RESUMO
Traditional medicine is a frequently utilized method to treat cardiovascular disease and its primary risk factors, including hypertension and dyslipidemia. Aloysia polystachya is a species that is commonly employed to treat various pathological conditions, and it has already been identified as having some cardioprotective effects. This study aimed to investigate the protective effects of the essential oil extracted from the leaves of A. polystachya in a rat model that simulates multiple cardiovascular risk factors. We evaluate the acute toxicity, as well as the cardioprotective effects, by giving different doses of A. polystachya essential oil (1.47 mg/kg, 4.40 mg/kg, and 13.20 mg/kg) over a period of 42 days. The control group was treated with rosuvastatin (5 mg/kg). At the end of the treatments, the renal function, electrocardiography, blood pressure, vascular reactivity, serum biochemical profile, and organ histopathology were evaluated. The main compounds identified in the essential oil of A. polystachya using gas chromatography coupled with mass spectrometry were beta-myrcene (1.08%), limonene (40.13%), and carvone (56.47%). The essential oil of A. polystachya not only lacks acute toxicity but also mitigates the reduction in the excretion of sodium, chloride, and creatinine in urine. Furthermore, it reduces electrocardiographic abnormalities and decreases blood pressure levels. Moreover, this treatment prevents an elevation in markers of inflammation and oxidative stress in the bloodstream. Our findings indicate significant cardioprotective effects of the essential oil of A. polystachya against multiple risk factors for cardiovascular diseases in hypertensive rats.
Assuntos
Cardiotônicos , Doenças Cardiovasculares , Óleos Voláteis , Animais , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Ratos , Masculino , Cardiotônicos/farmacologia , Doenças Cardiovasculares/tratamento farmacológico , Doenças Cardiovasculares/prevenção & controle , Folhas de Planta/química , Modelos Animais de Doenças , Verbenaceae/química , Pressão Sanguínea/efeitos dos fármacos , Ratos Wistar , Fatores de Risco de Doenças CardíacasRESUMO
Carpophilus dimidiatus (Fabricius) (Nitidulidae) and Oryzaephilus mercator (L.) (Silvanidae) are insect pests that cause severe damage in important walnut growing regions in the northwest of Argentina. The current management approaches for these pests involve the use of unsafe phosphorus pesticides whose overuse have led to farmworker poisoning, pest resistance issues, and environmental contamination. Plant extracts, particularly essential oils, are an alternative source of insect control agents. Excito-repellent essential oils can be used to develop ecofriendly tools for managing the pest population without affecting quality and visual appearance of the stored walnuts. Laboratory studies were conducted to assess the excito-repellent effects of C. dimidiatus and O. mercator of 12 essential oils derived from aromatic plants used as food additives and traditional medicine in Argentina: Aloysia citrodora (AC), Aloysia gratissima (AG), Aloysia gratissima var. Gratissima (AGG), Blepharocalyx salicipholius (BS), Hyptis mutabilis (HM), Lippia junelliana (LJ), Lippia turbinata (LT), Mentha x piperita (MP), Minthostachys mollis (MM), Minthostachys verticillata (MV), Origanum vulgare(OV), and Rosmarinus officinalis (RO). The most bioactive EOs (ERijk ≥ 70%) were Aloysia gratissima var. Gratissima (AGG), Minthostachys verticillata, and Lippia junelliana. Their bioactivity profile and chemical space, characterized from GC-MS measures, Generalized Estimating Equations, and Hierarchical Cluster Analysis, revealed that they are mixtures of very functionalized molecules with physicochemical properties similar to those of insecticides with low residual property that enter the insect body through the respiratory system by inhalation. The AGG, MV, and LJ oils are promising as protective agents of walnut products. In our laboratory, studies of their formulations for use in integrated pest management programs are still ongoing.
Assuntos
Repelentes de Insetos , Inseticidas , Óleos Voláteis , Praguicidas , Verbenaceae , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Verbenaceae/química , Inseticidas/toxicidade , Repelentes de Insetos/farmacologiaRESUMO
Medicinal plants belonging to the Verbenaceae family demonstrated antidepressant effects in preclinical studies. Depression is one of the largest contributors to the global health burden of all countries. Plants from the Aloysia genus are traditionally used for affective disorders, and some of them have proven anxiolytic and antidepressant activity. The aim of this work was to evaluate the antidepressant effect of the ethanolic extract of Aloysia gratissima var. gratissima (Agg) and Aloysia virgata var. platyphylla (Avp) in mice. A tail suspension test (TST) and forced swimming test (FST) were conducted after three doses in a period of 24 h and after 7 days of treatment. Imipramine was used as an antidepressant drug. The main results demonstrated that Agg extract reduced the immobility time in mice treated orally for 7 consecutive days when compared to the control group (reduced by about 77%, imipramine 70%). Animals treated with three doses of Avp in a 24-h period had reduced immobility time in the FST (60%), and after 7 days of treatment the reduction was greater (Avp 50, 100, and 200 about 85%; Avp 400, 96.5%; p < 0.0001, imipramine, 77%). LCMS analysis showed the presence of verbascoside, hoffmaniaketone, and hoffmaniaketone acetate in both, A. virgata var. platyphylla and A. gratissima var gratissima. The flavonoids nepetin and 6-hydroxyluteolin were also found in Agg. Both tested extracts demonstrated promising antidepressant-like activity in mice.
