Exploring the Fluconazole-Resistance Modifying Activity and Potential Mechanism of Action of Fixed Oil from Caryocar coriaceum Wittm. (Caryocaraceae) against Candida Species.

The fixed oil from the inner mesocarp of Caryocar coriaceum Wittm. is used in the Chapada do Araripe region of Brazil for the treatment of genitourinary candidiasis. This study aimed to evaluate the chemical composition, antifungal activity, reduction of fungal virulence, and the preliminary toxicity of the fixed oil from the inner mesocarp of C. coriaceum tested against three Candida yeasts. The oil was characterized by gas chromatography (GC-MS and GC-FID). Antifungal activity was assessed using the serial microdilution method. Additionally, the potential of the oil as an enhancer of fluconazole action was tested at sub-inhibitory concentrations (MIC/8). The mechanism of action of C. coriaceum fixed oil was determined by evaluating the inhibition of morphological transition in Candida spp. The chemical composition of the fixed oil of C. coriaceum comprised both unsaturated and saturated fatty acids. Oleic (61 %) and palmitic (33 %) acids were the major constituents. Regarding its anti-Candida activity, the oil inhibited the growth of C. albicans (IC50 : 371 µg/mL) and C. tropicalis (IC50 : 830 µg/mL). Furthermore, the oil reversed the antifungal resistance of C. albicans and C. tropicalis, restoring the susceptibility to fluconazole and reducing their IC50 from 12.33 µg/mL and 362 µg/mL to 0.22 µg/mL and 13.93 µg/mL, respectively. The fixed oil of C. coriaceum completely inhibited the morphological transition of C. albicans and C. tropicalis at a concentration of 512 µg/mL, but exhibited limited low antifungal potential against C. krusei. The observed antifungal activity may be attributed to the overproduction of reactive oxygen species. Additionally, the oil showed no toxic effect on the Drosophila melanogaster in vivo model. The fixed oil from the inner mesocarp of C. coriaceum emerge as a strong candidate for the development of new pharmaceutical formulations to treat infections caused by Candida spp.

Enhancing the Antifungal Efficacy of Fluconazole with a Diterpene: Abietic Acid as a Promising Adjuvant to Combat Antifungal Resistance in Candida spp.

The increasing antifungal resistance rates against conventional drugs reveal the urgent need to search for new therapeutic alternatives. In this context, natural bioactive compounds have a critical role in antifungal drug development. Since evidence demonstrates that abietic acid, a diterpene found in Pinus species, has significant antimicrobial properties, this study aimed to evaluate the antifungal activity of abietic acid against Candida spp and its ability to potentiate the activity of fluconazole. Abietic acid was tested both individually and in combination with fluconazole against Candida albicans (CA INCQS 40006), Candida krusei (CK INCQS 40095), and Candida tropicalis (CT INCQS 40042). The microdilution method was used to determine the IC50 and the cell viability curve. Minimum Fungicidal Concentration (MFC) was determined by subculture in a solid medium. The plasma membrane permeability was measured using a fluorescent SYTOX Green probe. While the IC50 of the drugs alone ranged between 1065 and 3255 µg/mL, the IC50 resulting from the combination of abietic acid and fluconazole ranged between 7563 and 160.1 µg/mL. Whether used in combination with fluconazole or isolated, abietic acid exhibited Minimum Fungicidal Concentration (MFC) values exceeding 1024 µg/mL against Candida albicans, Candida krusei and Candida tropicalis. However, it was observed that the antifungal effect of fluconazole was enhanced when used in combination with abietic acid against Candida albicans and Candida tropicalis. These findings suggest that while abietic acid alone has limited inherent antifungal activity, it can enhance the effectiveness of fluconazole, thereby reducing antifungal resistance.

Caryocar coriaceum fruits as a potential alternative to combat fungal and bacterial infections: In vitro evaluation of methanolic extracts.

Caryocar coriaceum, commonly known as 'pequi', is a medicinal species used traditionally for the herbal treatment of infectious and parasitic diseases in the Brazilian Northeast region. In this study, we investigated whether the fruits of C. coriaceum have bioactive chemical constituents against etiological agents of infectious diseases. The methanolic extract of the internal mesocarp of the fruits of C. coriaceum (MECC) was chemically analyzed and evaluated for its antimicrobial and drug-enhancing activity against multidrug-resistant pathogenic bacteria (Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus), and Candida spp. strains. The extract had flavones, flavonols, xanthones, catechins, and flavanones as major classes. A total of 11.26 mg GAE/g of phenolics, and 5.98 mg QE/g of flavonoids were found. No intrinsic antibacterial activity was observed; however, the extract was able to intensify the action of gentamicin and erythromycin against multi-resistant strains. The anti-Candida effect observed in this study was mainly due to the formation of reactive oxygen species. The extract was capable of causing damage to the plasmatic membrane of Candida tropicalis through pores formation. Our findings partially support the ethnopharmacological uses of the fruit pulp of C. coriaceum against infectious and parasitic diseases.

Chemical composition and antimicrobial potential of Acrocomia aculeata (Jacq.) Lodd. ex Mart. and Syagrus cearensis Noblick (Arecaceae).

