The aim of this study was to evaluate the wound-healing activity of a semisolid formulation of avocado oil, SSFAO 50%, or avocado oil in natura, on incisional and excisional cutaneous wound models in Wistar rats. An additional objective was to quantify the fatty acids present in avocado oil. On the 14th day, a significant increase was observed in percentage wound contraction and reepithelialization in the groups treated with 50% SSFAO or avocado oil compared to the petroleum jelly control. Anti-inflammatory activity, increase in density of collagen, and tensile strength were observed inSSFAO 50% or avocado oil groups, when compared to control groups. The analysis of the components of avocado oil by gas chromatography detected the majority presence of oleic fatty acid (47.20%), followed by palmitic (23.66%), linoleic (13.46%) docosadienoic (8.88%), palmitoleic (3.58%), linolenic (1.60%), eicosenoic (1.29%), and myristic acids (0.33%). Our results show that avocado oil is a rich source of oleic acid and contains essential fatty acids. When used in natura or in pharmaceutical formulations for topical use, avocado oil can promote increased collagen synthesis and decreased numbers of inflammatory cells during the wound-healing process and may thus be considered a new option for treating skin wounds.

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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.

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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-

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The present study describes the use of fucoidan, a negative sulfated polysaccharide, as a coating material for the development of liposomes targeted to macrophages infected with Mycobacterium tuberculosis. First, fucoidan was chemically modified to obtain a hydrophobized-fucoidan derivative (cholesteryl-fucoidan) using a two-step microwave-assisted (μW) method. The total reaction time was decreased from 14 hours to 1 hour while maintaining the overall yield. Cholesterylfucoidan was then used to prepare surface-modified liposomes containing usnic acid (UA-LipoFuc), an antimicrobial lichen derivative. UA-LipoFuc was evaluated for mean particle size, polydispersity index (PDI), surface charge (ζ), and UA encapsulation efficiency. In addition, a cytotoxicity study, competition assay and an evaluation of antimycobacterial activity against macrophages infected with M. tuberculosis (H37Ra) were performed. When the amount of fucoidan was increased (from 5 to 20 mg), vesicle size increased (from 168 ± 2.82 nm to 1.18 ± 0.01 μm). Changes in from +20 ± 0.41 mV for uncoated liposomes to −5.41 ± 0.23 mV for UA-LipoFuc suggested that the fucoidan was placed on the surface of the liposomes. UA-LipoFuc exhibited a lower IC50 (8.26 ± 1.11 μM) than uncoated liposomes (18.37 ± 3.34 μM), probably due to its higher uptake. UA-LipoFuc5 was internalized through the C-type carbohydrate recognition domain of the cell membrane. Finally, usnic acid, both in its free form and encapsulated in fucoidan-coated liposomes (UA-LipoFuc5), was effective against infected macrophages. Hence, this preliminary investigation suggests that encapsulated usnic acid will aid in further studies related to infected macrophages and may be a potential option for tuberculosis treatment.