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1.
Molecules ; 28(21)2023 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-37959858

RESUMO

Plants with medicinal benefits are a crucial source of compounds for developing drugs. This study was designed to determine the chemical composition, antibacterial, antibiofilm, antioxidant, and anti-enzymatic activities of Pulicaria incisa (Lam.) DC. We also reported the molecular interaction between identified molecules and several receptors associated with antimicrobial and antibiofilm activities. A total of seventeen and thirteen compounds were identified in aqueous and methanolic extracts of P. incisa, respectively. The methanolic extract yielded a higher total content of polyphenols and flavonoids of about 84.80 ± 2.8 mg GAE/g and 28.30 ± 1.2 mg QE/g, respectively. Significant antibacterial activity was recorded for both extracts, with minimum inhibitory concentration (MIC) values ranging from 30 to 36 µg/mL, and the result was comparable to the reference antibiotic control. Antibiofilm assays revealed that both extracts were able to reduce the attachment of bacterial cells to 96-well plates, but the highest antibiofilm activity was recorded against Staphylococcus aureus. The methanolic extract also showed anti-enzymatic potency and high antioxidant activity, as demonstrated by all assays used, including DPPH, FRAP, and ABTS. These results were further validated by in silico approaches, particularly the molecular interaction of the identified compounds with the targeted receptors. These findings present P. incisa as a significant source of antibacterial, antibiofilm, antioxidant, and anti-enzymatic molecules.


Assuntos
Antioxidantes , Pulicaria , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antibacterianos/farmacologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Metanol
2.
Plants (Basel) ; 12(6)2023 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-36986909

RESUMO

Andrographis paniculata is widely used as a traditional medicine in Asian countries. It has been classified as a safe and non-toxic medicine by traditional Chinese medicine. The investigation of the biological activities of A. paniculata is still focused on the crude extract and isolation of its main active compound, andrographolide, and its derivatives. However, the use of andrographolide alone has been shown to exacerbate unwanted effects. This highlights the importance of developing a fraction of A. paniculata with enhanced efficacy as an herbal-based medicine. In this study, the extraction and fractionation of A. paniculata, followed by quantitative analysis using high-performance liquid chromatography coupled with a DAD detector, were established to quantify the andrographolide and its derivative in each fraction. Biological activities, such as antioxidant, anticancer, antihypertensive, and anti-inflammatory activities, were evaluated to study their correlations with the quantification of active substances of A. paniculata extract and its fractions. The 50% methanolic fraction of A. paniculata exhibited the best cytotoxic activities against CACO-2 cells, as well as the best anti-inflammatory and antihypertensive activities compared to other extracts. The 50% methanolic fraction also displayed the highest quantification of its main active compound, andrographolide, and its derivatives, 14-deoxy-11,12-didehydroandrographolide, neoandrographolide, and andrograpanin, among others.

3.
J Ethnopharmacol ; 311: 116391, 2023 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-36948263

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Chamomile (M. chamomilla L.) is an herbaceous plant from family Astereaceae, that has a long history of use in traditional medicine. It has been used as herbal remedies for thousands of years to treat several diseases, including infections, neuropsychiatric, respiratory, gastrointestinal, and liver disorders. Chronic inflammation is involved in the pathogenesis of most infectious and non-infectious diseases and macrophages are considered the major cellular players that drive disease initiation and maintenance. AIM OF THE STUDY: The aim of this study was to evaluate the variation in the chemical profile of the essential oil of M. chamomilla plants collected in three experimental field sites in the Molise region. Additionally, we evaluated the pharmacological mechanism behind the anti-inflammatory effect of M. chamomilla essential oils. MATERIAL AND METHODS: Three essential oils (called GC1, GC2 and GC3) were extracted from aerial parts of M. chamomilla by hydrodistillation and chemical composition was analyzed by gas chromatography-mass spectrometry (GC-MS). The essential oils were tested for their ability to modulate pro-inflammatory murine macrophages and human peripheral blood mononuclear cells (PBMCs) functions. RESULTS: The chemical analysis of the samples revealed the presence of a high content of the oxygenated sesquiterpenes that represented more than the half of the entire oils. GC1, GC2 and GC3 essential oils significantly attenuated LPS/IFN-γ-induced inflammation by reducing M1 polarization. In details, they showed significant anti-inflammatory property by inhibiting NO, TNF-α and IL-6 production. These effects were correlated to a suppression of LPS-mediated p65 activation, the critical transactivation subunit for NF-κB transcription factor. Oxidative stress may trigger macrophages activation and elicit strong immune responses. Our study demonstrated that GC1, GC2 and GC3 were highly effective at increasing GCL and HMOX-1 anti-oxidant enzymes expression leading to the rapid scavenging of ROS. The antioxidant activity of these oils was explained throughout the activation of NRF2 signaling pathway. Next, we demonstrated that essential oils were able to reduce CD4+ T cell activation which are also involved in inflammatory processes. CONCLUSIONS: Our data describe for the first time that chamomile essential oils exerted their anti-inflammatory and antioxidant activity by modulating macrophages and CD4+ T cells-mediate immune response.


