Antimycobacterial And Cytotoxicity Activities Of Free And Liposome-encapsulated 3-(4'-bromo[1,1'-biphenyl-4-yl)-3-(4-bromo-phenyl)-n,n- Dimethyl-2-propen-1-amine

The antimycobacterial activity of 3-(4'-bromo[1,1'-biphenyl-4-yl)-3-(4- bromo-phenyl)-N,N-dimethyl-2-propen-1-amine (BBAP), free or incorporated in preformed liposomes, on extracellular M. tuberculosis H37Rv was 8 and 25 μM (MIC), respectively. Extracellular antimycobacterial activity was not significantly improved by entrapment of BBAP in liposomes, but there was a 6.1-fold reduction of BBAP cytotoxicity on J774 macrophages. Liposomal BBAP or its free form showed IC50 values of 165 and 27 μM, resulting in a selectivity index (SI=IC50/MIC) of 3.4 and 6.6, respectively. Free BBAP in concentrations from 10 to 80 μM were quite effective in eliminating intracellular M. tuberculosis while liposomal formulation was less effective at these concentrations.334871874Corbett, E.L., Watt, C.J., Walker, N., Mayer, D.B.M., Willians, B.G., Raviglione, M.C., Dye, C., (2003) Arch. Intern. Med., 163, p. 1009Vynnycky, E., Fine, P.E., (1997) Epidemiol. Infec., 119, p. 183Pandey, R., Khuller, G.K., (2005) J. Antimicrob. Chemother., 55, p. 430De Souza, A.O., Aily D., C.G., Sato, D.N., Durán, N., (1998) J. Antimicrob. Chemother., 42, p. 407De Souza, A.O., Junior, R.R.S., Ferreira-Julio, J.F., Rodriguez, J.A., Melo, P.S., Haun, M., Sato, D.N., Durán, N., (2001) Eur. J. Med. Chem., 36, p. 843De Souza, A.O., Pereira, D.G., Durán, N., (2002) Ann. Rev. Biomed. Sci., 4, p. 53De Souza, A.O., Hemerly, F.P., Busollo, A.C., Melo, P.S., Machado, G.M.C., Miranda, C.C., Santa-Rita, R.M., Durán, N., (2002) J. Antimicrob. Chemother., 50, p. 629De Souza, A.O., Santos, R.R., Sato, D.N., De Azevedo, M.M.M., Ferreira, D.A., Melo, P.S., Haun, M., Durán, N., (2004) J. Braz. Chem. Soc., 15, p. 682De Souza, A.O., Alderete, J.B., Faljoni-Alario, A., Silva, C.L., Durán, N., (2005) J. Chil. Chem. Soc., 50, p. 591De Conti, R., Gimenez, S.M.M., Haun, M., Pilli, R.A., De Castro, S.L., Durán, N., (1996) Eur. J. Med. Chem., 31, p. 915Bangham, A.D., Standish, M.M., Watkins, J.C., (1965) J. Mol. Biol., 13, p. 238Chen, P.S., Toribara, T.Y., Warner, H., (1956) Anal. Chem., 28, p. 1756Oh, Y.K., Nix, D.E., Straubinger, R.M., (1995) Antimicrob. Agents Chemother., 39, p. 2104Collins, L.A., Franzblau, S.G., (1997) Antimicrob. Agents Chemother., 41, p. 1004Denizot, F., Lang, R., (1986) J. Immun. Methods, 89, p. 27

Free 2-propen-1-amine Derivative And Inclusion Complexes With β-cyclodextrin: Scanning Electron Microscopy, Dissolution, Cytotoxicity And Antimycobacterial Activity

