Phenolic compounds, among them isopropyl caffeate, possess antioxidant potential, but not without toxicity and/or adverse effects. The present study aimed to evaluate the antioxidant activity and toxicity of isopropyl caffeate through in silico, in vitro and in vivo testing. The results showed that isopropyl caffeate presents no significant theoretical risk of toxicity, with likely moderate bioactivity: GPCR binding, ion channel modulation, nuclear receptor binding, and enzyme inhibition. Isopropyl caffeate induced hemolysis only at the concentrations of 500 and 1000 μg/ml. We observed types A and O erythrocyte protection from osmotic stress, no oxidation of erythrocytes, and even sequestrator and antioxidant behavior. However, moderate toxicity, according to the classification of GHS, was demonstrated through depressant effects on the central nervous system, though there was no influence on water and food consumption or on weight gain, and it did present possible hepatoprotection. We conclude that the effects induced by isopropyl caffeate are due to its antioxidant activity, capable of preventing production of free radicals and oxidative stress, a promising molecule with pharmacological potential.
The prevalence of candidiasis in the world is high. Candida species are able to create superficial and systemic infections. Candida albicans is an opportunistic pathogen, causing mycoses in immunocompromised patients as well as long-term antibiotic users. The present study objective was to evaluate in vitro anti-Candida effect of this compost isolated from Praxelis clematidea. The minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) were determined by the broth microdilution techniques. We also investigated possible flavonoid 5,7,4´trimethoxflavone (TMF) action on cell walls (0.8 M sorbitol) and cell membranes (TMF to ergosterol binding). The MIC50 of flavonoid were 64 g/mL and tha MFC50 was 64 g/mL. Involvement with the cell wall and ergosterol binding were comproved as possible mechanisms of action. In conclusion the flavonoid showed in vitro antifungal potential against strains of C. albicans.
O uso de medicamentos fitoterápicos vem crescendo mundialmente entre os programas preventivos e curativos, e tem estimulado a avaliação dos extratos de plantas para o uso na odontologia como controle do biofilme dental e outras desordens bucais. As plantas do gênero Lavandula, pertencem à família Lamiaceae, e têm sido utilizadas através dos anos para uma variedade de propósitos cosméticos e terapêuticos. Sua utilização na odontologia é, na grande maioria dos estudos, devido ao seu potencial ansiolítico. Entretanto, a Lavandula angustifólia demonstra outros potencias farmacológicos, como sua atividade antimicrobiana, antifúngica, anti-inflamatória e antinociceptiva. O presente estudo teve como objetivo integrar os conhecimentos já existentes sobre os aspectos das propriedades farmacológicas da Lavandula angustifolia Miller e sua aplicação na Odontologia. Trata-se de uma revisão bibliográfica no qual foi realizada uma seleção de artigos científicos a partir das bases de dados: Lilacs, MEDLINE, BVS e Scielo, além de monografias que atenderam aos requisitos do tema abordado, no período 2008 a 2018 com exceção de artigos clássicos que se apresentaram imprescindíveis ao presente estudo. Obteve-se um total de 1.532 artigos. Foram selecionados 38 artigos como amostra, que apresentaram a temática elencada para a pesquisa e que foram divididos por sessões: aspectos botânicos da planta; aspectos bioquímicos da planta; potencial antimicrobano; potencial anti-inflamatório; potencial ansiolítico e; potencial antinociceptivo. Pode-se concluir que a Lavandula angustifóliaMiller apresenta-se como uma boa alternativa para utilização na odontologia. Entretanto, a falta de trabalhos que abordem sua utilidade na odontologia revela a necessidade de se intensificar as pesquisas sobre o assunto.Descritores: Plantas Medicinais; Odontologia; Lavandula.ReferênciasFrancisco KSF. Fitoterapia: uma opção para o tratamento odontológico. Rev Saúde. 2010;4(1):18-24.Silveira SM, Cunha Júnior A, Scheuermann GN, Secchi FL, Silvani V, Marisete K et al . Composição química e atividade antibacteriana dos óleos essenciais de Cymbopogon winterianus (citronela), Eucalyptus paniculata (eucalipto) e Lavandula angustifolia (lavanda). Rev Inst Adolfo Lutz. 2012;71(3):462-70.Koulivand PH, Ghadiri MK, Gorji A. Lavender and the nervous system. Evid Based Complement Alternat Med. 2013;2013:681304.Verma RS, Rahman LU, Chanotiya CS, Verma RK, Chauhan A, Yadav A et al. Essential oil composition of Lavandula angustifolia Mill. cultivated in the mid hills of Uttarakhand, India. J Serb Chem Soc. 2010;75(3):343-48.Biasi LA, Deschamps C. 