Assuntos
Etanol , Verbenaceae , Camundongos , Animais , Imipramina/farmacologia , Extratos Vegetais/uso terapêutico , Verbenaceae/química , Antidepressivos/farmacologia , Antidepressivos/uso terapêuticoRESUMO
Background: Medicinal plants are part of traditional medicine and should be considered a therapeutic alternative for mental diseases. Several plants belonging to the Verbenaceae family have proved useful in treating general anxiety disorders, the most prevalent psychiatric disorders. Objective: This research aimed to verify the extract's safety, the effect on general behavior, and the effect on sleeping time, as well as to evaluate the anxiolytic-like effect of the methanol extract of Aloysia virgata var. platyphylla (Avp), in mice. Methodology: The toxicity test was done according to the OECD guide (mice groups n=5), and general behavior was observed during the assay. Sleeping time was assessed using the pentobarbital-induced hypnosis method (n=8). Male Swiss albino mice (n=6) were treated with 50 to 400 mg/kg of Avp extract and diazepam as a control. The anxiolytic-like effect was tested through the hole board and elevated plus-maze test. Results: The Avp extract has no side effects in tested doses, and no central nervous system depressant activity was noted. A. virgatavar. platyphyllaincreased exploration (number and time) in the hole board. In the elevated plus-maze, increased number and time into open arms were evidenced compared to the control group. Conclusion: With all these results, we concluded that the Avp extract is safe and has a potential anxiolytic-like activity in the animal model used
Antecedentes: Las plantas medicinales forman parte de la medicina tradicional y deben ser consideradas una alternativa terapéutica para las enfermedades mentales. Varias plantas pertenecientes a la familia Verbenaceae han demostrado su utilidad en el tratamiento de los trastornos de ansiedad, uno de los trastornos psiquiátricos más prevalentes. Objetivo: Esta investigación tuvo como objetivo verificar la seguridad del extracto, el efecto sobre el comportamiento general y el efecto sobre el tiempo de sueño, así como evaluar el efecto tipo ansiolítico del extracto metanólico de Aloysia virgata var. platyphylla(Avp), en ratones. Metodología: La prueba de toxicidad se realizó de acuerdo con la guía de la OCDE (grupos de ratones n=5), y se observó el comportamiento general durante el ensayo. El tiempo de sueño se evaluó mediante el método de hipnosis inducida por pentobarbital (n=8). Se trataron ratones albinos suizos macho (n=6) con 50 a 400 mg/kg de extracto de Avp y diazepam como control. El efecto ansiolítico se probó a través de la placa perforada y prueba del laberinto en cruz elevado. Resultados: El extracto de Avp no tiene efectos secundarios en las dosis probadas y no se observó actividad depresora del sistema nervioso central. A. virgata var. platyphylla aumentó la exploración (número y tiempo) en el tablero de agujeros. En el laberinto en cruz elevado, se evidenció un mayor número y tiempo en los brazos abiertos en comparación con el grupo de control. Conclusión: Con todos estos resultados, concluimos que el extracto de Avp es seguro y tiene una potencial actividad ansiolítica en el modelo animal utilizado
Assuntos
Animais , Masculino , Camundongos , Sono/efeitos dos fármacos , Ansiolíticos , Extratos Vegetais/farmacologia , Verbenaceae/química , Modelos AnimaisRESUMO
Aloysia Paláu is an important herbal genus from the Verbenaceae family and possesses numerous remedial properties in the folk medicine of Asian, European, and, in particular, South American countries. Only a few reports have discussed some phytochemical characteristics associated with Aloysia species. Right the lack of an exhaustive report prompted us to organize this review article. Accordingly, besides the ethnobotanical knowledge of Aloysia species, their essential oil profiles, phytochemistry of the polar isolated fractions, and the relevant biological activities are discussed in detail.[Formula: see text].
Assuntos
Óleos Voláteis , Verbenaceae , Etnobotânica , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Palau , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Verbenaceae/químicaRESUMO
Hernandulcin (HE) is a non-caloric sweetener synthesized by the Mexican medicinal plant Phyla scaberrima. Herein we present the results of HE production through cell suspensions of P.â scaberrima as well as the influence of pH, temperature, biosynthetic precursors and potential elicitors to enhance HE accumulation. The incorporation of mevalonolactone (30-400â mg L-1 ) farnesol (30-400â mg L-1 ), AgNO3 (0.025-0.175â M), cellulase (5-60â mg L-1 ; 0.3â units/mg), chitin (20-140â mg L-1 ) and (+)-epi-α-bisabolol (300-210â mg L-1 ) to the cell suspensions, resulted in a differential accumulation of HE and biomass. Among elicitors assayed, chitin, cellulase and farnesol increased HE production from 93.2 to â¼160â mg L-1 but, (+)-epi-α-bisabolol (obtained by a synthetic biology approach) increased HE accumulation up to 182.7â mg L-1 . HE produced by the cell suspensions was evaluated against nine strains from six species of gastrointestinal bacteria revealing moderate antibacterial activity (MIC, 214-465â µg mL-1 ) against Staphylococcus aureus, Escherichia coli and Helicobacter pylori. Similarly, HE showed weak toxicity against Lactobacillus sp. and Bifidobacterium bifidum (>1â mg mL-1 ), suggesting a selective antimicrobial activity on some species of gut microbiota. According to our results, chitin and (+)-epi-α-bisabolol were the most effective molecules to enhance HE accumulation in cell suspensions of P.â scaberrima.