This study aimed to evaluate the antibiotic effects of the fixed oils of Acrocomia aculeata (FOAA) and Syagrus cearenses (FOSC) against the bacterial strains and the fungi strains of the genus Candida spp. The method of serial microdilution using different concentrations was used for measuring the individual biological activity of the fixed oils. The fixed oil of A. aculeata showed the presence of oleic acid (24.36%), while the oil of S. cearensis displayed the content of myristic acid (18.29%), compounds detected in high concentration. The combination FOAA + Norfloxacin, and FOSC + Norfloxacin showed antibacterial activity against E. coli and S. aureus strains, demonstrating possible synergism and potentiation of the antibiotic action against multidrug-resistant strains. The combination FOAA + Fluconazole displayed a significant effect against Candida albicans (IC50 = 15.54), C. krusei (IC50 = 78.58), and C. tropicalis (IC50 = 1588 µg/mL). Regarding FOSC + Fluconazole, it was also observed their combined effect against the strains of C. albicans (IC50 = 3385 µg/mL), C. krusei (IC50 = 26.67 µg/mL), and C. tropicalis (IC50 = 1164 µg/mL). The findings of this study showed a significant synergism for both fixed oils tested when combined with the antibiotic.

Antifungal effect of the liposome encapsulation of the Trans- Caryophylene and its association with fluconazole.

Trans-Caryophyllene (TC), a sesquiterpene, with proven biological activities, which in this work was tested alone, encapsulated in liposomes and associated with Fluconazole in vitro in an attempt to enhance the effect of the drug. Liposomes were characterized from vesicle size, polydispersity index, and Zeta potential, and imaging by scanning electron microscopy. Antifungal assays were performed against Candida albicans, Candida tropicalis and Candida krusei by microdilution to determine the IC50 values and the viability curve. The Minimum Fungicidal Concentration (MFC) was performed by subcultivation in solid medium and the inhibitory effect of the association of TC and Fluconazole and tests to verify morphological changes was performed in micro-cultivation chambers based on concentrations on microdilution plates. The corresponding IC50 data of the substances ranged from 34.4 to 65249 µg/mL, considerably high values compared to the control (Fluconazole). The MFC of all compounds showing fungistatic effect. The performance of the compounds on the cell viability curve was similar in all tested strains, as they showed no antifungal potential when compared to the control (FCZ), when associated with FCZ they showed no significant antifungal activity. The free and liposomal TC also managed to restrict 100% of the fungal dimorphism, in both concentrations, against C. albicans, and against C. tropicalis the isolated TC did not show a significant inhibitory effect; however, against the C. krusei strain inhibited 100% in filamentous growth in both concentrations, which is statistically relevant. The liposomes were homogeneous, with vesicles with diameters of 185.46 nm for the control and 143.8 nm for the liposomal TC, and a surface charge potential of - 42.6 mV. By scanning microscopy, the spherical shapes of the vesicles were verified.

Traditional Uses, Phytochemistry, and Bioactivities of Mesosphaerum suaveolens (L.) Kuntze.

Mesosphaerum suaveolens (L.) Kuntze is a species widely used traditionally in the treatment of ailments, such as stomach pain, hemorrhoids, cough, verminosis, ulcer, liver disease, fever, influenza, nasal congestion, and inflammation. This review aims to provide a survey of available information on seven international electronic databases (Google Scholar, Medline, ResearchGate, Web of Science, Scopus, Science Direct, and PubMed) about botanical aspects, traditional uses, phytochemistry, and biological activities of M. suaveolens. Mesosphaerum suaveolens is a tropical America native species, but it can be found in several parts of the world as a ruderal plant. The species is the most studied species of the genus Lamiaceae due its phytochemical aspect, especially regarding the chemical composition of its essential oil. Besides the essential oils, M. suaveolens is a source of numerous secondary compounds such as triterpenes, diterpenes, and phenolic compounds, which are related to its biological activities, such as allelopathic, antibacterial, antifungal, insecticidal, and larvicidal activities as described in the literature.

Bioactive Compounds as Potential Agents for Sexually Transmitted Diseases Management: A Review to Explore Molecular Mechanisms of Action.

Sexually transmitted diseases (STDs) are produced by pathogens like bacteria, fungi, parasites, and viruses, and may generate severe health problems such as cancer, ulcers, and even problems in the newborn. This narrative review aims to present updated information about the use of natural bioactive compounds for the prevention and treatment of sexually transmitted infections. A search of the literature was performed using databases and search engines such as PubMed, Scopus, Google Scholar and Science Direct. From the pharmacotherapeutic management point of view, any strategies for prevention should contain medical approaches. The bioactive compounds obtained from natural products have shown biological effects against different microorganisms for the treatment of these diseases. The main results showed antimicrobial, antiprotozoal, antifungal and antiviral effects such as HIV. Also, the molecular mechanisms, signalling pathways and action targets of natural compounds were highlighted, thus justifying bacterial and antifungal inhibition, apoptosis or reduction of viral replication. From the data of our study, we can conclude that natural compounds may be a significant source for adjuvant drugs / complementary therapies in the treatment of STDs. With all these benefits, the future must conduct extensive clinical trials and the development of pharmaceutical nanotechnologies for a greater therapeutic effect.

Antifungal Properties of Nerolidol-Containing Liposomes in Association with Fluconazole.

