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1.
Plants (Basel) ; 8(11)2019 Oct 26.
Artigo em Inglês | MEDLINE | ID: mdl-31717792

RESUMO

The aim of this study was to validate a HPLC method for the assay of flavonoids in extracts obtained from natural sources, i.e., from Dirmophandra mollis Benth, Ginkgo biloba L., Ruta graveolens L., and Vitis vinífera L. The potential sun protecting effect, antioxidant activity, and cell viability of the extracts were also determined. Individual extracts (obtained from each individual species) and a mixed extract (containing the four extracts) were analyzed by the validated HPLC method for the identification of flavonoids and quantification of rutin and quercetin. An in vitro cell viability study was carried out using the neutral red method. The in vitro sun protection factor was determined by spectral transmittance and in vitro antioxidant efficacy was evaluated against DPPH, ABTS, and AAPH radicals. The HPLC method used for the identification and quantification of flavonoids in extracts exhibited linearity, precision, accuracy, and robustness. Detection and quantification limits were, respectively, 2.881 ± 0.9 µg·mL-1 and 0.864 ± 0.9 µg·mL-1 for quercetin, and 30.09 ± 1 µg·mL-1 and 9.027 ± 1.1 µg·mL-1 for rutin. All extracts did not affect cell viability at the evaluated concentration range and exhibited a sun protection effect and antioxidant activity. Among the evaluated extracts, Ginkgo biloba L. and the mixed extract depicted the most expressive antioxidant activity. The mixed extract exhibited sunscreen protection against ultraviolet A (UVA) and ultraviolet B (UVB) and a critical wavelength of 372.7 ± 0.1. Our results translate the enhanced flavonoids' composition of the mixed extract, which may be a potential alternative over sunscreens and antioxidants in pharmaceutic/cosmetic formulations.

2.
Antioxidants (Basel) ; 8(10)2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31581509

RESUMO

The aim of this study was to develop a phytocosmetic sunscreen emulsion with antioxidant effect, containing a blend of flavonoid-enriched plant extracts. In vitro sun protection factor, antioxidant activity, skin irritation, photostability, cutaneous permeation, and retention of flavonoids were evaluated. Thermodynamically stable emulsions were obtained and tested for sensorial analysis after loading the blend of extracts. The selected emulsion was stable when stored at low temperatures (5 C), for which after 120 days the concentration of quercetin and rutin were above their limit of quantification, i.e., 2.8 ± 0.39 µg/mL and 30.39 ± 0.39 µg/mL, respectively. Spreadability, low rupture strength and adhesiveness were shown to be similar to a conventional topical product. Higher brittleness, pseudo-plastic, and viscoelastic behaviors were also recorded for the developed phytocosmetic sunscreen. The product presented a critical wavelength of 387.0 nm and ultraviolet rays A and B (UVA/UVB) rate of 0.78, confirming that the developed formulation shows capacity for UVA/UVB protection, protecting skin against damages caused by Ultraviolet (UV) radiation. Rutin was shown to permeate the skin barrier and was also quantified in the stratum corneum (3.27 ± 1.92 µg/mL) by tape stripping and retention test (114.68 ± 8.70 µg/mL). The developed flavonoid-enriched phytocosmetic was shown to be non-irritant to skin by an in vitro assay. Our results confirm the antioxidant activity, sun protection, and physical properties of the developed phytocosmetic for topical application.

3.
Mater Sci Eng C Mater Biol Appl ; 100: 493-504, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30948086

RESUMO

Advanced wound dressings capable of interacting with lesions and changing the wound microenvironment to improve healing are promising to increase the therapeutic efficacy of this class of biomaterials. Aiming at the production of bioactive wound dressings with the ability to control the wound microenvironment, biomaterials of three different chemical compositions, but with the same architecture, were produced and compared. Electrospinning was employed to build up a biomimetic extracellular matrix (ECM) layer consisting of poly(caprolactone) (PCL), 50/50 dl-lactide/glycolide copolymer (PDLG) and poly(l-lactide) (PLLA). As a post-treatment to broaden the bioactivity of the dressings, an alginate coating was applied to sheathe and functionalize the surface of the hydrophobic electrospun wound dressings, in combination with the extract of the plant Arrabidaea chica Verlot, known for its anti-inflammatory and healing promotion properties. Wettable bioactive structures capable to interact with media simulating lesion microenvironments, with tensile strength and elongation at break ranging respectively from 155 to 273 MPa and from 0.94 to 1.39% were obtained. In simulated exudative microenvironment, water vapor transmission rate (WVTR) values around 700 g/m2/day were observed, while water vapor permeability rates (WVPR) reached about 300 g/m2/day. In simulated dehydrated microenvironment, values of WVTR around 200 g/m2/day and WVPR around 175 g/m2/day were attained.


