RESUMEN

The present work describes the extraction of a polyprenylated benzophenone-rich extract from Brazilian red propolis (ERPB), the development and validation of an RP-HPLC-UV method to characterize it, and its evaluation against breast cancer cell lines MCF-7 and MDA-MB-231, as well as the normal counterpart MCF-10 A. A mixture of gutifferone E and xanthochymol (1+2), and isolated oblongifolin B (3) were used as chemical standards for ERPB and were also evaluated. The concentrations of 1+2 and 3 corresponded to 16.68 % and 42.25 % of the total content of the extract, respectively, and the validation parameters evaluated were satisfactorily met. The cytotoxic effects of ERPB were assessed, and the obtained IC50 values were 19.58 µg/mL (MCF-10 A), 11.56 µg/mL (MCF-7), and 5.22 µg/mL (MDA-MB-231). In conclusion, ERPB exhibits promising cytotoxic effects on the tested breast cell lines. However, further investigation to elucidate its potential therapeutic applications and safety profile should be conducted.

RESUMEN

Ginger (Zingiber officinale), a globally distributed plant, is widely used in the industry for its flavourings, seasonings, and beverages. However, maintaining its quality and volatile components during processing has posed a challenge. This study, therefore, aimed to assess the impact of drying time (24, 48, and 72h) in a circulation oven at 40 °C on the chemical composition and yield of fresh and dried ginger. The essential oils were extracted using the hydrodistillation method, and their chemical analysis was conducted using gas chromatography. The drying time in the oven directly influenced the essential oil yield, with a longer time resulting in a higher yield. We identified 27 compounds in the essential oils, varying their predominance depending on the drying time. The PCA analysis revealed that the drying time can lead to the formation of different chemotypes for ginger, indicating that altering the drying time can yield significantly different chemical profiles.

RESUMEN

OBJECTIVE: To investigate the effects of Araucaria sp. brown propolis (ABP) against trinitrobenzenesulfonic acid (TNBS)-induced colitis in rats. METHODS: Animals received vehicle (1% DMSO, 1 ml/kg) or hydroalcoholic extract of ABP (hydroalcoholic extract of Araucaria sp. brown propolis (HEABP), 30, 100, and 300 mg/kg) orally, or dexamethasone (25 mg/kg, s.c.) for 5 days. On day 4, the animals received intracolonic TNBS (150 mg/kg), on day 6 they were euthanized. The weight of the animals, the macroscopic and microscopic colonic damage, reduced glutathione (GSH) and malondialdehyde (MDA) levels, and the activity of glutathione S-transferase (GST), catalase (CAT), superoxide dismutase (SOD), and myeloperoxidase (MPO) were measured in colon homogenate. The action of HEABP and two isolated compounds in neutrophil migration was recorded. KEY FINDINGS: HEABP (100 and 300 mg/kg), but not dexamethasone, decreased colonic lesion, and increased colonic mucin staining. In parallel, HEABP decreased MDA and restored GSH levels and the activity of SOD, CAT, and GST in the colon. A dose-dependent inhibition of MPO activity was observed (LogIC50 = 1.9). Moreover, HEBPA and the junicedric and abietic acids inhibited the neutrophil chemotaxis in vitro and HEBPA reduced neutrophil migration in vivo. CONCLUSION: HEABP may be promising in the therapies for inflammatory bowel diseases, reducing oxidative and inflammatory damage, especially mediated by neutrophils.

Asunto(s)

Colitis Ulcerosa , Malondialdehído , Estrés Oxidativo , Extractos Vegetales , Própolis , Ratas Wistar , Ácido Trinitrobencenosulfónico , Animales , Colitis Ulcerosa/tratamiento farmacológico , Colitis Ulcerosa/inducido químicamente , Colitis Ulcerosa/patología , Colitis Ulcerosa/metabolismo , Própolis/farmacología , Masculino , Estrés Oxidativo/efectos de los fármacos , Ratas , Extractos Vegetales/farmacología , Malondialdehído/metabolismo , Colon/efectos de los fármacos , Colon/patología , Colon/metabolismo , Peroxidasa/metabolismo , Glutatión/metabolismo , Superóxido Dismutasa/metabolismo , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Modelos Animales de Enfermedad , Dexametasona/farmacología , Tracheophyta/química , Catalasa/metabolismo , Relación Dosis-Respuesta a Droga , Antioxidantes/farmacología , Glutatión Transferasa/metabolismo

