DEFAR - Artigos publicados em periódicos
URI permanente para esta coleçãohttp://www.hml.repositorio.ufop.br/handle/123456789/531
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Item A systematic review of drug-carrying nanosystems used in the treatment of leishmaniasis.(2023) Registre, Charmante; Soares, Rodrigo Dian de Oliveira Aguiar; Rúbio, Karina Taciana Santos; Santos, Orlando David Henrique dos; Carneiro, Simone PintoLeishmaniasis is an infectious disease responsible for a huge rate of morbidity and mortality in humans. Chemotherapy consists of the use of pentavalent antimonial, amphotericin B, pentamidine, miltefosine, and paromomycin. However, these drugs are associated with some drawbacks such as high toxicity, administration by parenteral route, and most seriously the resistance of some strains of the parasite to them. Several strategies have been used to increase the therapeutic index and reduce the toxic effects of these drugs. Among them, the use of nanosystems that have great potential as a site-specific drug delivery system stands out. This review aims to compile results from studies that were carried out using first- and second-line antileishmanial drug- carrying nanosystems. The articles referred to here were published between 2011 and 2021. This study shows the promise of effective applicability of drug-carrying nanosystems in the field of antileishmanial therapeutics, with the perspective of providing better patient adherence to treatment, increased therapeutic efficacy, reduced toxicity of conventional drugs, as well as the potential to efficiently improve the treatment of leishmaniasis.Item Modulation of long non-coding RNAs by different classes of secondary metabolites from plants : a mini-review on antitumor effects.(2022) Almeida, Tamires Cunha; Seibert, Janaína Brandão; Amparo, Tatiane Roquete; Souza, Gustavo Henrique Bianco de; Silva, Glenda Nicioli da; Santos, Orlando David Henrique dosThe broad pharmacological spectrum of plants is related to their secondary metabolism, which is responsible for the synthesis of different compounds that have multiple effects on cellular physiology. Among the biological effects presented by phytochemicals, their use for the prevention and treatment of cancer can be highlighted. This occurs due to several mechanisms of antitumor ac- tion demonstrated by these compounds, including regulation of the cell signaling pathways and inhibi- tion of tumor growth. In this way, long non-coding RNAs (lncRNAs) appear to be promising targets for the treatment of cancer. Their deregulation has already been related to a variety of clinical- pathological parameters. However, the effects of secondary metabolites on lncRNAs are still restrict- ed. For this reason, the present review aimed to gather data on phytochemicals with action on lncRNAs in order to confirm their possible antitumor potential. According to the literature, terpenoid and flavonoid are the main examples of secondary metabolites involved with lncRNAs activity. In addition, the lncRNAs H19, CASC2, HOTAIR, NKILA, CCAT1, MALAT1, AFAP1-AS1, MEG3, and CDKN2B-AS1 can be highlighted as important targets in the search for new anti-tumor agents since they act as modulating pathways related to cell proliferation, cell cycle, apoptosis, cell migration and invasion. Finally, challenges for the use of natural products as a commercial drug were also discussed. The low yield, selectivity index and undesirable pharmacokinetic parameters were emphasized as a difficulty for obtaining these compounds on a large scale and for improving the potency of its biologi- cal effect. However, the synthesis and/or development of formulations were suggested as a possible approach to solve these problems. All of these data together confirm the potential of secondary me- tabolites as a source of new anti-tumor agents acting on lncRNAs.Item Associating chitosan and microemulsion as a topical vehicle for the administration of herbal medicines.(2021) Oliveira, Denise Aline de Jesus; Amaral, Juliano Geraldo; Garcia, Laryana Borges; Santos, Milena Soares dos; Silva, Lorena A. O.; Almeida, Maiara Prates de; Gomes, Angélica Ferraz; Barros, Danielle Rocha Pinho; Lopes, Norberto Peporine; Pereira, Gislaine Ribeiro; Santos, Orlando David Henrique dos; Ruela, André Luís MoraisA viscous solution of low molecular weight chitosan (CH) at 5% w/v (10.2 kDa, 75 % deacetylated, 1451 cP at 25 ◦C) was associated with a microemulsion (ME) that undergoes a phase transition after water absorption in situ (≈28 % w/w), forming a more viscous liquid crystal, which was potentially evaluated as a topical vehicle. The ME was selected from a phase diagram, selecting a composition based on Tween® 80 (52 %), myristate isopropyl (28 %), and the aqueous phase (water and polyethylene glycol 400, 60:40 w/w) (20 %), which was after replaced by CH and herbal medicines (HM). HM are alternatives to treat candidiasis, and Stryphnodendron adstringens shell extract, characterized by molecular networking, and Melaleuca alternifolia Chell essential oil (46 % of terpinen-4- ol), showed in vitro activity against Candida albicans. Associating CH in ME improved the mechanical properties of the topical formulation, as adhesiveness, which is an advantageous feature for the topical treatment of vul vovaginal candidiasis.Item Melaleuca leucadendron (L.) L. flower extract exhibits antioxidant and photoprotective activities in human keratinocytes exposed to ultraviolet B radiation.(2020) Silva, Luan Silvestro Bianchini; Perasoli, Fernanda Barçante; Carvalho, Karen Vitor; Vieira, Karla Murata; Lopes, Miriam Teresa Paz; Souza, Gustavo Henrique Bianco de; Santos, Orlando David Henrique dos; Freitas, Katia MichelleRecently, there has been a demand for the replacement of chemical sunscreens with natural compounds that could prevent or restore UV-induced skin damage. Here, we investigated the photoprotective influence of the Melaleuca leucadendron ethanolic flower extract (EEMec) on factors involved in cellular and molecular UVBinduced oxidative stress in human skin keratinocytes (HaCaT). The phytochemical constituents, antioxidant potential by DPPH assay, content of total phenolic and flavonoid compounds in EEMec were evaluated. HaCaT cells were treated with EEMec followed by irradiation with UVB. CAT activity; GSH and ROS levels; and SOD1, GPx, CAT and COX-2 expression assays were employed to verify the oxidative stress, as well as EEMec effect on transmembrane transport, and pro-inflammatory and pro-apoptotic protein expression. EEMec reverted the viability loss of HaCaT cells after irradiation with UVB, exhibited significant antioxidant capacity and free radical scavenging activity in vitro, inhibited COX-2 expression and ensure protection of DNA-damage. EEMec shown a great photoprotective property to prevent keratinocytes damage induced by UV radiation and, thus a candidate potential to application as an adjuvant in sunscreen formulations as a strategy to reduce risk of sunburn and prevent skin diseases associated with UV-induced inflammation and cancer.Item Desenvolvimento de nanoemulsão fotoprotetora de Passiflora edulis.(2019) Almeida, Juliana Cristina dos Santos; Ribeiro, Thascilaine de Souza; Silva, Luan Silvestro Bianchini; Perasoli, Fernanda Barçante; Figueiredo, Bruna Inez Carvalho de; Carvalho, Karen Vitor; Dôres, Rosana Gonçalves Rodrigues das; Souza, Gustavo Henrique Bianco de; Santos, Orlando David Henrique dosO surgimento de inúmeras doenças, como o câncer de pele e o fotoenvelhecimento estão relacionados com a radiação solar em excesso, constituindo um considerável problema de saúde pública. O desenvolvimento fotoprotetores têm sido estimulado com o intuito de proteger a pele dos efeitos nocivos da radiação ultravioleta (UV). O objetivo do presente trabalho foi avaliar o potencial fotoprotetor (FPS) do extrato etanólico bruto (EB) de Passiflora edulis; a associação com a nanoemulsão e a atividade fotoprotetora; além de caracterizar as nanoemulsões quanto ao diâmetro médio, índice de polidispersão (IP) e potencial zeta. Foram desenvolvidas três nanoemulsões tópicas para incorporação do extrato a 0,5%. As nanoemulsões foram avaliadas visualmente quanto à aparência macroscópica 24 horas após o preparo, observando a presença ou não de sinais de instabilidade, como precipitação e separação de fases. Na formulação A, B e C, o extrato bruto foi solubilizado em Croduret, PEG e DMSO, respectivamente. O FPS foi determinado pelo método espectrofotométrico. Visualmente, a formulação A incorporou 100% do EB adicionado e apresentou-se estável após 24 horas. Entretanto, as formulações B e C não incorporaram todo o EB adicionado, ocasionando em separação das nanoemulsões em duas fases. O FPS foi determinado para o extrato etanólico bruto e para a formulação A. Para o extrato etanólico, o valor de FPS encontrado foi igual 11 e para a formulação A antes e após a incorporação do EB, FPS 4 e FPS 20, respectivamente. O diâmetro médio da formulação A sem e com extrato foi de 70,24 ± 0,12 nm e 72,10 ± 0,39 nm, respectivamente, indicando que não houve mudança significativa do diâmetro médio da nanoemulsão após a incorporação do EB. O IP da formulação A antes e após a adição de EB foi inferior a 0,3, caracterizando as mesmas como monodispersas. Os resultados apresentados mostraram que a associação do EB à formulação A resultou no aumento da sua atividade fotoprotetora.Item Pyrazinoic acid-poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery.