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This study aimed to determine the repellent and insecticidal activity of four essential oils (EOs) from plants collected in the Chocó rain forest, Colombia, against T. castaneum . Conventional hydrodistillation was used to obtain the EOs. The repellent and insecticidal activities were evaluated by the preference area and gas dispersion methods, espectively. Statistical differences (p<0.05) were determined by applying a student's t-test. EOs of Siparuna guianensis, S. conica, Piper marginatum, and Nectandra acutifolia showed excellent repellent properties as the main findings, highlighting S. conicaEO with 84% repellency (1-hµL/cm2), while P. marginatum showed to be bioactive to the dose of 500 µL/mL (72 h), inducing mortality of 100% of the exposed population. In conclusion, the results evidenced the repellent properties of the EOs evaluated against T. castaneum , which allows us to conclude that these plant species are potential natural sources producing bio-repellents that contribute to the integrated control of T. castaneum.
Se evaluaron cuatro aceites esenciales (AEs) de plantas recolectadas en la selva pluvial del Chocó, Colombia, para determinar su actividad repelente e insecticida contra T. castaneum. Los AEs fueron obtenidos por hidrodestilación convencional. Las actividades repelentes e insecticidas se evaluaron por los métodos de área de preferencia y dispersión de gas, respectivamente. Las diferencias significativas (p<0,05) fueron determinadas aplicando una prueba t de student. Los AEs de Siparuna guianensis, S. conica, Piper marginatum y Nectandra acutifolia mostraron excelentes propiedades repelentes, destacando el AE de S. conicacon un 84% de repelencia (1µL/cm2), mientras que el AE de P. marginatummostró ser bioactivo a la dosis de 500 µL/mL (72 h) al inducir la mortalidad del 100% de la población expuesta. Se concluye que estas especies de plantas son fuentes naturales potencialmente viables para la producción de biorepelentes que contribuyan en el control integrado de T. castaneum.
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Tribolium/efeitos dos fármacos , Óleos Voláteis/farmacologia , Inseticidas/farmacologia , Colômbia , Repelentes de Insetos/farmacologiaRESUMO
This work investigated the safety of extracts obtained from plants growing in Colombia, which have previously shown UV-filter/antigenotoxic properties. The compounds in plant extracts obtained by the supercritical fluid (CO2) extraction method were identified using gas chromatography coupled to mass spectrometry (GC/MS) analysis. Cytotoxicity measured as cytotoxic concentration 50% (CC50) and genotoxicity of the plant extracts and some compounds were studied in human fibroblasts using the trypan blue exclusion assay and the Comet assay, respectively. The extracts from Pipper eriopodon and Salvia aratocensis species and the compound trans-ß-caryophyllene were clearly cytotoxic to human fibroblasts. Conversely, Achyrocline satureioides, Chromolaena pellia, and Lippia origanoides extracts were relatively less cytotoxic with CC50 values of 173, 184, and 89 µg/mL, respectively. The C. pellia and L. origanoides extracts produced some degree of DNA breaks at cytotoxic concentrations. The cytotoxicity of the studied compounds was as follows, with lower CC50 values representing the most cytotoxic compounds: resveratrol (91 µM) > pinocembrin (144 µM) > quercetin (222 µM) > titanium dioxide (704 µM). Quercetin was unique among the compounds assayed in being genotoxic to human fibroblasts. Our work indicates that phytochemicals can be cytotoxic and genotoxic, demonstrating the need to establish safe concentrations of these extracts for their potential use in cosmetics.
