In-vivo Assessment of Antipyretic and Anti-inflammatory Activities of Gymnosporia Royleana Extract in Mice / Evaluación in vivo de las Actividades Antipiréticas y Antiinflamatorias del Extracto de Gymnosporia Royleana en Ratones

ABSTRACT Objective: Despite the presence of multitude of synthetic drugs against fever and inflammation, none has been proven entirely safe. In contrast, the accepted safety of plant derived natural products is inspiring the world. Based on this fact as well as in view of the diversified activities reported from the genus Gymnosporia, the present study was designed to evaluate the antipyretic and anti-inflammatory activity of Gymnosporia royleana (G royleana). Methods: The methanolic extract of the aerial parts of G royleana was screened for in-vivo antipyretic activity using the brewer's yeast-induced pyrexia mice model and for anti-inflammatory activity using the carrageenan-induced paw oedema and xylene-induced ear oedema mice model. Results: In the antipyretic assay, G royleana extract showed considerable antipyretic activity in a dose dependent fashion. Statistically significant antipyretic effects (p < 0.05) were observed at the end of the second hour of administration for all doses of extract and remained significant until the end of the experiment. The plant extract also displayed promising anti-inflammatory activity, in a dose dependent fashion, in both models of inflammation ie carrageenan- and xylene-induced oedema models, when compared to the controls. In the carrageenan-induced oedema model, significant effects (p < 0.01) were observed for 300 and 600 mg/kg doses after 60 minutes of xylene administration (ie 55.51% and 65.88% inhibition of oedema, respectively). Conclusion: The study provided evidence supporting the antipyretic and anti-inflammatory activity of the G royleana methanolic extract.

RESUMEN Objetivo: A pesar de la presencia de multitud de fármacos sintéticos en el arsenal contra la fiebre y la inflamación, ninguno ha dado pruebas de ser completamente seguro. En contraste con ello, la seguridad aceptada de los productos naturales derivados de las plantas inspira al mundo. Sobre la base de este hecho, así como en vista de las actividades diversificadas que se reportan con respecto al género Gymnosporia, el presente estudio se diseñó con el objeto de evaluar el potencial antipirético y antiinflamatorio de Gymnosporia royleana (G royleana). Métodos: El extracto de metanol de las partes aéreas de G royleana fue tamizado en busca de actividad antipirética in vivo, utilizando el modelo de pirexia inducida por levadura de cerveza en ratones, y de actividad antiinflamatoria utilizando modelos de ratones con oedema de las patas inducido mediante carragenina, y oedema de las orejas inducido mediante xileno. Resultados: En el ensayo antipirético, el extracto de G royleana mostró una actividad antipirética considerable en forma dependiente de la dosis. Se observó un efecto antipirético estadísticamente significativo (p < 0.05) en el transcurso de la segunda hora de administración para todas las dosis de extracto y se mantuvo significativo hasta el final del experimento. El extracto de la planta también mostró una actividad antiinflamatoria prometedora, de una manera dependiente de la dosis, en ambos modelos de inflamación, es decir, modelos de oedema inducido por carragenina y xileno, en comparación con el control. En el modelo de oedema inducido por carragenina, se observó un efecto significativo (p < 0.01) para dosis de 300 y 600 mg / kg después de 60 minutos de administración de xileno (es decir, 55.51% y 65.88% de inhibición del oedema, respectivamente). Conclusión: El estudio proporcionó pruebas suficientes sobre el potencial antipirético y antiinflamatorio del extracto de G royleana.

Evaluation of antipyretic, sedative and hypnotic activities of methanol extract of Tabebuia hypoleuca (C. Wright ex Sauvalle) Urb. stems / [Evaluación de la actividad antipirética, sedante e hipnótica del extracto metanólico de los tallos de Tabebuia hypoleuca (C. Wright ex Sauvalle) Urb

Species of the genus Tabebuia are used in traditional medicine and are reported in the literature for their properties against various diseases. The objective of this study was to evaluate the antipyretic, sedative and hypnotic activities of methanol extract of Tabebuia hypoleuca stems (THME) using the Brewer's yeast induced pyrexia, Open field and Sodium thiopental-induced sleeping time tests, respectively. In the Brewer's yeast induced pyrexia test, THME at 500 mg/kg produced a significant (p<0.001) decrease of the fever as from the first hour after administration and was sustained for 4 h. In the Open-field test, THME did not cause any significant change in the number of crossings, rearing, preening and defecation, and either in the time of immobility. Moreover, THME did not produce changes in neither the sleeping latency nor the sleeping time induced by sodium thiopental. These results showed that THME administered orally at 500 mg/kg exerts antipyretic activity, probably mediated by the inhibition of the enzyme cyclooxygenase-2. This study also showed that THME does not exert sedative and hypnotic effects at the doses tested.

