10 research outputs found

    Synthesis, in vitro antiproliferative and anti-mycobacterium tuberculosis activities of novel β-carboline derivatives

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    A series of β-carboline derivatives with amino or guanidinium were synthesized and evaluated in vitro against anti-Mycobacterium tuberculosis and for antiproliferative activities against nine human cancer cell lines. The compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline (24.9 μg mL-1) and 1-(4-methoxyphenyl)-3-carboxamide(ethylamine) β-carboline (26.9 μg mL-1) were the most active against M. Tuberculosis (MTB). Compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline and 1-(4-methoxyphenyl)-3-carboxamide(propylamine) β-carboline, which had the same substituted groups, inhibited the growth of all human tumor cell lines with growth inhibitory activity (GI50) values from 1.37 to 9.20 mmol L-1. Also in this series, compounds 1-(4-hydroxyphenyl)-3-carboxamide(propylamine) β-carboline and 1-(3-nitrophenyl)-3-carboxamide(propylamine) β-carboline demonstrated significant activity against NCI/ADR cells. Among compounds with a terminal guanidine group, compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethyl)guanidine β-carboline (27.8 μg mL-1) and 1-(3-nitrophenyl)-3-carboxamide(ethyl) guanidine β-carboline (37.4 μg mL-1) demonstrated the greatest activity against MTB. Additionally, compounds 1-(4-methoxyphenyl)-3-carboxamide(ethyl)guanidine β-carboline (GI50 = 0.45 mmol L-1) effectively inhibited growth and was highly selective against NCI/ADR. The in silico study revealed that 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline, 1-(4-methoxyphenyl)-3-carboxamide(ethylamine) β-carboline, 1-(4-hydroxyphenyl)-3-carboxamide(propylamine) β-carboline, 1-(4-methoxyphenyl)-3-carboxamide(propylamine) β-carboline and 1-(3-nitrophenyl)-3-carboxamide(propylamine) β-carboline compounds follow the rules established by Lipinski, suggesting that this compound has no problems with oral bioavailability.27813981405CONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQCOORDENAÇÃO DE APERFEIÇOAMENTO DE PESSOAL DE NÍVEL SUPERIOR - CAPESSem informaçãoSem informaçã

    Synthesis, In Vitro Antiproliferative And Anti-mycobacterium Tuberculosis Activities Of Novel β-carboline Derivatives

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    Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)A series of β-carboline derivatives with amino or guanidinium were synthesized and evaluated in vitro against anti-Mycobacterium tuberculosis and for antiproliferative activities against nine human cancer cell lines. The compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline (24.9 μg mL-1) and 1-(4-methoxyphenyl)-3-carboxamide(ethylamine) β-carboline (26.9 μg mL-1) were the most active against M. Tuberculosis (MTB). Compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline and 1-(4-methoxyphenyl)-3-carboxamide(propylamine) β-carboline, which had the same substituted groups, inhibited the growth of all human tumor cell lines with growth inhibitory activity (GI50) values from 1.37 to 9.20 mmol L-1. Also in this series, compounds 1-(4-hydroxyphenyl)-3-carboxamide(propylamine) β-carboline and 1-(3-nitrophenyl)-3-carboxamide(propylamine) β-carboline demonstrated significant activity against NCI/ADR cells. Among compounds with a terminal guanidine group, compounds 1-(4-hydroxyphenyl)-3-carboxamide(ethyl)guanidine β-carboline (27.8 μg mL-1) and 1-(3-nitrophenyl)-3-carboxamide(ethyl) guanidine β-carboline (37.4 μg mL-1) demonstrated the greatest activity against MTB. Additionally, compounds 1-(4-methoxyphenyl)-3-carboxamide(ethyl)guanidine β-carboline (GI50 = 0.45 mmol L-1) effectively inhibited growth and was highly selective against NCI/ADR. The in silico study revealed that 1-(4-hydroxyphenyl)-3-carboxamide(ethylamine) β-carboline, 1-(4-methoxyphenyl)-3-carboxamide(ethylamine) β-carboline, 1-(4-hydroxyphenyl)-3-carboxamide(propylamine) β-carboline, 1-(4-methoxyphenyl)-3-carboxamide(propylamine) β-carboline and 1-(3-nitrophenyl)-3-carboxamide(propylamine) β-carboline compounds follow the rules established by Lipinski, suggesting that this compound has no problems with oral bioavailability. © 2016 Sociedade Brasileira de Química.27813981405CAPES, Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorCNPq, Conselho Nacional de Desenvolvimento Científico e TecnológicoCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq

    Synthesis And Evaluation Of New β-carboline-3-(4-benzylidene)- 4h-oxazol-5-one Derivatives As Antitumor Agents

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    In the present work, we report the synthesis and in vitro anticancer and antimicrobial activity evaluation of a new series of 1-substituted-β- carboline derivatives bearing a 4-benzylidene-4H-oxazol-5-one unity at C-3. The compound 2-[1-(4- methoxyphenyl)-9H-β-carbolin-3-yl]-4-(benzylidene)-4H- oxazol-5-one (11) was the most active derivative, exhibiting a potent cytotoxic activity against glioma (U251), prostate (PC-3) and ovarian (OVCAR-03) cancer cell lines with IC 50 values of 0.48, 1.50 and 1.07 μM, respectively. An in silico study of the ADME properties of the novel synthesized β-carboline derivatives was also performed. © 2012 by the Authors.17561006113Cao, R., Peng, W., Wang, Z., Xu, A., B-carboline alkaloids: Biochemical and pharmacological functions (2007) Curr. Med. 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Chem., 46, pp. 5127-5137Zhang, X., Yang, Y., Zhao, M., Liu, L., Zheng, M., Wang, Y., Wu, J., Peng, S., A class of trp-trp-aa-obzl: Synthesis, in vitro anti-proliferation/in vivo anti-tumor evaluation, intercalationmechanism investigation and 3d qsar analysis (2011) Eur. J. Med. Chem., 46, pp. 3410-3419Chen, Z., Cao, R., Shi, B., Yi, W., Yu, L., Song, H., Ren, Z., Synthesis and biological evaluation of novel b-carbolines as potent cytotoxic and dna intercalating agents (2010) Chem. Pharm. Bull., 58, pp. 901-907Ma, C., Cao, R., Shi, B., Zhou, X., Ma, Q., Sun, J., Guo, L., Song, H., Synthesis and cytotoxic evaluation of 1-carboxamide and 1-amino side chain substituted b-carbolines (2010) Eur. J. Med. Chem., 45, pp. 5513-5519Chen, Z., Cao, R., Yu, L., Shi, B., Sun, J., Guo, L., Ma, Q., Song, H., Synthesis, cytotoxic activities and dna binding properties of b-carboline derivatives (2010) Eur. J. Med. Chem., 45, pp. 4740-4745Cao, R., Guan, X., Shi, B., Chen, Z., Ren, Z., Peng, W., Song, H., Design synthesis and 3d-qsar of b-carboline derivatives as potent antitumor agents (2010) Eur. J. Med. Chem., 45, pp. 2503-2515Wu, J., Li, C., Zhao, M., Wang, W., Wang, Y., Peng, S., A class of novel carboline intercalators: Their synthesis, in vitro anti-proliferation, in vivo anti-tumor action, and 3d qsar analysis (2010) Bioorg. Med. Chem., 18, pp. 6220-6229Formagio, A.S.N., Tonin, L.T.D., Foglio, M.A., Madjarof, C., De Carvalho, J.E., Da Costa, W.F., Cardoso, F.P., Sarragiotto, M.H., Synthesis and antitumoral activity of novel 3-(2-substituted- 1,3,4-oxadiazol-5-yl) and 3-(5-substituted-1,2,4-triazol-3-yl) b-carboline derivatives (2008) Bioorg. Med. Chem., 16, pp. 9660-9667Savariz, F.C., Formagio, A.S.N., Barbosa, V.A., Foglio, M.A., De Carvalho, J.E., Duarte, M.C.T., Filho, B.P.D., Sarragiotto, M.H., Synthesis, antitumor and antimicrobial activity of novel 1-substituted phenyl-3-[3-alkylamino(methyl)-2-thioxo-1,3,4-oxadiazol-5-yl] b-carboline derivatives (2010) J. Braz. Chem. Soc., 21, pp. 288-298Barbosa, V.A., Formagio, A.S.N., Savariz, F.C., Foglio, M.A., Spindola, H.M., De Carvalho, J.E., Meyer, E., Sarragiotto, M.H., Synthesis and antitumor activity of b-carboline 3- (substitutedcarbohydrazide) derivatives (2011) Bioorg. Med. Chem., 19, pp. 6400-6408Wu, S., Fu, Y., Yan, R., Wu, Y., Lei, X., Ye, S., Synthesis of neamine-carboline conjugates for rna binding and their antibacterial activities (2010) Tetrahedron, 66, pp. 3433-3440Schupp, P., Poehner, T., Edrada, R., Ebel, R., Berg, A., Wray, V., Proksch, P., Eudistomins w and x, two new b-carbolines from the micronesian tunicate eudistoma sp (2003) J. Nat. 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    Synthesis And Antitumoral Activity Of Novel 3-(2-substituted-1,3,4-oxadiazol-5-yl) And 3-(5-substituted-1,2,4-triazol-3-yl) β-carboline Derivatives