Assuntos
Antibacterianos/farmacologia , Sesquiterpenos/farmacologia , Verbenaceae/química , Antibacterianos/química , Antibacterianos/metabolismo , Bifidobacterium bifidum/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Helicobacter pylori/efeitos dos fármacos , Lactobacillus/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Sesquiterpenos/química , Sesquiterpenos/metabolismo , Staphylococcus aureus/efeitos dos fármacos , Verbenaceae/citologiaRESUMO
Patients diagnosed with melanoma have a poor prognosis due to regional invasion and metastases. The receptor tyrosine kinase epidermal growth factor receptor (EGFR) is found in a subtype of melanoma with a poor prognosis and contributes to drug resistance. Aloysia citrodora essential oil (ALOC-EO) possesses an antitumor effect. Understanding signaling pathways that contribute to the antitumor of ALOC-EO is important to identify novel tumor types that can be targeted by ALOC-EO. Here, we investigated the effects of ALOC-EO on melanoma growth and tumor cell migration. ALOC-EO blocked melanoma growth in vitro and impaired primary tumor cell growth in vivo. Mechanistically, ALOC-EO blocked heparin-binding-epidermal growth factor (HB-EGF)-induced EGFR signaling and suppressed ERK1/2 phosphorylation. Myelosuppressive drugs upregulated HB-EGF and EGFR expression in melanoma cells. Cotreatment of myelosuppressive drugs with ALOC-EO improved the antitumor activity and inhibited the expression of matrix metalloproteinase-7 and -9 and a disintegrin and metalloproteinase domain-containing protein9. In summary, our study demonstrates that ALOC-EO blocks EGFR and ERK1/2 signaling, with preclinical efficacy as a monotherapy or in combination with myelosuppressive drugs in melanoma.
Assuntos
Antineoplásicos/farmacologia , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Receptores ErbB/metabolismo , Fator de Crescimento Semelhante a EGF de Ligação à Heparina/metabolismo , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Melanoma/metabolismo , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Neoplasias Cutâneas/metabolismo , Verbenaceae/química , Animais , Apoptose/efeitos dos fármacos , Bortezomib/farmacologia , Doxorrubicina/farmacologia , Sinergismo Farmacológico , Humanos , Melanoma/patologia , Camundongos , Fosforilação/efeitos dos fármacos , Neoplasias Cutâneas/patologiaRESUMO
CONTEXT: Stomach ulcer is one of the most common gastrointestinal problems in the world. OBJECTIVE: This study aimed to isolate flavonoid compounds from methanol extract of the aerial parts of Stachytarpheta jamaicensis (L.) Vahl. and evaluate its protective and therapeutic effects against gastric ulcer. MATERIALS AND METHODS: Chromatographic techniques were used for the identification of the isolated compounds. To explore the effects of the plant extract, it was administrated by oral gavage for one week either before or post-ethanol ulcer induction. Ranitidine was also evaluated as a reference drug. Stomach pH, gastric juice volume, lesions number, glutathione, superoxide dismutase, malondialdehyde, succinate dehydrogenase, lactate dehydrogenase, acid phosphatase, Interleukin-10, intracellular adhesion molecule-1, prostaglandin E2, and total protein levels were estimated in gastric tissue. Stomach histopathological features were also monitored. RESULTS: Six flavonoid compounds were isolated, where five of them were isolated for the first time (vitexin, isovitexin, apigenin 7,4'-dimethyl ether, 5,7,2'-trimethoxyflavone, and scutellarein), while apigenin was previously reported. Treatment with plant extract recorded amelioration in all the biochemical parameters. CONCLUSION: The methanol extract of plant aerial parts had prophylactic and treatment effects against gastric ulcer in rats, where its treatment effect exceeded its protective role. The extract recorded anti-inflammatory, and antioxidant effects due to the presence of flavonoid compounds.
Assuntos
Antiulcerosos/farmacologia , Flavonoides/farmacologia , Úlcera Gástrica/prevenção & controle , Verbenaceae/química , Animais , Antiulcerosos/uso terapêutico , Biomarcadores/metabolismo , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13/métodos , Flavonoides/química , Flavonoides/isolamento & purificação , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/enzimologia , Mucosa Gástrica/patologia , Mediadores da Inflamação/metabolismo , Masculino , Estrutura Molecular , Estresse Oxidativo , Componentes Aéreos da Planta/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Espectroscopia de Prótons por Ressonância Magnética/métodos , Ratos , Ratos Wistar , Espectrofotometria Ultravioleta/métodosRESUMO
Excessive exercise load can cause muscle soreness and fatigue, as well as inflammation and oxidative stress. Lemon verbena (Aloysia triphylla; Lippia citriodora) is often used as a spice in tea or beverages. Its leaves are rich in polyphenols, which have antioxidant and anti-inflammatory bioactivities. In the present study, we investigated whether supplementation with Planox® lemon verbena extract (LVE) could improve muscle damage and biochemical indicators after exhaustive exercise challenge. All subjects (30 males and 30 females) underwent a double-blind trial and were randomly divided into a placebo group (0 mg/human/day) and an LVE supplement group (400 mg/human/day), with gender-equal distribution. All subjects started supplementation 10 days before exhaustive exercise and continued it until all tests were completed. Before the intervention, after the exhaustive exercise, and on the following 3 days, the participants underwent 12-minute Cooper running/walking; blood collection; assessments of pain, muscle stiffness, maximum jump heights, and isometric maximum muscle strength. The results showed that supplementation with LVE effectively increased GPx and reduced CK, IL-6, 8-OHdG and muscle pain after the exhaustive exercise, but it had significant effect on strength recovery. In summary, LVE is a safe and edible natural plant extract that can reduce muscle damage and soreness after exercise. This trial was registered at clinicaltrials.gov as NCT04742244.
