RESUMO
Leaves of Croton stipulaceuswere extracted (EHex, ECHCl3and EEtOH extracts) to assesstheir antioxidant potential, anti-inflammatory activity in murine models and acute toxicity. EEtOH showed the highest effect in DPPH (37.80% inhibition), FRAP (1065.00 ± 55.30 µmolFe2+) and total polyphenols (231.24 ± 9.05 meq AG/gM). EHex was the most active, ~ 50% inhibition of TPA-induced ear edema; while EEtOH (dose of 2 mg/ear) showed the highest inhibition in the chronic model (97% inhibition), and inhibited MPO activity (48%). In carrageenan-induced edema, ECHCl3(dose 500 mg/kg) was the most active. None of the extracts showed acute toxicity (LD50) at 2 g/kg (p.o.). This work is the first report that supports the traditional use of C. stipulaceusas an anti-inflammatory.
De las hojas de Croton stipulaceusse obtuvieron diferentes extractos (EHex, ECHCl3y EEtOH) evaluando el potencial antioxidante y la actividad antiinflamatoria en modelos murinos y la toxicidad aguda. El EEtOH mostró mayor efecto en DPPH (37.80% inhibición), FRAP (1065.00 ± 55.30 µmolFe2+) y polifenolestotales (231.24 ± 9.05 meq AG/gM). El EHex fue el más activo, cercano al 50% de inhibición del edema auricular inducido con TPA; mientras que el EEtOH (dosis de 2 mg/oreja) mostró la mayor inhibición en el modelo crónico (97% inhibición), e inhibió la actividad de la MPO (48%). En el edema inducido con carragenina, el ECHCl3(dosis 500 mg/kg) fue el más activo. Ninguno de los extractos mostró una toxicidad aguda (DL50) mayor a 2 g/kg (p.o). Este trabajo es el primer reporte que sustenta el uso tradicional de C. stipulaceuscomo antiinflamatorio.
Assuntos
Animais , Ratos , Extratos Vegetais/administração & dosagem , Croton/química , Inflamação/tratamento farmacológico , Anti-Inflamatórios/administração & dosagem , Antioxidantes/administração & dosagem , Fenóis/análise , Extratos Vegetais/química , Folhas de Planta , Modelos Animais de Doenças , Anti-Inflamatórios/química , Antioxidantes/químicaRESUMO
Hyperammonemia is characterized by the excessive accumulation of ammonia in the body as a result of the loss of liver detoxification, leading to the development of hepatic encephalopathy (HE). These metabolic alterations carry cognitive and motor deficits and cause neuronal damage, with no effective treatment at present. In this study, we aimed to evaluate the effect of two subacute oral administrations of flaxseed oil (0.26 and 0.52 mL/kg) on short- and long-term memory, visuospatial memory, locomotor activity, motor coordination, and the neuronal morphology of the prefrontal cortex (PFC) via tests on Wistar rats with hyperammonemia. The goal was to identify its role in the regulation of cerebral edema, without liver damage causing cerebral failure. In contrast with an ammonium-rich diet, flaxseed oil and normal foods did not cause cognitive impairment or motor alterations, as evidenced in the short-term and visuospatial memory tests. Furthermore, the flaxseed oil treatment maintained a regular neuronal morphology of the prefrontal cortex, which represents a neuroprotective effect. We conclude that the oral administration of flaxseed oil prevents cognitive and motor impairments as well as neuronal alterations in rats with hyperammonemia, which supports the potential use of this oil to ameliorate the changes that occur in hepatic encephalopathy.
Assuntos
Linho , Encefalopatia Hepática , Hiperamonemia , Ratos , Animais , Encefalopatia Hepática/etiologia , Encefalopatia Hepática/prevenção & controle , Encefalopatia Hepática/metabolismo , Ratos Wistar , Óleo de Semente do Linho/farmacologia , Hiperamonemia/complicações , CogniçãoRESUMO
El presente artículo de reflexión revisa aspectos bioéticos en estudios científicos de plantas utilizadas en medicina tradicional para el tratamiento del cáncer en México. El conocimiento de las plantas medicinales documentadas en la medicina tradicional se relaciona con enfermedades como el cáncer. Esta enfermedad presenta altas tasas de mortalidad en el mundo, lo que incrementa la necesidad de nuevos fármacos para la quimioterapia. Aquí las plantas medicinales juegan un papel importante. Así, al ejecutar un estudio de plantas medicinales se deben considerar aspectos bioéticos fundamentales para la medicina tradicional como el muestreo, el estudio fitoquímico y biológico en líneas celulares de cáncer, basándose en la normatividad vigente, en estándares internacionales del Instituto Nacional del Cáncer y, principalmente, en los cuatro principios básicos de la bioética. Concluimos que es tarea de la comunidad científica avalar o desmentir el uso tradicional de las plantas medicinales para el tratamiento de enfermedades. El estudio de especies vegetales debe cumplir criterios donde la teoría, la investigación y la práctica ofrezcan soluciones a largo plazo y la protección ética de estas, del conocimiento tradicional y de los pacientes que recurren a esta alternativa.
