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1.
Int J Mol Sci ; 24(2)2023 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-36674653

RESUMO

This study aimed to examine if methanolic extracts of Pulsatilla vulgaris Mill. can inhibit HeLa cell proliferation through the modulation of cancer-related signaling pathways. The cytotoxicity and chemical composition of P. vulgaris leaves and root extracts were also determined. Research showed that root extract of P. vulgaris inhibited 12 signaling pathways in a cervical cancer cell line and the most potent activation inhibition was observed for MYC, Notch, Wnt, E2F, Ets, Stat3, Smad, Hdghog, AP-1, and NF-κB, at a concentration of 40 µg/mL. The methanolic extracts of P. vulgaris enhanced apoptotic death and deregulated cellular proliferation, differentiation, and progression toward the neoplastic phenotype by altering key signaling molecules required for cell cycle progression. This is the first study to report the influence of P. vulgaris on cancer signaling pathways. Additionally, our detailed phytochemical analysis of the methanolic extracts of P. vulgaris gives a conclusion that compounds, which strongly suppressed the growth and proliferation of HeLa cancer cells were mainly triterpenoid saponins accompanied by phenolic acids.


Assuntos
Neoplasias , Pulsatilla , Humanos , Células HeLa , Genes Reporter , Transdução de Sinais , Proliferação de Células , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Linhagem Celular Tumoral , Apoptose
2.
Molecules ; 28(4)2023 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-36838823

RESUMO

In the present study, biogenic selenium nanoparticles (SeNPs) have been prepared using Paenibacillus terreus and functionalized with nystatin (SeNP@PVP_Nystatin nanoconjugates) for inhibiting growth, morphogenesis, and a biofilm in Candida albicans. Ultraviolet-visible spectroscopy analysis has shown a characteristic absorption at 289, 303, and 318 nm, and X-ray diffraction analysis has shown characteristic peaks at different 2θ values for SeNPs. Electron microscopy analysis has shown that biogenic SeNPs are spherical in shape with a size in the range of 220-240 nm. Fourier transform infrared spectroscopy has confirmed the functionalization of nystatin on SeNPs (formation of SeNP@PVP_Nystatin nanoconjugates), and the zeta potential has confirmed the negative charge on the nanoconjugates. Biogenic SeNPs are inactive; however, nanoconjugates have shown antifungal activities on C. albicans (inhibited growth, morphogenesis, and a biofilm). The molecular mechanism for the action of nanoconjugates via a real-time polymerase chain reaction has shown that genes involved in the RAS/cAMP/PKA signaling pathway play an important role in antifungal activity. In cytotoxic studies, nanoconjugates have inhibited only 12% growth of the human embryonic kidney cell line 293 cells, indicating that the nanocomposites are not cytotoxic. Thus, the biogenic SeNPs produced by P. terreus can be used as innovative and effective drug carriers to increase the antifungal activity of nystatin.


Assuntos
Nanopartículas , Selênio , Humanos , Antifúngicos/farmacologia , Nistatina/farmacologia , Selênio/química , Candida albicans , Nanoconjugados , Nanopartículas/química , Biofilmes
3.
Molecules ; 28(7)2023 Apr 04.
Artigo em Inglês | MEDLINE | ID: mdl-37049975

RESUMO

Depression is a common and complex mental and emotional disorder that causes disability, morbidity, and quite often mortality around the world. Depression is closely related to several physical and metabolic conditions causing metabolic depression. Studies have indicated that there is a relationship between the intestinal microbiota and the brain, known as the gut-brain axis. While this microbiota-gut-brain connection is disturbed, dysfunctions of the brain, immune system, endocrine system, and gastrointestinal tract occur. Numerous studies show that intestinal dysbiosis characterized by abnormal microbiota and dysfunction of the microbiota-gut-brain axis could be a direct cause of mental and emotional disorders. Traditional treatment of depression includes psychotherapy and pharmacotherapy, and it mainly targets the brain. However, restoration of the intestinal microbiota and functions of the gut-brain axis via using probiotics, their metabolites, prebiotics, and healthy diet may alleviate depressive symptoms. Administration of probiotics labeled as psychobiotics and their metabolites as metabiotics, especially as an adjuvant to antidepressants, improves mental disorders. It is a new approach to the prevention, management, and treatment of mental and emotional illnesses, particularly major depressive disorder and metabolic depression. For the effectiveness of antidepressant therapy, psychobiotics should be administered at a dose higher than 1 billion CFU/day for at least 8 weeks.


