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1.
Talanta ; 228: 122216, 2021 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-33773702

RESUMO

Recent research showed that plant secondary metabolites in pollen may exacerbate the protein-mediated allergic reaction in pollen allergy. It was found that allergenic pollen from various plant families contain significant amounts of electrophiles which may covalently bind to nucleophilic groups of proteins, such as thiol moieties. Electrophiles in pollen of the Asteraceae species are typically sesquiterpene lactones, but the nature of electrophilic metabolites in allergenic pollen of other plant families is unknown. We developed a solid-supported cysteinyl probe in order to selectively extract physiologically relevant electrophiles from pollen extracts, and to enable their subsequent characterization by on-line and off-line spectroscopic analysis. The validity of this approach was evaluated with a selection of structurally different model compounds and with a spiked model extract.


Assuntos
Asteraceae , Hipersensibilidade , Alérgenos , Humanos , Extratos Vegetais , Proteínas de Plantas , Pólen
2.
BMC Complement Altern Med ; 19(1): 292, 2019 Nov 04.
Artigo em Inglês | MEDLINE | ID: mdl-31685022

RESUMO

BACKGROUND: The herbal medicine Bryophyllum pinnatum has been used as a tocolytic agent in anthroposophic medicine and, recently, in conventional settings alone or as an add-on medication with tocolytic agents such as atosiban or nifedipine. We wanted to compare the inhibitory effect of atosiban and nifedipine on human myometrial contractility in vitro in the absence and in the presence of B. pinnatum press juice (BPJ). METHODS: Myometrium biopsies were collected during elective Caesarean sections. Myometrial strips were placed under tension into an organ bath and allowed to contract spontaneously. Test substances alone and at concentrations known to moderately affect contractility in this setup, or in combination, were added to the organ bath, and contractility was recorded throughout the experiments. Changes in the strength (measured as area under the curve (AUC) and amplitude) and frequency of contractions after the addition of all test substances were determined. Cell viability assays were performed with the human myometrium hTERT-C3 and PHM1-41 cell lines. RESULTS: BPJ (2.5 µg/mL), atosiban (0.27 µg/mL), and nifedipine (3 ng/mL), moderately reduced the strength of spontaneous myometrium contractions. When BPJ was added together with atosiban or nifedipine, inhibition of contraction strength was significantly higher than with the tocolytics alone (p = 0.03 and p < 0.001, respectively). In the case of AUC, BPJ plus atosiban promoted a decrease to 48.8 ± 6.3% of initial, whereas BPJ and atosiban alone lowered it to 70.9 ± 4.7% and to 80.9 ± 4.1% of initial, respectively. Also in the case of AUC, BPJ plus nifedipine promoted a decrease to 39.9 ± 4.6% of initial, at the same time that BPJ and nifedipine alone lowered it to 78.9 ± 3.8% and 71.0 ± 3.4% of initial. Amplitude data supported those AUC data. The inhibitory effects of BPJ plus atosiban and of BPJ plus nifedipine on contractions strength were concentration-dependent. None of the test substances, alone or in combination, decreased myometrial cell viability. CONCLUSIONS: BPJ enhances the inhibitory effect of atosiban and nifedipine on the strength of myometrial contractions, without affecting myometrium tissue or cell viability. The combination treatment of BPJ with atosiban or nifedipine has therapeutic potential.


Assuntos
Kalanchoe/química , Miométrio/efeitos dos fármacos , Nifedipino/antagonistas & inibidores , Extratos Vegetais/farmacologia , Nascimento Prematuro/prevenção & controle , Tocolíticos/antagonistas & inibidores , Contração Uterina/efeitos dos fármacos , Vasotocina/análogos & derivados , Adulto , Antagonismo de Drogas , Feminino , Humanos , Técnicas In Vitro , Miométrio/fisiopatologia , Nifedipino/farmacologia , Gravidez , Tocolíticos/farmacologia , Vasotocina/antagonistas & inibidores , Vasotocina/farmacologia , Adulto Jovem
3.
BMC Complement Altern Med ; 19(1): 23, 2019 Jan 18.
Artigo em Inglês | MEDLINE | ID: mdl-30658716

