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1.
Food Chem Toxicol ; 156: 112483, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34375721

RESUMO

Metabolic variations, antioxidant potential and cytotoxic effects were investigated in the different plant parts like the leaf, stem, flower, pod, and root of C. majus L. using spectroscopic and chromatographic methods. Total phenolics and flavonoids were studied in the different parts of C. majus L., leaf showed higher flavonoid content (137.43 mg/g), while the pod showed the highest phenolic (23.67 mg/g) content, when compared with the stem, flower and root. In the ABTS antioxidant assay, the flower extract showed 57.94% effect, while the leaf, pod and root extract exhibited 39.10%, 36.08% and 28.88% activity, respectively. The pod and leaf extracts demonstrated the potential effect, exhibiting 45.46 and 41.61% activity, respectively, for the DPPH assay. Similar to the phosphomolybdenum assay, the flower revealed higher antioxidant activity (46.82%) than the other plant parts. The in vitro SRB assay facilitated evaluation of the cytotoxic effect against the HeLa and CaSki human cervical cancerous cells. The extract displayed dose-dependent inhibitory effect on both the cell lines. The highest cytotoxic effect was observed in the pod and flower extracts post 48 h of exposure at 1000 µg/mL. The results of C. majus L. offered new insights in the preliminary steps regarding the development of a high value product for phytomedicine applications though promising metabolic variations with antioxidant and anticancer potentials.

2.
Food Chem Toxicol ; 156: 112405, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34273428

RESUMO

The unique structure of Mycobacterium tuberculosis cell envelope provides impermeable barrier against environmental stimuli. In the situation that this barrier is disturbed Mycobacteria react at the transcriptional and translational level to redirect metabolic processes and to maintain integrity of the cell. In this work we aimed to explore the early metabolic response of M. tuberculosis to tanshinones, which are active antimycobacterial compounds of Salvia miltiorrhiza Bunge root. The investigation of the expression of sigma factors revealed the significant shifts in the general bacterial regulatory network, whereas LC-MS metabolomics evidenced the changes in the composition of bacterial cell envelope and indicated altered metabolic pathways. Tanshinones acted via the disruption of the cell envelope surface and generation of reactive oxygen species. Bacteria responded with overproduction of inner region of outer membrane, fluctuations in the production of glycerophosphoinositolglycans, as well as changes in the levels of mycobactins, accompanied by enrichment of metabolic pathways related to redox balance and repair of damages caused by tanshinones.

3.
Int J Mol Sci ; 22(14)2021 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-34299238

RESUMO

This study focused on the biological evaluation and chemical characterization of Geranium pyrenaicum Burm. f. Different solvent extracts (hexane, ethyl acetate, methanol, and water extracts) were prepared. The phytochemical profile, antioxidant, and enzyme inhibitory activity were investigated. Cytotoxicity was assessed using VERO, FaDu, HeLa and RKO cells. The antiviral activity was carried out against HSV-1 (Herpes simplex virus 1) propagated in VERO cell line. The aqueous extract, possessing high phenolic content (170.50 mg gallic acid equivalent/g extract), showed the highest reducing capacity (613.27 and 364.10 mg Trolox equivalent/g extract, for cupric reducing antioxidant capacity and ferric reducing antioxidant power, respectively), radical scavenging potential (469.82 mg Trolox equivalent/g extract, against 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)), metal chelating ability (52.39 mg ethylenediaminetetraacetic acid equivalent/g extract) and total antioxidant capacity (3.15 mmol Trolox equivalent/g extract). Liquid chromatography-electrospray ionization-quadrupole time-of-flight-mass spectrometry (LC-ESI-QTOF-MS/MS) alloved to tentatively identify a total of 56 compounds in the extracts, including ellagitannins, gallic acid and galloyl derivatives amongst others. The ethyl acetate extracts substantially depressed cholinesterase enzymes (4.49 and 12.26 mg galantamine equivalent/g extract against AChE and BChE, respectively) and α-amylase enzyme (1.04 mmol acarbose equivalent/g extract). On the other hand, the methanolic extract inhibited tyrosinase (121.42 mg kojic acid equivalent/g extract) and α-glucosidase (2.39 mmol acarbose equivalent/g extract) activities. The highest selectivity towards all cancer cell lines (SI 4.5-10.8) was observed with aqueous extract with the FaDu cells being the most sensitive (CC50 40.22 µg/mL). It can be concluded that the presence of certain bioactive antiviral molecules may be related to the high anti HSV-1 activity of the methanolic extract. This work has generated vital scientific data on this medicinal plant, which is a prospective candidate for the creation of innovative phyto-pharmaceuticals.