Assuntos
Transtorno Depressivo Maior , Microbioma Gastrointestinal , Probióticos , Humanos , Depressão/tratamento farmacológico , Probióticos/uso terapêutico , Prebióticos , Encéfalo
4.
Molecules ; 28(22)2023 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-38005252

RESUMO

In the present study, we performed comprehensive LC-MS chemical profiling and biological tests of Vepris boiviniana leaves and stem bark extracts of different polarities. In total, 60 bioactive compounds were tentatively identified in all extracts. The 80% ethanolic stem bark extract exhibited the highest activity in the ABTS assay, equal to 551.82 mg TE/g. The infusion extract of stem bark consistently demonstrated elevated antioxidant activity in all assays, with values ranging from 137.39 mg TE/g to 218.46 mg TE/g. Regarding the enzyme inhibitory assay, aqueous extracts from both bark and leaves exhibited substantial inhibition of AChE, with EC50 values of 2.41 mg GALAE/g and 2.25 mg GALAE/g, respectively. The 80% ethanolic leaf extract exhibited the lowest cytotoxicity in VERO cells (CC50: 613.27 µg/mL) and demonstrated selective cytotoxicity against cancer cells, particularly against H1HeLa cells, indicating potential therapeutic specificity. The 80% ethanolic bark extract exhibited elevated toxicity in VERO cells but had reduced anticancer selectivity. The n-hexane extracts, notably the leaves' n-hexane extract, displayed the highest toxicity towards non-cancerous cells with selectivity towards H1HeLa and RKO cells. In viral load assessment, all extracts reduced HHV-1 load by 0.14-0.54 log and HRV-14 viral load by 0.13-0.72 log, indicating limited antiviral activity. In conclusion, our research underscores the diverse bioactive properties of Vepris boiviniana extracts, exhibiting potent antioxidant, enzyme inhibitory, and cytotoxicity potential against cancer cells.


Assuntos
Antioxidantes , Extratos Vegetais , Animais , Chlorocebus aethiops , Antioxidantes/farmacologia , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Células Vero , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Etanol , Antivirais/farmacologia
5.
Molecules ; 27(6)2022 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-35335228

RESUMO

This study focused on the biological evaluation and chemical characterisation of Ficus sur Forssk. (F. sur) (Family: Moraceae). The methanolic and aqueous extracts' phytochemical profile, antioxidant, and enzyme inhibitory properties were investigated. The aqueous stem bark extract yielded the highest phenolic content (115.51 ± 1.60 mg gallic acid equivalent/g extract), while the methanolic leaves extract possessed the highest flavonoid content (27.47 ± 0.28 mg Rutin equivalent/g extract). In total, 118 compounds were identified in the tested extracts. The methanolic stem bark extract exhibited the most potent radical scavenging potential against 2,2-diphenyl-1 picrylhydrazyl and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (475.79 ± 6.83 and 804.31 ± 4.52 mg Trolox equivalent/g extract, respectively) and the highest reducing Cu2+ capacity (937.86 ± 14.44 mg Trolox equivalent/g extract). The methanolic stem bark extract substantially depressed tyrosinase (69.84 ± 0.35 mg kojic acid equivalent/g extract), α-amylase (0.77 ± 0.01 mmol acarbose equivalent/g extract), acetylcholinesterase and butyrylcholinesterase (2.91 ± 0.07 and 6.56 ± 0.34 mg galantamine equivalent/g extract, respectively) enzymes. F. sur extracts were tested for anticancer properties and antiviral activity towards human herpes virus type 1 (HHV-1). Stem bark infusion and methanolic extract showed antineoplastic activity against cervical adenocarcinoma and colon cancer cell lines, whereas leaf methanolic extract exerted moderate antiviral activity towards HHV-1. This investigation yielded important scientific data on F. sur which might be used to generate innovative phytopharmaceuticals.


