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Endophytic fungi residing symbiotically in plant tissues are promising sources of bioactive natural products. This study explored the anti-inflammatory potential of an endophytic fungus isolated from the Brazilian medicinal plant Poincianella pluviosa (Sibipiruna). The extract from the endophyte FPD13 exhibited potential ex vivo anti-inflammatory effects by inhibiting prostaglandin E2 (PGE2) release by 75.22%. Phytochemical analysis using High-Performance Liquid Chromatography (HPLC), Nuclear Magnetic Resonance (NMR), and Liquid Chromatography-High Resolution Mass Spectrometry (LC-HRMS) enabled the isolation and identification of three compounds, including the macrolide Nigrosporolide, the phenyl-propanol Tyrosol, and the terpene Decarestrictine A. Morphological characteristics and Internal Transcribed Spacers region (ITS) sequencing classified fungus FPD13 as Nigrospora zimmermanii. The results reveal the anti-inflammatory potential and chemical diversity of P. pluviosa endophytes, warranting further investigation into the bioactivity and structure elucidation of their bioactive metabolites.
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Neglected tropical diseases are significant causes of death and temporary or permanent disability for millions living in developing countries. Unfortunately, there is no effective treatment for these diseases. Thus, this work aimed to conduct a chemical analysis using HPLC/UV and GC/MS to identify the major constituents of the hydroalcoholic extracts of Capsicum frutescens and Capsicum baccatum fruits, evaluating these extracts and their constituents' schistosomicidal, leishmanicidal and trypanocidal activities. The results obtained for the extracts of C. frutescens are better when compared to those obtained for C. baccatum, which can be related to the different concentrations of capsaicin (1) present in the extracts. The lysis of trypomastigote forms results for capsaicin (1) led to a significant value of IC50 = 6.23 µM. Thus, the results point to capsaicin (1) as a possible active constituent in these extracts.
Asunto(s)
Capsicum , Capsaicina/farmacología , Cromatografía Líquida de Alta Presión , Extractos Vegetales/farmacología , Extractos Vegetales/análisis , Alcanfor/análisis , Mentol/análisis , Frutas/químicaRESUMEN
The use of various herbs and their compounds has been a strategy widely used in the fight against various human diseases. For example, rosmarinic acid, a bioactive phenolic compound commonly found in Rosemary plants (Rosmarinus officinalis Labiatae), has multiple therapeutic benefits in different diseases, such as cancer. Therefore, the study aimed to evaluate in silico and in vitro the inhibition potential of the enzyme Elastase from the porcine pancreas by rosmarinic acid isolated from the plant species R. officinalis Linn. Through Molecular Docking, the mechanism of action was investigated. In addition, rosmarinic acid presented a range of 5-60 µg/mL and significantly inhibited Elastase. At 60 µg/mL, there was an inhibition of 55% on the enzymatic activity. The results demonstrate the inhibition of Elastase by rosmarinic acid, which can lead to the development of new enzyme inhibitors that can be an inspiration for developing various drugs, including anticancer drugs.
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Ácido Rosmarínico , Rosmarinus , Humanos , Elastasa Pancreática , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología , Cinamatos/farmacología , Depsidos/farmacologíaRESUMEN
Plutella xylostella is considered the main pest of cabbage in Brazil and the world, causing damage of up to 100%. Thus, this study evaluated the insecticidal activity of extracts obtained from the fruits, seeds, bark, leaves, and flowers of Handroanthus impetiginosus against the diamondback moth, P. xylostella larvae. The seed extract showed the highest mortality (97.0%) compared to the control treatment. The LC50 values indicated that the seed and flower extracts (0.01003 and 0.01288 mg/L respectively) assumed the highest toxicity to P. xylostella larvae after 24 h of exposure. The results of this study indicated that the seeds extract is the most promising toxic extract, with measured mortality of approximately 97.0% for P. xylostella larvae after 144 h of exposure in kale plants. Seed extract showed the best insecticidal activity. Thus, this extract can be applied to develop an insecticide based on H. impetiginosus seed.