(1) Background: Infections by Candida species represent a serious threat to the health of immunocompromised individuals. Evidence has indicated that nerolidol has significant antifungal properties. Nonetheless, its use is restricted due to a low water solubility and high photosensitivity. The incorporation into liposomes may represent an efficient alternative to improve the physicochemical and biopharmaceutical properties of this compound. The present study aimed to characterize the antifungal properties of liposomal nerolidol, alone or in combination with fluconazole. Of note, this is the first study reporting the antifungal activity of liposomal nerolidol and its potentiating effect in association with fluconazole. (2) Methods: The Inhibitory Concentration 50%-IC50 and minimum fungicide concentrations (MFC) of the substances against Candida albicans (CA), Candida tropicalis (CT), and Candida krusei (CK) were established by subculture in a solid medium. To evaluate the antifungal-enhancing effect, the MFC of fluconazole was determined in the presence or absence of subinhibitory concentrations of nerolidol (free or liposomal). The analysis of fungal dimorphism was performed through optical microscopy and the characterization of liposomes was carried out considering the vesicular size, polydispersion index, and zeta medium potential, in addition to a scanning electron microscopy analysis. (3) Results: The physicochemical characterization revealed that liposomes were obtained as homogenous populations of spherical vesicles. The data obtained in the present study indicate that nerolidol acts as an antifungal agent against Candida albicans and Candida tropicalis, in addition to potentiating (only in the liposomal form) the effect of fluconazole. However, the compound had little inhibitory effect on fungal dimorphism. (4) Conclusions: The incorporation of nerolidol into liposomes improved its antifungal-modulating properties.

In vitro Antibiotic and Modulatory Activity of Mesosphaerum suaveolens (L.) Kuntze against Candida strains.

The emergence of fungal resistance to commercial drugs has been a major problem for the WHO. In this context, research with natural products is promising in the discovery of new active substances. Thus, this work evaluated the antifungal effect of a medicinal plant (i.e., Mesosphaerum suaveolens) against strains of the genus Candida, tested the combined effect with the drug fluconazole, and, finally, determined the phenolic constituents present in the species. Initially, aqueous extracts of leaves (AELMs) and aerial parts (AEAPMs) of the species were prepared. For microbiological assays, the minimum fungicidal concentration was determined by broth microdilution, and the combined effect of fluconazole extracts were verified by sub-inhibitory microdilution concentrations (CFM/8) followed by spectrophotometric readings which were used to determine the IC50. HPLC detected the presence of flavonoids and phenolic acids, detecting eight compounds present in the samples of which caffeic acid and quercetin were major components. The AELMs modulated fluconazole activity since it decreased fluconazole's IC50 from 7.8 µg/mL to an IC50 of 4.7 µg/mL (CA LM 77) and from 28.8 µg/mL to 18.26 µg/mL (CA INCQS 40006) for the C. albicans strains. The AEAPMs were able to potentiate the effect of fluconazole more effectively than the AELMs. Such an effect was significant for the 16 µg/mL concentration for CA LM 77 and 32 µg/mL for CA INCQS 40006. The AEAPMs as well as the AELMs presented clinically relevant activities for C. tropicalis strains. For the C. tropicalis LM 23 strain, the AEPMs obtained an IC50 of 25 µg/mL and the AELMs an IC50 of 359.9 µg/mL.

GC/MS analysis and antimicrobial activity of the Piper mikanianum (Kunth) Steud. essential oil.

The Piper mikanianum species were investigated by the antimicrobial potential and chemical composition. Chemical analysis was performed by gas chromatography coupled to mass spectrometry (GC/MS). The Minimum Inhibitory Concentration (MIC) as well as the 50% Inhibitory Concentration against Candida strains were determined by microdilution. The effect of the drug-oil combination was also evaluated to verify possible synergism. The Minimum Fungicidal Concentration (MFC) was evaluated by subculturing the microdilution in Petri dishes and the anti-pleomorphism potential of the oil was tested in humid chambers. Chemical analysis revealed safrol as the major compound. The results from the intrinsic activity evaluation of the oil did not reveal a clinical importance, however, it presented a synergistic effect when associated with gentamicin against the multidrug resistant E. coli strain and when associated with fluconazole against fungal strains. Moreover, the oil possessed a fungistatic effect. Total inhibition of filamentous structures occurred in both Candida species in the anti-virulence test. The P. mikanianum essential oil showed a potentiating activity of drugs for which resistance exists and an inhibitory effect of one of the main virulence factors of the Candida genus, morphological transition, which has been previously shown to be responsible for causing invasive infections in human tissues.

Evaluation of the Antifungal Activity of the Licania Rigida Leaf Ethanolic Extract against Biofilms Formed by Candida Sp. Isolates in Acrylic Resin Discs.

Candida sp. treatment has become a challenge due to the formation of biofilms which favor resistance to conventional antifungals, making the search for new compounds necessary. The objective of this study was to identify the composition of the Licania rigida Benth. leaf ethanolic extract and to verify its antifungal activity against Candida sp. and its biofilms. The composition identification was performed using the ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS/MS) technique. The antifungal activity of extract and fluconazole against planktonic cells and biofilms was verified through the minimum inhibitory concentration (MIC) following biofilm induction and quantification in acrylic resin discs by reducing tetrazolic salt, with all isolates forming biofilms within 48 h. Six constituents were identified in the extract, and the compounds identified are derivatives from phenolic compounds such as flavonoids (epi) gallocatechin Dimer, epigallocatechin and gallocatechin, Myricetin-O-hexoside, Myricitrin, and Quercetin-O-rhamnoside. The extract reduced biofilm formation in some of the strains analyzed, namely C. tropicalis URM5732, C. krusei INCQS40042, and C. krusei URM6352. This reduction was also observed in the treatment with fluconazole with some of the analyzed strains. The extract showed significant antifungal and anti-biofilm activities with some of the strains tested.

