Analgesic and anti-inflammatory potential of ethanolic extract from Serjania erecta leaves.

ETHNOPHARMACOLOGICAL RELEVANCE: The infusion of Serjania erecta Radlk (Sapindaceae) (popular name "cipó-cinco-folhas") leaves is used in popular medicine to treat back pain. The anti-inflammatory, anti-hyperalgesic and anti-nociceptive properties of the ethanolic extract from S. erecta leaves (EESE) has not been yet completely clarified. AIM OF THE STUDY: The present study investigated the anti-hyperalgesic, anti-nociceptive and anti-inflammatory properties of EESE in experimental models in mice. MATERIAL AND METHODS: EESE was fractionated by chromatographic techniques and the compound was identified by nuclear magnetic resonance (NMR), infrared (IR) spectrum, ultraviolet (UV) methods. Mice received a single dose of EESE by oral route (30, 100, and 300 mg/kg, p.o.) and were submitted to nociception induced by formalin, pleurisy induced by carrageenan and peritonitis induced by zymosan models. Mice also received EESE (30 and 100 mg/kg, p.o.) for 22 days in Complete Freund Adjuvant (CFA) model and another group received EESE for 7 days (30 and 100 mg/kg, p.o.) in pleurisy induced by Bacillus Calmette-Guerin (BCG). The cytotoxicity (MTT), phagocytic and chemotactic inhibitory activities of EESE were performed in in vitro assays. RESULTS: The fractionation of EESE led to the identification of kaempferol-3-O-α-L-rhamnopyranoside. The oral administration of all doses of EESE decreased the nociceptive response induced by formalin. EESE significantly inhibited leukocyte migration in carrageenan-induced pleurisy and zymosan peritonitis models. The daily administration of EESE during for 7 days inhibited the leukocyte migration and the mycobacteria growth of pleural material obtained from animals which received BCG. EESE significantly reduced edema, cold allodynia and mechanical hyperalgesia responses induced by CFA. EESE did not induce cytotoxicity, and also decreased the leukocyte phagocytic activity, as well as, neutrophil chemotaxis. CONCLUSIONS: EESE showed analgesic and anti-inflammatory properties in acute and persistent experimental models in mice. EESE also reduced in vitro leukocyte chemotaxis and phagocytic activity without inducing cytotoxicity. The continuous oral treatment with EESE was effective against hyperalgesia and inflammation and these results could explain the popular use of S. erecta as an analgesic natural agent.

Contribution of spathulenol to the anti-nociceptive effects of Psidium guineense.

Objectives: Araçá-verdadeiro is the popular name of Psidium guineense (Myrtaceae), whose fruits and leaves are used in Brazilian folk medicine for treatment of inflammation and pain. The focus of the present research was an investigation of the anti-nociceptive, and anti-inflammatory effects of the essential oil from P. guineense (EOPG) leaves, and of spathulenol. The anxiolytic and antidepressive effects associated with chronic pain were also investigated in models of acute or persistent nociception or/and inflammatory pain.Methods and Results: Oral treatment with EOPG (10-100 mg/kg) or spathulenol (10 mg/kg) significantly inhibited formalin-induced nociceptive responses, both sensitivity to cold and edema. Oral treatment with EOPG (10 mg/kg) and spathulenol (10 mg/kg) did not reduce locomotor activity (open field test). Local administration of spathulenol (1000 µg/paw) significantly prevented formalin-induced nociceptive sensitivity to cold and paw edema, and carrageenan-induced mechanical hyperalgesia, paw edema and sensitivity to cold. In the Freund's complete adjuvant (CFA) model, oral treatment with EOPG (10 mg/kg) or spathulenol (10 mg/kg) for 21 days significantly inhibited all analyzed parameters. The percentage maximal inhibition by spathulenol was 76.00% (mechanical hyperalgesia), 71.90% (cold response), 85.00% (edema), 77.16% (myeloperoxidase activity), 97.72% (time in the closed arms in the elevated plus maze), and 49.00% (immobility time in the tail suspension test), in the CFA model. Models employed male Swiss mice, except for the CFA test, which employed C57bL6 male mice (n=6 /group).Conclusion: This study demonstrates that EOPG is an anti-nociceptive and anti-hyperalgesic agent, in acute and continuous treatment, and an anxiolytic and antidepressive agent when tested with the chronic pain experimental state.