Assuntos
Ficus , Acetilcolinesterase , Butirilcolinesterase , Humanos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia
6.
Molecules ; 27(15)2022 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-35897865

RESUMO

Spathodea campanulata is an important medicinal plant with traditional uses in the tropical zone. In the current work, we aimed to determine the chemical profiles and biological effects of extracts (methanolic and infusion (water)) from the leaves and stem bark of S. campanulata. The chemical components of the tested extracts were identified using LC-ESI-QTOF-MS. Biological effects were tested in terms of antioxidant (radical scavenging, reducing power, and metal chelating), enzyme inhibitory (cholinesterase, amylase, glucosidase, and tyrosinase), antineoplastic, and antiviral activities. Fifty-seven components were identified in the tested extracts, including iridoids, flavonoids, and phenolic acids as the main constituents. In general, the leaves-MeOH extract was the most active in the antioxidant assays (DPPH, ABTS, CUPRAC, FRAP, metal chelating, and phosphomolybdenum). Antineoplastic effects were tested in normal (VERO cell line) and cancer cell lines (FaDu, HeLa, and RKO). The leaf infusion, as well as the extracts obtained from stem bark, showed antineoplastic activity (CC50 119.03-222.07 µg/mL). Antiviral effects were tested against HHV-1 and CVB3, and the leaf methanolic extract (500 µg/mL) exerted antiviral activity towards HHV-1, inhibiting the viral-induced cytopathic effect and reducing the viral infectious titre by 5.11 log and viral load by 1.45 log. In addition, molecular docking was performed to understand the interactions between selected chemical components and viral targets (HSV-1 DNA polymerase, HSV-1 protease, and HSV-1 thymidine kinase). The results presented suggest that S. campanulata may be a bright spot in moving from natural sources to industrial applications, including novel drugs, cosmeceuticals, and nutraceuticals.


Assuntos
Bignoniaceae , Farmácia , Antioxidantes/química , Antioxidantes/farmacologia , Antivirais/farmacologia , Bignoniaceae/química , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia
7.
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
8.
Molecules ; 26(22)2021 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-34833931

RESUMO

The essential oil component α-pinene has multiple biological activities. However, its application is limited owing to its volatility, low aqueous solubility, and chemical instability. For the aim of improving its physicochemical properties, α-pinene was encapsulated in conventional liposomes (CLs) and drug-in-cyclodextrin-in-liposomes (DCLs). Hydroxypropyl-ß-cyclodextrin/α-pinene (HP-ß-CD/α-pinene) inclusion complexes were prepared in aqueous solution, and the optimal solubilization of α-pinene occurred at HP-ß-CD:α-pinene molar ratio of 7.5:1. The ethanol-injection method was applied to produce different formulations using saturated (Phospholipon 90H) or unsaturated (Lipoid S100) phospholipids in combination with cholesterol. The size, the phospholipid and cholesterol incorporation rates, the encapsulation efficiency (EE), and the loading rate (LR) of α-pinene were determined, and the storage stability of liposomes was assessed. The results showed that α-pinene was efficiently entrapped in CLs and DCLs with high EE values. Moreover, Lipoid S100 CLs displayed the highest LR (22.9 ± 2.2%) of α-pinene compared to the other formulations. Both carrier systems HP-ß-CD/α-pinene inclusion complex and Lipoid S100 CLs presented a gradual release of α-pinene. Furthermore, the DPPH radical scavenging activity of α-pinene was maintained upon encapsulation in Lipoid S100 CLs. Finally, it was found that all formulations were stable after three months of storage at 4 °C.


Assuntos
Monoterpenos Bicíclicos/química , Ciclodextrinas/química , Lipossomos/química , 2-Hidroxipropil-beta-Ciclodextrina/química , Colesterol/química , Portadores de Fármacos/química , Composição de Medicamentos/métodos , Óleos Voláteis/química , Fosfolipídeos/química , Solubilidade
9.
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
10.
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
11.
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
12.
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
13.
Molecules ; 23(1)2018 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-29342972