Piper diospyrifolium Kunth.: Chemical analysis and antimicrobial (intrinsic and combined) activities.

The secular use of plants in popular medicine has emerged as a source for the discovery of new compounds capable of curing infections. Among microbial resistance to commercial drugs, species such as Piper diospyrifolium Kunth, which are used in popular therapy, are targets for pharmacological studies. With this in mind, antimicrobial experiments with the essential oil from the P. diospyrifolium (PDEO) species were performed and its constituents were elucidated. The oil compounds were identified by gas chromatography coupled to mass spectrometry (GC/MS). The broth microdilution method with colorimetric readings for bacterial tests (Escherichia coli and Staphylococcus aureus) and spectrophotometric readings for fungal tests (Candida albicans and Candida tropicalis), whose data were used to create a cell viability curve and calculate its IC50 against fungal cells, were used to determine the minimum inhibitory concentration of the oil and its combined action with commercial drugs. The oil's minimal fungicidal concentration and its action over fungal morphological transition were analyzed by subculture and microculture, respectively. Chemical analysis revealed Z-Carpacin, Pogostol and E-Caryophyllene as the most abundant compounds. Results from the intrinsic analysis were considered clinically irrelevant, however the oil presented a synergistic effect against multiresistant E. coli and S. aureus strains when associated with gentamicin, and against the standard and isolated C. tropicalis strains with fluconazole. A fungicidal effect was observed against the C. albicans isolate. Candida spp. hyphae inhibition was verified for all strains at the highest tested concentrations. The P. diospyrifolium essential oil presented a promising effect when associated with commercial drugs and against a fungal virulence factor. Thus, the oil presented active compounds which may help the development of new drugs, however, new studies are needed in order to clarify the oil's mechanism of action, as well as to identify its active constituents.

Chemical composition, antimicrobial, modulator and antioxidant activity of essential oil of Dysphania ambrosioides (L.) Mosyakin & Clemants.

The oil presented the α-Terpinene as the major compound with 54.09% presence. Antibacterial activity demonstrated significant MIC against Staphylococcus aureus (256 µg/mL) and moderate against Pseudomonas aeruginosa (512 µg/mL). The modulating effect of antibiotics was significant against P. aeruginosa potentiating the effect of all the antibiotics tested. The IC50 observed for CT LM 23 was clinically relevant (19.3 µg/mL), similar to that obtained for CA INCQS 40006 (25.2 µg/mL). The combined effect with fluconazole also showed significant results, 0.1 and 22.7 µg/mL, for CT LM 23 and CA INCQS 40006, respectively. For CA LM 77 the IC50 was 101.9 µg/mL and for CT INCQS 40042 a value of 53.3 µg/mL. Regarding the modulation, both were considered of clinical relevance, 3.3 and 6.4 µg/mL. OEDA has low antioxidant activity (>1024 µg/mL). Therefore, the popular use against infections was corroborated by this work.

Chemical identification and antimicrobial potential of essential oil of Piper rivinoides kunth (BETIS-WHITE).

The family Piperaceae is known for presenting in its species flavoring, healing and antimicrobial properties among others. The objective of the present study was: to study the chemical profile of the essential oil of Piper rivinoides (EOPR); to analyze its anti-bacterial and antifungal potential, as well as to evaluate the antifungal and antibiotic-modifying capacity. The chemical constituents were identified by gas chromatography with flame ionization detector (GC-FID), allowing the identification of 7 constituents of a total of 86.99%. E-Isoelemicin was identified as the main constituent of petroleum (40.81%). Clinically relevant MIC results were obtained against fungi in which the inhibitory concentration remained <256 µg/mL, as for Candida albicans 4127 (217.6 µg/mL). The association of EOPR with an antifungal showed a high synergistic affinity against the strains of C. tropicalis 40042 and 4262. We concluded that no intrinsic EOPR activity was observed at any concentrations tested against bacteria. However, EOPR associated with Gentamicin acted synergistically against S. aureus 10 and Escherichia coli 06, but with Erythromycin there was a synergistic effect against Escherichia coli 06, and antagonism with norfloxacin.

A citotoxicidade e a avaliação da atividade antiprotozoária de Melissa officcinalis L (CIDRO-MELISA) / The cytotoxicity activity and evaluation of antiprotozoa Melissa officcinalis L (CIDRO-MELISA)