RESUMO

BACKGROUND: Women diagnosed with breast cancer frequently seek complementary and alternative (CAM) treatment options that can help to cope with their disease and the side effects of conventional cancer therapy. Especially in Europe, breast cancer patients use herbal products containing mistletoe (Viscum album L.). The oldest and one of the most prescribed conventional drugs for the treatment of estrogen receptor positive breast cancer is tamoxifen. Aside from positive clinical experience with the combination of tamoxifen and mistletoe, little is known about possible herb-drug interactions (HDIs) between the two products. In the present in vitro study, we investigated the effect of standardized commercial mistletoe preparations on the activity of endoxifen, the major active metabolite of tamoxifen. METHODS: The estrogen receptor positive human breast carcinoma cell line MCF-7 was treated with (E/Z)-endoxifen hydrochloride in the presence and absence of a defined estradiol concentration. Each concentration of the drug was combined with fermented Viscum album L. extracts (VAE) at clinically relevant doses, and proliferation, apoptosis and cell cycle were analyzed. In parallel, possible inhibition of CYP3A4/5 and CYP2D6 was investigated using 50-donor mixed gender pooled human liver microsomes (HLMs). RESULTS: VAE did not inhibit endoxifen induced cytostasis and cytotoxicity. At higher concentrations, VAE showed an additive inhibitory effect. VAE preparations did not cause inhibition of CYP3A4/5 and CYP2D6 catalyzed tamoxifen metabolism. CONCLUSIONS: The in vitro results suggest that mistletoe preparations can be used in combination with tamoxifen without the risk of HDIs.


Assuntos
Citocromo P-450 CYP2D6/metabolismo , Citocromo P-450 CYP3A/metabolismo , Extratos Vegetais/farmacologia , Tamoxifeno/análogos & derivados , Viscum album/química , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Interações Ervas-Drogas , Humanos , Células MCF-7 , Extratos Vegetais/química , Tamoxifeno/química , Tamoxifeno/farmacologia
4.
Phytomedicine ; 23(8): 793-9, 2016 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-27288914

RESUMO

BACKGROUND: Berberis orthobotrys Bien ex Aitch. (Berberidaceae) is a plant indigenous of Pakistan that is locally used for the treatment of hypertension. HYPOTHESIS: This study evaluated the vasoactive properties of a Berberis orthobotrys root extract and its fractions, and investigated the role of the endothelium and the underlying mechanism. STUDY DESIGN: An aqueous methanolic extract of Berberis orthobotrys roots was prepared and submitted to a multi-step liquid-liquid fractionation with solvents of increasing polarity. Vascular reactivity of the different fractions was assessed using porcine coronary artery rings either with or without endothelium, and in the presence or absence of specific pharmacological tools. The ability of Berberis orthobotrys extracts to affect phosphodiesterase (PDE) activity was evaluated using a radioenzymatic method and purified phosphodiesterases. RESULTS: The aqueous methanol extract induced similar relaxations in coronary artery rings with and without endothelium, and, amongst the three derived preparations, the butanol fraction (BFBO) was slightly but significantly more effective than the ethyl acetate fraction and the aqueous residue in rings without endothelium. Analysis of the butanol fraction (BFBO) by LC-ELSD-MS indicated the presence of four major isoquinoline alkaloids including berberine. BFBO significantly potentiated the relaxations induced by cyclic GMP- and cyclic AMP-dependent relaxing agonists, and inhibited contractions to KCl, CaCl2, and U46619 in endothelium denuded rings. In contrast, BFBO did not affect relaxations to endothelium-dependent vasodilators. BFBO concentration-dependently inhibited the cyclic GMP-hydrolyzing activity of basal PDE1, calmodulin-activated PDE1 and PDE5, and of cyclic AMP-hydrolyzing activity of PDE3 and PDE4 with IC50 values ranging from 40 to 130µg/ml. CONCLUSION: The butanol fraction of the aqueous methanol extract of Berberis orthobotrys roots induced pronounced endothelium-independent relaxations and inhibited contractile responses by acting directly at the vascular smooth muscle in the coronary artery. Moreover, BFBO potentiated relaxations induced by both cyclic GMP- and cyclic AMP-dependent vasodilators most likely due to its ability to inhibit several vascular PDEs, and in particular PDE4 and PDE5.


Assuntos
Berberis/química , Vasos Coronários/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Relaxamento Muscular/efeitos dos fármacos , Inibidores de Fosfodiesterase/farmacologia , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Acetatos , Animais , Butanóis , Técnicas In Vitro , Músculo Liso Vascular/efeitos dos fármacos , Solventes , Suínos , Água
5.
Phytomedicine ; 22(1): 158-64, 2015 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-25636885

