ABSTRACT
Aims: Evaluation of the anti-inflammatory properties of new thiazolidine-2,4-diones derivatives. Study Design: Study the effects of new thiazolidine-2,4-diones derivatives on the inflammatory process. Place and Duration of Study: Departamento de Antibióticos, Universidade Federal de Pernambuco (UFPE), between June 2011 and July 2012. Methodology: Compounds thiazolidine-2,4-diones were tested for anti-inflammatory activity by air pouch model. Swiss albino mice were used for the study. Air cavities were produced by subcutaneous injection of 2.5 mL of sterile air into the intrascapular area of the back. An additional 2.5 mL of air was injected into the cavity every 3 days to keep the space open. Seven days after the initial air injection, 1 mL of a 1% solution of carrageenan dissolved in saline was injected directly into the pouch to produce an inflammatory response. The compoundsthiazolidine-2,4-diones and standard piroxicam were tested at doses of 3 mg/kg body weight. The total number of polymorphonuclear leukocytes (PMNL) was countedusing an improved. Results: The results support the use of these derivatives in inflammatory process. Among the compounds tested the ones that showed a greater effect in inhibiting the migration of neutrophils were the 3a, 3b, 3c, 3d and 3e. The anti-inflammatory effects showed by 3a-j were promising, probably due to the duality of action on PPAR alpha and gamma. Conclusion: In conclusion, this study has shown that the thiazolidine derivatives do possess significant anti-inflammatory effects in laboratory animals. The exact mechanism and the bioactive principles responsible for these actions remain to be explained.
ABSTRACT
Aims: This paper describes the anti-inflammatory and antinociceptive effects of the aqueous extract of Chrysobalanus icaco. Study Design: Study the anti-inflammatory and antinociceptive activity of the aqueous extract of C. icaco using in vivo models. Place and Duration of Study: Department of Antibiotics and Department of Pharmaceutical Science, Federal University of Pernambuco, Recife, Pernambuco, Brazil, between March 2010 and March 2012. Methodology: The anti-inflammatory activity was evaluated by carrageenan/dextraninduced paw edema, vascular permeability induced by acetic acid and subcutaneous air pouch models, with measurements of cell migration, nitric oxide and cytokines TNF-α and IL-6. Acetic acid-induced abdominal writhing, formalin and hot plate tests were performed to investigate the antinociceptive effects. Results: The aqueous extract of C. icaco (100, 200 and 400 mg/kg) reduced dextran/carrageenan-induced rat paw edema, the vascular permeability, cell migration, and nitric oxide concentration. However, it did not affect the levels of TNF-α and IL-6 produced in the pouch. The aqueous extract also demonstrated antinociceptive activity by acetic acid-induced abdominal writhing and formalin test, and was able to prolong the reaction time in the hot plate model in the first hour with activity similar to morphine (2.5 mg/kg, s.c.). There was no acute toxicity in mice after oral administration of the aqueous extract at doses of 2 g/kg. Conclusion: Our results indicate that the aqueous extract of C. icaco demonstrated antiinflammatory activity through the reduction of vascular permeability, inhibition of cellular migration and nitric oxide production and that the antinociceptive activity seems to be mediated by central mechanisms.
ABSTRACT
Aims: The aim of this study was to investigate the anti-inflammatory, antiarthritic and antinociceptive effects of two thiazolidinedione derivatives: 3-(2-bromo-benzyl)-5-(4- methylsufonyl-benzylidene)-thiazolidine-2,4-dione (LPSF/GQ-125) and 3-(2,6-difluorobenzyl)- 5-(4-methylsufonyl-benzylidene)-thiazolidine-2,4-dione (LPSF/GQ-192). Study Design: Study the effects of thiazolidinedione derivatives on the inflammatory process. Place and Duration of Study: Department of Antibiotics of the Federal University of Pernambuco, Brazil, between March 2010 and February 2012. Methodology: The carrageenan-induced air pouch in mice was performed and cytokine levels (TNF-α and IL-1β) were determined. Arthritis was induced in female wistar rats by complete Freund's adjuvant (CFA). To determine the antinociceptive activity, acetic acidinduced nociception and hot plate tests in mice were utilized. Results: Treatment with the compounds reduced leukocyte migration and the release of both TNF-α and IL-1β in the air pouch. Both LPSF/GQ-125 and LPSF/GQ-192 reduced the CFA-induced paw edema and the nociception induced by acetic acid; the hot plate test, however, showed no antinociceptive activity when compared to the control group. Conclusion: These results indicate that LPSF/GQ-125 and LPSF/GQ-192 exhibit promising anti-inflammatory, antinociceptive and antiarthritic activities related to their ability to inhibit TNF-α and IL-1β production as well as reduction of leukocyte migration.
ABSTRACT
BACKGROUND: Sepsis is a systemic inflammation associated with infection caused by pathogenic micro-organisms with high mortality rates. OBJECTIVE: In this study, we investigated the protective effect of Propionibacterium acnes-killed against polymicrobial sepsis induced by cecal ligation and puncture. METHODS: The mice were treated by intramuscular route in 1, 3, 5, and 7 days before the cecal ligation and puncture induction. The control group animals received vehicle (saline solution 0.9%) and the animals of the treated group received the P. acnes-killed (0.4 mg/animal). After anesthesia, midline laparotomy was performed with exposure of cecum followed by ligature and one transverse perforation of the same, with a 18 G needle, for induction of lethal sepsis. After surgery, the cecum of the animals was replaced into the peritoneal cavity, and it was closed with a 4.0 nylon suture. The survival of animals subjected to lethal sepsis was evaluated after cecal ligation and puncture induction. Six hours after the induction of sepsis, neutrophil migration, the number of bacteria, TNF-α, MCP-1, IL-6, and IL-10 were performed in the peritoneal lavage. RESULTS: Prophylactic treatment with P. acnes-killed increased the survival of the animals, followed by a significant decrease in the TNF-α, IL-10, and MCP-1 levels, 6 h after cecal ligation and puncture. Furthermore, P. acnes-killed administration reduced the number of bacteria in the peritoneal cavity with increased migration of leukocytes, especially neutrophils. CONCLUSION: P. acnes-killed promoted increased survival rate of animals with sepsis, in part attributed to its immunomodulatory properties against pathogenic microorganisms, as well as better control of infection by reducing bacterial counts.