The present reflection paper reviews bioethical aspects in scientific studies of plants used in traditional medicine for the treatment of cancer in Mexico. The knowledge of medicinal plants documented in traditional medicine is related to diseases such as cancer. This disease has high mortality rates worldwide, increasing the need for new chemotherapy drugs. Here medicinal plants play an important role. Thus, when executing a study of medicinal plants, fundamental bioethical aspects for traditional medicine such as sampling, phytochemical and biological study in cancer cell lines, based on current regulations, international standards of the National Cancer Institute and, mainly, the four basic principles of bioethics, should be considered. We conclude that it is the task of the scientific community to endorse or deny the traditional use of medicinal plants for the treatment of diseases. The study of plant species must meet criteria where theory, research and practice offer long-term solutions and the ethical protection of plant species, traditional knowledge and patients who resort to this alternative.
Assuntos
Plantas Medicinais , Bioética , Neoplasias/terapia , Grupos Populacionais , Compostos Fitoquímicos , Medicina Tradicional , MéxicoRESUMO
OBJECTIVE: To evaluate the anti-inflammatory, analgesic, antioxidant and acute toxicity of extracts obtained from a successive extraction with solvents of ascending polarity [hexane, hex; chloroform, CHCl3 and ethanol (EtOH)] of Ternstroemia sylvatica Schltdl. & Cham. METHODS: The antioxidant potential was evaluated by 2,2 diphenyl-1-picrylhydrazyl, the ferric reducing/antioxidant power assays and by determining the total phenolic content. The anti-inflammatory and antinociceptive effects were evaluated using the in vivo croton oil-induced ear edema, phorbol 12-myristate 13-acetate induced ear edema, carrageenan-induced paw edema, acetic acid-induced writhing and formalin murine models. The acute toxicity was tested using the Lorke's method in mice. RESULTS: The EtOH extract was the most active for the antioxidant potential tests diphenyl-1-picrylhydrazyl (68.70% inhibition), ferric reducing/antioxidant power [(2431.30 ± 102.10) mmol Fe2+ and total polyphenols content (215.80 ± 8.50) meqAG/g]. The anti-inflammatory activity was evaluated by topical application of croton oil (2 mg/ear dose) where the EtOH extract showed the strongest activity compared to the control group (45.13% inhibition), whereas in the phorbol 12-myristate 13-acetate model, at the same dose, the CHCl3 extract showed the highest inhibition (42.88%). In the carrageenan induced edema model, the EtOH extract showed a stronger inhibition compared to indomethacin (56.34% and 50.70% at doses of 250 and 500 mg/kg of extract, respectively) during the first hour. Similarly, the same extract showed the highest analgesic activity (30.60% inhibition) in the acetic acid contortion assay, and in the formalin test it showed a greater effect with respect to the control group in both phases. CONCLUSIONS: Our work confirms the value of Ternstroemia sylvatica as an important anti-inflammatory and analgesic plant, whose mechanism seems to be associated to its antioxidant effects, and supports its uses in the Mexican traditional medicine.
RESUMO
This work describes the use of Colubrina greggii as a model to investigate the use of chemometric analysis combined with data from a leishmanicidal bioassay, using Principal Component Analysis (PCA) and Orthogonal Projections to Latent Structures (O-PLS), to detect biologically active natural products in crude extracts from plants having little or no phytochemical information. A first analysis of the HPLC-UV profiles of the extract and its semi-purified fractions using both Principal Component Analysis (PCA) and Orthogonal Partial Least Squares (O-PLS) indicated that the components at tR 48.2, 48.7, 51.8min correlated with the variation in bioactivity. However, a further O-PLS analysis of the HPLC-UV profiles of fractions obtained through a final semi-preparative HPLC purification showed two components at tR 48.7 and 49.5min which correlated with the variation of the bioactivity in a high performance predictive model, with high determination coefficient, high correlation coefficient values (R(2) and Q(2)=0.99) and a low root mean square error (RMSE=0.018). This study demonstrates that the association of chemometric analysis with bioassay results can be an excellent strategy for the detection and isolation of bioactive metabolites from phytochemically unknown plant crude extracts.
