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1.
Chem Phys Lipids ; 240: 105137, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34529978

RESUMO

Flavonoids are a huge class of polyphenolic compounds ubiquitous in higher plants, in most food and beverages of natural origin. They could be considered as dietary phenols, which exert many health-promoting effects on human and animal physiology with a wide range of biomedical and nutritional functions such as activation or inhibition of enzymes like lipoxygenase and cyclooxygenase, the detoxification of carcinogens and chemoprevention. From a chemical point of view, these aromatic compounds can be divided in six subgroups depending on the position of aromatic B ring on C ring, the degree of unsaturation and oxidation, the position of hydroxyl groups and their functionalization. Between flavonoids, the prenylated ones represent a unique class occurring in nature where the C-prenylation is the most common, whereas O-prenylation is rarely present. The presence of this lipophilic functional group in different positions on the scaffold of flavonoids can sometimes lead to relevant changes in their biological activity due to an increased bioavailability. Capitalizing on the restricted incidence in nature of prenylated flavonoids, we have assessed the synthesis of C- and O-prenylated derivatives starting from two flavonoids, quercetin and artemetin, aimed at the exploration of structure-activity relationships. Results showed that prenylation significantly increased the cytotoxic effect of flavonoids in cancer HeLa cells, also improving their capacity to affect cell phospholipid and fatty acid composition. A marked cell bioavailability increase was demonstrated for the artemetin C-prenylated derivative.

2.
Minerva Med ; 2021 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-34180638

RESUMO

AIM: The aim of this study was the evaluation of the combination of Pycnogenol® (150 mg/day) and Centella asiatica (Centellicum® 3 x 225 mg/day) (PY-CE) for 8 months in subjects with sequelae of idiopathic interstitial pneumonia (IIP). Recently, post-COVID-19 lung disease is emerging with large numbers of patients left with chronic lung conditions. Considering the antifibrotic activity of the combination PY-CE, we also tested this supplementary management in post-COVID-19 lung patients. RESULTS: 19 subjects with idiopathic interstitial pneumonia (IIP) were included in the study. High Resolution CT scans at inclusion confirmed the presence of lung fibrosis: 10 patients were treated with the Pycnogenol® Centellicum® combination and 9 subjects with standard management (SM) served as controls. Oxidative stress that was very high in all subjects at inclusion, decreased significantly in the supplement group (p<0.05). The Karnofsky performance scale index significantly improved in the supplement group in comparison with controls (p<0.05). The symptoms (fatigue, muscular pain, dyspnea) were significantly lower after 8 months in supplemented patients (p<0.05) as compared with controls. At the end of the study, the small cystic lesions (honeycombing) and traction bronchiectasis were stable or in partial regression in 4 subjects in the supplemented group (vs none in the control group) with a significant improvement in tissue edema in the supplemented subjects. On ultrasound lung scans the white (more echogenic) fibrotic component at inclusion was 18.5±2.2% in the images in controls vs 19.4±2.7% in the supplement group. At the end of the study, there was no improvement in controls (18.9±2.5%) vs a significant improvement in supplemented subjects (16.2±2.1%; p<0.05). In addition, 18 subjects with post-COVID-19 lung disease were included in the study; 10 patients were treated with the Pycnogenol® Centellicum® combination and evaluated after 4 weeks; 8 patients served as controls. Preliminary results show that symptoms associated with post-COVID-19 lung disease after 4 weeks were significantly improved with the supplement combination (p<0.05). Oxidative stress and the Karnofsky performance scale index scale were significantly improved in the supplements group as compared with controls (p<0.05). CONCLUSIONS: According to these observations, Pycnogenol® controls and decreases edema in several conditions and Centellicum® - modulating the apposition of collagen - modulates the development of irregular cicatrization, keloidal scarring and fibrosis. More time is needed to evaluate this effect in a larger number of post-COVID-19 patients with lung disease. This disease has affected millions of subjects worldwide, leaving severe consequences. Pycnogenol® and Centellicum® may improve the residual clinical picture in post-COVID-19 lung disease (PCL) patients and may reduce the number of subjects evolving into lung fibrosis. The evolution from edema to fibrosis seems to be slower or attenuated with this supplement combination both in Idiopathic pulmonary fibrosis (IPF) and in PCL patients.