Assuntos
Geranium/metabolismo , Extratos Vegetais/química , Animais , Antioxidantes , Antivirais , Linhagem Celular , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/análise , Humanos , Fenóis/análise , Compostos Fitoquímicos/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Estudos Prospectivos , Espectrometria de Massas por Ionização por Electrospray/métodos , Espectrometria de Massas em Tandem/métodos
4.
Sci Rep ; 11(1): 10654, 2021 05 20.
Artigo em Inglês | MEDLINE | ID: mdl-34017038

RESUMO

The purpose of this study was to determine if a methanolic extract of the Pulsatilla patens (L.) Mill. can inhibit the progression of cancer through the modulation of cancer-related metabolic signaling pathways. We analyzed a panel of 13 inducible luciferase reporter gene vectors which expression is driven by enhancer elements that bind to specific transcription factors for the evaluation of the activity of cancer signaling pathways. The root extract of P. patens exhibited strong inhibition of several signaling pathways in HeLa cells, a cervical cancer cell line, and was found to be the most potent in inhibiting the activation of Stat3, Smad, AP-1, NF-κB, MYC, Ets, Wnt and Hdghog, at a concentration of 40 µg/mL. The methanolic extracts of P. patens enhanced apoptotic death, deregulated cellular proliferation, differentiation, and progression towards the neoplastic phenotype by altering key signaling molecules required for cell cycle progression. This is the first study to report the influence of Pulsatilla species on cancer signaling pathways. Further, our detailed phytochemical analysis of the methanolic extracts of the P. patens allowed to deduce that compounds, which strongly suppressed the growth and proliferation of HeLa cancer cells were mainly triterpenoid saponins accompanied by phenolic acids.

5.
Food Chem Toxicol ; 153: 112289, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34029669

RESUMO

Fritillaria thunbergii Miq. (Zhe beimu) ranked as oldest known homeopathic traditional folk medicine in China. The bulbs are medicinally important curing cough, inflammation, gastric ulcers, hypertension, diarrhea, and bronchitis. The aim of this review is to enlighten the deeper knowledge about F. thunbergii giving a comprehensive overview on its traditional uses, phytochemistry and pharmacology for future investigation of plant-based drugs and therapeutic applications. Total 48 medicinally important species of Fritillaria were described; total 122 compounds have been identified as results only 72 chemical constituents were described with proper chemical and biological details. F. thunbergii and its bulbs mainly constitute alkaloids, essential oils, diterpenoids, carbohydrates, sterols, amino acids, nucleosides, fatty acids, and lignans. The pharmacological studies demonstrate that F. thunbergii and its bulbs displays a wide range of bioactivities e.g., anti-inflammatory, anticancer, antitussive, expectorant, anti-ulcer, antimicrobial, antioxidant, anti-thyroid, regulation of blood rheology, anti-diarrhea, neuroprotection, and analgesic effects. Although promising reports on the various chemical bioactive constituents and biological properties of F. thunbergii have been published, very few reviews are related specifically to the traditional uses, phytochemistry and pharmacological applications. Further, various other studies on these plants should deserve our more attention for future investigation for drug development and its therapeutic applications.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Fritillaria/química , Animais , Medicamentos de Ervas Chinesas/química , Etnofarmacologia , Humanos , Raízes de Plantas/química
6.
mSystems ; 6(3)2021 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-33947802