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Sobrevivência Celular , Fibroblastos , Extratos Vegetais , Protetores Solares , Humanos , Protetores Solares/toxicidade , Protetores Solares/química , Extratos Vegetais/toxicidade , Extratos Vegetais/química , Fibroblastos/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Ensaio Cometa , Salvia/química , Dano ao DNA/efeitos dos fármacos , Células Cultivadas , Lippia/química , Cromatografia Gasosa-Espectrometria de MassasRESUMO
The lack of effective conventional therapie s against dengue has created an interest in herbal preparations as alternative therapies. In the present study, in vitro effects of Cordia curassavica essential oil (EO) on both dengue virus replication and cytokine production were examined. Predictions of molecular interactions between EO compounds and virus and cell proteins were performed with AutoDock Vina. The EO inhibited replication of dengue virus serotypes at IC 50 < 30 µg/mL, and it reduced 87% TNF - α, 67% IL - 8 and 46% IFN - α in LPS - stimulated PBMCs. The main EO compounds were trans - ß - caryophyllene (21.4%), germacrene D (17.8%), α - copaene (16.5%), trans - ß - guaiene (8.2%), and α - pinene (6.0%). The first two compounds, δ - cadinene, α - muurolene, α - cubebene and ß - burbonene were coupled to proteins involved in the TLR - 4 cytokine effector pathway. 3,7 - Guaiadiene was coupled to the viral E and C proteins. This study demonstrates the potential of C. curassavica EO as a starting point for discovering novel therapeutic for dengue.
La falta de terapias eficaces para el dengue ha suscitado interés por preparados herbales como terapias alternativas. En el presente estudio se examinaron efectos in vitro del aceite e sencial (AE) de Cordia curassavica sobre la replicación del virus dengue y producción de citoquinas. Se realizaron predicciones de interacciones moleculares entre los compuestos del AE y proteínas virales y celulares con AutoDock Vina. El AE inhibió la rep licación de serotipos del virus a CI 50 < 30 µg/mL y redujo 87% TNF - α, 67% IL - 8 y 46% IFN - α en MNCP. Los principales compuestos del AE fueron trans - ß - cariofileno, germacreno D, α - copaeno, trans - ß - guaieno y α - pineno. Los dos primeros compuestos, el δ - cadineno, el α - muuroleno, el α - cubebeno y el ß - burboneno se acoplaron a proteínas implicadas en la vía efectora de citoquinas TLR - 4. El 3,7 - guaiadiene se acopló a las proteínas virales E y C. Este estudio demuestra el potencial del AE de C. curassavica como punto de partida para descubrir nuevas tera pias para el dengue.
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Replicação Viral/efeitos dos fármacos , Óleos Voláteis/farmacologia , Citocinas , Cordia/química , Vírus da Dengue/efeitos dos fármacos , Terpenos/análise , Técnicas In Vitro , Ensaio de Imunoadsorção Enzimática , Óleos Voláteis/química , Medicamento Fitoterápico , Cromatografia Gasosa-Espectrometria de MassasRESUMO
Hyptis colombiana (Lamiaceae family), a species also treated as Cantinoa colombiana in a recently segregated genus from Hyptis, is a perennial herb or subshrub native to the Andes of northern South America. H. colombiana leaves are commonly used in traditional medicine to treat respiratory and digestive illnesses. In this study, H. colombiana plants at different phenological stages (vegetative, flowering, and post-flowering) were harvested to obtain essential oils (EOs) and extracts (from fresh plant materials or post-distillation waste) whose chemical compositions and antioxidant activities were determined. H. colombiana EOs distilled by microwave-assisted hydrodistillation were analyzed by GC/MS/FID, and hydroalcoholic extracts obtained from fresh plant materials or post-distillation waste were analyzed by UHPLC-ESI+/--Orbitrap-MS. The antioxidant activity was evaluated by the ABTS+⢠and ORAC assays. The principal compounds found in EOs were sesquiterpene hydrocarbons (65%); specifically, (E)-ß-caryophyllene and germacrene D. Pyranone, rosmarinic acid, rutin, and p-hydroxybenzoic acid were the main constituents in H. colombiana extracts. After analyzing the chemical composition and antioxidant activity (ORAC) of EOs and hydroethanolic extracts from flowering H. colombiana plants, minimal variations were found. It is advisable to harvest H. colombiana plants during their flowering stage to acquire EOs and extracts that can be utilized in the agro-industry of EOs and their natural derivatives.