Inclusion complexes and physical mixtures of isomeric mixture of E/Z (50:50) of 3-(4′-bromo-[1,1′-biphenyl]-4-yl)-3-(4-bromophenyl)-N,N- dimethyl-2-propen-1-amine (BBAP) and β-cyclodextrin (β-CD) in the molar proportion of 1:1 and 1:2 were analyzed by scanning electron microscopy. The dissolution behavior of BBAP and of the inclusion complexes were also evaluated for six hours. By scanning electron microscopy (SEM), it was possible to observe an inclusion complex formed between BBAP and β-CD by co-evaporation, either in the molar proportion of 1:1 or 1:2. In the physical mixtures, no complex was observed as previously detected by physicochemical analysis. The dissolution studies showed that the inclusion complexes BBAP/β-CD 1:1 and 1:2 released respectively 49.07 ± 1.48 and 40.26 ± 3.90% of BBAP during six hours. Free BBAP was less soluble than the inclusion complex and reached 9.00 ± 0.75% of dissolution. Biological assays, such as cytotoxicity to J774 macrophages and to a permanent lung fibroblast cell line (V79), indicated that the BBAP does not exhibit any additional toxic effect with the β-CD complexes. However, the complexes were less cytotoxic to V79 cells than the free form. The BBAP/β-CD inclusion complexes were more effective (MIC) than the free compound on several mycobacteria strains. Similar behavior was observed for BBAP/β-CD complexes and rifampicin, a front-line antitubercular drug, on M. tuberculosis H37Rv growing inside J774 macrophages.155682689Bibby, D.C., Davies, N.M., Tucker, I.G., (2000) Int. J. Pharm., 197, p. 1De Souza, A.O., Sato, D.N., Aily, D.C.G., Durán, N., (1998) J. Antimicrob. Chemother., 42, p. 407Pereira, D.G., De Castro, S.L., Durán, N., (1998) Acta Tropica, 69, p. 205De Souza, A.O., Santos Júnior, R.R., Ferreira-Júlio, J.F., Rodrigues, J.A., Melo, P.S., Haun, M., Sato, D.N., Durán, N., (2001) Eur. J. Med. Chem., 36, p. 843De Souza, A.O., Hemerly, F.P., Busollo, A.C., Melo, P.S., Machado, G.M.C., Miranda, C.C., Santa-Rita, R.M., Durán, N., (2002) J. Antimicrob. Chemother., 50, p. 629De Conti, R., Gimenez, S.M.N., Haun, M., Pilli, R.A., De Castro, S.L., Durán, N., (1996) Eur. J. Med. Chem., 31, p. 915De Souza, A.O., Santos Jr., R.R., Sato, D.N., Lima, H.O.S., Andrade-Santana, M.H., Alderete, J.B., Faljoni-Alario, A., Durán, N., (2000) Abstracts of the 29 a Reunião Anual Da Sociedade Brasileira de Bioquímica, , Caxambu, BrazilHiguchi, T., Connors, K.A., (1965) Adv. Anal. Chem. Instrum., 4, p. 117Collins, L.A., Franzblau, S.G., (1997) Antimicrob. Agents Chemother., 41, p. 1004Oh, Y.K., Nix, D.E., Straubinger, R.M., (1995) Antimicrob Agents Chemother., 39, p. 2104Cingi, M.R., De Angelis, I., Fortunati, E., Reggiani, D., Bianchi, V., Tiozzo, R., Zucco, F., (1991) Toxicol. In Vitro, 5, p. 119Denizot, F., Lang, R., (1986) J. Immun. Methods, 89, p. 271Borenfreund, E., Puerner, J.A., (1984) J. Tiss. Cult. Meth., 9, p. 7Melo, P.S., Maria, S.S., Vidal, B.C., Haun, M., Durán, N., (2000) In Vitro Cell Rev. Biol. Animal, 36, p. 539Melo, P.S., Durán, N., Haun, M., (2001) Toxicology, 159, p. 135Shrivastava, R., John, G.W., Rispat, G., Chevalier, A., Massingham, R., (1991) ATLA - Alt. Lab. Anim., 19, p. 39

Erratum To: Quality Of Sweat Test (st) Based On The Proportion Of Sweat Sodium (na) And Sweat Chloride (cl) As Diagnostic Parameter Of Cystic Fibrosis: Are We On The Right Way?