(2019) Carneiro, Simone Pinto; Moine, Laurence; Tessier, Barbara; Valérie, Nicolas; Santos, Orlando David Henrique dos; Fattal, EliasTuberculosis is an infectious disease affecting mostly lungs, that is still considered a health global problem as it causes millions of deaths worldwide. Current treatment is effective but associated with severe adverse effects due to the high doses of each anti-tuberculosis drug daily administrated by oral therapy. For the first time, a pyrazinoic acid (PA) biodegradable nanoconjugate was synthesized and developed for pulmonary administration in an attempt to reduce the administered doses by achieving a high drug payload and controlled release at the target site. The conjugate was synthesized by coupling pyrazinoic acid on carboxylic groups of poly(malic acid), which is a biodegradable and biocompatible polymer, and posteriorly self-assembled into nanoconjugates. Characterization confirmed the formation of nanometric, spherical and negatively charged pyrazinoic acid nanoconjugate (NC-PA). NC-PA was stable for 60 days at 4 and 37°C and able to deliver PA in a sustained release manner over time. On macrophages, they exhibited no cell toxicity for a wide range of concentrations (from 1 to 100 µg/mL), demonstrating the safety of NC-PA. In addition, the nanoconjugate was efficiently taken up by RAW 264.7 cells over 6 hours reaching a maximum value after 3 hours of incubation. In conclusion, innovative nanoconjugates are a promising alternative to deliver drugs directly to the lungs and contributing to improving tuberculosis therapy.Item Photoprotective activity and increase of SPF in sunscreen formulation using lyophilized red propolis extracts from Alagoas.(2019) Almeida, Wanessa Aparecida da Silveira; Antunes, Amanda dos Santos; Penido, Ricardo Gonçalves; Correa, Helen Silva da Gloria; Nascimento, Andréa Mendes do; Andrade, Ângela Leão; Santos, Vagner Rodrigues; Cazati, Thiago; Amparo, Tatiane Roquete; Souza, Gustavo Henrique Bianco de; Freitas, Katia Michelle; Santos, Orlando David Henrique dos; Sousa, Lucas Resende Dutra; Santos, Viviane Martins Rebello dosThe excessive sun exposure, coupled with lack of sun protection represents one of the biggest risks to the occurrence of skin cancer and photoaging. Recent strategies for photoprotection have included the incorporation of natural antioxidant and anti-inflammatory compounds, into sunscreens, and the oral administration of natural antioxidant extracts. In this work, we use Brazilian red propolis extract because its antioxidant and anti-inflammatory activities. The aim of this work was to evaluate the sun protection factor and antioxidant activity of different hydroalcoholic extracts of red propolis (70% and 75%) prepared from lyophilized red propolis at room and high temperatures. The sun protection factor in vitro was determined by a spectrophotometric method developed by Mansur. The hydroalcoholic extracts of red propolis incorporated with Filter UVA-UVB 5% Gel Permulem TR-1 presented absorption in the UVB region. Also, the in vitro capacity of the hydroalcoholic extracts of red propolis to increase photoprotective activity of Filter UVA-UVB 5% Gel was evaluated. The hydroalcoholic extracts of red propolis incorporated presented higher values of sun protection factor and showed synergism in the photoprotective activity of Filter UVA-UVB 5% Gel Permulem TR-1. The antioxidant activity and sun protection factor are correlated with total phenolics content of the extracts and the hydroalcoholic extract of red propolis 75% at room temperature was choosen. The formulation developed with Filter UVA-UVB 5% Gel Permulem TR-1 with this hydroalcoholic extract of red propolis showed safe to be applied on the skin according HET-CAM test. Suggests indication of hydroalcoholic extract of red propolis (75% – room temperature) associated to photoprotective formulations for use in photoprotective products.Item Chemical constituents and allelopathic activity of the essential oil from leaves of Eremanthus erythropappus.