Assuntos
Bandagens , Materiais Revestidos Biocompatíveis/farmacologia , Fenômenos Mecânicos , Cicatrização , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Liberação Controlada de Fármacos , Íons , Testes de Sensibilidade Microbiana , Permeabilidade , Extratos Vegetais/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Vapor , Termogravimetria , Fatores de Tempo , Água/química , Difração de Raios X
4.
Biomed Pharmacother ; 112: 108693, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30798128

RESUMO

This study evaluated the pharmacological effect of the association of crude extract from the fruits of Pterodon pubescens (Pp) with the essential oil of Cordia verbenacea (Cv) in antinociception and anti-inflammatory experimental models. The effective doses of each extract and the combinations used in the associations of extracts were defined by acetic acid-induced writhing test. The separate extracts were also evaluated on formalin test. Interaction between extracts was assessed by isobologram method. The effects of different concentrations of associations (A50, A100 and A200) were evaluated on formalin test, tail flick and hot plate. The anti-inflammatory activity was evaluated in paw edema induced by carrageenan and PGE2, carrageenan-induced peritonitis and mechanical allodynia induced by Complete Freund's Adjuvant (CFA). The associations were markedly synergistic, as assessed using isobolographic analyses. On formalin and on acetic acid-induced writhing tests, associations demonstrated greater efficacy when compared to extracts separately. In paw edema models, significant reductions of edema were observed. On mechanical allodynia induced by CFA, associations were effective at acute phase with pronounced effect at chronic phase. The associations were not effective in hot plate, tail flick and carrageenan-induced peritonitis tests. Phytochemical analysis by HPLC-DAD and FID showed important concentrations of α-Humulene, trans-Caryophyllene, geranylgeraniol, isomers 6α-hydroxy-7ß-acetoxy-vouacapan-17ßoate methyl ester and 6α-acetoxy-7ß-hydroxy-vouacapan-17ß-oate methyl ester (compounds m/z 404) and 6α,7ß-dihydroxyvouacapan-17ß-oate methyl ester (m/z 362). These findings demonstrate that the associations promote synergistic antinociceptive effect and important anti-inflammatory activities, especially on chronic inflammation conditions, at lower doses than the separate crude extracts, without demonstrating side effects, probably acting in different pharmacological receptors. The inhibition of inflammation suggests a relationship with inflammatory mediators and PGE2 pathway and might be exploited to achieve greater anti-inflammatory efficacy, being considered as a potential phytotherapy.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Cordia , Modelos Animais de Doenças , Fabaceae , Dor/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Relação Dose-Resposta a Droga , Sinergismo Farmacológico , Feminino , Masculino , Camundongos , Dor/metabolismo , Medição da Dor/efeitos dos fármacos , Medição da Dor/métodos , Extratos Vegetais/isolamento & purificação
5.
BMJ Open ; 8(10): e019505, 2018 10 18.
Artigo em Inglês | MEDLINE | ID: mdl-30341109

RESUMO

INTRODUCTION: Oral mucositis is an iatrogenic condition of erythematous inflammatory changes which tends to occur on buccal and labial surfaces, the ventral surface of the tongue, the floor of the mouth and the soft palate of patients receiving chemotherapy. This protocol of ongoing randomised parallel group clinical trial aims to access the therapeutic effect of an herbal gel containing 2.5% Arrabidaea chica Verlot standardised extract on oral mucositis in patients with head and neck cancer compared with low-level laser therapy. METHODS AND ANALYSIS: Patients with head and neck cancer held at Clinics Hospital of University of Campinas, Sao Paulo, who develop early signs/symptoms of oral mucositis are eligible. Baseline characteristics of participants include oral mucositis grade and quality of life assessments. Enrolment started in November 2017 with allocation of patients to one of the study groups by means of randomisation. Patients will be treated either with Arrabidaea chica or laser until wound healing. Monitoring includes daily assessment of mucositis grade and diameter measurement by photographs and millimetre periodontal probe. Treatments will be concluded once mucositis is healed. A blinded assessor will evaluate mucositis cure after referred by the study team. At this point, the gel tube will be weighed to indirectly assess patient's compliance. At close-out, data will be analysed by a blinded researcher following the procedures described in the statistical analyses. ETHICS AND DISSEMINATION: This clinical trial was approved by the ethics committee of research in humans at the Faculty of Medical Sciences of University of Campinas (report no. 1,613,563/2016). Results from this trial will be communicated in peer-reviewed publications and scientific presentations. TRIAL REGISTRATION NUMBER: RBR-5×4397.