Assuntos
Óleos Voláteis , Humanos , Animais , Camundongos , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Óleos Voláteis/análise , Camomila , Leucócitos Mononucleares , Antioxidantes/farmacologia , Lipopolissacarídeos/farmacologia , Lipopolissacarídeos/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Macrófagos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios/análise , Inflamação/tratamento farmacológico
4.
Phytother Res ; 35(3): 1432-1442, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33058354

RESUMO

Malignant melanoma is the deadliest skin cancer, due to its propensity to metastasize. MAPKs and NF-κB pathways are constitutively activated in melanoma and promote cell proliferation, cell invasion, metastasis formation, and resistance to therapeutic regimens. Thus, they represent potential targets for melanoma prevention and treatment. Phytochemicals are gaining considerable attention for the management of melanoma because of their several cellular and molecular targets. A screening of a small library of sesquiterpenes lactones selected cynaropicrin, isolated from the aerial parts of Centaurea drabifolia subsp. detonsa, for its potential anticancer effect against melanoma cells. Treatment of human melanoma cells A375 with cynaropicrin resulted in inhibition of cell proliferation and induction of caspase-3-dependent apoptosis. Furthermore, cynaropicrin reduced several cellular malignant features such migration, invasion, and colonies formation through the inhibition of ERK1/2 and NF-κB activity. Cynaropicrin was able to reduce intracellular reactive oxygen species generation, which are involved in all the stages of carcinogenesis. Indeed, cynaropicrin increased the expression of several antioxidant genes, such as glutamate-cysteine ligase and heme oxygenase-1, by promoting the activation of the transcription factor Nrf-2. In conclusion, our results individuate cynaropicrin as a potential adjuvant chemotherapeutic agent for melanoma by targeting several protumorigenic signaling pathways.


Assuntos
Lactonas/uso terapêutico , Melanoma/tratamento farmacológico , Quinases de Proteína Quinase Ativadas por Mitógeno/metabolismo , NF-kappa B/metabolismo , Sesquiterpenos/uso terapêutico , Apoptose , Proliferação de Células , Progressão da Doença , Humanos , Lactonas/farmacologia , Sesquiterpenos/farmacologia , Transdução de Sinais
5.
Biomed Res Int ; 2019: 3548396, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31111049