RESUMO

AIMS: To determine if the phytotherapeutic agent, Bryophyllum pinnatum, could serve as an alternative drug for the overactive bladder syndrome, and to characterise the fraction responsible for the inhibition of detrusor contractility. METHODS: Fractions were prepared from the MeOH extract of B. pinnatum and further analysed by HPLC-PDA-MS. Detrusor muscle strips were prepared from porcine bladders and the electrically induced muscle contractility measured by organ bath. The effect of B. pinnatum leaf press juice (2.5-10%), a flavonoid fraction (0.1-1 mg/ml), and a bufadienolide fraction (0.1-40 µg/ml) on detrusor contractility was assessed and compared with controls (polar fraction (0.5-5 mg/ml) and oxybutynin (10(-8)-10(-6) M)). RESULTS: The press juice, at a concentration of 10% led to a reduction of detrusor contractility. Bladder strips treated with the flavonoid fraction showed a significant reduction of the contractility to 21.3 ± 5.2% (1 mg/ml) while the bufadienolide fraction had no inhibitory effect in the investigated concentrations. The polar fraction showed a reduction of the contractility in a pH-dependent fashion. At 10(-6) M concentration oxybutynin reduced the detrusor contractility to 21.9 ± 4.7%. CONCLUSIONS: The flavonoid fraction of Bryophyllum pinnatum reduces the porcine detrusor contractility in a dose- and time-dependent manner. Fractions from B. pinnatum may be a new pharmacological approach for the treatment of OAB.


Assuntos
Flavonoides/farmacologia , Kalanchoe/química , Contração Muscular/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Bufanolídeos/farmacologia , Feminino , Técnicas In Vitro , Estrutura Molecular , Músculo Liso/efeitos dos fármacos , Fitoterapia , Folhas de Planta/química , Suínos , Bexiga Urinária/efeitos dos fármacos , Bexiga Urinária Hiperativa/tratamento farmacológico
6.
Phytomedicine ; 21(5): 753-7, 2014 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-24373544

RESUMO

INTRODUCTION: Poor sleep quality in pregnancy is frequent. A treatment with sedatives is problematic due to possible adverse effects for mother and embryo/foetus. In the present study, we investigated the sedative effect of Bryophyllum pinnatum, a phytotherapeutic medication used in anthroposophic medicine. In previous clinical studies on its tocolytic effect, B. pinnatum showed a good risk/benefit ratio for mother and child. A recent analysis of the prescribing pattern for B. pinnatum in a network of anthroposophic physicians revealed sleep disorders as one of the most frequent diagnoses for which these preparations are prescribed. MATERIALS AND METHODS: In this prospective, multi-centre, observational study, pregnant women suffering from sleep problems were treated with B. pinnatum (350mg tablets, 50% leaf press juice, Weleda AG, Arlesheim, dosage at physician's consideration). Sleep quality, daily sleepiness and fatigue were assessed with the aid of standardised questionnaires, at the beginning of the treatment and after 2 weeks. Possible adverse drug reactions perceived by the patients during the treatment were recorded. RESULTS: The number of wake-ups, as well as the subjective quality of sleep was significantly improved at the end of the treatment with B. pinnatum. The Epworth Sleeping Scale decreased, indicating a decrease of the tiredness during the day. There was, however, no evidence for prolongation of the sleep duration, reduction in the time to fall asleep, as well as change in the Fatigue Severity Scale after B. pinnatum. No serious adverse drug reactions were detected. CONCLUSION: B. pinnatum is a suitable treatment of sleep problems in pregnancy. The data of this study encourage further clinical investigations on the use of B. pinnatum in sleep disorders.


Assuntos
Kalanchoe , Fitoterapia , Preparações de Plantas/uso terapêutico , Complicações na Gravidez/tratamento farmacológico , Transtornos do Sono-Vigília/tratamento farmacológico , Adulto , Medicina Antroposófica , Fadiga/tratamento farmacológico , Feminino , Humanos , Pessoa de Meia-Idade , Gravidez , Estudos Prospectivos , Adulto Jovem
7.
Phytomedicine ; 19(10): 947-51, 2012 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-22824522

RESUMO

AIMS: A broad spectrum of synthetic agents is available for the treatment of overactive bladder. Anti-cholinergic drugs show a poor compliance due to side effects. There is an increasing use of plant extracts in medicine. We have therefore investigated the inhibitory effects of leaf press juice from Bryophyllum pinnatum (Lam.) Oken (Kalanchoe pinnata L.) on bladder strips and compared the effects to that of oxybutynin. METHODS: Strips of porcine detrusor were prepared in Krebs solution and contractility was measured in a myograph system chamber aired with O2/CO2 at 37 °C. To induce contractions, electrical field stimulation (32 Hz, 40 V) was used for the inhibitory effect measurements, and carbachol (50 µM) for the relaxant effect measurements. Recordings were obtained in the absence and presence of increasing concentrations of Bryophyllum pinnatum leaf press juice (BPJ, 0.1-10%), and oxybutynin (10⁻7-10⁻³ M) as a reference substance. RESULTS: In inhibition experiments, BPJ as well as oxybutynin inhibited electrically induced contractions of porcine detrusor. BPJ at concentrations of 5% inhibited the contraction compared to a time matched control significantly by 74.6±10.2% (p<0.001). BPJ as well as oxybutynin relaxed carbachol pre-contracted porcine detrusor strips. The maximum relaxant effect of BPJ compared to a time matched control was 18.7±3.7 (p<0.05) at a concentration of 10% BPJ. CONCLUSIONS: Our investigations show that BPJ inhibits contractions induced by electrical field stimulation and relaxes carbachol-induced contractions. However, the effect was lower than that of the reference substance oxybutynin. It is important to continue in vitro experiments as well as clinical studies with BPJ that might offer a new treatment option for patients with OAB.