RESUMO

Mycobacterium tuberculosis developed efficient adaptation mechanisms in response to different environmental conditions. This resulted in the ability to survive in human macrophages and in resistance to numerous antibiotics. To get insight into bacterial responses to potent antimycobacterial natural compounds, we tested how usnic acid, a lichen-derived secondary metabolite, would influence mycobacteria at transcriptomic and metabolomic levels. The analysis of expression of sigma factors revealed a profound impact of usnic acid on one of the primary genetic regulatory systems of M. tuberculosis Combined liquid chromatography-mass spectrometry and nuclear magnetic resonance analyses allowed us to observe the perturbations in metabolic pathways, as well as in lipid composition, which took place within 24 h of exposure. Early bacterial response was related to redox homeostasis, lipid synthesis, and nucleic acid repair. Usnic acid treatment provoked disturbances of redox state in mycobacterial cells and increased production of structural elements of the cell wall and cell membrane. In addition, to increase the number of molecules related to restoration of redox balance, the rearrangements of the cell envelope were the first defense mechanisms observed under usnic acid treatment.IMPORTANCE The evaluation of mechanisms of mycobacterial response to natural products has been barely studied. However, it might be helpful to reveal bacterial adaptation strategies, which are eventually crucial for the discovery of new drug targets and, hence, understanding the resistance mechanisms. This study showed that the first-line mycobacterial defense against usnic acid, a potent antimicrobial agent, is the remodeling of the cell envelope and restoring redox homeostasis. Transcriptomic data correlated with metabolomics analysis. The observed metabolic changes appeared similar to those exerted by antibiotics.

7.
Food Chem Toxicol ; 151: 112113, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33722602

RESUMO

Camptothecin (CPT), a well-known monoterpenoid indole alkaloid with broad-spectrum anti-cancer activity, is produced from plants and endophytes. In view of the limitations of plants as sources of camptothecin in productivity and efficiency, endophytes serve as the fast growth, high cost-effectiveness, good reproducibility, and feasible genetic manipulation, so they have the potential to meet the huge market demand of the pharmaceutical industry. In this review, we summarized the isolation, identification and fermentation of CPT-producing endophytes, as well as the biosynthesis, extraction and detection of camptothecin from endophytes. Among them, we put emphasis on increasing the production of camptothecin in endophytes through different strategies such as changing the proportion of carbon, nitrogen and phosphate source, adding the precursors, elicitors or adsorbent resin, utilizing co-culture fermentation or fermenter culture. However, cell subculture and metabolic reprogramming affect the expression of camptothecin biosynthetic genes in CPT-producing endophytes, which poses a challenge to the industrial production of camptothecin. Therefore, it will be useful to gain insights through the review of these researches and provide alternative approaches to develop economical, eco-friendly and reliable natural products.


Assuntos
Antineoplásicos Fitogênicos/biossíntese , Camptotecina/biossíntese , Endófitos/metabolismo , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Reatores Biológicos , Camptotecina/química , Camptotecina/farmacologia , Fermentação , Regulação da Expressão Gênica/efeitos dos fármacos , Transcrição Genética/efeitos dos fármacos
8.
J Pharm Biomed Anal ; 198: 114018, 2021 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-33730614

RESUMO

Caesalpinia bonduc and C. decapeleta var. japonica have great importance in traditional medicine systems but scientific information's are still lacking for their potentials. To explore their bioactivity, we assessed the antioxidant, enzyme inhibitory abilities of the dichloromethane (DCM), ethyl acetate, methanol, and water extracts prepared from the leaves and bark. The cytotoxicity and anticancer properties of the extracts were also assessed in vitro. The water extract of C. decapeleta leaves possessed highest phenolic content (108.16 mg gallic acid equivalent (GAE)/g extract), while the highest flavonoid content was recorded for the C. bonduc leaf methanolic extract (27.89 mg rutin equivalent (RE)/g extract). In general, C. decapeleta extracts possessed higher radical scavenging potential compared to C. bonduc extracts. C. decapeleta DCM leaves extract (10.20 mg galantamine equivalent (GALAE)/g extract) showed highest inhibition against butyrylcholinesterase. The cytotoxicity of the most potent methanolic and aqueous extracts were assessed against four cell lines. The chemical profiles of both species appeared to be different. C. bonduc was abundant in organic and phenolic acids as well as their esters. Flavonoid glycosides, bonducellin and its derivatives and caesalminaxins were identified. Whereas, C. decalpetala possessed many galloylated compounds. The cytotoxicity of C. bonduc and C. decapetala extracts was tested using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) based assay on VERO (kidney of an adult African Green monkey cells), HeLa (human cervical adenocarcinoma cells), RKO (human colon carcinoma cells), FaDu (human hypopharyngeal squamous carcinoma cells) cell lines. C. bonduc bark water extract exhibited the highest cytotoxicity towards HeLa (50 % cytotoxic concentration (CC50): 28.5 µg/mL) cancer cell line, as compared to normal VERO cells (CC50:35.87 µg/mL). For C. decapetala, the highest cytotoxicity was found for bark methanol extract on the HeLa cells with CC50 of 46.08 µg/mL and selectivity index of 3.33. In the gene ontology analysis, prostate cancer, nuclear factor kappa B (NF-kappa B) signaling, proteoglycans in cancer pathways might support the results of the cytotoxic assays. These results showed that the tested Caesalpinia species, showing potent inhibitory action against butyrylcholinesterase, might represent novel phytotherapeutic avenues for the management of Alzheimer's disease.