RESUMEN

Brazilian green propolis is used in folk medicine because of its various biological properties. The hydroalcoholic extract of Brazilian green propolis is characteristic for possessing several pharmacological properties. Phytochemical investigations have attributed some of these properties to the presence of compounds, which were chosen as analytical markers. This paper reports the development and analytical validation using UPLC-MS/MS in MRM mode. Veratraldehyde was used as an internal standard in qualitative and quantitative analyses of the extracts. Relative standard deviation values obtained for intra-day and inter-day precision were lower than 4%. Of the five parameters for robustness, wavelength detection and flow rate were the critical ones. Limits of detection and quantification ranged from 0.300 to 39.500 ng.mL-1 and from 1.400 to 85.00 ng.mL-1, respectively. The recoveries were between 94.00 and 119.00%, with relative standard deviation values around 5.0%. The developed method is precise, sensitive, and reliable for analysing Brazilian green propolis.

RESUMEN

Among the several terpenes existing in nature, Citronellal, a monoterpene aldehyde, deserves to be highlighted for its biological properties that have been pointed out in numerous studies. This work aimed to conduct a literature review on its biological properties. Citronellal is a prominent compound in the essential oils of Cymbopogon genus plants. Apart from being employed as a fragrance ingredient in aromas, fragrances, and cosmetics, it is also used as an intermediate in synthesising (-)-menthol. Various studies have demonstrated Citronellal's potential as an antibacterial compound, particularly anti-Staphylococcus and Escherichia bacteria. Citronellal also has antifungal properties against several fungi, especially fungi of the genus Candida. The studies found showed that Citronellal also has insecticidal, acaricidal, antiparasitic, anaesthetic, antiviral, antioxidant, antinociceptive, cardioprotective, antihypertensive, anti-inflammatory, antidiabetic, and anticancer properties.

RESUMEN

Baccharin is one of the major compounds found in Brazilian green propolis and its botanical source, Baccharis dracunculifolia. Considering the biological effects of propolis and B. dracunculifolia, this study aims to evaluate the analgesic and anti-inflammatory potential of baccharin. The neurodepressor potential was performed by the open field test, analgesia by mechanical stimulation with Dynamic Plantar Aesthesiometer, and by thermal stimulation with Hargreaves apparatus. In addition, the anti-inflammatory potential was achieved by the paw edema assay, histopathological evaluation, and NF-kB expression. Doses of 2.5, 5, and 10 mg/kg of baccharin were evaluated. After euthanasia, plantar tissue was collected and prepared for histology. As a result, analgesic activity was observed at a dose of 10 mg/kg of baccharin in thermal stimulation under an inflammatory process and anti-inflammatory potential at a dose of 5 mg/kg of baccharin from the second hour in the paw edema test. A decrease in cellular infiltrate and down-modulation of NF-kB, besides the reduction of edema in the histopathology was observed. There was no evidence of kidney and liver toxicity and neurodepressive potential at the doses tested. Thus, baccharin has a promising anti-inflammatory effect possibly associated with antiedematogenic activity by inhibiting mediators such as prostaglandins, inhibiting the migration of polymorphonuclear cells, and modulating NF-kB expression.

Asunto(s)

Analgésicos , Antiinflamatorios , Baccharis , Edema , FN-kappa B , Própolis , Animales , Masculino , Ratas , Analgésicos/farmacología , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Baccharis/química , Brasil , Edema/tratamiento farmacológico , Edema/inducido químicamente , FN-kappa B/metabolismo , Própolis/farmacología , Ratas Wistar , Tricotecenos

RESUMEN

Tetranychus urticae, popularly known as spider mite, is a pest that causes several economic losses to crops. Thus, this work evaluated the effect of essential oils from the leaves of Piper macedoi and Piper arboreum on managing T. urticae. The chemical compounds present in essential oils were identified by gas chromatography. Tests were carried out to evaluate the acaricidal activity by fumigation effect and direct contact with T. urticae. The results showed that LC50 values for the essential oils of P. macedoi and P. arboreum in the fumigation effect were 16.15 and 50.53 µL L-1 air, respectively. Using the contact application route, the LC50 values for the essential oil of P. macedoi was 17.16 µL mL-1, and for P arboreum, it was 15.17 µL mL-1. So, this work showed that essential oils of Piper macedoi and Piper arboreum could be used as possible alternative to managing T. urticae.