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Applying elicitors in plants growing under natural conditions change the metabolic content of volatile compounds extracted from their tissues. Here, we have investigated how abiotic elicitors influence the volatile composition of the ethyl acetate extract of Anacardium othonianum seedlings propagated in vitro and ex-vitro cultures. Abiotic factors such as salicylic acid, silver nitrate, light quality, and cultivation mode affected the composition of volatile compounds in ethyl acetate extract of A. othonianum leaves seedlings. GC/MS analysis demonstrated that α-tocopherol was the main metabolite in cultures added with chemical elicitors, reaching 22.48 ± 4.06% in the case of 30 µM salicylic acid. Higher concentrations of salicylic acid decreased the amount of α-tocopherol. The addition of AgNO3 had a linear effect on α-tocopherol. Thus, the production of this metabolite indicates that salicylic acid and AgNO3 elicitors positively affect α-tocopherol production at specific concentrations helping to understand how plant culture can be better manipulated.
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Two-spotted spider mite causes significant damage to various crops, often requiring synthetic acaricides for their control. However, the frequent use of these products causes several environmental problems. Thus, this work aimed to evaluate the acaricidal action, using the application by fumigation on female adults of Tetranychus urticae of essential oil from the leaves of Rosmarinus officinalis L., and its major compound, α-pinene. In addition, the essential oil was characterized by gas chromatography and mass spectrometry. α-pinene was the compound with the highest relative area in the oil (29.2%). In fumigation tests, α-pinene showed more significant toxicity than rosemary essential oil on two-spotted spider mite females with LC50 and LC90 values of 1.58 and 49.61 µL/L air, showing the impact of the chemical composition of the essential oil on the biological activity.
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This study demonstrates in vivo analgesic and anti-inflammatory properties of hydroalcoholic extracts of leaves, bark and flowers from the Handroanthus impetiginosus (Bignoniaceae) plant, recognized as 'Ipê roxo' in Brazil. The extracts were evaluated in male Swiss albino mice via oral administration. Moreover, results of the in vivo paw oedema test induced by carrageenan revealed that extracts of leaves and bark displayed relevant anti-inflammatory activity potential at the dosage of 100 mg/kg, 300 mg/kg, and 500 mg/kg. Likewise, the results obtained for leaves and flowers extracts suggested potent analgesic action in the conventional hot plate test. UPLC/MS analysis of the hydroalcoholic extracts samples identified metabolites belonging to several classes, mainly naphthoquinones and iridoids derivatives as well as flavonoids. Thus, the obtained results indicate that the extracts of H. impetiginosus plant parts could be considered as a complementary herbal medicine for the treatment of pain and inflammation disorders.
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Aedes aegypti is the primary vector of virus transmission that causes dengue, yellow fever, chikungunya and zika. The primary prevention method has been vector control and synthetic insecticides that can cause environmental side effects. Thus, the work aimed to evaluate the larvicidal potential of extracts and isolated compounds from Piper cubeba against A. aegypti larvae. The larvicidal activity method was executed according to the World Health Organization protocol. The larvae were analyzed by scanning electron microscopy (SEM). Through molecular docking, the action mechanism was investigated. The hydroalcoholic and hexane extracts showed similar larvicidal activity with LC50 of 191.1 µg/mL and 185.84 µg/mL, respectively. Between isolated compounds, hinokinin presented LC50= 97.74 µg/mL. The SEM analysis showed structural damage to the larva's tegument caused by extracts and isolated compounds. Therefore, the results demonstrate the larvicidal action of hinokinin and extracts, which can lead to the development of new natural larvicides.
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bicyclic [3.2.1] octane neolignans have garnered increasing interest, because of their unique structural features and biological activities. This study describes the isolation and identification of a new bicyclic octane neolignan 1 obtained through fractionation of the crude extract of the stem of Aniba firmula (Lauraceae family). The structure of bicyclic octane neolignan 1 was determined through NMR analysis and mass spectrometry data.
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Lauraceae , Lignanos , Lignanos/química , Octanos , Lauraceae/química , Espectroscopía de Resonancia MagnéticaRESUMEN
The phytochemical investigation of the stem bark crude extract of Aniba firmula (Lauraceae) led to the isolation of undescribed bicyclic [3.2.1] octane neolignans, 1 and 2, characterized by unusual bicyclic patterns and two other known bicyclic neolignans 3 and 4. Anti-inflammatory bicyclic [3.2.1] octane neolignans metabolites were previously reported in the literature, and the A. firmula stands out in the Lauraceae family as a source of potentially bioactive compounds. Thus, herein the anti-inflammatory potential of four isolated compounds from A. firmula was accessed via an ex vivo anti-inflammatory model that included plasmatic quantification of the prostaglandin E2 (PGE2) inflammatory mediator. Compounds 2 and 3 exhibited significant anti-inflammatory activity by inhibiting the production of PGE2 in plasma samples, thus by interference with the cyclooxygenase (COX) inflammatory pathway. Therefore, these findings demonstrate that the bicyclic octane neolignan classes [3.2.1] can present anti-inflammatory potential.