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Hyptis , Óleos Voláteis , Antioxidantes/farmacologia , Antioxidantes/química , Hyptis/química , Óleos Voláteis/química , Folhas de Planta , Extratos Vegetais/químicaRESUMO
The insertion of circular economy principles into the essential oil (EO) production chain aims to reduce waste generation and make integral use of harvested plant material. Higher profits from integral use with reduced waste generation contribute to the eventual use of the EO value chain as an alternative to illicit crops in Colombia (mostly coca). In this study, Java-type citronella (Cymbopogon winterianus) and palmarosa (C. martinii) plant materials were used in two consecutive processes to obtain EOs and extracts. The residual biomass after EO distillation was subjected to ultrasound-assisted hydroethanolic extraction to afford extracts that contained bioactive compounds. Citronella and palmarosa were distilled with typical EO yields (1.0 ± 0.1% for citronella; 0.41 ± 0.06% for palmarosa; n = 5) either through hydrodistillation assisted by microwave radiation or through steam distillation, and their composition (determined via GC/FID/MS analysis) and physicochemical parameters fell within their ISO standard specifications. The concentration of citronellal, the major compound of citronella oil, was 500 ± 152 mg/g. Geraniol, the main component of palmarosa oil, was found at 900 ± 55 mg/g. The citronella and palmarosa hydroalcoholic extracts (4-11% yield) were analyzed with UHPLC-ESI-Orbitrap-MS, which permitted the identification of 30 compounds, mainly C-glycosylated flavones and hydroxycinnamic acids. Both extracts had similar antioxidant activity values, evaluated using the ABTS+â and ORAC assays (110 ± 44 µmol Trolox®/g extract and 1300 ± 141 µmol Trolox®/g extract, respectively).
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Cymbopogon , Colômbia , Biomassa , Cromatografia Gasosa , Extratos VegetaisRESUMO
Sloanea is a plant genus, native to tropical regions, used in medicinal practices for its anti-inflammatory properties. This study aimed to determine the antioxidant activity, sun protective factor (SPF), and antifungal of extracts obtained from two species of Sloanea and to develop extract-based gels with antioxidants, photoprotective, and anti-Candida albicans effects. Ethanolic extracts from S. medusula and S. calva collected in Chocó, Colombia, were used for antioxidant activity and SPF determination using the DPPH assay and the Mansur equation, respectively. Extracts were characterized using HPLC-MS and used to prepare the gels. The viscosity of the extract-based gels was evaluated using an MCR92 rheometer. In addition, the anti-Candida activity of extracts against five yeasts and anti-C. albicans of gels were evaluated following the Clinical and Laboratory Standards Institute M27, 4th Edition. High DPPH radical scavenging activity (42.4% and 44.7%) and a high SPF value (32.5 and 35.4) were obtained for the extracts of S. medusula and S. calva, respectively. Similarly, extract-based gels showed significant DPPH radical scavenging activity of 54.5% and 53.0% and maximum SPF values of 60 and 57. Extract from S. medusula showed an important antifungal activity against C. albicans (minimal inhibitory concentration (MIC) of 2 µg/mL). In contrast, S. calva extract was active against C. krusei, C. albicans (MIC of 2 µg/mL) and C. tropicalis (MIC of 4 µg/mL). Sloanea medusula gel (0.15%) exhibited an important C. albicans growth inhibition (98%), while with S. calva gel (0.3%) growth inhibition was slightly lower (76%). Polyphenolic and triterpenoid compounds were tentatively identified for S. medusula and S. calva, respectively. Both extracts can be considered promising sources for developing photoprotective gels to treat skin infections caused by C. albicans.
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Salvia aratocensis (Lamiaceae) is an endemic shrub from the Chicamocha River Canyon in Santander (Colombia). Its essential oil (EO) was distilled from the aerial parts of the plant via steam distillation and microwave-assisted hydrodistillation and analyzed using GC/MS and GC/FID. Hydroethanolic extracts were isolated from dry plants before distillation and from the residual plant material after distillation. The extracts were characterized via UHPLC-ESI(+/-)-Orbitrap-HRMS. The S. aratocensis essential oil was rich in oxygenated sesquiterpenes (60-69%) and presented τ-cadinol (44-48%) and 1,10-di-epi-cubenol (21-24%) as its major components. The in vitro antioxidant activity of the EOs, measured via an ABTS+⢠assay, was 32-49 µmol Trolox® g-1 and that measured using the ORAC assay was 1520-1610 µmol Trolox® g-1. Ursolic acid (28.9-39.8 mg g-1) and luteolin-7-O-glucuronide (1.16-25.3 mg g-1) were the major S. aratocensis extract constituents. The antioxidant activity of the S. aratocensis extract, obtained from undistilled plant material, was higher (82 ± 4 µmol Trolox® g-1, ABTS+â¢; 1300 ± 14 µmol Trolox® g-1, ORAC) than that of the extracts obtained from the residual plant material (51-73 µmol Trolox® g-1, ABTS+â¢; 752-1205 µmol Trolox® g-1, ORAC). S. aratocensis EO and extract had higher ORAC antioxidant capacity than the reference substances butyl hydroxy toluene (98 µmol Trolox® g-1) and α-tocopherol (450 µmol Trolox® g-1). S. aratocensis EOs and extracts have the potential to be used as natural antioxidants for cosmetics and pharmaceutical products.