RESUMEN

Food processing includes operations that transform raw materials into new products, ensuring the preservation and supply of safe food; however, this view is not always understood by consumers who tend to associate any type of processing with something negative and harmful to health. Given this, the objective of this study was to explore the associations of Brazilian consumers in relation to healthy foods, industrialized foods, and ultra-processed foods, as well as to evaluate the role of socio-demographic characteristics and interest in health in these associations. To this end, 512 Brazilians completed a word association task on these three concepts and then answered a questionnaire about interest in health and socio-demographic issues. In general, participants associated "Healthy food" mainly with "Unprocessed products." Conversely, "Industrialized foods" and "Ultra-processed foods" were associated with "Processed products," "Negative perceptions," "Health harm," and "Industry". Despite this, it was found that "Industrialized foods" were also perceived positively, mainly due to convenience. Consumer associations were influenced (p ≤ 0.05) both by interest in health and by socio-demographic profile. Individuals with a high interest in health mainly associated "Industrialized foods" and "Ultra-processed foods" with the presence of preservatives, additives, and pesticides, and with diseases. As for those with low interest in health, there was a greater lack of knowledge of the concepts. Doubts and lack of knowledge were observed for "Industrialized foods" and "Ultra-processed foods," mainly among consumers with low educational level. The results indicate the need to develop communication strategies that reach consumers to facilitate understanding and, in this way, help them to make more conscious food choices.

Asunto(s)

Alimentos Procesados , Alimentos , Pueblos Sudamericanos , Humanos , Brasil , Comunicación

RESUMEN

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.

RESUMEN

Melanoma, an aggressive and potentially fatal skin cancer, is constrained by immunosuppression, resistance, and high toxicity in its treatment. Consequently, there is an urgent need for innovative antineoplastic agents. Therefore, this study investigated the antimelanoma potential of guttiferone E (GE). In an allogeneic murine B16 melanoma model, GE was administered subcutaneously and intraperitoneally. Antitumor evaluation included tumor volume/weight measurements and histopathological and immunohistochemical analysis. Furthermore, the toxicity of the treatments was evaluated through body/organ weights, biochemical parameters, and genotoxicity. Subcutaneous administration of 20 mg/kg of GE resulted in a significant reduction in both tumor volume and weight, effectively suppressing melanoma cell proliferation as evidenced by a decrease in mitotic figures. The tumor growth inhibition rate was equivalent to 54%. This treatment upregulated cleaved caspase-3, indicating apoptosis induction. On the other hand, intraperitoneal administration of GE showed no antimelanoma effect. Remarkably, GE treatments exhibited no toxicity, evidenced by non-significant differences in body weight gain, as well as organ weight, biochemical parameters of nephrotoxicity and hepatotoxicity, and genotoxic damage. This study revealed, for the first time, the efficacy of subcutaneous administration of GE in reducing melanoma, in the absence of toxicity. Furthermore, it was observed that the apoptotic signaling pathway is involved in the antimelanoma property of GE. These findings offer valuable insights for further exploring GE's therapeutic applications in melanoma treatment.

Asunto(s)

Melanoma Experimental , Ratones Endogámicos C57BL , Animales , Melanoma Experimental/tratamiento farmacológico , Melanoma Experimental/patología , Melanoma Experimental/metabolismo , Apoptosis/efectos de los fármacos , Ratones , Masculino , Antineoplásicos/toxicidad , Antineoplásicos/administración & dosificación , Benzofenonas/farmacología , Benzofenonas/administración & dosificación , Benzofenonas/toxicidad , Neoplasias Cutáneas/tratamiento farmacológico , Neoplasias Cutáneas/patología , Proliferación Celular/efectos de los fármacos , Carga Tumoral/efectos de los fármacos , Línea Celular Tumoral , Inyecciones Subcutáneas , Femenino

RESUMEN

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.

