摘要
This study aims to explore the effects of chemical ingredient groups B and C in Kansui Radix stir-fried with vinegar on the diversity of gut microbiota in the rat model of malignant ascites, identify the key differential microbial taxa, and reveal the biological mechanism of water-expelling effect of the two chemical ingredient groups. The rat model of malignant ascites induced by Walker-256 cells was established, and phenolphthalein was used as the positive drug. The rats were orally administrated with corresponding agents for consecutive 7 days. On day 6, fresh feces samples were collected from the rats, and 16 S rDNA high-throughput sequencing and GC-MS were employed to determine the composition of gut microbiota and the content of short-chain fatty acids, respectively. On day 7, serum and intestinal tissue samples were collected for the determination of related indicators. Compared with the control group, the model group showed decreased feces volume and urine volume(P<0.01), increased volume of ascites and levels of Na~+, K~+, and Cl~- in urine(P<0.01), down-regulated mRNA and protein levels of intestinal AQP8(P<0.01), lowered abundance of beneficial Lactobacillus(P<0.01) while risen abundance of potential pathogenic Lachnospiraceae and Anaeroplasma(P<0.01), and reduced content of short-chain fatty acids(P<0.01). Compared with the model group, administration with chemical ingredient groups B and C alleviated all the above indicators(P<0.01). In conclusion, chemical ingredient groups B and C in Kansui Radix stir-fried with vinegar could alleviate the disordered gut microbiota in rats with malignant ascites to expel water through increasing the abundance of beneficial Lactobacillus and reducing the abundance of harmful Lachnospiraceae and Anaeroplasma. This study can provide a reference for the reasonable clinical application of Kansui Radix stir-fried with vinegar.
Subject(s)
Animals , Rats , Acetic Acid/chemistry , Ascites/drug therapy , Euphorbia/chemistry , Gastrointestinal Microbiome , Plant Roots/chemistry摘要
This study investigated the antibacterial potential of Euphorbia hirtawhole plant extracts, honey and conventional antibiotics and their synergistic effects against selected multidrug resistant and typed bacterial strains associated with otitis media. E. hirtawhole plant extract was purified using column chromatography technique. The antibacterial assays of extracts were done using standard microbiological procedures. Protein, sodium and potassium ion leakage of the synergistic mixtures was determined using flame-photometry. At 100 mg/ml, acetone extracts presented highest inhibition against S. aureus (NCTC 6571) with 32 ± 0.83 mm zone of inhibition. The fractional inhibitory concentration indices displayed higher synergism in combination of plant extract, honey and ciprofloxacin against P. mirabilisat 0.02 compared to drug combination synergy standard (≤ 0.5). This work revealed augmentation of ciprofloxacin potency when combined with purified E. hirta acetone extract and honey and implies their high potential in the treatment of multidrug resistant infectionof otitis media.
Este estudio investigó el potencial antibacteriano de extractos de plantas enteras de Euphorbia hirta, miel y antibióticos convencionales y sus efectos sinérgicos contra cepas bacterianas seleccionadas multirresistentes y tipificadas asociadas con la otitis media. El extracto de la planta entera de E. hirtase purificó usando la técnica de cromatografía en columna. Los ensayos antibacterianos de extractos se realizaron utilizando procedimientos microbiológicos estándar. La fuga de iones de proteínas, sodio y potasio de las mezclas sinérgicas se determinó mediante fotometría de llama. A 100 mg/ml, los extractos de acetona presentaron la mayor inhibición contra S. aureus (NCTC 6571) con una zona de inhibición de 32 ± 0,83 mm. Los índices de concentración inhibitoria fraccional mostraron un mayor sinergismo en combinación de extracto de planta, miel y ciprofloxacina contra P. mirabilisa 0,02 en comparación con el estándar de sinergia de combinación de fármacos (≤ 0,5). Este trabajo reveló un aumento de la potencia de la ciprofloxacina cuando se combina con extracto de acetona purificado de E. hirtay miel e implica sualto potencial en el tratamiento de infecciones de otitis media resistentes a múltiples fármacos.