Assuntos
Protocolos Antineoplásicos/normas , Bignoniaceae , Terapia com Luz de Baixa Intensidade/métodos , Extratos Vegetais/uso terapêutico , Estomatite/tratamento farmacológico , Feminino , Neoplasias de Cabeça e Pescoço/complicações , Humanos , Masculino , Ensaios Clínicos Controlados Aleatórios como Assunto
6.
Braz Oral Res ; 32: e41, 2018 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-29846389

RESUMO

The aim of this study was to evaluate in vitro the antifungal, antibiofilm and antiproliferative activities of the extract from the leaves of Guapira graciliflora Mart. The phytochemical characterization of the extract was performed using electrospray ionization mass spectrometry (ESI-MS). The antimicrobial activity of the extract and its fractions was evaluated using the broth microdilution method against species of Candida. The inhibition of C. albicans biofilm was evaluated based on the number of colony-forming units (CFU) and metabolic activity (MTT). The antiproliferative activity of the extract and its fraction was evaluated in the presence of human tumor and non-tumor cells, and the cytotoxicity of the extract was determined on the RAW 264.7 macrophage line - both using the sulforhodamine B method. The phytochemical characterization indicated the presence of the flavonoids rutin and kaempferol. The extract and the methanol fraction exhibited moderate antifungal activity against C. albicans, C. krusei, and C. glabrata, and strong activity against C. dubliniensis. In the biofilms at 24 and 48 hours, the concentration of 12500 µg/mL of the extract was the most effective at reducing the number of CFU s/mL (44.4% and 42.9%, respectively) and the metabolic activity of C. albicans cells (34.6% and 52%, respectively). The extract and its fractions had no antiproliferative effect on the tumor lines tested, with mean activity (log GI50) equal to or greater than 1.71 µg/mL. Macrophage cell viability remained higher than 80% for concentrations of the extract of up to 62.5 µg/mL. G. graciliflora has flavonoids in its chemical composition and demonstrates potential antifungal and antibiofilm activity, with no evidence of a significant change in the viability of human tumor and non-tumor cell lines.


Assuntos
Antifúngicos/farmacologia , Biofilmes/efeitos dos fármacos , Candida/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Nyctaginaceae/química , Extratos Vegetais/farmacologia , Antifúngicos/isolamento & purificação , Biofilmes/crescimento & desenvolvimento , Sobrevivência Celular/efeitos dos fármacos , Dose Letal Mediana , Testes de Sensibilidade Microbiana
7.
Braz. oral res. (Online) ; 32: e41, 2018. tab, graf
Artigo em Inglês | LILACS | ID: biblio-889473

RESUMO

Abstract: The aim of this study was to evaluate in vitro the antifungal, antibiofilm and antiproliferative activities of the extract from the leaves of Guapira graciliflora Mart. The phytochemical characterization of the extract was performed using electrospray ionization mass spectrometry (ESI-MS). The antimicrobial activity of the extract and its fractions was evaluated using the broth microdilution method against species of Candida. The inhibition of C. albicans biofilm was evaluated based on the number of colony-forming units (CFU) and metabolic activity (MTT). The antiproliferative activity of the extract and its fraction was evaluated in the presence of human tumor and non-tumor cells, and the cytotoxicity of the extract was determined on the RAW 264.7 macrophage line - both using the sulforhodamine B method. The phytochemical characterization indicated the presence of the flavonoids rutin and kaempferol. The extract and the methanol fraction exhibited moderate antifungal activity against C. albicans, C. krusei, and C. glabrata, and strong activity against C. dubliniensis. In the biofilms at 24 and 48 hours, the concentration of 12500 µg/mL of the extract was the most effective at reducing the number of CFU s/mL (44.4% and 42.9%, respectively) and the metabolic activity of C. albicans cells (34.6% and 52%, respectively). The extract and its fractions had no antiproliferative effect on the tumor lines tested, with mean activity (log GI50) equal to or greater than 1.71 µg/mL. Macrophage cell viability remained higher than 80% for concentrations of the extract of up to 62.5 µg/mL. G. graciliflora has flavonoids in its chemical composition and demonstrates potential antifungal and antibiofilm activity, with no evidence of a significant change in the viability of human tumor and non-tumor cell lines.