Assuntos
Antioxidantes/administração & dosagem , Suplementos Nutricionais , Mialgia/dietoterapia , Extratos Vegetais/administração & dosagem , Verbenaceae/química , Administração Oral , Adulto , Antioxidantes/efeitos adversos , Método Duplo-Cego , Exercício Físico/efeitos adversos , Feminino , Humanos , Contração Isométrica/fisiologia , Masculino , Músculo Esquelético/fisiopatologia , Mialgia/diagnóstico , Mialgia/etiologia , Mialgia/fisiopatologia , Estresse Oxidativo , Placebos/administração & dosagem , Placebos/efeitos adversos , Extratos Vegetais/efeitos adversos , Adulto JovemRESUMO
The inclusion of a medicinal plant leaf extract (MPLE) from sage (Salvia officinalis) and lemon verbena (Lippia citriodora), rich in verbascoside and triterpenic compounds like ursolic acid, was evaluated in gilthead seabream (Sparus aurata) fed a low fishmeal-based diet (48% crude protein, 17% crude fat, 21.7 MJ kg-1, 7% fishmeal, 15% fish oil) for 92 days. In particular, the study focused on the effect of these phytogenic compounds on the gut condition by analyzing the transcriptomic profiling (microarray analysis) and histological structure of the intestinal mucosa, as well as the histochemical properties of mucins stored in goblet cells. A total number of 506 differentially expressed genes (285 up- and 221 down-regulated) were found when comparing the transcriptomic profiling of the intestine from fish fed the control and MPLE diets. The gut transcripteractome revealed an expression profile that favored biological mechanisms associated to the 1) immune system, particularly involving T cell activation and differentiation, 2) gut integrity (i.e., adherens and tight junctions) and cellular proliferation, and 3) cellular proteolytic pathways. The histological analysis showed that the MPLE dietary supplementation promoted an increase in the number of intestinal goblet cells and modified the composition of mucins' glycoproteins stored in goblet cells, with an increase in the staining intensity of neutral mucins, as well as in mucins rich in carboxylated and weakly sulfated glycoconjugates, particularly those rich in sialic acid residues. The integration of transcriptomic and histological results showed that the evaluated MPLE from sage and lemon verbena is responsible for the maintenance of intestinal health, supporting gut homeostasis and increasing the integrity of the intestinal epithelium, which suggests that this phytogenic may be considered as a promising sustainable functional additive for aquafeeds.
Assuntos
Imunidade nas Mucosas/efeitos dos fármacos , Fatores Imunológicos/farmacologia , Junções Intercelulares/efeitos dos fármacos , Mucosa Intestinal/efeitos dos fármacos , Extratos Vegetais/farmacologia , Salvia officinalis , Dourada , Linfócitos T/efeitos dos fármacos , Verbenaceae , Junções Aderentes/efeitos dos fármacos , Junções Aderentes/metabolismo , Animais , Diferenciação Celular/efeitos dos fármacos , Células Caliciformes/efeitos dos fármacos , Células Caliciformes/imunologia , Células Caliciformes/metabolismo , Fatores Imunológicos/isolamento & purificação , Junções Intercelulares/metabolismo , Mucosa Intestinal/imunologia , Mucosa Intestinal/metabolismo , Ativação Linfocitária/efeitos dos fármacos , Mucinas/metabolismo , Permeabilidade/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Salvia officinalis/química , Dourada/genética , Dourada/imunologia , Dourada/metabolismo , Linfócitos T/imunologia , Linfócitos T/metabolismo , Junções Íntimas/efeitos dos fármacos , Junções Íntimas/metabolismo , Transcriptoma , Verbenaceae/químicaRESUMO
BACKGROUND: Excess hepatic triglyceride (TG) accumulation (steatosis) commonly observed in obesity, may lead to non-alcoholic fatty liver disease (NAFLD). Altered regulation of intracellular lipid droplets (LD) and TG metabolism, as well as activation of JNK-mediated proinflammatory pathways may trigger liver steatosis-related disorders. Drosophila melanogaster is an animal model used for studying obesity and its associated disorders. In Drosophila, lipids and glycogen are stored in the fat body (FB), which resembles mammalian adipose tissue and liver. Dietary oversupply leads to obesity-related disorders, which are characterized by FB dysfunction. Infusions of Lampaya medicinalis Phil. (Verbenaceae) are used in folk medicine of Chile to counteract inflammatory diseases. Hydroethanolic extract of lampaya (HEL) contains considerable amounts of flavonoids that may explain its anti-inflammatory effect. METHODS: We studied whether HEL affects palmitic acid (PA, C16:0) and oleic acid (OA; C18:1)-induced TG accumulation and proinflammatory marker content in HepG2 hepatocytes as well as impaired lipid storage and proinflammatory molecule expression in Drosophila melanogaster fed a high-fat diet (HFD). RESULTS: In HepG2 hepatocytes, exposure to OA/PA elevated TG content, FABP4, ATGL and DGAT2 expression, and the JNK proinflammatory pathway, as well as TNF-α and IL-6 production, while diminished FAS expression. These effects were prevented by HEL co-treatment. In Drosophila larvae fed a HFD, HEL prevented TG accumulation and downregulated proinflammatory JNK pathway activation. CONCLUSION: HEL effect counteracting OA/PA- and HFD-induced lipid accumulation and proinflammatory marker expression in HepG2 hepatocytes and Drosophila larvae may represent a preventive approach against hepatic steatosis and inflammation, associated to obesity and NAFLD.
