monoterpenos Cicloexânicos , Cicloexenos/análise , Cicloexenos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Monoterpenos/análise , Monoterpenos/farmacologia , Óleos Voláteis/farmacologia , Floresta Úmida , Sesquiterpenos/análise , Sesquiterpenos/farmacologia
8.
Parasite ; 26: 23, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30994444

RESUMO

Aedes aegypti, the main arbovirus vector of the Yellow fever, Dengue, Chikungunya and Zika viruses, is widely distributed in tropical and subtropical areas throughout the world. Preventive control efforts have been implemented worldwide aimed at reducing its impact on human health. The recent reduction of chemicals available for vector control due to their negative impact on the environment and human health and the increase in mosquito resistance to insecticides have driven the research community to identify and evaluate sustainable alternatives to synthetic insecticides. In this study, the potential larvicidal effect of essential oils extracted from Ocimum campechianum, Ocotea quixos and Piper aduncum were tested in vitro. GC and GC-MS analyses showed that the main compounds were eugenol (18%), 1,8-cineole (39%) and dillapiole (48%), respectively. Susceptibility to essential oils was measured according to the WHO protocol. After 24 h, the mean percentage mortality ranged from 2.7 to 100% for P. aduncum, from 2.2 to 100% for O. campechianum, and from 2.9 to 100% for O. quixos. The highest potential was displayed by P. aduncum, followed by O. campechianum and O. quixos, with LC50 values of 25.7, 69.3 and 75.5 ppm, respectively. The rapid and effective larvicidal activity of these three oils led us to consider these results to be promising, also considering the possibility of local cultivation of these plants in tropical and subtropical areas and the simple technology for their large-scale preparation and production. Further studies are needed to evaluate the individual components and their activity as larvicides.


Assuntos
Aedes/efeitos dos fármacos , Ocimum/química , Ocotea/química , Óleos Voláteis/farmacologia , Piper/química , Extratos Vegetais/farmacologia , Animais , Larva/efeitos dos fármacos , Mosquitos Vetores/efeitos dos fármacos , Extratos Vegetais/química
9.
Artigo em Inglês | MEDLINE | ID: mdl-30713575

RESUMO

Piper carpunya Ruiz & Pav. (Piperaceae) is a perennial aromatic shrub of Amazonian area of Ecuador and Peru, belonging to the ethnomedicine of these countries. The traditional preparations of the crude drug (fresh leaves used topically as is, and dried leaves in infusions or decoctions) are known for anti-inflammatory, antiulcer, antidiarrheal, antiparasitic effects, and wound healing properties. In light of this traditional evidence, chemical composition (GC-MS) and biological activity, i.e., antioxidant, antifungal (yeast) capacities, and genotoxicity, of Amazonian P. carpunya leaf essential oil (EO) have been investigated in order to valorize some of the putative ethnomedical effects. The EO was obtained through steam distillation of fresh leaves (yield: 7.6 g/kg [0.76%]; refractive index at 20°C: 1.49; density: 0.928 g/mL). Chemical characterization performed through GC-MS evidenced the presence of 21 compounds (96.2% of the total). The most abundant constituents were piperitone (26.2%), limonene (9.5%), elemicin (7.2%), and ß-phellandrene (5.6%). In vitro DPPH antioxidant assay showed a weak radical scavenging ability (IC50) if compared to positive control. Low bioactivity of the EO was also demonstrated against yeast, but it showed an interesting synergistic activity (FIC index of EO+fluconazole) against Candida sp. strains. Ames test evidenced the safety of the EO concerning genotoxicity.

11.
Oncotarget ; 9(24): 17181-17198, 2018 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-29682215

RESUMO

Physical exercise is considered to be one of the beneficial factors of a proper lifestyle and is nowadays seen as an indispensable element for good health, able to lower the risk of disorders of the cardiovascular, endocrine and osteomuscular apparatus, immune system diseases and the onset of potential neoplasms. A moderate and programmed physical exercise has often been reported to be therapeutic both in the adulthood and in aging, since capable to promote fitness. Regular exercise alleviates the negative effects caused by free radicals and offers many health benefits, including reduced risk of all-cause mortality, sarcopenia in the skeletal muscle, chronic disease, and premature death in elderly people. However, physical performance is also known to induce oxidative stress, inflammation, and muscle fatigue. Many efforts have been carried out to identify micronutrients and natural compounds, also known as nutraceuticals, able to prevent or attenuate the exercise-induced oxidative stress and inflammation. The aim of this review is to discuss the benefits deriving from a constant physical activity and by the intake of antioxidant compounds to protect the body from oxidative stress. The attention will be focused mainly on three natural antioxidants, which are quercetin, resveratrol and curcumin. Their properties and activity will be described, as well as their benefits on physical activity and on aging, which is expected to increase through the years and can get favorable benefits from a constant exercise activity.