Assuntos
Candida/efeitos dos fármacos , Extratos Vegetais/farmacologia , Biofilmes/efeitos dos fármacos , Nyctaginaceae/química , Proliferação de Células/efeitos dos fármacos , Antifúngicos/farmacologia , Testes de Sensibilidade Microbiana , Sobrevivência Celular/efeitos dos fármacos , Biofilmes/crescimento & desenvolvimento , Dose Letal Mediana , Antifúngicos/isolamento & purificação
8.
Artigo em Inglês | MEDLINE | ID: mdl-25713595

RESUMO

Despite the advances in anticancer drug discovery field, the worldwide cancer incidence is remarkable, highlighting the need for new therapies focusing on both cancer cell and its microenvironment. The tumor microenvironment offers multiple targets for cancer therapy, including inflammation. Nowadays, almost 75% of the anticancer agents used in chemotherapy are derived from natural products, and plants are an important source of new promising therapies. Continuing our research on Piper umbellatum species, here we describe the anticancer (in vitro antiproliferative activity and in vivo Ehrlich solid tumor model) and anti-inflammatory (carrageenan-induced paw edema and peritonitis models) activities of a standardized dichloromethane extract (SDE) from P. umbellatum leaves, containing 23.9% of 4-nerolidylcatechol. SDE showed in vitro and in vivo antiproliferative activity, reducing Ehrlich solid tumor growth by 38.7 and 52.2% when doses of 200 and 400 mg/kg, respectively, were administered daily by oral route. Daily treatments did not produce signals of toxicity. SDE also reduced paw edema and leukocyte migration on carrageenan-induced inflammation models, suggesting that the anticancer activity of SDE from Piper umbellatum leaves could involve antiproliferative and anti-inflammatory effects. These findings highlight P. umbellatum as a source of compounds against cancer and inflammation.

9.
Rev. bras. farmacogn ; 21(4): 622-626, jul.-ago. 2011. tab
Artigo em Inglês | LILACS-Express | ID: lil-596222

RESUMO

Gaylussacia brasiliensis (Spreng.) Meissn., Ericaceae, is used in folk medicine for treatment of several inflammatory processes and as healing agent. The scope of this work was to evaluate the in vitro antiproliferative activity of crude dichloromethane extract (CHD) and to identify the compound(s) responsible for this activity. CHD was evaluated and showed a concentration dependent inhibition on all cells lines. Therefore CHD was submitted to several classical columns chromatography providing the most active fraction (FC), inhibiting all cells line at 25 µg/mL. FC was further fractionated affording isolated compound 2β, 3β-dihydroxy-urs-12-ene-28-oic acid , identified on basis of 2D-NMR experiments and showed concentration-dependent activity and selectivity for kidney and breast cell lines.

10.
Planta Med ; 77(13): 1482-8, 2011 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21391177

RESUMO

Despite numerous studies with the Piper genus, there are no previous results reporting in vitro or in vivo Piper regnellii (Miq.) C. DC. var. regnellii anticancer activity. The aim of this study was to investigate P. regnellii in vitro and in vivo anticancer activity and further identify its active compounds. In vitro antiproliferative activity was evaluated in 8 human cancer cell lines: melanoma (UACC-62), breast (MCF7), kidney (786-0), lung (NCI-H460), prostate (PC-3), ovary (OVCAR-3), colon (HT29), and leukemia (K-562). Total growth inhibition (TGI) values were chosen to measure antiproliferative activity. Among the cell lines evaluated, eupomatenoid-5 demonstrated better in vitro antiproliferative activity towards prostate, ovary, kidney, and breast cancer cell lines. In vivo studies were carried out with Ehrlich solid tumor on Balb/C mice treated with 100, 300, and 1000 mg/kg of P. regnellii leaves dichloromethane crude extract (DCE), with 30 and 100 mg/kg of the active fraction (FRB), and with 30 mg/kg of eupomatenoid-5. The i. p. administration of DCE, FRB, and eupomatenoid-5 significantly inhibited tumor progression in comparison to control mice (saline). Therefore, this study showed that neolignans of Piper regnellii have promising anticancer activity. Further studies will be undertaken to determine the mechanism of action and toxicity of these compounds.


Assuntos
Antineoplásicos/farmacologia , Benzofuranos/farmacologia , Lignanas/farmacologia , Fenóis/farmacologia , Piper/química , Extratos Vegetais/farmacologia , Animais , Antineoplásicos/química , Benzofuranos/química , Carcinoma de Ehrlich/tratamento farmacológico , Linhagem Celular Tumoral , Feminino , Humanos , Lignanas/química , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Fenóis/química , Extratos Vegetais/química , Folhas de Planta/química
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