Assuntos
Kalanchoe , Ácidos Mandélicos/uso terapêutico , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Parassimpatolíticos/uso terapêutico , Bexiga Urinária Hiperativa , Bexiga Urinária/efeitos dos fármacos , Animais , Carbacol/farmacologia , Agonistas Colinérgicos/farmacologia , Estimulação Elétrica , Ácidos Mandélicos/farmacologia , Antagonistas Muscarínicos/farmacologia , Antagonistas Muscarínicos/uso terapêutico , Músculo Liso/fisiologia , Parassimpatolíticos/farmacologia , Fitoterapia , Folhas de Planta , Preparações de Plantas/farmacologia , Preparações de Plantas/uso terapêutico , Suínos , Bexiga Urinária/fisiologia , Bexiga Urinária Hiperativa/tratamento farmacológico
8.
Br J Pharmacol ; 165(3): 765-76, 2012 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-21797843

RESUMO

BACKGROUND AND PURPOSE: Leukotrienes (LTs) are pro-inflammatory mediators produced by 5-lipoxygenase (5-LO). Currently available 5-LO inhibitors either lack efficacy or are toxic and novel approaches are required to establish a successful anti-LT therapy. Here we provide a detailed evaluation of the effectiveness of the plant-derived alkaloid tryptanthrin as an inhibitor of LT biosynthesis. EXPERIMENTAL APPROACH: We analysed LT formation and performed mechanistic studies in human neutrophils stimulated with pathophysiologically relevant stimuli (LPS and formyl peptide), as well as in cell-free assays (neutrophil homogenates or recombinant human 5-LO) and in human whole blood. The in vivo effectiveness of tryptanthrin was evaluated in the rat model of carrageenan-induced pleurisy. KEY RESULTS: Tryptanthrin potently reduced LT-formation in human neutrophils (IC(50) = 0.6µM). However, tryptanthrin is not a redox-active compound and did not directly interfere with 5-LO activity in cell-free assays. Similarly, tryptanthrin did not inhibit the release of arachidonic acid, the activation of MAPKs, or the increase in [Ca(2+) ](i) , but it modified the subcellular localization of 5-LO. Moreover, tryptanthrin potently suppressed LT formation in human whole blood (IC(50) = 10µM) and reduced LTB(4) levels in the rat pleurisy model after a single oral dose of 10mg·kg(-1) . CONCLUSIONS AND IMPLICATIONS: Our data reveal that tryptanthrin is a potent natural inhibitor of cellular LT biosynthesis with proven efficacy in whole blood and is effective in vivo after oral administration. Its unique pharmacological profile supports further analysis to exploit its pharmacological potential.


Assuntos
Anti-Inflamatórios/farmacologia , Araquidonato 5-Lipoxigenase/metabolismo , Antagonistas de Leucotrienos/farmacologia , Neutrófilos/efeitos dos fármacos , Pleurisia/metabolismo , Quinazolinas/farmacologia , Adulto , Animais , Anti-Inflamatórios/uso terapêutico , Cálcio/metabolismo , Carragenina , Células Cultivadas , Medicamentos de Ervas Chinesas , Humanos , Antagonistas de Leucotrienos/uso terapêutico , Leucotrienos/metabolismo , Masculino , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Neutrófilos/metabolismo , Pleurisia/induzido quimicamente , Pleurisia/tratamento farmacológico , Quinazolinas/uso terapêutico , Ratos , Ratos Wistar , Espécies Reativas de Oxigênio/metabolismo
9.
Phytomedicine ; 19(1): 74-82, 2011 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-21802930