Subject(s)
Humans , Otitis Media/drug therapy , Plant Extracts/therapeutic use , Euphorbia/chemistry , Anti-Bacterial Agents/therapeutic use , Proteus mirabilis/drug effects , Staphylococcus aureus/drug effects , Terpenes/analysis , Flavonoids/analysis , Plant Extracts/pharmacology , Ciprofloxacin/pharmacology , Microbial Sensitivity Tests , Flame Emission Photometry , Chromatography, Thin Layer , Drug Resistance, Multiple , Drug Synergism , Glycosides/analysis , Honey , Gas Chromatography-Mass Spectrometry , Anti-Bacterial Agents/pharmacology摘要
To reveal the toxic mechanism of Kansui stir-baked with vinegar(VEK), conducta comparative study on the metabolites of fecal samples of rats before and after being treated with chemical constituents group B and C(VEKB/VEKC) extracted from VEK by metabolomics approach. The fecal samples of each group were analyzed using ultra performance liquid chromatography-quadrupole-time of flight-mass spectrometry(UFLC-Q-TOF-MS). Then the data was processed by principal component analysis(PCA) and partial least square discriminant analysis(OPLS-DA) to screen and identify biomarkers relating to the toxicity of VEK. Besides, t-test was adopted for univariate statistical analysis, so as to study the changes of these biomarkers in drug groups before and after being treated with VEKB/VEKC and explore the effect of VEKB/VEKC on the metabolism of rat feces. Furthermore, the toxic mechanism of VEKB/VEKC was explored based on the results of the metabolic pathway analysis. The results displayed that compared with control group, the metabolism of fecal samples of VEKB and VEKC treated groups show obvious changes, and the VEKB treated group show more significant changes. A total of 16 potential biomarkers and 5 metabolic pathways relating to the toxicity of VEK were found and identified. And the toxicity of VEK might be associated with the disorder of such metabolic pathways as tryptophan metabolism, primary bile acid biosynthesis, amino sugar and nucleotide sugar metabolism, purine metabolism, and degradation of valine, leucine and isoleucine. This study provides a scientific basis for the clinical safety application of VEK.
Subject(s)
Animals , Rats , Acetic Acid , Biomarkers , Chromatography, High Pressure Liquid , Euphorbia/chemistry , Feces/chemistry , Mass Spectrometry , Metabolome摘要
RESUMEN: Estudios recientes han demostrado que los compuestos activos presentes en extractos de C. chayamansa, E. prostrata y J. dioica tienen propiedades antioxidantes. Los resultados obtenidos en nuestro estudio fueron compuestos fenólicos solubles mostraron en C. chayamansa 6,34, E. prostrata 10,67, J. dioica 1,83 mg equiv de ácido gálico/gm BS respectivamente. Los antioxidantes solubles en agua por el método ABTS fueron para C. chayamansa 5.9, E. prostrata 12.7 y para J. dioica 2.5 mM equiv. de trolox/gr BS. Los resultados histopatológicos muestran una mejoría en los tejidos tratados con los extractos después de la inducción a hiperglicemia.
SUMMARY: Recent studies have shown that the active compounds present in extracts of C. chayamansa, E. prostrata and J. dioica have antioxidant properties. The results obtained in our study were soluble phenolic compounds showed in C. chayamansa 6.34, E. prostrata 10.67, J. dioica 1.83 mg equiv of gallic acid/gm BS respectively. The antioxidants soluble in water by the ABTS method were for C. chayamansa 5.9, E. prostrata 12.7 and for J. dioica 2.5 mM equiv. of trolox/gr BS. The histopathological results show an improvement in the tissues treated with the extracts after the induction to hyperglycemia.
Subject(s)
Animals , Rats , Plant Extracts/administration & dosage , Euphorbia/chemistry , Jatropha/chemistry , Hyperglycemia/drug therapy , Antioxidants/administration & dosage , Phenols/analysis , Flavonoids/analysis , Plant Extracts/chemistry , Rats, Wistar , Phenolic Compounds , Hyperglycemia/chemically induced , Kidney/drug effects , Liver/drug effects , Antioxidants/chemistry摘要
Abstract INTRODUCTION In Brazil, Biomphalaria glabrata, B. tenagophila, and B. straminea are intermediate hosts of Schistosoma mansoni, the etiological agent of schistosomiasis mansoni. Molluscicide use is recommended by the WHO for controlling the transmission of this parasite. Euphorbia milii latex has shown promising results as an alternative molluscicide. Thus, a natural molluscicide prototype kit based on freeze-dried E. milii latex was developed and evaluated against Biomphalaria spp. METHODS E. milii latex was collected, processed, and lyophilized. Two diluents were defined for freeze-dried latex rehydration, and a prototype kit, called MoluSchall, was produced. A stability test was conducted using prototype kits stored at different temperatures, and a toxicity assay was performed using Danio rerio. Additionally, MoluSchall was tested against B. glabrata under semi-natural conditions according to defined conditions in the laboratory. RESULTS MoluSchall was lethal to three Brazilian snail species while exhibiting low toxicity to D. rerio. Regardless of storage temperature, MoluSchall was stable for 24 months and was effective against B. glabrata under semi-natural conditions, with the same LD100 as observed under laboratory conditions. CONCLUSIONS MoluSchall is a natural, effective, and inexpensive molluscicide with lower environmental toxicity than existing molluscicides. Its production offers a possible alternative strategy for controlling S. mansoni transmission.