Blutaparon portulacoides ethanolic extract reduced IL-1ß and inflammatory parameters induced by the Mycobacterium complex and carrageenan in mice.

Information on the health benefits of ethanolic extracts obtained from Blutaparon portulacoides stem (EEBP) hasn´t been consistently described in the literature until the present moment. This study investigated the antimycobacterial, anti-inflammatory and toxicological effects of EEBP in models of inflammation/infection, as well as its chemical composition. Chemical analysis of EEBP by electrospray ionization-mass spectrometry/HPLC-MS/MS identified 3,5,3'-Trihydroxy-4'-methoxy-6,7-methylenedioxy-flavone, gomphrenol, ferulic, vanillic, and caffeic acids. The minimum inhibitory concentration of EEBP and isoniazid in the presence of Mycobacterium tuberculosis was 123.4 and 0.030 µg/ml, respectively. EEBP oral administration (p.o.) (300-1000 mg/kg) or dexamethasone subcutaneous injection (s.c.) (1 mg/kg) significantly inhibited leukocytes and proteins resulting from carrageenan-induced pleurisy in Swiss mice. In the BCG-induced pleurisy model, the oral treatments performed once a day for 7 days, with EEBP (30 and 100 mg/kg) and isoniazid (25 mg/kg), inhibited the increase in plasmatic IL-1ß levels and in pleural exudate from C57BL-6 mice, and reduced M. tuberculosis growth in organs (colony forming units assays). EEBP (30-300 mg/kg, p.o.) and dexamethasone (1 mg/s.c.) significantly prevented carrageenan-induced oedema and mechanical hyperalgesia in Swiss mice. The treatments (once a day for 22 days) with EEBP (30 mg/kg, p.o.) and dexamethasone (1 mg/s.c.) substantially inhibited oedema and mechanical- and cold-hyperalgesia at 11, 16 and 22 days after the administration of Freund's Complete Adjuvant in C57bL6 mice. No evidence of physio-pathologic was observed in Wistar rats acutely treated with EEBP (2000 mg/kg, p.o.). This study confirms the anti-inflammatory and antibiotic properties of EEBP, opening possibilities for the development of safe new drugs with dual anti-inflammatory/antimycobacterial activities which could be favorable from a pharmacoeconomic perspective.

Antiarthritic and Antihyperalgesic Properties of Ethanolic Extract from Gomphrena celosioides Mart. (Amaranthaceae) Aerial Parts.

Gomphrena celosioides Mart. (Amaranthaceae) is used in folk medicine as a natural analgesic, and in Brazil, the species of genus Gomphrena is used for rheumatism. However, scientific evidence which supports its popular use as an analgesic is scarce. This study assessed the antiarthritic and antihyperalgesic activities of the ethanolic extract obtained from G. celosioides aerial parts on Swiss or C57BL/6 mice. The antiarthritic and antihyperalgesic potential of Gomphrena celosioides was evaluated using paw edema, mechanical hyperalgesia, cold allodynia, carrageenan-induced pleurisy, articular inflammation zymosan-induced, Freund's complete adjuvant-induced inflammation zymosan-induced peritonitis, and carrageenan-induced adhesion and rolling experiment models. All doses of G. celosioides (300, 700, and 1000 mg/kg) significantly reduced edema formation in all the intervals evaluated, whereas the mechanical hyperalgesia was reduced 3 hours after the carrageenan injection. The cold hyperalgesia was significantly decreased 3 (700 mg/kg) and 4 hours (700 and 1000 mg/kg) after the carrageenan injection. Ethanolic extract of G. celosioides at 1000 mg/kg reduced the total leukocyte number, without interfering in the protein extravasation in carrageenan-induced pleurisy model. Ethanolic extract of G. celosioides (300 mg/kg) was also able to reduce significantly the leukocyte migration in zymosan-induced articular edema, while a reduction of the adhesion and migration and leukocyte rolling was induced by the ethanolic extract of G. celosioides (300 mg/kg) in zymosan-induced peritonitis. In Freund's complete adjuvant-induced inflammation model, an edema formation and mechanical hyperalgesia reduction were induced by the ethanolic extract of G. celosioides on day 22, whereas the cold allodynia was reduced on day 6 of treatment with the extract. These results show that ethanolic extract of G. celosioides has antihyperalgesic and antiarthritic potential in different acute and persistent models, explaining, at least in part, the ethnopharmacological relevance of this plant as a natural analgesic agent.