RESUMO

Background: On account of emergence of multi- and extensively drug-resistant Mycobacterium tuberculosis (Mtb) strains, combinations of drugs with natural compounds were tested to search for antibiotic activity enhancers. In this work we studied terpenes (α-pinene, bisabolol, ß-elemene, (R)-limonene, (S)-limonene, myrcene, sabinene), which are the main constituents of essential oil obtained from Mutellina purpurea L., a plant with described antitubercular activity, to investigate their interactions with antibiotics against reference Mtb strains and multidrug-resistant clinical isolates. Methods: The serial dilution method was used to evaluate the minimal inhibitory concentration (MIC) of tested compounds, while the fractional inhibitory concentration index (FICI) was calculated for characterization of interactions. Moreover, IC50 values of tested compounds were determined using monkey kidney epithelial cell line (GMK). Results: The combinations of all studied terpenes with ethambutol or rifampicin resulted in a synergistic interaction. Bisabolol and (R)-limonene decreased the MIC for rifampicin at least two-fold for all tested strains, however no synergistic action was observed against virulent strains. The tested terpenes showed slight (bisabolol) or no cytotoxic effect against normal eukaryotic cells in vitro. Conclusions: The obtained enhanced activity (FICI < 0.5) of ethambutol and rifampicin against H37Ra strain under the influence of the studied terpenes may be correlated to the capability of essential oil constituents to modify bacterial resistance mechanisms in general. The observed differences in avirulent and virulent bacteria susceptibility to terpenes tested separately and in combinations with antibiotics can be correlated with the differences in the cell wall structure between H37Ra mutant and all virulent strains.


Assuntos
Antituberculosos/farmacologia , Produtos Biológicos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Terpenos/farmacologia , Antituberculosos/química , Produtos Biológicos/química , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Sinergismo Farmacológico , Humanos , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/genética , Terpenos/química
14.
Med Princ Pract ; 26(2): 108-112, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-27883995

RESUMO

OBJECTIVE: In this study, we aimed to describe the influence of natural terpenes on the antimycobacterial activity of first-line tuberculostatic drugs against isolated Mycobacterium tuberculosis. MATERIALS AND METHODS: The natural terpenes used in this study were R-limonene, S-limonene, myrcene, sabinene, α-pinene, and ß-elemene. The values of the minimum inhibitory concentration (MIC) for these terpenes, as well as for combinations of terpenes with tuberculostatic antibiotics (ethambutol, isoniazid, and rifampicin), were determined using a tube log2 dilution method in the range of 125-0.059 µg/mL. RESULTS: S-limonene had a strong synergistic effect with all tested antibiotics (MIC decreased from 16 to 0.475 µg/mL for ethambutol, from 16 to 0.237 µg/mL for rifampicin, and from 32 to 0.475 µg/mL for isoniazid). Combinations of myrcene, R-limonene, ß-elemene, and sabinene with tuberculostatic antibiotics resulted in a decreased MIC of the antibiotics (from 3.9 to 0.475 µg/mL for ethambutol, from 15 to 0.475 µg/mL for isoniazid, and from 0.475 to 0.237 µg/mL for rifampicin) while combinations of α-pinene with ethambutol and isoniazid resulted in increased MIC values (from 16 to 125 µg/mL for ethambutol, and from 32 to 125 µg/mL for isoniazid). Rifampicin had a synergistic increase in activity with all the tested compounds. CONCLUSIONS: Our study showed that terpenes enhance the activity of tuberculostatic antibiotics.


Assuntos
Antituberculosos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Terpenos/farmacologia , Monoterpenos Acíclicos , Alcenos/farmacologia , Monoterpenos Bicíclicos , Cicloexenos/farmacologia , Relação Dose-Resposta a Droga , Quimioterapia Combinada , Etambutol/farmacologia , Humanos , Isoniazida/farmacologia , Limoneno , Testes de Sensibilidade Microbiana , Monoterpenos/farmacologia , Rifampina/farmacologia , Sesquiterpenos/farmacologia
15.
Drug Chem Toxicol ; 38(1): 1-8, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-24580112