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The Copaifera oleoresins are widely used in folk medicine to treat various diseases. The goal of this study was to develop a validated reverse-phase high-performance liquid chromatography method with photodiode array detection (RP-HPLC-PDA) to quantify eight terpenes: ent-hardwickiic acid, ent-copalic acid, ent-7α-acetoxy hardwickiic acid, ent-16-hydroxy-3,13-clerodadiene-15,18-dioic acid, ent-5,13-labdadiene-15-oic acid, junenol, ent-kaurenoic acid, and 13E-ent-labda-7,13-dien-15-oic acid in the oleoresins of Copaifera pubiflora L. (OCP), Copaifera trapezifolia L. (OCT) and Copaifera langsdorffii L. (OCL). The linearity of the method was confirmed in the range of 20.00-500 µg.mL-1 (r2 > 0.999). The limit of quantification was between 1,05 and 16.89 µg.mL-1. Precision and accuracy ranges were found to be %RSD <0.2 and 96% to 110%, respectively. Based on the obtained results, the developed analytical method is rapid, precise, accurate, and sensitive for quantifying these terpenes in Copaifera's oleoresins.
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Schistosomiasis mansoni is an infectious parasitic disease caused by worms of the genus Schistosoma, and praziquantel (PZQ) is the medication available for the treatment of schistosomiasis. However, the existence of resistant strains reinforces the need to develop new schistosomicidal drugs safely and effectively. Thus, the (±)-licarin A neolignan incorporated into poly-Æ-caprolactone (PCL) nanoparticles and not incorporated were evaluated for their in vivo schistosomicidal activity. The (±)-licarin A -loaded poly(ε-caprolactone) nanoparticles and the pure (±)-licarin A showed a reduction in the number of worm eggs present in spleens of mice infected with Schistosoma mansoni. In addition, the (±)-licarin A incorporated in the concentration of 20 mg/kg and 200 mg/kg reduced the number of worms, presenting percentages of 56.3% and 41.7%, respectively.
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Nanopartículas , Esquistosomiasis mansoni , Esquistosomicidas , Animales , Caproatos , Lactonas , Lignanos , Ratones , Poliésteres , Schistosoma mansoni , Esquistosomiasis mansoni/tratamiento farmacológico , Esquistosomiasis mansoni/parasitología , Esquistosomicidas/farmacología , Esquistosomicidas/uso terapéuticoRESUMEN
Humanity has used propolis since ancient times, and its use as a food supplement has significantly increased. Several reports on propolis´ biological activity and toxicity have highlighted its anti-inflammatory properties, unlike many natural food supplements. This review addresses the anti-inflammatory roles of Brazilian green, brown, and red propolis produced by Apis mellifera, their extracts, isolated compounds, and their mode of action. Despite advances in anti-inflammatory therapies, the development of inflammatory processes in several diseases has been a concern for centuries. Demands for new anti-inflammatory drugs have led to studies on propolis products as diet components to treat and prevent inflammatory disorders. Brazilian green, brown, and red propolis are alternatives for obtaining extracts and compounds of valuable anti-inflammatory properties. PRACTICAL APPLICATIONS: Currently, propolis is a food supplement, and to the best of our knowledge, several studies have shown that despite advances in anti-inflammatory therapies, the inflammatory process continues to be a significant concern. However, due to the demand for new anti-inflammatory drugs, propolis products as dietary components can be used to treat and prevent inflammatory disorders.
