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Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes. / Martins, Ligia F.; Mesquita, Juliana T.; Pinto, Erika G. et al.
In: Journal of natural products, Vol. 79, No. 9, 16.09.2016, p. 2202-2210.

Research output: Contribution to journalArticlepeer-review

HarvardHarvard

Martins, LF, Mesquita, JT, Pinto, EG, Costa-Silva, TA, Borborema, SET, Galisteo Junior, AJ, Neves, BJ, Andrade, CH, Bennett, E, Black, G, Harper, P, Evans, D, Fituri, H, Leyland, JP, Martin, C, Roberts, T, Thornhill, AJ, Vale, S, Howard-Jones, A, Thomas, D, Williams, HL, Overman, L, Berlinck, R, Murphy, P & Tempone, A 2016, 'Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes', Journal of natural products, vol. 79, no. 9, pp. 2202-2210. https://doi.org/10.1021/acs.jnatprod.6b00256

APA

Martins, L. F., Mesquita, J. T., Pinto, E. G., Costa-Silva, T. A., Borborema, S. E. T., Galisteo Junior, A. J., Neves, B. J., Andrade, C. H., Bennett, E., Black, G., Harper, P., Evans, D., Fituri, H., Leyland, J. P., Martin, C., Roberts, T., Thornhill, A. J., Vale, S., Howard-Jones, A., ... Tempone, A. (2016). Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes. Journal of natural products, 79(9), 2202-2210. https://doi.org/10.1021/acs.jnatprod.6b00256

CBE

Martins LF, Mesquita JT, Pinto EG, Costa-Silva TA, Borborema SET, Galisteo Junior AJ, Neves BJ, Andrade CH, Bennett E, Black G, et al. 2016. Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes. Journal of natural products. 79(9):2202-2210. https://doi.org/10.1021/acs.jnatprod.6b00256

MLA

VancouverVancouver

Martins LF, Mesquita JT, Pinto EG, Costa-Silva TA, Borborema SET, Galisteo Junior AJ et al. Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes. Journal of natural products. 2016 Sept 16;79(9):2202-2210. Epub 2016 Sept 2. doi: 10.1021/acs.jnatprod.6b00256

Author

Martins, Ligia F. ; Mesquita, Juliana T. ; Pinto, Erika G. et al. / Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes. In: Journal of natural products. 2016 ; Vol. 79, No. 9. pp. 2202-2210.

RIS

TY - JOUR

T1 - Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes

AU - Martins, Ligia F.

AU - Mesquita, Juliana T.

AU - Pinto, Erika G.

AU - Costa-Silva, Thais A.

AU - Borborema, Samantha E. T.

AU - Galisteo Junior, Andres J.

AU - Neves, Bruno J.

AU - Andrade, Carolina H.

AU - Bennett, Elliot

AU - Black, Gregory

AU - Harper, Philip

AU - Evans, Daniel

AU - Fituri, Hisham

AU - Leyland, John P.

AU - Martin, Claire

AU - Roberts, Terence

AU - Thornhill, Andrew J.

AU - Vale, Steven

AU - Howard-Jones, Andrew

AU - Thomas, Dafydd

AU - Williams, Harri L.

AU - Overman, Larry

AU - Berlinck, Roberto

AU - Murphy, Patrick

AU - Tempone, Andre

PY - 2016/9/16

Y1 - 2016/9/16

N2 - ABSTRACT: Synthetic analogues of marine sponge guanidinealkaloids showed in vitro antiparasitic activity againstLeishmania (L.) infantum and Trypanosoma cruzi. Guanidines10 and 11 presented the highest selectivity index when testedagainst Leishmania. The antiparasitic activity of 10 and 11 wasinvestigated in host cells and in parasites. Both compoundsinduced depolarization of mitochondrial membrane potential,upregulation of reactive oxygen species levels, and increasedplasma membrane permeability in Leishmania parasites.Immunomodulatory assays suggested an NO-independenteffect of guanidines 10 and 11 on macrophages. The samecompounds also promoted anti-inflammatory activity in L. (L.)infantum-infected macrophages cocultived with splenocytes,reducing the production of cytokines MCP-1 and IFN-γ.Guanidines 10 and 11 affect the bioenergetic metabolism of Leishmania, with selective elimination of parasites via a hostindependentmechanism.

AB - ABSTRACT: Synthetic analogues of marine sponge guanidinealkaloids showed in vitro antiparasitic activity againstLeishmania (L.) infantum and Trypanosoma cruzi. Guanidines10 and 11 presented the highest selectivity index when testedagainst Leishmania. The antiparasitic activity of 10 and 11 wasinvestigated in host cells and in parasites. Both compoundsinduced depolarization of mitochondrial membrane potential,upregulation of reactive oxygen species levels, and increasedplasma membrane permeability in Leishmania parasites.Immunomodulatory assays suggested an NO-independenteffect of guanidines 10 and 11 on macrophages. The samecompounds also promoted anti-inflammatory activity in L. (L.)infantum-infected macrophages cocultived with splenocytes,reducing the production of cytokines MCP-1 and IFN-γ.Guanidines 10 and 11 affect the bioenergetic metabolism of Leishmania, with selective elimination of parasites via a hostindependentmechanism.

U2 - 10.1021/acs.jnatprod.6b00256

DO - 10.1021/acs.jnatprod.6b00256

M3 - Article

VL - 79

SP - 2202

EP - 2210

JO - Journal of natural products

JF - Journal of natural products

SN - 0163-3864

IS - 9

ER -