hypericum and Edema

Hypericum perforatum is a medicinal plant species containing many polyphenolic compounds, namely flavonoids and phenolic acids. In this study we evaluate the effect of Hypericum perforatum in animal model of periodontitis.. Periodontitis was induced in adult male Sprague-Dawley rats by placing a nylon thread ligature around the lower 1st molars. Hypericum perforatum was administered at the dose of 2 mg/kg os, daily for eight days. At day 8, the gingivomucosal tissue encircling the mandibular first molar was removed.. Periodontitis in rats resulted in an inflammatory process characterized by edema, neutrophil infiltration and cytokine production that was followed by the recruitment of other inflammatory cells, production of a range of inflammatory mediators such as NF-κB and iNOS expression, the nitration of tyrosine residues and activation of the nuclear enzyme poly (ADP-ribose) polymerase; apoptosis and the degree of gingivomucosal tissues injury. We report here that Hypericum perforatum exerts potent anti-inflammatory effects significantly reducing all of the parameters of inflammation as described above.. Taken together, our results clearly demonstrate that treatment with Hypericum reduces the development of inflammation and tissue injury, events associated with periodontitis.

Topics: Animals; Anti-Inflammatory Agents; Apoptosis; Cytokines; Disease Models, Animal; Edema; Flavonoids; Hypericum; Inflammation Mediators; Male; Mouth Mucosa; Neutrophil Infiltration; Periodontitis; Phenols; Phytotherapy; Plant Extracts; Poly(ADP-ribose) Polymerases; Polyphenols; Rats; Rats, Sprague-Dawley; Tyrosine

Plants of the genus Hypericum are widely used in folk medicine for the treatment of gastric ailments (including pectic ulcers), burns, swelling, inflammation, anxiety, as well as for bacterial and viral infections. The aerial parts of Hypericum rumeliacum Boiss. subsp. apollinis (Boiss. & Heldr.) Robson & Strid (Guttiferae), a perennial herb growing wild in Greece, were subjected to biological and phytochemical studies. The H. rumeliacum methanol extract showed, on the DPPH test, antioxidant activity (IC(50) = 23.61 microg/mL). The antiinflammatory activity of the extract (70 mg/kg, i.p.), in the carrageenan-induced paw oedema in rat, was studied. In this experimental model an inhibition of paw oedema, significant from the first to third hour, was observed. The histological examination confirmed resolution of the inflammatory process observed in vivo. Through HPLC analysis of the H. rumeliacum methanol extract, the naphthodianthrones hypericin, pseudohypericin and some polyphenol compounds, such as chlorogenic acid, rutin and isoquercitrin, were identified and quantified. The antioxidant activity of H. rumeliacum could be chiefly related to polyphenol compounds that are well known as the main contributors to the free radical-scavenging effects. The antiinflammatory effect of the methanol extract of the aerial parts could be due to the synergic action both of hypericin and polyphenol compounds.

Topics: Animals; Anthracenes; Anti-Inflammatory Agents; Antioxidants; Chlorogenic Acid; Chondrus; Chromatography, High Pressure Liquid; Edema; Flavonoids; Hindlimb; Hypericum; Male; Methanol; Perylene; Phenols; Plant Components, Aerial; Plant Extracts; Polyphenols; Quercetin; Rats; Rats, Wistar; Rutin

A study has been carried out on the chemical composition and in vivo anti-oedematogenic activity of several extracts from Hypericum grandifolium Choisy (Hypericaceae) collected in Tenerife (Canary Islands). The HPLC-MS analysis (HPLC-ESI/MS and HPLC-FT/MS) revealed the presence of hyperforin, flavonoids and probably benzophenone derivatives, while naphthodianthrones were absent. Pharmacological results revealed that the methanol extracts and the aqueous, butanol and chloroform fractions obtained therefrom possess anti-oedematogenic activity against TPA-induced ear oedema and carrageenan-induced paw oedema, the chloroform fraction being the most active. Subfractions derived from the chloroform fraction also showed anti-oedematogenic activity. From these results, it can be suggested that different constituents, such as the flavonoids and the benzophenone derivatives, could be responsible, at least in part, for the anti-oedematogenic effects observed for this species.