Asunto(s)

Ácido Rosmarínico , Rosmarinus , Humanos , Elastasa Pancreática , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología , Cinamatos/farmacología , Depsidos/farmacología

RESUMEN

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/química

RESUMEN

Tomato is one of the most produced and consumed fruits in the world. However, it is a crop that faces several phytosanitary problems, such as fusarium wilt, caused by Fusarium oxysporum. Thus, this study aimed to evaluate citronella and melaleuca essential oils in vitro potential in the fungus F. oxysporum management. The chemical identification of the components in the essential oils was performed by gas chromatography with flame ionization and mass spectrometer detectors. The IC50 and IC90 were determined by linear regression and the percentage of inhibition of the fungus by analysis of variance. The major compounds in citronella essential oil were citronellal, Geraniol, and citronellol; in melaleuca (tea tree) oil were terpinen-4-ol and α-terpinene. Both oils promoted more significant inhibition at concentrations of 1.5 and 2.5 µL/mL, besides not presenting significant differences with commercial fungicides, confirming the high potential for using this control method in agriculture.

Asunto(s)

Cymbopogon , Fungicidas Industriales , Fusarium , Lamiaceae , Aceites Volátiles , Solanum lycopersicum , Aceite de Árbol de Té , Fungicidas Industriales/farmacología , Árboles , Hongos , Aceites Volátiles/farmacología , Aceites Volátiles/química , Té , Enfermedades de las Plantas/microbiología

RESUMEN

Owing to the potentially harmful adverse effects of current anti-inflammatory drugs, there is a need to identify new alternative substances. Thus, this study aimed to perform a phytochemical analysis of A. polyphylla to identify compounds responsible for its anti-inflammatory activity. Several fractions of the A. polyphylla extract were obtained and evaluated in an ex vivo anti-inflammatory assay using fresh human blood. Among the evaluated fractions, the BH fraction displayed the highest percentage of PGE2 inhibition (74.8%) compared to the reference drugs dexamethasone and indomethacin, demonstrating its excellent potential for anti-inflammatory activity. Astragalin (P1), a known 3-O-glucoside of kaempferol, was isolated from the A. polyphylla extract for the first time. In addition, a new compound (P2) was isolated and identified as the apigenin-3-C-glycosylated flavonoid. Astragalin showed moderate PGE2 activity (48.3%), whereas P2 was not anti-inflammatory. This study contributes to the phytochemical studies of A. polyphylla and confirms its anti-inflammatory potential.

Asunto(s)

Acacia , Fabaceae , Humanos , Flavonoides/farmacología , Flavonoides/química , Apigenina/farmacología , Antiinflamatorios/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fabaceae/química , Fitoquímicos

RESUMEN

Strawberry is a food rich in bioactive compounds with great antioxidant potential. However, due to the high incidence of pests that affect crop cultivation, phytosanitary management still lacks control methods for agroecological cultivation. Thus, the present research aimed to evaluate the chemical composition and the potential of the essential oil of the leaves of Piper macedoi in the control of Cerosipha forbesi in laboratory and semi-field conditions. The concentration of essential oil in the leaves of P. macedoi that showed the highest mortality was 2.0 ml/L of oil, with a mortality above 91% under laboratory conditions. A mortality rate of 80% for all concentrations tested was observed after 24 h in all conditions tested. Thus, using essential oil from the leaf of P. macedoi can be a highly viable strategy in managing the aphid C. forbesi since it showed high mortality rates with small doses of oil.

Asunto(s)

Áfidos , Fragaria , Aceites Volátiles , Piper , Animales , Aceites Volátiles/química , Piper/química

RESUMEN

Chagas disease is a public health problem affecting approximately seven million people worldwide. Thus, there is a need to discover drugs for the adequate treatment of this disease because currently available drugs have serious side effects. Therefore, this study aimed to evaluate the in vitro trypanocidal activity of (-)-6,6'-dinitrohinokinin, obtained from the partial synthesis of (-)-hinokinin, on the trypomastigotes and amastigotes forms. For the trypomastigote assay, blood was collected from mice infected with Trypanosoma cruzi through cardiac puncture at the parasitemic peak. The results show that (-)-6,6'-dinitrohinokinin was effective against the trypomastigote forms, presenting an IC50 of 19.83 µM and lysis percentage values ​​of 78.4% and 69.4% at concentrations of 200 and 100 µM, respectively. Molecular docking calculations indicate that (-)-6,6'-dinitrohinokinin favorably interacts with the amino acids present in the active site of the protein trypanothione reductase, a typical target for anti-trypanosomal drug development. According to the results, the (-)-6,6'-dinitrohinokinin showed more significant trypanocidal activity with IC50 of 1.83 µM than benzonidazole positive control with IC50 of 53.2 µM, showing to be a prototype molecule promising for the development of a new antiparasitic drug.