RESUMO

Introduction. HPV infection is a highly infectious disease; about 65% of partners of individuals with genital warts will develop genital condylomatosis. Only in 20-30% it regresses spontaneously and relapse rates range deeply (9-80%). Echinacea extracts possess antiviral and immunomodulator activities. The aim of this study was to evaluate the efficacy of the therapy, using a formulation based on HPVADL18® (on dry extracts of 200 mg Echinacea Purpurea (EP) roots plus E. Angustifolia (EA)), on the posttreatment relapse incidence of genital condylomatosis. Materials and Methods. It is a prospective single-arm study. Patients with a satisfactory and positive vulvoscopy, colposcopy, or peniscopy for genital condylomatosis were divided into two random groups and subjected to destructive therapy with Co2 Laser. Group A (N=64) immediately after the laser therapy started a 4-month treatment with oral HPVADL18®; Group B (N=61) did not undergo any additional therapy. Patients were subjected to a follow-up after 1, 6, and 12 months. Differences in relapse incidence between the two groups during follow-up controls were evaluated by χ2-test; the groups were stratified by age, gender, and condylomatosis extension degree. Results and Discussion. Gender, age, and condyloma lesions' extension degree showed no statistically significant differences between the two trial groups. The relapse incidence differs statistically between the two studied groups and progressively decreases during the 12 months after treatment in both groups. Statistically significant reduction of relapse rates has been shown in Group A in patients over 25 years old. This difference is significant for both men and women. The relapse incidence is superior in case of extended condylomatosis. Conclusions. In conclusion, the presence of a latent infection causes condylomatosis relapse; in order to reduce the relapse risk an induction of a protective immune response seems to be essential to allow rapid viral clearance from genital areas surrounding lesion and treatment zones. Echinacea promotes this process. EP and EA dry root extracts seem to be a valid adjuvant therapy in reducing relapse incidence of lesions in patients treated for genital condylomatosis.


Assuntos
Condiloma Acuminado/tratamento farmacológico , Suplementos Nutricionais , Echinacea/química , Genitália/efeitos dos fármacos , Imunomodulação , Recidiva Local de Neoplasia/tratamento farmacológico , Extratos Vegetais/farmacologia , Adulto , Colposcopia , Feminino , Humanos , Incidência , Masculino , Infecções por Papillomavirus/complicações , Pênis , Raízes de Plantas/química , Estudos Prospectivos , Recidiva , Escroto , Neoplasias do Colo do Útero/tratamento farmacológico , Adulto Jovem
6.
J Agric Food Chem ; 67(11): 3159-3167, 2019 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-30807134

RESUMO

Bergamot ( Citrus bergamia) is cultivated in Southern Italy almost exclusively to produce the prized essential oil, a top note in several perfumes. The juice of bergamot, until recently poorly studied, is the object of a growing scientific interest due to its claimed activity to treat metabolic syndrome. The aim of this investigation was a detailed characterization of bergamot juice polyphenolic fraction (BPF) based on a UPLC-DAD-MS analysis complemented by preparative chromatographic separations, followed by NMR characterization of the isolated compounds. The combination of these techniques efficiently covered different classes of secondary metabolites, leading to the identification of 39 components, several of which had never been reported from bergamot. One of them, bergamjuicin (35), is a new flavanone glycoside, whose structure has been determined by MS and NMR techniques. The reported results could provide a guide for future routine analyses of BPF, a material of great nutraceutical and industrial interest.


Assuntos
Citrus/química , Compostos Fitoquímicos/química , Extratos Vegetais/química , Polifenóis/química , Cromatografia Líquida de Alta Pressão , Frutas/química , Espectroscopia de Ressonância Magnética , Espectrometria de Massas
7.
Nat Prod Res ; 33(12): 1798-1803, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29397771

RESUMO

During our search for potential templates of HIV-1 reverse transcriptase (RT) and integrase (IN) dual inhibitors, the methanolic extract obtained from aerial parts of Limonium morisianum was investigated. Repeated bioassay-guided chromatographic purifications led to the isolation of the following secondary metabolites: myricetin, myricetin 3-O-rutinoside, myricetin-3-O-(6″-O-galloyl)-ß-d-galactopyranoside, (-)-epigallocatechin 3-O-gallate, tryptamine, ferulic and phloretic acids. The isolated compounds were tested on both HIV-1 RT-associated RNase H and IN activities. Interestingly, (-)-epigallocatechin-3-O-gallate and myricetin-3-O-(6″-O-galloyl)-ß-d-galactopyranoside potently inhibited both enzyme activities with IC50 values ranging from 0.21 to 10.9 µM. Differently, tryptamine and ferulic acid exhibited a significant inhibition only on the IN strand transfer reaction, showing a selectivity for this viral enzyme. Taken together these results strongly support the potential of this plant as a valuable anti HIV-1 drugs source worthy of further investigations.


