RESUMO
Eight new compounds (1-8), along with three known related compounds (9-11) were isolated from the leaves of Sauropus spatulifolius Beille. Their structures and configurations were elucidated by means of spectrometric and the modified Mosher's method. Among the new compounds, compounds 1 and 2 were identified as ethyl 3, 6-anhydro-2-deoxy-ß-D-arabino-hexofuranoside (1) and ethyl 3, 6-anhydro-2-deoxy- hexofuranoside (2). Compounds 3-5 were the 2-acetylpyrrole derivatives and identified as 2-(2-acetyl-1H-pyrrol-1-yl)-4-hydroxybutyric acid (3), methyl 4-(2-acetyl-lH-pyrrol- 1-yl) butanoate (4) and 1, 4-bis (2-acetyl-1H-pyrrol-1-yl) butane (5), respectively. Compound 6 was elucidated as 7-megastigmane-3, 8, 9-triol. Compounds 7, 8 were identified as kaempferol-3-O-2-deoxy-ß-D-glucoside (7) and kaempferol-3-O-ß-D- glucopyranosyl-(1-6)-2-deoxy-ß-D-glucoside (8). In addition, the cytotoxic activities of all the compounds were also evaluated, where compounds 3, 5, 7, 9\10 and 11 exhibited the magnificent inhibition activity on lung fibroblast differentiation induced by TGF-ß1with low toxicity against the RLE-6TN cell.
Assuntos
Flavonoides/isolamento & purificação , Glicosídeos/isolamento & purificação , Malpighiales/metabolismo , Extratos Vegetais/isolamento & purificação , Animais , Bioensaio , Diferenciação Celular/efeitos dos fármacos , Linhagem Celular , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Flavonoides/química , Flavonoides/farmacologia , Glicosídeos/química , Glicosídeos/farmacologia , Humanos , Pulmão/citologia , Pulmão/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Malpighiales/química , Camundongos , Estrutura Molecular , Rotação Ocular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Folhas de Planta/metabolismo , CoelhosRESUMO
Our present and previous phytochemical investigations on Leptopus lolonum have resulted in the isolation of almost 30 phenylpropanoid-conjugated pentacyclic triterpenoids (PCPTs). During the continuous study on PCPTs, this kind of triterpenoid ester is considered as a natural product with low toxicity because of it's widely distribution in natural plants and edible fruits including kiwi fruit, durian, jujube, pawpaw, apple and pear. In the present work, we report the isolation, structural elucidation and cytotoxic evaluation of four new PCPTs (1-4) which obtained from L. lolonum. In addition, the possible biosynthesis pathway for 28-norlupane triterpenoid and potent effect of phenylpropanoid moiety for increasing the cytotxic effect of triterpenoids were also discussed. Among these compounds, compound 1 exhibited the highest cytotoxic effect on HepG2 cells with IC50 value of 11.87 µM. Further flow cytometry and western blot analysis demonstrated that 1 caused G1 cell cycle arrest by up-regulated the expression of phosphorylated p53 protein in HepG2 cells and induced cell apoptosis via MAPK and Akt pathways. These results emphasized the potential of PCPTs as lead compounds for developing anti-cancer drugs.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Malpighiales/química , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais/química , Propanóis/química , Propanóis/isolamento & purificação , Propanóis/farmacologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Relação Estrutura-Atividade , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologiaRESUMO
Nine previously undescribed dichapetalin-type triterpenoids (1-9), along with 12 reported compounds (10-21), were isolated from the twigs of Dichapetalum gelonioides. Their chemical structures were mainly elucidated by comprehensive analysis of HRMS, 1D and 2D NMR spectroscopic data. The absolute configuration of compound 1 was further determined based on single-crystal X-ray diffraction. In addition, a part of compounds were evaluated the effects of inhibitory NO production in LPS-induced RAW264.7 macrophages.
