Bromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro

Background: Human immunodeficiency virus type 1 (HIV-1) infection and Acquired immunodeficiency syndrome are mayor global public health issues. HIV-1 infection is now manageable as a chronic disease thanks to the development of antiretroviral therapy; however, the existence of HIV drug resistance a...

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Autores principales:	Leon Gabriel GÓMEZ-ARCHILA, Wildeman ZAPATA, Elkin GALEANO, Alejandro MARTÍNEZ, Francisco Javier DÍAZ CASTRILLÓN, María Teresa RUGELES
Formato:	article
Lenguaje:	EN
Publicado:	Universidad de Antioquia 2014
Materias:	HIV-1 marine resoruces antiviral activity bromotyrosine marine sponge Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675
Acceso en línea:	https://doaj.org/article/e34a25bde3134274aa95e0ec91c94a2b
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spelling	oai:doaj.org-article:e34a25bde3134274aa95e0ec91c94a2b2021-11-19T04:10:48ZBromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro0121-40042145-2660https://doaj.org/article/e34a25bde3134274aa95e0ec91c94a2b2014-07-01T00:00:00Zhttps://revistas.udea.edu.co/index.php/vitae/article/view/16797https://doaj.org/toc/0121-4004https://doaj.org/toc/2145-2660 Background: Human immunodeficiency virus type 1 (HIV-1) infection and Acquired immunodeficiency syndrome are mayor global public health issues. HIV-1 infection is now manageable as a chronic disease thanks to the development of antiretroviral therapy; however, the existence of HIV drug resistance and collateral effects have increased the search for therapeutic alternatives. Compounds of marine resources have been studied for their antiviral potential. Objectives: To evaluate the antiviral activity of isolated bromotyrosine-derivative compounds from the Colombian marine sponges, Verongula rigida and Aiolochoria crassa against HIV-1 infection in vitro. Methods: Cytotoxicity of 11 bromotyrosine-derivative compounds was determined by the MTT assay. Inhibition of HIV-1 replication was performed using the U373-MAGI cell line, which was infected with recombinant green fluorescent protein (GFP)-expressing viruses pseudotyped, in the presence or absence of the compounds. The percentage of infected cells was evaluated by flow cytometry. In addition, the inhibition of reverse transcription and nuclear import was determined by quantification of early and late reverse transcription products and 2-LTR circles, respectively, using quantitative PCR. Results: Aeroplysinin-1, purealidin B and 3-bromo-5-hydroxy-Omethyltyrosine inhibited the HIV-1 replication in a dose-dependent manner, with a median maximum percentage of inhibition of 74% (20 μM), 57% (80 μM) and 47% (80 μM), respectively. Importantly, none of these concentrations were cytotoxic. Aeroplysinin-1, 19-deoxyfistularin 3, purealidin B, fistularin 3 and 3-bromo-5-hydroxy-O-methyltyrosine inhibited the nuclear import efficiently; while 3,5-dibromo-N,N,N,O-tetramethyltyraminium, aeroplysinin-1, purealidin B, fistularin 3 and 3-bromo-5-hydroxy-Omethyltyrosine inhibited X4 HIV-1 cell entry with a median maximum percentage of inhibition ranging between 2 to 30%. Conclusions: Aeroplysinin-1, 19-deoxyfistularin 3, purealidin B, fistularin 3 and 3-bromo-5-hydroxy-O-methyltyrosine inhibited HIV replication at different steps. This study opens the possibility of chemically synthesizing these compounds and evaluating them as alternative therapies against HIV-1. Leon Gabriel GÓMEZ-ARCHILAWildeman ZAPATAElkin GALEANOAlejandro MARTÍNEZFrancisco Javier DÍAZ CASTRILLÓNMaría Teresa RUGELESUniversidad de AntioquiaarticleHIV-1marine resorucesantiviral activitybromotyrosinemarine spongeFood processing and manufactureTP368-456Pharmaceutical industryHD9665-9675ENVitae, Vol 21, Iss 2 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	HIV-1 marine resoruces antiviral activity bromotyrosine marine sponge Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675
spellingShingle	HIV-1 marine resoruces antiviral activity bromotyrosine marine sponge Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675 Leon Gabriel GÓMEZ-ARCHILA Wildeman ZAPATA Elkin GALEANO Alejandro MARTÍNEZ Francisco Javier DÍAZ CASTRILLÓN María Teresa RUGELES Bromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro
description	Background: Human immunodeficiency virus type 1 (HIV-1) infection and Acquired immunodeficiency syndrome are mayor global public health issues. HIV-1 infection is now manageable as a chronic disease thanks to the development of antiretroviral therapy; however, the existence of HIV drug resistance and collateral effects have increased the search for therapeutic alternatives. Compounds of marine resources have been studied for their antiviral potential. Objectives: To evaluate the antiviral activity of isolated bromotyrosine-derivative compounds from the Colombian marine sponges, Verongula rigida and Aiolochoria crassa against HIV-1 infection in vitro. Methods: Cytotoxicity of 11 bromotyrosine-derivative compounds was determined by the MTT assay. Inhibition of HIV-1 replication was performed using the U373-MAGI cell line, which was infected with recombinant green fluorescent protein (GFP)-expressing viruses pseudotyped, in the presence or absence of the compounds. The percentage of infected cells was evaluated by flow cytometry. In addition, the inhibition of reverse transcription and nuclear import was determined by quantification of early and late reverse transcription products and 2-LTR circles, respectively, using quantitative PCR. Results: Aeroplysinin-1, purealidin B and 3-bromo-5-hydroxy-Omethyltyrosine inhibited the HIV-1 replication in a dose-dependent manner, with a median maximum percentage of inhibition of 74% (20 μM), 57% (80 μM) and 47% (80 μM), respectively. Importantly, none of these concentrations were cytotoxic. Aeroplysinin-1, 19-deoxyfistularin 3, purealidin B, fistularin 3 and 3-bromo-5-hydroxy-O-methyltyrosine inhibited the nuclear import efficiently; while 3,5-dibromo-N,N,N,O-tetramethyltyraminium, aeroplysinin-1, purealidin B, fistularin 3 and 3-bromo-5-hydroxy-Omethyltyrosine inhibited X4 HIV-1 cell entry with a median maximum percentage of inhibition ranging between 2 to 30%. Conclusions: Aeroplysinin-1, 19-deoxyfistularin 3, purealidin B, fistularin 3 and 3-bromo-5-hydroxy-O-methyltyrosine inhibited HIV replication at different steps. This study opens the possibility of chemically synthesizing these compounds and evaluating them as alternative therapies against HIV-1.
format	article
author	Leon Gabriel GÓMEZ-ARCHILA Wildeman ZAPATA Elkin GALEANO Alejandro MARTÍNEZ Francisco Javier DÍAZ CASTRILLÓN María Teresa RUGELES
author_facet	Leon Gabriel GÓMEZ-ARCHILA Wildeman ZAPATA Elkin GALEANO Alejandro MARTÍNEZ Francisco Javier DÍAZ CASTRILLÓN María Teresa RUGELES
author_sort	Leon Gabriel GÓMEZ-ARCHILA
title	Bromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro
title_short	Bromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro
title_full	Bromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro
title_fullStr	Bromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro
title_full_unstemmed	Bromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro
title_sort	bromotyrosine derivatives from marine sponges inhibit the hiv-1 replication in vitro
publisher	Universidad de Antioquia
publishDate	2014
url	https://doaj.org/article/e34a25bde3134274aa95e0ec91c94a2b
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Bromotyrosine derivatives from marine sponges inhibit the HIV-1 replication in vitro

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