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    Several novel 1-substituted-phenyl β-carbolines bearing the 2-substituted-1,3,4-oxadiazol-5-yl and 5-substituted-1,2,4-triazol-3-yl groups at C-3 were synthesized and evaluated for their in vitro anticancer activity. The assay results pointed thirteen compounds with growth inhibition effect (GI 50 < 100 μM) for all eight different types of human cancer cell lines tested. The β-carbolines 7a and 7h, bearing the 3-(2-metylthio-1,3,4-oxadiazol-5-yl) group, displayed high selectivity and potent anticancer activity against ovarian cell line with GI 50 values lying in the nanomolar concentration range (GI 50 = 10 nM for both compounds). The 1-(N,N-dimethylaminophenyl)-3-(5-thioxo-1,2,4-triazol-3-yl) β-carboline (8g) was the most active compound, showing particular effectiveness on lung (GI 50 = 0.06 μM), ovarian and renal cell lines. The potent anticancer activity presented for synthesized compounds 7a, 7h, and 8g, together with their easiness of synthesis, makes these compounds promising anticancer agents. © 2008 Elsevier Ltd. All rights reserved.162296609667Tonin, L.T.D., Barbosa, V.A., Bocca, C.C., Ramos, E.R.F., Nakamura, C.V., Costa, W.F., daBasso, E.A., Sarragiotto, M.H., (2008) Eur. J. Med. Chem, , 10.1016/j.ejmech.2008.03.044Wang, Y.-H., Tang, J.-G., Wang, R.-R., Yang, L.-M., Dong, Z.-J., Du, L., Shen, X., Zheng, Y.-T., (2007) Biochem. Biophys. Res. Commun., 355, p. 1091Gupta, L., Srivastava, K., Singh, S., Puri, S.K., Chauhan, P.M.S., (2008) Bioorg. Med. Chem. Lett., 18, p. 3306Kumar, A., Katiyar, S.B., Gupta, S., Chauhan, P.M.S., (2006) Eur. J. Med. Chem., 41, p. 106Rivas, P., Cassels, B.K., Morello, A., Repetto, Y., (1999) Comp. Biochem. Physiol. C, 122, p. 27Zheng, L., Chen, H., Han, X., Lin, W., Yan, X., (2005) World J. Microbiol. Biotechnol., 21, p. 201Guan, H., Chen, H., Peng, W., Ma, Y., Cao, R., Liu, X., Xu, A., (2006) Eur. J. Med. Chem., 41, p. 1167Wu, Q., Cao, R., Feng, M., Guan, X., Ma, C., Liu, J., Song, H., Peng, W., (2008) Eur. J. Med. Chem., , 10.1016/j.ejmech.2008.03.030Shen, Y.-C., Chen, C.-Y., Hsieh, P.-W., Duh, C.-y., Lin, Y.-M., Ko, C.