No abstract

The purpose of this study was to investigate the effects of a semisolid formulation of linseed oil, SSFLO (1%, 5%, or 10%) or in natura linseed oil on skin wounds of rats. We used wound models, incisional and excisional, to evaluate, respectively, the contraction/reepithelialization of the wound and resistance to mechanical traction. The groups (n = 6) treated with SSFLO (1% or 5%) began the process of reepithelialization, to a significant extent (P < .05), on the sixth day, when compared to the petroleum jelly control group. On 14th day for the groups treated with SSFLO (1% or 5%), 100% reepithelialization was found, while in the petroleum jelly control group, this was only 33.33%. Our study showed that topical administration of SSFLO (1% or 5%) in excisional wounds allowed reepithelialization in 100% of treated animals. Therefore, a therapeutic potential of linseed oil, when used at low concentrations in the solid pharmaceutical formulations, is suggested for the process of dermal repair.

Some species of the genus Miconia are used in Brazilian folk medicine as analgesic and anti-inflammatory; however, several species of this genus are still poorly studied. Therefore, the aims of this study were to investigate the phytochemistry characterization by UPLC-DAD-QTOF-MS/MS, acute toxicity, anti-inflammatory and antinociceptive properties of Miconia minutiflora (Bonpl.) DC. The methanol extract of M. minutiflora (Mm-MeOH) was subjected to ultra-high-performance liquid chromatography (UPLC-DAD-QTOF-MS/MS) for the identification of the main phytocompounds. The anti-inflammatory properties of the extracts were studied using several inflammation models induced by carrageenan and acetic acid-induced vascular permeability. Antinociceptive effects of Mm-MeOH were assessed in nociception induced by intraperitoneal acetic acid or subplantar formalin injection. The role of α-adrenergic, cholinergic, and opioid receptors in modulating the extract's antinociceptive activity was determined. Analyses by UPLC-DAD-QTOF-MS/MS revealed the presence of ellagic acid, gallotannin, and terpenes in the methanol extract. Mm-MeOH (100 mg/kg) reduced carrageenan-induced paw edema and vascular permeability and inhibited leukocyte migration toward the air pouch and pleural cavity. Furthermore, Mm-MeOH decreased tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) levels. Administration of Mm-MeOH reduced the number of writhes by 58.9% and increased the pain threshold in the formalin test. The anti-inflammatory action mechanism of Mm-MeOH is associated with inhibition of proinflammatory cytokines TNF-α and IL-1β, whereas the antinociceptive actions involve peripheral and central mechanisms with participation of α2-adrenergic receptors. These effects may be attributed to the presence of polyphenolics in the extract.

The main limitation in the use of anti-inflammatory drugs or drugs that inhibit some aspects of inflammation is their secondary effects, especially on the gastro-intestinal tract, during chronic use. Therefore, anti-inflammatory drugs without such effects have been one of the main objectives of researchers. 1)Modern organic chemistry development has provided an increased number of substances for various therapeutic aims. Among the methods for obtaining new drugs, molecular modification or variation using the Bioisostery concept is often used. Using this chemical concept, substitute groups can be introduced in one or more positions of a main molecule, creating similar compounds with varied biological activities that can show interesting medical properties. With this process, we can analyze the influence of the modification of an atom or a group of atoms on the main molecule's biological activity. The molecular alterations can result in molecules with similar, antagonistic or more larger potent activity than that of the original compound.2)The thiazolidinic and imidazolidinic nuclei represent a category of compounds that present promising biological activities: insecticidal, 3) antimicrobial, antifungal, narcotic, sedative, anesthetic, anticonvulsive and nematocidal. 4) Góes et al. (1991) 5) showed that thiazolidine and imidazolidine derivatives (or isosters) possess antifungal (against Candida albicans and Neurospora crassa) and moderate antibiotic activity (against E. coli, S. aureus and others).Among the compounds that possess a thiazolidinic nucleus, 2,4-thiazolidinedione ( Fig. 1) and rhodanine (Fig. 2) were studied by Lima (1999) 6) with respect to the antiedematogenic properties of their isosters. In this study antiedematogenic activity was found for two bioisosters, N-tryptophyl-5-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2,4-thiazolidinedione (GS28) (MWϭ476) (Fig. 3) and N-tryptophyl-5-(3,5-di-tert-butyl-4-hydroxybenzylidene) rhodanine (GS26) (MWϭ492) (Fig. 4). Studies related to acute toxicity (LD 50 ) of GS26 and GS28 in a range of oral doses of 25, 50, 100, 250, 500 and 1000 mg/kg did not indicate any toxicity. The aim of this study was to determine the existence of antiedematogenic properties on thiazolidinic isosters GS26 and GS28 in the response evoked by well-known edematogenic agents. Chemistry Two new compounds N-tryptophyl-5-(3,5-di-

Suplementação de antioxidantes no tratamento da lesão pulmonar aguda: meta-análise OriginAl Article intrODUctiOn Antioxidant supplementation (1-3) may prolong the initial phase or inhibit the propagation phase of reactive oxygen species (ROS) and reactive nitrogen species (RNS). (4) Disrupted oxidant-antioxidant balance has a major role in the genesis of inflammatory diseases, such as acute lung injury (ALI) or acute respiratory distress syndrome (ARDS). (5,6) Antioxidants have been traditionally administered via oral, (3) intraperitoneal (1) or intravenous (2) routes. Patients with ARDS have a significant decrease when compared to healthy subjects at concentrations of reduced glutathione (138 ± 25 vs. 7 ± 4 μM), ascorbic acid (85 ± 21 vs. 27 ± 10 μM) concentrations in the bronchoalveolar lavage fluid (BALF), α-tocopherol (11.46 ± 0.55 vs. 7.73 ± 0.54 mg/L), β-carotene and selenium. (7,8) The plasma concentrations of lipid peroxides are also significantly increased versus controls [e.g., malondialdehyde (MDA), 2.2 vs. 1.3 nM]. (9,10) Additionally, patients with ARDS or patients who are at risk of ARDS show significantly reduced plasma polyunsaturated fatty acid concentrations

, 50670-901 Recife -PE Recebido em 13/11/03; aceito em 22/6/04; publicado na web em 8/10/04 SYNTHESIS AND ANTIEDEMATOGENIC ACTIVITY OF SOME N-TRYPTHOPHYL-5-BENZYLIDENE-2,4-THIAZOLIDINEDIONE AND N-TRYPTHOPHYL-5-BENZYLIDENE-RHODANINE DERIVATIVES. Derivatives of Ntryptophyl-5-benzylidene-2,4-thiazolidinedione (7a-c) and N-tryptophyl-5-benzylidene-rhodanine (7d-f) were prepared by condensation of the intermediates 5 and 6 with different benzaldehydes, respectively. Their structural elucidation was carried through by IR, 1 H NMR and MS. The acute toxicity and antiedematogenic activity of the compounds 7b,c and 7e,f were evaluated. The data did not reveal any sign of toxicity, and no mortality was registered. As indomethacin (10 mg/kg; v.o.), the antiedematogenic activity of the compounds 7b (50 mg/kg; v.o.) and 7e, 7f (50 or 100 mg/kg; v.o.) against carrageenan-induced paw edema was verified at time intervals of 180 min.

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The maternal western diet exacerbates the inflammatory response in the offspring, but does not alter the action of the non-steroidal antiinflammatory drug Dieta ocidentalizada materna exacerba a resposta inflamatória na prole, mas não altera a eficácia da ação de droga anti-inflamatória não esteroidal