Estudio fitoquímico de hojas de Cavendishia compacta (Ericaceae) y evaluación de su actividad antiinflamatoria / Phytochemical study of leaves of Cavendishia compacta (Ericaceae) and evaluation of its anti-inflammatory activity

RESUMEN Se realizó el estudio fitoquímico de hojas de Cavendishia compacta. La separación de extractos y fracciones por cromatografías en columna, capa delgada y capa delgada preparativa, permitieron obtener una mezcla de diterpenos conformada por kaurano, rimuneno y biformeno; una mezcla de compuestos aromáticos constituida por acetofenona y benzaldehído; una mezcla de triterpenos constituida por α-amirina y β-amirina y el aislamiento de morina y miricetina. La actividad antiinflamatoria se evaluó al extracto etanólico y las fracciones de hexano, dicolorometano y acetato de etilo, utilizando el modelo de edema auricular inducido por TPA, siendo el extracto etanólico y la fracción de dicolorometano los que presentaron un efecto antiinflamatorio moderado de 49,3% y 39,8% respectivamente.

Summary The phytochemical study of leaves of Cavendishia compacta was carried out. The separation of extracts and fractions by column chromatography, thin layer and preparative thin layer allowed to obtain a mixture of diterpenes consisting of kaurane, rimunene and biformene; a mixture of aromatic compounds constituted by acetophenone and benzaldehyde; a mixture of triterpenes constituted by α -amirine and β-amirin and the isolation of morine and myricetin. The anti-inflammatory activity was evaluated to the ethanolic extract and fractions of hexane, dichloromethane and ethyl acetate using the model of atrial edema induced by TPA, being the etha-nolic extract and the fraction of dicholoromethane those that presented a moderate anti-inflammatory effect of 49.3 % and 39.8% respectivel.

In vivo redox effects of Aspidosperma quebracho-blanco Schltdl., Lantana grisebachii Stuck and Ilex paraguariensis A. St.-Hil. on blood, thymus and spleen of mice.

Argentinian native plants Aspidosperma quebracho-blanco, Lantana grisebachii and Ilex paraguariensis are known to have antiinflammatory and antioxidant properties. We demonstrated it in vivo by the redox changes in murine hemolymphatic tissues after infusive extract intake of these plants as revealed in organic trophism, tissue phenolics, hydroperoxides, superoxide, nitrites and γ-glutamyltranspeptidase in thymus, blood and spleen. A. quebracho-blanco reduced hydroperoxidation in blood and spleen of both sexes, with γ-glutamyltranspeptidase negativization in lymphatic organs and thymic nitrosative up-regulation. Males have shown increased phenolic content in blood after treatment. L. grisebachii and I. paraguariensis treatment exhibited incomplete antioxidation and oxidative induction in the studied tissues. Different results according to sex were found in redox response to phenolics and their kinetics, with males showing antioxidant effects, whereas females showed oxidative susceptibility. A. quebracho-blanco exhibited protection of murine tissues against oxidation in both sexes and modulation of their trophism, supporting its therapeutic uses in inflammatory diseases. Also, gender had significant influence in phenolic biodistribution and redox response.

Design, Synthesis, Biological Evaluation and Docking Studies of Some New Diclofenac Analogues.

Aim: There is still a need for new, selective COX-2 inhibitors with an improved safety profile, therefore, a series of diclofenac analogues were designed and different physicochemical properties were calculated such as log P, hydrogen donor, hydrogenacceptor, molecular weight and pKa etc and compared with diclofenac and study was aimed to design and calculate different physicochemical properties and attempt to introduce diclofenac derivatives with improved anti-inflammatory profile along with docking focusingon CO X-2. Materials and Method: Carrageenan-induced paw edema to evaluate the antiinflammatory activity of the conjugates 4 groups (n = 6) of Wistar rats (150–200 g) were examined. A first group of rats was used as a control without using the drug, group II received Diclofenac 20 mg kg–1, received PEG600-Diclo conjugate and PEG4000-Diclo conjugate (52.60 mg kg−1 and 214 mg kg−1 respectively), where the dose was molecularly equivalent to the diclofenac. Results: Result showed a significant (p<0.05) dose dependent increase in reaction time in mice in the method at the doses of 150 and 200 mg/kg body weight. Also docking studies specifically on COX-2 exhibited promising anti-inflammatory effect as demonstrated by statistically significant (p<0.05) inhibition of paw volume at the dose of 150 mg/kg body weight and the dose of 500 mg/kg body weight at the three hours of study. Conclusion: In this study molecular docking results, along with biological assay data, show that all compounds have a potential anti-inflammatory activity comparable to diclofenac.