3.
Antioxidants (Basel) ; 10(2)2021 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-33498213

RESUMO

The aim of the study is to compare the qualitative and semi-quantitative profile of the polyphenol fraction purified from the leaf (BLPF) and fruit (BFPF) of bergamot (Citrus bergamia), and to evaluate their antioxidant and anti-inflammatory activity. The analytical qualitative profile was carried out by LC-ESI/MS using three different approaches: targeted (searching analytes already reported in bergamot extract), semi-targeted (a selective search of 3-hydroxy-3-methylglutarate [HMG] derivatives involved in the cholesterol reducing activity of BPF) and untargeted. A total number of 108 compounds were identified by using the three approaches, 100 of which are present in both the extracts thus demonstrating a good qualitative overlapping of polyphenols between the two extracts. The antioxidant activity was higher for BLPF in respect to BFPF but when normalized in respect to the polyphenol content they were almost overlapping. Both the extracts were found to dose dependently inhibit cell inflammation stimulated with IL-1α. In conclusion, the comparison of the qualitative and quantitative profile of polyphenols as well as of the antioxidant and anti-inflammatory activity of bergamot leaf and fruit well indicates that leaf is a valid source of bergamot polyphenol extraction and an even richer source of polyphenol in respect to the fruit.

4.
Molecules ; 25(23)2020 Dec 07.
Artigo em Inglês | MEDLINE | ID: mdl-33297504

RESUMO

The employment studies of natural extracts in the prevention and treatment of several diseases highlighted the role of different species of genus Ferula L., belonging to the Apiaceae family, dicotyledonous plants present in many temperate zones of our planet. Ferula communis L. is the main source of sesquiterpene ferutinin, a bioactive compound studied both in vitro and in vivo, because of different effects, such as phytoestrogenic, antioxidant, anti-inflammatory, but also antiproliferative and cytotoxic activity, performed in a dose-dependent and cell-dependent way. The present review will focus on the molecular mechanisms involved in the different activities of Ferutinin, starting from its antioxidant potential at low doses until its ionophoric property and the subsequent mitochondrial dysfunction induced through administration of high doses, which represent the key point of its anticancer action. Furthermore, we will summarize the data acquired from some experimental studies on different cell types and on several diseases. The results obtained showed an important antioxidant and phytoestrogenic regulation with lack of typical side effects related to estrogenic therapy. The preferential cell death induction for tumor cell lines suggests that ferutinin may have anti-neoplastic properties, and may be used as an antiproliferative and cytotoxic agent in an estrogen dependent and independent manner. Nevertheless, more data are needed to clearly understand the effect of ferutinin in animals before using it as a phytoestrogen or anticancer drug.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Benzoatos/farmacologia , Cicloeptanos/farmacologia , Ferula/química , Extratos Vegetais/farmacologia , Sesquiterpenos/farmacologia , Antineoplásicos/química , Antineoplásicos/uso terapêutico , Antioxidantes/química , Antioxidantes/uso terapêutico , Apoptose/efeitos dos fármacos , Benzoatos/química , Benzoatos/uso terapêutico , Compostos Bicíclicos com Pontes/química , Compostos Bicíclicos com Pontes/farmacologia , Compostos Bicíclicos com Pontes/uso terapêutico , Linhagem Celular Tumoral , Cicloeptanos/química , Cicloeptanos/uso terapêutico , Relação Dose-Resposta a Droga , Transporte de Elétrons/efeitos dos fármacos , Terapia de Reposição Hormonal , Humanos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Fitoestrógenos/química , Fitoestrógenos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Espécies Reativas de Oxigênio/metabolismo , Sesquiterpenos/química , Sesquiterpenos/uso terapêutico
5.
Artigo em Inglês | MEDLINE | ID: mdl-32849284

RESUMO

Background: Non-alcoholic fatty liver disease is the most common cause of liver-related morbidity and mortality in the world. However, no effective pharmacological treatment for this condition has been found. Purpose: This study evaluated the effect of a nutraceutical containing bioactive components from Bergamot citrus and wild cardoon as a treatment for individuals with fatty liver disease. The primary outcome measure was the change in liver fat content. Methods: A total of 102 patients with liver steatosis were enrolled in a double-blind placebo controlled clinical trial. The intervention group received a nutraceutical containing a Bergamot polyphenol fraction and Cynara Cardunculus extract, 300 mg/day for 12 weeks. The control group received a placebo daily. Liver fat content, by transient elastography, serum transaminases, lipids and glucose were measured at the baseline and the end of the study. Results: We found a greater liver fat content reduction in the participants taking the nutraceutical rather than placebo (-48.2 ± 39 vs. -26.9 ± 43 dB/m, p = 0.02); The percentage CAP score reduction was statistically significant in those with android obesity, overweight/obesity as well as in women. However, after adjustment for weight change, the percentage CAP score reduction was statistically significant only in those over 50 years (44 vs. 78% in placebo and nutraceutical, respectively, p = 0.007). Conclusions: This specific nutraceutical containing bioactive components from Bergamot and wild cardoon reduced the liver fat content during 12 weeks in individuals with liver steatosis over 50 years. If confirmed, this nutraceutical could become the cornerstone treatment of patients affected by liver steatosis. Clinical Trial Registration: www.isrctn.com, identifier ISRCTN12833814.


