RESUMO
The present study focuses on the anti-inflammatory activity of Justicia gendarussa Burm.f. on an acute model of inflammation: the carrageenan-induced paw edema assay. Methanolic extract of J. gendarussa (JRM) roots at a dose of 100 mg/kg significantly inhibited edema formation 5 h after carrageenan induction. JRM inhibited carrageenan-elicited total cycloxygenase activity, 5-lipoxygenase and 15-lipoxygenase activities in blood mononuclear cells of rats, decreased neutrophil infiltration in paw tissue as shown by low myeloperoxidase activity, and also caused a 53% inhibition in cyclooxygenase-2 activity in paw tissue. Purification of JRM by liquid-liquid partitioning yielded an ethyl acetate fraction of JRM that showed interleukin-6 downregulation potential and the ability to inhibit prostaglandin E2 production in vivo. The present investigation provides pharmacological evidence to support the folklore claim that J. gendarussa is an anti-inflammatory agent.
Assuntos
Acanthaceae/química , Anti-Inflamatórios/uso terapêutico , Carragenina/toxicidade , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/química , Dinoprostona/metabolismo , Edema/induzido quimicamente , Edema/tratamento farmacológico , Edema/metabolismo , Inflamação/metabolismo , Interleucina-6/metabolismo , Lipoxigenase/metabolismo , Masculino , Extratos Vegetais/química , Prostaglandina-Endoperóxido Sintases/metabolismo , Ratos , Ratos WistarRESUMO
The purpose of this study was to investigate the anti-inflammatory function and mechanism(s) of action of an active component-betulinic acid isolated from Bacopa monniera. Betulinic acid, a pentacyclic triterpenoid markedly suppressed lipopolysaccharide (LPS) induced IL-6 production in blood mononuclear cells both in vivo and in vitro. Betulinic acid also prevented LPS induced nuclear translocation of p65 NF-kappaB in hPBMCs. LPS induced nuclear translocation of NF-kappaB and IL-6 production was also abolished by p38 and ERK MAPK inhibitors PD98059 and SB203580. Addition of each of these inhibitors to cell cultures along with betulinic acid caused significant downregulation of IL-6 production and inhibition of p65 NF-kappaB nuclear translocation. The inhibitory effect of both betulinic acid and the inhibitors was higher than that of cells treated with inhibitors alone. These results suggest that betulinic acid inhibited IL-6 production by preventing p65 NF-kappaB nuclear translocation and there is a possibility that this prevention of p65 nuclear translocation may involve p38 and ERK MAPKs as cross talks occur between MAPK and NF-kappaB pathways. This study provides an insight into the probable mechanism(s) underlying the anti-inflammatory and therapeutic properties of betulinic acid.
Assuntos
Anti-Inflamatórios/farmacologia , Interleucina-6/biossíntese , Leucócitos Mononucleares/metabolismo , NF-kappa B/antagonistas & inibidores , Triterpenos/farmacologia , Animais , Anti-Inflamatórios/administração & dosagem , Bacopa/imunologia , Células Cultivadas , Flavonoides/farmacologia , Humanos , Imidazóis/farmacologia , Interleucina-6/genética , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/imunologia , Leucócitos Mononucleares/patologia , Lipopolissacarídeos/imunologia , Lipopolissacarídeos/metabolismo , Masculino , Triterpenos Pentacíclicos , Piridinas/farmacologia , Ratos , Ratos Wistar , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/imunologia , Triterpenos/administração & dosagem , Proteínas Quinases p38 Ativadas por Mitógeno/antagonistas & inibidores , Ácido BetulínicoRESUMO
Bacopa monniera (L.) Wettst is an Ayurvedic herb with antirheumatic potential. This study investigated the therapeutic efficacy of Bacopa monniera in treating rheumatoid arthritis using a type II collagen-induced arthritis rat model. Arthritis was induced in male Wistar rats by immunization with bovine type II collagen in complete Freund's adjuvant. Bacopa monniera extract (BME) was administered after the development of arthritis from day 14 onwards. The total duration of experiment was 60 days. Paw swelling, arthritic index, inflammatory mediators such as cyclooxygenase, lipoxygenase, myeloperoxidase and serum anti-collagen IgG and IgM levels were analysed in control and experimental rats. Arthritic induction significantly increased paw edema and other classical signs of arthritis coupled to upregulation of inflammatory mediators such as cyclooxygenase, lipoxygenase, neutrophil infiltration and increased anti-collagen IgM and IgG levels in serum. BME significantly inhibited the footpad swelling and arthritic symptoms. BME was effective in inhibiting cyclooxygenase and lipoxygenase activities in arthritic rats. Decreased neutrophil infiltration was evident from decreased myeloperoxidase activity and histopathological data where an improvement in joint architecture was also observed. Serum anti-collagen IgM and IgG levels were consistently decreased. Thus the study demonstrates the potential antiarthritic effect of Bacopa monniera for treating arthritis which might confer its antirheumatic activity.