RESUMO
Lygodium microphyllum Cav. (Family: Lygodiaceae) is a perennial, snake fern and an invasive weed in Florida and also known as old world climbing fern. This study is intended to evaluate the antipyretic, analgesic, anti-inflammatory, antidiarrheal and anthelmintic activity of methanol extract of Lygodium microphyllum Cav. leaves (MELM) by in vivo, in vitro and in silico approaches. In addition, Biovia, PyRx autoDock Vina, UCSF Chimera have been applied to investigate the docking study in order to evaluate the binding interaction and an online tool was used to explore the ADME/T properties of selected bioactive compounds. In acetic acid induced writhing study, MELM inhibited 44.28% and 56.61% of writhes at 200 and 400 (mg/kg) respectively compared to standard drug Diclofenac-Na (10 mg/kg) (74.42% inhibition). In anti-inflammatory experiment by formalin triggered licking method, MELM caused significant (p < 0.05) inhibition of licking in both early phase (42.97%, 63.30%) and late phase (43.35%, 63.03%) at the doses of 200 and 400 mg/kg respectively, whereas reference drug Ibuprofen inhibited paw licking 77.18% in early phase and 76.86% in late phase. MELM also showed promising antipyretic potential where the maximum reduction of fever was produced by MELM 400 mg/kg whose fever lowering capacity is close to the prescribe drug Indomethacin 4 mg/kg, i.p. In Castor oil triggered diarrhea method, MELM delayed the onset time of diarrhea, continuous persistence of wet feces, and decreased the weight of wet feces remarkably. Defection inhibition was achieved 27.56% and 51.72%, for MELM 200 and at 400 (mg/kg) respectively while loperamide 2 (mg/kg) yields 55.17% inhibition of the diarrheal defecation. In anthelmintic bioassay, MELM took 5.83 ± 0.83 and 41.67 ± 1.78 min respectively for paralyzing and death compared to standard drug albendazole; (paralysis time 4.00 ± 0.73 min and death time 31,00 ± 1.71 min). Isoeleutherol, isoquercetin and quercetin were found prominent in molecular docking study and ADME/T analysis verified their drug likeliness. The research validates the moderate analgesic, anti-inflammatory, and remarkable antipyretic, antidiarrheal, anthelmintic activities of the plant extract which can be used an alternative source of novel therapeutics.
Assuntos
Anti-Helmínticos/farmacologia , Diarreia/tratamento farmacológico , Gleiquênias/química , Febre/tratamento farmacológico , Inflamação/tratamento farmacológico , Dor/tratamento farmacológico , Extratos Vegetais/farmacologia , Folhas de Planta/química , Albendazol/farmacologia , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Antidiarreicos/farmacologia , Antipiréticos/farmacologia , Fezes/química , Gleiquênias/toxicidade , Ibuprofeno/uso terapêutico , Loperamida/farmacologia , Camundongos , Simulação de Acoplamento Molecular , Extratos Vegetais/toxicidade , Folhas de Planta/toxicidadeRESUMO
CONTEXT: Diplazium esculentum, a commonly consumed seasonal vegetable, has been reported to have some pathological effects in some animals. But, its effect on the male reproductive function has not yet been studied. OBJECTIVE: To investigate the effects of boiled D. esculentum (BDE), the form which human consumes, on male reproductive functions of Swiss albino mice. MATERIALS AND METHODS: Male (120 in no.) and female (80 in no.) Swiss albino mice (6-8 weeks of age) were fed orally with 80, 160 and 320 mg/kg bw of BDE within a span of 180 d. After the treatment, body weight, absolute- and relative-testis weight, relative-weight of other organs, their biochemical parameters, hypo-osmotic swelling test (HOST) of spermatozoa, testis histology and fertility and fecundity tests were performed to justify the toxic effects of D. esculentum on male reproductive functions. RESULTS: Significant dose- and time-dependent decreases were observed in body weight, absolute- and relative-testis weight, relative-weights of other organs and their biochemical parameters, percentage of live spermatozoa and percentage of fertility and fecundity in BDE fed mice. Significant decreases were observed in diameter, perimeter and area of the seminiferous tubules of mice treated for 180 d. The percentage of empty seminiferous tubules was increased significantly in BDE treated mice when compared to the controls. DISCUSSION AND CONCLUSION: These results suggest that the intake of D. esculentum, even after cooking, may induce infertility by altering the male reproductive function, and therefore, should be evaluated further as a potential antifertility agent.