(2018) Pinto, Ana Paula Resende; Seibert, Janaína Brandão; Santos, Orlando David Henrique dos; Vieira Filho, Sidney Augusto; Nascimento, Andréa Mendes doThe essential oil from leaves of Eremanthus erythropappus (DC.) MacLeish (Asteraceae) collected in South-eastern Brazil was extracted using a combination of water and steam distillation and investigated by chromatography/mass spectrometry (GC-MS). The sesquiterpene hydrocarbons were predominant (46.6%), followed by oxygenated sesquiterpenes (29.3%) and monoterpene hydrocarbons (18.8%). The major compounds were (β)-caryophyllene (29.3%), caryophyllene oxide (22.1%) and β-pinene (12.8%). The allelopathic activity of E. erythropappus essential oil on the seed germination and radicle length of seedlings was evaluated in lettuce (Lactuca sativa L.), tomato (Lycopersicum esculentum Mill.) and in two field weeds (field mustard – Brassica rapa L. and hairy beggarticks – Bidens pilosa L.). Among the weed species tested, the most significant inhibition of seed germination was observed in field mustard, as measured by the half–minimal inhibitory concentration, IC50 (IC50 = 26.5 μL mL–1), and the most significant inhibitory effect on radicle length of seedlings was observed in seedlings of hairy beggarticks (IC50 = 16.3 μL mL–1). In contrast, the lowest allelopathic effects of E. erythropappus essential oil on seed germination and radicle length of seedlings were observed in tomato (IC50 = >200 μL mL–1 and 130.1 μL mL–1 respectively) and lettuce (IC50 = 97.1 μL mL–1 and 35.1 μL mL–1 respectively). These results revealed significant allelopathic potential of E. erythropappus essential oil against weeds, but minimal effect on lettuce and tomato germination, and thus suggests it is feasible to use E. erythropappus sustainability as an eco-friendly bioherbicide in cropping settings.Item Seasonality study of essential oil from leaves of Cymbopogon densiflorus and nanoemulsion development with antioxidant activity.(2019) Seibert, Janaína Brandão; Rodrigues, Ivanildes Vasconcelos; Carneiro, Simone Pinto; Amparo, Tatiane Roquete; Lanza, Juliane Sousa; Frezard, Frederic Jean Georges; Souza, Gustavo Henrique Bianco de; Santos, Orlando David Henrique dosThe development of formulations that maintain the biological and physical chemistry properties of essential oils is an important choice when they are used as an active ingredient. This study aimed to characterize the essential oil from leaves of Cymbopogon densiflorus and evaluate the antioxidant activity of the oil, and to produce a nanoemulsion formulation containing it. The essential oil was obtained by hydrodistillation, and seasonality was analysed every 2 months by gas chromatography–mass spectrometry, showing that more than 90% of the composition was maintained for the whole period and that the major compounds were trans‐p‐menta‐2,8‐dien‐1‐ol, cis‐p‐menta‐2,8‐dien‐1‐ol, trans‐p‐menta‐1(7),8‐dien‐2‐ol, cis‐piperitol, and cis‐p‐menta‐1(7),8‐dien‐2‐ol. Stable nanoemulsions were prepared by phase inversion method encapsulating the essential oil. The antioxidant activity was evaluated by 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) free radical scavenging and 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulphonic acid (ABTS) methods. In the first test, free and nanoemulsified essential oil showed half‐maximal inhibitory concentration (IC50) values equivalent to 14.689 and 3.692 mg mL−1, respectively. In the second test, these values were 0.567 and 0.43 mg mL−1. The development of nanoemulsion‐based essential oil from leaves of C. densiflorus was viable, and the formulated oil was able to reproduce the antioxidant activity at a concentration four times lower than that of the pure essential oil.Item Development of propolis nanoemulsion with antioxidant and antimicrobial activity for use as a potential natural preservative.(2019) Seibert, Janaína Brandão; Silva, Jessica Paola Bautista; Amparo, Tatiane Roquete; Petit, Alicia; Pervier, Pauline; Almeida, Juliana Cristina dos Santos; Azevedo, Mariana Costa; Silveira, Benila Maria; Brandão, Geraldo Célio; Souza, Gustavo Henrique Bianco de; Teixeira, Luiz Fernando de Medeiros; Santos, Orlando David Henrique dosPropolis has demonstrated potential use as food preservative but it presents strong and unpleasant flavor that alters the sensory characteristics foods. A nanoemulsion was proposed to carry the Brazilian propolis extracts for use as natural food preservative. Antimicrobial and antioxidant activities and chemical constituents of the extracts were investigated. The latter were made by sequential extraction using different solvents (hexane, ethyl acetate and ethanol). Antimicrobial activity was evaluated by agar diffusion and microdilution methods and antioxidant activity by DPPH and ABTS assays. Extracts showed antibacterial and antioxidant activity, highlighting the ethanolic which contained artepillin-C, kaempferide, drupanin and p-coumaric acid as main compounds by LC-MS analysis. The nanoemulsion developed by phase inversion method was characterized and stable under thermal-stress and centrifugation conditions. Biological properties evaluated were effectively maintained by the formulation. It was concluded that the nanoemulsion can be used as a food preservative, preventing degradation and masking the propolis off-flavor.