Assuntos
Anti-Inflamatórios/farmacologia , Malpighiales/química , Triterpenos/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , China , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Células RAW 264.7 , Triterpenos/isolamento & purificaçãoRESUMO
The bioactive compounds of pequi peel flours were characterized. Flavonoid contents ranged from 19.67 to 87.61 mg/100 g, high in comparison to many vegetables described in the literature. Gallic acid (11.52-418.67 mg/100 g), gallate ethyl (2026.75 - 5205.90 mg/100 g), ellagic acid (509.47 - 1630.66 mg/100 g), lutein (0.17-1.36 mg/100 g), ß-carotene (0.82 - 1.49 mg/100 g), and ß-cryptoxanthin (0.07 - 0.11 mg/100 g) were identified by HPLC, contributing to a greater valorization of the pequi peel flours. Phytochemical tests indicated the presence of hydrolyzable tannins and saponins. The detection of these compounds makes the product commercially attractive, in addition to generating value for an agro-industrial residue. The results obtained in this study confirm the multifunctional potential of pequi peel flour as a functional ingredient.
Assuntos
Farinha/análise , Malpighiales/química , Ácido Elágico/análise , Flavonoides/análise , Frutas/química , Ácido Gálico/análogos & derivados , Ácido Gálico/análise , Taninos Hidrolisáveis/análiseRESUMO
The search for active microorganisms for the biotransformation of guttiferone A (1) and C (6) has been successfully undertaken from a collection of endophytic fungi of Symphonia globulifera. Of the twenty-five isolates obtained from the leaves, three are active and have been identified as Bipolaris cactivora. The products obtained are the result of xanthone cyclisation with the formation of two regioisomers among four possible and corresponding to 1,16-oxy-guttiferone and 3,16-oxy-guttiferone. The biotransformation conditions were studied. Interestingly, both oxy-guttiferones A are present in the plant, and the ratio of 3,16-oxy-guttiferone to 1,16-oxy-guttiferone is 4 : 1, very close to that observed by biotransformation (3.8 : 1). These results are consistent with the involvement of endophytes in their formation pathway from guttiferone A, in planta. Finally, biotransformation made it possible to obtain and describe for the first time oxy-guttiferones C.
Assuntos
Benzofenonas/metabolismo , Bipolaris/metabolismo , Endófitos/metabolismo , Malpighiales/microbiologia , Biotransformação , Malpighiales/química , Folhas de Planta/química , Folhas de Planta/microbiologiaRESUMO
Two new prenylated 4-phenylcoumarins, named kielcoumarin A (1) and kielcoumarin B (2) together with three known compounds, mammea B/BA (3), mammea B/BA cyclo F (4) and ferruol A (5), were obtained from stems and roots of Kielmeyera argentea (Calophyllaceae). Their structures were elucidated based on spectroscopic data. Cytotoxic activity of the 4-alkylcoumarins 3-5 was evaluated in vitro against human U251 glioblastoma cell line. Compound 3 showed significative activity with EC50 value of 6.6 µM while compounds 4 and 5 showed respective EC50 values of 52.0 and 37.0 µM.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Cumarínicos/farmacologia , Malpighiales/química , Antineoplásicos Fitogênicos/isolamento & purificação , Brasil , Cumarínicos/isolamento & purificação , Humanos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Raízes de Plantas/química , Caules de Planta/química , PrenilaçãoRESUMO
Most of Euphorbiaceae plants are considered as folk medicinal plants because of their various pharmacological effects. However, there are eight Leptopus genus plants which belong to Euphorbiaceae have never be investigated. Thus, four Leptopus genus plants were collected to study their chemical constituents and pharmacological activities. In the present work, the cytotoxicities of the extracts of four Leptopus genus plants were evaluated before phytochemical experiments. And nine new phenylpropanoid-conjugated pentacyclic triterpenoids, along with twenty-two known compounds were isolated from the whole plants of Leptopus lolonum. The structures of these new compounds were unequivocally elucidated by HRESIMS and 1D/2D NMR data. All triterpenoids were screened for their cytotoxicities against four cancer cell lines including HepG2, MCF-7, A549 and HeLa. Among these isolates, the triterpenoid with a phenylpropanoid unit showed increasing cytotoxicity on cancer cells, which suggested the importance of the phenylpropanoid moiety.
