Anti-inflammatory and antinociceptive effects of a pectinolide-enriched fraction from Mesosphaerum pectinatum (L.) Kuntze.

ETHNOPHARMACOLOGICAL RELEVANCE: Mesosphaerum pectinatum (L.) Kuntze (Lamiaceae), also known as sambacaitá, is a medicinal plant widely used in northeastern Brazil for the treatment of inflammatory and painful conditions, bacterial infections and cancer. Hence, the medicinal use of this species is quite meaningful to the search for bioactive compounds. AIM OF THE STUDY: To evaluate the antinociceptive and anti-inflammatory activities of the pectinolide-enriched fraction of Mesosphaerum pectinatum (PEF) in animal models. MATERIALS AND METHODS: The PEF was analyzed with HPLC-DAD and 1H and 13C NMR. After the analysis, compounds of the pectinolide class were detected as major constituents in this fraction. The PEF (50, 100 and 200 mg/kg, p.o.) and the reference drugs - morphine (3.0 mg/kg, p.o.) and dexamethasone (2.0 mg/kg, p.o.) - were evaluated using models for nociception (hot plate, formalin-induced licking response) or inflammation (carrageenan-induced peritonitis and ear edema model). RESULTS: The PEF significantly decreased the licking time of the animals treated when compared to the control group (second phase). In the carrageenan-induced peritonitis model, PEF (100 and 200 mg/kg) significantly decreased total and differential leukocyte counts. The PEF (0.3, 1.0 and 3.0 mg/ear) significantly reduced mice ear edema at the same extent and like the results obtained with the standard drug (dexamethasone). The MPO activity was reduced in mice ear at doses of 1 and 3 mg/ear. Antinociceptive effect on the hot plate test was not observed, demonstrating that there is no analgesic activity. CONCLUSION: Our results suggest that the pectinolide-enriched fraction exhibits anti-inflammatory effects and that it is involved with inhibiting the release of the inflammatory mediators.

Hepatoprotective Effect of Essential Oils from Hyptis crenata in Sepsis-Induced Liver Dysfunction.

No specific therapeutics are available for the treatment of sepsis-induced liver dysfunction, a clinical complication strongly associated with the high mortality rate of septic patients. This study investigated the effect of the essential oil of Hyptis crenata (EOHc), a lamiaceae plant used to treat liver disturbances in Brazilian folk medicine, on liver function during early sepsis. Sepsis was induced by the cecal ligation and puncture (CLP) model. Rats were divided into four groups: Sham, Sham+EOHc, CLP, and CLP+EOHc. EOHc (300 mg/kg) was orally administered 12 and 24 h after surgery. The animals were sacrificed for blood collection and liver tissue samples 48 h after surgery. Hepatic function was evaluated by measuring serum bilirubin, alkaline phosphatase (ALP), aspartate aminotransferase, and alanine aminotransferase (ALT) levels. The levels of malondialdehyde and the activity of superoxide dismutase, catalase, and GSH peroxidase (GSH-Px) were measured for assessment of oxidative stress. Liver morphology was analyzed by hematoxylin and eosin staining. EOHc normalized serum ALP, ALT, and bilirubin levels and inhibited morphological changes. In addition, we observed that EOHc inhibited elevation in hepatic lipid peroxidation and reduction of the glutathione peroxidase activity induced by sepsis. Our data show that EOHc plays a protective effect against liver injury induced by sepsis.

Protective effect of carvacrol on acetic acid-induced colitis.

The pharmacological therapy for inflammatory bowel diseases continues to be problematic, and requires new alternative options. In this study, we tested the hypothesis that carvacrol (CAR), a phenolic monoterpene with anti-inflammatory and antioxidant activities, can treat experimental colitis in mice. C57BL/6 mice (n=8/group) were subjected to intrarectal administration of acetic acid (5%) to induce colitis. Mice were pretreated with CAR (25, 50 or 100mg/kg, p.o.) every 12h for three days prior to the induction. Abdominal hyperalgesia, macroscopic and microscopic colon damage, myeloperoxidase (MPO) activity, tumor necrosis factor (TNF)-α and interleukin (IL)-1ß levels, oxidative stress markers, and antioxidant enzyme activities were evaluated. Pretreatment with all doses of CAR significantly decreased abdominal hyperalgesia and colon MPO activity and TNF-α and IL-1ß levels. A reduction in macroscopic and microscopic damage (p<0.05) was observed at doses of 50 and 100mg/kg CAR. Pretreatment with CAR significantly reduced lipid peroxidation (for all doses) and increased sulfhydryl groups (at 100mg/kg). This effect was accompanied by a significant increase in catalase, superoxide dismutase, and glutathione peroxidase activities. These findings indicate that CAR protected mice from acetic acid-induced colitis by reducing inflammatory, nociceptive, and oxidative damages.

The ethanol extract of Leonurus sibiricus L. induces antioxidant, antinociceptive and topical anti-inflammatory effects.

ETHNOPHARMACOLOGICAL RELEVANCE: Leonurus sibiricus L. (Lamiaceae), popularly known as motherwort, or "erva-de-macaé" or "rubim" in Brazil, is a plant used for the treatment of inflammatory conditions, but few studies have evaluated this anti-inflammatory activity or other activities that may be relevant. AIM OF THE STUDY: This study was undertaken to investigate the antioxidant, antinociceptive and topical anti-inflammatory effects of the ethanol extract of L. sibiricus (EELs). MATERIALS AND METHODS: Chromatographic analysis, determination of total phenolic and flavonoid contents and in vitro antioxidant assays were performed, while the formalin test and ear inflammation induced by 12-0-tetradecanoylphorbol-13-acetate (TPA) were performed in mice. RESULTS: We observed that total phenolic and flavonoids content in EELs were respectively 60.1mg of gallic acid equivalent/g of extract and 15.4mg of catechin equivalent/g of extract. Chlorogenic, caffeic, p-coumaric and ferulic acids, as well as quercetin were identified in EELs. This extract also led to the consumption of the radicals 2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) and nitric oxide, increased the ferric reducing/antioxidant power (FRAP) and inhibited the spontaneous or FeSO4-induced in vitro lipid peroxidation. In the formalin test, oral pretreatment with EELs (400mg/kg) reduced (p<0.001) the licking/biting time in the second phase, but not in the first phase. In the ear inflammation induced by TPA, the concomitant topical administration of EELs (0.3-3mg/ear) significantly reduced the edema, myeloperoxidase activity, levels of tumoral necrosis factor-α and interleukin-1ß and lipoperoxidation, as well as increased FRAP in ear tissue when compared to vehicle-treated ears. CONCLUSIONS: These results indicate that EELs has antioxidant, antinociceptive and topical anti-inflammatory activities, supporting the use of this plant in folk medicine.