Introdução: as Leishmanioses correspondem a um complexo de doenças tropicais causada por mais de vinte diferentes espécies de protozoários intracelulares pertencentes ao gênero Leishmania. A Doença de Chagas é uma doença que representa um dos principais problemas de saúde pública em vários países, afetando sobretudo a população carente e rural. Melissa officinalis L., é uma erva perene, uma planta exótica, cuja família é Lamiaceae, que tem sido amplamente utilizada na medicina popular com finalidades terapêuticas. O seu óleo essencial tem sido usado como antioxidante, antimicótica, antifúngica, sedativa e antivirótica. Objetivo: avaliar a citotoxicidade, composição química e atividade antiparasitária do óleo essencial da espécie M. officinalis. Métodos: M. officcinalis foi coletada no município do Crato, CE, Brasil, e foi depositada no herbário da Universidade Regional do Cariri URCA. A análise da composição química do óleo essencial de M. officcinalis, foi realizada através de Cromatografia Gasosa acoplada à Espectrometria de Massas. No estudo da atividade leishmanicida in vitro, utilizou-se formas promastigotas de L. braziliensis e epimastigotas de Trypanosoma cruzi. Para a atividade citotóxica utilizou-se a linhagem de fibroblastos de mamífero NCTC clone 929. Resultados: a través da análise do óleo essencial de M. officcinalis feita por CG/EM, foi possível identificar 12 constituintes que totalizavam 99,83 por cento, dentre os quais alguns foram majoritários: Geranial, Z Citral, 1- Limonene e Carvone. Foi verificado baixa toxicidade contra os fibroblastos. M. officcinalis exibiu maior capacidade para impedir a replicação contra a forma promastigota do protozoário, nas concentrações testadas. Conclusão: a espécie pode ser uma fonte importante na busca de agentes novos e seletivos para o tratamento de doenças tropicais causadas por protozoários, cujas propriedades necessitam ser investigadas quanto aso seus mecanismos(AU)

Introducción: Leishmaniasis corresponde a un complejo de enfermedades tropicales causadas por más de veinte especies diferentes de protozoos intracelulares que pertenece al género Leishmania. La enfermedad de Chagas es una enfermedad que es uno de los principales problemas de salud pública en muchos países, que afectan especialmente a la población pobre y rural. Melissa officinalis L., es una hierba perenne, una planta exótica, cuya familia Lamiaceae, ha sido ampliamente utilizado en la medicina popular para fines terapéuticos. Su aceite esencial se ha usado como un antioxidante, antimicótico, antifúngica, antiviral y sedante. Objetivo: evaluar la citotoxicidad, la composición química y la actividad antiparasitaria del aceite esencial de la especie M. officinalis. Métodos: M. officinalis se recogió en el municipio de Crato, CE, Brasil, y fue depositado en el herbario de la Universidad Regional del Cariri URCA. El análisis de la composición química del aceite esencial de M. officcinalis se realizó por espectrometría de masa de cromatografía de gas. En el estudio de la actividad invitro leishmanicida se utilizó promastigotes L. braziliensis y Trypanosoma cruzi. Para la actividad citotóxica se utilizó la cepa de fibroblastos de mamífero NCTC clon 929. Resultados: a través de análisis de aceite esencial de M. officinalis hizo por GC/ EM se identificó un total de 12 constituyentes 99,83 por ciento, entre los cuales algunos eran mayoría: geranial, Z citral, limoneno y carvona 1. Se comprobó una baja toxicidad contra fibroblastos. M. officcinalis exhibió mayor capacidad para evitar la replicación contra la forma promastigote de parásito, a las concentraciones ensayadas. Conclusión: la especie puede ser una fuente importante en la búsqueda de nuevos agentes y selectivos para el tratamiento de enfermedades tropicales causadas por protozoos, cuyas propiedades deben ser investigados con respecto a sus mecanismos(AU)

Introduction: Leishmaniasis is a complex of tropical diseases caused by more than twenty different species of intracellular protozoa from the genus Leishmania. Chagas disease is one of the main public health problems in many countries. It mostly affects the poor, rural population. Melissa officinalis L. is a perennial herb, an exotic plant from the family Lamiaceae which has been widely used in folk medicine for therapeutic purposes. Its essential oil has been used as antioxidant, antifungal, antiviral and sedative. Objective: Evaluate the cytotoxicity, chemical composition and antiparasitic activity of essential oil of the species M. officinalis. Methods: M. officinalis specimens were collected from the municipality of Crato, CE, Brazil, and deposited in the herbarium at the Regional University of Cariri (URCA). Analysis of the chemical composition of essential oil of M. officinalis was performed by gas chromatography / mass spectrometry. L. braziliensis and Trypanosoma cruzi promastigotes were used for the study of in vitro leishmanicidal activity. Mammalian fibroblast strain NCTC clone 929 was used to evaluate cytotoxic activity. Results: Analysis of essential oil from M. officinalis by GC / MS led to identification of a total 12 constituents 99.83 percent, among which some were a majority: geranial, Z citral, limonene and 1-carvone. Toxicity against fibroblasts was found to be low. M. officinalis displayed greater capacity to avoid replication against the promastigote form of the parasite at the concentrations assayed. Conclusion: The species may be an important source of new agents and selective media for the treatment of tropical diseases caused by protozoa, whose properties should be studied with respect to their mechanisms(AU)

A citotoxicidade e a avaliação da atividade antiprotozoária de Melissa officcinalis L (CIDRO-MELISA) / Actividad citotóxica y evaluación antiparasitaria de Melissa officcinalis L. (CIDRO-MELISA) / The cytotoxicity activity and evaluation of antiprotozoa Melissa officcinalis L (CIDRO-MELISA)