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Própolis , Animales , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Abejas , Brasil , Suplementos Dietéticos , Própolis/farmacologíaRESUMEN
Characterized as an acute and chronic parasitic disease, schistosomiasis mansoni has as its central pathology the formation of hepatic granulomas in response to the parasite's eggs trapped in the host's liver. In recent years, research on propolis has grown; however, there is little anthelmintic work on this bee product. In the propolis scenario, Brazilian ones receive attention, with green and red propolis standing out. This study aims to evaluate in vivo the standardized extract of Brazilian green propolis (Pex) against Schistosoma mansoni. The in vivo antiparasitic activity of Pex was conducted in female BALB/c mice infected with S. mansoni and of the three groups treated with Pex (300 mg/kg); G2 (35th to 42nd dpi) reduced the total worm burden by 55.32%, followed by G3 (42nd to 49th dpi) and G4 (49th to 56th dpi), with about 46%. Furthermore, G2 significantly reduced the total egg load in the ileum (59.33%) and showed an increase in the dead eggs. Similarly, histological analysis of the livers showed a significant reduction in the number and diameter of the granulomas. Based on these results, there is an interesting schistosomicidal activity of Pex and its potential against the formation of hepatic granulomas, paving the way for more detailed studies of propolis in the animal model of schistosomiasis mansoni.
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Própolis , Esquistosomiasis mansoni , Animales , Modelos Animales de Enfermedad , Femenino , Granuloma/tratamiento farmacológico , Hígado , Ratones , Ratones Endogámicos BALB C , Schistosoma mansoni , Esquistosomiasis mansoni/tratamiento farmacológicoRESUMEN
Lignan dinitrohinokinin displays important biological activities, which led to the preparation of its poly-ε-caprolactone nanoparticles. Kinetics analysis revealed initially slow drug release followed by a prolonged, moderate release 6 h later due to DNHK diffusion through the polymeric matrix. Molecular dynamics simulations show that DNHK molecules that interact stronger with other DNHK molecules near the PCL/DNHK surface are more difficult to dissociate from the nanoparticle. The smaller diameter nanocapsules with negative surface charge conferred good colloidal stability. The formulations showed a size distribution with monodisperse systems formation. In vivo evaluation of schistosomicidal activity against Schistosoma mansoni showed that DNHK, when incorporated into nanoparticles, caused egg number reduction of 4.2% and 28.1% at 40 mg/kg and 94.2% and 84.4% at 400 mg/kg in the liver and the spleen, respectively. The PCL nanoparticles were stable in aqueous dispersion and could be optimized to be used as a promising lignan release agent.
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Lignanos , Nanopartículas , Esquistosomicidas , Portadores de Fármacos , Lignanos/farmacología , PoliésteresRESUMEN
This work aimed to synthesize poly (D, L-lactic-co-glycolic acid) (PLGA) microparticles containing hinokinin (HNK) and to evaluate their cytotoxic activity against tumoral SiHa cells and non-tumoral HaCaT cells. Hinokinin was incorporated into PLGA (PLGA-HNK) with an encapsulation efficiency of 84.18 ± 2.32%. PLGA and PLGA-HNK were characterized by SEM microscopy and showed spherical morphology with an average size of â¼3.33. Encapsulation efficiency was determined by a calibration curve using UV-vis spectroscopy. PLGA-HNK more active inhibiting proliferation of SiHa cells (IC50 = 14.68 µM) than free HNK (IC50 = 225.5 µM). In relation to HaCaT cells, PLGA-HNK showed no significant difference compared to the negative control. These results led to an increase in HNK bioavailability and thereby, biological activity. In silico prediction analysis suggests that HNK is cytotoxic against SiHa cells with E6 and MDM2 inhibition as possible main mechanism of action.
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Antineoplásicos , Nanopartículas , 4-Butirolactona/análogos & derivados , Antineoplásicos/química , Antineoplásicos/farmacología , Benzodioxoles , Ácido Láctico/química , Lignanos , Nanopartículas/química , Tamaño de la Partícula , Ácido Poliglicólico/química , Copolímero de Ácido Poliláctico-Ácido PoliglicólicoRESUMEN
Cholinesterase (ChE) inhibitors are currently the main drugs used to treat the cognitive symptoms of Alzheimer's disease (AD). Dual cholinesterase inhibitors, that is, compounds capable of inhibiting both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), are considered a new potential approach for the long-term treatment of patients with AD. We evaluated the ethyl acetate extract of Phomopsis sp., grown in liquid medium malt extract and potato dextrose (PDB), an endophyte isolated from the Brazilian medicinal plant Hancornia speciosa. The anticholinesterase (AChE) and butyrylcholinesterase (BuChE) activities were evaluated. The extracts exhibited dual action against AChE and BuChE. The compounds isolated from these extracts, nectriapyrone (1) and tryptophol (2), showed inhibitory action on BuChE (IC50 = 29.05 and 34.15 µM respectively), being selective towards BuChE. The discovery of selective BuChE inhibitors is extremely important for the development of drugs that can be used in the treatment of patients diagnosed with AD.
