Abstract:Tephrosia toxicaria (Sw.) Pers., which is currently known as T. sinapou (Buc'hoz) A. Chev., Fabaceae, is a source of compounds such as fl avonoids, however, few studies addressed the anti-infl ammatory and antioxidant effects of T. sinapou. Therefore, we evaluated the antioxidant mechanisms of the T. sinapou ethyl acetate extract in vitro, and whether the extract affects leukocyte recruitment in four models of infl ammation and the involvement of nitric oxide and cytokines in its mechanism. In vitro, it was observed that the extract presented hydrogen donating ability to 2,2-diphenyl-1-picryl-hydrazyl radical (DPPH • ), 2,2'-azino-di-(3-ethylbenzthiazoline-6-sulphonic acid) radical (ABTS + ), and also effi ciently inhibited iron-dependent and independent lipid peroxidation and iron chelation assays. In vivo, it inhibited the recruitment of total leukocytes and neutrophil induced by carrageenin, zymosan, glycogen and lipopolysaccharide in the peritoneal cavity of mice. Two mechanisms were detected: 1) T. sinapou effect on leukocyte recruitment depends on nitric oxide since was dose-dependently inhibited by treatment with L-NAME (nitric oxide synthase inhibitor), and 2) the extract also inhibited the production of crucial cytokines for the leukocyte recruitment; tumor necrosis factor α and interleukin-1β. Concluding, T. sinapou ethyl acetate extract reduces oxidative stress in vitro, and infl ammatory leukocyte recruitment by a mechanism related to inhibition of cytokine production, and in a nitric oxide dependent manner in vivo.
Context: Tephrosia toxicaria is currently known as Tephrosia sinapou (Buc'hoz) A. Chev. (Fabaceae) and is a source of compounds such as flavonoids that inhibit inflammatory pain. Objective: To investigate the analgesic effect and mechanisms of the ethyl acetate extract of T. sinapou in inflammatory pain in mice. Materials and methods: Behavioral responses were evaluated using mechanical (1-24 h) and thermal hyperalgesia (0.5-5 h), writhing response (20 min) and rota-rod (1-5 h) tests. Neutrophil recruitment (myeloperoxidase activity), cytokines (tumor necrosis factor [TNF]a and interleukin [IL]-1b), aspartate aminotransferase (AST) and alanine aminotransferase (ALT) serum levels were determined by colorimetric assays. Pharmacological treatments were opioid receptor antagonist (naloxone, 0.1-1 mg/kg) and control opioid (morphine, 5 mg/kg). Inflammatory stimuli were carrageenin (100 mg/paw), complete Freund's adjuvant (CFA, 10 ml/paw), prostaglandin E 2 (PGE 2 , 100 ng/paw) and acetic acid (0.8%). Results: The intraperitoneal pre-treatment with extract inhibited in a dose-dependent (30-300 mg/kg) dependent manner the mechanical hyperalgesia induced by carrageenin (up to 93% inhibition). The post-treatment (100 mg/kg) inhibited CFA-induced hyperalgesia (up to 63% inhibition). Naloxone (1 mg/kg) prevented the inhibitory effect of the extract over carrageenin-induced mechanical (100%) and thermal (100%) hyperalgesia, neutrophil recruitment (52%) and TNFa (63%) and IL-1b (98%) production, thermal threshold in naïve mice (99%), PGE 2 -induced mechanical hyperalgesia (88%) and acetic acid-induced writhing response (49%). There was no significant alteration in the rota-rod test, and AST and ALT serum levels by extract treatment. Discussion and conclusion: Tephrosia sinapou ethyl acetate extract reduces inflammatory pain by activating an opioid receptor-dependent mechanism.
Recebido em 14/12/05; aceito em 4/8/06; publicado na web em 10/1/07 ALKALOIDS FROM FLOWERS AND LEAVES OF Erythrina speciosa ANDREWS. In vitro bioassays with leave extracts of Erythrina speciosa showed promising activity against Trypanosoma cruzi. From the flowers of E. speciosa two alkaloids were isolated: erysotrine and erythartine. The leaves furnished one alkaloid, nororientaline. The structures were determined on the basis of spectroscopic evidence. This is the first report about the investigation of alkaloids in flowers and leaves of this species, as well the first report of nororientaline occurrence in this plant.Keywords: Erythrina speciosa; alkaloids; trypanocidal activity. INTRODUÇÃOOs extratos de folhas, cascas e de raízes de várias espécies do gênero Erythrina são usados na medicina popular no tratamento de diversas doenças, tais como disenteria, asma, dor estomacal, infertilidade feminina e, principalmente, infecções microbianas. O gênero é conhecido pela bioprodução significativa de alcalóides, sendo que estudos mais recentes revelaram também a presença de flavanonas, isoflavonas e pteropcarpanos , o que serviu como estímulo adicional para iniciar atividades de investigação química da espécie.O presente trabalho descreve o isolamento e a caracterização estrutural dos alcalóides erisotrina (1) e eritrartina (2) obtidos do extrato etanólico das flores e da nororientalina (3), do extrato etanólico das folhas de E. speciosa. A literatura registra o isolamento de alcalóides de sementes e cascas de E. speciosa 2,10,11 , porém este é o primeiro registro de estudo de flores e folhas desta espécie. RESULTADOS E DISCUSSÃOO fracionamento cromatográfico do extrato etanólico das flores de E. speciosa forneceu um grupo de frações eluídas com uma mistura de diclorometano/etanol 10%, que revelou teste positivo com reagente de Dragendorff, sugerindo a presença de substância nitrogenada. A purificação deste material resultou no isolamento e posterior identificação dos alcalóides erisotrina (1) e eritrartina (2) .
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