Subject(s)
Animals , Schistosoma mansoni/drug effects , Biomphalaria/parasitology , Schistosomiasis mansoni/prevention & control , Euphorbia/chemistry , Latex/pharmacology , Molluscacides/pharmacology , Biomphalaria/drug effects , Latex/isolation & purification , Molluscacides/isolation & purification摘要
The aim of current study was to determinate ex vivo and chromatographic fingerprint by HPLC of four extracts of Euphorbia furcillata K. Ethyl acetate extract of Euphorbia furcillata (EaEEf) was the most effective and potent extract (Emax=98.69±1.24%) and its effect was partially endothelium-dependent. Functional vasorelaxant mechanism of action of EaEEf was determinate, EaEEf showed efficient relaxation of KCl [80 mM]-induced contraction and norepinephrine and CaCl2 contraction curves showed diminution of maximal contraction in the presence of EAEEf and EaEEf-relaxation curve was shifted to the right in the presence of L-NAME (nitric oxide synthase inhibitor) and ODQ (guanylate cyclase inhibitor). Chromatographic fingerprints analysis suggests presence of diterpenoid such as abietane, tigliane, and ingenane skeletons. Our experiments suggest the EaEEf vasorelaxant activity could be attributed to diterpenoid molecules whose mechanism involves nitric oxide production and calcium channel blockade.
Se determinoÌ el efecto vasorrelajante ex vivo y los perfiles cromatograÌficos mediante HPLC de cuatro extractos de Euphorbia furcillata K.. El extracto de acetato de etilo de E. furcillata (EaEEf) fue el maÌs eficaz y potente en la contraccioÌn inducida por norepinefrina (Emax=98.69±1.24%) y el efecto fue parcialmente dependiente del endotelio vascular. Se determinoÌ el mecanismo de accioÌn vasorrelajante para EaEEf, este mostroÌ ser eficaz sobre la contraccioÌn inducida por KCl [80 mM] y la curva de contraccioÌn en respuesta a norepinefrina y CaCl2 en presencia de EaEEf mostroÌ disminucioÌn en la contraccioÌn maÌxima, mientras que la curva de relajacioÌn de EaEEf en presencia de L-NAME (inhibidor de oÌxido niÌtrico sintasa) y ODQ (inhibidor de guanilato ciclasa) se desplazoÌ hacia la derecha. El anaÌlisis cromatograÌfico de EaEEf sugiere la presencia de moleÌculas diterpenoides como abietano, tigliano y esqueletos de ingenano. Nuestros resultados sugieren que el efecto vasorrelajante de EaEEf podriÌa atribuirse a moleÌculas diterpenoides, cuyo mecanismo de accioÌn involucra la produccioÌn de oÌxido niÌtrico y bloqueo de canales de calcio.
Subject(s)
Animals , Male , Rats , Vasodilator Agents/pharmacology , Plant Extracts/pharmacology , Euphorbia/chemistry , Calcium Channel Blockers/metabolism , Chromatography, High Pressure Liquid , Rats, Wistar , Cyclic GMP/metabolism , Nitric Oxide/metabolism摘要
Objetivo. Determinar los fitoconstituyentes del extracto hidroalcohólico de Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana) y evaluar su actividad catártica. Materiales y métodos. Se elaboró un extracto hidroalcohólico con etanol al 70% (70:30) del tubérculo fresco de Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana), el cual fue analizado mediante un perfil fitoquímico cualitativo y el uso de espectroscopia UV/V y espectroscopia infrarroja (IR). Se tuvieron 36 ratones albinos, distribuidos en seis grupos de seis cada uno: Grupo I, suero fisiológico 0,9%); Grupo II, control positivo (senósido 250 mg/kg), y Grupos III, IV, V y VI (experimentales) a los que se les administró el extracto hidroalcohólico de Euphorbia huachanhana (Klotzsch & Garcke) Boiss (EH) a dosis 200 mg/kg, 400 mg/kg, 600 mg/kg y 800 mg/kg. Se evaluó la actividad catártica mediante la frecuencia de defecación y el porcentaje de motilidad intestinal con administración de carbón activado al 10%. Resultados. Se evidenció la presencia de flavonoides, compuestos fenólicos, carbohidratos, taninos, esteroides, azúcares reductores, aminoácidos y antraquinonas. Mediante espectroscopia UV/V se tuvo una banda de absorción de 290 nm lo que corresponde a una antraquinona; por espectroscopia infrarroja (IR) se evidenció la presencia de grupos hidroxilo y carbonilo. La mayor frecuencia de defecación (7,7 por hora) y el mejor tránsito intestinal (92,3%) fueron encontrados en el grupo que recibió EH a 200 mg/kg, estas diferencias fueron significativas en comparación al grupo blanco (p<0,05). Conclusiones. Se encontró, como molécula de interés, la presencia de una antraquinona con grupos funcionales hidroxilo y carbonilo; asimismo, la administración del extracto hidroalcohólico de Euphorbia huachanhana (Klotzsch & Garcke) Boiss a dosis de 200 mg/kg ofreció los mejores resultados en actividad catártica. Sin embargo, el diseño utilizado no permite establecer que la presencia de estas moléculas son la causa directa del efecto catártico observado.