Antimicrobial activity of plant extracts against carbapenem-producing Klebsiella pneumoniae and in vivo toxicological assessment.

The global spread of multidrug-resistant strains has prompted the scientific community to explore novel sources of chemicals with antimicrobial activity. The aim of the study was to examine the antimicrobial activity in vitro of 28 extracts against carbapenem-producing Klebsiella pneumoniae, individually and in combination with antibiotics and in vivo toxicological assessment of the most active product. The multi-resistant K. pneumoniae strain was submitted for phenotypic and molecular characterization. The antibacterial activity of 28 plant extracts was evaluated alone and in combination with antibiotics against this strain through the agar disk diffusion. Of these, 16 extracts showed synergism against carbapenem-producing K. pneumoniae, being that B. crassifolia extract exhibited synergism with three antibiotics. Based on this assessment, B. crassifolia-extract-induced toxicity on Swiss male mice was evaluated by administering this extract and subsequently determining apoptosis and splenic phagocytosis using the comet and micronucleus assays. The results of this study showed that B. crassifolia extract had synergistic activity promising and groups treated with B. crassifolia exhibited no genotoxic or mutagenic activity, indicating that B. crassifolia extract exerted beneficial effects and appeared safe to use at the studied concentrations.

Anti-inflammatory and anti-arthritic activity in extract from the leaves of Eriobotrya japonica.

ETHNOPHARMACOLOGICAL RELEVANCE: The Eriobotrya japonica (EJ) is a Chinese medicinal plant that is currently grown in Brazil. E. japonica leaves infusion is traditionally used in the treatment of inflammation; however, there are few scientific studies showing the effects of these properties on joint articular and persistent experimental inflammation. AIM OF THE STUDY: The present research had objective investigation of the effect of infusion obtained from leaves of E. japonica (EJLE) on acute and persistent experimental articular inflammation. MATERIALS AND METHODS: The Swiss mice were treated orally with EJLE and analyzed for acute pleural inflammation (30, 100, and 300 mg/kg), paw edema induced by carrageenan (100 mg/kg), acute knee inflammation induced by zymosan (100 mg/kg), and persistent inflammation induced by Complete Freund's Adjuvant (CFA) (30 and 100 mg/kg). Mechanical hyperalgesia, cold and edema were analyzed. RESULTS: The chromatographic analysis of EJLE revealed the presence of corosolic acid, oleanolic acid, and ursolic acid. EJLE presented anti-inflammatory activity in the pleurisy model, inhibiting leukocyte migration, protein extravasation and nitric oxide production. In the articular inflammation model, EJLE reduced the number of leukocytes in the joint cavity, paw edema and hyperalgesia (4 h after induction). In the persistent inflammation model induced by CFA, the extract reduced paw edema after 11 days of mechanical and cold hyperalgesia on day 6. CONCLUSIONS: The EJLE has anti-inflammatory and antihyperalgesic potential in models of acute and persistent experimental articular inflammation, making this infusion a new possibility for complementary treating acute or chronic articular inflammatory diseases.