Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 38
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
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.
Molecules ; 26(1)2020 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-33375454

RESUMO

The essential oil (EO), the methanolic (MeOH), and the 70% ethanolic (70% EtOH) extracts obtained from the aerial parts of Ocimum campechianum Mill. (Ecuador) were chemically characterized through gas-chromatography coupled to mass spectrometry detector (GC-MS), high-performance liquid chromatography coupled to diode array-mass spectrometry detectors (HPLC-DAD-MS) and studied for their in vitro biological activity. The radical scavenger activity, performed by spectrophotometric 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, highlighted significant IC50 values for the EO, extracts and their main constituents (eugenol and rosmarinic acid). EO (and eugenol) showed noteworthy activity against Pseudomonas syringae pv. syringae and a moderate effect against clinical Candida strains, with possible synergism in association to fluconazole against the latter microorganisms. The extracts and pure molecules exhibited weak cytotoxic activity against the HaCat cell line and no mutagenicity against Salmonella typhimurium TA98 and TA100 strains, giving indication of safety. Instead, EO showed a weak activity against adenocarcinomic human alveolar basal epithelial cells (A549). The above-mentioned evidence leads us to suggest a potential use of the crude drug, extracts, and EO in cosmetic formulation and food supplements as antioxidant agents. In addition, EO may also have a possible application in plant protection and anti-Candida formulations.


Assuntos
Cinamatos/farmacologia , Depsídeos/farmacologia , Eugenol/farmacologia , Ocimum/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Células A549 , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Benzotiazóis/química , Compostos de Bifenilo/química , Candida/efeitos dos fármacos , Morte Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Sinergismo Farmacológico , Equador , Fluconazol/farmacologia , Humanos , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Mutagênese , Óleos Voláteis/análise , Picratos/química , Ácidos Sulfônicos/química
3.
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
4.
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
5.
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
6.
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.

7.
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
8.
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
9.
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.

10.
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
11.
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
12.
Front Pharmacol ; 8: 236, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28553226

RESUMO

Extracts from Nigella arvensis L. seeds, which are widely used as anti-inflammatory remedies in traditional medicine of Northern Africa, were able to inhibit the expression of the pro-inflammatory neutrophil chemokine Interleukin (IL)-8 in Cystic Fibrosis (CF) bronchial epithelial IB3-1 cells exposed to the Gram-negative bacterium Pseudomonas aeruginosa. The chemical composition of the extracts led to the identification of three major components, ß-sitosterol, stigmasterol, and campesterol, which are the most abundant phytosterols, cholesterol-like molecules, usually found in plants. ß-sitosterol (BSS) was the only compound that significantly reproduced the inhibition of the P. aeruginosa-dependent expression of IL-8 at nanomolar concentrations. BSS was tested in CF airway epithelial CuFi-1 cells infected with P. aeruginosa. BSS (100 nM), showed a significant and consistent inhibitory activity on expression of the P. aeruginosa-stimulated expression chemokines IL-8, GRO-α GRO-ß, which play a pivotal role in the recruitment of neutrophils in CF inflamed lungs. Preliminary mechanistic analysis showed that BSS partially inhibits the P. aeruginosa-dependent activation of Protein Kinase C isoform alpha, which is known to be involved in the transmembrane signaling activating IL-8 gene expression in bronchial epithelial cells. These data indicate BSS as a promising molecule to control excessive lung inflammation in CF patients.

13.
J Microencapsul ; 34(1): 63-72, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28097914

RESUMO

This study describes the preparation, characterisation and in vitro activity of nanostructured lipid carriers (NLCs) encapsulating natural molecules with antimicrobial activity, such as plumbagin, hydroquinon, eugenol, alpha-asarone and alpha-tocopherol. NLCs were prepared by melt and ultrasonication method, characterised by Cryo-TEM for morphology and SdFFF for dimensional distribution and active encapsulation yields. In vitro tests were conducted on bacteria, fungi and human cell cultures. In vitro tests demonstrated that plumbagin is strongly toxic towards F. oxysporum especially when active molecules are loaded on NLC. Plumbagin was completely non toxic on cyanobacterial model strain up to a threshold over which cell viability was completely lost. NLC loaded with active molecules showed a lower toxicity as compared to their free form on human cultured cells. Although further studies need to be performed, these systems can be potentially proposed to control phytopathogenic organisms.


