RESUMO
Bioactive compounds derived from secondary metabolism in animals have refined selectivity and potency for certain biological targets. The superfamily Dendrobatoidea is adapted to the dietary sequestration and secretion of toxic alkaloids, which play a role in several biological activities, and thus serve as a potential source for pharmacological and biotechnological applications. This article constitutes a scoping review to understand the trends in experimental research involving bioactive alkaloids derived from Dendrobatoidea based upon scientometric approaches. Forty-eight (48) publications were found in 30 journals in the period of 60 years, between 1962 and 2022. More than 23 structural classes of alkaloids were cited, with 27.63% for batrachotoxins, 13.64% for pyridinics, with an emphasis on epibatidine, 16.36% for pumiliotoxins, and 11.82% for histrionicotoxins. These tests included in vivo (54.9%), in vitro (39.4%), and in silico simulations (5.6%). Most compounds (54.8%) were isolated from skin extracts, whereas the remainder were obtained through molecular synthesis. Thirteen main biological activities were identified, including acetylcholinesterase inhibitors (27.59%), sodium channel inhibitors (12.07%), cardiac (12.07%), analgesic (8.62%), and neuromuscular effects (8.62%). The substances were cited as being of natural origin in the "Dendrobatidae" family, genus "Phyllobates," "Dendrobates," and seven species: Epipedobates tricolor, Phyllobates aurotaenia, Oophaga histrionica, Oophaga pumilio, Phyllobates terribilis, Epipedobates anthonyi, and Ameerega flavopicta. To date, only a few biological activities have been experimentally tested; hence, further studies on the bioprospecting of animal compounds and ecological approaches are needed.
Assuntos
Alcaloides , Peçonhas , Animais , Acetilcolinesterase , Anuros/metabolismo , Batraquiotoxinas/química , Alcaloides/química , Alcaloides/metabolismoRESUMO
This work aimed to prepare a nanoemulsion containing the essential oil of the Protium heptaphyllum resin and evaluate its biocidal activities against the different stages of development of the Aedes aegypti mosquito. Ovicide, pupicide, adulticide and repellency assays were performed. The main constituents were p-cymene (27.70%) and α-pinene (22.31%). The developed nanoemulsion showed kinetic stability and monomodal distribution at a hydrophilic-lipophilic balance of 14 with a droplet size of 115.56 ± 1.68 nn and a zeta potential of -29.63 ± 3.46 mV. The nanoemulsion showed insecticidal action with LC50 0.404 µg·mL-1 for the ovicidal effect. In the pupicidal test, at the concentration of 160 µg·mL-1, 100% mortality was reached after 24 h. For adulticidal activity, a diagnostic concentration of 200 µg·mL-1 (120 min) was determined. In the repellency test, a concentration of 200 µg·mL-1 during the 180 min of the test showed a protection index of 77.67%. In conclusion, the nanobiotechnological product derived from the essential oil of P. heptaphyllum resin can be considered as a promising colloid that can be used to control infectious disease vectors through a wide range of possible modes of applications, probably as this bioactive delivery system may allow the optimal effect of the P. heptaphyllum terpenes in aqueous media and may also induce satisfactory delivery to air interfaces.
Assuntos
Aedes/efeitos dos fármacos , Inseticidas/química , Inseticidas/farmacologia , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Sapindaceae/química , Animais , Relação Dose-Resposta a Droga , Estabilidade de Medicamentos , Emulsões , Estrutura Molecular , Nanopartículas , Resinas Vegetais/químicaRESUMO
The essential oil from Rosmarinus officinalis L. (OERO) has bioactive compounds with anti-inflammatory activity. The objective of this study was to evaluate the anti-inflammatory potency of nanoemulsions containing essential oil of Rosmarinus officinalis L. (NOERO, NECHA, NECULT, and NECOM) in vitro and in vivo. This study was accomplished in a quantitative format through tests with diphenyl picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cellular antioxidant activity (CCA), determination of nitric oxide production, cellular viability and anti-inflammatory activity in zebrafish. OERO's were submitted to the analysis-coupled gas chromatography-mass spectrometry (GC-MS), which highlighted 1,8-cineol and camphor as major compounds. NOEROs were obtained by a low-energy method and presenting the medium size smaller than 200 nm. The efficiency of encapsulation by spectrometry and gas chromatographic analysis was 67.61 and 75.38%, respectively. In the CCA assay, all of the samples presented percentage values of inhibition similar to the quercetin pattern, indicating antioxidant activity. In the test for determination of NO·, all of the samples inhibited the production of NO· when compared to LPS, and NOEROS were more effective than OEROS to 5 µg/mL. In the cell viability assay, the cells remained viable after contact with the samples, demonstrating an absence of cytotoxicity. This study showed that all nanoemulsions (NECHA, NECULT, and NECOM) showed no toxicity to macrophages, besides demonstrating antioxidant activity and potentiation of the essential oil effect in the proliferation of viable fibroblasts. Nanoemulsions has also shown the ability to potentiate the anti-inflammatory action of essential oils by exerting immunomodulatory activity by inhibiting the production of the pro-inflammatory mediator nitric oxide. The results obtained with NECHA in zebrafish confirm the hypothesis that prominent terpenic compounds, alpha-pinene, 1,8-cineole, and camphor, became more available at the target sites, inhibiting the inflammatory process in this animal species.