Assuntos
Antineoplásicos Fitogênicos/química , Malpighiales/química , Propanóis/química , Triterpenos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Malpighiales/metabolismo , Conformação Molecular , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo , Plantas Medicinais/química , Plantas Medicinais/metabolismo , Relação Estrutura-Atividade , Triterpenos/isolamento & purificação , Triterpenos/farmacologiaRESUMO
Pequi fruit peels are an underexploited source of polyphenols. The anti-diabetic potential of an extract and fractions from the peels were evaluated in a panel of assays. The extract and fractions thereof inhibited the release of cytokines involved in insulin resistance - TNF, IL-1ß, and CCL2 - by lipopolysaccharide-stimulated THP-1 cells. The ethyl acetate fraction inhibited in vitro α-glucosidase (pIC50 = 4.8 ± 0.1), an enzyme involved in the metabolization of starch and disaccharides to glucose, whereas a fraction enriched in tannins (16C) induced a more potent α-glucosidase inhibition (pIC50 = 5.3 ± 0.1). In the starch tolerance test in mice, fraction 16C reduced blood glucose level (181 ± 10 mg/dL) in comparison to the vehicle-treated group (238 ± 11 mg/dL). UPLC-DAD-ESI-MS/MS analyses disclosed phenolic acids and tannins as constituents, including corilagin and geraniin. These results highlight the potential of pequi fruit peels for developing functional foods to manage type-2 diabetes.
Assuntos
Frutas/química , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Malpighiales/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Glicemia/metabolismo , Camundongos , Polifenóis/análise , Espectrometria de Massas em TandemRESUMO
OBJECTIVE: the purpose of this study was to investigate the effects of Chrysobalanus icaco on adiposity and its mechanism of action in the gene and protein expression of acetyl-CoA carboxylase (ACC), a key enzyme in lipogenesis. METHOD: Wistar rats were divided into a regular or control group (CG) and a high-fat diet (HFD) group. HFD was treated with saline or aqueous extract of Chrysobalanus icaco (AECI) for four weeks. Body weight and food intake were assessed. Subcutaneous, retroperitoneal and periepididymal adipose tissue samples were collected and weighed. Adipocytes from periepididymal tissue were isolated and analyzed. The gene and protein expression of ACC in subcutaneous tissue was determined. RESULTS: AECI showed no effect on intake or body weight. However, the weight of the fat pads and the gene and protein expression of ACC were lower, and glucose tolerance was improved. CONCLUSION: the aqueous extract of Chrysobalanus icaco proved beneficial for the treatment of obesity, preventing fat storage and improving glycemic homeostasis
OBJETIVO: el objetivo de este estudio fue investigar los efectos del extracto acuoso de Chrysobalanus icaco (AECI) en la adiposidad y su mecanismo de acción en la expresión génica y proteica de la acetil-CoA-carboxilasa (ACC), una enzima clave para la lipogénesis. MÉTODOS: se usaron ratones macho Wistar que se asignaron a una dieta estándar de control (CG) o a una rica en grasa (HFD). La HFD se trató con solución salina o con extracto acuoso de Chrysobalanus icaco (AECI) durante cuatro semanas. Se evaluaron el peso corporal y el consumo alimentario. Se aislaron y analizaron muestras de tejido adiposo subcutáneo, retroperitoneal y periepididímico. Se determinó la expresión génica y proteica de ACC en el tejido subcutáneo. RESULTADOS: el AECI no mostró ningún efecto sobre la ingesta de alimento y tampoco sobre el peso corporal. Sin embargo, el tratamiento con AECI redujo el peso de los tejidos adiposos y la expresión génica y proteica de ACC, y mejoró también la tolerancia a la glucosa. CONCLUSIÓN: Chrysobalanus icaco (AECI) resultó ser beneficioso para el tratamiento de la obesidad, previniendo el almacenamiento de grasa y mejorando la homeostasis glucémica
Assuntos
Animais , Masculino , Ratos , Malpighiales/química , Acetil-CoA Carboxilase/efeitos dos fármacos , Lipogênese/efeitos dos fármacos , Tecido Adiposo/efeitos dos fármacos , 24457 , Ratos Wistar , HomeostaseRESUMO