Assuntos
Anti-Infecciosos/administração & dosagem , Portadores de Fármacos/química , Lipídeos/química , Nanoestruturas/química , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Linhagem Celular , Cianobactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Humanos , Micoses/tratamento farmacológico , Nanoestruturas/ultraestrutura
14.
Int J Food Microbiol ; 238: 33-39, 2016 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-27591384

RESUMO

The identification of effective antimicrobial agents also active on biofilms is a topic of crucial importance in food and industrial environment. For that purpose methanol extracts of Turkish plants, Ficus carica L., Juglans regia L., Olea europaea L., Punica granatum L. and Rhus coriaria L., were investigated. Among the extracts, P. granatum L. and R. coriaria L. showed the best antibacterial activity with minimum inhibitory concentrations (MIC) of 78-625µg/ml for Listeria monocytogenes and Staphylococcus aureus and 312-1250µg/ml for Escherichia coli and Pseudomonas aeruginosa. SubMICs produced a significant biofilm inhibition equal to 80-60% for L. monocytogenes and 90-80% for S. aureus. The extracts showed also the highest polyphenol content and the strongest antioxidant activity. Bioassay-guided and HPLC procedures demonstrated the presence of apigenin 4'-O-ß-glucoside in P. granatum L. and myricetrin and quercitrin in R. coriaria L. Antigenotoxicity of plant extracts was also observed The present findings promote the value-adding of P. granatum L. and R. coriaria L. leaves as natural antimicrobial/antioxidant agents for control of food-related bacterial biofilms.


Assuntos
Biofilmes/efeitos dos fármacos , Microbiologia de Alimentos , Magnoliopsida/química , Extratos Vegetais/farmacologia , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Metanol/química , Testes de Sensibilidade Microbiana , Folhas de Planta/química
15.
Toxins (Basel) ; 8(5)2016 05 12.
Artigo em Inglês | MEDLINE | ID: mdl-27187469

RESUMO

Cancer chemotherapy is characterized by an elevated intrinsic toxicity and the development of drug resistance. Thus, there is a compelling need for new intervention strategies with an improved therapeutic profile. Immunogenic cell death (ICD) represents an innovative anticancer strategy where dying cancer cells release damage-associated molecular patterns promoting tumor-specific immune responses. The roots of Withania somnifera (W. somnifera) are used in the Indian traditional medicine for their anti-inflammatory, immunomodulating, neuroprotective, and anticancer activities. The present study is designed to explore the antileukemic activity of the dimethyl sulfoxide extract obtained from the roots of W. somnifera (WE). We studied its cytostatic and cytotoxic activity, its ability to induce ICD, and its genotoxic potential on a human T-lymphoblastoid cell line by using different flow cytometric assays. Our results show that WE has a significant cytotoxic and cytostatic potential, and induces ICD. Its proapoptotic mechanism involves intracellular Ca(2+) accumulation and the generation of reactive oxygen species. In our experimental conditions, the extract possesses a genotoxic potential. Since the use of Withania is suggested in different contexts including anti-infertility and osteoarthritis care, its genotoxicity should be carefully considered for an accurate assessment of its risk-benefit profile.


Assuntos
Antineoplásicos/farmacologia , Mutagênicos/farmacologia , Extratos Vegetais/farmacologia , Withania , Trifosfato de Adenosina/metabolismo , Apoptose/efeitos dos fármacos , Cálcio/metabolismo , Calreticulina/metabolismo , Dano ao DNA , Proteínas de Choque Térmico HSP70/metabolismo , Proteínas de Choque Térmico HSP90/metabolismo , Humanos , Células Jurkat , Leucemia de Células T , Estresse Oxidativo/efeitos dos fármacos , Raízes de Plantas
16.
Artigo em Inglês | MEDLINE | ID: mdl-27118979