During production of the original article [1] the Methods section included an incorrect sentence. The following sentence "For the analysis of variables with numerical distribution, Fisher's exact test and one-way analysis of variance were used" should be corrected as "For the analysis of variables with numerical distribution, Student's t-test and one-way analysis of variance were used". © The Author(s).12

SU(1,1) Coherent States For Position-Dependent Mass Singular Oscillators

The Schroedinger equation for position-dependent mass singular oscillators is solved by means of the factorization method and point transformations. These systems share their spectrum with the conventional singular oscillator. Ladder operators are constructed to close the su(1,1) Lie algebra and the involved point transformations are shown to preserve the structure of the Barut-Girardello and Perelomov coherent states.Comment: 11 pages, 5 figures. This shortened version (includes new references) has been adapted for its publication in International Journal of Theoretical Physic

Characteristcs chemical and soil salinization in the Irrigated District of California, SE, Brazil

O manejo inadequado da irrigação pode resultar no acúmulo de sais no solo, cuja intensidade depende da qualidade da água utilizada na irrigação, da fração de lixiviação adotada e da demanda evapotranspirativa da região. O presente trabalho teve como objetivo avaliar os atributos físicos e químicos dos solos do perímetro irrigado Califórnia, localizado no extremo noroeste do Estado de Sergipe. Para tal, foram realizadas amostragens em 42 lotes, correspondendo a 16,4% dos lotes deste perímetro. As maiores concentrações de sais e de sódio ocorreram na camada superficial (0–0,2m) do solo, o que evidenciou a falta de um manejo da irrigação adequado visando ao controle da salinidade. O aumento do pH do solo foi correlacionado significativamente com a porcentagem de sódio trocável, atingindo valores acima de 9,5. Correlações positivas significativas foram observadas entre a condutividade elétrica e os teores de Ca e Mg, indicando que sais desses íons podem estar se acumulando no solo pela ascensão do lençol freático, associado à ausência de lixiviação e drenagem. _________________________________________________________________________________________ ABSTRACT: The improper irrigation management may result in the accumulation of salts in the soil profile, which intensity depends on the irrigation water quality, the leaching fraction adopted and on the evapotranspiration demand of the region. The objective of the present study was to study the physical and chemical characteristics of the soils in the irrigated district of California, located in the northwest of the State of Sergipe. Thus, soil sampling were made in 54 lots, corresponding to 16.4% of the lots of this district. The highest salt and sodium concentrations occurred in the shallowest soil layer (0–0.2m), evidencing the lack of an appropriate irrigation management in order to control the salinity build up. The increasing of the soil pH was significantly correlated to the exchangeable sodium percentage, reaching values over 9.5. Significant positive correlations were observed between the electrical conductivity and the Ca and Mg content, indicating that salts of both ions could be accumulating in soil by the capillary rise of the water table, associated to the lack of leaching and drainage

EFFECT OF CHARCOAL -ENRICHED SUBSTRATE ON SEEDLINGS OF RHIZOBIUM-INOCULATED LEGUME TREES

ABSTRACT Native legume trees are planted in agroforestry systems for their hardiness and symbiosis with soil bacteria of the genus rhizobium, efficient in N2 fixation. The enrichment of the substrate composition with fine charcoal for seedling production of these trees is interesting for increasing soil porosity, water retention and the proliferation of beneficial microorganisms. Experiments were carried out to analyze the effect of substrate enrichment with charcoal on the quality of Clitoria fairchildiana, Enterolobium schomburgkii and Inga edulis seedlings. The treatments consisted of a 3:2:0.5 (v:v) mixture of clay soil, sand and bovine manure and a 3:2 (v:v) mixture of clay soil and sand combined with charcoal rates of 0, 10, 19 and 29%. After mixing the components, substrate samples were collected and chemically analyzed. The experiment was arranged in a completely randomized design with 5 treatments and 10 replications. The seedlings were inoculated with homologues rhizobia and growth controlled monthly. The plants were collected to determine the number of nodules and dry biomass of roots, shoots and nodules. Seedling growth was similar on substrates containing charcoal or manure, except for E. schomburkii, which increased by more than 100% on the charcoal-containing substrates. The number and dry biomass of nodules in the charcoal-containing substrates was up to 100% and 300% higher than in the manure-containing treatment, respectively. The results indicated that the substitution of manure by charcoal favors the seedling quality of the studied species