RESUMO

AIMS: The use of preparations from Bryophyllum pinnatum (Lamarck) Oken (Kalanchoe pinnata (Lamarck) Persoon) in tocolysis is supported by clinical evidence. We studied here the effect of B. pinnatum leaf press juice and its chemical fractions on the response of human myometrial strips. No data are available if the influence on myometrial strips of the juice differs from that of its components in the chemical fractions, in order to increase the pharmacological effect. METHODOLOGY: In vitro study to test the effect of repeated addition of B. pinnatum leaf press juice (BPJ) and its chemical components in several dilutions (undiluted, 1-10%) on myometrium strips hang up in a myograph chamber. Chemical analysis is including HPLC, MPLC with Sephadex LH-20 and TLC. RESULTS: All test solutions are inhibiting contractility by reducing the amplitude and the area under the curve (AUC) of the contractions. Undiluted BPJ and its undiluted chemical fraction 4 are reducing most effective these two parameters: the amplitude was at 78% of the baseline (95% CI (77-89); p<0.05) at the second addition of the BPJ and at 70% (95% CI (50-90); p<0.05) of the first addition of fraction 4; the AUC was at 82% (95% CI (69-95); p<0.05) of the baseline at the first addition of the press juice and at 51% (95% CI (27-74); p<0.05) at the first addition of fraction 4. The BPJ decreased amplitude and AUC significantly faster and increased frequency significantly faster than the control. Fractions could be tentatively assigned to bufadienolids, flavonoids and cinnamic acids. Fraction 4, accounted for flavonoids, increased the frequency of the contractions most effectively: 557% of the baseline (95% CI (316-797); p<0.05) at the first addition. CONCLUSION: Leaf juice of B. pinnatum and its flavonoid fraction are most effective in relaxing myometrial strips by inducing frequency.


Assuntos
Flavonoides/farmacologia , Kalanchoe/química , Miométrio/efeitos dos fármacos , Contração Uterina/efeitos dos fármacos , Feminino , Humanos , Técnicas In Vitro , Extratos Vegetais/farmacologia , Folhas de Planta/química , Gravidez , Tocólise
10.
Bioorg Med Chem ; 19(16): 4876-81, 2011 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-21775156

RESUMO

Phytochemical investigations of the n-hexane extract from the roots of Peltodon longipes (Lamiaceae) resulted in the isolation of 12 known abietane diterpenes (1-12). Structures were established on the basis of one and two dimensional nuclear magnetic resonance spectroscopic data ((1)H and (13)C, COSY, HSQC and HMBC), electron ionization mass spectrometric analysis (EIMS) as well as comparison with data from literature. These compounds, as well as eight known diterpenes (13-19) from Salvia miltiorrhiza, and two from Salvia sahendica (20 and 21) were evaluated for their cytotoxic effects in human pancreatic (MIAPaCa-2) and melanoma (MV-3) tumor cell lines using the MTT assay. Tanshinone IIa (13), 7α-acetoxyroyleanone (1), 1,2-dihydrotanshinone (16) and cryptotanshinone (14) had the highest cytotoxic effects in MIAPaCa-2, displaying IC(50) of 1.9, 4.7, 5.6, and 5.8 µM, respectively. Structure-activity relationships of abietane diterpenoid quinones are discussed.


Assuntos
Abietanos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Citotoxinas/farmacologia , Lamiaceae , Extratos Vegetais/farmacologia , Salvia , Abietanos/análise , Abietanos/química , Abietanos/isolamento & purificação , Antineoplásicos Fitogênicos/análise , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Citotoxinas/química , Citotoxinas/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Fitoterapia , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Raízes de Plantas , Relação Estrutura-Atividade
11.
Phytomedicine ; 17(12): 980-6, 2010 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-20381326

RESUMO

The use of preparations from Bryophyllum pinnatum in tocolysis is supported by both clinical (retrospective comparative studies) and experimental (using uterus strips) evidence. We studied here the effect of B. pinnatum juice on the response of cultured human myometrial cells to stimulation by oxytocin, a hormone known to be involved in the control of uterine contractions by increasing the intracellular free calcium concentration ([Ca2+]i). In this work, [Ca2+]i was measured online during stimulation of human myometrial cells (hTERT-C3 and M11) with oxytocin, which had been pre-incubated in the absence or in the presence of B. pinnatum juice. Since no functional voltage-gated Ca2+ channels could be detected in these myometrial cells, the effect of B. pinnatum juice was as well studied in SH-SY5Y neuroblastoma cells, which are known to have such channels and can be depolarised with KCl. B. pinnatum juice prevented the oxytocin-induced increase in [Ca2+]i in hTERT-C3 human myometrial cells in a dose-dependent manner, achieving a ca. 80% inhibition at a 2% concentration. Comparable results were obtained with M11 human primary myometrial cells. In hTERT-C3 cells, prevention of the oxytocin-induced increase in [Ca2+]i was independent of the extracellular Ca2+ concentration and of voltage-dependent Ca2+-channels. B. pinnatum juice delayed, but did not prevent the depolarization-induced increase in [Ca2+]i in SH-SY5Y cells. Taken together, the data suggest a specific and concentration-dependent effect of B. pinnatum juice on the oxytocin signalling pathway, which seems to corroborate its use in tocolysis. Such a specific mechanism would explain the rare and minor side-effects in tocolysis with B. pinnatum as well as its high therapeutic index.