RESUMO

Bioautography has been used as rapid and easy strategy to detect and identify bioactive fractions/molecules in the never before investigated Hedyosmum sprucei Solms (Chloranthaceae) essential oil (EO). The antioxidant activity, performed through DPPH bioautographic assay and spectrophotometric evaluations (IC50 = 230 ± 10 µg/mL), seemed to be mainly due to α-cadinol and α-muurolol. (HP)TLC bioautography, focused on antimicrobial capacities, pointed out α-cadinol, α-muurolol, τ-muurolol, caryophyllene oxide, and methyleugenol as the most effective compounds against Staphylococcus aureus, considered as testing strain. Moreover, the microdilution method, assessed among a wide panel of microorganisms, revealed Listeria grayi and Staphylococcus aureus as the most sensitive among human tested strains and Clavibacter michiganensis among phytopathogens. GC-MS chemical profile showed that bioactive molecules represented only a small quantity of the whole EO: germacrene D (23.16%), ß-caryophyllene (15.53%), δ-cadinene (5.50%), α-copaene (5.08%), and α-phellandrene (3.48%) were the main compounds, highlighting an uncommon composition among the genus Hedyosmum. Finally, H. sprucei EO was checked for cytotoxic potential against A549 (lung cancer) and MCF-7 (breast cancer) cell lines showing promising cytotoxic effects against both cell lines after 48 h (IC50 A549 = 44.05 ± 2.35 µg/mL; IC50 MCF-7 = 32.76 ± 4.92 µg/mL) and 72 h (IC50 A549 = 43.55 ± 2.80 µg/mL; IC50 MCF-7 = 33.64 ± 0.43 µg/mL).

17.
Chem Biodivers ; 13(1): 66-76, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26765353

RESUMO

The hydrodistilled oil of Cryptocarya massoy bark was characterized by GC-FID and GC/MS analyses, allowing the identification of unusual C10 massoia lactone (3, 56.2%), C12 massoia lactone (4, 16.5%), benzyl benzoate (1, 12.7%), C8 massoia lactone (3.4%), δ-decalactone (5, 1.5%), and benzyl salicylate (2, 1.8%) as main constituents. The phytotoxic activities of the oil, three enriched fractions (lactone-rich, ester-rich, and sesquiterpene-rich), and four constituents (compounds 1, 2, 5, and δ-dodecalactone (6)) against Lycopersicon esculentum and Cucumis sativus seeds and seedlings were screened. At a concentration of 1000 µl/l, the essential oil and the massoia lactone-rich fraction caused a complete inhibition of the germination of both seeds, and, when applied on tomato plantlets, they induced an 85 and 100% dieback, respectively. These performances exceeded those of the well-known phytotoxic essential oils of Syzygium aromaticum and Cymbopogon citratus, already used in commercial products for the weed and pest management. The same substances were also evaluated against four phytopathogenic bacteria and ten phytopathogenic fungi, providing EC50 values against the most susceptible strains in the 100-500 µl/l range for the essential oil and in the 10-50 µl/l range for compound 6 and the lactone-rich fraction. The phytotoxic behavior was related mainly to massoia lactones and benzyl esters, while a greater amount of 6 may infer a good activity against some phytopathogenic fungi. Further investigations of these secondary metabolites are warranted, to evaluate their use as natural herbicides.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Cryptocarya/química , Fungos/efeitos dos fármacos , Óleos Vegetais/farmacologia , Sementes/efeitos dos fármacos , Antibacterianos/isolamento & purificação , Antibacterianos/toxicidade , Antifúngicos/isolamento & purificação , Antifúngicos/toxicidade , Cucumis sativus/efeitos dos fármacos , Cucumis sativus/crescimento & desenvolvimento , Relação Dose-Resposta a Droga , Lycopersicon esculentum/efeitos dos fármacos , Lycopersicon esculentum/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Estrutura Molecular , Casca de Planta/química , Óleos Vegetais/química , Óleos Vegetais/isolamento & purificação , Sementes/crescimento & desenvolvimento , Relação Estrutura-Atividade
18.
Nutr Cancer ; 67(4): 664-75, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25837780

RESUMO

The frequent failure of standard cancer chemotherapy requires the development of novel drugs capable of killing otherwise drug-resistant tumors. Here, we have investigated a chloroform extract of Laurus nobilis seeds. Fatty acids and 23 constituents of the volatile fraction were identified by gas chromotography/flame ionization detection (GC/FID) and gas chromatography/mass spectrometry (GC/MS), in good agreement with (1)H NMR (nuclear magnetic resonance) spectrum. Multidrug-resistant P-glycoprotein-expressing CEM/ADR5000 leukemia cells were hypersensitive (collaterally sensitive) toward this extract compared to drug-sensitive CCRF-CEM cells, whereas CEM/ADR5000 cells were 2586-fold resistant to doxorubicin as control drug. Collateral sensitivity was verified by measurement of apoptotic cells by flow cytometry. The log10IC50 values of 3 compounds in the extract (limonene, eucalyptol, oleic acid) did not correlate with mRNA expression of the P-glycoprotein-coding ABCB1/MDR1 gene and accumulation of the P-glycoprotein substrate rhodamine in the NCI panel of tumor cell lines. A microarray-based profile of 20 genes predicted resistance to doxorubicin and 7 other anticancer drugs involved in the multidrug resistance phenotype but not to limonene, eucalyptol and oleic acid. In conclusion, our results show that Laurus nobilis seed extract is suitable to kill multidrug-resistant P-glycoprotein expressing tumor cells.