RESUMO

The delayed cardiomyopathy caused by doxorubicin - an chemotherapeutic drug with broad spectrum of anticancer activity - is mainly triggered by oxidative stress. The aim of this study was to assess an effect of Mutellina purpurea methanolic extract fraction and other antioxidants of plant origin: rutin, quercetin and chlorogenic acid (all 1 mg% w/v) on oxidative stress and morphological changes induced by doxorubicin in cardiomyocytes H9c2. Mitochondrial oxidative stress in cardiomyocytes induced by 1 µM doxorubicin was evidenced by MitoTracker and RedoxSensor Red CC-1 dyes. Moreover, cardiomyocytes morphological changes and cell viability were evaluated. The tested fraction slightly reduced mitochondrial ROS fluorescence, similar to quercetin. Chlorogenic acid revealed concentration dependent prooxidative and antioxidative properties in the applied H9c2 model. The evaluation of the protective effect of tested compounds on doxorubicin-induced cytotoxicity was based on the examination of induced oxidative stress and morphology changes. The protective effect was described in the following order: rutin > chlorogenic acid (0.5 µM) > LH8 and quercetin. According to the MTT test, rutin seems to be the most promising compound that should be tested in a future studies.


Assuntos
Antibióticos Antineoplásicos/toxicidade , Antioxidantes/farmacologia , Apiaceae/química , Doxorrubicina/toxicidade , Mioblastos Cardíacos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Polifenóis/farmacologia , Animais , Antioxidantes/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Mioblastos Cardíacos/metabolismo , Mioblastos Cardíacos/patologia , Polifenóis/isolamento & purificação , Ratos
16.
Med Princ Pract ; 24(6): 527-32, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26381133

RESUMO

OBJECTIVE: The aim of this study was to evaluate the antimycobacterial activity of the essential oil (EO) of Mutellina purpurea L. and its main constituents against the M. tuberculosis H37Ra strain. MATERIALS AND METHODS: The M. purpurea EO was obtained by hydrodistillation, while its main constituents were purchased. The minimal inhibitory concentration values were determined by the log2 dilution method. Visualization of the effects of the tested substances on M. tuberculosis was performed using a transmission electron microscope (TEM). Mathematical shape descriptors such as area, circularity, aspect ratio and roundness were calculated to describe morphological changes in bacterial cell shape. RESULTS: The EO of M.purpurea and all substances tested in this experiment showed a significant antimycobacterial activity. The most active was α-pinene followed by bisabolol and myrcene (8, 16 and 32 µg/ml, respectively). The EO and limonene exhibited the same antimicrobial activity (64 µg/ml). The TEM images and shape descriptors showed significant changes in the overall tuberculosis cell shape and cytoplasm homogeneity (uniformity and consistency) CONCLUSIONS: In this study, the low molecular weight compounds of mono- and sesquiterpenes penetrated/destabilized the complex mycobacterial cell wall and decreased its viability. There is a need for further experiments to explain the mechanism of action of these small particles.


Assuntos
Antibacterianos/farmacologia , Apiaceae , Forma Celular/efeitos dos fármacos , Citoplasma/efeitos dos fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Óleos Voláteis/farmacologia , Antibacterianos/química , Monoterpenos Bicíclicos , Cicloexenos/farmacologia , Relação Dose-Resposta a Droga , Humanos , Limoneno , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Transmissão , Sesquiterpenos Monocíclicos , Monoterpenos/farmacologia , Óleos Voláteis/química , Sesquiterpenos/farmacologia , Terpenos/farmacologia
17.
Acta Pol Pharm ; 72(3): 507-15, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26642659

RESUMO

In this study, both qualitative and quantitative analyses of chemical composition of M. purpurea essential oil obtained in the Deryng and Clevenger-type apparatuses were compared. As a result, content of volatile compounds were: 785.67 mg/mL and 833.33 mg/mL in the oil obtained in the Deryng (D-EO) and Clevenger-type apparatuses (C-EO), respectively. The major components of both essential oils from M. purpurea were: a-pinene, sabinene, myrcene, (Z)-sesquisabinene hydrate, (E)-sesquisabinene hydrate, and a-bis-abolol. The correlation coefficients values are not determined by the differences in the concentrations of the components resulting from the application of two different methods of distillation.