Evaluación del efecto antiinflamatorio de un extracto orgánico de Allophylus cominia (L) Sw. sobre la actividad de COX-2 y FLA-2s / Evaluation of the antiinflammatory effect of an organic extract of Allophylus cominia (L) Sw. on COX-2 and sPLA-2 activity

Allophylus cominia (L) Sw (Sapindaceae), is one of the most popular Cuban medicinal plant. The aimed of this study was to explore, if the antidiabetic organic extract has also anti-inflammatory effect, considering that inflammation is correlationated with diabetes. It was evaluated in vitro inhibitory activity of chloroform extract of leaves on cyclooxygenase-2 (COX-2) and secreted phospholipase A2 (sPLA-2), which are important cellular mediators in the signaling cascade of the inflammatory process. The extract studied shown inhibitory activity on COX-2, while not shown on FLA-2s. This study provides direct evidence of the activity of A. cominia on mechanisms related to anti-inflammatory effects involving the eicosanoid cascade.

Allophylus cominia (L) Sw (Sapindáceas) es una de las plantas medicinales más afamadas de la medicina tradicional en Cuba. El objetivo de este estudio fue explorar si el extracto orgánico con actividad antidiabética tenía también efecto de tipo antiinflamatorio, considerando que la inflamación es un evento relacionado con la diabetes. En tal sentido se evaluó in vitro la actividad inhibitoria del extracto clorofórmico de las hojas de Allophylus cominia (L) Sw sobre cicloxigenasa-2 (COX-2) y fosofolipasa A2 secretada (FLA-2s), las cuales constituyen importantes mediadores celulares en la cascada de señalización del proceso inflamatorio. El extracto estudiado exhibió actividad inhibitoria sobre COX-2, mientras que no la mostró sobre FLA-2s. Este trabajo brinda evidencias directas de la actividad de A. cominia sobre mecanismos vinculados al efecto antinflamatorio que involucran la cascada de eicosanoides.

Antiinflammatory activity of fractionated extracts of Achyranthes aspera Linn leaves.

The present work has been designed to evaluate the potency of anti-inflammatory activity of different fractions of ethanolic extract of Achyranthes aspera leaves. Carrageenan induced rat paw oedema method was used for screening. Ethanolic, ethyl acetate and hexane fraction was screened among which ethyl acetate fraction was found to be most potent one with percentage inhibition of 50, 74, 84, 86% at 1st to 4th hour respectively. By this experiment it seems that leaves of Achyranthes aspera can be used for the treatment of acute inflammation.

Evaluation of antiinflammatory and analgesic activities of alcoholic extract of kaempferia galanga in rats.

Alcoholic extract of Kaempferia galanga was tested for analgesic and antiinflammatory activities in animal models. Three doses, 300 mg/kg, 600 mg/kg and 1200 mg/kg of the plant extract prepared as a suspension in 2 ml of 2% gum acacia were used. Acute and sub acute inflammatory activities were studied in rats by carrageenan induced paw edema and cotton pellet induced granuloma models respectively. In both models, the standard drug used was aspirin 100 mg/kg. Two doses 600 mg/kg and 1200 mg/kg of plant extract exhibited significant (P<0.001) antiinflammatory activity in carrageenan model and cotton pellet granuloma model in comparison to control. Analgesic activity was studied in rats using hot plate and tail-flick models. Codeine 5 mg/kg and vehicle served as standard and control respectively. The two doses of plant extract exhibited significant analgesic activity in tail flick model (P<0.001) and hot plate model (P<0.001) in comparison to control. In conclusion K. galanga possesses antiinflammatory and analgesic activities.

Antiinflammatory activity of ricinus communis derived polymer

Aim: The present study aimed to evaluate the antiinflammatory activity of the polymer derived from Ricinus communis and its mechanism of action. Methods: The antiinflammatory activity was investigated in chronic and acute animal models and the mechanism of action involved in the antiinflammatory activity was determined by the in vitro phospholipase A2 (PLA2) enzyme assay. Results: In mouse ear edema (10.0 mg/ear) and granulomatous tissue formation (500 mg/kg) models, the polymer inhibited the inflammatory response in 75.08 ± 1.80% and 61.70 ± 1.80% of the cases, respectively (p<0.001). Oral administration of the Ricinus communis polymer (500 mg/kg) inhibited 72.00 ± 1.20% of formalin-induced inflammation. Topical administration of the polymer on oral lesions of mice showed that the oral mucosa was recovered in 60.00 ± 1.40% (p<0.05) of the cases. In in vitro assay, the phospholipase A2 enzyme was inhibited by the Ricinus communis polymer (5.0 mg/mL) in a dose-dependent manner (84.60 ± 1.41%). Conclusion: the polymer derived from Ricinus communis showed a significant antiinflammatory activity, confirming that the pharmacological mechanism involved in this antiinflammatory action was related to the inhibition of the PLA2 enzyme.