-L., (2005) Chem. Pharm. Bull., 53, p. 32Cao, R., Peng, W., Chen, H., Hou, X., Guan, H., Chen, Q., Ma, Y., Xu, A., (2005) Eur. J. Med. Chem., 40, p. 249Ishida, J., Wang, H.-K., Bastow, K.F., Hu, C.-Q., Lee, K.-H., (1999) Bioorg. Med. Chem. Lett., 9, p. 3319Cao, R., Chen, H., Ma, Y., Hou, X., Guan, H., Liu, X., Xu, A., (2005) Eur. J. Med. Chem., 40, p. 991Cao, R., Chen, Q., Hou, X., Chen, H., Guan, H., Ma, Y., Peng, W., Xu, A., (2004) Bioorg. Med. Chem., 12, p. 4613Zhao, M., Bi, L., Wang, W., Wang, C., Baudy-Floc'h, M., Ju, J., Peng, S., (2006) Bioorg. Med. Chem., 14, p. 6998Cao, R., Peng, W., Chen, H., Ma, Y., Liu, X., Hou, X., Guan, H., Xu, A., (2005) Biochem. Biophys. Res. Commun., 338, p. 1557Boursereau, Y., Coldham, I., (2004) Bioorg. Med. Chem. Lett., 14, p. 5841Xiao, S., Lin, W., Wang, C., Yang, M., (2001) Bioorg. Med. Chem. Lett., 11, p. 437Deveau, A.M., Labroli, M.A., Dieckhaus, C.M., Barthen, M.T., Smith, K.S., Macdonald, T.L., (2001) Bioorg. Med. Chem. Lett., 11, p. 1251Song, Y., Kesuma, D., Wang, J., Deng, Y., Duan, J., Wang, J.H., Qi, R.Z., (2004) Biochem. Biophys. Res. Commun., 317, p. 128Song, Y., Wang, J., Teng, S.F., Kesuma, D., Deng, Y., Duan, J., Wang, J.H., Sim, M.M., (2002) Bioorg. Med. Chem. Lett., 12, p. 1129Castro, A.C., Dang, L.C., Soucy, F., Grenier, L., Mazdiyasni, H., Hottelet, M., Parent, L., Adams, J., (2003) Bioorg. Med. Chem. Lett., 13, p. 2419Holla, B.S., Poojary, K.N., Rao, B.S., Shivananda, M.K., (2002) Eur. J. Med. Chem., 37, p. 511Al-Soud, Y.A., Al-Masoudi, N.A., Ferwanah, A.E.-R.S., (2003) Bioorg. Med. Chem., 11, p. 1701Demirbas, N., Karaoglu, S.A., Demirbas, A., Sancak, K., (2004) Eur. J. Med. Chem., 39, p. 793Aboraia, A.S., Abdel-Rahman, H.M., Mahfouz, N.M., EL-Gendy, M.A., (2006) Bioorg. Med. Chem., 14, p. 1236Tan, T.M.C., Chen, H., Kong, K.H., Bai, J., Li, Y., Lim, S.G., Ang, T.H., Lam, Y., (2006) Antiviral Res., 71, p. 7Amir, M., Shikha, K., (2004) Eur. J. Med. Chem., 39, p. 535Khalil, N.S.A.M., (2006) Carbohydr. Res., 341, p. 2187Wu, J., Liu, X., Cheng, X., Cao, Y., Wang, D., Li, Z., Xu, W., Clercq, E.D., (2007) Molecules, 12, p. 2003Monks, A.D., Skehan, P., Shoemaker, R., Paull, K., Vistica, D., Hose, C., Langley, J., Boyd, M., (1991) J. Natl. Cancer Inst., 83, p. 75