Assuntos
Tecido Adiposo/efeitos dos fármacos , Dieta Hiperlipídica/efeitos adversos , Extratos Vegetais/farmacologia , Triglicerídeos/metabolismo , Verbenaceae/química , Animais , Drosophila melanogaster , Corpo Adiposo/efeitos dos fármacos , Células Hep G2 , Hepatócitos/citologia , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Humanos , Inflamação/metabolismoRESUMO
We analysed whether the hydroethanolic extracts from leaves of Haplopappus baylahuen Remy (bailahuen) and Aloysia citriodora Palau (cedron) inhibit the growth and ability of Salmonella Enteritidis to form biofilms and to adhere to human intestinal epithelial cells. Herein, we first determined the total phenolic content and antioxidant and antibacterial activities of the extracts. Then, Salmonella Enteritidis was treated with the extracts to analyse biofilm formation by scanning electronic microscopy and the violet crystal test. We also measured the efflux pump activity of Salmonella Enteritidis since biofilm formation is associated with this phenomenon. Furthermore, the human intestinal cell line Caco-2 was infected with Salmonella Enteritidis pretreated with the extracts, and 30 min later, the number of bacteria that adhered to the cell surface was quantified. Finally, we determined by qPCR the expression of genes associated with biofilm formation, namely, the diguanilate cyclase AdrA protein gene (adrA) and the BapA protein gene (bapA), and genes associated with adhesion, namely, the transcriptional regulator HilA (hilA). The phenolic content and antioxidant and bactericide activities were higher in bailahuen than in the cedron extract. Biofilm formation was inhibited by the extracts in a dose-dependent manner, while the activity of efflux pumps was decreased only with the cedron extract. Adhesion to Caco-2 cells was also inhibited without differences between doses and extracts. The extracts decreased the expression of adrA; with the cedron extract being the most efficient. The expression of hilA is affected only with the cedron extract. We concluded that hydroethanolic extracts of bailahuen and cedron differentially inhibit the growth of Salmonella Enteritidis and affect its the ability to form biofilms and to adhere to human intestinal epithelial cells. These results highlight the presence of molecules in bailahuen and cedron with a high potential for the control of the Salmonella Enteritidis pathogenesis.
Assuntos
Antibacterianos/administração & dosagem , Biofilmes , Etanol/administração & dosagem , Intestinos/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Salmonella enteritidis/efeitos dos fármacos , Salmonella enteritidis/fisiologia , Antioxidantes/administração & dosagem , Células CACO-2 , Células Cultivadas , Etanol/isolamento & purificação , Haplopappus/química , Humanos , Fenóis/isolamento & purificação , Verbenaceae/químicaRESUMO
BACKGROUND: A. gratissima is a shrub used in folk medicine as analgesic and sedative. However, studies on its antinociceptive activity are scarce. This research aimed to evaluate the antinociceptive effect of a supercritical carbon dioxide (SCCO2) extract of A. gratissima leaves (EAG) in mice. METHODS: A. gratissima leaves were subjected to extraction with supercritical CO2 (60 °C, 200 bar). The chemical composition of EAG was determined by gas chromatography-mass spectrometry (GC-MS). The antinociceptive profile of the extract (1, 10 and 30 mg/kg, p.o.) was established using acetic acid-induced abdominal contraction tests and formalin-induced paw-licking tests. The open field and rota-rod tests were used to evaluate a possible interference of EAG on mice motor performance. The contribution of the opioid system and adenosine triphosphate (ATP) sensitive K+ channels in the mechanism(s) of EAG action was evaluated by specific receptor blockers. EAG's acute toxicity was investigated using OECD 423 guideline. RESULTS: The GC-MS revealed the presence of sesquiterpenes (guaiol and pinocamphone) in the EAG. Doses of 10 mg/kg and 30 mg/kg significantly reduced the number of abdominal writhes and paw licking time in mice in the formalin test. The EAG did not affect the locomotor activity and motor coordination of the mice. The antinociceptive effect of the EAG was prevented by glibenclamide in the mice formalin test, unlike naloxone pre-treatment. The acute administration of EAG caused no mortality. CONCLUSION: A. gratissima leaves possess antinociceptive effect, mediated by K+ channels sensitive to ATP.