Introdução: as Leishmanioses correspondem a um complexo de doenças tropicais causada por mais de vinte diferentes espécies de protozoários intracelulares pertencentes ao gênero Leishmania. A Doença de Chagas é uma doença que representa um dos principais problemas de saúde pública em vários países, afetando sobretudo a população carente e rural. Melissa officinalis L., é uma erva perene, uma planta exótica, cuja família é Lamiaceae, que tem sido amplamente utilizada na medicina popular com finalidades terapêuticas. O seu óleo essencial tem sido usado como antioxidante, antimicótica, antifúngica, sedativa e antivirótica. Objetivo: avaliar a citotoxicidade, composição química e atividade antiparasitária do óleo essencial da espécie M. officinalis. Métodos: M. officcinalis foi coletada no município do Crato, CE, Brasil, e foi depositada no herbário da Universidade Regional do Cariri URCA. A análise da composição química do óleo essencial de M. officcinalis, foi realizada através de Cromatografia Gasosa acoplada à Espectrometria de Massas. No estudo da atividade leishmanicida in vitro, utilizou-se formas promastigotas de L. braziliensis e epimastigotas de Trypanosoma cruzi. Para a atividade citotóxica utilizou-se a linhagem de fibroblastos de mamífero NCTC clone 929. Resultados: a través da análise do óleo essencial de M. officcinalis feita por CG/EM, foi possível identificar 12 constituintes que totalizavam 99,83 por cento, dentre os quais alguns foram majoritários: Geranial, Z Citral, 1- Limonene e Carvone. Foi verificado baixa toxicidade contra os fibroblastos. M. officcinalis exibiu maior capacidade para impedir a replicação contra a forma promastigota do protozoário, nas concentrações testadas. Conclusão: a espécie pode ser uma fonte importante na busca de agentes novos e seletivos para o tratamento de doenças tropicais causadas por protozoários, cujas propriedades necessitam ser investigadas quanto aso seus mecanismos(AU)

Introducción: Leishmaniasis corresponde a un complejo de enfermedades tropicales causadas por más de veinte especies diferentes de protozoos intracelulares que pertenece al género Leishmania. La enfermedad de Chagas es una enfermedad que es uno de los principales problemas de salud pública en muchos países, que afectan especialmente a la población pobre y rural. Melissa officinalis L., es una hierba perenne, una planta exótica, cuya familia Lamiaceae, ha sido ampliamente utilizado en la medicina popular para fines terapéuticos. Su aceite esencial se ha usado como un antioxidante, antimicótico, antifúngica, antiviral y sedante. Objetivo: evaluar la citotoxicidad, la composición química y la actividad antiparasitaria del aceite esencial de la especie M. officinalis. Métodos: M. officinalis se recogió en el municipio de Crato, CE, Brasil, y fue depositado en el herbario de la Universidad Regional del Cariri URCA. El análisis de la composición química del aceite esencial de M. officcinalis se realizó por espectrometría de masa de cromatografía de gas. En el estudio de la actividad invitro leishmanicida se utilizó promastigotes L. braziliensis y Trypanosoma cruzi. Para la actividad citotóxica se utilizó la cepa de fibroblastos de mamífero NCTC clon 929. Resultados: a través de análisis de aceite esencial de M. officinalis hizo por GC/ EM se identificó un total de 12 constituyentes 99,83 por ciento, entre los cuales algunos eran mayoría: geranial, Z citral, limoneno y carvona 1. Se comprobó una baja toxicidad contra fibroblastos. M. officcinalis exhibió mayor capacidad para evitar la replicación contra la forma promastigote de parásito, a las concentraciones ensayadas. Conclusión: la especie puede ser una fuente importante en la búsqueda de nuevos agentes y selectivos para el tratamiento de enfermedades tropicales causadas por protozoos, cuyas propiedades deben ser investigados con respecto a sus mecanismos(AU)

Introduction: Leishmaniasis is a complex of tropical diseases caused by more than twenty different species of intracellular protozoa from the genus Leishmania. Chagas disease is one of the main public health problems in many countries. It mostly affects the poor, rural population. Melissa officinalis L. is a perennial herb, an exotic plant from the family Lamiaceae which has been widely used in folk medicine for therapeutic purposes. Its essential oil has been used as antioxidant, antifungal, antiviral and sedative. Objective: Evaluate the cytotoxicity, chemical composition and antiparasitic activity of essential oil of the species M. officinalis. Methods: M. officinalis specimens were collected from the municipality of Crato, CE, Brazil, and deposited in the herbarium at the Regional University of Cariri (URCA). Analysis of the chemical composition of essential oil of M. officinalis was performed by gas chromatography / mass spectrometry. L. braziliensis and Trypanosoma cruzi promastigotes were used for the study of in vitro leishmanicidal activity. Mammalian fibroblast strain NCTC clone 929 was used to evaluate cytotoxic activity. Results: Analysis of essential oil from M. officinalis by GC / MS led to identification of a total 12 constituents 99.83 percent, among which some were a majority: geranial, Z citral, limonene and 1-carvone. Toxicity against fibroblasts was found to be low. M. officinalis displayed greater capacity to avoid replication against the promastigote form of the parasite at the concentrations assayed. Conclusion: The species may be an important source of new agents and selective media for the treatment of tropical diseases caused by protozoa, whose properties should be studied with respect to their mechanisms(AU)

Antimicrobial Activity and Modulatory Effect of Essential Oil from the Leaf of Rhaphiodon echinus (Nees & Mart) Schauer on Some Antimicrobial Drugs.

