Anti-secretory, anti-inflammatory and anti- Helicobacter pylori activities of several fractions isolated from Piper carpunya Ruiz & Pav

• Published in: Journal of ethnopharmacology 2010-04, Vol.128 (3), p.583-589
• Main Authors: Quílez, A., Berenguer, B., Gilardoni, G., Souccar, C., de Mendonça, S., Oliveira, L.F.S., Martín-Calero, M.J., Vidari, G.
• Format: Article
• Language: English
• Subjects: adenosinetriphosphatase; Animals; Anti- Helicobacter pylori activity; Anti-inflammatory activity; Anti-Inflammatory Agents - analysis; Anti-Inflammatory Agents - pharmacology; Anti-Inflammatory Agents - therapeutic use; anti-secretory activity; anti-ulcer activity; antibacterial properties; Antineoplastic Combined Chemotherapy Protocols; antioxidant activity; Apigenin - analysis; Apigenin - pharmacology; Apigenin - therapeutic use; Biological and medical sciences; Cisplatin; cultured cells; DNA-directed DNA polymerase; Doxorubicin; enzyme inhibition; enzyme inhibitors; Etoposide; Flavonoids; Flavonoids - analysis; Flavonoids - isolation & purification; Flavonoids - pharmacology; fractionation; free radical scavengers; General pharmacology; H +, K +-ATPase activity; Helicobacter pylori; Helicobacter pylori - drug effects; herbal medicines; in vitro studies; inhibitory concentration 50; leaves; Male; Medical sciences; medicinal plants; Medicine, Traditional; nuclear magnetic resonance spectroscopy; peroxidase; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; phytochemicals; Piper; Piper - chemistry; Piper carpunya; plant extracts; Plant Leaves - chemistry; Prenylated benzoic acid derivatives; protective effect; Rabbits; Rats; Rats, Wistar; South America; Stomach - drug effects; stomach ulcers; traditional medicine
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2010.01.060

The ethanolic extract of the leaves of Piper carpunya was subjected to column chromatography and 16 pure compounds were isolated and identified. Among these, the terpenoids sitosterol, stigmasterol and phytol as well as the flavonoids vitexin, isovitexin, rhamnopyranosylvitexin and isoembigenin probably contribute to the significant myeloperoxidase, Helicobater pylori and H +, K +-ATPase inhibitory activity observed with many of the fractions. Furthermore, neolignan, which is a DNA polymerase β lyase inhibitor, and (6S, 9S)-roseoside, that shows strong anti-bacterial activity, were isolated, for the first time, from the genus Piper. The leaves of Piper carpunya Ruiz & Pav. (syn Piper lenticellosum C.D.C.) (Piperaceae), are widely used in folk medicine in tropical and subtropical countries of South America as an anti-inflammatory, anti-ulcer, anti-diarrheal and anti-parasitical remedy as well as an ailment for skin irritations. To study the anti-inflammatory, anti-secretory and anti- Helicobacter pylori activities of different fractions isolated from an ethanolic extract of the leaves of Piper carpunya, in order to provide evidence for the use of this plant as an anti-ulcer remedy. Moreover, to isolate the main compounds of the extract and relate their biological activity to the experimental results obtained with the fractions. Sixteen fractions were obtained from the ethanolic extract (F I–XVI) and 16 pure compounds were isolated and identified from these fractions. We studied the effects of the fractions (0.1–400 μg/mL) on the release of myeloperoxidase (MPO) enzyme from rat peritoneal leukocytes, on rabbit gastric microsomal H +, K +-ATPase activity and anti- Helicobacter pylori anti-microbial activity using the microdilution method (MM). The main compounds contained in the fractions were isolated and identified by 1H- and 13C NMR spectra analysis and comparison with the literature data. Eight fractions showed inhibition of MPO enzyme (F I–IV, X, XII, XIV and XV). The highest inhibition was observed with F XIV (50 μg/mL, 60.9%, p < 0.001). F X and XII were the most active ones, inhibiting the gastric H +, K +-ATPase activity with IC 50 values equal to 22.3 μg/mL and 28.1 μg/mL, respectively. All fractions, except F XV, presented detectable anti- Helicobacter pylori activity, with a diameter of inhibition zones ranging from 11 mm up to 50 mm. The best anti- Helicobacter pylori activity was obtained with F III and V. Both fractions killed Helicobacter pylo