Topics: Animals; Carrageenan; Chromatography, High Pressure Liquid; Edema; Hypericum; Mass Spectrometry; Mice; Phytotherapy; Plant Extracts; Tetradecanoylphorbol Acetate

Three preparations of Hypericum perforatum L. (a hydroalcoholic extract, a lipophilic extract and an ethylacetic fraction) and the pure compounds hypericin, adhyperforin, amentoflavone, hyperoside, isoquercitrin, hyperforin dicyclohexylammonium (DHCA) salt and dicyclohexylamine were evaluated for their topical anti-inflammatory activity. H. perforatum preparations provoked a dose-dependent reduction of Croton-oil-induced ear oedema in mice, showing the following rank order of activity: lipophilic extract > ethylacetic fraction > hydroalcoholic extract (ID50 (dose that inhibited oedema by 50%) 220, 267 and >1000 microg cm(-2), respectively). Amentoflavone (ID50 0.16 micromol cm(-2)), hypericin (ID50 0.25 micromol cm(-2)), hyperforin DHCA salt (ID50 0.25 micromol cm(-2)) and adhyperofrin (ID50 0.30 micromol cm(-2)) had anti-inflammatory activity that was more potent or comparable to that of indometacin (ID50 0.26 micromol cm(-2)), whereas isoquercitrin and hyperoside were less active (ID50 about 1 micromol cm(-2)). As dicyclohexylamine alone was inactive, the effect of hyperforin DHCA salt can be attributed completely to the phloroglucinol moiety. The pharmacological activity and phytochemical profile of the tested extracts and fraction suggest that different constituents are involved in the topical antiphlogistic property of H. perforatum in-vivo.

Topics: Administration, Topical; Animals; Anthracenes; Anti-Inflammatory Agents; Bridged Bicyclo Compounds; Croton Oil; Dose-Response Relationship, Drug; Edema; Flavonoids; Flowers; Hypericum; Inhibitory Concentration 50; Male; Mice; Perylene; Phloroglucinol; Phytotherapy; Plant Extracts; Plants, Medicinal; Terpenes

The pharmacological activity of Hypericum perforatum was assessed using models of inflammation, nociception, and gastric mucosal injury in rats. H. perforatum was given systemically as well as orally. When administered systemically, H. perforatum (50-300 mg/kg, s.c.) produced a dose-related and significant inhibition of the edematogenic response to s.p. injection of carrageenan. The percentages of maximal inhibition by the above doses were 53.7, 61.3, and 75.3%, respectively (compared to 90% after 50 mg/kg fluoxetine and 60.7% after 72 mg/kg etodolac). In tests of nociception, H. perforatum, administered orally, displayed antinociceptive activity in the tail electric stimulation and hot plate tests. The antinociceptive activity was observed with 25 mg/kg and a maximal increase in hot plate latency by 50% (compared to 73.2 and 77.8% increases by 5 or 10 mg/kg fluoxetine, respectively). In contrast, the acetic acid-induced (0.6%, i.p.) writhing was significantly reduced by fluoxetine or etodolac, but not H. perforatum. Also, the nociceptive response caused by i.p. injection of capsaicin (1.6 microg/paw) was unaffected by H. perforatum, but reduced by fluoxetine. Injection of H. perforatum (50, 125, or 250 mg/kg, s.c.) to pylorus-ligated rats, decreased gastric acid secretion, but increased indomethacin-induced gastric mucosal lesions dose dependently. These results demonstrate that H. perforatum exhibits antiedematogenic and antinociceptive properties, which may be of value for the management of inflammatory painful conditions. The agent, however, causes gastric irritation and may aggravate that of NSAIDs.

