RESUMO
Naturally occurring coumarins are bioactive compounds widely used in Asian traditional medicine. They have been shown to inhibit proliferation, induce apoptosis, and/or enhance the cytotoxicity of currently used drugs against a variety of cancer cell types. The aim of our study was to examine the antiproliferative activity of different linear furanocoumarins on human rhabdomyosarcoma, lung, and larynx cancer cell lines, and dissolve their cellular mechanism of action. The coumarins were isolated from fruits of Angelica archangelica L. or Pastinaca sativa L., and separated using high-performance counter-current chromatography (HPCCC). The identity and purity of isolated compounds were confirmed by HPLC-DAD and NMR analyses. Cell viability and toxicity assessments were performed by means of methylthiazolyldiphenyl-tetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays, respectively. Induction of apoptosis and cell cycle progression were measured using flow cytometry analysis. qPCR method was applied to detect changes in gene expression. Linear furanocoumarins in a dose-dependent manner inhibited proliferation of cancer cells with diverse activity regarding compounds and cancer cell type specificity. Imperatorin (IMP) exhibited the most potent growth inhibitory effects against human rhabdomyosarcoma and larynx cancer cell lines owing to inhibition of the cell cycle progression connected with specific changes in gene expression, including CDKN1A. As there are no specific chemotherapy treatments dedicated to laryngeal squamous cell carcinoma and rhabdomyosarcoma, and IMP seems to be non-toxic for normal cells, our results could open a new direction in the search for effective anti-cancer agents.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Furocumarinas/farmacologia , Neoplasias Laríngeas/patologia , Rabdomiossarcoma/patologia , Angelica archangelica/química , Apoptose , Ciclo Celular , Linhagem Celular Tumoral , Proliferação de Células , Sobrevivência Celular , Cromatografia , Inibidor de Quinase Dependente de Ciclina p21/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Fibroblastos/efeitos dos fármacos , Citometria de Fluxo , Frutas/química , Humanos , L-Lactato Desidrogenase/metabolismo , Neoplasias Laríngeas/tratamento farmacológico , Pastinaca/química , Rabdomiossarcoma/tratamento farmacológicoRESUMO
In the last decade, there has been growing interest in the food industry in replacing synthetic chemicals with natural products with bioactive properties. This study's aims were to determine the chemical composition and the antioxidant properties of the essential oil of Pastianica sylvestris. The essential oil was isolated with a yield of 0.41% (w/v) by steam distillation from the dried seeds and subsequently analysed by GC-MS. Octyl acetate (78.49%) and octyl hexanoate (6.68%) were the main components. The essential oil exhibited an excellent activity for the inhibition of primary and secondary oxidation products for cold-pressed sunflower oil comparable with butylated hydroxyanisole (BHA) and butylated hydroxytoluene (BHT), which were evaluated using peroxide and thiobarbituric acid values. The antioxidant activity of the essential oil was additionally validated using DPPH radical scavenging (0.0016 ± 0.0885 mg/mL), and ß-carotene-linoleic acid bleaching assays. Also, the amounts of total phenol components (0.0053 ± 0.0023 mg GAE/g) were determined.
Assuntos
Acetatos/química , Antioxidantes/química , Óleos Voláteis/química , Pastinaca/química , Sementes/química , Acetatos/isolamento & purificação , Antioxidantes/isolamento & purificação , Bioensaio , Compostos de Bifenilo/antagonistas & inibidores , Compostos de Bifenilo/química , Hidroxianisol Butilado/química , Hidroxianisol Butilado/isolamento & purificação , Hidroxitolueno Butilado/química , Cromatografia Gasosa-Espectrometria de Massas , Ácido Linoleico/química , Óleos Voláteis/isolamento & purificação , Fenóis/química , Picratos/antagonistas & inibidores , Picratos/química , Extratos Vegetais/química , Óleo de Girassol/química , Tiobarbitúricos/química , beta Caroteno/químicaRESUMO
The aim of this study is to evaluate the in vitro amoebicidal activity of the aqueous extracts of Pastinaca armenea and Inula oculus-christi from Turkey. In the presence of aqueous extracts (ranging from 1.0 to 32.0 mg/ml), numbers of the viable Acanthamoeba castellanii trophozoites and cysts were decreased during the experimental process. Both extracts showed a time- and dose-dependent amoebicidal action on the trophozoites and cysts. Among the extracts tested, I. oculus showed the strongest amoebicidal effect on the trophozoites and cysts. In the presence of 32.00 mg/ml extract solution in the media, no viable trophozoites were determined from the time of 24 h. Moreover, in the presence of 16.00 mg/ml I. oculus-christi extract, no viable trophozoites were detected in 72 h of the experiment. Effectiveness of I. oculus-christi extract was found moderate against the cysts. In the presence of 32.00 mg/ml extract, only 25.3% of the total cysts were killed effectively. In the case of P. armenea, 40.3% and 23.0% of the trophozoites and cysts were killed in the presence of 32.00 mg/ml extract at the end of the experimental process (72 h), respectively.
Assuntos
Acanthamoeba castellanii/efeitos dos fármacos , Amebicidas/farmacologia , Inula/química , Pastinaca/química , Extratos Vegetais/farmacologia , Amebicidas/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Extratos Vegetais/isolamento & purificação , Esporos de Protozoários/efeitos dos fármacos , Fatores de Tempo , Trofozoítos/efeitos dos fármacos , TurquiaRESUMO
As phototoxic skin reactions caused by psoralen are induced by wavelengths within the UVA1 spectrum, we assessed the potential of the small amount of psoralen in a normal diet to provoke phototoxicity in volunteers with skin types I and II. Threshold erythema was unaffected by ingestion of a 200-g portion of parsnip.
Assuntos
Dieta , Eritema/induzido quimicamente , Furocumarinas/efeitos adversos , Transtornos de Fotossensibilidade/induzido quimicamente , Radiossensibilizantes/efeitos adversos , Raios Ultravioleta/efeitos adversos , Adulto , Idoso , Apium/efeitos adversos , Apium/química , Eritema/etiologia , Feminino , Manipulação de Alimentos , Furocumarinas/análise , Temperatura Alta , Humanos , Masculino , Metoxaleno/efeitos adversos , Metoxaleno/análise , Pessoa de Meia-Idade , Pastinaca/efeitos adversos , Pastinaca/química , Transtornos de Fotossensibilidade/etiologia , Epiderme Vegetal/efeitos adversos , Epiderme Vegetal/química , Radiossensibilizantes/análise , Pele/efeitos dos fármacos , Pele/efeitos da radiação , Terapia Ultravioleta/efeitos adversosRESUMO
A dichloromethane extract of root celery yielded falcarinol, falcarindiol, panaxydiol, and the new polyacetylene 8-O-methylfalcarindiol. The structure of the new compound was established by one- and two-dimensional (1D and 2D) NMR, mass spectrometry, and optical rotation data. Nonpolar extracts of roots and bulbs of carrots, celery, fennel, parsley, and parsnip were investigated for their content of polyacetylenes by high-performance liquid chromatography with diode array detection (HPLC-DAD). All five species contained polyacetylenes, although carrots and fennel only in minor amounts. Additionally, the cytotoxicity of the four polyacetylenes against five different cell lines was evaluated by the annexin V-PI assay. Falcarinol proved to be the most active compound with a pronounced toxicity against acute lymphoblastic leukemia cell line CEM-C7H2, with an IC(50) of 3.5 micromol/L. The possible chemopreventive impact of the presented findings is discussed briefly.