Assuntos
Anti-Inflamatórios/farmacologia , Nanopartículas , Óleos Voláteis/farmacologia , Rosmarinus/química , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Modelos Animais de Doenças , Emulsões , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Inflamação/tratamento farmacológico , Inflamação/patologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Óxido Nítrico/metabolismo , Óleos Voláteis/administração & dosagem , Óleos Voláteis/isolamento & purificação , Tamanho da Partícula , Peixe-ZebraRESUMO
The essential oil was obtained by hydrodistillation and the identification and quantification of components were achieved with the use of GC-MS analysis. The antioxidant activity was evaluated by the method of sequestration of DPPH. Essential oils were used for study the cytotoxic front larvae of Artemia salina. In the evaluation of the antimicrobial activity of essential oils, we employed the disk-diffusion method. The potential larvicide in mosquito larvae of the third stage of development of Aedes aegypti to different concentrations of essential oils was evaluated. The major compounds found in the essential oils of M. piperita were linalool (51.8%) and epoxyocimene (19.3%). The percentage of antioxidant activity was 79.9 ± 1.6%. The essential oil showed LC50 = 414.6 µg/mL front of A. saline and is considered highly toxic. It shows sensitivity and halos significant inhibition against E. coli. The essential possessed partial larvicidal efficiency against A. aegypti.
Assuntos
Mentha piperita/química , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Aedes , Animais , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Artemia/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Inseticidas , LarvaRESUMO
Mercury contamination in the Amazon arising from both natural sources and intensive mining activities in the region is a significant public health concern. This metal is used to separate Au from sediments. Accordingly, this study aimed to assess the impact of mining on mercury contamination in the animal and human populations of the Amazon. This overall objective was pursued through a systematic review of the existing literature to assess the impact of Hg and identify gaps in geographic coverage arising from this assessment. Herein, we employed PECO and PRISMA-ScR protocols to select articles published between 2017 and 2023 based on projected points on a map within the biogeographic boundaries of the Amazon. We found that mercury concentrations increase with trophic levels, reaching high values of 3.7 µg/g in the muscles of predatory fish and 34.9 µg/g in human hair. The mean level of mercury in human hair in the whole (Amazon) region exceeds 6 µg/g, surpassing tolerance levels. Although mining regions show high concentrations of Hg, the highest incidence was observed among populations with fish-based diets. It was concluded that continuous research and monitoring of fish in the region are required in order to accurately assess the risk associated with Hg contamination, especially since fish are the main source of protein in this region.
RESUMO
Endophytic fungi are those that present part of their life cycle in healthy tissues of different plant hosts in symbiosis without causing harm. At the same time, fungus-plant symbiosis makes it possible for microorganisms to synthesize their own bioactive secondary metabolites while in the stationary stage. To accomplish this, the endophytic fungus Trichoderma asperellum was isolated from Bertholletia excelsa (Brazil nut) almonds. The fungus was cultivated and extracted with ethyl acetate, obtaining AM07Ac. Then, using HPTLC (High-performance thin-layer chromatography) and nuclear magnetic resonance (1H NMR), ß-amyrin, kaempferol, and brucine were identified as major compounds. Further in vivo assays in zebrafish demonstrated the activity of AM07Ac on melanogenesis by producing a concentration-response inhibitory effect, which, through an in silico study, proved to be related to the noted major compounds known to inhibit tyrosinase activity. The inhibition of tyrosinase prevents melanin accumulation in skin. Therefore, these results imply the importance of investigating microorganisms and their pharmacological activities, in particular the endophytic fungus Trichoderma asperellum as a generator of active metabolites for melanogenesis modulation.
RESUMO
In this bioremediation study, the fungus Penicillium sp. isolated from kefir grains was evaluated for its resistance to copper in the culture medium. Penicillium sp. was cultivated in liquid medium prepared using 2% malt-agar at pH 7.0. Biomass of the fungus was significantly reduced, but only when 800 mg·L-1 of Cu(NO3)2 copper nitrate was used. The effect on radial growth of the fungus in experiments combining different pH values and the inorganic contaminant showed an inhibition of 73% at pH 4.0, 75% at pH 7.0 and 77% at pH 9.0 in liquid medium. Thus, even though the growth of Penicillium sp. could be inhibited with relatively high doses of copper nitrate, images obtained with scanning electron microscopy showed the preservation of fungal cell integrity. Therefore, it can be concluded that Penicillium sp. isolated from kefir grains can survive while performing bioremediation to minimize the negative effects of copper on the environment through biosorption.