Assuntos
Resistencia a Medicamentos Antineoplásicos , Laurus/química , Extratos Vegetais/farmacologia , Sementes/química , Subfamília B de Transportador de Cassetes de Ligação de ATP/genética , Subfamília B de Transportador de Cassetes de Ligação de ATP/metabolismo , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Doxorrubicina/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Leucemia/patologia
19.
Phytother Res ; 29(6): 857-63, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25753739

RESUMO

Indian Sarsaparilla (Hemidesmus indicus R. Br.) is widely used in Indian traditional medicine. In the present work, we explored the effects of decoction, traditional Ayurvedic preparation, and hydroalcoholic extract, a phytocomplex more traditionally studied and commercialized as food supplement in western medicine, from the roots as possible source of chemicals with new functional potential linked to their nutritional uses. The antiproliferative and antioxidant properties were assayed. To test antiproliferative affects, different cancer cell lines, growing both as monolayers (CaCo2, MCF-7, A549, K562, MDA-MB-231, Jurkat, HepG2, and LoVo) and in suspension (K562 and Jurkat) were used. The decoction showed strong activity on HepG2 cells, while the hydroalcoholic extracts were active on HepG2, LoVo, MCF-7, K562, and Jurkat cell lines. Weak inhibition of cancer cell proliferation was observed for the principal constituents of the preparations: 2-hydroxy-4-methoxybenzaldehyde, 2-hydroxy-4-methoxybenzoic acid, and 3-hydroxy-4-methoxybenzaldehyde that were tested alone. The antiradical activity was tested with 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)diammonium salt tests and inhibition of nitric oxide production in lipopolysaccharide-stimulated RAW 264.7 macrophages. Interesting result has also been obtained for hydroalcoholic extract regarding genoprotective potential (58.79% of inhibition at 37.5 µg/mL).


Assuntos
Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Hemidesmus/química , Extratos Vegetais/farmacologia , Animais , Linhagem Celular Tumoral/efeitos dos fármacos , Flavonoides/química , Humanos , Macrófagos/efeitos dos fármacos , Medicina Ayurvédica , Camundongos , Extratos Vegetais/química , Raízes de Plantas/química , Polifenóis/química , Proantocianidinas/química
20.
Nat Prod Res ; 29(22): 2071-9, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25612143

RESUMO

Decoctions (DECs) and hydro-alcoholic extracts (HEs) prepared from roots of Boerhaavia diffusa L. (Nyctaginaceae) and Curculigo orchioides Gaertn. (Hypoxidaceae) were phytochemically characterised by HPLC-DAD and profiled for their antioxidant, antigenotoxic and cytotoxic activities. B. diffusa DEC was rich in ferulic acid and vanillin, while the HE also contained boeravinone B and eupalitin. Both C. orchioides HE and DEC displayed the main occurrence of orcinol-ß-d-glucoside and curculigoside A. Antioxidant activity was assayed through spectrophotometric DPPH, ABTS and ß-carotene bleaching test, and using (HP)TLC bioautographic strategies. For both crude drugs, HE was the best performing preparation. Properly modified SOS-Chromotest evidenced a 10% inhibition by phytocomplexes against 4-nitroquinoline-N-oxide, and a higher bioactivity for vanillin (36.60 ± 1.68%) and ferulic acid (35.09 ± 1.53%). C. orchioides HE was the preparation which showed higher cytotoxicity against drug-sensitive human T-lymphoblastoid cell line (CCRF-CEM) and multidrug-resistant leukaemia cell line (CEM/ADR5000), and eupalitin was the only pure compound to exhibit an IC50 value.


Assuntos
Curculigo/química , Nyctaginaceae/química , Compostos Fitoquímicos/análise , Extratos Vegetais/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Linhagem Celular Tumoral , Humanos , Medicina Ayurvédica , Fenóis/química , Fenóis/isolamento & purificação , Raízes de Plantas/química
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...