G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity

Rafael Ceña-Diez,1,2 Alba Martin-Moreno,1 F Javier de la Mata,2,3 Rafael Gómez-Ramirez,2,3 Eduardo Muñoz,4 Manuel Ardoy,5 Ma Ángeles Muñoz-Fernández1,2 1Immunology Section, Head Inmuno-Biology Molecular Laboratory, Gregorio Mara&...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Ceña-Diez R, Martin-Moreno A, de la Mata FJ, Gómez-Ramirez R, Muñoz E, Ardoy M, Muñoz-Fernández MA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Topical microbicide HIV-1 HSV-2 Platycodin D G1-S4 and G2-S16 dendrimers Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/00d743609bbb48c6b78516d535e328e1
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:00d743609bbb48c6b78516d535e328e1
record_format	dspace
spelling	oai:doaj.org-article:00d743609bbb48c6b78516d535e328e12021-12-02T03:15:59ZG1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity1178-2013https://doaj.org/article/00d743609bbb48c6b78516d535e328e12019-04-01T00:00:00Zhttps://www.dovepress.com/g1-s4-or-g2-s16-carbosilan-dendrimer-in-combination-with-platycodin-d--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Rafael Ceña-Diez,1,2 Alba Martin-Moreno,1 F Javier de la Mata,2,3 Rafael Gómez-Ramirez,2,3 Eduardo Muñoz,4 Manuel Ardoy,5 Ma Ángeles Muñoz-Fernández1,2 1Immunology Section, Head Inmuno-Biology Molecular Laboratory, Gregorio Marañón University General Hospital, Gregorio Marañón Health Research Institute (IiSGM), Spanish HIV HGM BioBank, Madrid, Spain; 2Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Madrid, Spain; 3Organic and Inorganic Chemistry Department, Alcalá University, Alcalá de Henares, Spain; 4Department of Cell Biology, Physiology and Immunology, Instituto Maimónides de Investigación Biomédicas de Córdoba (IMIBIC), Reina Sofía University Hospital, University of Córdoba, Córdoba, Spain; 5Human Reproduction Unit, Gregorio Marañon University General Hospital, Madrid, Spain Purpose: HIV-1 and herpes simplex virus type-2 (HSV-2) represent two of the most relevant sexually transmitted diseases (STDs) worldwide. Moreover, each year there are >200 million pregnancies worldwide, and more than half are unintended. Continued high rates of unintended pregnancies and spread of HIV-1 and HSV-2 require new approaches to address these problems. G1-S4 and G2-S16 dendrimers emerge as potential candidates for the development of a topical microbicide due to their safety and effectivity against HIV-1 and HSV-2 infection, both in vitro and in vivo. Our goal is to develop a dual topical microbicide to prevent the transmission of STDs and unintended pregnancies. Platycodin D (PD) was selected for its great spermicidal activity, topical application, and biocompatibility. Materials and methods: Toxicology and inhibitory profile of G1-S4/PD and G2-S16/PD were evaluated in vitro and in vivo. Spermicidal activity was assessed by a computer-assisted sperm analysis system (CASA). Results: G1-S4/PD and G2-S16/PD presented >95% of HIV-1 inhibition in TZM-bl cells and peripheral blood mononuclear cells. CASA assessment determined that 0.25 mM of PD with therapeutic concentrations of G1-S4 or G2-S16 was able to induce 100% immobilization of the sperm in 30 seconds. To evaluate the toxicity in vivo, a vaginal toxicity assay was performed in BALB/c mice. No significant changes or damage to the vaginal epithelium after 7 consecutive days of application were observed. Conclusion: Our data indicate that G1-S4/PD and G2-S16/PD combinations are promising candidates to be developed for vaginal microbicides with contraceptive activity. Keywords: topical microbicide, HIV-1, HSV-2, Platycodin D, G1-S4 dendrimer, G2-S16 dendrimerCeña-Diez RMartin-Moreno Ade la Mata FJGómez-Ramirez RMuñoz EArdoy MMuñoz-Fernández MADove Medical PressarticleTopical microbicideHIV-1HSV-2Platycodin DG1-S4 and G2-S16 dendrimersMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 2371-2381 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Topical microbicide HIV-1 HSV-2 Platycodin D G1-S4 and G2-S16 dendrimers Medicine (General) R5-920
spellingShingle	Topical microbicide HIV-1 HSV-2 Platycodin D G1-S4 and G2-S16 dendrimers Medicine (General) R5-920 Ceña-Diez R Martin-Moreno A de la Mata FJ Gómez-Ramirez R Muñoz E Ardoy M Muñoz-Fernández MA G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity
description	Rafael Ceña-Diez,1,2 Alba Martin-Moreno,1 F Javier de la Mata,2,3 Rafael Gómez-Ramirez,2,3 Eduardo Muñoz,4 Manuel Ardoy,5 Ma Ángeles Muñoz-Fernández1,2 1Immunology Section, Head Inmuno-Biology Molecular Laboratory, Gregorio Marañón University General Hospital, Gregorio Marañón Health Research Institute (IiSGM), Spanish HIV HGM BioBank, Madrid, Spain; 2Networking Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Madrid, Spain; 3Organic and Inorganic Chemistry Department, Alcalá University, Alcalá de Henares, Spain; 4Department of Cell Biology, Physiology and Immunology, Instituto Maimónides de Investigación Biomédicas de Córdoba (IMIBIC), Reina Sofía University Hospital, University of Córdoba, Córdoba, Spain; 5Human Reproduction Unit, Gregorio Marañon University General Hospital, Madrid, Spain Purpose: HIV-1 and herpes simplex virus type-2 (HSV-2) represent two of the most relevant sexually transmitted diseases (STDs) worldwide. Moreover, each year there are >200 million pregnancies worldwide, and more than half are unintended. Continued high rates of unintended pregnancies and spread of HIV-1 and HSV-2 require new approaches to address these problems. G1-S4 and G2-S16 dendrimers emerge as potential candidates for the development of a topical microbicide due to their safety and effectivity against HIV-1 and HSV-2 infection, both in vitro and in vivo. Our goal is to develop a dual topical microbicide to prevent the transmission of STDs and unintended pregnancies. Platycodin D (PD) was selected for its great spermicidal activity, topical application, and biocompatibility. Materials and methods: Toxicology and inhibitory profile of G1-S4/PD and G2-S16/PD were evaluated in vitro and in vivo. Spermicidal activity was assessed by a computer-assisted sperm analysis system (CASA). Results: G1-S4/PD and G2-S16/PD presented >95% of HIV-1 inhibition in TZM-bl cells and peripheral blood mononuclear cells. CASA assessment determined that 0.25 mM of PD with therapeutic concentrations of G1-S4 or G2-S16 was able to induce 100% immobilization of the sperm in 30 seconds. To evaluate the toxicity in vivo, a vaginal toxicity assay was performed in BALB/c mice. No significant changes or damage to the vaginal epithelium after 7 consecutive days of application were observed. Conclusion: Our data indicate that G1-S4/PD and G2-S16/PD combinations are promising candidates to be developed for vaginal microbicides with contraceptive activity. Keywords: topical microbicide, HIV-1, HSV-2, Platycodin D, G1-S4 dendrimer, G2-S16 dendrimer
format	article
author	Ceña-Diez R Martin-Moreno A de la Mata FJ Gómez-Ramirez R Muñoz E Ardoy M Muñoz-Fernández MA
author_facet	Ceña-Diez R Martin-Moreno A de la Mata FJ Gómez-Ramirez R Muñoz E Ardoy M Muñoz-Fernández MA
author_sort	Ceña-Diez R
title	G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity
title_short	G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity
title_full	G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity
title_fullStr	G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity
title_full_unstemmed	G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity
title_sort	g1-s4 or g2-s16 carbosilan dendrimer in combination with platycodin d as a promising vaginal microbicide candidate with contraceptive activity
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/00d743609bbb48c6b78516d535e328e1
work_keys_str_mv	AT cenadiezr g1s4org2s16carbosilandendrimerincombinationwithplatycodindasapromisingvaginalmicrobicidecandidatewithcontraceptiveactivity AT martinmorenoa g1s4org2s16carbosilandendrimerincombinationwithplatycodindasapromisingvaginalmicrobicidecandidatewithcontraceptiveactivity AT delamatafj g1s4org2s16carbosilandendrimerincombinationwithplatycodindasapromisingvaginalmicrobicidecandidatewithcontraceptiveactivity AT gomezramirezr g1s4org2s16carbosilandendrimerincombinationwithplatycodindasapromisingvaginalmicrobicidecandidatewithcontraceptiveactivity AT munoze g1s4org2s16carbosilandendrimerincombinationwithplatycodindasapromisingvaginalmicrobicidecandidatewithcontraceptiveactivity AT ardoym g1s4org2s16carbosilandendrimerincombinationwithplatycodindasapromisingvaginalmicrobicidecandidatewithcontraceptiveactivity AT munozfernandezma g1s4org2s16carbosilandendrimerincombinationwithplatycodindasapromisingvaginalmicrobicidecandidatewithcontraceptiveactivity
_version_	1718401834269278208

G1-S4 or G2-S16 carbosilan dendrimer in combination with Platycodin D as a promising vaginal microbicide candidate with contraceptive activity

Ejemplares similares