Objective. To determine the phytoconstituents of the Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana) tuber hydroalcoholic extract and to evaluate its cathartic activity. Materials and methods. An hydroalcoholic extract was elaborated with 70% ethanol (70:30) using fresh tuber of Euphorbia huachanhana (Klotzsch & Garcke) Boiss (huachangana). That extract was analyzed for its phytochemical profile, and by UV/V spectroscopy and infrared spectroscopy (IR) to search some bioactive molecules. Thirty-six albino mice were distributed in six groups of six each one: Group I, 0.9% saline solution; Group II, Positive Control (Sennoside 250 mg/kg); and Groups III, IV, V and VI (Experimental) to which hydroalcoholic extract of Euphorbia huachanhana (Klotzsch & Garcke) Boiss (EH) were administered at doses 200 mg/kg, 400 mg/kg; 600 mg/kg and 800 mg/kg. The cathartic activity was evaluated by frequency of defecation and percentage of intestinal motility with administration of 10% activated carbon. Results. Presence of flavonoids, phenolic compounds, carbohydrates, tannins, steroids, reducing sugars, amino acids and anthraquinones was evidenced. An absorption band of 290 nm was observed by UV / V spectroscopy and infrared spectroscopy (IR), which corresponds to an anthraquinone, and the presence of hydroxyl and carbonyl groups was evidenced. The highest frequency of defecation (7.7 per hour) and the best intestinal transit (92.3%) were found on group which received EH at 200 mg/kg, these differences were statistically significant in comparison to the 0.9% saline solution group (p<0.05). Conclusions. The presence of an anthraquinone with hydroxyl and carbonyl groups was found as a molecule of interest. Additionally, the administration of Euphorbia huachanhana (Klotzsch & Garcke) Boiss hydroalcoholic extract at a dose of 200 mg / kg gave the best cathartic activity. However, this experimental design does not allow establishing that the presence of these molecules are the direct cause of the observed cathartic effect.
Subject(s)
Animals , Mice , Euphorbia/chemistry , Gastrointestinal Motility , Plants, Medicinal , Complementary Therapies , Plant Extracts , Phytochemicals , Medicine, Traditional摘要
Euphorbia dioeca Kunth belongs to the Wanderers herb complex that is traditionally used for skin diseases and recently as antidiabetic. The methanol and aqueous extracts were evaluated for their in vitro alpha-glucosidase inhibitory activity and an oral starch tolerance test. These extracts showed an IC50 of 0.55 and 0.85 mg/mL, respectively. In diabetic Long Evans rats, the methanol and aqueous extracts reduced significantly the postprandial hyperglycemia peak in 15.2 percent and 12.8 percent, respectively. The alpha-glucosidase inhibitory activity is related with the presence of glycosides, phenolic compounds and flavonoids. Additionally, the safety parameters of both extracts were assessed by means of an acute toxicity test, being classified as innocuous. The traditional use of E. dioeca to control type 2 diabetes was confirmed, being an important source of alfa-glucosidase inhibitors.
Euphorbia dioeca Kunth, pertenece al complejo de plantas medicinales denominado Hierba de la Golondrina; el cual se utiliza para diversos padecimientos, destacando su uso como antidiabético. En dicho marco, se evaluó tanto la actividad inhibitoria de alfa-glucosidasa in vitro, como su desempeño en una prueba de tolerancia a una carga de almidón postprandial. Los extractos inhibieron la actividad de la alfa-glucosidasa con una CI50 de 0.55 y 0.85 mg/mL, respectivamente. Los extractos metanólico y acuoso disminuyeron significativamente el pico hiperglucémico postprandial en un 15.2 por ciento y un 12.8 por ciento, respectivamente, cuando se evaluó en ratas diabéticas. La actividad inhibitoria de alfa-glucosidasa, reflejada en ambas pruebas, está relacionada con la presencia de glicósidos, compuestos fenólicos y flavonoides. De manera adicional, ambos extractos fueron evaluados en una prueba de toxicidad aguda, siendo clasificados como inocuos. Se corroboró el uso tradicional de E. dioeca para el control de la diabetes tipo 2, siendo una importante fuente de compuestos inhibidores de alfa-glucosidasa.
Subject(s)
Animals , Mice , /drug therapy , Euphorbia/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Plant Extracts/pharmacology , Hyperglycemia/drug therapy , Mice, Inbred BALB C摘要
AbstractTo assess the pro-angiogenic activity of Euphorbia tirucalli, commonly known as “avelós” plant, we performed a series of tests by applying an aqueous E. tirucalli latex solution (10 mg/mL) to the chorioallantoic membranes (CAMs) of 80 fertilized chicken eggs incubated in a temperature- and humidity-controlled automatic incubator. The results indicated that the aqueous latex solution increased vascular network formation compared to that with the negative control (p < 0.05) and the inhibitor control (p < 0.05). This suggests that under the experimental conditions tested, the aqueous latex solution induced an inflammatory response leading to neoangiogenesis.
ResumoCom o objetivo de analisar a atividade angiogênica apresentada pela Euphorbia tirucalli, popularmente conhecida comumente como “avelós”, foram realizados ensaios utilizando solução aquosa de látex na concentração de 10 mg/ml, aplicada em membrana corioalantóide (MCA) de 80 ovos férteis de galinha, incubado em estufa automática com temperatura e umidade controladas. Os resultados apontaram que a ação da solução aquosa provocou aumento da percentagem da rede vascular formada em relação aos controles negativo (p<0,05) e inibidor (p<0,05), indicando que nas condições deste experimento, foi responsável pela ativação da resposta inflamatória e crescimento de novos vasos sanguíneos.