Assuntos
Analgésicos , Extratos Vegetais , Verbenaceae , Analgésicos/farmacologia , Animais , Dióxido de Carbono , Canais KATP/metabolismo , Camundongos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Verbenaceae/químicaRESUMO
OBJECTIVE: Duranta repens is reported to contain a wide array of secondary metabolites, including α-amylase and α-glucosidase inhibitors, and - has potent antioxidant activity. The present study evaluated the network pharmacology of D. repens (whole plant) with targets related to diabetes mellitus and assessed its outcome by evaluating the effects of the hydroalcoholic extract of D. repens in streptozotocin-nicotinamide-induced diabetes mellitus in rats. METHODS: Phytoconstituents of D. repens were retrieved from an open-source database and published literature, and their targets were predicted for diabetes mellitus using BindingDB and the therapeutic target database. Protein-protein interaction was predicted using STRING, and pathways involved in diabetes mellitus were identified using the Kyoto Encyclopedia of Genes and Genomes pathway browser. Druglikeness, ADMET profile (absorption, distribution, metabolism, excretion and toxicity) and cytotoxicity of compounds modulating proteins involved in diabetes were predicted using MolSoft, admetSAR2.0 and CLC-Pred, respectively. The interaction network among phytoconstituents, proteins and pathways was constructed using Cytoscape, and the docking study was performed using AutoDock4.0. The hydroalcoholic extract of D. repens was evaluated using streptozotocin-nicotinamide-induced diabetes mellitus animal model for 28 d, followed by an oral glucose tolerance test. At the end of the study, biochemical parameters like glycogen content, hepatic enzymes, antioxidant biomarkers and lipid profiles were quantified. Further, the liver and pancreas were collected for a histopathology study. RESULTS: Thirty-six different secondary metabolites from D. repens were identified to regulate thirty-one targets involved in diabetes mellitus, in which protein-tyrosine phosphatase 1B (PTP1B) was primarily targeted. Enrichment analysis of modulated proteins identified 12 different pathways in diabetic pathogenesis in which the phosphatidylinositol 3-kinase-protein kinase B (PI3K-Akt) signaling pathway was chiefly regulated. The docking study found that durantanin I possessed the highest binding affinity (-8.9 kcal/mol) with PTP1B. Similarly, ADMET profiling showed that the majority of bioactive constituents from D. repens had higher human intestinal absorptivity and minimal cytotoxicity to normal cell lines, than tumor cell lines. Further, an in vivo animal study reflected the efficacy of the hydroalcoholic extract of D. repens to lower the elevated blood glucose level by stimulating insulin secretion, maintaining pancreatic ß cell mass, regulating glycolysis/gluconeogenesis and enhancing the glucose uptake in skeletal muscles. CONCLUSION: The present study reflected the probable network interaction of bioactive constituents from D. repens, their targets and modulated pathways, which identified the prime regulation of the PI3K-Akt signaling pathway and PTP1B protein. Modulation of PTP1B protein and PI3K-Akt signaling pathway could contribute to enhancing glucose uptake, insulin production and glycolysis and decreasing gluconeogenesis in diabetes, which was evaluated via the experimental study.
Assuntos
Diabetes Mellitus Tipo 2 , Hipoglicemiantes/farmacologia , Resistência à Insulina , Extratos Vegetais/farmacologia , Verbenaceae/química , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Insulina , Fígado/metabolismo , Pâncreas/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Ratos , Transdução de Sinais/efeitos dos fármacosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Chilean population relies on medicinal plants for treating a wide range of illnesses, especially those of the gastrointestinal system. Junellia spathulata (Gillies & Hook.) Moldenke var. spathulata (Verbenaceae), called as "verbena-azul-de-cordilleira", is a medicinal plant native to Argentina and Chile traditionally used for treating digestive disorders. Although the species of the genus are important as therapeutic resources for the Andean population, the plants are very scarcely studied. AIMS OF THE STUDY: The purpose of the present study was to find out the main constituents and investigate the protective effect of J. spathulata against oxidative stress induced by the potent oxidant 2,2'-azobis (2-amidinopropane) dihydrochloride (AAPH) in human hepatoblastoma cells. MATERIALS AND METHODS: The crude methanol extract of J. spathulata and an iridoid obtained by chromatographic processes were tested to access the hepatoprotective effect and cytotoxicity in HepG2 cell. In addition, the reducing power of the samples and their ability to scavenge free radicals were evaluated using FRAP and ORAC assay systems. RESULTS: The iridoid asperuloside, the main compound of the crude methanol extract of J. spathulata, was isolated and identified by means of NMR analysis. The crude methanol extract of J. spathulata and asperuloside protected HepG2 cells against oxidative damage triggered by AAPH-derived free radicals. This effect can be credited to the ability of the extract and asperuloside to protect the liver cells from chemical-induced injury, which might be correlated to their free radical scavenging potential. CONCLUSIONS: This study experimentally evidenced the ethnopharmacological usefulness of J. spathulata as a treatment of digestive disorders. Our result could stimulate further investigations of hepatoprotective agents in other Chilean Junellia species.