Topics: Acetic Acid; Analgesics, Non-Narcotic; Animals; Anti-Inflammatory Agents, Non-Steroidal; Capsaicin; Carrageenan; Drug Evaluation, Preclinical; Edema; Electroshock; Etodolac; Fluoxetine; Gastric Acid; Gastric Mucosa; Hot Temperature; Hypericum; Indomethacin; Pain; Peritonitis; Plant Extracts; Rats; Rats, Sprague-Dawley; Selective Serotonin Reuptake Inhibitors; Stomach Ulcer

Echinacea purpurea (L.) Moench and Hypericum perforatum (L.) were evaluated for their anti-inflammatory activity against carrageenan-induced paw oedema in mice. Each drug was administered orally to mice at 30 and 100 mg kg(-1), twice daily. Only the higher dose significantly inhibited, time dependently, the formation of oedema, evaluated as area under the curve (echinacea P < 0.01; hypericum P < 0.05). Western blot analysis showed that in-vivo treatment with these extracts could modulate lipopolysaccharide (LPS) and interferon-gamma induced cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression in peritoneal macrophages. In particular, treatment with 100 mg kg(-1) hypericum inhibited both iNOS and COX-2 expression, whereas treatment with 100 mg kg(-1) echinacea down-regulated only COX-2 expression. The present study suggests that the anti-inflammatory effect of these extracts could be in part related to their modulation of COX-2 expression.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Blotting, Western; Carrageenan; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Cyclooxygenase Inhibitors; Echinacea; Edema; Enzyme Inhibitors; Hypericum; Indomethacin; Isoenzymes; Macrophages, Peritoneal; Male; Mice; Mice, Inbred BALB C; Nitric Oxide Synthase; Nitric Oxide Synthase Type II; Plant Extracts; Prostaglandin-Endoperoxide Synthases

The aim of the present study was to explore the probable antiinflammatory effect of Hypericum triquetrifolium Turra. in a rat model of carrageenan induced inflammation. Male Wistar rats were treated intraperitoneally with 0.4% dimethylsulphoxide (DMSO) (as control group) and H. triquetrifolium extract (25, 50, 60 mg/kg), 30 min before 0.1 ml 1% carrageenan injection. Paw volume was measured before and 1, 2, 3, 4, 5 and 6 h after the injection of carrageenan. The results are expressed as the mean+/-s.e. mean and the statistical significance of differences between groups was analyzed by One Way Analysis of Variance (ANOVA). The intraplantar injection of carrageenan caused a time-dependent paw edema in the rat although saline injection caused no swelling. Intraperitoneal administration of H. triquetrifolium extract (25, 50, 60 mg/kg) inhibited paw swelling dose-dependently at 2, 3, 4, 5 and 6 h after carrageenan injection (P<0.05). We can conclude that H. triquetrifolium extract may exert an antiinflammatory effect in rats.

Topics: Animals; Anti-Inflammatory Agents; Carrageenan; Edema; Hypericum; Male; Methanol; Phytotherapy; Plant Extracts; Rats; Rats, Wistar; Solvents

A standardised 50% aqueous ethanolic extract of the Indian variety of Hypericum perforatum (IHp) was examined for its putative anti-inflammatory and analgesic activity at the doses of 100 and 200 mg/kg, po. The experimental paradigms used were carrageenan induced pedal edema and cotton pellet induced granuloma for anti-inflammatory activity, whereas the tail flick, hot plate and acetic acid induced writhing methods were used to asses analgesic activity. Indomethacin (20 mg/kg, ip) was used as the standard anti-inflammatory drug. Pentazocine (10 mg/kg, ip) and aspirin (25 mg/kg, ip), both clinically used analgesics, were used as standard analgesics for comparison. IHp extract showed significant anti-inflammatory and analgesic activity at both dose levels, in all the paradigms used. Additionally, IHp potentiated the anti-inflammatory activity of indomethacin and analgesic activities of pentazocine and aspirin.

Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Aspirin; Edema; Female; Granuloma, Foreign-Body; Hypericum; Male; Mice; Pain Threshold; Pentazocine; Plant Extracts; Plants, Medicinal; Rats