Assuntos
Canais de Cálcio/efeitos dos fármacos , Cálcio/metabolismo , Kalanchoe , Miométrio/efeitos dos fármacos , Preparações de Plantas/farmacologia , Linhagem Celular , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Feminino , Humanos , Miométrio/metabolismo , Neuroblastoma , Ocitocina/metabolismo , Transdução de Sinais/efeitos dos fármacos
12.
J Ethnopharmacol ; 126(3): 463-7, 2009 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-19781615

RESUMO

UNLABELLED: PHARMACOLOGICAL RELEVANCE: Presentation of the scratch assay as a convenient and inexpensive in vitro tool to gain first insights in the wound healing potential of plant extracts and natural compounds. AIM OF THE STUDY: The present study deals with the optimization of the scratch assay which can be used as an in vitro model for quantification of fibroblast migration to and proliferation into the wounded area. It is suitable for the first evaluation of the wound re-epithelialization potential of crude herbal extracts, isolated compounds and pharmaceutical preparations. As a proof of concept three preparations from traditional medicinal plants were investigated. MATERIALS AND METHODS: Swiss 3T3 albino mouse fibroblasts were used in monolayers and platelet derived growth factor as positive control. Hexane and ethanolic extracts from Calendula officinalis and Matricaria recutita, Hypericum oil as well as the triterpenoids faradiol myristate and palmitate were studied. To differentiate between proliferation and migration antimitotic mitomycin C was added. RESULTS: Both extracts of Calendula officinalis stimulated proliferation and migration of fibroblasts at low concentrations, e.g. 10 microg/ml enhanced cell numbers by 64.35% and 70.53%, respectively. Inhibition of proliferation showed that this effect is mainly due to stimulation of migration. Faradiol myristate and palmitate gave comparable stimulation rates at an almost 50 microg/ml concentration, indicating that they contribute partially, but not most significantly to the wound healing effects of Calendula preparations. Extracts from Matricaria recutita were only moderately active. Hypericum oil was cytotoxic at concentrations higher than 0.5 microg/ml. CONCLUSIONS: The scratch assay in the present form can be used as a promising scientific approach and platform to differentiate between plant extracts known for their wound healing and their anti-inflammatory properties.


Assuntos
Calendula/química , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Células 3T3 , Animais , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Fibroblastos/efeitos dos fármacos , Camundongos
13.
Tanzan J Health Res ; 11(4): 226-34, 2009 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-20734703

RESUMO

The antiplasmodial, anti-trypanosomal and anti-leishmanial activity of 25 plant extracts obtained from seven Tanzanian medicinal plants: Annickia (Enantia) kummeriae (Annonaceae), Artemisia annua (Asteraceae), Pseudospondias microcarpa (Anacardiaceae), Drypetes natalensis (Euphorbiaceae), Acridocarpus chloropterus (Malpighiaceae), Maytenus senegalensis (Celastraceae) and Neurautanenia mitis (Papilonaceae), were evaluated in vitro against Plasmodium falciparum K1, Trypanosoma brucei rhodesiense STIB 900 and axenic Leishmania donovani MHOM-ET-67/82. Out of the 25 extracts tested, 17 showed good antiplasmodial activity (IC50 0.04-5.0 microg/ml), 7 exhibited moderate anti-trypanosomal activity (IC50 2.3-2.8 microg/ml), while 5 displayed mild anti-leishmanial activity (IC50 8.8-9.79 microg/ml). A. kummeriae, A. annua, P. microcarpa, D. natalensis, M. senegalensis and N. mitis extracts had good antiplasmodial activity (IC50 0.04-2.1 microg/ml) and selectivity indices (29.2-2,250 microg/ml). The high antiplasmodial, moderate anti-trypanosomal and mild anti-leishmanial activity make these plants good candidates for bioassay-guided isolation of anti-protozoal compounds which could serve as new lead structures for drug development.