BACKGROUND: Recent ethnomedicinal studies on Bridelia ferruginea Benth (family Phyllanthaceae) as an antiplasmodial remedy have established its potency as a strong prophylactic and chemosuppressive agent. Human consumption of medicinal herbs without adequate evaluation of its efficacy and safety can result in grave physiological and pathological consequences. Therefore, this study assessed the antiplasmodial bioactivity, biochemical, hematological, histopathological and toxicity profile of the ethanolic stem bark extract of B. ferruginea in mice. METHODS: Ethanolic stem bark extract of B. ferruginea (200, 400 and 800 mg/kg) were orally administered to Plasmodium berghei-infected mice in models and were subsequently observed for mortality, behavioral changes and signs of toxicity. Acute evaluation was experimented at 1,000 mg/kg for 28 days. Occult blood obtained from the euthanized mice were subjected to biochemical and hematological assays. A comprehensive assessment of the histology of the liver and kidney was also ascertained. The median lethal dose (LD50) was determined and extrapolated using the regression equation obtained from the plot of the probits of mortalities (y) and the log of doses (log10C). RESULTS: Different concentrations of the phytochemical secondary metabolites were revealed. Antiplasmodial bioactivity was established at the 200, 400 and 800 mg/kg of the herbal extract with a dearth in parasitemia at different days post-treatment. The 800 mg/kg group responded by exhibiting a dose-dependent decrease in parasitemia comparable with the chloroquine bi-phosphate group. Significant alterations in the histology of the liver and kidney of the 1,000 mg/kg group was documented. There was a reduction in the titers of LDH, ALT, AST, and urea in the treated group when compared with the control (p < 0.05). Antioxidant profiles were also highly significant with elevation in SOD, GPx, and CAT, but a reduction in MDA. LD50 was established at 424 mg/kg. CONCLUSION: B. ferruginea Benth (family Phyllanthaceae) is a potent antiplasmodial, antioxidant, regenerative and ameliorative herbal remedy if administered in controlled dosage.
Assuntos
Malária/tratamento farmacológico , Malpighiales/química , Casca de Planta/química , Extratos Vegetais/farmacologia , Plasmodium berghei/efeitos dos fármacos , Animais , Antimaláricos/farmacologia , Modelos Animais de Doenças , Etanol/farmacologia , Malária/parasitologia , Camundongos , Camundongos Endogâmicos BALB C , Plantas MedicinaisRESUMO
Extraction of mamao luang (hereafter called mamao) with different solvents and varying solid to liquid (S:L) ratio was conducted to verify its antioxidant activities. Total phenolic content (TPC), total flavonoid content, total monomeric anthocyanin content, and antioxidant activities, namely, 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity and ferric reducing antioxidant power (FRAP) of the unrefined extracts, were analyzed. The extraction with 70% acetone and 70% methanol and the S:L ratio of 1:30 seemed to be more appropriate and gave significantly (P < 0.05) higher values of the previously mentioned properties. Whole ground fruits were then incorporated into the blended chicken patties to compare their antioxidant and antimicrobial properties with butylated hydroxyanisole (BHA). During refrigeration storage of 20 days, the highest level (1,000 mg TPC/kg meat) could retard lipid oxidation relatively comparable to the efficiency of BHA (200 ppm). However, when microbiological aspect was considered together, a limited storage of 12 days was consequently suggested. PRACTICAL APPLICATION: Mamao fruit is a splendid source of phenolic compounds. The antioxidant properties have been demonstrated using DPPH and FRAP assay. The suitable type of solvent and S:L ratio were provided for the extraction. Our findings have shown that addition of mamao, a source of natural antioxidants, especially at the highest level increased oxidative stability of chicken patties. The research outcomes identify the potential bioactive compound and provide beneficial information related to the feasibility of incorporation of mamao phenolics as antioxidant agents in suitable food matrices. However, further investigation is still required for successful application in meat and meat products.