Especies del género Tabebuia se utilizan en la medicina tradicional y se reportan en la literatura por sus propiedades contra diversas enfermedades. El objetivo de este estudio fue evaluar la actividad antipirética, sedante e hipnótica del extracto metanólico de los tallos de Tabebuia hypoleuca (THME) utilizando las pruebas de pirexia inducida por levadura de cerveza, campo abierto y tiempo de sueño inducido por tiopental sódico respectivamente. En el ensayo de pirexia inducida por levadura de cerveza, THME a 500 mg/kg produjo una reducción significativa (p<0.001) de la fiebre a partir de la primera hora después de la administración y se mantuvo durante cuatro horas. En el ensayo de campo abierto, THME no causó ningún cambio significativo en el número de cruces, levantamientos, acicalamientos y defecación, ni en el tiempo de inmovilidad. Además, THME no produjo cambios ni en la latencia de sueño, ni en el tiempo de sueño inducido por tiopental sódico. Estos resultados mostraron que THME administrado oralmente en dosis de 500 mg/kg posee actividad antipirética, mediado probablemente a la inhibición de la enzima ciclooxigenasa-2. Este estudio también demostró que THME no posee actividad sedante e hipnótica en las dosis ensayadas.

Antipyretic potential of herbal coded formulation [Pyrexol]

The antipyretic effect of the aqueous extract of herbal coded formulation containing equal amount of Salix alba, Emblica officinalis, Glycyrrhiza glabra, Adhatoda vasica, Viola odorata, Thea sinensis, Veleriana officinalis, Foeniculum vulgare, Sisymbrium irrio and Achillea millefolium was investigated using the yeast induced pyrexia model in rabbits. Paracetamol was used as a control group. Rectal temperatures of all rabbits were recorded immediately before the administration of the extract or paracetamol and again at 1 hour, after this, temperature was noted at 1 hrs interval for 5 hrs using digital thermometer. At 240 mg/kg dose the extract showed significant reduction in yeast-induced elevated temperature as compared with that of standard drug paracetamol [150 mg/kg]. It is concluded that herbal coded medicine at a dose of 240 mg/kg has marked antipyretic activity in animal models and this strongly supports the ethno pharmacological uses of medicinal plants of this formulation

Antimitotic and antimutagenic action of the Hymenaea stigonocarpa bark on dividing cells / Ação antimitótica e antimutagênica do ritidoma de Hymenaea stigonocarpa Mart ex Hayne na divisão celular

Abstract The objective of this study was to evaluate the action of Hymenaea stigonocarpa bark hydroalcoholic extract against a mutagenic compound using A. cepa meristematic root cells as a test system. The treatment groups were: Negative Control (NC) – distilled water; Positive Control (PC) – paracetamol at a concentration of 0.008 mg/mL, Jatoba Control (JC) – aqueous fraction jatobá-do-cerrado at 0.5 or 1.0 or 1.5 mg/mL, and Simultaneous Treatment (ST) - jatobá-do-cerrado aqueous fraction at a concentration of 0.5 or 1.0 or 1.5 mg/mL associated with paracetamol solution at a concentration of 0.008 mg/mL. All groups were analyzed at 24 and 48 h. Five onion bulbs (five replications) were used for each treatment group. The root tips were fixed in Carnoy and slides prepared by the crush technique. Cells were analyzed throughout the cell cycle, totaling 5,000 for each treatment group at each exposure time. Mitotic indices were subjected to statistical analysis using the chi-square test (p<0.05). From the results it was found that the ST group, at the three concentrations, significantly potentiated the antiproliferative effect of the test system cells when compared to PC, NC and TJ at the three concentrations. Furthermore, the three ST concentrations significantly reduced the number of cell aberrations when compared to the number of aberrant cells obtained for the PC, demonstrating antimutagenic action on the A. cepa test system cells.

Resumo O objetivo do presente trabalho foi avaliar a ação do extrato hidroalcólico do ritidoma de Hymenaea stigonocarpa frente a um composto mutagênico, utilizando como sistema teste as células meristemáticas de raízes de A. cepa. Os grupos tratamentos avaliados foram: Controle Negativo (CN) – água destilada; Controle Positivo (CP) – paracetamol na concentração de 0,008 mg/mL, Controle Jatobá (CJ) – fração aquosa de jatobá-do-cerrado na concentração de 0,5 ou 1,0 ou 1,5 mg/mL, e Tratamento Simultâneo (TS) – fração aquosa de jatobá-do-cerrado na concentração de 0,5 ou 1,0 ou 1,5 mg/mL associada a solução de paracetamol na concentração de 0,008 mg/mL. Todos os grupos foram analisados nos tempos de 24 e 48 h. Para cada grupo tratamento cinco bulbos de cebolas (cinco repetições) foram utilizados. As radículas foram fixadas em Carnoy e as lâminas preparadas pela técnica de esmagamento. Analisaram-se células em todo ciclo celular, totalizando 5.000 para cada grupo tratamento em cada tempo de exposição. Os índices mitóticos obtidos foram submetidos à análise estatística do Qui-quadrado (p<0,05). A partir dos resultados verificou-se que o grupo TS, nas três concentrações, potencializou o efeito antiproliferativo significativo as células do sistema teste quando comparado ao CP, CN e TJ nas três concentrações. Ainda, o TS nas três concentrações reduziu de forma significativa o número de aberrações celulares quando comparado com o número de células aberrantes obtidas para o CP, demonstrando ação antimutagênica as células do sistema teste A. cepa.