    Polar Constituents Of The Leaves Of Machaonia Brasiliensis (rubiaceae) [constituintes Polares Das Folhas De Machaonia Brasiliensis (rubiaceae)]

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    Chemical investigation of the MeOH extract of the leaves of Machaonia brasiliensis (Rubiaceae) resulted in the isolation and identification of 3β-O-β-glucopyranosyl stigmasterol, 3β-O-β-glucopyranosyl sitosterol, secologanoside, 7-O-β-glucopyranosyl quercetagetin, 4,5-O-dicaffeoylquinic acid and 5-O-caffeoylquinic acid. The structures of these compounds were established by spectroscopic analysis, including 2D NMR experiments. The chemotaxonomic relevance of the isolation of secologanoside is discussed.274525527Corrêa, M.P., (1984) Dicionário de Plantas Úteis Do Brasil e Das Exóticas Cultivadas, 5, p. 522. , Instituto Brasileiro de Desenvolvimento Florestal: Rio de JaneiroMachado, C.A., (1994) Caderno de Farmácia, 10, p. 36Mahato, S.B., Kundu, A.P., (1994) Phytochemistry, 37, p. 1517Matida, A.K., Rossi, M.H., Blumenthal, E.E.A., Schuquel, I.T.A., Malheiros, A., Vidotti, G.J., (1996) Anais Assoc. Bras. Quím., 45, p. 147Calis, I., Sticher, O., (1984) Phytochemistry, 23, p. 2539Nair, A.G.R., Gunasegaran, R., Krishnan, S., Bayet, C., Voirin, B., (1995) Phytochemistry, 40, p. 283D'Agostino, M., De Simone, F., Piacente, S., Pizza, C., Senatore, F., (1997) Phytochemistry, 45, p. 201Tatefuji, T., Izumi, N., Ohta, T., Arai, S., Ikeda, M., Kurimoto, M., (1996) Biol. Pharm. Bull., 19, p. 966Cheminat, A., Zawatsky, R., Becher, H., Brouillard, R., (1988) Phytochemistry, 27, p. 2787Corthout, J., Pieters, L., Claeys, M., Berghe, D.V., Vlietinck, A., (1992) Phytochemistry, 31, p. 1979Inouye, H., Takeda, Y., Nishimura, H., Kanomi, A., Okuda, T., Puff, C., (1988) Phytochemistry, 27, p. 2591Barroso, G.M., (1986) Sistemática de Angiospermas Do Brasil, 3, p. 326. , Imprensa Universitária: Viços

    Synthesis And Antitumor Activity Of β-carboline 3-(substituted- Carbohydrazide) Derivatives

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    A series of β-carboline derivatives bearing a substituted- carbohydrazide moiety at C-3 were synthesized and evaluated for their antitumor activity against eight human cancer cell lines. The b-carboline N-(substituted-benzylidene)carbohydrazides showed, in general, a greater antitumor activity than their N-(alkylidene)carbohydrazide analogues. The N 9-methylation of b-carboline N-(substituted-benzylidene) carbohydrazides resulted in a decrease of antitumor activity. Among compounds tested, the benzylidenecarbohydrazides 3, 4, 11, 13, 16, 21 and 22 were the most active, possessing IC 50 less than 10 μMfor six of the eight tumor cell lines assayed. The derivative 4 displayed the most significant activity toward all tested cell lines, with a remarkable cytotoxicity against renal (786-0) cell lines (IC 50 = 0.04 lM). Compound 4 was assayed for its in vivo antineoplastic activity in the Ehrlich solid carcinoma assay. © 2011 Elsevier Ltd. 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    Synthesis, Antitumor, Antitrypanosomal And Antileishmanial Activities Of Benzo[4,5]canthin-6-ones Bearing The N′-(substituted Benzylidene)- Carbohydrazide And N-alkylcarboxamide Groups At C-2