Assuntos
Antioxidantes/análise , Aditivos Alimentares/análise , Malpighiales/química , Produtos da Carne/análise , Extratos Vegetais/análise , Animais , Antocianinas/análise , Antioxidantes/isolamento & purificação , Galinhas , Flavonoides/análise , Aditivos Alimentares/isolamento & purificação , Frutas/química , Oxirredução , Fenóis/análise , Extratos Vegetais/isolamento & purificaçãoRESUMO
BACKGROUND: Uvaria chamae (Annonaceae), Phyllantus amarus (Phyllantaceae) and Lantana camara (Verbenaceae) are empirically alleged to be used as Beninese medicinal plants in the treatment of salmonellosis. This study aimed to produce scientific data on in vitro and in vivo efficacy of Uvaria chamae, Lantana camara and Phyllantus amarus on multiresistant Salmonella spp isolated in Benin. RESULTS: After performing in vitro tests on aqueous and ethanolic extracts of these plants, only the aqueous extract of Uvaria chamae (leaves) showed the best anti-Salmonella's activity and was used for this in vivo experiment. The induction of salmonellosis revealed 9 × 108 CFU/ml was the optimal concentration triggering and maintaining symptoms in chicks. This infective concentration was used for in vivo assessment. Twenty-four hours post inoculation, the symptoms of salmonellosis (wet cloaca, diarrhea stools and somnolence) were observed in infected groups. After 7 days of treatment, the reduction of bacterial load at 100 mg/L, 200 mg/L, 400 mg/L of the extract was respectively 85%, 52.38% and 98% for Uvaria chamae, Phyllantus amarus and Lantana camara in the chick's groups infected with Salmonella Typhimurium ATCC 14028. On the other hand, colistin completely cancelled the bacterial load (reduction rate of 100%). With the groups infected with Salmonella spp (virulent strain), the reduction rate of bacterial load at 100 mg/L, 200 mg/L, 400 mg/L of extract was 0%, 98.66%, and 99.33%. The extracts at 200 and 400 mg/L were more active than colistin, which reduced the bacterial load by 33.33%. The toxicity tests did not show any negative effect of Colistin and the Uvaria chamae's extract on the biochemical and hematological parameters of the chicks. CONCLUSION: The aqueous extract of Uvaria chamae is active in vitro and in vivo on multiresistant strains of Salmonella enterica. This plant is a good candidate for the development of an improved traditional medicine for the management of salmonellosis.
Assuntos
Lantana/química , Malpighiales/química , Extratos Vegetais/farmacologia , Doenças das Aves Domésticas/tratamento farmacológico , Salmonella/efeitos dos fármacos , Uvaria/química , Animais , Benin , Galinhas , Extratos Vegetais/química , Plantas Medicinais , Doenças das Aves Domésticas/microbiologia , Salmonelose Animal/tratamento farmacológico , Salmonelose Animal/microbiologiaRESUMO
In this study the physicochemical characterization of the pulp and almond fixed oil was carried out; their antibacterial activity and aminoglycoside antibiotic modifying action against standard and multiresistant Gram-positive and -negative bacteria were investigated using the broth microdilution assay. Physical properties such as moisture, pH, acidity, peroxide index, relative density and refractive index indicate stability and chemical quality of the oils. In the GC/MS chemical composition analysis, a high unsaturated fatty acid content and the presence of oleic and palmitic acids were observed in the oils. In the antibacterial assay, more significant results were obtained for Escherichia coli, while other standard and multi-resistant strains presented MIC values ≥ 1024 µg/mL. Furthermore, the fixed oils in association with antibiotics were able to significantly improve antibacterial activity against S. aureus with a reduction in MICs.
Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Malpighiales/química , Óleos de Plantas/farmacologia , Aminoglicosídeos/farmacologia , Escherichia coli/efeitos dos fármacos , Ácidos Graxos/análise , Cromatografia Gasosa-Espectrometria de Massas , Testes de Sensibilidade Microbiana , Óleos de Plantas/química , Staphylococcus aureus/efeitos dos fármacosRESUMO
BACKGOUND: Obesity and dyslipidemia are major risk factors associated with non-alcoholic fatty liver disease (NAFLD). NAFLD refers to the accumulation of fat in more than 5% of the liver without alcohol consumption. NAFLD is the most common liver disease and is rapidly becoming a global public health problem. Maoberry (Antidesma bunius) is a fruit rich in antioxidants, especially phenolic compounds, which are reported to have benefits for patients with NAFLD. METHODS: We evaluated the effect of Maoberry extract on fat metabolism in liver tissues of high fat diet-induced rats. Five (5) groups (n = 12) of male Sprague-Dawley (SD) rats were divided into those given a high fat diet with no treatment (HF), different dosages of Maoberry extracts (0.38 [ML], 0.76 [MM) and 1.52 [MH] g/kg body weight) and 10 mg/kg statin (STAT). The rats were fed a high fat diet for 4 weeks to induce obesity and subsequently continued more for 12 weeks with treatments of Maoberry extracts or STAT. The levels of triglyceride, liver enzymes, oxidative stress and inflammation markers, triglyceride synthesis regulators, and pathology of the liver in high fat diet-induced rats were investigated. RESULTS: Feeding Maoberry extract in MH groups resulted in decreasing levels of serum alanine aminotransferase (ALT), liver triglyceride, liver thiobarbituric acid reactive substances (TBARS) and mRNA expression of tumour necrosis factor (TNF)-α, interleukin (IL)-6, glycerol-3-phosphate acyltransferase (GPAT)-1 and acetyl-coenzyme A carboxylase (ACC) compared with the HF group (P < 0.05). Moreover, histopathological study of the liver showed reduced fat droplets in the Maoberry extract treatment groups, especially in MH groups and STAT treatment groups. CONCLUSIONS: The improvements of fat metabolism in liver tissues of rats fed a high-fat diet were observed in Maoberry extracts treatment groups. The underline mechanism that link to fat metabolism might be through the process accompanied with down-regulated the gene expression of key enzymes of lipid production, antioxidant activity, and anti-inflammation properties of Maoberry extracts which contains high levels of phenolic and flavonoid compounds.
Assuntos
Antioxidantes/administração & dosagem , Gorduras/metabolismo , Fígado/efeitos dos fármacos , Malpighiales/química , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Acetil-CoA C-Acetiltransferase/genética , Acetil-CoA C-Acetiltransferase/metabolismo , Animais , Antioxidantes/química , Dieta Hiperlipídica/efeitos adversos , Frutas/química , Humanos , Interleucina-6/genética , Interleucina-6/metabolismo , Fígado/metabolismo , Masculino , Hepatopatia Gordurosa não Alcoólica/etiologia , Hepatopatia Gordurosa não Alcoólica/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley , Triglicerídeos/metabolismo , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismoRESUMO
Phyllanthus amarus is widely grown in this sub-continent and used traditionally to treat many common ailments. In the present study, lignan rich fraction of P. amarus extract was used on cervical cancer cell lines (HeLa, SiHa and C33A) to study it's mechanism of cell death induction. As the cells were treated with IC50 doses of LRF, characteristic apoptotic features were observed. Increased sub G0 population were observed both in Hela and C33 cells, while G1/S arrest was observed in SiHa cells than their untreated counterparts. Increased production of ROS and change in MMP were also detected in the treated cells. Presence of γH2AX, was observed by immunofluorescence. Reduced expression of HPV (16/18) as well as ET-1, an autocrine growth substance, were observed in the treated cells. Immunoblotting as well as ICFC studies showed enhanced expressions of BAX, Caspase 3 and PARP (cleaved) in the treated cells. A major lignan, phyllanthin was isolated from the chloroform fraction and showed strong irreversible affinities for viral E6 and MDM2 in in silico analysis. The study conclusively indicates that LRF has the potential to induce apoptotic cell death in cervical cancer cells by activation of p53 and p21 against DNA damage.
Assuntos
Apoptose , Lignanas/química , Malpighiales/química , Extratos Vegetais/farmacologia , Linhagem Celular Tumoral , Dano ao DNA , Células HeLa , Papillomavirus Humano 16 , Papillomavirus Humano 18 , Humanos , Ligação de Hidrogênio , Potencial da Membrana Mitocondrial , Microscopia de Fluorescência , Mitocôndrias/metabolismo , Compostos Fitoquímicos/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Difração de Raios XRESUMO
BACKGROUND: Glochidion zeylanicum (GZ), a common plant in Thailand and Eastern Asia, is rich in antioxidants. However, the possible anti-aging and oxidative stress resistance properties of GZ leaf extracts (hexane and methanol extracts) have not been reported. PURPOSE: We aimed to provide the first science-based evidence of the beneficial effects of GZ on anti-aging and oxidative stress resistance in the Caenorhabditis elegans model. METHODS: The phytochemical composition of the hexane and methanol extracts were analyzed using GLC-MS and LC-MS. Fingerprinting analysis of the extract was performed by RP-HPLC. We determined total phenolics, flavonoids, and antioxidant properties via DPPH and ABTS assays. Oxidative stress resistance, anti-aging and lifespan were studied in C. elegans treated with leaf extracts. RESULTS: GZ leaf extracts protected the worms against oxidative stress and attenuated ROS accumulation. The expression of stress-response genes, such as SOD-3, and GST-4 were up-regulated, whereas HSP-16.2 was down-regulated after GZ treatment. The oxidative stress resistance properties of GZ possibly involved the DAF-16/FoxO and SKN-1/Nrf-2 transcription factors. GZ leaf extracts improved pharyngeal pumping function and autofluorescent pigment attenuation suggesting anti-aging properties. GZ leaf extracts modulated the lifespan extension in C. elegans. CONCLUSION: This study reports novel anti-aging and antioxidant activities of GZ leaf extracts, suggesting a novel bioactivity for a medicinally important plant and supplementary drug against oxidative stress.