Assuntos
Fármacos Anti-HIV/farmacologia , Inibidores de Integrase de HIV/farmacologia , Transcriptase Reversa do HIV/antagonistas & inibidores , Plumbaginaceae/química , Fármacos Anti-HIV/química , Flavonoides/química , Flavonoides/farmacologia , Galactose/análogos & derivados , Galactose/química , Galactose/farmacologia , Inibidores de Integrase de HIV/química , Itália , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Inibidores da Transcriptase Reversa/química , Inibidores da Transcriptase Reversa/farmacologia , Ribonuclease H/antagonistas & inibidores
8.
Nutrients ; 10(9)2018 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-30223482

RESUMO

Doxorubicin is a highly active antineoplastic agent, but its clinical use is limited because of its cardiotoxicity. Although nutraceuticals endowed with anti-inflammatory properties exert cardioprotective activity, their bioavailability and stability are inconsistent. In an attempt to address this issue, we evaluated whether bioavailable nanoemulsions loaded with nutraceuticals (curcumin and fresh and dry tomato extracts rich in lycopene) protect cardiomyoblasts (H9C2 cells) from doxorubicin-induced toxicity. Nanoemulsions were produced with a high-pressure homogenizer. H9C2 cells were incubated with nanoemulsions loaded with different nutraceuticals alone or in combination with doxorubicin. Cell viability was evaluated with a modified MTT method. The levels of the lipid peroxidation products malondialdehyde (MDA) and 4-hydroxy-2-butanone (4-HNA), and of the cardiotoxic-related interleukins IL-6, IL-8, IL-1ß and IL-10, tumor necrosis factor-alpha (TNF-α), and nitric oxide were analyzed in cardiomyoblasts. The hydrodynamic size of nanoemulsions was around 100 nm. Cell viability enhancement was 35⁻40% higher in cardiomyoblasts treated with nanoemulsion + doxorubicin than in cardiomyoblasts treated with doxorubicin alone. Nanoemulsions also protected against oxidative stress as witnessed by a reduction of MDA and 4-HNA. Notably, nanoemulsions inhibited the release of IL-6, IL-8, IL-1ß, TNF-α and nitric oxide by around 35⁻40% and increased IL-10 production by 25⁻27% versus cells not treated with emulsions. Of the nutraceuticals evaluated, lycopene-rich nanoemulsions had the best cardioprotective profile. In conclusion, nanoemulsions loaded with the nutraceuticals described herein protect against cardiotoxicity, by reducing inflammation and lipid oxidative stress. These results set the stage for studies in preclinical models.


Assuntos
Anti-Inflamatórios/farmacologia , Curcumina/farmacologia , Suplementos Nutricionais , Doxorrubicina/toxicidade , Portadores de Fármacos , Cardiopatias/prevenção & controle , Licopeno/farmacologia , Miócitos Cardíacos/efeitos dos fármacos , Nanopartículas , Animais , Antioxidantes/farmacologia , Cardiotoxicidade , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Citocinas/metabolismo , Citoproteção , Composição de Medicamentos , Emulsões , Cardiopatias/induzido quimicamente , Cardiopatias/metabolismo , Cardiopatias/patologia , Mediadores da Inflamação/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Miócitos Cardíacos/metabolismo , Miócitos Cardíacos/patologia , Estresse Oxidativo/efeitos dos fármacos , Ratos
9.
Fitoterapia ; 120: 98-102, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28579551