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    A series of novel benzo[4,5]canthin-6-ones, bearing the N′-(substituted benzylidene)-carbohydrazide (11a-e) and N-alkylcarboxamide (13a-g) moieties at position-2, were synthesized and screened for their in vitro antitumor activity, against seven human cancer cell lines, and for antitrypanosomal and antileishmanial activities against Trypanosoma cruzi and Leishmania amazonensis. The results indicated that N-methylpiperazyl- 6-oxobenzo[4,5]canthine-2-carboxamide (13f) displayed potent antitumor activity with IC50 values in the range of 1.15-8.46 μM for all cell lines tested. Compounds 13f and 13g bearing an N-methylpiperazylcarboxamide and N-morpholylcarboxamide at C-2, respectively, showed potent activities towards both Trypanosoma cruzi and Leishmania amazonensis parasites, with IC 50 in the range of 0.4 to 16.70 μM. © 2012 The Pharmaceutical Society of Japan.601113721379De Souza Almeida, E.S., Filho, V.C., Niero, R., Clasen, B.K., Balogun, S.O., De Oliveira Martins, D.T., (2011) J. Ethnopharmacol., 134, pp. 630-636Jiao, W.H., Gao, H., Zhao, F., Lin, H.W., Pan, Y.M., Zhou, G.X., Yao, X.S., (2011) Chem. Pharm. Bull., 59, pp. 359-364Hsieh, P.W., Chang, F.R., Lee, K.H., Hwang, T.L., Chang, S.M., Wu, Y.C., (2004) J. Nat. Prod., 67, pp. 1175-1177Ferreira, M.E., Cebrián-Torrejón, G., Corrales, A.S., Vera De Bilbao, N., Rolón, M., Gomez, C.V., Leblanc, K., Fournet, A., (2011) J. Ethnopharmacol., 133, pp. 986-993Ferreira, M.E., Rojas De Arias, A., Torres De Ortiz, S., Inchausti, A., Nakayama, H., Thouvenel, C., Hocquemiller, R., Fournet, A., (2002) J. Ethnopharmacol., 80, pp. 199-202Soriano-Agatón, F., Lagoutte, D., Poupon, E., Roblot, F., Fournet, A., Gantier, J.C., Hocquemiller, R., (2005) J. Nat. Prod., 68, pp. 1581-1587Fournet, A.R.F., Lagoutte, D., Poupon, E., Soriano-Agaton, F., (2007), Pat. WO2007110500-A1, FR2899229-A1, EP1998770-A1, WO2007110500-A8, CN101448499-A, IN200808917-P1, EP1998770-B1, DE602007005992-EAmmirante, M., Di Giacomo, R., De Martino, L., Rosati, A., Festa, M., Gentilella, A., Pascale, M.C., De Feo, V., (2006) Cancer Res., 66, pp. 4385-4393Kuo, P.C., Shi, L.S., Damu, A.G., Su, C.R., Huang, C.H., Ke, C.H., Wu, J.B., Wu, T.S., (2003) J. Nat. Prod., 66, pp. 1324-1327Miyake, K., Tezuka, Y., Awale, S., Li, F., Kadota, S., (2010) Nat. Prod. Commun., 5, pp. 17-22Jiang, M.X., Zhou, Y.J., (2008) J. Asian Nat. Prod. Res., 10, pp. 1009-1012Peduto, A., More, V., De Caprariis, P., Festa, M., Capasso, A., Piacente, S., De Martino, L., Filosa, R., (2011) Mini Rev. Med. Chem., 11, pp. 486-491Barbosa, V.A., Formagio, A.S., Savariz, F.C., Foglio, M.A., Spindola, H.M., De Carvalho, J.E., Meyer, E., Sarragiotto, M.H., (2011) Bioorg. Med. Chem., 19, pp. 6400-6408Tonin, L.T.D., Barbosa, V.A., Bocca, C.C., Ramos, E.R.F., Nakamura, C.V., Da Costa, W.F., Basso, E.A., Sarragiotto, M.H., (2009) Eur. J. Med. Chem., 44, pp. 1745-1750Valdez, R.H., Tonin, L.T.D., Ueda-Nakamura, T., Dias Filho, B.P., Morgado-Diaz, J.A., Sarragiotto, M.H., Nakamura, C.V., (2009) Acta Trop., 110, pp. 7-14Tonin, L.T.D., Panice, M.R., Nakamura, C.V., Rocha, K.J.P., Dos Santos, A.O., Ueda-Nakamura, T., Da Costa, W.F., Sarragiotto, M.H., (2010) Biomed. Pharmacother., 64, pp. 386-389Pedroso, R.B., Tonin, L.T.D., Ueda-Nakamura, T., Dias Filho, B.P., Sarragiotto, M.H., Nakamura, C.V., (2011) Ann. Trop. Med. Parasitol., 105, pp. 549-557Cao, R., Peng, W., Wang, Z., Xu, A., (2007) Curr. Med. Chem., 14, pp. 479-500Gohil, V.M., Brahmbhatt, K.G., Loiseau, P.M., Bhutani, K.K., (2012) Bioorg. Med. Chem. Lett., 22, pp. 3905-3907Rivas, P., Cassels, B.K., Morello, A., Repetto, Y., (1999) Comp. Biochem. Physiol. C Pharmacol. Toxicol. Endocrinol., 122, pp. 27-31Ferreira, M.E., Nakayama, H., De Arias, A.R., Schinini, A., De Bilbao, N.V., Serna, E., Lagoutte, D., Fournet, A., (2007) J. Ethnopharmacol., 109, pp. 258-263Di Giorgio, C., Delmas, F., Ollivier, E., Elias, R., Balansard, G., Timon-David, P., (2004) Exp. Parasitol., 106, pp. 67-74Monks, A., Scudiero, D., Skehan, P., Shoemaker, R., Paull, K., Vistica, D., Hose, C., Boyd, M., (1991) J. Natl. Cancer Inst., 83, pp. 757-76