Assuntos
Compostos Fitoquímicos/metabolismo , Extratos Vegetais/metabolismo , Antiparasitários/isolamento & purificação , Antiparasitários/metabolismo , Antiparasitários/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Colubrina/química , Colubrina/metabolismo , Misturas Complexas , Análise dos Mínimos Quadrados , Leishmania mexicana/efeitos dos fármacos , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Plantas Medicinais , Análise de Componente Principal , Raios UltravioletaRESUMO
Salvia divinorum (Lamiaceae) is a herb native to Mexico where it is used by Mazatec shamans for spiritual and divination purposes. S. divinorum products are easily available to consumers and are used worldwide as legal highs because of the hallucinogenic effects caused mainly by salvinorin A. Highly popular videos and websites on the internet depicting the use of S. divinorum products have contributed to an increase in their consumption. Recent reports have highlighted the potential of these products to induce psychosis in consumers. In Mexico, dried leaf extracts of S. divinorum are sold in different strengths, claiming to correlate with increasing amounts of salvinorin A. In order to determine the variability of salvinorin A content between brands and to investigate possible correlation between brand strengths, this study sought to quantify salvinorin A in commercial products available in Mexico using an HPLC method. The HPLC analytical method showed a correlation coefficient R(2)>0.99, with LOD of 0.44 µg/mL and LOQ of 1.34 µg/mL. The retention time for salvinorin A was 23.09±0.95 min and the measured concentrations ranged between 8.32±0.65 and 56.52±3.77 mg/g dried leaf. The results for brand c did not show an agreement between the declared and the calculated amount of salvinorin A. Additionally, the emergence in Mexico of high strength salvia products (100×), the lack of regulation and the observed variability of salvinorin A content between brands of commercial legal highs products of S. divinorum could result in a health problem for consumers.
Assuntos
Diterpenos Clerodânicos/análise , Extratos Vegetais/análise , Psicotrópicos/química , Salvia/química , Cromatografia Líquida , Comércio , Humanos , MéxicoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Cnidoscolus chayamansa Mc Vaugh (Euphorbiaceae) is commonly known as 'chaya' in Central America. In South East Mexico, because of its high nutritional values, is an important part of the diet of many indigenous communities. Chaya is also used as a traditional remedy for the treatment of diabetes, rheumatism, gastrointestinal disorders and inflammation-related diseases. Although Cnidoscolus chayamansa is one of most used and valued medicinal plants, only few studies on documenting its pharmacological properties can be found. MATERIALS AND METHODS: Dried leaves of Cnidoscolus chayamansa were subjected to a successive maceration using Hex, EtOAc and EtOH. The antioxidant activities of the extracts were tested using the DPPH radical scavenging, Ferric reducing/antioxidant power and total phenolic content assays. To determine the anti-inflammatory activity, the TPA-induced mouse ear edema and the carrageenan-induced mouse paw edema assays were used. The cardioprotective effects of the EtOH extract was determined using the ischemia/reperfusion (I/R) rat model. Finally, the acute toxicity was determined using Lorke's method. RESULTS: The results showed a similar anti-inflammatory activity (≈30%) for all extracts but only the EtOAc extract showed relevant activity when applied intraperitoneally. When tested for their antioxidant activity none of the extracts showed a significant activity suggesting that the antinflammatory activity is not related to a direct free radical scavenging of the extracts. Additionally, the EtOH extract showed a strong cardioprotective effect at 500mg/kg when given orally. Both the EtOAc and the EtOH extract have a LD50 >5g/kg, confirming their safety in acute oral administration. CONCLUSIONS: All these results are relevant for a better understanding of the therapeutic used of Cnidoscolus chayamansa in the Mexican traditional medicine and highlights its cardioprotective potential.
Assuntos
Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Cardiotônicos/uso terapêutico , Euphorbiaceae , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/toxicidade , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/toxicidade , Compostos de Bifenilo/metabolismo , Cardiotônicos/química , Cardiotônicos/farmacologia , Cardiotônicos/toxicidade , Carragenina , Orelha/patologia , Edema/induzido quimicamente , Edema/tratamento farmacológico , Masculino , Medicina Tradicional , México , Camundongos , Fenóis/análise , Fitoterapia , Picratos/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Folhas de Planta , Ratos , Ratos Wistar , Traumatismo por Reperfusão/tratamento farmacológico , Acetato de Tetradecanoilforbol , Testes de Toxicidade AgudaRESUMO
The crude ethanolic extract of leaves, stem-bark and roots of J. flammea were tested for their cytotoxic effect against two mammalian cell lines (HeLa and RAW 264.7) and four bacterial species (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa). When tested at the concentration of 100 microg/mL, the root extract showed the highest cytotoxic activity against mammalian cells followed by the stem-bark extract while the leaves extract did not show significant activity. No antibacterial activity was detected for all extracts when tested up to 500 microg/disc in the disc diffusion assay. The cytotoxic root extract was subjected to fractionation using solvents of ascending polarity: petroleum ether, chloroform, ethylacetate, butanol and water. The water fraction which showed cytotoxic activity was further subjected to routine bioassay-guided fraction to lead to the isolation of sakurasosaponin as the active principle. The recorded IC50 value for sakurasosaponin was 11.3 +/- 1.52 and 3.8 +/- 0.25 microM (n=3) against HeLa and RAW 264.7 respectively. The identification of sakurasosaponin was based on analysis of spectroscopic data.