ABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: In folk medicine Hyptis suaveolens (Lamiaceae) has been reported to relieve respiratory and gastrointestinal infections, indigestion, cold, pain, fever, cramps, skin diseases, gastric ulcer and inflammatory disorders. This study investigated the effects and the mechanisms of action of Hyptis suaveolens (L.) Poit (Lamiaceae) ethanol extract (Hs-EtOH) and hexane phase (Hs-HexF) against intestinal inflammation. MATERIAL AND METHODS: Acute and relapse TNBS-induced ulcerative colitis protocols were used to evaluate intestinal anti-inflammatory activity. Damage evaluations, biochemical, histological and immunostaining parameters were determined. RESULTS: Both extracts decreased macroscopic colonic inflammation and the area of lesion induced by TNBS. Nevertheless, only Hs-HexF was able to reduce colonic wall thickness, edema and diffuse inflammatory cell infiltration and to prevent GSH depletion in the acute model of ulcerative colitis. In the chronic phase with relapse of colonic ulceration, yet again only Hs-HexF significantly attenuated inflammatory parameters and presented a decrease in nitrite/nitrate, MDA, MPO, IL-1-ß and TNF-α and increased levels of SOD, CAT, GSH and IL-10. Hs-HexF also significantly reduced positive cells immunostained for PCNA. CONCLUSION: The data indicate intestinal anti-inflammatory activity for H. suaveolens, due to the participation of the antioxidant system, decreased neutrophil infiltration and cytokine modulation, as well as, owing to regulation of cell proliferation.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Colitis, Ulcerative/prevention & control , Hyptis/chemistry , Plant Extracts/pharmacology , Animals , Anti-Inflammatory Agents/isolation & purification , Antioxidants/isolation & purification , Antioxidants/pharmacology , Cell Proliferation/drug effects , Disease Models, Animal , Immunologic Factors/isolation & purification , Immunologic Factors/pharmacology , Inflammation/drug therapy , Inflammation/pathology , Male , Rats , Rats, Wistar , Trinitrobenzenesulfonic AcidABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: The leaves and roots of Cissampelos sympodialis (Menispermaceae) are used by indian tribes and in folk medicine to treat genitourinary infections, inflammation, asthma and gastrointestinal disorders. MATERIAL AND METHODS: The standardized ethanolic extract (Cs-EtOHE) and alkaloids total fraction (Cs-TAF) obtained from aerial parts of C. sympodialis were evaluated in several models of acute gastric ulcers. The antisecretory and/or neutralizing mechanisms of the gastric acid secretion, cytoprotective, antioxidant and immunoregulatory mechanisms were also evaluated. RESULTS: Cs-EtOHE and Cs-TAF presented a reduction in gastric mucosa lesions against ethanol, NSAIDs, hypothermic restraint-stress and gastric juice containment induced ulcer models. This activity is related to alkaloids present in the extract, and involves the participation of sulfhydryl compounds, nitric oxide, KATP channels, prostaglandins, decreased levels of IL-1ß and TNF-α and increased levels of GSH and IL-10. CONCLUSION: The data indicate gastroprotective activity, due to the participation of the cytoprotective, antioxidant and immunoregulatory mechanisms.
Subject(s)
Anti-Inflammatory Agents , Anti-Ulcer Agents , Antioxidants , Cissampelos , Plant Extracts , Stomach Ulcer/drug therapy , Animals , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal , Anti-Ulcer Agents/pharmacology , Anti-Ulcer Agents/therapeutic use , Antioxidants/pharmacology , Antioxidants/therapeutic use , Colon/metabolism , Cytokines/metabolism , Disease Models, Animal , Ethanol , Gastric Mucosa/drug effects , Gastric Mucosa/metabolism , Gastric Mucosa/pathology , Glutathione/metabolism , KATP Channels/metabolism , Male , Mice , Nitric Oxide/metabolism , Phytotherapy , Plant Components, Aerial , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Prostaglandins/metabolism , Rats, Wistar , Restraint, Physical , Stomach Ulcer/etiology , Stomach Ulcer/metabolism , Stomach Ulcer/pathology , Stress, PhysiologicalABSTRACT
AIM: To investigate the acute toxicity, phytochemical profile, antidiarrheal activity and mechanisms of action of Maytenus erythroxylon (M. erythroxylon) ethanol extract. METHODS: A castor oil-induced diarrhea model was used to evaluate antidiarrheal activity. Intestinal transit and gastric emptying protocols were used to evaluate a possible antimotility effect. KATP channels, nitric oxide, presynaptic α2-adrenergic and tissue adrenergic receptors were investigated to uncover antimotility mechanisms of action and castor oil-induced enteropooling to elucidate antisecretory mechanisms. RESULTS: All tested doses of the extract (62.5, 125, 250 and 500 mg/kg) possessed antidiarrheal activity, with a significant decrease of the evacuation index. This activity is possibly related to a reduced gastric emptying (125, 250 and 500 mg/kg) and to a decreased percentage of intestinal transit for all tested doses. That last effect seems to be modulated by nitric oxide, KATP channels and tissue adrenergic receptors. Besides, the extract also presented antisecretory effect due to a decrease of intestinal fluid accumulation. CONCLUSION: The antidiarrheal effect of M. erythroxylon found in this study involves antimotility and antisecretory mechanisms that may be attributed to the chemical compounds found in this species: saponins, flavonoids, tannins, triterpenes and steroids.