RESUMO

The apolar organic extract obtained from aerial parts of Centaurea drabifolia Sibth. & Sm. subsp. detonsa (Bornm.) Wagenitz, growing wild in Turkey, was investigated for the first time for its secondary metabolite composition. Seven sesquiterpene lactones belonging to the guaiane class (1-7), including the new compound 4, along with a fatty acid lactone derivative (8), were isolated. The structures of these compounds were established by spectroscopic analysis, including 2D NMR spectroscopic techniques, with the stereostructure of the new guaiane 4 determined with the help of MTPA derivatization. Cytotoxic activities of compounds 1-7 were evaluated against two cancer cell lines, namely acute lymphoblastic leukemia (CCRF-CEM) and its multidrug-resistant subline CEM/ADR5000. Results showed that aguerin B (1) and cynaropicrin (2) showed a potent activity on both cell lines revealing interesting details about the structure-activity relationships in the class of acylated guaiane sesquiterpenes.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Lactonas/farmacologia , Leucemia/patologia , Sesquiterpenos de Guaiano/farmacologia , Sesquiterpenos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Centaurea/química , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Lactonas/isolamento & purificação , Leucemia/tratamento farmacológico , Estrutura Molecular , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Sesquiterpenos/isolamento & purificação , Sesquiterpenos de Guaiano/isolamento & purificação , Relação Estrutura-Atividade , Turquia
10.
Fitoterapia ; 116: 61-65, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27871974

RESUMO

Onopordum illyricum L. is a medicinal plant used in the Mediterranean area as antipyretic for the treatment of respiratory and urinary inflammations and to treat skin ulcers. Repeated chromatographic purification of O. illyricum aerial parts led to the isolation of six known sesquiterpenes, which were evaluated for the inhibition of the pro-inflammatory transcription factors NF-κB and STAT3 and for the activation of the transcription factor Nrf2, which regulates the cellular antioxidant response. Structure-activity relationships were interpreted by the NMR-based cysteamine assay. The sesquiterpene lactone vernomelitensin significantly inhibited NF-κB and STAT3, showing also a significant Nrf2 activation. Accordingly, the cysteamine assay selected vernomelitensin as the most reactive of the isolated sesquiterpenes, identifying the α,ß-unsaturated aldehyde moiety as responsible for the higher (re)activity.


Assuntos
Anti-Inflamatórios/farmacologia , Lactonas/farmacologia , Onopordum/química , Plantas Medicinais/química , Sesquiterpenos/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Células HeLa , Humanos , Itália , Lactonas/isolamento & purificação , Camundongos , Estrutura Molecular , NF-kappa B/antagonistas & inibidores , Células NIH 3T3 , Componentes Aéreos da Planta/química , Fator de Transcrição STAT3/antagonistas & inibidores , Sesquiterpenos/isolamento & purificação , Relação Estrutura-Atividade
11.
Planta Med ; 82(9-10): 761-6, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27002390

RESUMO

Transient receptor potential channels and cannabinoid receptors are deputed to the regulation of sensory, homeostatic, and inflammatory events in the human organism. Therefore, their modulation promises to have relevant applications in important therapeutic areas such as inflammation, pain, and cancer. This review summarizes the contribution of marine research in this relatively young field, highlighting the potential of the chemodiversity carried by marine natural products in the discovery of new ligands.


Assuntos
Produtos Biológicos/farmacologia , Receptores de Canabinoides/efeitos dos fármacos , Canais de Potencial de Receptor Transitório/efeitos dos fármacos , Animais , Antozoários/química , Organismos Aquáticos , Cianobactérias/química , Fungos/química , Humanos , Poríferos/química
12.
Nat Prod Res ; 30(6): 735-9, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26179294

RESUMO

The essential oils from Origanum dictamnus, Origanum libanoticum and Origanum microphyllum were analysed by GC-MS, finding carvacrol, p-cymene, linalool, γ-terpinene and terpinen-4-ol as major components. The antioxidant activity by the DPPH and FRAP tests and the antiproliferative activity against two human cancer cell lines, LoVo and HepG2, were investigated, showing that the essential oil of O. dictamnus was statistically the most inhibitory on both the cell lines, while all the oils exerted a weak antioxidant activity. Furthermore, the samples were tested against 10 Gram-negative and Gram-positive bacteria; all the oils were active on Gram-positive bacteria but O. dictamnus essential oil was the most effective (MIC = 25-50 µg/mL), showing also a good activity against the Gram-negative Escherichia coli (MIC = 50 µg/mL). Data suggest that these essential oils and particularly O. dictamnus oil could be used as valuable new flavours with functional properties for food or nutraceutical products.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Óleos Voláteis/química , Origanum/química , Monoterpenos Acíclicos , Antibacterianos/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Linhagem Celular Tumoral , Monoterpenos Cicloexânicos , Cimenos , Escherichia coli/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Grécia , Humanos , Líbano , Monoterpenos/isolamento & purificação , Monoterpenos/farmacologia , Origanum/classificação , Óleos de Plantas/química
13.
Nat Prod Commun ; 10(6): 1075-8, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-26197555