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Óleos Voláteis , Salvia , Antioxidantes/farmacologia , Antioxidantes/química , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Salvia/química , Extratos Vegetais/farmacologia , Extratos Vegetais/químicaRESUMO
The large-scale use of alcohol (OH)-based disinfectants to control pathogenic viruses is of great concern because of their side effects on humans and harmful impact on the environment. There is an urgent need to develop safe and environmentally friendly disinfectants. Essential oils (EOs) are generally recognized as safe (GRAS) by the FDA, and many exhibit strong antiviral efficacy against pathogenic human enveloped viruses. The present study investigated the virucidal disinfectant activity of solutions containing EO and OH against DENV-2 and CHIKV, which were used as surrogate viruses for human pathogenic enveloped viruses. The quantitative suspension test was used. A solution containing 12% EO + 10% OH reduced > 4.0 log10 TCID50 (100% reduction) of both viruses within 1 min of exposure. In addition, solutions containing 12% EO and 3% EO without OH reduced > 4.0 log10 TCID50 of both viruses after 10 min and 30 min of exposure, respectively. The binding affinities of 42 EO compounds and viral envelope proteins were investigated through docking analyses. Sesquiterpene showed the highest binding affinities (from -6.7 to -8.0 kcal/mol) with DENV-2 E and CHIKV E1-E2-E3 proteins. The data provide a first step toward defining the potential of EOs as disinfectants.
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Desinfetantes , Óleos Voláteis , Vírus , Humanos , Óleos Voláteis/farmacologia , Desinfetantes/farmacologia , Desinfetantes/química , Antivirais/farmacologia , EtanolRESUMO
Bacteria can communicate through quorum sensing, allowing them to develop different survival or virulence traits that lead to increased bacterial resistance against conventional antibiotic therapy. Here, fifteen essential oils (EOs) were investigated for their antimicrobial and anti-quorum-sensing activities using Chromobacterium violaceum CV026 as a model. All EOs were isolated from plant material via hydrodistillation and analyzed using GC/MS. In vitro antimicrobial activity was determined using the microdilution technique. Subinhibitory concentrations were used to determine anti-quorum-sensing activity by inhibition of violacein production. Finally, a possible mechanism of action for most bioactive EOs was determined using a metabolomic approach. Among the EOs evaluated, the EO from Lippia origanoides exhibited antimicrobial and anti-quorum activities at 0.37 and 0.15 mg/mL, respectively. Based on the experimental results, the antibiofilm activity of EO can be attributed to the blockage of tryptophan metabolism in the metabolic pathway of violacein synthesis. The metabolomic analyses made it possible to see effects mainly at the levels of tryptophan metabolism, nucleotide biosynthesis, arginine metabolism and vitamin biosynthesis. This allows us to highlight the EO of L. origanoides as a promising candidate for further studies in the design of antimicrobial compounds against bacterial resistance.
