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      Evaluations of the Antimicrobial Activities and Chemical Compositions of Body Fat from the Amphibians Leptodactylus macrosternum Miranda-Ribeiro (1926) and Leptodactylus vastus Adolf Lutz (1930) in Northeastern Brazil

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          Abstract

          Leptodactylus macrosternum and L. vastus (family: Leptodactylidae) are commonly encountered in the “Caatinga” biome in northern Brazil. The body fat of L. vastus is used as a zootherapeutic for treating a number of human maladies. The aim of this work was to determine the chemical composition of the body fats of L. macrosternum and L. vastus and to evaluate their antimicrobial activities as well as the ecological implications of their use in traditional folk medicine. Oils were extracted from body fat located in the ventral region of L. macrosternum (OLM) and L. vastus (OLV) using hexane as a solvent. The fatty acids were identified by GC-MS. The antimicrobial activities of the oils, either alone or in combination with antibiotics and antifungal drugs, were tested on standard strains of microorganisms as well as on multiresistant strains of Escherichia coli and Staphylococcus. OLM contained 40% saturated and 60% unsaturated fatty acids, while OLV contained 58.33% saturated and 41.67% unsaturated fatty acids. Our results indicated that both OLM and OLV demonstrated relevant antimicrobial activities (with MIC 256  μ g/mL for both) against Pseudomonas aeruginosa and Candida krusei. However, no antimicrobial effects were observed when these oils were combined with antibiotics or antifungal drugs.

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          Most cited references53

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          Magainins, a class of antimicrobial peptides from Xenopus skin: isolation, characterization of two active forms, and partial cDNA sequence of a precursor.

          M. Zasloff (1987)
          A family of peptides with broad-spectrum antimicrobial activity has been isolated from the skin of the African clawed frog Xenopus laevis. It consists of two closely related peptides that are each 23 amino acids and differ by two substitutions. These peptides are water soluble, nonhemolytic at their effective antimicrobial concentrations, and potentially amphiphilic. At low concentrations they inhibit growth of numerous species of bacteria and fungi and induce osmotic lysis of protozoa. The sequence of a partial cDNA of the precursor reveals that both peptides derive from a common larger protein. These peptides appear to represent a previously unrecognized class of vertebrate antimicrobial activities.
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            Fatty acid synthesis is a target for antibacterial activity of unsaturated fatty acids.

            Long-chain unsaturated fatty acids, such as linoleic acid, show antibacterial activity and are the key ingredients of antimicrobial food additives and some antibacterial herbs. However, the precise mechanism for this antimicrobial activity remains unclear. We found that linoleic acid inhibited bacterial enoyl-acyl carrier protein reductase (FabI), an essential component of bacterial fatty acid synthesis, which has served as a promising target for antibacterial drugs. Additional unsaturated fatty acids including palmitoleic acid, oleic acid, linolenic acid, and arachidonic acid also exhibited the inhibition of FabI. However, neither the saturated form (stearic acid) nor the methyl ester of linoleic acid inhibited FabI. These FabI-inhibitory activities of various fatty acids and their derivatives very well correlated with the inhibition of fatty acid biosynthesis using [(14)C] acetate incorporation assay, and importantly, also correlated with antibacterial activity. Furthermore, the supplementation with exogenous fatty acids reversed the antibacterial effect of linoleic acid, which showing that it target fatty acid synthesis. Our data demonstrate for the first time that the antibacterial action of unsaturated fatty acids is mediated by the inhibition of fatty acid synthesis.
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              The impact of natural products upon modern drug discovery.

              A. Ganesan (2008)
              In the period 1970-2006, a total of 24 unique natural products were discovered that led to an approved drug. We analyze these successful leads in terms of drug-like properties, and show that they can be divided into two equal subsets. The first falls in the 'Lipinski universe' and complies with the Rule of Five. The second is a 'parallel universe' that violates the rules. Nevertheless, the latter compounds remain largely compliant in terms of logP and H-bond donors, highlighting the importance of these two metrics in predicting bioavailability. Natural products are often cited as an exception to Lipinski's rules. We believe this is because nature has learned to maintain low hydrophobicity and intermolecular H-bond donating potential when it needs to make biologically active compounds with high molecular weight and large numbers of rotatable bonds. In addition, natural products are more likely than purely synthetic compounds to resemble biosynthetic intermediates or endogenous metabolites, and hence take advantage of active transport mechanisms. Interestingly, the natural product leads in the Lipinski and parallel universe had an identical success rate (50%) in delivering an oral drug.
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                Author and article information

                Journal
                Evid Based Complement Alternat Med
                Evid Based Complement Alternat Med
                ECAM
                Evidence-based Complementary and Alternative Medicine : eCAM
                Hindawi Publishing Corporation
                1741-427X
                1741-4288
                2013
                23 April 2013
                23 April 2013
                : 2013
                : 913671
                Affiliations
                1Laboratory of Zoology, Regional University of Cariri-URCA, Pimenta, 63105-000 Crato, CE, Brazil
                2Laboratory of Microbiology and Molecular Biology, Regional University of Cariri-URCA, Pimenta, 63105-000 Crato, CE, Brazil
                3Laboratory of Natural Products Research, Regional University of Cariri-URCA, Pimenta, 63105-000 Crato, CE, Brazil
                4Laboratory of Phamacology and Medicinal Chemistry, Regional University of Cariri-URCA, Pimenta, 63105-000 Crato, CE, Brazil
                5Department of Biology, Paraiba State University-UEPB, 58429-500 João Pessoa, PB, Brazil
                Author notes
                *Mario Eduardo Santos Cabral: mario.biologo10@ 123456gmail.com

                Academic Editor: Edwin L. Cooper

                Article
                10.1155/2013/913671
                3655571
                23710241
                8ec1baee-10f9-4168-b92a-df867b95aeeb
                Copyright © 2013 Mario Eduardo Santos Cabral et al.

                This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                : 17 January 2013
                : 18 March 2013
                : 4 April 2013
                Categories
                Research Article

                Complementary & Alternative medicine
                Complementary & Alternative medicine

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