12.
Eur J Med Chem ; 151: 285-293, 2018 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-29627723

RESUMO

A series of trimethylangelicin (TMA) derivatives were designed and synthesized to overcome the unwanted effects of TMA, promising agent for treatment of inflammation-related diseases and other pathologies, such as cystic fibrosis. The new generation TMA analogues bore hindered substituents at the 4 position in order to minimize or avoid the photoreactions with DNA. Among them, the 4-isopropyl-6-ethyl derivative 23 exhibited TMA-like inhibitory activity on NF-κB/DNA interactions but it proved unable to photoreact with pyrimidine bases of DNA, nor to induce any other DNA damage. The isopropyl analogue 23 was proven to lack mutagenicity when assayed through Ames test and exhibited no anti-proliferative activity on cystic fibrosis IB3-1 cells, displaying at the same time inhibition of the TNF-α induced release of the NF-κB regulated PDGF-B chain, IL-10, IL-15, IL-17 and IFN-γ. Therefore compound 23 deserves further assay to determine its anti-inflammatory properties, since it lacks photoreaction properties and mutagenicity-related side effects.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Furocumarinas/química , Furocumarinas/farmacologia , NF-kappa B/antagonistas & inibidores , Animais , Anti-Inflamatórios/síntese química , Linhagem Celular , DNA/imunologia , Desenho de Fármacos , Furocumarinas/síntese química , Humanos , Interferon gama/imunologia , Interleucina-10/imunologia , NF-kappa B/imunologia , Salmão , Fator de Necrose Tumoral alfa/imunologia
13.
Toxins (Basel) ; 10(2)2018 02 06.
Artigo em Inglês | MEDLINE | ID: mdl-29415441

RESUMO

In traditional Indian medicine, the crude drug Hemidesmus indicus root-commonly known as Indian sarsaparilla-is used alone or in poly-herbal preparations for the treatment of a wide range of diseases. The present study focuses on the cancer chemopreventive and therapeutic potential of H. indicus extracts on an acute lymphoblastic leukemia cell line (CCRF-CEM). With this aim in mind, we subjected H. indicus roots to two subsequent extractions (hydro-alcoholic extraction and soxhlet extraction). As DNA damage is an important prerequisite for the induction of mutations/cancer by genotoxic carcinogens, cancer chemoprevention may be achieved by preventing genotoxicity. Through an integrated experimental approach, we explored the genoprotective potential of the soxhlet H. indicus extract against different mutagenic compounds and its cytotoxic, proapoptotic, and cytostatic properties. In our experimental conditions, H. indicus induced a cytotoxic effect involving the activation of both intrinsic and extrinsic apoptotic pathways and blocked the cell cycle in the S phase. Moreover, the antigenotoxicity results showed that the extract was able to mitigate DNA damage, an essential mechanism for its applicability as a chemopreventive agent, via either the modulation of extracellular and intracellular events involved in DNA damage. These data add to the growing body of evidence that H. indicus can represent a noteworthy strategy to target early and late stages of cancer.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Hemidesmus , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/análise , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Dano ao DNA , Hemidesmus/química , Humanos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Raízes de Plantas/química , Leucemia-Linfoma Linfoblástico de Células Precursoras/tratamento farmacológico , Substâncias Protetoras/farmacologia
14.
Nat Prod Res ; 32(12): 1415-1427, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28670915

RESUMO

Natural products frequently exert pharmacological activities. The present review gives an overview of the ethnobotany, phytochemistry and pharmacology of the Cedrus genus, e.g. cytotoxic, spasmolytic immunomodulatory, antiallergic, anti-inflammatory and analgesic activities. Cancer patients frequently seek remedies from traditional medicinal plants that are believed to exert less side effects than conventional therapy with synthetic drugs. A long-lasting goal of anti-cancer and anti-microbial therapy research is to find compounds with reduced side effects compared to currently approved drugs. In this respect, Cedrus species might be of interest. The essential oil isolated from Cedrus libani leaves may bear potential for drug development due to its high concentrations of germacrene D and ß-caryophyllene. The essential oils from Cedrus species also show bioactivity against bacteria and viruses. More preclinical analyses (e.g. in vivo experiments) as well as clinical trials are required to evaluate the potential of essential oils from Cedrus species for drug development.