Assuntos
Leishmania donovani/efeitos dos fármacos , Dose Letal Mediana , Extratos Vegetais/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Trypanosoma brucei rhodesiense/efeitos dos fármacos , Animais , Concentração Inibidora 50 , Folhas de Planta , Raízes de Plantas , Plantas Medicinais/química , Tanzânia
14.
Fitoterapia ; 76(3-4): 324-32, 2005 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-15893435

RESUMO

In the pursuit of the anti-inflammatory constituents in lipophilic woad extracts, the 5-lipoxygenase (5-LOX) inhibitory activity was investigated by HPLC-based activity profiling. In a low-resolution profiling, two time windows with peaks of activity were found. The first coincided with tryptanthrin, a known dual inhibitor of cyclooxygenase-2 (COX-2) and 5-LOX, whereas the major inhibitory fraction was towards the end of the HPLC run. The active fractions were profiled in a peak-resolved manner, and the compounds analyzed by LC-MS, GC and TLC. The activity in the lipophilic fractions of the Isatis extract could be linked to an unsaturated fatty acid, alpha-linolenic acid.


Assuntos
Isatis/química , Inibidores de Lipoxigenase , Extratos Vegetais/farmacologia , Folhas de Planta/química , Quinazolinas/farmacologia , Cromatografia Líquida de Alta Pressão , Células HL-60 , Humanos , Estrutura Molecular , Extratos Vegetais/química , Quinazolinas/química , Ácido alfa-Linolênico/química
15.
Phytochem Anal ; 15(1): 46-54, 2004.
Artigo em Inglês | MEDLINE | ID: mdl-14979527

RESUMO

The possibilities and limitations of supercritical fluid extraction of natural products of low, medium and high polarity under very high pressure and with polar modifiers has been investigated. The medicinal herbs marigold (Calendula officinalis), hawthorn (Crataegus sp.) and chamomile (Matricaria recutita) were used as models in this study. Extraction profiles and the spectra of extractable metabolites were recorded following extraction with mixtures of carbon dioxide:ethanol of varying proportions (0-20% ethanol) and at various pressures in the range 300-689 bar. Components were identified by HPLC-PAD-MS or GC-MS and quantified by HPLC or GC as appropriate. Extraction yields under the varying conditions depended to a large extent on the profiles of secondary metabolites present in the three drugs. Whereas the extractability of lipophilic compounds increased substantially at pressures above 300 bar, the yields of polyphenolic and glycosidic compounds remained low even at 689 bar and with 20% modifier in the extraction fluid.


Assuntos
Calendula/química , Camomila/química , Cromatografia com Fluido Supercrítico/métodos , Crataegus/química , Etanol/química , Plantas Medicinais/química , Dióxido de Carbono/química , Cromatografia Líquida de Alta Pressão , Flores/química , Reprodutibilidade dos Testes
16.
J Ethnopharmacol ; 89(2-3): 251-60, 2003 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-14611888

RESUMO

A selection of 32 fungal strains, belonging to 8 genera of entomopathogenic Deuteromycetes collected in various provinces of China, were screened for activities on targets involved in degenerative diseases of the central nervous system. The strains were grown under various fermentation conditions, and a total of 256 different extracts were obtained. The bioassays included functional screens for NMDA antagonistic activity in stably transfected fibroblasts, for neuritogenic activities in PC-12 cells, and tests for MAO inhibitory and radical scavenging properties. Several extracts with promising activities were identified. Some Paecilomyces extracts induced pronounced axonal-like outgrowths in PC-12 cells. In Paecilomyces militaris RCEF 0095, the neuritogenic activity could be linked to yellow pigments. Three Beauveria and Paecilomyces strains showed radical scavenging properties, which could be localized in the extract by a bioautographic assay on TLC. An extract obtained from the mycelium of Paecilomyces tenuipes RCEF 0275 showed moderate MAO inhibitory activity, whereas extracts of Sporothrix chondracris RCEF 0187 antagonized NMDA receptor mediated cell toxicity.


Assuntos
Antifúngicos/uso terapêutico , Fármacos do Sistema Nervoso Central/uso terapêutico , Doenças do Sistema Nervoso Central/tratamento farmacológico , Fungos Mitospóricos/metabolismo , Animais , Sobrevivência Celular , Células Cultivadas , Cromatografia em Camada Fina , Avaliação Pré-Clínica de Medicamentos , Fermentação , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Sequestradores de Radicais Livres/uso terapêutico , Mitocôndrias Hepáticas/metabolismo , Monoaminoxidase/metabolismo , Ratos
17.
Fitoterapia ; 74(4): 328-38, 2003 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-12781802

RESUMO

A method for the efficient preparative purification of faradiol 3-O-laurate, palmitate and myristate, the major anti-inflammatory triterpenoid esters in the flower heads of the medicinal plant Calendula officinalis has been developed. Gram quantities of the individual compounds were obtained with 96 to 98% purity by a combination of supercritical fluid extraction (SFE), normal-phase and reversed-phase column chromatography. During the work-up of the faradiol esters, accompanying minor compounds of the triterpene ester fraction were purified and identified by spectroscopic means as maniladiol 3-O-laurate and myristate.