RESUMO

The phytochemical composition of the essential oils of three Sideritis libanotica subspecies, namely S. libanotica ssp. libanotica, S. libanotica ssp. linearis and S. libanotica ssp. michroclamys, all collected in Lebanon, was analyzed by GC and GC-MS. The diterpene sideridiol was recognized as the main constituent of both S. libanotica ssp. libanotica (50.8%) and S. libanotica ssp. michroclamys (18.4%) oils, while hexadecanoic acid (10.5%) prevailed in S. libanotica ssp. linearis. The antioxidant activity of the oils was studied in two cell free systems by DPPH radical scavenging and ferric ion reduction (FRAP) assays; only S. libanotica ssp. linearis showed a moderate activity when assayed by the FRAP test (0.6 ± 0.01 mmol TE/mL).


Assuntos
Antioxidantes/química , Óleos Voláteis/química , Óleos de Plantas/química , Sideritis/química , Cromatografia Gasosa-Espectrometria de Massas , Sideritis/classificação
14.
Molecules ; 20(1): 1571-8, 2015 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-25603502

RESUMO

The petroleum ether extract of Magydaris tomentosa flowers (Desf.) W. D. J. Koch has been analyzed by GC-MS. It is mainly constituted by furanocoumarins such as xanthotoxin, xanthotoxol, isopimpinellin, and bergaptene. Other coumarins such as 7-methoxy-8-(2-formyl-2-methylpropyl) coumarin and osthole also occurred. The antiproliferative activity of Magydaris tomentosa flower extract has been evaluated in vitro on murine monocye/macrophages (J774A.1), human melanoma (A375) and human breast cancer (MCF-7) tumor cell lines, showing a major activity against the latter.


Assuntos
Alcanos/química , Apiaceae/química , Extratos Vegetais/farmacologia , Animais , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cumarínicos/química , Flores/química , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Camundongos
15.
Nat Prod Res ; 29(17): 1630-40, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25537231

RESUMO

The objectives of our research were to study the chemical composition and the in vitro anticancer effect of the essential oil of Salvia verbenaca growing in natural sites in comparison with those of cultivated (Sc) plants. The oil from wild (Sw) S. verbenaca presented hexadecanoic acid (23.1%) as the main constituent, while the oil from Sc plants contained high quantities of hexahydrofarnesyl acetone (9.7%), scarce in the natural oil (0.7%). The growth-inhibitory and proapoptotic effects of the essential oils from Sw and Sc S. verbenaca were evaluated in the human melanoma cell line M14, testing cell vitality, cell membrane integrity, genomic DNA fragmentation and caspase-3 activity. Both the essential oils were able to inhibit the growth of the cancer cells examined inducing also apoptotic cell death, but the essential oil from cultivated samples exhibited the major effects.


Assuntos
Antineoplásicos Fitogênicos/química , Óleos Voláteis/química , Óleos de Plantas/química , Salvia/química , Apoptose , Caspase 3/metabolismo , Linhagem Celular Tumoral/efeitos dos fármacos , Fragmentação do DNA , Humanos , Melanoma/patologia , Ácido Palmítico/química , Ácido Palmítico/isolamento & purificação , Terpenos/química , Terpenos/isolamento & purificação
16.
Nat Prod Res ; 29(9): 857-63, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25533422