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Microbial infections resistant to conventional antibiotics constitute one of the most important causes of mortality in the world. In some bacterial species, such as Escherichia coli and Staphylococcus aureus pathogens, biofilm formation can favor their antimicrobial resistance. These biofilm-forming bacteria produce a compact and protective matrix, allowing their adherence and colonization to different surfaces, and contributing to resistance, recurrence, and chronicity of the infections. Therefore, different therapeutic alternatives have been investigated to interrupt both cellular communication routes and biofilm formation. Among these, essential oils (EO) from Lippia origanoides thymol-carvacrol II chemotype (LOTC II) plants have demonstrated biological activity against different biofilm-forming pathogenic bacteria. In this work, we determined the effect of LOTC II EO on the expression of genes associated with quorum sensing (QS) communication, biofilm formation, and virulence of E. coli ATCC 25922 and S. aureus ATCC 29213. This EO was found to have high efficacy against biofilm formation, decreasing-by negative regulation-the expression of genes involved in motility (fimH), adherence and cellular aggregation (csgD), and exopolysaccharide production (pgaC) in E. coli. In addition, this effect was also determined in S. aureus where the L. origanoides EO diminished the expression of genes involved in QS communication (agrA), production of exopolysaccharides by PIA/PNG (icaA), synthesis of alpha hemolysin (hla), transcriptional regulators of the production of extracellular toxins (RNA III), QS and biofilm formation transcriptional regulators (sarA) and global regulators of biofilm formation (rbf and aur). Positive regulation was observed on the expression of genes encoding inhibitors of biofilm formation (e.g., sdiA and ariR). These findings suggest that LOTCII EO can affect biological pathways associated with QS communication, biofilm formation, and virulence of E. coli and S. aureus at subinhibitory concentrations and could be a promising candidate as a natural antibacterial alternative to conventional antibiotics.
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Nontyphoidal Salmonella species are one of the main bacterial causes of foodborne diseases, causing a public health problem. In addition, the ability to form biofilms, multiresistance to traditional drugs, and the absence of effective therapies against these microorganisms are some of the principal reasons for the increase in bacterial diseases. In this study, the anti-biofilm activity of twenty essential oils (EOs) on Salmonella enterica serovar Enteritidis ATCC 13076 was evaluated, as well as the metabolic changes caused by Lippia origanoides thymol chemotype EO (LOT-II) on planktonic and sessile cells. The anti-biofilm effect was evaluated by the crystal violet staining method, and cell viability was evaluated through the XTT method. The effect of EOs was observed by scanning electron microscopy (SEM) analysis. Untargeted metabolomics analyses were conducted to determine the effect of LOT-II EO on the cellular metabolome. LOT-II EO inhibited S. Enteritidis biofilm formation by more than 60%, without decreasing metabolic activity. Metabolic profile analysis identified changes in the modulation of metabolites in planktonic and sessile cells after LOT-II EO treatment. These changes showed alterations in different metabolic pathways, mainly in central carbon metabolism and nucleotide and amino acid metabolism. Finally, the possible mechanism of action of L. origanoides EO is proposed based on a metabolomics approach. Further studies are required to advance at the molecular level on the cellular targets affected by EOs, which are promising natural products for developing new therapeutic agents against Salmonella sp. strains.
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PURPOSE: The aim of this study was to optimize the immunoresponsive and anti-Candida albicans (C. albicans) properties of guided bone regeneration-resorbable membranes (collagen) using additives based on synergistic mixtures of chlorhexidine with terpene-enriched fractions from Lippia alba essential oils (EO). METHODS: The anti-C. albicans activity of the fractions (individually or combined with chlorhexidine) was evaluated using planktonic and sessile cultures. J774A.1 murine macrophage cells were used to determine the cytotoxicity and immunoresponsive effects of the therapies. RESULTS: The anti-planktonic and anti-sessile performance of chlorhexidine on C. albicans was improved 2- to 4-fold by supplementation with citral-rich fractions. On macrophages, this fraction also exhibited a potentially cytoprotective action against the toxic effects of chlorhexidine, minimizing damage to the cell membrane, mitochondrial membrane potential, and nuclear integrity. Macrophages growing on collagen-membrane fragments and stimulated with the citral fraction (alone or with chlorhexidine) showed a significant increase in releasing the osteogenic cytokine TNF-α and enhancing the IL-4. CONCLUSION: This combined therapy appears as a promising platform for the development of a prophylactic or therapeutic biocidal solution that can optimize the pharmacological characteristics of chlorhexidine (epithelium tolerance and anti-C. albicans consolidation on surfaces), as well as potentiating the immunoresponsive properties of collagen membranes.