Assuntos
Peso Corporal , Citrus/química , Cynara/química , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Obesidade/fisiopatologia , Sobrepeso/fisiopatologia , Extratos Vegetais/uso terapêutico , Adulto , Idoso , Método Duplo-Cego , Feminino , Humanos , Itália/epidemiologia , Masculino , Pessoa de Meia-Idade , Hepatopatia Gordurosa não Alcoólica/epidemiologia , Hepatopatia Gordurosa não Alcoólica/patologia , Fitoterapia
6.
J Tradit Complement Med ; 10(3): 268-274, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32670822

RESUMO

Background and aim: Non-Alcoholic Fatty Liver Disease (NAFLD) represents a risk factor for cardiovascular diseases. NAFLD is worsened by the simultaneous occurrence of type 2 diabetes mellitus (T2DM) causing an enhancement of inflammatory and fibrotic processes. Although insulin resistance appears the link between NAFLD and T2DM, current pharmacological treatments of T2DM failed to produce relevant benefits in preventing T2DM-related liver dysfunction. In this randomized, double blind, placebo-controlled clinical study, we evaluated the effect of Bergacyn, an innovative formulation originating from the combination of Bergamot Polyphenolic Fraction (BPF) and Cynara cardunculus (CyC). Experimental procedure: 80 adult patients with a history of at least 12 months of T2DM and NAFLD received orally BPF (300 mg/daily) Cyc (300 mg/daily), separately or formulated in combination 50/50% (Bergacyn; 300 mg/daily), or placebo all containing 300 mg of bergamot albedo fibers micronized and co-grinded as excipients. Results and conclusion: Serum measurements and liver ultrasound analyses showed that concomitant administration of BPF and CyC produced significant improvement of NAFLD biomarkers in patients with T2DM. This effect was associated with a substantial reduction of oxidative stress/inflammatory biomarkers, thus contributing to a significant improvement of NO-mediated reactive vasodilation. Furthermore, the effect of Bergacyn showed a synergistic effect of both extracts, thus suggesting that this peculiar formulation represents a novel therapeutic strategy to counteract vascular inflammation and endothelial dysfunction in patients suffering from T2DM and NAFLD. Further studies in larger cohort of diabetic patients are required to better identify the potential of Bergacyn on metabolic disorders accompanying T2DM and NAFLD.

7.
Nutrients ; 12(5)2020 May 21.
Artigo em Inglês | MEDLINE | ID: mdl-32455840

RESUMO

Metabolic syndrome (MetS) represents a set of clinical findings that include visceral adiposity, insulin-resistance, high triglycerides (TG), low high-density lipoprotein cholesterol (HDL-C) levels and hypertension, which is linked to an increased risk of developing type 2 diabetes mellitus (T2DM) and atherosclerotic cardiovascular disease (ASCVD). The pathogenesis of MetS involves both genetic and acquired factors triggering oxidative stress, cellular dysfunction and systemic inflammation process mainly responsible for the pathophysiological mechanism. In recent years, MetS has gained importance due to the exponential increase in obesity worldwide. However, at present, it remains underdiagnosed and undertreated. The present review will summarize the pathogenesis of MetS and the existing pharmacological therapies currently used and focus attention on the beneficial effects of natural compounds to reduce the risk and progression of MetS. In this regard, emerging evidence suggests a potential protective role of bergamot extracts, in particular bergamot flavonoids, in the management of different features of MetS, due to their pleiotropic anti-oxidative, anti-inflammatory and lipid-lowering effects.