Subject(s)
Animals , Chick Embryo , Angiogenesis Inducing Agents/pharmacology , Euphorbia/chemistry , Latex/pharmacology , Chickens , Chorioallantoic Membrane摘要
OBJECTIVE: Investigate the relationship of the tumor volume after preoperative chemotherapy (TVAPQ) and before preoperative chemotherapy (TVBPQ) with overall survival at two and at five years, and lifetime. METHODS: Our sample consisted of consecutive patients evaluated in the period from 1989 to 2009 in an Onco-Hematology Service. Clinical, histological and volumetric data were collected from the medical records. For analysis, chi-square, Kaplan-Meier, log-rank and Cox regression tests were used. RESULTS: The sample consisted of 32 patients, 53.1% were male with a median age at diagnosis of 43 months. There was a significant association between TVAPQ>500mL and the difference between the TVBPQ and TVAPQ (p=0.015) and histologic types of risk (p=0.008). It was also verified an association between the difference between the TVBPQ and TVAPQ and the predominant stromal tumor (p=0.037). When assessing the TVAPQ of all patients, without a cutoff, there was an association of the variable with lifetime (p=0.013), i.e., for each increase of 10mL in TVAPQ there was an average increase of 2% in the risk of death. CONCLUSIONS: Although our results indicate that the TVAPQ could be considered alone as a predictor of poor prognosis regardless of the cutoff suggested in the literature, more studies are needed to replace the histology and staging by tumor size as best prognostic variable. .
OBJETIVO: Investigar a relação entre o volume do tumor após a quimioterapia pré-operatória (VTPOS) e antes da quimioterapia pré-operatória (VTPRE) com sobrevida geral aos dois e cinco anos e tempo de vida. MÉTODOS: A amostra foi composta por pacientes consecutivos avaliados de 1989 a 2009, em um serviço de onco-hematologia. Os dados clínicos, histológicos e volumétricos foram coletados a partir dos registros médicos. Para análise, usaram-se os testes qui-quadrado, Kaplan-Meier, log-rank e regressão de Cox. RESULTADOS: A amostra foi composta de 32 pacientes, 53,1% do sexo masculino, com mediana de idade ao diagnóstico de 43 meses. Houve associação significativa entre VTPOS >500 mL e a diferença entre o VTPRE e VTPOS (p=0,015) e os tipos histológicos de risco (p=0,008). Verificou-se também uma associação entre a diferença entre o VTPRE e VTPOS e o tumor de predomínio estromal (p=0,037). Quando se avaliou o VTPOS de todos os pacientes, sem um ponto de corte definido, observou-se associação dessa variável com o tempo de vida (p=0,013), isto é, para cada aumento de 10 mL no VTPOS houve um aumento médio de 2% no risco de morte. CONCLUSÕES: Embora os resultados indiquem que o VTPOS poderia ser considerado um preditor isolado de mau prognóstico, independentemente do ponto de corte sugerido na literatura, mais estudos são necessários para substituir a histologia e estadiamento pelo tamanho do tumor como melhor variável prognóstica. .
Subject(s)
Animals , Humans , Mice , Antineoplastic Agents, Phytogenic/pharmacology , Diterpenes/pharmacology , Drug Resistance, Multiple/drug effects , Drug Resistance, Neoplasm/drug effects , Macrocyclic Compounds/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Cell Proliferation/drug effects , Diterpenes/chemistry , Diterpenes/isolation & purification , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Euphorbia/chemistry , Macrocyclic Compounds/chemistry , Macrocyclic Compounds/isolation & purification , Molecular Conformation , Phenotype , Structure-Activity Relationship , Tumor Cells, Cultured摘要
Anti-carcinogenic potential of hydro-ethanolic extract of Euphorbia neriifolia (EN) leaves and an isolated flavonoid (ENF) was investigated against N-Nitrosodiethylamine (DENA)-induced renal carcinogenesis in mice. Experimental mice were pretreated with 150 and 400 mg/kg body wt of EN, 0.5% and 1% mg/kg body wt of butylated hydroxylanisole (BHA) as a standard antioxidant and 50 mg/kg body wt of ENF for 21 days prior to the administration of a single dose of 50 mg/kg body wt of DENA. Levels of renal markers (urea and creatinine), xenobiotic metabolic enzymes (Cyt P450 and Cyt b5), lipid peroxidation (LPO), antioxidants (SOD, CAT, GST and GSH) and other biochemical parameters — AST, ALT, ALP, total protein (TP), and total cholesterol (TC) were measured to determine the renal carcinogenesis caused by DENA. DENA administration significantly (p<0.001) decreased the body weight and increased the tissue weight. It significantly (p<0.001) enhanced the levels of Cyt P450, Cyt b5 and LPO and decreased the levels of SOD, CAT, GST and GSH content. The activities of AST, ALT and ALP and the TP content and renal markers were also significantly decreased (p<0.001), while TC level was markedly increased after DENA administration, as compared with the normal control group (p<0.001). Pretreatment with EN and ENF counteracted DENA-induced oxidative stress (LPO) and exerted its protective effects by restoring the levels of antioxidants (SOD, CAT, GST and GSH), biochemical parameters (AST, ALT, ALP, TP and TC), renal markers (urea and creatinine) and xenobiotic enzymes (Cyt P450 and Cyt b5) in renal tissue. In conclusion, the present study showed significant anti-carcinogenic potential of the hydro-ethanolic extract of E. neriifolia and ENF against DENA-induced renal carcinogenicity.