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Int J Agric Biol. 2013;15(4):772-76.Lam M, Jou Pc, Lattif Aa, Lee Y, Malbasa Cl, Mukherjee Pk et al. Photodynamic therapy with Pc 4 induces apoptosis of Candida albicans. Photochem Photobiol. 2011;87(4):904-9.Pereira CA, Romeiro RL, Costa AC, Machado AK, Junqueira JC, Jorge AO. Susceptibility of Candida albicans, staphylococcus aureus, and streptococcus mutans biofilms to photodynamic inactivation: an in vitro study. Lasers Med Sci. 2011;26(3):341-48.Neville BW, Damm DD, Allen CM, Bouquot JE. Patologia Oral e Maxilofacial. 3. ed. Rio De Janeiro: Elsevier;2009.de Rapper S, Kamatou G, Viljoen A, van Vuuren S. The in vitro antimicrobial activity of lavandula angustifolia essential oil in combination with other aroma-therapeutic oils. Evid Based Complement Alternat Med. 2013;2013:852049.Uniyal V, Bhatt RP, Saxena S, Talwar A. Antifungal activity of essential oils and their volatile constituents against respiratory tract pathogens causing Aspergilloma and Aspergillosis by gaseous contact. J Appl Nat Sci. 2012;4(1):65-70.Ribeiro BP, Pereira WS, Sousa AIP, Guerra RNM, Nascimento FRF. Alteração no perfil bioquímico induzido por reação inflamatória granulomatosa em camundondos. Rev Ciênc Saúde. 2010;12(1):73-9.Rubin E, Gorstein F, Rubin R, Schwarting R, Strayer D. Patologia. Bases clínicopatológicas da Medicina. 4. ed. Rio de Janeiro: Guanabara Koogan;2006.Silva GL. Avaliação da atividade antioxidante, antiinflamatória e antinociceptiva do óleo essencial de lavanda (Lavandula angustifolia Mill) [dissertação]. Dissertação (Mestrado). Porto Alegre: Universidade Católica do Rio Grande do Sul;2009.Cryan, JF, Sweeney FF. The age of anxiety: role of animal models of anxiolytic action in drug discovery. Br J Pharmacol. 2011;164(4):1129-61.Barik J, Marti F, Morel C, Fernandez SP, Lanteri C, Godeheu G et al. Chronic stress triggers social aversion via glucocorticoid receptor in dopaminoceptive neurons. Science. 2013;339(6117):332-35.Martin EI, Ressler KJ, Binder E, Nemeroff CB. The neurobiology of anxiety disorders: brain imaging, genetics, and psychoneuroendocrinology. Psychiatr Clin North Am. 2009;32(3):549-75.Oler JA, Fox AS, Shelton SE, Rogers J, Dyer TD, Davidson RJ et al. Amygdalar and hippocampal substrates of anxious temperament differ in their heritability. Nature. 2010;466(7308):864-68.Loggia ML, Schweinhardt P, Villemure MC, Bushnell Mc. Effects of psychological state on pain perception in the dental environment. J Can Dent Assoc. 2008;74(7):651-56.Carvalho RWF, Falcão PGCB, Campos GJL, Bastos AS, Pereira JC, Pereira MAS et al. Ansiedade frente ao tratamento odontológico: prevalência e fatores predictores em brasileiros. Ciênc Saúde Colet. 2012;17(7):1915-22.Siviero M, Nhani VT, Prado EFGB. Análise da ansiedade como fator preditor de dor aguda em pacientes submetidos à exodontias ambulatoriais. Rev Odontol UNESP. 2008;37(4):329-36Coelho LS, Correa-Netto NF, Masukawa MY, Lima AC, Maluf S, Linardi A et al. Inhaled Lavandula angustifolia essential oil inhibits consolidation of contextual-but not tone-fear conditioning in rats. J Ethnopharmacol. 2018;215:34-41.Oliveira RRB, Góis RMO, Siqueira RS, Almeida JRGS, Lima JT, Nunes XP et al . Antinociceptive effect of the ethanolic extract of Amburana cearensis (Allemão) A.C. Sm., Fabaceae, in rodents. Rev bras farmacogn. 2009;19(3):672-76.Millan MJ. Descending control of pain. Prog Neurobiol. 2002;66(6):355-474.Julius D, Basbaum AI. Molecular mechanisms of nociception. Nature. 2001;413(6852):203-10.Centers for Disease Control and Prevention. Unintentional drug poisoning in the United States. CDC: Atlanta, 2010. Disponível em: https://www.cdc.gov/homeandrecreationalsafety/pdf/poison-issue-brief.pdf.Donatello NN. Ativação de receptores opioides periféricos e espinais pela inalação do óleo essencial de lavandula augustifolia reduz hiperalgesia mecânica em modelos animais de neuropatia e inflamação crônica [dissertação]. 