Assuntos
Farmácia , Extratos Vegetais , Animais , Antioxidantes/farmacologia , Chlorocebus aethiops , Biologia Computacional , Células HeLa , Humanos , Extratos Vegetais/farmacologia , Células Vero
9.
Artigo em Inglês | MEDLINE | ID: mdl-32671026

RESUMO

Essential oils (EOs) and their main constituents, the terpenes, are widely studied, mostly relating to their antioxidant ability and bioactivity, such as antimicrobial, anticancer, anti-inflammatory, and range of other actions in the living systems. However, there is limited information on their bioavailability, especially upon clinical studies. Having in mind both strong biological effects and health benefits of EOs and their specific physicochemical properties (volatility, lipophilic character, low water solubility or insolubility, viscosity, expressed odor, concentration-dependent toxicity, etc.), there is a need for their encapsulation for target delivery. Encapsulation of EOs and their constituents is the prerequisite for enhancing their oxidative stability, thermostability, photostability, shelf life, and biological activity. We considered various carrier types such a (1) monophase and polyphase polysaccharide hydrogel carriers, (2) polysaccharide-protein carriers, and (3) lipid carriers in the context of physicochemical and engineering factors. Physicochemical factors are encapsulation efficiency, chemical stability under gastric conditions, mechanical stability, and thermal stability of carrier matrices. Choice of carrier material also determines the encapsulation technique. Consequently, the engineering factors are related to the advantage and disadvantage of various encapsulation techniques frequently used in the literature. In addition, it was intended to address the interactions between (1) main carrier components, such as polysaccharides, proteins, and lipids themselves (in order to form chemically and mechanically stable structure); (2) main carrier components with pepsin under gastric conditions (in order to form resistant material under gastric conditions); and (3) main carrier components with EOs (in order to enhance encapsulation efficiency), as a necessary precondition for whole process optimization. Finally, different sources for obtaining natural carrier macromolecules are surveyed, especially the agro-waste materials and agricultural and food by-products. This review article highlights the bioavailability aspects of encapsulated EOs and physicochemical and engineering factors concerning natural macromolecule carriers for their target delivery and application.

10.
Foods ; 9(6)2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-32492817

RESUMO

Fibigia clypeata (L.) Medik. is a poorly studied plant species belonging to the Brassicaceae family, and usually used as cress in the salads. The current investigation aimed at assessing the antioxidant potential and inhibitory activity of ethyl acetate, methanol, and aqueous extracts of F. clypeata against key enzymes targeted in the management of type II diabetes (α-amylase and α-glucosidase), Alzheimer's disease (acetylcholinesterase and butyrylcholinesterase), and skin hyperpigmentation (tyrosinase). Cytotoxicity of the extracts was also determined using normal VERO and cancer FaDu and SCC-25 cell lines. Besides, LC-MS was employed to investigate the detailed phytochemical profiles of the extracts. The methanol extract showed potent enzyme inhibitory activity (4.87 mg galantamine equivalent/g, 3.52 mg galantamine equivalent/g, 126.80 mg kojic acid equivalent/g, and 24.68 mg acarbose equivalent/g, for acetylcholinesterase, butyrylcholinesterase, tyrosinase, and α-glucosidase, respectively) and antioxidant potential (96.52, 109.10, 154.02, and 104.85 mg trolox equivalent/g, for DPPH, ABTS, CUPRAC, and FRAP assays, respectively). Interestingly, caffeic acid-O-hexoside derivative, caffeyl alcohol O-glucopyranoside, and ferulic acid derivative were identified in all extracts. F. clypeata extracts showed no cytotoxicity towards VERO cell line and a weak cytotoxic potential against FaDu and SCC-25 cell lines. Interesting scientific evidence gathered from the present study support further investigation on F. clypeata in the view of designing and developing a novel therapeutic agent for the management of Alzheimer's disease, type II diabetes, skin hyperpigmentation problems, as well as cancer.