RESUMO
This study evaluated the larvicidal activity of Origanum majorana Linnaeus essential oil, identified the chemical composition, evaluated the antimicrobial, cytotoxic and antioxidant potential. The larvicidal activity was evaluated against larvae of the third stage of Aedes aegypti Linaeus, whereas the chemical composition was identified by gas chromatography coupled to mass spectrometer, the antimicrobial activity was carried out against the bacteria Pseudomonas aeruginosa, Escherichia coli and Staphylococcus auereus, the antioxidant activity was evaluated from of 2.2-diphenyl-1-picryl-hydrazila sequestration and Artemia salina Leach cytotoxicity. Regarding to the results, the larvicidal activity showed that O. majorana L. essential oil caused high mortality in A. aegypti L. larvae. In the chromatographic analysis, the main component found in O. majorana L. essential oil was pulegone (57.05%), followed by the other components verbenone (16.92%), trans-p-menthan-2-one (8.57%), iso-menthone (5.58%), piperitone (2.83%), 3-octanol (2.35%) and isopulegol (1.47%). The antimicrobial activity showed that E. coli and P. aeruginosa bacteria were more sensitive to oil than S. aureus, which was resistant at all concentrations. Essential oil did not present antioxidant activity, but it has high cytotoxic activity against A. salina L.
Assuntos
Aedes/efeitos dos fármacos , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Inseticidas/farmacologia , Larva/efeitos dos fármacos , Óleos Voláteis/farmacologia , Origanum/química , Animais , Antibacterianos/química , Antioxidantes/farmacologia , Bactérias/crescimento & desenvolvimento , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Folhas de Planta/química , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/crescimento & desenvolvimento , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimentoRESUMO
Aedes aegypti is the main vector of dengue fever transmission, yellow fever, Zika, and chikungunya in tropical and subtropical regions and it is considered to cause health risks to millions of people in the world. In this study, we search to obtain new molecules with insecticidal potential against Ae. aegypti via virtual screening. Pyriproxyfen was chosen as a template compound to search molecules in the database Zinc_Natural_Stock (ZNSt) with structural similarity using ROCS (rapid overlay of chemical structures) and EON (electrostatic similarity) software, and in the final search, the top 100 were selected. Subsequently, in silico pharmacokinetic and toxicological properties were determined resulting in a total of 14 molecules, and these were submitted to the PASS online server for the prediction of biological insecticide and acetylcholinesterase activities, and only two selected molecules followed for the molecular docking study to evaluate the binding free energy and interaction mode. After these procedures were performed, toxicity risk assessment such as LD50 values in mg/kg and toxicity class using the PROTOX online server, were undertaken. Molecule ZINC00001624 presented potential for inhibition for the acetylcholinesterase enzyme (insect and human) with a binding affinity value of -10.5 and -10.3 kcal/mol, respectively. The interaction with the juvenile hormone was -11.4 kcal/mol for the molecule ZINC00001021. Molecules ZINC00001021 and ZINC00001624 had excellent predictions in all the steps of the study and may be indicated as the most promising molecules resulting from the virtual screening of new insecticidal agents.
RESUMO
Aeollanthus suaveolens species popularly known as catinga de mulata belongs to the Lamiaceae family. In the Amazon region, it is used in folk medicine for the treatment of gastritis, convulsions of epileptic origin, stomach pain and diarrhea in the form of tea and juice. Essential oils have analgesic, anti-inflammatory, and antimicrobial activity. This study evaluated the chemical composition of the A. suaveolens essential oil, and its cytotoxic, antimicrobial and antioxidant activity on Artemia salina Leach. The plant species was collected in Fazendinha district in the city of Macapa-AP. The essential oil obtained from the process was performed by hydrodistillation and identification of components by gas chromatography coupled with mass spectrometer. The antioxidant activity was evaluated by the kidnapping method of 2,2- diphenyl -1-picrilhidrazil radical, while the cytotoxic activity was assessed using saline A. and the microbiological activity was carried out by microdilution method with Escherichia coli, Salmonella sp. and Staphylococcus aureus bacteria. In a chromatographic analysis, the major constituents found in the essential oil of A. suaveolens were (E) -ß-farnesene (37.615%), Linalool (33.375%), α-Santalene (3.255%) and linalyl acetate (3.222%). The results showed that the Escherichia coli and Salmonella sp. bacteria were more susceptible to MIC 50 mg.mL-1 when compared with the Staphylococcus aureus bacterium MIC 100 mg.mL-1. With respect to MBC concentration of 100 mg.mL-1 it was sufficient to inhibit the growth of E. coli. The essential oil did not show antioxidant activity, however, has a high cytotoxic activity against the A. salina, LC50 8.90 µg.mL-1.