Pharmacologycal activity of peperina (Minthostachys verticillata) on gastrointestinal tract.

ETHNOPHARMACOLOGICAL RELEVANCE: Minthostachys verticillata (Griseb.) Epling (Lamiaceae), known as Peperina is a medicinal native plant, with a traditional use as a digestive, antispasmodic and antidiarrheic. AIM OF THE STUDY: Despite its folkloric use, no scientific evaluation of this plant related to the gastrointestinal inflammatory process has been carried out to date. The present study aims to assess the effects of M. verticillata on gastrointestinal system in experimental models. MATERIALS AND METHODS: M. verticillata (250 and 500 mg/kg) was orally tested in a colitis model induced by acetic acid. Colon weight/length ratio, oxidative stress (oxidized and reduced glutathione), histological changes using Alcian blue and hematoxylin & eosin staining and expression of IL1ß, TNFα, iNOS, COX-2 were evaluated. The effect of the extract in three additional in vivo models were studied: intestinal motility and diarrhea induced by ricin oil, and visceral pain induced by intracolonic administration of capsaicin. Finally, the activity on concentration response curves of acetylcholine, calcium chloride, potassium and serotonin were achieved in isolated rat jejunum. RESULTS: In the colitis model, M. verticillata induced a significant reduction in the colon weight/length ratio, oxidative stress and expression levels of IL-1ß, iNOS and COX-2. Also, the extract diminished the severity of microscopic tissue damage and showed protective effect on goblet cells. Intestinal motility, diarrhea, visceral pain-related behaviors and referred hyperalgesia were significantly reduced when the animals were treated with the extract. Furthermore, in isolated jejunum, M. verticillata significantly reduced the contraction induced by serotonin and acetylcholine. Likewise, the extract non-competitively inhibited the response-concentration induced by CaCl2 and inhibited both low and high K+-induced contractions. CONCLUSIONS: This is the first study to validate traditional use of M. verticillata for digestive disorders and demonstrated that its aqueous extract could represent a promising strategy in targeting the multifactorial pathophysiology of inflammatory bowel disease.

Beneficial properties of Passiflora caerulea on experimental colitis.

ETHNOPHARMACOLOGICAL RELEVANCE: Passiflora caerulea L. (Passifloraceae) is a medicinal plant commonly used in traditional medicine in South America for different pathologies associated with the gastrointestinal tract. AIM OF THE STUDY: In the present study, the activity of the ethanolic extract of P. caerulea on an experimental colitis model related to inflammatory bowel disease has been investigated. MATERIALS AND METHODS: Colitis was induced by intracolonic instillation of a 2mL of 4% (v/v) acetic acid solution. Macroscopic scoring, myeloperoxidase activity and thiobarbituric acid reactive substances levels were evaluated on isolated colon mucosae. The histopathological studies of colon mucosae were performed by hematoxylin and eosin and Alcian blue staining. Diarrhoea was induced by the administration of castor oil (0.3mL/mouse). The first watery defecation time, the total amount of solid, semi-solid and watery stools and the amount of watery stools were determined. The effect of the extract on a cumulative concentration-response curve of acetylcholine and CaCl2 on isolated rat jejunum was also evaluated. The phytochemical analysis was performed. RESULTS: The extract (250mg/kg, p.o.) induced a significant reduction in the weight/length ratio, the macroscopic lesion score, TBARS levels and the microscopic tissue damage when compared with the acetic acid-treated group of animals. P. caerulea (125mg/kg, p.o.) decreased significantly the amount of watery stools in the castor oil-induced-diarrhoea model. Moreover, the P. caerulea extract antagonized the jejunum contractions induced by Ach (Emax for 0.3mg/mL: 76.25%; Emax for 1mg/mL: 63.47%; Emax for 3mg/mL: 42.01%) and CaCl2 (Emax for 0.3mg/mL: 75.69%; Emax for1 mg/mL: 56.1%; Emax for 3mg/mL: 53.4%). Isoorientin, vitexin, isovitexin, and vicenin-2 were identified in the extract. CONCLUSION: P. caerulea showed anti-inflammatory, anti-diarrhoeal and spasmolityc activities on preclinical models.

Protective antifungal activity of essential oils extracted from Buddleja perfoliata and Pelargonium graveolens against fungi isolated from stored grains.

AIMS: The chemical composition and antifungal activity of essential oils extracted from Buddleja perfoliata and Pelargonium graveolens were analysed to assess their efficacy as a potential alternative to synthetic chemical fungicides to protect stored grain. METHODS AND RESULTS: Essential oils were obtained by hydrodistillation, while GC-MS were used to characterize the components of theses oils. The main components identified from the essential oil of B. perfoliata were cubenol, eudesmol, germacrene D-4-ol and cis-verbenol; whereas (-)-aristolene, ß-citronellol and geraniol, were identified in P. graveolens. These essential oils were tested against a panel of fungal strains isolated from stored grains. Toxicity of the essential oils was assessed using two models represented by human-derived macrophages and the brine shrimp assay. Moreover, inflammatory response of the oils was assessed by measuring secretion of the pro-inflammatory cytokines IL-6 and TNF-α using a human-derived macrophage cell line. Results show potent antifungal activity against a collection of fungi, with minimal inhibitory concentrations ranging from 0·3 to 50 µg ml(-1) for both plants. A moderated cytotoxicity was observed, but no inflammatory responses. CONCLUSIONS: These oils can be used as an alternative for synthetic chemical fungicides used to protect stored grains. SIGNIFICANCE AND IMPACT OF THE STUDY: Synthetic chemical fungicides are used to protect stored grains, but their broad use raises concerns about effects on the environment and human health. The impact of the present report is that the use of essential oils is an eco-friendly alternative for fungal control in postharvest grains with a low impact to the environment.

Suppressive effects of caraway (Carum carvi) extracts on 2, 3, 7, 8-tetrachloro-dibenzo-p-dioxin-dependent gene expression of cytochrome P450 1A1 in the rat H4IIE cells.

Cytochrome P450 1A1 (CYP1A1) is among the cytochrome P450 classes known to convert xenobiotics and endogenous compounds to toxic and/or carcinogenic metabolites. Suppression of CYP1A1 over expression by certain compounds is implicated in prevention of cancer caused by chemical carcinogens. Chemopreventive agents containing high levels of flavonoids and steroids-like compounds are known to suppress CYP1A1. This study was carried out for assessment of the genomic and proteomic effects of caraway (Carum carvi) extracts containing high levels of both flavonoids and steroid-like substances on ethoxy resorufin dealkylation (EROD) activity and CYP1A1 at mRNA levels. Rat hepatoma cells co-treated with a CYP1A1 inducer i.e. TCDD (2, 3, 7, 8-tetrachlorodibenzo-p-dioxin) and different preparations of caraway extracts at concentrations of 0, 0.13, 1.3, and 13 microM in culture medium. After incubation (37 degrees C and 7% CO2 for 20 h), changes in EROD specific activity recorded and compared in cells under different treatments. The results show that caraway seed extract prepared in three different organic solvents suppressed the enzyme activity in hepatoma cells in a dose-dependent manner. The extracts added above 0.13 microM could significantly inhibit EROD activity and higher levels of each extract (1.3 and 13 microM) caused approximately 10-fold suppression in the enzyme activity. Accordingly, data obtained from the RT-PCR (TaqMan) clearly showed the suppressive effects of plant extract on CYP1A1-related mRNA expression. These data clearly show that substances in caraway seeds extractable in organic solvents can potentially reverse the TCDD-dependent induction in cytochrome P450 1A1.