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Flavonoid compounds are widely used as natural protective species, which can act as anti-inflammatory, antioxidant, anticoagulant, antihypertensive and antitumor agents. This study set out to investigate the probable pharmacological activities, along with the antibacterial and antioxidant effects, of flavone and its hydroxy derivatives: 3-hydroxyflavone, 5-hydroxyflavone and 6-hydroxyflavone. To do so, we investigated their pharmacological characteristics, using in silico tests that indicate likelihood of activity or inactivity, with the PASS online software, and the antimicrobial potential against Gram positive and Gram negative bacteria was also analyzed, including bacteria of clinical importance. We also tested for oxidant and antioxidant potential in these molecules in the presence of reactive oxygen species (ROS) and phenylhydrazine (Ph). The results revealed the following characteristics: pharmacological activities for the flavonoids as agonists of cell membrane integrity and as permeability inhibitors, as antagonists of anaphylatoxin receptors, as inhibitors of both kinase and peroxidase, and as having both antimutagenic capacity and vaso-protective potential. All of the flavonoids exhibited moderate antibacterial activity against Gram positive and Gram negative strains, with the flavones being bactericidal at 200 μg/mL for the strains of P. aeruginosa ATCC 8027, S. aureus ATCC 25619 and E. coli 104; the other flavonoids revealed bacteriostatic action. The substances did not promote erythrocyte oxidation and behaved as sequestrators and antioxidants of hydrogen peroxide (H2O2) and phenylhydrazine (Ph). It was concluded that the analyzed compounds have various pharmacological activities in accordance with the predictions of PASS online, as their antibacterial and antioxidant activities were confirmed. The study also helps to consolidate the use of computational chemistry in silico tools to guide new drug search and discovery protocols.
ResumoA B. forfica L uma das espécies mais populares do gênero Bahuina, pertencente à família Fabaceae, possui aproximadamente 300 espécies distribuídas principalmente pelas regiões tropicais do globo terreste. A pata-de-vaca nome popular dado a B. forficata tem suas diversas partes amplamente utilizadas para a preparação de produtos medicinais "caseiros" na terapia de diversas doenças, desde infecções, dores até como um agente hipoglicemiante para o tratamento da Diabetes. Os primeiros estudos clínicos com a pata-devaca se iniciaram no período de 1929 justificando o seu uso como hipoglicemiante e posteriormente estudos decorrentes no ano de 2004 validam o primeiro estudo clínico realizado, trazendo cada vez mais o interesse da comunidade cientifica para esta espécie medicinal. O propósito deste trabalho foi investigar e apresentar as propriedades farmacológicas, em especial hipoglicemiante, da B. forficata através de uma revisão narrativa da literatura. Metodologia: Foi realizada uma revisão narrativa da literatura científica, definindo-se como uma análise mais ampla dos conhecimentos já produzidos, tomando como base de dados trabalhos científicos na faixa anual de 2007 a 2017. Diante da revisão da literatura realizada foi possível evidenciar os efeitos hipoglicemiantes do extrato da B. forficata, bem como o seu emprego em diferentes formas farmacêuticas, desde pós a granulados. Concluiu-se que embora a B. forficata se mostre promissora para a área farmacêutica são necessários mais estudos associados a possíveis formas farmacêuticas que podem ser utilizadas, uma vez que o emprego de plantas medicinais na terapia de controle da diabetes seja uma forma de facilitar a adesão dos pacientes ao tratamento. Descritores: Diabetes Mellitus; Hipoglicemiantes; Fitoterapia; Bauhinia. AbstractThe B. forfica L one of the most popular species of the Bahuina genus, belonging to the Fabaceae family, has approximately 300 species distributed mainly in tropical regions of the earth globe. The popular name paw given to B. forficata has its various parts widely used for the preparation of "home" medicinal products in the therapy of various diseases, from infections, pains to as a hypoglycemic agent for the treatment of Diabetes. The first clinical studies with the paw-of-cow began in the period of 1929 justifying its use as hypoglycemic and later studies in 2004 validate the first clinical study carried out, bringing increasingly the interest of the scientific community for this species medicinal. The aim of this paper was to investigate and present the pharmacological properties, especially hypoglycemic, of B. forficata through a narrative review of the literature. A narrative review of the scientific literature was carried out, defining itself as a broader analysis of the knowledge already produced, based on scientific studies in the annual range from 2007 to 2017. In the face of the literature revision carried out, the hypoglycaemic effects of the B. forficata extract, as well as its use in different pharmaceutical forms, from p...
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