Subject(s)
Animals , Anticarcinogenic Agents/isolation & purification , Anticarcinogenic Agents/pharmacology , Body Weight/drug effects , Carcinogenesis/drug effects , Diethylnitrosamine/toxicity , Euphorbia/chemistry , Flavonoids/isolation & purification , Flavonoids/pharmacology , Kidney/drug effects , Kidney/metabolism , Kidney/pathology , Kidney Neoplasms/chemically induced , Kidney Neoplasms/enzymology , Kidney Neoplasms/metabolism , Kidney Neoplasms/pathology , Male , Mice , Organ Size/drug effects , Plant Leaves/chemistry , Biomarkers, Tumor/metabolism , Xenobiotics/metabolism摘要
PURPOSE: To evaluate the effects of crude extract of Euphorbia tirucalli in cutaneous wound healing. METHODS: A total of 20 Swiss mice were randomly divided into two groups, aveloz (GA) and control (CG), and each group was further divided into two subgroups based on the deaths scheduled for the 7th and 14th days after surgery. The animals underwent a resection of cutaneous fragment with 1cm in diameter on the dorsum; the GA was applied in each animal on the subsequent days, 0.1 mL (30 mg/mL) hydroalcoholic extract of Euphorbia tirucalli was applied on the wound, while the same volume of 0.9% saline solution was applied to the GC. It was evaluated the lesion diameter and after programmed death, a surgical specimen was resected for histopathology. RESULTS: In the macroscopic analysis, no statistically significant difference was observed (p = 0.120 and p = 0.186, for the 7th and 14th days of death, respectively). The histological evaluation revealed no statistically significant difference in the variables acute inflammation (p = 0.014) and fibrosis (p = 0.018), when compared the group aveloz with the control group on day 14. CONCLUSION: The crude hydroalcoholic extract of Euphorbia tirucalli L. demonstrated better outcomes in the healing process, acute inflammation and fibrosis on the 14 day postoperatively.
Subject(s)
Animals , Male , Mice , Euphorbia/chemistry , Inflammation/drug therapy , Phytotherapy , Plant Extracts/therapeutic use , Wound Healing/drug effects , Fibrosis , Fibroblasts/drug effects , Inflammation/pathology , Plant Extracts/pharmacology , Random Allocation , Skin/drug effects , Skin/pathology , Time Factors摘要
In order to assess the anticancer action of extracts obtained by latex from Calotropis procera and Pedilanthus tithymaloides, samples were collected from adult plants. Soluble proteins were extracted with 16 uL of 50 mM sodium acetate pH 5/ug integral latex and centrifugation at 16,000 x g for 15 min, the supernatant was named "latex crude extract" (LCE). The "latex methanolic extract" (LME) was obtained on dried latex. Both extracts were tested in vitro by cytotoxic and cytostatic activity in Jurkat cell cultures. Cellular viability, proliferation, necrosis and apoptosis were evaluated. LCE and LME of C. procera were found with cytotoxic and cytostatic activity after 24 incubation hours (p < 0,05) with doses from 1ug/mL. The LCE and LME of P. tithymaloides presented cytotoxic effect (p < 0,05) from 50 ug/mL and from 1ug/mL, respectively.
Con el objetivo de evaluar el potencial anticanceroso de extractos de látex de Calotropis procera y Pedilanthus tithymaloides se colectaron muestras de plantas adultas. Las proteínas solubles fueron extraídas con 16 uL de acetato de sodio 50 mM pH 5/ug de látex integral y centrifugación a 16.000 x g durante 15 min, denominándose al sobrenadante extracto crudo de látex (ECL). El extracto metanólico de látex (EML) se obtuvo sobre látex deshidratado. Ambos extractos fueron probados en su actividad citotóxica y citostática in vitro sobre cultivos de células Jurkat. Se realizaron estudios de viabilidad, proliferación, necrosis y apoptosis celular. El ECL y el EML de C. procera presentaron actividad citotóxica y citostática después de 24 y 48 horas de incubación (p < 0,05) con dosis desde 1 ug/mL. Los ECL y EML de P. tithymaloides presentaron efectos citotóxicos (p < 0,05) a partir de 50 ug/mL y desde 1 ug/mL respectivamente.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Calotropis/chemistry , Euphorbia/chemistry , Plant Extracts/pharmacology , Apoptosis , Cell Culture Techniques , Cell Survival , Jurkat Cells , Latex , Methanol , Cell Proliferation摘要
The present work was carried out to evaluate the molluscicidal activity of active ingredient Taraxerol with the acetone extract of Euphorbia tirucalli against Lymnaea acuminata snail. The (fecundity, hatchability and survivability) of snail L. acuminata exposed to this extract was studied. The effects of the tested extracts on life-history traits of harmful snail L. acuminata have also been evaluated, and this study also expounds the inhibitory effects of these extracts singly as well as in binary combination (1:1 ratio). It concluded that these herbal products act as a potential source of molluscicides, and that they would also have the advantage of easy availability, low cost, biodegradability and greater acceptance amongst users than synthetic pesticide.