Assuntos
Monoterpenos Ciclopentânicos/farmacologia , Sequestradores de Radicais Livres/farmacologia , Glucosídeos/farmacologia , Hepatócitos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Piranos/farmacologia , Verbenaceae , Sobrevivência Celular/efeitos dos fármacos , Chile , Monoterpenos Ciclopentânicos/isolamento & purificação , Sequestradores de Radicais Livres/isolamento & purificação , Glucosídeos/isolamento & purificação , Células Hep G2 , Hepatócitos/metabolismo , Hepatócitos/patologia , Humanos , Extratos Vegetais/isolamento & purificação , Piranos/isolamento & purificação , Verbenaceae/químicaRESUMO
INTRODUCCIÓN: La enfermedad del hígado graso no alcohólico (EHGNA) es la forma más común de enfermedad hepática. A nivel celular se caracteriza por la acumulación de triglicéridos (TG) en forma de gotas lipídicas (GL) dando lugar a esteatosis e inflamación. Entre los factores relevantes para la síntesis de TG se encuentran las enzimas DGAT1/2 que catalizan la etapa final de la síntesis de TG, y la proteína FABP4 que transporta lípidos intracelulares y se expresa en modelos de enfermedad hepática dependiente de obesidad. Por otra parte, TNF-α es una reconocida citoquina involucrada en el proceso inflamatorio en la EHGNA. La medicina popular del norte de Chile ha utilizado la planta Lampaya medicinalis Phil. (Verbenaceae) para el tratamiento de algunas enfermedades inflamatorias. OBJETIVO: Evaluar el efecto de un extracto hidroalcóholico de lampaya (EHL) sobre la esteatosis y expresión de marcadores de inflamación en hepatocitos tratados con ácidos grasos. Diseño experimental: Estudio in vitro en cultivos de la línea celular humana HepG2 tratadas con ácido oleico (AO) y ácido palmítico (AP). MÉTODOS: Se incubó hepatocitos HepG2 con AO/AP por 24 horas en presencia o no de EHL. Se evaluó la presencia de GL y el contenido de TG intracelulares por Oil Red O y Nile Red, respectivamente. La expresión de DGAT1/2, FABP4 y TNF-α fue evaluada por qPCR. RESULTADOS: Los hepatocitos tratados con AO/AP mostraron un aumento en las GL y TG, así como una mayor expresión de DGAT2 en comparación al control. El cotratamiento con EHL revirtió los efectos inducidos por AO/AP. CONCLUSIONES: EHL revierte el incremento en las GL, TG y en la expresión de DGAT2 inducido por AO/AP en células HepG2. Estos hallazgos sugieren un efecto hepatoprotector de la Lampaya contra la esteatosis, y apoyarían su uso complementario en el tratamiento de patologías con componente inflamatorio como la EHGNA.
Non-alcoholic fatty liver disease (NAFLD) is the most common liver disease. At the cellular level, it is characterized by the accumulation of triglycerides (TG) in the form of lipid droplets (LD), which leads to steatosis and inflammation. Among relevant factors for TG synthesis are the enzymes DGAT1/2 catalyzing the final stage of TG synthesis, and the protein FABP4 which transports intracellular lipids and is expressed in cell models of obesity-dependent liver disease. Additionally, TNF-α is a cytokine involved in the inflammatory process associated to NAFDL. Lampaya medicinalis Phil. (Verbenaceae) is a plant used in folk medicine in northern Chile to treat some inflammatory diseases. OBJECTIVE: To evaluate the effect of the hydroalcoholic extract of lampaya (HEL) on steatosis and the expression of inflammatory markers in hepatocytes treated with fatty acids. Study design: In vitro study in cultures of the human HepG2 cell line treated with oleic acid (OA) and palmitic acid (PA). METHODS: HepG2 hepatocytes were incubated with OA/PA for 24 hours in the presence and absence of HEL. The formation of LD and the accumulation of intracellular TG were assessed by Oil Red O and Nile Red, respectively. The expression of DGAT1/2, FABP4 and TNF-α was assessed by qPCR. RESULTS: The treatment with OA/PA increased the levels of LD and TG as well as the expression of DGAT2 in HepG2 hepatocytes compared to control cells. HEL cotreatment counteracted OA/PA-induced effects. CONCLUSIONS: HEL prevents the increase in LD and TG levels and DGAT2 expression induced by OA/PA in HepG2 cells. These findings suggest that lampaya may have a protective effect against hepatic steatosis, which would support its complementary use in the treatment of pathologies associated with inflammation, such as NAFLD.
Assuntos
Humanos , Extratos Vegetais/farmacologia , Hepatócitos/efeitos dos fármacos , Verbenaceae/química , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Triglicerídeos/análise , Técnicas In Vitro , Extratos Vegetais/uso terapêutico , Sobrevivência Celular , Reação em Cadeia da Polimerase , Técnicas de Cultura de Células , Ácido Oleico , Etanol/química , Células Hep G2/efeitos dos fármacos , InflamaçãoRESUMO
Previously phytochemical investigations carried out on the flowers and trunk bark extracts of Citharexylum spinosum L. tree, allowed the isolation of twenty molecules belonging to several families of natural substances [triterpene acids, iridoid glycosides, phenylethanoid glycosides, 8,3'-neolignan glycosides, together with other phenolic compounds]. In the present work, a biological evaluation (anti-tyrosinase, anticholinesterase and cytotoxic activities) was performed on the prepared extracts and the isolated secondary metabolites. The results showed that the EtOAc extract of the trunk bark displayed the highest anti-tyrosinase effect with a percent inhibition of 55.0 ± 1.8% at a concentration of 100 µg/mL. The highest anticholinesterase activity was presented by the same extract with an IC50 value of 99.97 ± 3.01 µg/mL. The EtOAc extract of flowers and that of the trunk bark displayed the best cytotoxic property with IC50 values of 96.00 ± 2.85 and 88.75 ± 2.00 µg/mL, respectively, against the human cervical cancer cell line (HeLa), and IC50 values of 188.23 ± 3.88 and 197.00 ± 4.25 µg/mL, respectively, against the human lung cancer (A549) cell lines. Biological investigation of the pure compounds showed that the two 8,3'-neolignan glycosides, plucheosides D1-D2, generate the highest anti-tyrosinase potency with a percent inhibition of 61.4 ± 2.0 and 79.5 ± 2.3%, respectively, at a concentration of 100 µM. The iridoid glycosides exhibited a significant anticholinesterase activity with IC50 values ranging from 17.19 ± 1.02 to 52.24 ± 2.50 µM. Triterpene pentacyclic acids and iridoid glycosides exerted encouraging cytotoxic effects against HeLa with IC50 values ranging from 9.00 ± 1.10 to 25.00 ± 1.00 µM. The study of the structure-activity relationship (SAR) has been sufficiently and widely discussed. The natural compounds that exhibited the significant bioactivities were docked.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Inibidores Enzimáticos/farmacologia , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Verbenaceae/química , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Colinesterases/metabolismo , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Camundongos , Estrutura Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-AtividadeRESUMO