RESUMO

In this study, the chemical compositions of the essential oils from aerial parts (JmA) and radices (JmR) of Jacobaea maritima (L.) Pelser & Meijden, collected in Croatia, and of Jacobaea maritima subsp. bicolor (Willd.) B. Nord. & Greuter, collected in Sicily, were evaluated by using gas chromatography and gas chromatography-mass spectrometry. The main components of the essential oil from J. maritima, both in JmA and JmR, were pentacosane (15.7%), heptacosane (13.1%) and nonacosane (8.1%) whereas the essential oil from J. maritima subsp. bicolor was characterised by the presence of hexadecanoic acid (14.6%), caryophyllene oxide (9.3%) and hexahydrofarnesylacetone (6.5%). The comparison of the essential oil with other studied oils of the genus Jacobaea is discussed.


Assuntos
Asteraceae/química , Óleos Voláteis/química , Óleos de Plantas/química , Alcanos/química , Alcanos/isolamento & purificação , Croácia , Cromatografia Gasosa-Espectrometria de Massas , Ácido Palmítico/química , Ácido Palmítico/isolamento & purificação , Sesquiterpenos Policíclicos , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Sicília
17.
Fitoterapia ; 99: 198-203, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25285382

RESUMO

A new acetophenone derivative named gnaphaliol 9-O-propanoate (1) was isolated from the chloroform fraction of EtOH extract of Helichrysum italicum ssp. italicum flowers along with the five known acetophenones 12-acetoxytremetone (2), 13-(2-methylpropanoyloxy)toxol (3), [2,3-dihydro-2-[1-(hydroxymethyl)ethenyl]-5-benzofuranyl]-ethanone (4), 1-[2-[1-[(acetyloxy)methyl]ethenyl]-2,3-dihydro-3-hydroxy-5-benzofuranyl]-ethanone (5) and gnaphaliol (6). The structures of compounds 1-6 were elucidated by extensive spectroscopic methods including 1D- ((1)H and (13)C) and 2D-NMR (DQF-COSY, HSQC, HMBC, TOCSY and ROESY) experiments as well as ESIMS analysis. The isolated compounds were investigated for their cytotoxicity, anti-inflammatory and antioxidant properties. Biological assays on human colonic epithelial cells showed that compound 2 possessed antioxidant effects reducing reactive oxygen species (ROS) production.


Assuntos
Acetofenonas/química , Células Epiteliais/efeitos dos fármacos , Flores/química , Helichrysum/química , Animais , Anti-Inflamatórios/química , Antioxidantes/química , Linhagem Celular , Humanos , Macrófagos/efeitos dos fármacos , Camundongos , Estresse Oxidativo , Espécies Reativas de Oxigênio/metabolismo
18.
Arch Gynecol Obstet ; 290(2): 283-9, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-24599566

RESUMO

PURPOSE: To evaluate the effect of a protocol of local anesthesia and epinephrine associated with sedo-analgesia on post-TVT-O pain in comparison with infiltration of saline and epinephrine. METHODS: Forty-two patients undergoing TVT-O were randomized into two groups to receive periurethral infiltration with epinephrine only (group A, n = 21) or with epinephrine plus 1 % lidocaine hydrochloride (group B, n = 21). Post-operative pain was assessed using a visual analog scale (VAS) from 0 (absence of pain) to 10 (maximum pain possible), 1, 6, 12 and 24 h after the procedure. The total amount of analgesia was recorded and the proportion of women reporting a pain VAS score ≥4, 1 h after the procedure was calculated. ANOVA for repeated measures and Bonferroni correction, the Student's t test for independent samples, the Mann-Whitney U test, the Fisher exact test, or the χ (2) test for parametric was used. RESULTS: Pain level was significantly lower in group B 1 (p = 0.01) and 6 h (p = 0.05) after surgery, but not 12 and 24 h after the procedure. No significant difference was observed in the proportion of women requesting analgesia and in the total dosage of analgesics between the two groups. A significant higher proportion of women in group A reported a pain VAS score higher than four 1 h after surgery in comparison with patients in group B. CONCLUSIONS: This randomized study seems to indicate that systematic infiltration before TVT-O positioning with local anesthetic may reduce immediate post-operative pain.