Assuntos
Cedrus/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Plantas Medicinais/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios , Antineoplásicos Fitogênicos/farmacologia , Humanos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Sesquiterpenos Policíclicos , Sesquiterpenos/análise
15.
Artigo em Inglês | MEDLINE | ID: mdl-30643525

RESUMO

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-ß-glucuronide and myricetin 3-O-ß-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.

16.
Mediators Inflamm ; 2017: 2389487, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29089668

RESUMO

The angelicin analogue 4,6,4'-trimethylangelicin (TMA) was recently reported as a strong inhibitor of nuclear factor-κB (NF-κB) activity and of the expression of the interleukin-8 (IL-8) gene in bronchial epithelial cells in which the inflammatory response has been challenged with P. aeruginosa, the most common bacterium found in the airways of patients affected by cystic fibrosis (CF). These findings encouraged us to analyze new synthetic analogues of TMA in order to evaluate their biological activities on human bronchial epithelial CF IB3-1 cells and to find more potent anti-NF-κB agents exhibiting only minor antiproliferative effects. Analogues able to inhibit NF-κB/DNA interaction at lower concentration than TMA were found and selected to investigate their biological activity on IB3-1 cells induced with TNF-α. In this biological system, NF-κB-mediated IL-8 gene expression was investigated. Some analogues showed similar activity to the lead compound TMA. Other analogues displayed higher activities; in particular, the most interesting compounds showing relevant anti-inflammatory effects were found to cause 56-83% reduction of IL-8 mRNA expression at low concentrations (1-10 µM), without changes in cell proliferation pattern, demonstrating their potential interest for a possible development of anti-inflammatory therapy of cystic fibrosis.


Assuntos
Fibrose Cística/metabolismo , Furocumarinas/química , Furocumarinas/farmacologia , Interleucina-8/metabolismo , NF-kappa B/metabolismo , Linhagem Celular , Humanos , Interleucina-8/genética , Estrutura Molecular , NF-kappa B/genética
17.
Eur J Med Chem ; 140: 604-614, 2017 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-28992569

RESUMO

Antimicrobial resistance is one of the major and growing concerns in hospital- and community acquired infections, and new antimicrobial agents are therefore urgently required. It was reported that oxidative stress could contribute to the selection of resistant bacterial strains, since reactive oxygen species (ROS) revealed to be an essential driving force. In the present work 4-alkylidene-azetidinones, a new class of antibacterial agents, were functionalized with phytochemical polyphenolic acids such as protocatechuic, piperonyl, caffeic, ferulic, or sinapic acids and investigated as dual target antibacterial-antioxidant compounds. The best candidates showed good activities against multidrug resistant clinical isolates of MRSA (MICs 2-8 µg/mL). Among the new compounds, two revealed the best antioxidant capacity with TEAC-DPPH and TEAC-ABTS being significantly more active than Trolox®.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Azetidinas/química , Polifenóis/química , Azetidinas/farmacologia , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Cromatografia Líquida de Alta Pressão , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Espectroscopia de Prótons por Ressonância Magnética , Espectrometria de Massas por Ionização por Electrospray
18.
J Pharm Biomed Anal ; 146: 1-6, 2017 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-28841426

RESUMO

The genus Echinacea (Asteraceae) includes species traditionally used in phytotherapy. Among them, Echinacea pallida (Nutt.) Nutt. root extracts are characterized by a representative antiproliferative activity, due to the presence of acetylenic compounds. In this study, supercritical fluid extraction (SFE) was applied and compared with conventional Soxhlet extraction (SE) in order to obtain a bioactive extract highly rich in polyacetylenes and polyenes from E. pallida roots. The composition of the extracts was monitored by means of HPLC-UV/DAD and HPLC-ESI-MSn by using an Ascentis Express C18 column (150mm×3.0mm I.D., 2.7µm, Supelco, Bellefonte, PA, USA) with a mobile phase composed of (A) water and (B) acetonitrile, under gradient elution. By keeping SFE time at the threshold of 1h (15min static and 45min dynamic for 1 cycle) with the oven temperature set at 40-45°C and 90bar of pressure, an overall extraction yield of 1.18-1.21% (w/w) was obtained, with a high selectivity for not oxidized lipophilic compounds. The biological activity of the extracts was evaluated against human non-small lung A549 and breast carcinoma MCF-7 cancer cell lines. The cytotoxic effect of the SFE extract was more pronounced towards the MCF-7 than the A549 cancer cells, with IC50 values ranging from 21.01±2.89 to 31.11±2.l4µg/mL; cell viability was affected mainly between 24 and 48h of exposure. The results show the possibility of a new "green" approach to obtain extracts highly rich in genuine polyacetylenes and polyenes from E. pallida roots. The bioactivity evaluation confirmed the cytotoxicity of E. pallida extracts against the considered cancer cell lines, especially against MCF-7 cells, thus suggesting to represent a valuable tool for applicative purposes in cancer prevention.