Evaluación de extractos y fracciones de plantas colombianas en modelos de inflamación aguda, subcrónica y crónica / Evaluation of acute, subchronic and chronic inflammation activity of extracts and extracts fractions of Colombian plants

Se evaluó la actividad antiinflamatoria de extractos y fracciones de Acnistus arborescens, Baccharis latifolia, Myrcianthes leucoxila, Physalis peruviana y Salvia rubescens en los modelos in vivo de inflamación edema tópico en oreja de ratón, edema plantar por carragenina en rata y bolsa de aire en ratón, con profundización en modelo de artritis por adyuvante en rata. Inicialmente se realizó el screening de un total de 34 fracciones en el modelo de edema auricular en ratón, de los cuales se seleccionaron dos de Acnistus arborescens, cuatro de Baccharis latifolia y de Myrcianthes leucoxila y dos de Salvia rubescens. Posteriormente se evaluó la actividad de dichas fracciones en el modelo de edema plantar por carragenina en rata seleccionando aquellos que mostraron mayor actividad para ser evaluados luego en el modelo de bolsa de aire en ratón. Después de esta evaluación continuaron el estudio las fracciones S2 y S7 de S. rubescens, provenientes del extracto hidroalcohólico, y AA-F de A. arborescens, que corresponde a la fracción de diclorometano. La última fase correspondió a la evaluación de S2 y AA-F en el modelo de artritis por adyuvante en ratas Wistar, que empleó el protocolo de evaluación de actividad preventiva en el desarrollo de artritis y se observó que no ejercieron dicha actividad.

Some extracts and fractions of Acnistus arborescens, Baccharis latifolia, Myrcianthes leucoxila, Physalis peruviana and Salvia rubescens were examined for antiinflammatory activity in vivo models as mice ear oedema, carrageenan induced rat paw oedema, zimosan injected-rat air pouch and Freund's adjuvant arthritis. In initial screening on mice ear oedema model were selected two of A. arborescens, four of B. latifolia and M. leucoxila and two of S. rubescens among thirty four fractions which showed greater antiinflammatory activity. Later, these fractions were evaluated in carrageenan induced rat paw oedema model and those that showed greater activity have been selected to be evaluated in the zimosan injected-mice air pouch model. S2 and S7 fractions of S. rubescens, that came from hydroalcoholic extract, and AA-F of A. arborescens, that corresponded diclorometane fraction, were those that until this phase of the study showed greater antiinflammatory activity. The last phase corresponded to the evaluation of S2 and AA-F in the model Freund's adjuvant arthritis in Wistar rats using the protocol of evaluation of preventive activity in the development of arthritis showed that did not exhibit this activity.

Efeito antinociceptivo e antiinflamatório do extrato aquoso da entrecasca de Coutarea hexandra Schum. (Rubiaceae) / Antinociceptive and anti-inflammatory properties of Coutarea hexandra barks aqueous extract Schum. (Rubiaceae)

No estado de Sergipe, o chá da entrecasca de Coutarea hexandra Shum. (Rubiaceae) é popularmente utilizado no combate à dor e à inflamação. Estes usos etnofarmacológicos vieram motivar os estudos sobre os efeitos antinociceptivo e antiinflamatório, bem como sobre a toxicidade aguda do extrato aquoso liofilizado da entrecasca de Coutarea hexandra. Doses orais do extrato aquoso significativamente reduziram as contorções abdominais induzidas por ácido acético, aumentaram o tempo de latência ao calor no teste da placa quente, reduziram o edema de pata induzido por carragenina e, na segunda fase do teste da formalina, também reduziram a resposta dos animais à formalina. O efeito detectado no teste da formalina não foi revertido por naloxona ou cafeína. Nos ensaios de toxicidade aguda, não foi observada a morte de nenhum animal até a dose de 5 g/kg. Em conclusão, o extrato aquoso da entrecasca de C. hexandra possui efeitos antiinflamatório e antinociceptivo e não apresenta toxicidade aguda em camundongos. O efeito antinociceptivo não está relacionado à ativação dos sistemas opióide e adenosina e, ao menos parcialmente, é decorrente da atuação do extrato aquoso em nível central.

The aqueous extract of Coutarea hexandra Shum. (Rubiaceae) is extensively used on local folk medicine as anti-inflammatory and antinociceptive. In view of these facts, it was of our interest to evaluate the anti-inflammatory and antinociceptive activities. Its acute toxicity was also evaluated. The aqueous extract of Coutarea hexandra reduced acetic acid-induced writhing, increased the latency in the hot plate test, and reduced the second phase nociceptive response in the formalin test. Neither naloxone nor caffeine reversed aqueous extract of Coutarea hexandra effect in the second phase of the formalin test. The aqueous extract of Coutarea hexandra also reduced the rat paw edema induced by carrageenan. There was no animal death with doses up to 5 g/kg in the acute toxicity assays. These results showed that aqueous extract of C. hexandra has low acute toxicity, as well as, anti-inflammatory and antinociceptive effects, substantiating its popular usage. The antinociceptive effect seems to involve a central component, although it is not directly related to the opioid and adenosine systems.