Foodborne illnesses caused by the consumption of food contaminated with foodborne pathogens at infectious doses are becoming a common health issue throughout the world. Metal nanoparticles with potential antimicrobial properties are an area that can be explored to discover novel antimicrobial agents. The traditional synthesis methods of metal nanoparticles involve the use of toxic chemicals and the generation of harmful byproducts. In this study, a greener method to synthesize silver nanoparticles (AgNPs) with potential antimicrobial properties was investigated. The aqueous extract of the medicinal plant Phyla dulcis Trev. (verbenaceae) was used as the reducing and stabilizing agent to synthesize AgNPs using microwave irradiation. The formation of AgNPs was confirmed using ultraviolet-visible spectroscopy by the appearance of characteristic surface plasmon resonance peaks in the 430-440 nm wavelength range. The size and stability of the AgNPs were studied using Zetasizer nano-series for 5 weeks after synthesis. The average particle size remained between 63 and 76 nm during the first 4 weeks and increased to 114 nm in the fifth week showing possible aggregation after the fourth week. The zeta potential remained between -20 and -24 mV throughout the 5 weeks showing relatively good stability. Scanning electron microscopy/energy dispersive X-ray spectroscopy showed the association of phytoconstituents with the AgNPs. X-ray photoelectron spectroscopy analysis confirmed the formation of metallic nanoparticles starting from silver nitrate. Finally, the AgNPs were tested to be effective against Escherichia coli O157:H7 (ATCC 43888), Salmonella Typhimurium (novobiocin and nalidixic acid resistant strain), Listeria monocytogenes (4b; ATCC 19115), and Staphylococcus aureus (ATCC 6538) strains, which are known to be common foodborne pathogens.
Assuntos
Anti-Infecciosos , Nanopartículas Metálicas , Extratos Vegetais , Prata , Anti-Infecciosos/farmacologia , Química Verde , Testes de Sensibilidade Microbiana , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plantas Medicinais/química , Prata/farmacologia , Verbenaceae/químicaRESUMO
Herbal infusions are a new emerging trend among consumers, appearing in the market in many different forms. Due to intense competition, the commercial success of herbal infusions largely depends on flavour. The identification of the best combinations of steeping time and water temperature for the preparation of Aloysia triphylla infusions using a central composite design and response surface methodology was performed. The procedure aimed to maximize its antioxidant activity, phenolic and aromatic compounds, and consumers' liking of the infusions. The antioxidant activity and phenolic content were evaluated using the 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid radical cation) method and the Folin-Ciocalteu procedure. The analysis of aromatic compounds was performed based on the method of terpenic compounds. Sensory evaluation encompassed overall liking using a 9-point hedonic scale. Antioxidant activity and extraction of most phenolic compounds was higher for longer steeping times and higher temperatures, with some presenting a contrasting effect due to degradation at higher temperatures for longer steeping times. Results for terpenic compounds showed similar contrasting patterns. Based on the quadratic response surface, it was possible to predict the maximum overall liking for lemon verbena infusions prepared by brewing for 6 min at 96 â. Under such conditions, extraction of bioactive compounds was kept at a high level, close to the maximum attainable, while reducing the extraction of bitter compounds. These results are considered of great importance for the development of premium infusions from organic lemon verbena leaves.
Assuntos
Hidrocarbonetos Aromáticos/análise , Fenóis/análise , Temperatura , Verbenaceae/química , Antioxidantes/análise , Extratos Vegetais/análise , Folhas de Planta/química , Paladar , Fatores de Tempo , Compostos Orgânicos VoláteisRESUMO
Background The brain is the centre of the nervous system in all vertebrates. The central cholinergic pathways play a prominent role in learning and memory processes. Dementia is a mental disorder characterized by the loss of intellectual ability, which invariably involves the impairment of memory. The crude extracts of the Gmelina arborea plant are reported to possess wound-healing, anti-diarrheal, anti-oxidant, anti-diabetic, and anti-ulcer property. The present study was designed to evaluate the effects of G. arborea on learning and memory in albino Wistar rats. Methods A total of 36 healthy rats were selected for the study, which were divided in to six groups. Standard screening tests such as the elevated plus maze (EPM), Morris water maze (MWM), and step-down passive avoidance (SDA) tests were used for testing the learning and memory processes. Results Gmelina arborea at higher doses (1000 mg/kg) showed statistically significant activity in EPM, MWM, and SDA tests for assessing the learning and memory paradigms when compared to the control group in amnesia-induced and non-amnesia groups of rats. Conclusions This is the first ever study to report the effects of G. arborea on learning and memory in both amnesia-induced and non-amnesia groups of rats. Our results show that G. arborea potentiates the processes of learning and memory. The observed pharmacological activities should be further evaluated by detailed experimental studies and revalidated by clinical trials.