Assuntos
Echinacea/química , Extratos Vegetais/química , Raízes de Plantas/química , Polienos/química , Poli-Inos/química , Células A549 , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Células MCF-7 , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Polienos/farmacologia , Poli-Inos/farmacologia
19.
Molecules ; 22(8)2017 Jul 29.
Artigo em Inglês | MEDLINE | ID: mdl-28758919

RESUMO

The flavonoid quercetin (3,3',4',5,7-pentahydroxyflavone) is widely distributed in plants, foods, and beverages. This polyphenol compound exhibits varied biological actions such as antioxidant, radical-scavenging, anti-inflammatory, antibacterial, antiviral, gastroprotective, immune-modulator, and finds also application in the treatment of obesity, cardiovascular diseases and diabetes. Besides, quercetin can prevent neurological disorders and exerts protection against mitochondrial damages. Various in vitro studies have assessed the anticancer effects of quercetin, although there are no conclusive data regarding its mode of action. However, low bioavailability, poor aqueous solubility as well as rapid body clearance, fast metabolism and enzymatic degradation hamper the use of quercetin as therapeutic agent, so intense research efforts have been focused on the modification of the quercetin scaffold to obtain analogs with potentially improved properties for clinical applications. This review gives an overview of the developments in the synthesis and anticancer-related activities of quercetin derivatives reported from 2012 to 2016.


Assuntos
Antineoplásicos , Neoplasias/tratamento farmacológico , Quercetina , Animais , Antineoplásicos/síntese química , Antineoplásicos/farmacocinética , Antineoplásicos/farmacologia , Humanos , Neoplasias/metabolismo , Neoplasias/patologia , Quercetina/análogos & derivados , Quercetina/síntese química , Quercetina/farmacocinética , Quercetina/farmacologia
20.
Molecules ; 22(7)2017 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-28704964

RESUMO

In this study, we performed the chemical characterization of Myrcia splendens (Sw.) DC. (Myrtaceae) essential oil from Amazonian Ecuador and the assessment of its bioactivity in terms of cytotoxic, antibacterial, and antioxidant activity as starting point for possible applicative uses. M. splendens essential oil, obtained by hydro-distillation, was analyzed by Gas Chromatography-Mass Spectrometry (GC-MS) and Gas Chromatography-Flame Ionization Detector (GC-FID): the major components were found to be trans-nerolidol (67.81%) and α-bisabolol (17.51%). Furthermore, we assessed the cytotoxic activity against MCF-7 (breast), A549 (lung) human tumor cell lines, and HaCaT (human keratinocytes) non-tumor cell line through 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) test: promising results in terms of selectivity and efficacy against the MCF-7 cell line (IC50 of 5.59 ± 0.13 µg/mL at 48 h) were obtained, mainly due to α-bisabolol. Furthermore, antibacterial activity against Gram positive and negative bacteria were performed through High Performance Thin Layer Chromatography (HPTLC) bioautographic assay and microdilution method: trans-nerolidol and ß-cedren-9-one were the main molecules responsible for the low antibacterial effects against human pathogens. Nevertheless, interesting values of Minimum Inhibitory Concentration (MIC) were noticeable against phytopathogen strains. Radical scavenging activity performed by HPTLC bioautographic and spectrophotometric 1,1-diphenyl-2-picrylhydrazyl (DPPH) approaches were negligible. In conclusion, the essential oil revealed a good potential for plant defense and anti-cancer applications.


Assuntos
Myrtaceae/química , Óleos Voláteis/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Linhagem Celular , Linhagem Celular Tumoral , Equador , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Humanos , Sesquiterpenos Monocíclicos , Óleos Voláteis/farmacologia , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia
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