BACKGROUND: Rhaphiodon echinus is a weed plant used in the Brazilian folk medicinal for the treatment of infectious diseases. In this study, the essential oil of R. echinus leaf was investigated for its antimicrobial properties. METHODS: The chemical constituents of the essential oil were characterized by GC-MS. The antimicrobial properties were determined by studying by the microdilution method the effect of the oil alone, and in combination with antifungal or antibiotic drugs against the fungi Candida albicans, Candida krusei and Candida tropicalis and the microbes Escherichia coli, Staphylococcus aureus and Pseudomonas. In addition, the iron (II) chelation potential of the oil was determined. RESULTS: The results showed the presence of ß-caryophyllene and bicyclogermacrene in major compounds, and revealed a low antifungal and antibacterial activity of the essential oil, but a strong modulatory effect on antimicrobial drugs when associated with the oil. The essential oil showed iron (II) chelation activity. CONCLUSIONS: The GC-MS characterization revealed the presence of monoterpenes and sesquiterpenes in the essential oil and metal chelation potential, which may be responsible in part for the modulatory effect of the oil. These findings suggest that essential oil of R. echinus is a natural product capable of enhancing the antibacterial and antifungal activity of antimicrobial drugs.

Avaliação da atividade antimicrobiana e moduladora do extrato etanólico de Libidibia ferrea (Mart. ex Tul.) L.P. Queiroz / Evaluación de la actividad antimicrobiana y modulatória del extracto etanólico de Libidibia ferrea (Mart. ex Tul.) L.P. Queiroz / Evaluation of antimicrobial and modulatory activity of the ethanol extract of Libidibia ferrea (Mart. ex Tul.) L.P. Queiroz

Introdução: Staphylococcus aureus é mencionada na literatura como um importante patógeno, algumas espécimes acarretam infecções oportunistas em muitos animais e homens. Escherichia coli é uma das principais causas de doenças infecciosas humanas. Pertencente à família das Enterobacteriaceae, compartilham diversos fatores de virulência descrita por sua resistência a vários antibióticos, as contaminações são provavelmente iniciadas por modificações de defesas do hospedeiro. Pseudomonas aeruginosaé conhecida por causar infecção aguda pela produção de toxinas. Objetivo: avaliar o efeito antimicrobiano do extrato etanólico de Libidibia ferrea (Mart. ex Tul.) L.P. Queiroz, e modulação da atividade antibiótica. Métodos: o material botânico de Libidibia ferrea foi coletado no município de Penaforte, Ceará, Brasil. Para a obtenção dos extratos foram coletadas entrecasca e vagem frescas, submersos em etanol separadamente por 72 h, sendo após esse período, filtrado e concentrado em condensador rotativo a vácuo. Foram realizados testes de atividade antimicrobiana e modulação da atividade antimicrobiana com cepas padrões e multirresistentes de bactérias. Resultados: o extrato demonstrou atividade moduladora quando combinados com alguns antimicrobianos contra algumas linhagens testadas. Conclusões: portanto, é sugerido que o extrato de L. ferrea pode ser utilizada como uma fonte de produtos naturais na terapêutica antimicrobiana e no combate a multirresistência bacteriana(AU)

Introducción: Staphylococcus aureus se menciona en la literatura como un patógeno importante, algunos provocan infecciones oportunistas en animales y hombres. Escherichia coli es una de las principales causas de enfermedades infecciosas humanas. Ambas pertenecen a la familia Enterobacteriaceae, comparten muchos factores de virulencia y se caracterizan por su resistencia a múltiples antibióticos, su contaminación tal vez iniciada por la modificación de las defensas del hospedero. Pseudomonas aeruginosa causa de infección aguda mediante la producción de toxinas. Objetivo: evaluar el efecto antimicrobiano del extracto de etanol de Libidibia ferrea (Mart ex Tul.) LP Queiroz, y la modulación de la actividad antibiótica. Métodos: L. ferrea fue recopilada en el municipio de Penaforte, Ceará, Brasil. Para obtener los extractos se recogieron corteza y frutos frescos, sumergidos en etanol por separado durante 72 h, después se filtraron y se concentraron en un condensador rotatorio. Se realizaron pruebas de actividad antimicrobiana y la modulación de la actividad antimicrobiana con cepas multirresistentes de bacterias. Resultados: los extractos mostraron actividad moduladora cuando se combina con algunos antibióticos contra algunas cepas ensayadas. Conclusión: por lo tanto, se sugiere que el extracto de L. ferrea puede ser utilizado como una fuente de productos naturales en la terapia antimicrobiana y en la resistencia a múltiples fármacos bacteriana combate(AU)

Introduction: Staphylococcus aureus is mentioned in the literature as an important pathogen, some opportunistic bacteria may cause several problems in many animals and humans. Escherichia coli is a leading cause of human infectious diseases. Belonging to the family Enterobacteriaceae, share many virulence factors described by their resistance to multiple antibiotics, the contamination is probably initiated by modifications in the host defenses. Pseudomonas aeruginosa is known to cause acute infection by producing toxins. Objective: evaluate the antimicrobial effect of the ethanol extract of Libidibia ferrea (Mart ex Tul.) LP Queiroz, and modulation of antibiotic activity. Methods: L. ferrea was collected in the municipality of Penaforte, Ceará, Brazil. To obtain the extracts were collected bark and fruits, submerged in ethanol separately for 72 h, after this period, filtered and concentrated in a rotary vacuum condenser. Antimicrobial activity tests were performed and modulation of antimicrobial activity with standards and multiresistant strains of bacteria. Results: the extract showed antibacterial activity when combined with some antibiotics against the assayed strains, demonstrating a modulatory potential. Conclusion: therefore, it is suggested that L. ferrea extract can be used as a source of natural products in the antimicrobial therapy and in the combat bacterial multidrug resistance(AU)