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Lippia , Óleos Voláteis , Camundongos , Animais , Óleos Voláteis/farmacologia , Clorexidina , Regeneração ÓsseaRESUMO
Plants of the genus Scutellaria (Lamiaceae) have a wide variety of bioactive secondary metabolites with diverse biological properties, e.g., anti-inflammatory, antiallergenic, antioxidant, antiviral, and antitumor activities. The chemical composition of the hydroethanolic extracts, obtained from dried plants of S. incarnata, S. coccinea, and S. ventenatii × S. incarnata, was determined by UHPLC/ESI-Q-Orbitrap-MS. The flavones were found in a higher proportion. Baicalin and dihydrobaicalein-glucuronide were the major extract components in S. incarnata (287.127 ± 0.005 mg/g and 140.18 ± 0.07 mg/g), in S. coccinea (158.3 ± 0.34 mg/g and 51.20 ± 0.02 mg/g), and in S. ventenatii × S. incarnata (186.87 ± 0.01 mg/g and 44.89 ± 0.06 mg/g). The S. coccinea extract showed the highest antioxidant activity in the four complementary techniques employed to evaluate all extracts: ORAC (3828 ± 3.0 µmol Trolox®/g extract), ABTS+⢠(747 ± 1.8 µmol Trolox®/g extract), online HPLC-ABTS+⢠(910 ± 1.3 µmol Trolox®/g extract), and ß-carotene (74.3 ± 0.8 µmol Trolox®/g extract).
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Antioxidantes , Scutellaria , Antioxidantes/farmacologia , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Colômbia , Fenóis/químicaRESUMO
Cymbopogon nardus (citronella) essential oil (EO) has been widely used in the cosmetic and food industry due to its repellent and fumigant properties. The aim of this study was to evaluate its effects on the life cycle and midgut morphology of the natural predator Ceraeochrysa claveri. Larvae were fed on sugarcane borer eggs (Diatraea saccharalis) pretreated with citronella EO solutions (1-100 µg/mL in methanol, 5 s) or solvent and air-dried at room temperature for 30 min. Larval and pupal stage duration, the percentage of emergence of the insect, and malformed insects were recorded. One day after adults emerged from their cocoons, adult insects were used to obtain their midgut and analyzed using light microscopy. The chemical composition of C. nardus EO revealed that citronellal (25.3%), citronellol (17.9%), geraniol (11.6%), elemol (6.5%), δ-cadinone (3.6%), and germacrene D (3.4%) were the predominant compounds. Exposure to the EO produced a significant change in development duration for third instar and prepupa of the insect. The observed alterations in the lifecycle included prepupae with no cocoon formation, dead pupa inside the cocoon, and malformed adults. Several injuries in the midgut epithelium of exposed adults were registered, such as detachment of columnar cells leaving only swollen regenerative cells fixed on the basement membrane, and the formation of epithelial folds. In summary, these data suggest that C. nardus oil has adverse effects on the life cycle and midgut morphology of a beneficial predator.
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Most Candida species are opportunistic pathogens with the ability to form biofilms, which increases their resistance to antifungal drug therapies and the host immune response. Essential oils (EOs) are an alternative for developing new antimicrobial drugs, due to their broad effect on cellular viability, cell communication, and metabolism. In this work, we evaluated the antifungal and antibiofilm potential of fifty EOs on C. albicans ATCC 10231, C. parapsilosis ATCC 22019, and Candida auris CDC B11903. The EOs' antifungal activity was measured by means of a broth microdilution technique to determine the minimum inhibitory and fungicidal concentrations (MICs/MFCs) against the different Candida spp. strains. The effects on biofilm formation were determined by a crystal violet assay using 96-well round-bottom microplates incubated for 48 h at 35 °C. The EOs from Lippia alba (Verbenaceae family) carvone-limonene chemotype and L. origanoides exhibited the highest antifungal activity against C. auris. The L. origanoides EOs also presented antifungal and antibiofilm activity against all three Candida spp., thus representing a promising alternative for developing new antifungal products focused on yeast infections, especially those related to biofilm formation, virulence factors, and antimicrobial resistance.