In vivo antipyretic, antiemetic, in vitro membrane stabilization, antimicrobial, and cytotoxic activities of different extracts from Spilanthes paniculata leaves

BACKGROUND: The study was conducted to evaluate the in vitro antimicrobial activity, cytotoxic, and membrane stabilization activities, and in vivo antiemetic and antipyretic potentials of ethanolic extract, n-hexane and ethyl acetate soluble fractions of Spilanthes paniculata leaves for the first time widely used in the traditional treatments in Bangladesh. RESULTS: In antipyretic activity assay, a significant reduction (P < 0.05) was observed in the temperature in the mice tested. At dose 400 mg/kg-body weight, the n-hexane soluble fraction showed the effect (36.7 ± 0.63°C ) as like as the standard (dose 150 mg/kg-body weight) after 5 h of administration. Extracts showed significant (P < 0.001) potential when tested for the antiemetic activity compared to the standard, metoclopramide. At dose 50 mg/kg-body weight, the standard showed 67.23% inhibition, whereas n-hexane and ethyl acetate soluble fractions showed 37.53% and 24.93% inhibition of emesis respectively at dose 400 mg/kg-body weight. In antimicrobial activity assay, the n-hexane soluble fraction (400 µg/disc) showed salient activity against the tested organisms. It exerts highest activity against Salmonella typhi (16.9 mm zone of inhibition); besides, crude, and ethyl acetate extracts showed resistance to Bacillus cereus and Bacillus subtilis, and Vibrio cholera respectively. All the extracts were tested for lysis of the erythrocytes. At the concentration of 1mg/ml, ethanol extract, and n-hexane and ethyl acetate soluble fractions significantly inhibited hypotonic solution induced lysis of the human red blood cell (HRBC) (27.406 ± 3.57, 46.034 ± 3.251, and 30.72 ± 5.679% respectively); where standard drug acetylsalicylic acid (concentration 0.1 mg/ml) showed 77.276 ± 0.321% inhibition. In case of heat induced HRBC hemolysis, the plant extracts also showed significant activity (34.21 ± 4.72, 21.81 ± 3.08, and 27.62 ± 8.79% inhibition respectively). In the brine shrimp lethality bioassay, the n-hexane fraction showed potent (LC50 value 48.978 µg/ml) activity, whereas ethyl acetate fraction showed mild (LC50 value 216.77 µg/ml) cytotoxic activity. CONCLUSIONS: Our results showed that the n-hexane extract has better effects than the other in all trials. In the context, it can be said that the leaves of S. paniculata possess remarkable pharmacological effects, and justify its folkloric use as antimicrobial, antipyretic, anti-inflammatory, and antiemetic agent. Therefore, further research may be suggested to find possible mode of action of the plant part.

Antipyretic and antioxidant activities of 5-trifluoromethyl-4,5-dihydro-1H-pyrazoles in rats

The objective of this study was to determine the effect of eight 5-hydroxy-5-trifluoromethyl-4,5-dihydro-1H-1-carboxyamidepyrazoles (TFDPs) on rat body temperature and baker’s yeast-induced fever. TFDPs or vehicle (5 percent Tween 80 in 0.9 percent NaCl, 5 mL/kg) were injected subcutaneously and rectal temperature was measured as a function of time in 28-day-old male Wistar rats (N = 5-12 per group). Antipyretic activity was determined in feverish animals injected with baker’s yeast (Saccharomyces cerevisiae suspension, 0.135 mg/kg, 10 mL/kg, ip). 3-Ethyl- and 3-propyl-TFDP (140 and 200 μmol/kg, respectively, 4 h after yeast injection) attenuated baker’s yeast-induced fever by 61 and 82 percent, respectively. These two effective antipyretics were selected for subsequent analysis of putative mechanisms of action. We then determined the effects on cyclooxygenase-1 and -2 (COX-1 and COX-2) activities on 1,1-diphenyl-2-picrylhydrazyl (DPPH) oxidation in vitro, on tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) levels and on leukocyte counts in the washes of peritoneal cavities of rats injected with baker’s yeast. While 3-ethyl- and 3-propyl-TFDP did not reduce baker’s yeast-induced increases of IL-1β or TNF-α levels, 3-ethyl-TFDP caused a 42 percent reduction in peritoneal leukocyte count. 3-Ethyl- and 3-propyl-TFDP did not alter COX-1 or COX-2 activities in vitro, but presented antioxidant activity in the DPPH assay with an IC50 of 39 mM (25-62) and 163 mM (136-196), respectively. The data indicate that mechanisms of action of these two novel antipyretic pyrazole derivatives do not involve the classic inhibition of the COX pathway or pyrogenic cytokine release.