Assuntos
Gleiquênias/toxicidade , Infertilidade Masculina/induzido quimicamente , Extratos Vegetais/toxicidade , Reprodução/efeitos dos fármacos , Túbulos Seminíferos/efeitos dos fármacos , Testículo/efeitos dos fármacos , Animais , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Feminino , Fertilidade/efeitos dos fármacos , Infertilidade Masculina/patologia , Infertilidade Masculina/fisiopatologia , Masculino , Camundongos , Tamanho do Órgão , Fitoterapia , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Gravidez , Medição de Risco , Túbulos Seminíferos/patologia , Espermatozoides/efeitos dos fármacos , Espermatozoides/patologia , Testículo/patologia , Testículo/fisiopatologia , Fatores de Tempo , Testes de Toxicidade , Redução de Peso/efeitos dos fármacosRESUMO
. Doenças parasitárias infecciosas como leishmaniose e doença de Chagas tem se difundido nas últimas décadas a locais onde antes não se observava sua ocorrência. São consideradas negligenciadas por assolarem países pobres e serem marginalizadas farmacologicamente. O tratamento não apresenta muitas opções de fármacos e estes demonstram relevante toxicidade contribuindo para o aparecimento de diversos efeitos colaterais. A pesquisa com produtos naturais tem se mostrado uma interessante alternativa para a procura por novos fármacos. Lygodium venustum é uma samambaia cosmopolita de hábito lianescente encontrada na encosta na Chapada do Araripe, considerada por algumas populações americanas como planta medicinal para o tratamento de dermatoses, infecções, micoses e tricomoníases. Neste estudo foi avaliada sua atividade anti-parasitária contra Leishmania brasiliensis e Trypanosoma cruzi, bem como sua citotoxicidade através de ensaios n vitro. Foram testadas a fração hexânica e o extrato etanólico obtido das folhas de Lygodium venustum em diferentes concentrações. Para os testes in vitro de T. cruzi, foi utilizado o clone CL-B5 e para Leishmania brasiliensis foram utilizadas formas promastigotas. O ensaio de citotoxicidade foi realizado com linhagens de fbroblastos. L. venustum não apresentou atividade antiparasitária clinicamente relevante na forma de extrato etanólico bruto nem como fração hexânica contra Leishmania. A fração hexânica apresentou uma atividade intermediária contra T. cruzi, porém a concentração de efeito moderado possui citotoxicidade máxima tornando-se inviável para aplicação clínica. Entretanto, a citoxicicidade apresentada poderá ser útil em pesquisas sobre atividade antineoplásica em células tumorais.
Infectious and parasitic diseases like leishmaniasis and Chagas disease have spreading recent decades to places not observed before. They are considered neglected by desolating poor countries and marginalized pharmacologically. There are not many options for the treatment and these drugs have shown signifcant toxicity contributing to the appearance of several side effects. Research on natural products has been shown to be an interesting alternative to the search for new drugs. Lygodium venustum is a cosmopolitan fern with latescence habit found on the Chapada do Araripe, considered by some American popula-tions as a medicinal plant for the treatment of skin diseases, infections, fungal infections and trichomoniasis. This study evaluated its antiparasitic activity against Trypanosoma cruzi and Leishmania brasiliensis, as well as its cytotoxicity through trials in vitro. We tested the ethanolic extract and hexane fraction obtained from the leaves of L. venustum at different concentrations. For in vitro tests of T. cruzi, we used the clone CL-B5 and for L. brasiliensis we used promastigotes. The cytotoxicity assay was performed with strains of fbroblasts. L.venustum showed no antiparasitic activity clinically relevant in the form of crude ethanolic extractor as the hexane fraction against Leishmania. The hexane fraction showed an intermediate activity against T.cruzi, but the concentration of moderate effect has maximum cytotoxicity becoming unfeasible for clinical application. However, the cytotoxicity presented may be useful in research on antineoplastic activity in tumor cells.