Assuntos
Analgesia/métodos , Anestesia Local/métodos , Dor Pós-Operatória/tratamento farmacológico , Slings Suburetrais , Incontinência Urinária por Estresse/cirurgia , Analgésicos/administração & dosagem , Anestésicos Locais/administração & dosagem , Método Duplo-Cego , Vias de Administração de Medicamentos , Epinefrina/administração & dosagem , Feminino , Humanos , Lidocaína/administração & dosagem , Pessoa de Meia-Idade , Manejo da Dor , Medição da Dor , Placebos , Resultado do Tratamento
19.
J Ethnopharmacol ; 150(3): 901-6, 2013 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-24140587

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: In the Mediterranean Area, the flowers of Helichrysum italicum ssp. italicum are a traditional remedy for the treatment of intestinal complaints and are used as herbal tea for curing digestive, stomachic and intestinal diseases. In order to find scientific evidence for the traditional utilization of this plant, the effect of an ethanolic extract of Helichrysum italicum was investigated by using in vivo and in vitro experimental models. Then, through bioassay-guided fractionation procedures, active component(s) were identified. MATERIAL AND METHODS: Contractility in vitro was evaluated by stimulating the isolated ileum, in an organ bath, with acetylcholine and barium chloride; motility in vivo was evaluated by measuring upper gastrointestinal transit, both in control mice and in mice with experimental intestinal inflammation induced by croton oil. Chromatographic separation techniques such as HPLC and silica gel columns have yielded the active principles of Helichrysum italicum. RESULTS: We found that the ethanolic extract of Helichrysum italicum ssp. italicum flowers elicited antispasmodic actions in the isolated mouse ileum and inhibited transit preferentially in the inflamed gut. A bioassay guided fractionation of the extract yielded the known compounds 12-acetoxytremetone (1) and 2,3-dihydro-2-[1-(hydroxymethyl)ethenyl]-5-benzofuranyl]-ethanone (2). CONCLUSION: Present study supported the traditional use of Helichrysum italicum ssp. italicum flowers for intestinal complaints and through bioassay-guided fractionation procedures from the crude extract we showed that 12-acetoxytremetone (1) and 2,3-dihydro-2-[1-(hydroxymethyl)ethenyl]-5-benzofuranyl]-ethanone (2) acted in a synergistic way to produce an intestinal antispasmodic effect.


Assuntos
Helichrysum , Íleo/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Óleo de Cróton , Flores/química , Trânsito Gastrointestinal/efeitos dos fármacos , Íleo/fisiologia , Técnicas In Vitro , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Masculino , Camundongos , Camundongos Endogâmicos ICR , Contração Muscular/efeitos dos fármacos , Parassimpatolíticos/uso terapêutico , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/uso terapêutico , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico
20.
Food Chem Toxicol ; 55: 304-12, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-23313609

RESUMO

Solanum tuberosum L. var. Vitelotte is a potato variety widely used for human consumption. The pigments responsible for its attractive color belong to the class of anthocyanins. The objectives of this study were to characterize and measure the concentration of anthocyanins in pigmented potatoes and to evaluate their antioxidant and antimicrobial activities and their anti-proliferative effects in solid and hematological cancer cell lines. Anthocyanins exert anti-bacterial activity against different bacterial strains and a slight activity against three fungal strains. The Gram-positive bacterium Staphylococcus aureus and the fungus Rhyzoctonia solani were the most affected microorganisms. Antioxidant activities were evaluated by DPPH and FRAP methods; the extract showed a higher reducing capability than anti-radical activity. Moreover, we found that in different cancer cell models the anthocyanins cause inhibition of proliferation and apoptosis in a dose dependent manner. These biological activities are likely due to the high content of malvidin 3-O-p-coumaroyl-rutinoside-5-O-glucoside and petunidin 3-O-p-coumaroyl-rutinoside-5-O-glucoside.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Extratos Vegetais/farmacologia , Solanum tuberosum/química , Linhagem Celular , Humanos , Testes de Sensibilidade Microbiana
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