RESUMEN

Jungia floribunda Less. is a shrub belonging to the Asteraceae. The infusion of its leaves has been used, in folk medicine of several South American countries, as anti-inflammatory and hypoglycaemic agent. In the present study, the infusion of leaves from J. floribunda was obtained and its chemical composition was determined by UHPLC-MS associated with molecular network allowing the annotation of flavonoids, sesquiterpene lactones, coumarins, and chlorogenic acid derivatives. Besides, in vitro elastase activity assay was carried out with the infusion. As observed, elastase was inhibited at concentrations ranging from 15 to 240 µg/mL, reaching to 71% of inhibition at the maximum of evaluated concentration. Given that species of plants are promising sources for the discovery of new drugs, these results corroborate the infusion of J. floribunda as a potential source of bioactive compounds for the discovery of new inhibitors for elastase, besides its ethnopharmacological aspects.

RESUMEN

Many species from Myrtaceae have traditionally been used in traditional medicine as anti-inflammatory, antimicrobial, antidiarrheal, antioxidant and antirheumatic, besides in blood cholesterol reduction. In the present work, the anti-inflammatory activity of essential oils from eighteen Myrtaceae spp. were evaluated according to their ex-vivo anti-inflammatory activity in human blood, and the corresponding biomarkers were determined using untargeted metabolomics data and multivariate data analysis. From these studied species, six displayed anti-inflammatory activity with percentage rates of inhibition of PGE2 release above 70%. Caryophyllene oxide (1), humulene epoxide II (2), ß-selinene (3), α-amorphene (4), α-selinene (5), germacrene A (6), ß-bisabolene (7), α-muurolene (8), α-humulene (9), ß-gurjunene (10), myrcene (11), ß-elemene (12), α-cadinol (13), α-copaene (14), E-nerolidol (15) and ledol (16) were annotated as potential anti-inflammatory biomarkers. The results obtained in this study point to essential oils from species of the Myrtaceae family as a rich source of anti-inflammatory agents.

RESUMEN

Propolis is a natural product widely used in folk medicine. Among its various applications, its antiparasitic properties stand out. Due to its great biodiversity, Brazil is a major producer of several types of propolis. This study proposes to evaluate the leishmanicidal properties of the hydroalcoholic extract of propolis collected in the southern region of Brazil (Brown propolis - HEBP) and its main isolated compounds: abietic acid (1), 13-epi-cupressic acid (2), 13-epi-torulosol (3), dehydroabietic acid (4), cis-communic acid (5) and ent-agatic acid (6). In general, the diterpenes did not show activity against the promastigotes of Leishmania (Leishmania) amazonensis at the evaluated concentrations. However, the HEBP was very active with an inhibition concentration of 50% at 8.32 µg/mL. Moreover, transmission electron microscopy (TEM) and scanning electron microscopy (SEM) assays showed morphological and structural alterations in promastigote forms of L. (L.) amazonensis when incubated with HEBP.

RESUMEN

Cutaneous and visceral leishmaniasis are public health problems in Africa, Asia, Europe, and America. The treatment has a high cost and toxicity. Thus, this work aims to evaluate the leishmanicidal activity of alpha-bisabolol and its three synthetic derivatives, P1, P2, and P3, on the promastigotes and amastigotes Leishmania infantum and L. amazonensis forms. Alpha-bisabolol showed the lowest IC50 with 3.43 for L. amazonensis promastigotes, while P1 was the most toxic for L. infantum with an IC50 of 9.10. The derivative P3 was better for the amastigote form, with an IC50 of 3.39 for L. amazonensis. All the compounds effectively decreased the intracellular load of amastigote and its ability to turn promastigote again. Thus, alpha-bisabolol and its three synthetic derivatives were effective in their leishmanicidal activity. Therefore, it can be an option for developing new treatments against leishmaniasis.