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Acetilcolinesterasa , Enfermedad de Alzheimer , Alcoholes , Enfermedad de Alzheimer/tratamiento farmacológico , Butirilcolinesterasa , Inhibidores de la Colinesterasa/farmacología , Humanos , Indoles , PhomopsisRESUMEN
Propolis is a bee product that has been used in medicine since ancient times. Although its anti-inflammatory, antioxidant, antimicrobial, antitumor, and immunomodulatory activities have been investigated, its anti-parasitic properties remain poorly explored, especially regarding helminths. This review surveys the results obtained with propolis around the world against human parasites. Regarding protozoa, studies carried out with the protozoa Trypanosoma spp. and Leishmania spp. have demonstrated promising results inâ vitro and inâ vivo. However, there are fewer studies for Plasmodium spp., the etiological agent of malaria and less so for helminths, particularly for Fasciola spp. and Schistosoma spp. Despite the favorable inâ vitro results with propolis, helminth assays need to be further investigated. However, propolis has shown itself to be an excellent natural product for parasitology, thus opening new paths and approaches in its activity against protozoa and helminths.
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Antiparasitarios/farmacología , Fenoles/farmacología , Extractos Vegetales/farmacología , Própolis/química , Animales , Antiparasitarios/química , Antiparasitarios/aislamiento & purificación , Brasil , Helmintos/efectos de los fármacos , Leishmania/efectos de los fármacos , Estructura Molecular , Pruebas de Sensibilidad Parasitaria , Fenoles/química , Fenoles/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Plasmodium/efectos de los fármacos , Trypanosoma/efectos de los fármacosRESUMEN
ATP-Binding Cassette (ABC) transporters are the main class of transmembrane transporters involved in pathogenic fungal resistance against chemotherapeutic agents. Herein we report results which show that batzelladine D (1) and norbatzelladine L (2) reverse the fluconazole resistance phenotype mediated by Pdr5p transporter on Saccharomyces cerevisiae. Both alkaloids were able to chemosensitize the Pdr5p-overexpressing strain by synergistic interaction with fluconazole. Both compounds also showed an inhibitory effect on the catalytic activity and on the intracellular accumulation of rhodamine 6G, and did not show significant in vitro mammalian cells toxicity.
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Alcaloides/farmacología , Fluconazol/farmacología , Poríferos/química , Pirimidinas/farmacología , Rodaminas/antagonistas & inhibidores , Transportadoras de Casetes de Unión a ATP/metabolismo , Alcaloides/química , Alcaloides/aislamiento & purificación , Animales , Células Cultivadas , Relación Dosis-Respuesta a Droga , Ratones , Estructura Molecular , Pirimidinas/química , Pirimidinas/aislamiento & purificación , Rodaminas/metabolismo , Proteínas de Saccharomyces cerevisiae/metabolismo , Relación Estructura-ActividadRESUMEN
The chemotherapy of schistosomiasis remains centered in the use of praziquantel, however, there has been growing resistant parasites to this drug. Thus, the aim of this work was to evaluate inâ vitro schistosomicidal activity of the hexanes/dichloromethane 1 : 1 extract of Brazilian green propolis (Pex), as well as its major isolated compounds artepillin C, caffeic acid, coumaric acid and drupanin against Schistosoma mansoni. The Pex was active by displaying an IC50 value of 36.60 (26.26-51.13)â µg mL-1 at 72 h against adult worms of S. mansoni. The major isolated compounds were inactive with IC50 values >100â µM, however, the combination of the isolated compounds (CM) in the same range found in the extract was active with an IC50 value of 41.17 (39.89-42.46)â µg mL-1 at 72 h. Pex and CM induced alteration in the tegument of S. mansoni, and caffeic acid caused alteration in egg's maturation. Pex displayed inâ vitro activity against adult worms' and eggs' viability of S. mansoni, which opens new perspectives to better understand the synergistic and/or additive effects promoted by both Pex extract and CM against schistosomiasis features.