O presente trabalho foi levado a efeito para avaliar a atividade moluscicida do ingrediente ativo Taraxerol junto com o extrato de acetona da Euphorbia tirucalli contra o caramujo Lymnaea acuminata. Foram estudados a fecundidade, o desenvolvimento e sobrevivência do caramujo Lymnaea acuminata exposto a estes extratos. Os efeitos danosos destes extratos testados na vida do caramujo L. acuminata foram também avaliados e este estudo demonstra os efeitos inibidores destes extratos isolados ou em combinação binária (relação l:1). Concluiu-se que estes produtos vegetais agem como fontes potenciais de moluscicidas e que eles também têm a vantagem de obtenção fácil, baixo custo, biodegradabilidade e maior aceitação entre os usuários do que os pesticidas sintéticos.
Subject(s)
Animals , Euphorbia/chemistry , Lymnaea/drug effects , Molluscacides , Oleanolic Acid/analogs & derivatives , Plant Extracts , Dose-Response Relationship, Drug , Reproduction/drug effects摘要
The toxic effect of binary and tertiary combinations of Euphorbia hirta Linn latex powder with other plant molluscicidal compounds, were evaluated against the freshwater snails Lymnaea (Radix) acuminata and Indoplanorbis exustus in pond. These combinations showed significant time and dose dependent effect against both the snails. These compounds at higher doses were also lethal to freshwater fish Channa punctatus (Bloch) (Channidae {Ophicephalidae}), which shares the habitat with these snails, but the LC90 (24h) doses of snails have no apparent killing properties in fish populations when treated in mixed population of snails and fish.
Os efeitos tóxicos das combinações binárias e terciárias do pó de látex da Euphorbia hirta Linn assim como outros compostos vegetais moluscicidas foram avaliados em sua ação sobre caramujos de água doce Lymnaea (Radix) acuminata e Indoplanorbis exustus em represas. Estas combinações mostraram significante efeito dose e tempo dependente contra ambos os caramujos. Estes compostos em doses altas foram também letais para peixes de água doce Channa punctatus (Bloch) (Channidae {Ophicephalidae}), que compartilham o ambiente com estes caramujos mas a dose LC90 (24h) para caramujos aparentemente não tem propriedade de matar as populações de peixes quando uma população mista de peixes e caramujos são tratadas.
Subject(s)
Animals , Euphorbia/chemistry , Latex , Molluscacides , Plant Extracts , Snails , Disease Vectors , Lymnaea , Latex/isolation & purification , Molluscacides/isolation & purification , Snails/classification摘要
Euphorbia tirucalli [Euphorbiaceae family] an environmental risk factor for Burkitt's lymphoma also has pharmacological activities. In the northeast of region in Brazil its latex is used as an antimicrobial, antiparasitic in the treatment of coughs, rheumatism, cancer and other disease as folk treatment. The prevalent constituents of this plant latex are diterpenes from the Inganen types [ingenol esters] as well as the tigliane [phorbol esters]. Scientifically, there is not any data till now about anticancer effects of the Euphorbia tirucalli Linn., since the Ingenol esters have already presented tumor-promoting ability. Microtubules [MTs], and cytoskeletal proteins are essential in eukaryotic cells for a variety of functions, such as cellular transport, cell motility and mitosis. Single Inganen in cytoplasm can interact with these proteins and affect on their crucial functions. In this study, we showed the effects of Inganen on MT organization using ultraviolet spectrophotometer and fluorometry. The fluorescent spectroscopy showed a significant tubulin conformational change at the presence of Inganen which decrease polymerization of tubulin as well as the ultraviolet spectroscopy results. The aim of this study is to find the potential function of Inganen for treatment of cancer in cells and human organs
Subject(s)
Humans , Euphorbia/chemistry , Microtubules/chemistry , Microtubules/drug effects , Polymers/chemistry , Spectrometry, Fluorescence摘要
It has been shown previously that the laticifer fluid of Calotropis procera (Ait.) R.Br. is highly toxic to the egg hatching and larval development of Aedes aegypti L. In the present study, the larvicidal potential of other laticifer fluids obtained from Cryptostegia grandiflora R.Br., Plumeria rubra L. and Euphorbia tirucalli L. was evaluated. We attempted to correlate larvicidal activity with the presence of endogenous proteolytic activity in the protein fraction of the fluids. After collection, the fluids were processed by centrifugation and dialysis to obtain the soluble laticifer protein (LP) fractions and eliminate water insoluble and low molecular mass molecules. LP did not visibly affect egg hatching at the doses assayed. LP from Cr. grandiflora exhibited the highest larval toxicity, while P. rubra was almost inactive. E. tirucalli was slightly active, but its activity could not be correlated to proteins since no protein was detected in the fluid. The larvicidal effects of LP from C. procera and Cr. grandiflora showed a significant relationship with the proteolytic activity of cysteine proteinases, which are present in both materials. A purified cysteine proteinase (papain) from the latex of Carica papaya (obtained from Sigma) was similarly effective, whereas trypsin and chymotrypsin (both serine proteinases) were ineffective. The results provide evidence for the involvement of cysteine proteinase activity in the larvicidal action of some laticifer fluids. C. procera is an invasive species found in areas infested with Ae. aegypti and thus could prove useful for combating mosquito proliferation. This is the first report to present evidence for the use of proteolytic enzymes as chemical agents to destroy Ae. aegypti larvae.