Assuntos
Antioxidantes/farmacologia , Citrus/química , Síndrome Metabólica/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Humanos , Hipoglicemiantes/farmacologia , Resistência à Insulina , Obesidade/tratamento farmacológico , Obesidade Abdominal/tratamento farmacológico , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/uso terapêutico
8.
Nutrients ; 12(5)2020 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-32429274

RESUMO

Hyperlipidemia and insulin-resistance are often associated with Non-Alcoholic Fatty Liver Disease (NAFLD) thereby representing a true issue worldwide due to increased risk of developing cardiovascular and systemic disorders. Although clear evidence suggests that circulating fatty acids contribute to pathophysiological mechanisms underlying NAFLD and hyperlipidemia, further studies are required to better identify potential beneficial approaches for counteracting such a disease. Recently, several artichoke extracts have been used for both reducing hyperlipidemia, insulin-resistance and NAFLD, though the mechanism is unclear. Here we used a wild type of Cynara Cardunculus extract (CyC), rich in sesquiterpens and antioxidant active ingredients, in rats fed a High Fat Diet (HFD) compared to a Normal Fat Diet (NFD). In particular, in rats fed HFD for four consecutive weeks, we found a significant increase of serum cholesterol, triglyceride and serum glucose. This effect was accompanied by increased body weight and by histopathological features of liver steatosis. The alterations of metabolic parameters found in HFDs were antagonised dose-dependently by daily oral supplementation of rats with CyC 10 and 20 mg/kg over four weeks, an effect associated to significant improvement of liver steatosis. The effect of CyC (20 mg/kg) was also associated to enhanced expression of both OCTN1 and OCTN2 carnitine-linked transporters. Thus, present data suggest a contribution of carnitine system in the protective effect of CyC in diet-induced hyperlipidemia, insulin-resistance and NAFLD.


Assuntos
Cynara , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Proteínas de Transporte de Cátions Orgânicos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Membro 5 da Família 22 de Carreadores de Soluto/efeitos dos fármacos , Simportadores/efeitos dos fármacos , Animais , Glicemia/efeitos dos fármacos , Colesterol/sangue , Dieta Hiperlipídica/efeitos adversos , Suplementos Nutricionais , Hiperlipidemias/sangue , Hiperlipidemias/tratamento farmacológico , Hiperlipidemias/etiologia , Resistência à Insulina , Masculino , Hepatopatia Gordurosa não Alcoólica/sangue , Hepatopatia Gordurosa não Alcoólica/etiologia , Ratos , Ratos Sprague-Dawley , Triglicerídeos/sangue
9.
Artigo em Inglês | MEDLINE | ID: mdl-30501605

RESUMO

OBJECTIVE: Hyperlipemia represents an independent risk factor in the development of atherosclerosis in patients undergoing type 2 diabetes mellitus (DM). Moreover, the pharmacological treatment of dyslipemia in patients undergoing type 2 DM (e.g. by means of statins), is accompanied by relevant side effects and oral supplementation with natural antioxidants, such as Citrus polyphenols, has recently been suggested to improve cardioprotection in such patients. However, due to the poor gastrointestinal absorption of polyphenols, novel formulations have recently been developed for getting a better bioavailability of polyphenolic rich fractions of citrus species extract rich in polyphenols. METHODS: Here, we investigated the effect of standard bergamot polyphenolic fraction (BPF®) as well as of its phytosomal formulation (BPF Phyto), in patients with type 2 DM and hyperlipemia. A randomized, double blind, placebo-controlled study was carried out in 60 patients suffering from type 2 DM and mixed hyperlipemia. Patients were divided into three groups: one receiving placebo, the second receiving standard BPF and the third BPF Phyto. RESULTS: In the groups receiving BPF and BPF Phyto, a significant reduction of fasting plasma glucose, serum LDL cholesterol and triglycerides accompanied by increased HDL cholesterol was observed. This effect was associated with significant reduction of small dense atherogenic LDL particles, as detected by means of proton NMR Spectroscopy, thus confirming the hypolipemic and hypoglycemic effect of bergamot extract both when using standard formulation as well as BPF Phyto. No differences were seen in the therapeutic response among groups receiving BPF and BPF Phyto, thus suggesting a substantial bioequivalence in their hypoglycemic and hypolipemic profile. However, when comparing the pharmacokinetic profile of naringin (the major component of BPF) and its metabolites, in patients treated with BPF Phyto, an at least 2,5 fold increase in its absorption was found, confirming in human studies the better profile of BPF Phyto compared to standard BPF. CONCLUSION: These data suggest that better absorption and tissue distribution of BPF Phyto formulation represents an innovative approach in supplementation treatments of cardiometabolic disorders.