Assuntos
Anti-Inflamatórios/química , Calendula , Fitoterapia , Extratos Vegetais/química , Triterpenos/química , Cromatografia Líquida de Alta Pressão , Ésteres/química , Topos Floridos , Humanos
18.
Phytother Res ; 17(4): 385-90, 2003 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-12722146

RESUMO

Petroleum ether, acetone, 80% MeOH and water extracts of crown gall, a plant tumour, obtained from Eucalyptus globulus tree were screened for cytotoxic, antioxidant, antiinflammatory, embryotoxic, antitumour-promoting and antimicrobial activities. In terms of bioactivity the 80% MeOH extract was most effective followed by the acetone extract. The petroleum ether extract showed weak to moderate cytotoxic activity in dose-dependent manner against PC12 cells, mouse L fibroblasts and 1321N1 glia cells, whereas the hydroalcohol extract had no or a weak cytotoxic effect. The 80% MeOH extract exhibited strong antioxidant activity. Based on the in vitro HET-CAM assay all the extracts were effective against inflammation. The extracts did not show any embryotoxic effect at the concentrations tested. Antitumour-promoting activity (100% inhibition; 100 microg/mL) was observed in the 80% MeOH and acetone extracts. In the antimicrobial screening all extracts displayed predominantly antifungal activity against Candida sp. The extracts also showed various levels of antibacterial activity against E. faecalis, Ps. aeruginosa, Bac. subtilis and Staph. epidermidis. From the results of the investigations it can be concluded that crown gall is a valuable plant tumour tissue having interesting biological activities.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Tumores de Planta , Animais , Antibacterianos , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/uso terapêutico , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/uso terapêutico , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/uso terapêutico , Antioxidantes/administração & dosagem , Antioxidantes/uso terapêutico , Bactérias/efeitos dos fármacos , Compostos de Bifenilo , Candida/efeitos dos fármacos , Bovinos , Linhagem Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Eucalyptus , Fibroblastos/efeitos dos fármacos , Humanos , Peroxidação de Lipídeos/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana , Neuroglia/efeitos dos fármacos , Óvulo/efeitos dos fármacos , Picratos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Células Tumorais Cultivadas/efeitos dos fármacos
20.
Planta Med ; 67(5): 411-6, 2001 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-11488453

RESUMO

Various extracts prepared from the traditional dye and medicinal plant Isatis tinctoria L. were submitted to a broad in vitro screening against 16 anti-inflammatory targets. Dichloromethane (DCM) extracts from dried leaves showed a marked cyclooxygenase (COX) inhibitory activity with a preferential effect on COX-2 catalysed prostaglandin synthesis. A supercritical fluid extraction (SFE) procedure employing CO2-modifier mixtures was developed by which the bioactivity profile and chromatographic fingerprint of the DCM extract could be reproduced. High-resolution activity directed on-line identification of the COX-2 inhibitory principle, using a combination of LC-DAD-MS with a microtitre-based bioassay, led to the identification of tryptanthrin (1) as the constituent responsible for essentially all COX-2 inhibitory activity in the crude extract. Following on-line identification, 1 was isolated at preparative scale and its structure confirmed by comparison with synthetic tryptanthrin. In an assay with lipopolysaccharide stimulated Mono Mac 6 cells, tryptanthrin (1) was of comparable potency (IC50 = 64 nM) than the preferential COX-2 inhibitors nimesulide (IC50 = 39 nM) and NS 398 (IC50 = 2 nM). The SFE extract and 1 showed no cytotoxicity in Mono Mac 6 and RAW 264.7 cells when tested at 100 microg/ml and 10 microM, respectively.


Assuntos
Anti-Inflamatórios/farmacologia , Brassicaceae/química , Inibidores de Ciclo-Oxigenase/isolamento & purificação , Inibidores Enzimáticos/isolamento & purificação , Isoenzimas/antagonistas & inibidores , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Células , Corantes , Ciclo-Oxigenase 2 , Inibidores de Ciclo-Oxigenase 2 , Inibidores de Ciclo-Oxigenase/farmacologia , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas , Inibidores Enzimáticos/farmacologia , Isoenzimas/metabolismo , Estrutura Molecular , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Raízes de Plantas/química , Prostaglandina-Endoperóxido Sintases/metabolismo , Quinazolinas/síntese química , Quinazolinas/farmacologia
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