Atividade antibacteriana e moduladora de Cecropia pachystachya Trécul sobre a ação de aminoglicosídeos / Antibacterial and modulatory activity of Cecropia pachystachya Trécul on the action of aminoglycosides / Actividad antibacteriana y moduladora de Cecropia pachystachya Trécul en la acción de los aminoglucósidos

Introdução: a Cecropia pachystachya Trécul., é conhecida como toré (Urticaceae), com ocorrência em todo o território brasileiro, usada na medicina popular no tratamento de infecções respiratórias e gonorreia. Objetivo: avaliar a atividade antibacteriana e moduladora sobre antibióticos, do extrato etanólico e frações metanólicas das folhas e caule de C. pachystachya T., contra linhagens bacterianas padrões e multirresistentes. Métodos: o material vegetal (folhas e caule), coletado na Chapada do Araripe, foi triturado e submerso em solvente etanol PA, e submetido à destilação do solvente no aparelho evaporador rotativo para a produção dos extratos, que foi particionado e submetido ao solvente metanólico, fornecendo as frações metanólicas. Um ensaio de microdiluição foi realizado para verificar a atividade antibacteriana e as possíveis interações dos aminoglicosídeos associados às amostras estudadas, utilizando uma concentração sub-inibitória de 128 µg/mL (CIM/8). Resultados: o efeito mais representativo a associação da neomicina com o EEFCP (Extrato Etanólico das Folhas de C. pachystachya T) e sua fração com redução da CIM de 312.5 para 39,06 µg/mL e redução de 312,50 para 78,13 µg/mL, respectivamente ambos contra Staphylococcus aureus 358. Quando frente a E. coli 27, foi observado antagonismo. Conclusões: os dados obtidos indicam que o extrato e as frações metanólicas de C. pachystachya, podem ser uma alternativa relevante na pesquisa de substâncias que tenham ação contra as bactérias Staphylococcus multirresistentes. Entretanto, o mesmo também pode interferir negativamente na ação das drogas testadas. Contudo são necessários novos teste in vivo para melhor comprovar essa ação.

Introduction: Cecropia pachystachya Trécul, commonly known as 'toré' (Urticaceae) and distributed throughout Brazil, is used in folk medicine to treat respiratory and sexually transmitted infections such as gonorrhea. Objective: evaluate the antibacterial and modulatory activity on antibiotics of the ethanolic extract and methanolic fractions of C. pachystachya T. leaves and stems against standard and multiresistant bacterial strains. Methods: the plant material (leaves and stems) was collected in Araripe, crushed and put into ethanol PA as solvent. Distillation of the solvent was then performed in a rotary evaporator to produce the extracts, which were divided and subjected to the methanolic solvent to obtain the fractions. A microdilution assay was conducted to verify antibacterial activity and the possible interactions of aminoglycosides associated with the study samples. A sub-inhibitory concentration of 128 ?g/mL (MIC/8) was used. Results: the most representative effect was the association of neomycin with EEFCP (ethanolic extract of leaves of C. pachystachya T.) and its fraction, with a MIC reduction of 312.5 for 39.06 µg/mL and 312.50 for 78.13 µg/mL, respectively, against Staphylococcus aureus 358. An antagonistic effect was observed against E. coli 27. Conclusions: the data obtained indicate that C. pachystachya methanolic fractions and extract may be an important alternative in the search for substances with an action against multiresistant Staphylococcus bacteria. However, such a substance may also negatively affect the action of the drugs studied. It is necessary to conduct new experiments in vivo to verify such an action.

Introducción: Cecropia pachystachya Trécul., es conocida como "toré" (Urticaceae), presente en todo el territorio brasileño, utilizada en la medicina popular para el tratamiento de infecciones respiratorias y de transmisión sexual (gonorrea). Objetivo: evaluar la actividad antibacteriana y moduladora sobre antibióticos del extracto etanólico y fracciones metanólicas de las hojas y tallo de C. pachystachya T. contra cepas bacterianas estándar y multirresistentes. Métodos: el material vegetal (hojas y tallos), colectado en el Araripe, fue triturado y sumergido en etanol PA como solvente. Seguidamente, fue sometido a destilación del solvente en un evaporador rotativo para la producción de los extractos, que fueron divididos y sometidos al solvente metanólico, formando así las fracciones. Se llevó a cabo un ensayo de microdilución para verificar la actividad antibacteriana y las posibles interacciones de aminoglucósidos asociados con las muestras estudiadas, se utilizó una concentración sub-inhibitoria de 128 µg/mL (CIM/8). Resultados: el efecto más representativo resultó el de la asociación de neomicina con el EEFCP (Extrato Etanólico de hojas de C. pachystachya T) y su fracción con disminución de la CIM de 312,5 para 39,06 µg/mL y 312,50 para 78,13 µg/mL, respectivamente contra Staphylococcus aureus 358. Se observó un efecto antagónico contra E. coli 27. Conclusiones: los datos obtenidos indican que el extracto y fracciones metanólicas de C. pachystachya, pueden ser una alternativa importante en la búsqueda de sustancias que tienen acción contra las bacterias Staphylococcus multirresistentes. Sin embargo, puede afectar negativamente a la acción de las drogas estudiadas. No obstante, es necesario realizar nuevos experimentos in vivo para comprobar esta acción.