Assuntos
Citrus/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hiperlipidemias/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Hipolipemiantes/uso terapêutico , Lecitinas/uso terapêutico , Extratos Vegetais/uso terapêutico , Adulto , Fracionamento Químico , Colesterol , Diabetes Mellitus Tipo 2/complicações , Diabetes Mellitus Tipo 2/metabolismo , Método Duplo-Cego , Composição de Medicamentos , Feminino , Humanos , Hiperglicemia/tratamento farmacológico , Hiperglicemia/etiologia , Hiperglicemia/metabolismo , Hiperlipidemias/etiologia , Hiperlipidemias/metabolismo , Lecitinas/farmacocinética , Masculino , Pessoa de Meia-Idade , Placebos , Extratos Vegetais/química , Extratos Vegetais/farmacocinética , Óleos Vegetais/administração & dosagem , Óleos Vegetais/química , Polifenóis/administração & dosagem , Polifenóis/isolamento & purificação , Polifenóis/farmacocinética , Polifenóis/uso terapêutico
10.
Artigo em Inglês | MEDLINE | ID: mdl-25954317

RESUMO

Objective. Functional dyspepsia (FD) is a frequent clinical finding in western world. The aim of this study is to compare the efficacy of a ginger and artichoke supplementation versus placebo in the treatment of FD. Methods. A prospective multicentre, double blind, randomized, placebo controlled, parallel-group comparison of the supplement and placebo over a period of 4 weeks was performed. Two capsules/day were supplied (before lunch and dinner) to 126 FD patients (supplementation/placebo: 65/61). Results. After 14 days of treatment, only supplementation group (SG) showed a significant amelioration (SG: α S = +1.195 MCA score units (u), P = 0.017; placebo: α P = +0.347 u, P = 0.513). The intercept (α) resulted to be significantly higher in SG than in placebo (α S - α P = +0.848 u, P < 0.001). At the end of the study, the advantage of SG versus placebo persists without variation (ß S - ß P = +0.077 u, P = 0.542). In SG, a significant advantage is observed for nausea (ß S - ß P = -0.398 u, P < 0.001), epigastric fullness (ß S - ß P = -0.241, P < 0.001), epigastric pain (ß S - ß P = -0.173 u, P = 0.002), and bloating (ß S - ß P = -0.167 u, P = 0.017). Conclusions. The association between ginger and artichoke leaf extracts appears safe and efficacious in the treatment of FD and could represent a promising treatment for this disease.

11.
Anticancer Agents Med Chem ; 14(10): 1397-1401, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25173557

RESUMO

Hyperforin is a natural phloroglucinol that has been know for the treatment of depression. Hyperforin displays also antibacterial, antiproliferant and antiangiogenic activity. Synthetic derivatives of hyperforin have also recently been reported to possess increased bioactivity. The clinical applications are limited by the hydrophobic characteristics and the instability of the molecule. In this review we discuss about some of the derivatives of hyperforin (aristoforin, tetrahydrohyperforin and octahydrohyperforin) that demonstrated promising antitumor activity. Among these, octahydrohyperforin also possesses antibacterial activity against both the planktonic and biofilm states of bacteria.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Floroglucinol/análogos & derivados , Terpenos/farmacologia , Animais , Linhagem Celular Tumoral , Humanos , Hypericum/química , Floroglucinol/farmacologia , Fármacos Fotossensibilizantes/farmacologia
12.
Phytother Res ; 28(1): 33-41, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-23440660

RESUMO

The aim of this study is to evaluate the efficacy of a dietary supplementation with an extract from Cynara scolymus (Cs) on the glucose pattern in a group of patients with naïve impaired fasting glycaemia (IFG). A randomized, double-blind, placebo-controlled trial has been performed in 55 overweight subjects with IFG (fasting blood glucose [FBG]: 6.11 ± 0.56 mmol/l). These subjects were randomly assigned to supplement their diet with either an extract from Cs (600 mg/d) (26 subjects) or placebo (29 matched subjects) for 8 weeks. The decrease of FBG was the primary endpoint. The assessment of Homeostatic Metabolic Assessment (HOMA), glycosylated haemoglobin, A1c-Derived Average Glucose (ADAG), lipidic pattern and anthropometric parameters were the secondary endpoints. The within groups and percent changes from baseline were analyzed by the signed rank test. The comparison between groups was performed by Wilcoxon's two sample test. The supplemented group had significant decreases of: FBG (-9.6%), HOMA (-11.7%), glycosylated haemoglobin (-2.3%), ADAG (-3.1%) and lipidic pattern. The placebo group did not show any significant difference. Compared with the placebo, the supplemented group showed a significant difference in FBG, HOMA and lipidic pattern. These data demonstrate the efficacy of Cs extract on the reduction of glycometabolic parameters in overweight subjects with IFG.