Assuntos
Gleiquênias/toxicidade , Leishmania braziliensis , Tripanossomicidas/análise , Trypanosoma cruzi , Antiparasitários/análiseRESUMO
The aim of this study was to evaluate the antitumor potential of Macrothelypteris torresiana by studying in vitro antitumor activity of the protoapigenone, as well as in vivo antitumor activity and acute/subacute oral toxicity of the total flavonoid fraction from the roots of M. torresiana. Considering that the protoapigenone is a main constituent of the total flavonoid fraction and it might play a key role in the antitumor activity of M. torresiana, the MTT assay was used to investigate the in vitro antitumor activity of the protoapigenone. Our study revealed that the protoapigenone of M. torresiana showed significant antitumor activity towards Hep G2, Tca-8113, MCF-7, M5 and K562 with IC(50) values of 2.3, 0.6, 0.8, 0.3 and 0.9 µg/ml, respectively. The antitumor potential of the total flavonoid fraction was evaluated using preparations 1, 2 and 3, which were prepared by total flavonoid fraction directly diluted with sterile saline, dissolved using sodium carboxymethyl cellulose (CMC-Na) and included by hydroxypropyl-ß-cyclodextrin, respectively. These were investigated in vivo using mouse sarcoma S-180 in BALB/c mice after completing tumor inoculation for 24h. Pronounced antitumor activity was observed in the treated groups for preparations 2 and 3, and the high and medium doses in particular showed very high inhibition ratio of tumor growth (>50%). No significant difference was observed when compared to the positive control group (5-fluorouracil). The acute/subacute oral toxicity test was performed, and the results of acute oral toxicity showed that the LD(50) values of preparations 2 and 3 were 2.76 and 0.87 g/kg body wt., respectively. According to the results of the subacute oral toxicity study, the total flavonoid fraction had low toxicity. The overall results of this study suggest that the total flavonoid fraction from the roots of M. torresiana shows significant antitumor activity and represents a potential source of medicine for the treatment of cancer.
Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Cicloexanonas/uso terapêutico , Gleiquênias/química , Flavonas/uso terapêutico , Neoplasias/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Sarcoma/tratamento farmacológico , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Cicloexanonas/isolamento & purificação , Cicloexanonas/farmacologia , Feminino , Gleiquênias/toxicidade , Flavonas/isolamento & purificação , Flavonas/farmacologia , Células Hep G2 , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas , Ensaios Antitumorais Modelo de Xenoenxerto/métodosRESUMO
Se realizó un estudio de toxicidad aguda en ratas Sprague Dawley de ambos sexos mediante la administración oral única del producto QT2B21 obtenido a partir de la especie de helecho Nephrolepis cordifolia, para determinar su toxicidad. Fueron evaluados 3 niveles de dosis: 33,33, 133,32 y 533,28 mg/kg. Se determinaron algunos índices hematológicos sin encontrar efectos tóxicos atribuibles a la administración del producto. Se realizaron los estudios anatomopatológico (por inspección macroscópica) e histopatológico de los principales órganos. La inspección de estos no demostró alteraciones macroscópicas. Según el resultado del estudio histopatológico, sólo fueron observadas diferencias estadísticamente significativas en el porcentaje de peso relativo de los testículos en el grupo tratado con la dosis intermedia con respecto al grupo control. Este efecto no fue dependiente de la dosis. Se concluyó que la administración única por vía oral del producto QT2B21, no produjo alteraciones por toxicidad que pudieran ser atribuidas al mismo. Se consideró este producto como tolerable en ratas Sprague Dawley de ambos sexos en el rango de dosis desde 33,33 hasta 533,28 mg/kg de peso.(AU)
Assuntos
Animais , Ratos , Plantas Medicinais/toxicidade , Extratos Vegetais/toxicidade , Gleiquênias/toxicidade , Ratos Sprague-DawleyRESUMO
Onychium contiguum (Family Cryptogrammaceae) is a common terrestrial fern in the Himalayas and in many other parts of the world. It is also present on the pastures in areas where grazing animals suffer from bovine urinary bladder cancer. This fern is occasionally grazed by animals and in some areas it is present as a contaminant in grasses stored for winter feeding. Certain species of the genus Onychium are used in folk medicine. Long-term exposure of experimental animals to O. contiguum appeared to cause tumours of the ileum. urinary bladder and mammary glands.