11.
Artigo em Inglês | MEDLINE | ID: mdl-32351951

RESUMO

The growing demand for more sustainable, alternative processes leading to production of plant-derived preparations imposes the use of plants waste generated mainly by agri-food and pharmaceutical industries. These mostly unexploited but large quantities of plants waste also increase the interest in developing alternative approaches for sustainable production of therapeutic molecules. In order to reduce the amount of plant waste by further processing, different novel extraction techniques can be applied. Fruits and their industrial by-products are rich sources of different classes of compounds with therapeutic properties. The processed fruits waste can be reused and lead to novel pharmaceuticals, food supplements or functional foods. This review intends to briefly summarize recent aspects regarding the production of different active compounds from fruit by-products, and their therapeutic properties. The potential use of fruits by-products in different industries will be also discussed.

12.
Biomolecules ; 10(3)2020 02 26.
Artigo em Inglês | MEDLINE | ID: mdl-32111061

RESUMO

The antimycobacterial activity of cinnamaldehyde has already been proven for laboratory strains and for clinical isolates. What is more, cinnamaldehyde was shown to threaten the mycobacterial plasma membrane integrity and to activate the stress response system. Following promising applications of metabolomics in drug discovery and development we aimed to explore the mycobacteria response to cinnamaldehyde within cinnamon essential oil treatment by untargeted liquid chromatography-mass spectrometry. The use of predictive metabolite pathway analysis and description of produced lipids enabled the evaluation of the stress symptoms shown by bacteria. This study suggests that bacteria exposed to cinnamaldehyde could reorganize their outer membrane as a physical barrier against stress factors. They probably lowered cell wall permeability and inner membrane fluidity, and possibly redirected carbon flow to store energy in triacylglycerols. Being a reactive compound, cinnamaldehyde may also contribute to disturbances in bacteria redox homeostasis and detoxification mechanisms.


Assuntos
Acroleína/análogos & derivados , Antituberculosos/farmacologia , Cinnamomum zeylanicum/química , Mycobacterium tuberculosis/efeitos dos fármacos , Óleos Voláteis/farmacologia , Acroleína/química , Acroleína/farmacologia , Antituberculosos/química , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Redes e Vias Metabólicas/efeitos dos fármacos , Metabolômica , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/metabolismo , Óleos Voláteis/química , Tuberculose/tratamento farmacológico , Tuberculose/microbiologia
13.
Molecules ; 25(2)2020 Jan 12.
Artigo em Inglês | MEDLINE | ID: mdl-31940923

RESUMO

Continuously growing demand for plant derived therapeutic molecules obtained in a sustainable and eco-friendly manner favors biotechnological production and development of innovative extraction techniques to obtain phytoconstituents. What is more, improving and optimization of alternative techniques for the isolation of high value natural compounds are issues having both social and economic importance. In this critical review, the aspects regarding plant biotechnology and green downstream processing, leading to the production and extraction of increased levels of fine chemicals from both plant cell, tissue, and organ culture or fresh plant materials and the remaining by-products, are discussed.


Assuntos
Biotecnologia/métodos , Cromatografia/métodos , Extração Líquido-Líquido/métodos , Compostos Fitoquímicos/isolamento & purificação , Extração em Fase Sólida/métodos , Apiaceae/química , Asteraceae/química , Biotecnologia/instrumentação , Biotecnologia/tendências , Cromatografia/instrumentação , Fabaceae/química , Humanos , Lamiaceae/química , Micro-Ondas , Myrtaceae/química , Compostos Fitoquímicos/química , Células Vegetais/química , Plantas Medicinais , Sonicação/métodos
14.
Food Chem Toxicol ; 135: 111052, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31837349