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The study aimed to determine the enhanced effects of essential oils (EOs) and plant-derived molecules (PDMs) as penetration enhancers (PEs) for transdermal drug delivery (TDD) of caffeine. A 1% w/w solution of eight EOs and seven PDMs was included in the 1% caffeine carbopol hydrogel. Franz diffusion cell experiments were performed using mice with full-thickness skin. At various times over 24 h, 300 µL of the receptor were withdrawn and replaced with fresh medium. Caffeine was analyzed spectrophotometrically at 272 nm. The skin irritation effects of the hydrogels applied once a day for 21 days were investigated in mice. The steady-state flux (JSS) of the caffeine hydrogel was 30 ± 19.6 µg cm-2 h-1. An increase in caffeine JSS was induced by Lippia origanoides > Turnera diffusa > eugenol > carvacrol > limonene, with values of 150 ± 14.1, 130 ± 47.6, 101 ± 21.7, 90 ± 18.4, and 86 ± 21.0 µg cm-2 h-1, respectively. The Kp of caffeine was 2.8 ± 0.26 cm h-1, almost 2-4 times lower than that induced by Lippia origanoides > Turnera diffusa > limonene > eugenol > carvacrol, with Kp values of 11 ± 1.7, 8.8 ± 4.2, 6.8 ± 1.7, 6.3 ± 1.2, and 5.15 ± 1.0 cm h-1, respectively. No irritating effects were observed. Lippia origanoides, Turnera diffusa, eugenol, carvacrol, and limonene improved caffeine's skin permeation. These compounds may be as effective as the PE in TDD systems.
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Óleos Voláteis , Camundongos , Animais , Óleos Voláteis/farmacologia , Limoneno , Eugenol , Colômbia , Cafeína , Administração Cutânea , HidrogéisRESUMO
Hibiscus rosa-sinensis plants are mainly cultivated as ornamental plants, but they also have food and medicinal uses. In this work, 16 H. rosa-sinensis cultivars were studied to measure their colorimetric parameters and the chemical composition of hydroethanolic extracts obtained from their petals. These extracts were characterized using UHPLC-ESI+-Obitrap-MS, and their antioxidant activity was evaluated using the ORAC assay. The identified flavonoids included anthocyanins derived from cyanidin, glycosylated flavonols derived from quercetin and kaempferol, and flavan-3-ols such as catechin and epicatechin. Cyanidin-sophoroside was the anthocyanin present in extracts of lilac, pink, orange, and red flowers, but was not detected in extracts of white or yellow flowers. The total flavonol concentration in the flower extracts was inversely proportional to the total anthocyanin content. The flavonol concentration varied according to the cultivar in the following order: red < pink < orange < yellow ≈ white, with the extract from the red flower presenting the lowest flavonol concentration and the highest anthocyanin concentration. The antioxidant activity increased in proportion to the anthocyanin concentration, from 1580 µmol Trolox®/g sample (white cultivar) to 3840 µmol Trolox®/g sample (red cultivar).
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Catequina , Hibiscus , Rosa , Flavonoides/análise , Antocianinas/química , Antioxidantes/análise , Hibiscus/química , Flavonóis/química , Catequina/análise , Flores/química , CorRESUMO
Searching for new bioactive molecules to design insecticides is a complex process since pesticides should be highly selective, active against the vector, and bio-safe for humans. Aiming to find natural compounds for mosquito control, we evaluated the insecticidal activity of essential oils (EOs) from 20 American native plants against Aedes aegypti larvae using bioassay, biochemical, and in silico analyses. The highest larvicide activity was exhibited by EOs from Steiractinia aspera (LC50 = 42.4 µg/mL), Turnera diffusa (LC50 = 70.9 µg/mL), Piper aduncum (LC50 = 55.8 µg/mL), Lippia origanoides (chemotype thymol/carvacrol) (LC50 = 61.9 µg/mL), L. origanoides (chemotype carvacrol/thymol) (LC50 = 59.8 µg/mL), Hyptis dilatata (LC50 = 61.1 µg/mL), Elaphandra quinquenervis (LC50 = 61.1 µg/mL), and Calycolpus moritzianus (LC50 = 73.29 µg/mL) after 24 h. This biological activity may be related to the disruption of the electron transport chain through the mitochondrial protein complexes. We hypothesized that the observed EOs' effect is due to their major components, where computational approaches such as homology modeling and molecular docking may suggest the possible binding pose of secondary metabolites that inhibit the mitochondrial enzymes and acetylcholinesterase activity (AChE). Our results provided insights into the possible mechanism of action of EOs and their major compounds for new insecticide designs targeting the mitochondria and AChE activity in A. aegypti for effective and safe insecticide.