Assuntos
Glicemia/análise , Cynara scolymus/química , Suplementos Nutricionais , Hiperglicemia/tratamento farmacológico , Sobrepeso/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Adulto , Antropometria , Colesterol/sangue , Método Duplo-Cego , Feminino , Hemoglobina A Glicada/metabolismo , Humanos , Hiperglicemia/fisiopatologia , Masculino , Pessoa de Meia-Idade , Triglicerídeos/sangue , Adulto Jovem
13.
Future Oncol ; 9(11): 1717-25, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24156331

RESUMO

SAMITAL(®) (Indena SpA, Milan, Italy) is a new multicomponent and multiacting botanical formulation rationally designed for the relief of oral mucositis induced by chemotherapy and/or radiotherapy in oncological patients. Each of the individual botanical constituents of SAMITAL-standardized extracts of Vaccinium myrtillus, Macleaya cordata and Echinacea angustifolia have a long history of clinical use that corroborates their safety and activity in SAMITAL. A number of pilot trials in oncological patients demonstrated that SAMITAL has good clinical efficacy and tolerability as evidenced by its significant effects in terms of reduction of mucositis, pain and a general improvement in patient quality of life. Importantly, the use of this botanical formulation had the added benefit that patients were able to complete their chemotherapy/radiotherapy regimen. Phase II trials with SAMITAL as part of an overall clinical development program are currently ongoing in Italy and are planned in the USA.


Assuntos
Antineoplásicos/efeitos adversos , Mucosite/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Lesões por Radiação/tratamento farmacológico , Animais , Antineoplásicos/uso terapêutico , Ensaios Clínicos como Assunto , Neoplasias de Cabeça e Pescoço/tratamento farmacológico , Neoplasias de Cabeça e Pescoço/radioterapia , Humanos , Mucosite/induzido quimicamente , Qualidade de Vida
14.
Future Oncol ; 9(11): 1727-32, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24156332

RESUMO

AIM: We sought to evaluate the efficacy and safety of SAMITAL(®) (Indena SpA, Milan, Italy), a highly standardized botanical formulation, in reducing mucositis in patients undergoing treatment for hematological malignancies. PATIENTS & METHODS: In this observational, uncontrolled study, a total of 25 consecutively enrolled patients (19 males, aged 18-74 years) with chemotherapy-induced mucositis were compassionately treated orally with SAMITAL (three to four times per day) for 4-22 days per cycle. RESULTS: Patients demonstrated clinically relevant reductions in WHO mucositis grade with a reduction in pain, mucosal erosions, bleeding, dysphagia/feeding impairment and improvements in quality of life. SAMITAL was well tolerated and no local or systemic pharmacological, allergic, toxic or synergistic/antagonistic side effects were reported. Of note, SAMITAL also showed efficacy when administered prophylactically. CONCLUSION: These results add weight to previous experiences with SAMITAL. However, randomized, placebo-controlled clinical trials will need to confirm the suitability of SAMITAL for use in the treatment of mucositis.


Assuntos
Antineoplásicos/efeitos adversos , Mucosite/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Antineoplásicos/uso terapêutico , Feminino , Humanos , Leucemia/tratamento farmacológico , Linfoma/tratamento farmacológico , Masculino , Pessoa de Meia-Idade , Mucosite/induzido quimicamente , Adulto Jovem
15.
J Nat Prod ; 76(9): 1819-23, 2013 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-23981190

RESUMO

Bacterial biofilms are organized communities of microorganisms, embedded in a self-produced matrix, growing on a biotic surface and resistant to many antimicrobial agents when associated with a medical device. These biofilms require the development of new strategies for the prevention and treatment of infectious disease, including the potential use of natural products. One interesting natural product example is Hypericum, a plant genus that contains species known to have antimicrobial properties. The major constituent of Hypericum perforatum is an unstable compound named hyperforin (1); for this reason it was not believed to play a significant role in the pharmacological effects. In this investigation a hydrogenated hyperforin analogue (2) was tested on several ATCC and clinical isolate strains, in their planktonic and biofilm form (Staphylococcus aureus, MRSA, and Enterococcus faecalis). Compound 2 was effective against planktonic and biofilm cultures, probably due to higher stability, showing the percentage of cells killed in the range from 45% to 52%. These results are noteworthy from the point of view of future development of these polyprenylated phloroglucinols as potential antibiotics.