RESUMO

Ethnobotanical evidences report the use of Rhododendron luteum Sweet (Ericaceae) in traditional medicinal systems. However, R. luteum has been associated to the occurrence of 'mad honey' poisoning. In the present study, the ethyl acetate, methanol, and water extracts of R. luteum were investigated for their in vitro antioxidant, enzyme inhibition, and cytotoxic properties. The cytotoxicity of R. luteum extracts on A549 lung cancer cell line was evaluated using MTT cell viability assay. Besides, HPLC-ESI-MSn approach was employed to elucidate the secondary metabolite profiles of R. luteum in order to establish any structure-activity relationship. Methanol and water extracts of R. luteum possessed highest radical scavenging and reducing properties while the ethyl acetate extract showed highest metal chelating properties. In terms of enzyme inhibition, the methanol and ethyl acetate extracts of R. luteum, possessing epigallocatechin, were active inhibitors of cholinesterase enzymes, α-glucosidase, and tyrosinase. Water extract caused growth inhibition of A549 cells with 207.2 µg/ml IC50 value. Though R. luteum has received little scientific attention due to the occurrence of grayanotoxins in the plant, however, data presented in this work shows promising biological activity of R. luteum and highlighted its role as a potential source of antioxidant and key enzyme inhibitors.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/farmacologia , Rhododendron/química , Células A549 , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos
15.
Molecules ; 24(23)2019 Nov 20.
Artigo em Inglês | MEDLINE | ID: mdl-31757027

RESUMO

Large amounts of agro-industrial waste are being generated each year, leading to pollution and economic loss. At the same time, these side streams are rich source of active compounds including antioxidants. Recovered compounds can be re-utilized as food additives, functional foods, nutra-/pharmaceuticals, cosmeceuticals, beauty products, and bio-packaging. Advanced extraction techniques are promising tools to recover target compounds such as antioxidants from agro-industrial side streams. Due to the disadvantages of classical extraction techniques (such as large amounts of solvents, increased time of extraction, large amounts of remaining waste after the extraction procedure, etc.), and advanced techniques emerged, in order to obtain more efficient and sustainable processes. In this review paper aspects regarding different modern extraction techniques related to recovery of antioxidant compounds from wastes generated in different industries and their applications are briefly discussed.


Assuntos
Agricultura , Antioxidantes , Cosmecêuticos , Resíduos Industriais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Cosmecêuticos/química , Cosmecêuticos/isolamento & purificação
16.
Food Chem Toxicol ; 129: 115-124, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31029723

RESUMO

Essential oils (EO) possess a wide range of biological activities. However, their application in aqueous media is often limited due to their hydrophobicity and volatile character. This study was designed to prepare stable, water-dilutable microemulsions (ME) containing essential oils of citronella (Cymbopogon nardus (L.) Rendle), mint (Mentha x piperita L. 'Multimentha') and eucalyptus (Eucalyptus globulus Labill.) and to evaluate their in vitro antioxidant and cytotoxic properties. The comparison of cytotoxicity of EO solubilised in microemulsions and in dimethyl sulfoxide as well as the recovery of volatiles from cells culture medium over time was also performed. The clear ME were obtained in a range between 10% and 50% of aqueous phase for citronella EO and up to 60% of aqueous phase for mint and eucalyptus EO, in all ratios of Tween 80 to oil phase (from 5:1 to 9:1). Microemulsions of EO (EO/ME) showed higher antioxidant activity compared to EO. The increase in activity was 13.96%, 22.25% and 45.60% for eucalyptus, mint and citronella EO, respectively. The analysis of cytotoxicity profiles of EO/ME and EO/DMSO in Vero and HeLa cell lines showed differences in activity, however, they were statistically significant only in case of mint EO. Furthermore, it can be concluded that after 24 h of incubation ME vehicle itself was responsible for the observed cytotoxic effect. At the same time ME provided good solubility of constituents of EO and diminished evaporation of volatiles from culture medium.


Assuntos
Antioxidantes/química , Emulsões , Óleos Voláteis/química , Animais , Chlorocebus aethiops , Meios de Cultura , Células HeLa , Humanos , Solubilidade , Células Vero
17.
Food Chem Toxicol ; 125: 161-169, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30610933

