ABSTRACT
This study determined phytochemical composition, antifungal activity and toxicity in vitro and in vivo of Syzygium cumini leaves extract (Sc). Thus, was characterized by gas chromatography coupled to mass spectrometry and submitted to determination of Minimum Inhibitory (MIC) and Fungicidal concentrations (MFC) on reference and clinical strains of Candida spp. and by growth kinetics assays. Toxicity was verified using in vitro assays of hemolysis, osmotic fragility, oxidant and antioxidant activity in human erythrocytes and by in vivo acute systemic toxicity in Galleria mellonella larvae. Fourteen different compounds were identified in Sc, which showed antifungal activity (MIC between 31.25-125µg/mL) with fungistatic effect on Candida. At antifungal concentrations, it demonstrated low cytotoxicity, antioxidant activity and neglible in vivotoxicity. Thus, Sc demonstrated a promising antifungal potential, with low toxicity, indicating that this extract can be a safe and effective alternative antifungal agent.
Este estudio determinó la composición fitoquímica, la actividad antifúngica y la toxicidad in vitro e in vivo del extracto de hojas de Syzygium cumini (Sc). Así, se caracterizó mediante cromatografía de gases acoplada a espectrometría de masas y se sometió a determinación de Concentraciones Mínimas Inhibitorias (CMI) y Fungicidas (MFC) sobre cepas de referencia y clínicas de Candida spp. y mediante ensayos de cinética de crecimiento. La toxicidad se verificó mediante ensayos in vitro de hemólisis, fragilidad osmótica, actividad oxidante y antioxidante en eritrocitos humanos y por toxicidad sistémica aguda in vivo en larvas de Galleria mellonella. Se identificaron catorce compuestos diferentes en Sc, que mostraron actividad antifúngica (CMI entre 31.25-125 µg/mL) con efecto fungistático sobre Candida. En concentraciones antifúngicas, demostró baja citotoxicidad, actividad antioxidante y toxicidad in vivo insignificante. Por lo tanto, Sc demostró un potencial antifúngico prometedor, con baja toxicidad, lo que indica que este extracto puede ser un agente antifúngico alternativo seguro y eficaz.
Subject(s)
Humans , Plant Extracts/pharmacology , Plant Extracts/chemistry , Syzygium/chemistry , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Candida/drug effects , Plant Extracts/toxicity , Microbial Sensitivity Tests , Toxicity Tests , Plant Leaves/chemistry , Phenolic Compounds/analysis , Gas Chromatography-Mass Spectrometry , Antifungal Agents/toxicity , AntioxidantsABSTRACT
This study aimed to evaluate the in silico, in vitro, and ex-vivo toxicity of vitexin, the flavonoid 5,7,4'- trihydroxyflavone-8-C-ß-glucopyranoside from Waltheria viscosissima. The chemical structure and predicted bioactive properties were also in silico analyzed. The in vitro and ex-vivo assays were performed according to the Ethics Code of the World Medical Association and were approved by the Ethics Committee of University Center of Patos (protocol number: 3.621.284). In silico analysis suggested that the molecule presents good oral bioavailability and good absorption; penetrating biological membranes. The toxicity tests revealed the potential effectiveness of the molecule in cellular protection against free radicals, in addition to possible antimutagenic, anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and apoptosis agonist activity. Hemolytic and genotoxic assessment detected low hemolysis rates in human red blood cells and no cellular toxicity against oral mucosa cells. The data suggest that vitexin is a safe molecule for possible therapeutic application and its toxicity profile indicates viability for future studies.
ABSTRACT
Plant species have been used for therapeutic purposes since ancient times and are still in use today since these products represent a source of raw material for the production of phytotherapeutic formulations. Screening and investigation of plants with pharmacological potential require the evaluation of characteristics related to their action, efficacy and safety in different steps. Among these steps, pre- clinical trials are used to evaluate the properties of the test product in in vitro experiments, such as cytotoxicity assays. Within this context, this study consists of a bibliometric analysis of some in vitro cytotoxicity and toxicity assays in erythrocytes used during bioprospecting of medicinal plants. The results demonstrated the wide application of erythrocytes to evaluate the biological effects of medicinal plant extracts. The methods were found to be valid and effective for the preliminary investigation of the in vitro cytotoxicity and toxicity of plant products.
El uso de especies vegetales para fines terapeÌuticos es una praÌctica histoÌrica y todaviÌa bastante actual, ya que estos productos pueden representar una fuente de materia prima para la produccioÌn de formulaciones fitoteraÌpicas. En investigacioÌn de plantas con potencial farmacoloÌgico requiere la evaluacioÌn de su accioÌn, eficacia y seguridad, a traveÌs de diferentes etapas. Entre estas, en los ensayos precliÌnicos se evaluÌan las propiedades del producto-prueba en experimentos in vitro, tales como ensayos de citotoxicidad, entre otros. En este aspecto, el presente estudio consiste en un anaÌlisis bibliomeÌtrico acerca de algunas pruebas de citotoxicidad y toxicidad in vitro en eritrocitos realizados en los ensayos de bioprospeccioÌn de plantas medicinales. Los resultados evidencian la amplia utilizacioÌn de eritrocitos para la evaluacioÌn de los efectos bioloÌgicos de extractos de plantas medicinales, apuntaÌndolos como meÌtodos vaÌlidos y eficaces para la investigacioÌn preliminar de la citotoxicidad y toxicidad in vitro de productos vegetales.