Subject(s)
Animals , Aedes/drug effects , Apocynaceae/chemistry , Apocynaceae/chemistry , Cysteine Proteases/pharmacology , Euphorbia/chemistry , Insect Proteins/drug effects , Latex/pharmacology , Aedes/growth & development , Cysteine Proteases/isolation & purification , Insect Proteins/physiology , Larva/drug effects , Larva/growth & development , Latex/chemistry , Latex/isolation & purification摘要
The reproductive activity of Biomphalaria glabrata exposed to Euphorbia splendens var. hislopii latex was evaluated. Parameters related to fecundity and fertility were observed. The snails were exposed to the LD50 (1 mg/l) of crude latex. At the first week post exposure (p.e.), the egg laying was reduced. After the fourth week p.e., an increase of the number of eggs/snail occurred. The results showed a marked reduction in the hatching of the snails, revealing an interference of latex exposure with the reproductive process of B. glabrata of E. splendens var. hislopii. The LD50 of the latex may be used as an alternative method to control the size of the populations of B. glabrata in field.
Subject(s)
Animals , Female , Male , Biomphalaria/drug effects , Euphorbia/chemistry , Latex/pharmacology , Biomphalaria/physiology , Latex/isolation & purification , Plant Extracts/pharmacology , Reproduction/drug effects , Reproduction/physiology摘要
Molluscides have been used as one of the strategies to control schistosomiasis. Many plant extracts with molluscidal effects have been tested, but the action of the latex of Euphorbia splendens var. hislopii is considered the most promising because it meets the recommendations of the World Health Organization (WHO). The objective of this study was to determine the lethal dose and identify the effects of the different doses of latex of E. splendens var. hislopii on the physiology of Biomphalaria glabrata submitted to treatment for 24 h. The concentrations of glucose, uric acid and total proteins in the hemolymph and of glycogen in the digestive gland and cephalopodal mass were determined. The LD50 value was 1 mg/l. The highest escape index was found to be at a concentration of 0.6 mg/l. The results showed that the latex of E. splendens var. hislopii caused a sharp reduction in the reserves of glycogen in the digestive gland and elevation of the protein content in the hemolymph of B. glabrata.
Subject(s)
Animals , Biomphalaria/drug effects , Euphorbia/chemistry , Latex/pharmacology , Biomphalaria/physiology , Glucose/analogs & derivatives , Glycogen/analogs & derivatives , Hemolymph/chemistry , Latex/isolation & purification , Plant Extracts/pharmacology , Proteins/analysis , Uric Acid/analogs & derivatives摘要
Laboratory evaluation was made to assess the molluscicidal activity of different fractions of Euphorbia royleana (Family- Euphorbiaceae) latex obtained through sephadex gel column against freshwater snail Lymnaea (Radix) acuminata Lamarack. This snail is the vector of liver fluke, Fasciola hepatica Linnaeus and Fasciola gigantica Cobbold, which causes endemic fascioliasis in cattle and livestock. The toxic effect of the different fractions was time dependent and fifth fraction obtained through benzene: ethyl acetate (5:5) had maximum molluscicidal activity against Lymnaea acuminata. There was a significant negative correlation between LC values and exposure periods thus increase in exposure time, the LC50 value of V fraction of Euphorbia royleana latex was decreased from 14.28 mg/l (24 hr) to 9.28 mg/l (96 hr) against Lymnaea acuminata. After exposure to sub-lethal concentrations of this fraction there were significant time and dose dependent alterations observed in pyruvate, lactate levels, ALAT, AAT, AChE and cytochrome oxidase enzyme activities in different body tissues of Lymnaea acuminata. It is proposed that the fifth fraction of E. royleana latex can be used as a molluscicide for controlling the harmful snail population from aquatic ecosystem without any harm due to their reversible toxic action.