Assuntos
Biofilmes/efeitos dos fármacos , Floroglucinol/análogos & derivados , Terpenos/farmacologia , Biofilmes/crescimento & desenvolvimento , Enterococcus faecalis/efeitos dos fármacos , Hypericum/química , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Floroglucinol/farmacologia , Staphylococcus aureus/efeitos dos fármacos
16.
Phytother Res ; 27(6): 944-7, 2013 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22899449

RESUMO

Treatment with a rational combination of standardized extracts of Phaseolus vulgaris and Cynara scolymus reduced food intake and glycemia in rats. The present study was designed to assess the effect of this extract combination and of each single extract in an experimental model of food craving, made up of rats displaying exaggerated seeking and taking behaviors for a chocolate-flavoured beverage. After training to lever-respond for the chocolate-flavoured beverage, rats were treated with vehicle, Phaseolus vulgaris extract alone (200 mg/kg), Cynara scolymus extract alone (400 mg/kg), or combination of Phaseolus vulgaris (200 mg/kg) and Cynara scolymus (400 mg/kg) extracts. The Phaseolus vulgaris extract and the extract combination exerted similar and substantial decrements in the number of lever-responses and amount of self-administered chocolate-flavoured beverage; conversely, the Cynara scolymus extract was totally ineffective. These results suggest that (i) the capacity of the extract combination to reduce the self-administration of the chocolate-flavoured beverage entirely relied on the Phaseolus vulgaris extract, (ii) Phaseolus vulgaris extract may interfere with the mechanisms regulating food-related addictive-like behaviors, and (iii) combinations of Phaseolus vulgaris and Cynara scolymus extracts may possess a broad spectrum of activities, from treatment of metabolic syndrome to overweight, obesity, and possibly food-related addictive disorders.


Assuntos
Cynara scolymus/química , Ingestão de Alimentos/efeitos dos fármacos , Phaseolus/química , Extratos Vegetais/farmacologia , Animais , Bebidas , Cacau , Ratos , Ratos Wistar , Autoadministração
17.
Fitoterapia ; 85: 14-9, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-23262270

RESUMO

Different lines of experimental evidence indicate that treatment with extracts from and derivatives of Phaseolus vulgaris reduces intake of food, including highly palatable foods and beverages, in rats. The present study was designed to extend to mice these lines of evidence. To this end, CD1 mice were treated acutely with a standardized extract of P. vulgaris and then exposed to unlimited access to regular food pellets (Experiment 1) or 1-hour limited access to three different palatable foods/beverages, such as butter cookies (Experiment 2), a condensed-milk beverage (Experiment 3), and a chocolate-flavored beverage (Experiment 4). Treatment with P. vulgaris extract resulted in a significant reduction in the intake of regular food pellets, that was still evident 24h later, as well as of the three palatable nourishments. Together, these results (a) extend to mice several previous findings on the capacity of P. vulgaris extracts to suppress food intake in rats, (b) suggest that P. vulgaris extracts may interfere with the central mechanisms regulating appetite, food intake, palatability, and/or the rewarding and hedonic properties of food, and (c) P. vulgaris extracts may represent a potentially effective therapy for overeating, obesity, and food craving.


Assuntos
Depressores do Apetite/análise , Ingestão de Alimentos/efeitos dos fármacos , Hiperfagia/tratamento farmacológico , Phaseolus/química , Extratos Vegetais/uso terapêutico , Animais , Bebidas , Cacau , Avaliação Pré-Clínica de Medicamentos , Alimentos , Masculino , Camundongos , Fitoterapia , Extratos Vegetais/farmacologia
18.
Int J Food Sci Nutr ; 64(1): 7-15, 2013 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-22746542

RESUMO

The aim of this study was to evaluate the effects of artichoke leaf extract (ALE) supplementation (250 mg, 2 b.i.d.) on the lipid pattern. A randomized, double-blind, placebo-controlled clinical trial was performed on 92 overweight subjects with primary mild hypercholesterolaemia for 8 weeks. Forty-six subjects were randomized to supplementation (age: 54.2 ± 6.6 years, body mass index (BMI): 25.8 ± 3.9 kg/m(2), male/female: 20/26) and 46 subjects to placebo (age: 53.8 ± 9.0 years, BMI: 24.8 ± 1.6 kg/m(2), male/female: 21/25). Verum supplementation was associated with a significant increase in mean high-density lipoprotein (HDL)-cholesterol (p < 0.001) and in mean change in HDL-cholesterol (HDL-C) (p = 0.004). A significantly decreased difference was also found for the mean change in total cholesterol (p = 0.033), low-density lipoprotein (LDL)-cholesterol (p < 0.001), total cholesterol/HDL ratio (p < 0.001) and LDL/HDL ratio (p < 0.001), when verum and placebo treatment were compared. These results indicate that ALE could play a relevant role in the management of mild hypercholesterolaemia, favouring in particular the increase in HDL-C, besides decreasing total cholesterol and LDL-cholesterol.


