BROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-1

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 an...

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Autores principales:	León G GÓMEZ-ARCHILA, Wildeman ZAPATA, Elkin GALEANO, Alejandro MARTÍNEZ, Francisco J DÍAZ, María T RUGELES
Formato:	article
Lenguaje:	EN
Publicado:	Universidad de Antioquia 2014
Materias:	HIV-1 marine resources antiviral activity bromotyrosine marine sponge VIH-1 recursos marinos actividad antiviral bromotirosina esponja marina Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675
Acceso en línea:	https://doaj.org/article/b12a63cbcc2f426686d4e578d5f6683a
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spelling	oai:doaj.org-article:b12a63cbcc2f426686d4e578d5f6683a2021-12-02T03:46:13ZBROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-10121-4004https://doaj.org/article/b12a63cbcc2f426686d4e578d5f6683a2014-08-01T00:00:00Zhttp://www.scielo.org.co/scielo.php?script=sci_arttext&pid=S0121-40042014000200006&lng=en&tlng=enhttps://doaj.org/toc/0121-4004Background: 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.León G GÓMEZ-ARCHILAWildeman ZAPATAElkin GALEANOAlejandro MARTÍNEZFrancisco J DÍAZMaría T RUGELESUniversidad de AntioquiaarticleHIV-1marine resourcesantiviral activitybromotyrosinemarine spongeVIH-1recursos marinosactividad antiviralbromotirosinaesponja marinaFood processing and manufactureTP368-456Pharmaceutical industryHD9665-9675ENVitae, Vol 21, Iss 2, Pp 114-125 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	HIV-1 marine resources antiviral activity bromotyrosine marine sponge VIH-1 recursos marinos actividad antiviral bromotirosina esponja marina Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675
spellingShingle	HIV-1 marine resources antiviral activity bromotyrosine marine sponge VIH-1 recursos marinos actividad antiviral bromotirosina esponja marina Food processing and manufacture TP368-456 Pharmaceutical industry HD9665-9675 León G GÓMEZ-ARCHILA Wildeman ZAPATA Elkin GALEANO Alejandro MARTÍNEZ Francisco J DÍAZ María T RUGELES BROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-1
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	León G GÓMEZ-ARCHILA Wildeman ZAPATA Elkin GALEANO Alejandro MARTÍNEZ Francisco J DÍAZ María T RUGELES
author_facet	León G GÓMEZ-ARCHILA Wildeman ZAPATA Elkin GALEANO Alejandro MARTÍNEZ Francisco J DÍAZ María T RUGELES
author_sort	León G GÓMEZ-ARCHILA
title	BROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-1
title_short	BROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-1
title_full	BROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-1
title_fullStr	BROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-1
title_full_unstemmed	BROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-1
title_sort	bromotirosinas derivadas de esponjas marinas inhiben la replicación in vitro del vih-1
publisher	Universidad de Antioquia
publishDate	2014
url	https://doaj.org/article/b12a63cbcc2f426686d4e578d5f6683a
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BROMOTIROSINAS DERIVADAS DE ESPONJAS MARINAS INHIBEN LA REPLICACIÓN IN VITRO DEL VIH-1

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