Assuntos
Aedes , Asteraceae , Inseticidas , Óleos Voláteis , Animais , Acetilcolinesterase , Asteraceae/química , Inseticidas/farmacologia , Simulação de Acoplamento Molecular , Mosquitos Vetores , Óleos Voláteis/farmacologia , TimolRESUMO
RESUMEN En el trabajo se estudió un consorcio microbiano metanogénico de una mina de carbón de la cuenca de Bogotá en Colombia. Se establecieron cultivos de enriquecimiento de carbón ex situ para el crecimiento y la producción de gas de novo. El gas biogénico producido por los cultivos se analizó mediante cromatografía de gases con detectores de ionización de llama y conductividad térmica. Los cultivos se utilizaron para aislar estirpes microbianas y para generar bibliotecas del gene 16S rARN empleando de cebadores de bacteria y de arquea. El análisis de cromatografía de gases mostró producción de metano a 37 oC, pero no a 60 oC, donde el CO2 fue el componente principal del gas biogénico. El análisis de la secuencia del gen 16S rARN de estirpes microbianos y de las bibliotecas de clones, estableció que el consorcio microbiano metanogénico estuvo formado por especies de bacterias de los géneros Bacillus y Gracilibacter más la arquea del género Methanothermobacter. El consorcio microbiano metanogénico identificado es potencialmente responsable de la generación de gas biogénico en la mina de carbón La Ciscuda. Los resultados sugirieron que los metanógenos de este consorcio producían metano por vía hidrogenotrófica o de reducción de CO2.
ABSTRACT The work studied the methanogenic microbial consortium in a coal mine from the Bogotá basin in Colombia. Ex situ coal-enrichment cultures were established for in vitro growth and de novo gas production. Biogenic gas produced by cultures was analyzed by gas chromatography using thermal conductivity and flame ionization detectors. Cultures were used to isolate microbial specimens and to generate 16S rRNA gene libraries employing bacterial and archaeal primer sets. The gas chromatographic analysis showed methane production at 37 oC, but not at 60 oC, where CO2 was the major component of the biogenic gas. 16S rRNA gene sequence analysis of microbial isolates and clone libraries established that the methanogenic microbial consortium was formed by bacteria species from Bacillus and Gracilibacter genera plus archaea from the Methanothermobacter genus. This meth-anogenic microbial consortium was potentially responsible for biogenic gas generation in La Ciscuda coal mine. The results suggested that these methanogens produced methane by hydrogenotrophic or CO2 reduction pathways.
RESUMO
Obesity is characterized by an expansion of adipose tissue due to excessive accumulation of triglycerides in adipocytes, causing hypertrophy and hyperplasia, followed by hypoxia, alterations in adipocyte functionality, and chronic inflammation. However, current treatments require changes in lifestyle that are difficult to achieve and some treatments do not generate sustained weight loss over time. Therefore, we evaluated the effect of the essential oil (EO) of Lippia alba (Verbenaceae) carvone chemotype on viability, lipid mobilization, and adipogenesis of adipocytes in two normal and pathological cellular models in vitro. In 3T3-L1 adipocytes, a normal and a pathological model of obesity were induced, and then the cells were treated with L. alba carvone chemotype EO to evaluate cell viability, lipid mobilization, and adipogenesis. L. alba carvone chemotype EO does not decrease adipocyte viability at concentrations of 0.1, 1, and 5 µg/mL; furthermore, there was evidence of changes in lipid mobilization and adipogenesis, leading to a reversal of adipocyte hypertrophy. These results could be due to effects produced by EO on lipogenic and lipolytic pathways, as well as modifications in the expression of adipogenesis genes. L. alba carvone chemotype EO could be considered as a possible treatment for obesity, using the adipocyte as a therapeutic target.