Assuntos
Proteínas de Caenorhabditis elegans/metabolismo , Proteínas de Ligação a DNA/metabolismo , Fatores de Transcrição Forkhead/metabolismo , Malpighiales/química , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Fatores de Transcrição/metabolismo , Animais , Antioxidantes/metabolismo , Caenorhabditis elegans , Flavonoides/análise , Longevidade/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Fenóis/análise , Folhas de Planta/química , Plantas Medicinais , Espécies Reativas de Oxigênio/metabolismoRESUMO
Gastrointestinal nematodes remain a major constraint on the health, welfare, and production of small ruminants. This study was conducted to evaluate three plant extracts (from Bridelia ferruginea, Combretum glutinosum, and Mitragyna inermis) as effective remedies against gastrointestinal parasites of small ruminants. Phytochemical screening was conducted on the plant leaves, and the potential anthelmintic properties of these plants were tested in vitro on Haemonchus contortus using the egg hatch, larval migration, and adult worm motility assays. The phytochemical screening of the leaves revealed the presence of several bioactive components in all the plants. The number of eggs that hatched was reduced in a concentration-dependent manner (p < 0.01) upon treatment with the methanol extract of B. ferruginea and the acetone extracts of C. glutinosum and M. inermis. The inhibitory effect of the acetone extract of B. ferruginea and the methanol extracts of C. glutinosum and M. inermis was not concentration-dependent (p > 0.05). There was a significant difference (p < 0.05) in the reduction in larval migration between the lowest concentrations (75 to 150 µg/mL) and the highest concentrations (300 to 1200 µg/mL) of plant extracts. The ability of plant extracts to affect the mobility of the adult worms was not concentration-dependent (p > 0.05); however, it was dependent on the time of incubation (p < 0.01). At the highest concentration (2400 µg/mL), all adult worms were motionless after 24 h of exposure, while at the lowest concentration (< 150 µg/mL), this occurred after 48 h of exposure. M. inermis and C. glutinosum extracts were more effective than B. ferruginea extracts (p < 0.05). Overall, these results suggest that these plants used by small-scale farmers possess antiparasitic properties useful for helminthiasis control. However, the effects of the plants remain to be confirmed via in vivo assays and toxicity tests in further studies.
Assuntos
Anti-Helmínticos/farmacologia , Combretum/química , Haemonchus/efeitos dos fármacos , Malpighiales/química , Mitragyna/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Trato Gastrointestinal/parasitologia , Larva/efeitos dos fármacos , Locomoção/efeitos dos fármacos , Folhas de Planta/química , Ruminantes/parasitologiaRESUMO
It was deemed of interest to investigate Antidesm bunius aerial parts from phytochemical and biological points of view due to limited previous studies. Isolation and identification of phenolic compounds and evaluation of the potential antimicrobial and cytotoxic effects of A. bunius aerial parts was investigated. The petroleum ether (PEE) and 80% EtOH extracts (EE), as well as, n-hexane (HF), CHCl3 (CF), EtOAc (EAF), n-BuOH (BF) and H2O soluble fractions (WF) of the latter were prepared. Phytochemical study has been performed for isolation and identification of the major polyphenols. Antimicrobial activity, using diffusion agar technique, and potential cytotoxic effect against HepG2, MCF7 and HCT cell lines were evaluated. Malic acid (I), caffeic acid (II), methyl benzoate (III), (+)-catechin (IV), (-)-epicatechin (V), epicatechin-(4ßâ8)-catechin (procynidin B1, VI) and epicatechin-(4ßâ8)-epicatechin (procyanidin B2, VII) were isolated. Compounds I-VII showed strong to moderate antimicrobial activity, with MIC values in the range of 1.95-125µg/ml except for compounds 1 and IV, which did not show any effect. All tested samples showed dose dependent cytotoxic effect against all three tested cell lines. PEE showed strong cytotoxic activity (IC50=23.7-38.2µg/ml). Furthermore, compound VI showed potent cytotoxicity against HepG2, MCF7 and HCT cell lines (IC50=24.7, 16.5 and 18.0µg/ml) respectively. The strong to moderate antimicrobial activity and cytotoxic effect of the plant could be attributed to its content of phenolic acids, flavan-3-ols and/or proanthocyanidins. These findings were confirmed by results obtained for the isolated compounds.
Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Bactérias/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Fungos/efeitos dos fármacos , Malpighiales , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Bactérias/crescimento & desenvolvimento , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Relação Dose-Resposta a Droga , Fungos/crescimento & desenvolvimento , Células Hep G2 , Humanos , Concentração Inibidora 50 , Células MCF-7 , Malpighiales/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Solventes/químicaRESUMO
Sodium chloride reduction in foods is a significant focus of the dairy industry; however, it can interfere with dairy product quality. Thus, researchers have carried out studies on alternatives to maintain dairy product safety when presenting reduced NaCl content, such as natural antimicrobial addition. Caryocar brasiliense (pequi) is a fruit with high phenolic compound concentrations in the pulp and peel and known antioxidant and antimicrobial properties. This study aimed to define the optimum stage for pequi waste extract addition during cheese manufacturing in order to maintain and prolong the shelf life of reduced-sodium goat Minas Frescal cheese. Four different goat Minas Frescal cheese treatments were carried out: control cheese (without extract; CC), pequi extract addition to milk (CM), pequi extract addition to mass (CS), and cheese immersion in pequi extract (CIE). The treatments were subjected to microbiological (Staphylococcus spp., Escherichia coli, Enterobacteriaceae, coliforms and fecal coliforms, Lactococcus spp., and lactic acid bacteria counts), textural (hardness and consistency), and instrumental color (luminosity, yellow intensity, red intensity, chroma, hue angle, and total color change) analyses. No Enterobacteriaceae, Staphylococcus spp., E. coli, or coliforms and fecal coliforms were detected during storage for any of the assessed samples, including CC. Regarding texture, all samples presented a trend for decreasing rigidity during storage. In addition, lower luminosity values were also observed in cheeses produced with added pequi extract (CM, CS, and CIE) when compared with CC. All cheeses produced with added pequi were stable regarding all evaluated parameters; however, pequi extract addition to milk (CM) was shown to be more efficient, leading to higher textural parameters and better microbiological quality during storage. Thus, the CM treatment is the most recommended for pequi waste extract addition during Minas Frescal cheese manufacture.
Assuntos
Anti-Infecciosos/farmacologia , Queijo/microbiologia , Malpighiales/química , Leite/microbiologia , Extratos Vegetais/farmacologia , Animais , Indústria de Laticínios , Enterobacteriaceae/efeitos dos fármacos , Escherichia coli , Cabras , Lactobacillales , Lactococcus/efeitos dos fármacos , Leite/química , Cloreto de Sódio/análise , Staphylococcus/efeitos dos fármacosRESUMO
A phytochemical investigation on the twigs and leaves of Flueggea virosa (Euphorbiaceae) led to the isolation of flueggenoids A - E (1-5), five new 13-methyl-ent-podocarpanes, together with eleven known compounds (6-16). Their structures and absolute configurations were elucidated on the basis of extensive MS and NMR data analysis, and/or single-crystal X-ray diffraction, time-dependent density functional theory (TDDFT)-based electronic circular dichroism (ECD) calculations, and chemical transformation. All isolates were evaluated for anti-HCV activity, the results showed that terpenoids of F. virosa had nonnegligible contribution for the anti-HCV activity.