    Antiprotozoal and molluscicidal activities of five Brazilian plants

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    Leishmaniasis, Chagas' disease and schistosomiasis (bilharzia) are parasitic diseases with wide distribution on the American continent, affecting millions of people. In the present study, biological assays for antiprotozoal and molluscicidal activities were carried out with ethanolic extracts of plant species from the Brazilian part of the Upper Paraná River. Crude extracts were obtained by percolation with absolute ethanol from the leaves of Cayaponia podantha Cogn., Nectandra falcifolia (Nees) Castiglioni and Paullinia elegans Cambess., as well as from the aerial parts of Helicteres gardneriana St. Hil. & Naud. and Melochia arenosa Benth., all belonging to genera used in folk medicine. Trypanocidal activity of plants was assayed on epimastigote cultures in liver infusion tryptose. Anti-leishmanial activity was determined over cultures of promastigote forms of the parasite in Schneider's Drosophila medium. Microscopic countings of parasites, after their incubation in the presence of different concentrations of the crude extracts, were made in order to determine the percentage of growth inhibition. C. podantha and M. arenosa, at a concentration of 10 µg/mL, showed 90.4 ± 11.52 and 88.9 ± 2.20% growth inhibition, respectively, of epimastigote forms of Trypanosoma cruzi, whereas N. falcifolia demonstrated an LD50 of 138.5 µg/mL against promastigote forms of Leishmania (Viannia) braziliensis. Regarding molluscicidal activity, the acute toxicity of the extracts on Biomphalaria glabrata was evaluated by a rapid screening procedure. M. arenosa was 100% lethal to snails at 200 µg/mL and showed an LD50 of 143 µg/mL. Screening of plant extracts represents a continuous effort to find new antiparasitic drugs
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