Assuntos
Destilação/instrumentação , Flores/química , Óleos Voláteis/isolamento & purificação
18.
Front Microbiol ; 15: 1353875, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38414774

RESUMO

Natural products are promising antimicrobials, usually having multiple and different cellular targets than synthetic antibiotics. Their influence on bacteria at various metabolic and functional levels contributes to higher efficacy even against drug-resistant strains. One such compound is a naturally occurring p-benzoquinone - thymoquinone. It is effective against different bacteria, including multidrug-resistant and extremely drug-resistant Mycobacterium tuberculosis. Its antibacterial mechanism of action was studied in several bacterial species except mycobacteria. To get an insight into the antimycobacterial activity of thymoquinone at the molecular level, we performed metabolomic and transcriptomic analyzes of bacteria exposed to this compound. The expression of genes coding stress-responsive sigma factors revealed that thymoquinone rapidly induces the production of sigE transcripts. At the same time, prolonged influence results in the overexpression of all sigma factor genes and significantly upregulates sigF. The metabolomic analysis confirmed that the antimycobacterial activity of thymoquinone was related to the depletion of NAD and ATP pools and the downregulation of plasma membrane lipids. This state was observed after 24 h and was persistent the next day, suggesting that bacteria could not activate catabolic mechanisms and produce energy. Additionally, the presence of a thymoquinone nitrogen derivative in the bacterial broth and the culture was reported.

19.
Antioxidants (Basel) ; 13(6)2024 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-38929082

RESUMO

The present study was performed to determine the chemical constituents, cytotoxicity, antioxidant and enzyme inhibition activities of the aerial parts of Glaucium acutidentatum Hausskn. and Bornm. (family Papaveraceae). Methanolic and aqueous extracts were prepared by maceration, homogenizer-assisted extraction (HAE) and infusion. Results showed that the highest total phenolic and flavonoids contents were obtained from the methanol extracts obtained by HAE (53.22 ± 0.10 mg GAE/g) and maceration (30.28 ± 0.51 mg RE/g), respectively. The aporphine, beznyltetrahydroisoquinoline, and protopine types of Glaucium alkaloids have been tentatively identified. Among them, glaucine was identified in all extracts. Flavonoids, phenolic acids, coumarins, organic acids and fatty acids were also detected. Methanolic extract obtained using the HAE method displayed the highest anti-DPPH (41.42 ± 0.62 mg TE/g), total antioxidant (1.20 ± 0.17 mmol TE/g), Cu2+ (113.55 ± 6.44 mg TE/g), and Fe3+ (74.52 ± 4.74 mg TE/g) reducing properties. The aqueous extracts obtained by infusion and HAE methods exerted the best anti-ABTS (103.59 ± 1.49 mg TE/g) and chelating (19.81 ± 0.05 mg EDTAE/g) activities, respectively. Methanolic extract from HAE recorded the highest acetylcholinesterase (2.55 ± 0.10 mg GALAE/g) and α-amylase (0.51 ± 0.02 mmol ACAE/g) inhibition activities, while that obtained by maceration showed the best butyrylcholinesterase (3.76 ± 0.31 mg GALAE/g) inhibition activity. Both extracts revealed the best tyrosinase inhibitory activity (25.15 ± 1.00 and 26.79 ± 2.36 mg KAE/g, p ≥ 0.05). G. acutidentatum maceration-derived aqueous extract showed selective anticancer activity against cells originating from human hypopharyngeal carcinoma. In conclusion, these findings indicated that G. acutidentatum is a promising source of alkaloids and phenolic compounds for variable pharmaceutical formulations.

20.
Acta Pol Pharm ; 70(1): 35-40, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23610957

RESUMO

In this paper, comparison of the volatile components composition in the samples obtained by hydrodistillation and solid-phase microextraction of Salvia officinalis was described. Different sample preparation techniques showed considerable differences in volatiles composition, especially with respect to sesqui- and diterpenoids. The comparison of the sage essential oil obtained by hydrodistillation in the Deryng and Clevenger type apparatus, according to the pharmacopoeial methods (FP VI and VII), showed the presence of the same terpenoids in both essential oils, however, the relative percentage composition of the components were different. These differences are caused by the different extraction times used in both methods. Since each essential oil to be admitted to medicinal use should meet requirements regarding the composition of major chemical components, the minimum time for the hydrodistillation of the essential oils from sage should be 1 h.


Assuntos
Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis/análise , Óleos de Plantas/análise , Salvia officinalis/química , Destilação , Óleos Voláteis/isolamento & purificação , Óleos Voláteis/normas , Folhas de Planta , Óleos de Plantas/isolamento & purificação , Óleos de Plantas/normas , Plantas Medicinais , Controle de Qualidade , Microextração em Fase Sólida , Fatores de Tempo
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