RESUMO

Nigella damascena L belongs to Ranunculaceae family and is mentioned in Eastern traditional medicine for the treatment of high temperatures, regulation of menstruation or catarrhal affections. The anti-inflammatory activity of compounds present in the essential oil obtained from seeds of this plant can be found in literature, however no studies on immunomodulatory activity are provided. Hence, in this work anti-inflammatory activity of N. damascena seed essential oil as well as damascenine and main compound ß-elemene was evaluated on ex-vivo lipopolysaccharide (LPS)-stimulated human neutrophils. For isolation of damascenine fast and efficient protocol was elaborated using high performance countercurrent chromatography technique for the first time. Also detailed spectroscopic characteristic of damascenine was provided for the first time. Damascenine was separated from the essential oil in a mixture of petroleum ether/acetonitrile/acetone (2:1.5:0.5 v/v/v) in reversed phase mode in 12 min with 99.47% purity. Essential oil, damascenine and ß-elemene presented immunomodulatory activity evaluated in LPS-stimulated neutrophils ex vivo. All studied samples significantly inhibited release of interleukin 1 beta (IL-1ß) and interleukin 8 (IL-8). What is more, damascenine and ß-elemene decreased matrix metallopeptidase 9 (MMP-9) production similar to dexamethasone. The release of tumor necrosis factor (TNF-α) was also inhibited in all range of concentrations, however the activity was weaker then activity of dexametasone. The previously reported anti-inflammatory activity of damascenine and ß-elemene investigated in murine models was confirmed in our study on human neuthrophils suggesting their possible strong inhibitory effect on inflammatory response progression.


Assuntos
Neutrófilos/efeitos dos fármacos , Nigella damascena/química , Óleos Voláteis/farmacologia , Sesquiterpenos/farmacologia , ortoaminobenzoatos/farmacologia , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Distribuição Contracorrente , Humanos , Neutrófilos/imunologia , Espectroscopia de Prótons por Ressonância Magnética
19.
Molecules ; 23(9)2018 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-30231479

RESUMO

The purpose of the study was to evaluate the antimycobacterial activity and the possible action mode of cinnamon bark essential oil and its main constituent-cinnamaldehyde-against the Mycobacterium tuberculosis ATCC 25177 strain. Cinnamaldehyde was proved to be the main bioactive compound responsible for mycobacterial growth inhibition and bactericidal effects. The antimycobacterial activity of cinnamaldehyde was found to be comparable with that of ethambutol, one of the first-line anti-TB antibiotics. The selectivity index determined using cell culture studies in vitro showed a high biological potential of cinnamaldehyde. In M. tuberculosis cells exposed to cinnamaldehyde the cell membrane stress sensing and envelope preserving system are activated. Overexpression of clgR gene indicates a threat to the stability of the cell membrane and suggests a possible mechanism of action. No synergism was detected with the basic set of antibiotics used in tuberculosis treatment: ethambutol, isoniazid, streptomycin, rifampicin, and ciprofloxacin.


Assuntos
Acroleína/análogos & derivados , Antituberculosos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Acroleína/química , Acroleína/farmacologia , Antituberculosos/química , Cromatografia Gasosa-Espectrometria de Massas , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Óleos Voláteis/farmacologia
20.
Molecules ; 23(2)2018 01 28.
Artigo em Inglês | MEDLINE | ID: mdl-29382097

RESUMO

The most commonly used plant source of ß-elemene is Curcuma wenyujin Y. H. Chen & C. Ling (syn. of Curcuma aromatic Salisb.) with its content in supercritical CO2 extract up to 27.83%. However, the other rich source of this compound is Nigella damascena L. essential oil, in which ß-elemene accounts for 47%. In this work, the effective protocol for preparative isolation of ß-elemene from a new source-N. damascena essential oil-using high performance counter-current chromatography HPCCC was elaborated. Furthermore, since sesquiterpens are known as potent antimicrobials, the need for finding new agents designed to combat multi-drug resistant strains was addressed and the purified target compound and the essential oil were tested for its activity against a panel of Gram-positive and Gram-negative bacteria, fungi, and mycobacterial strains. The application of the mixture of petroleum ether, acetonitrile, and acetone in the ratio 2:1.5:0.5 (v/v) in the reversed phase mode yielded ß-elemene with high purity in 70 min. The results obtained for antimicrobial assay clearly indicated that N. damascena essential oil and isolated ß-elemene exert action against Mycobacterium tuberculosis strain H37Ra.


Assuntos
Anti-Infecciosos , Mycobacterium tuberculosis/crescimento & desenvolvimento , Nigella damascena/química , Óleos Voláteis/química , Sesquiterpenos , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Testes de Sensibilidade Microbiana , Sesquiterpenos/química , Sesquiterpenos/farmacologia
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