Subject(s)
Antidiarrheals/pharmacology , Diarrhea/drug therapy , Gastric Emptying/drug effects , Gastrointestinal Transit/drug effects , Maytenus/chemistry , Plant Extracts/pharmacology , Animals , Antidiarrheals/therapeutic use , Castor Oil/toxicity , Diarrhea/chemically induced , Disease Models, Animal , Ethanol/chemistry , Female , Intestinal Mucosa/drug effects , Intestinal Mucosa/metabolism , Intestinal Secretions/drug effects , KATP Channels/metabolism , Male , Mice , Nitric Oxide/metabolism , Plant Extracts/therapeutic use , Receptors, Adrenergic/metabolismABSTRACT
BACKGROUND: Cissampelos sympodialis (Menispermaceae), known as "Milona" has a specific verified medicinal use for the treatment of diarrhea and respiratory tract diseases. This work aims to evaluate the antimotility and antidiarrheal activity of crude ethanolic extract (EtOHE-Cs), and the total alkaloid fraction (TAF-Cs) obtained from aerial parts of C. sympodialis. METHODS: Normal intestinal transit and gastric emptying were used to evaluate antimotility activity. Castor oil-induced diarrhea and castor oil-induced enteropooling were used to evaluate antidiarrheal activity. RESULTS: The results indicated that EtOHE-Cs has no antimotility activity, but did demonstrate antidiarrheal activity (at 500 mg/kg), and this activity is related to reduction of intestinal fluid accumulation. The TAF-Cs (at 250 and 500 mg/kg) showed antidiarrheal activity by reducing gastrointestinal motility (gastric emptying and normal intestinal transit). CONCLUSIONS: The antidiarrheal activity of C. sympodialis can be attributed to the chemical compounds already isolated and quantified in this species, mainly alkaloids.
Subject(s)
Antidiarrheals , Cissampelos/chemistry , Gastric Emptying/drug effects , Gastrointestinal Transit/drug effects , Plant Extracts , Plants, Medicinal/chemistry , Alkaloids , Animals , Antidiarrheals/chemistry , Antidiarrheals/pharmacology , Male , Mice , Plant Extracts/chemistry , Plant Extracts/pharmacologyABSTRACT
des-7'-O-methylroraimine (compound 1) and epi-des-7'-O-methylroraimine (compound 2), two new isomeric bisbenzylisoquinoline alkaloids were isolated and characterized as a mixture from the rhizomes of Cissampelos sympodialis Eichl. The unambiguous structural elucidation of both isomers was performed with the aid of HR-ESI-MS, FT-IR, and NMR techniques including COSY, HMQC, HMBC, and NOESY.
Subject(s)
Alkaloids/isolation & purification , Benzylisoquinolines/isolation & purification , Menispermaceae/chemistry , Alkaloids/chemistry , Benzylisoquinolines/chemistry , Carbon Isotopes , Magnetic Resonance Spectroscopy/standards , Molecular Structure , Protons , Reference StandardsABSTRACT
Cissampelos sympodialis Eichl is a species of the family Meniespermaceae known as Milona, which extracts showed low toxicity and several pharmacological activities as anti-inflammatory, anti-allergic or anti-depressive. In the present study two classic analgesia models in mice were used to evaluate the hydroalcoholic extract of C. sympodialis leaves (HAECs) at doses of 50, 100 and 200 mg/kg, i.p. In the test of writhing by acetic acid HAECs- treatment induced a significant reduction in the number of abdominal contortions in a dose-dependent manner (p <0,05). In the formalin test, HAECs-200 mg/kg induced a significant inhibition of the second phase (15-30 minutes) (p <0,05). Results suggest that the HAECs presented outlying antinociceptive peripheral activity probably related with the alleged anti-inflammatory proprieties of extracts of this plant.
Existen varios estudios que evidencian que la Cissampelos sympodialis posee atividad anti-inflamatoria, antialérgica, antidepresiva y de baja toxicidad. Este estudio evaluó los efectos de la administración intraperitoneal, del extracto hidroalcohólico de hojas de cissampelos sympodialis (EHACS), en las dosis de 50, 100 y 200 mg/Kg, en modelos de analgesia en camumdongos. En el modelo de las contracciones inducidas por el ácido acético (0,85 por ciento) fue encontrada una reducción en el número de contracciones proporcional a las dosis usadas (p<0,05). En el test de la reacción al formaldeído las dosis utilizadas no presentaron efecto significante en la primera fase del test (0-5 minutos). Sin embargo, la dosis de 200mg/Kg presentó una significante inhibición en la segunda fase (15 30 minutos) del test (p<0,05). Los resultados mostraron que el EHACS presentó una actividad antinociceptiva periférica probablemente relacionada con la alegada actividad anti-inflamatoria.