Assuntos
HDL-Colesterol/sangue , Cynara scolymus , Suplementos Nutricionais , Hipercolesterolemia/tratamento farmacológico , Sobrepeso/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Adulto , Colesterol/sangue , LDL-Colesterol/sangue , Método Duplo-Cego , Feminino , Humanos , Hipercolesterolemia/sangue , Hipercolesterolemia/complicações , Masculino , Pessoa de Meia-Idade , Sobrepeso/sangue , Sobrepeso/complicações , Extratos Vegetais/farmacologia , Folhas de Planta
19.
Phytother Res ; 27(2): 258-63, 2013 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-22565861

RESUMO

Extracts from Phaseolus vulgaris and Cynara scolymus may reduce food intake and/or postprandial glycemia. This study investigated the effect of standardized extracts of P. vulgaris and C. scolymus and their combination on food intake and glycemia in rats. P. vulgaris and C. scolymus extracts, and their 1:2 combination, were administered acutely to rats (a) given access to regular food and water, (b) given access to regular food, water, and a chocolate-flavored beverage, or (c) infused with a starch bolus. P. vulgaris extract and the combination produced comparable reductions in intake of regular food and chocolate-flavored beverage; conversely, C. scolymus extract was ineffective on both parameters. P. vulgaris and C. scolymus extracts additively contributed to the reducing effect of the combination on glycemic rise. These results suggest that a mixture of P. vulgaris and C. scolymus extracts is preferable over each single extract, as it combines the anorectic effect of the P. vulgaris extract with the hypoglycemic effect of both extracts. These data support the recent clinical use of the combination of P. vulgaris and C. scolymus extracts in the control of appetite, food intake, and postprandial glycemia and represent a successful example of translational research in the nutraceutical field.


Assuntos
Glicemia/efeitos dos fármacos , Cynara scolymus/química , Ingestão de Alimentos/efeitos dos fármacos , Phaseolus/química , Extratos Vegetais/farmacologia , Animais , Apetite/efeitos dos fármacos , Bebidas , Hipoglicemiantes/farmacologia , Masculino , Ratos , Ratos Wistar
20.
Future Oncol ; 8(11): 1481-6, 2012 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23148620

RESUMO

BACKGROUND: Gastrointestinal mucositis is a common debilitating complication of chemotherapy and one for which there is currently no effective long-term treatment. OBJECTIVES: To report our experience with the use of SAMITAL(®), a new oral suspension formulation based on the combination of three standardized extracts from Vaccinium myrtillus, Macleaya cordata fruits and Echinacea angustifolia roots in the prevention and treatment of chemotherapy-induced gastrointestinal mucositis in pediatric patients. METHODS: 20 pediatric patients undergoing chemotherapy for a range of oncological conditions were followed. Patients initially received oral SAMITAL(®) to treat gastrointestinal mucositis and were then given SAMITAL(®) prophylactically to prevent recurrences with successive cycles of chemotherapy. RESULTS: SAMITAL(®) significantly decreased gastrointestinal mucositis grade after the first episode with a reduction of mean scores from 3.2 ± 0.7 at baseline to 0.4 ± 0.6 at the end of treatment (p < 0.001). SAMITAL(®) reduced pain, mucosal erosions, bleeding and dysphagia/feeding impairment. SAMITAL(®) improved patients' overall condition and quality of life after the first administration and lowered the need for parenteral nutrition. Importantly, it allowed chemotherapy cycles to be continued without complications. CONCLUSION: Results from this case series suggest that SAMITAL(®) may play an important role in the prevention and treatment of chemotherapy-induced gastrointestinal mucositis in children and adolescents and as such warrants investigation in controlled studies.


Assuntos
Antineoplásicos/efeitos adversos , Mucosite/tratamento farmacológico , Mucosite/etiologia , Neoplasias/complicações , Fitoterapia , Extratos Vegetais/uso terapêutico , Adolescente , Antineoplásicos/uso terapêutico , Criança , Pré-Escolar , Feminino , Humanos , Lactente , Masculino , Neoplasias/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Extratos Vegetais/efeitos adversos , Resultado do Tratamento
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