Subject(s)
Biological Assay/methods , Plant Extracts/toxicity , Erythrocytes/drug effects , Antioxidants/toxicity , Osmotic Fragility , Oxidative Stress , Erythrocytes/cytology , Bioprospecting , Hemolysis/drug effectsABSTRACT
The fungi of the genus Candida play a relevant role in the emergence of oral infections and are increasingly more frequent the cases of infections by non-albicans strains. In light of this context and the need for new alternatives to the antimicrobial therapy, the monoterpene [7-hidroxicitronelal] (7-HO) was evaluated for its antifungal effects. For the obtainment of the MIC and MFC values the broth microdilution method was used. The MIC and the MFC of this monoterpene for 60% of the tested strains was of 256µg/mL and 512µg/mL respectively. Furthermore, the standard antifungal nystatin (100UI/mL) was used as positive control for the inhibition of fungal growth. Therefore, were used 4 clinical strains of the species tropicalis (LM 06, LM 14, LM 31 and LM 36) and a standard strain (C. tropicalis ATCC 13803), originated from the Mycology collection of the Mycology Laboratory (LM) of the Health Sciences Center (CCS) of the Federal University of Paraiba (UFPB). The results obtained in this study showed fungicide activity of the compound (7-OH) against the strains of C. tropicalis.
Os fungos do gênero Candida tem um papel relevante no aparecimento de infecções orais e são cada vez mais frequentes os casos de infecções por cepas não-albicans. Diante deste contexto e da necessidade de novas alternativas para a terapia antimicrobiana, o monoterpeno [7-hidroxicitronelal] (7-HO) foi avaliado pelos seus efeitos antifúngicos. Para a obtenção dos valores da CIM e da CFM foi utilizado o método da microdiluição em caldo. A CIM e a CFM deste monoterpeno para 60% das cepas testadas foram de 256µg/mL e 512µg/mL respectivamente. Além disso, o antifúngico padrão nistatina (100UI/mL) foi utilizado como controle positivo para inibir o crescimento fúngico. Por tanto, foram utilizadas 4 cepas clínicas da espécie tropicalis (LM 06, LM 14, LM 31 e LM 36) e uma cepa padrão (C. tropicalis ATCC 13803), oriundas da Micoteca do Laboratório de Micologia (LM) do Centro de Ciências da Saúde (CCS) da Universidade Federal da Paraíba (UFPB). Os resultados obtidos neste estudo mostraram atividade fungicida do composto (7-OH) contra as cepas de C. tropicalis.
Subject(s)
In Vitro Techniques , Candidiasis, Oral , Monoterpenes , Antifungal AgentsABSTRACT
Este trabalho tem como objetivo avaliar a atividade antimicrobiana do extrato do Croton sonderianus (marmeleiro) frente a bactérias que fazem parte do biofilme dental, como Streptococcus salivaris, mutans, mitis, sanguis e sobrinus. Os ensaios foram realizados pela técnica de difusão em meio sólido com base no tamanho dos halos de inibição. Os mesmos procedimentos foram utilizados com a clorexidina. Os resultados mostraram que todas as amostras ensaiadas foram sensíveis ao extrato com CIM (mg.mL-1) de 1:16 (0,62%), 1:32 (0,31%), 1:64 (0,15%), 1:32 (0,31%), 1:16 (0,62%), respectivamente. S. mitis foi a linhagem mais sensível. Os resultados mostram a potencialidade do extrato do Croton sonderianus na inibição do crescimento bacteriano de micro-organismos formadores do biofilme dental, sugerindo a possibilidade do emprego desse extrato como meio alternativo no controle desses patógenos naprática odontológica.
This study aims to evaluate the antimicrobial activity of the extract of Croton sonderianus (marmeleiro) against bacteria that are part of the biofilm, such as Streptococcus salivaris, mutans, mitis, sanguis, sobrinus. The tests were carried out by diffusion technique on solid medium based on the size of inhibition zones. The same procedures were used with chlorhexidine. The results showed that all samples tested were sensitive to the extract with MIC (mg.mL-1) of 1:16 (0.62%), 1:32 (0.31%), 1:64 (0.15%) 1:32 (0.31%), 1:16 (0.62%), respectively. S. mitis strainwas more sensitive. The results show the potential of the extract of Croton sonderianus in growth inhibition of microorganisms forming the biofilm suggesting the possibility of using this extract as an alternative means to control these pathogens in dental practice.
Subject(s)
Croton , Bacteria , Dental Caries , Lactobacillus , Products with Antimicrobial Action , Streptococcus , Pathology, Oral , Dental Plaque , Anti-Infective Agents , Chlorhexidine , Microbiota , Streptococcus mitis , Streptococcus oralisABSTRACT
A partir da década de 60, surgiu a engenharia genética ou tecnologia do DNA recombinante, com técnicas que permitem a manipulaçäo do ácido desoxirribonucléico (DNA). Por meio dessas técnicas, genes de um organismo podem ser transferidos para outro. Esses genes transferidos quebram a seqüência de DNA do organismo receptor, tornando-o capaz de produzir novas substancias. Assim säo obtidos os alimentos transgênicos. Atualmente, questiona-se sua utilizaçäo frente aos riscos e benefícios de seu emprego.(au)