Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine Model

One of the most important steps in preclinical drug discovery is to demonstrate the in vivo efficacy of potential leishmanicidal compounds and good characteristics at the level of parasite killing prior to initiating human clinical trials. This paper describes the use of dehydrothyrsiferol (DT), iso...

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Main Authors: Atteneri López-Arencibia, Carlos J. Bethencourt-Estrella, Desirée San Nicolás-Hernández, Rubén L. Rodríguez-Expósito, Angélica Domínguez-de-Barros, Lizbeth Salazar-Villatoro, Maritza Omaña-Molina, Francisco Cen-Pacheco, Ana R. Díaz-Marrero, José J. Fernández, Elizabeth Córdoba-Lanús, Jacob Lorenzo-Morales, José E. Piñero
Format: Article
Language:English
Published: MDPI AG 2024-12-01
Series:Marine Drugs
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Online Access:https://www.mdpi.com/1660-3397/23/1/13
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author Atteneri López-Arencibia
Carlos J. Bethencourt-Estrella
Desirée San Nicolás-Hernández
Rubén L. Rodríguez-Expósito
Angélica Domínguez-de-Barros
Lizbeth Salazar-Villatoro
Maritza Omaña-Molina
Francisco Cen-Pacheco
Ana R. Díaz-Marrero
José J. Fernández
Elizabeth Córdoba-Lanús
Jacob Lorenzo-Morales
José E. Piñero
author_facet Atteneri López-Arencibia
Carlos J. Bethencourt-Estrella
Desirée San Nicolás-Hernández
Rubén L. Rodríguez-Expósito
Angélica Domínguez-de-Barros
Lizbeth Salazar-Villatoro
Maritza Omaña-Molina
Francisco Cen-Pacheco
Ana R. Díaz-Marrero
José J. Fernández
Elizabeth Córdoba-Lanús
Jacob Lorenzo-Morales
José E. Piñero
author_sort Atteneri López-Arencibia
collection DOAJ
description One of the most important steps in preclinical drug discovery is to demonstrate the in vivo efficacy of potential leishmanicidal compounds and good characteristics at the level of parasite killing prior to initiating human clinical trials. This paper describes the use of dehydrothyrsiferol (DT), isolated from the red alga <i>Laurencia viridis</i>, in a pharmaceutical form supported on Sepigel, and the in vivo efficacy against a mouse model of cutaneous leishmaniasis. Studying the ultrastructural effect of DT was also carried out to verify the suspected damage at the cellular level and determine the severity of damages produced in the homeostasis of promastigotes. BALB/c mice infected with <i>Leishmania amazonensis</i> were divided into four groups: untreated mice, mice treated with miltefosine orally and mice treated topically with 1% and 0.5% DT-Sepigel; treatment was carried out for two weeks. Treatment with DT significantly reduced the parasite load in skin, liver and spleen compared with the untreated group. In addition, DT-Sepigel at the lowest concentration (0.5%) showed the best results, reducing lesion size by 87% at 3 weeks post-treatment. DT-Sepigel has demonstrated to be a potent topical treatment that, in combined drug trials, may aim at combating cutaneous leishmaniasis.
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spelling doaj-art-4a6a9a01b7a74736968ebbd7e2f40f102025-01-24T13:39:28ZengMDPI AGMarine Drugs1660-33972024-12-012311310.3390/md23010013Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine ModelAtteneri López-Arencibia0Carlos J. Bethencourt-Estrella1Desirée San Nicolás-Hernández2Rubén L. Rodríguez-Expósito3Angélica Domínguez-de-Barros4Lizbeth Salazar-Villatoro5Maritza Omaña-Molina6Francisco Cen-Pacheco7Ana R. Díaz-Marrero8José J. Fernández9Elizabeth Córdoba-Lanús10Jacob Lorenzo-Morales11José E. Piñero12Instituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38206 La Laguna, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38206 La Laguna, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38206 La Laguna, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38206 La Laguna, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38206 La Laguna, SpainDepartamento de Infectómica y Patogénesis Molecular, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Ciudad de Mexico 07360, MexicoDepartamento de Infectómica y Patogénesis Molecular, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Ciudad de Mexico 07360, MexicoInstituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, SpainInstituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, SpainInstituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38206 La Laguna, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38206 La Laguna, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38206 La Laguna, SpainOne of the most important steps in preclinical drug discovery is to demonstrate the in vivo efficacy of potential leishmanicidal compounds and good characteristics at the level of parasite killing prior to initiating human clinical trials. This paper describes the use of dehydrothyrsiferol (DT), isolated from the red alga <i>Laurencia viridis</i>, in a pharmaceutical form supported on Sepigel, and the in vivo efficacy against a mouse model of cutaneous leishmaniasis. Studying the ultrastructural effect of DT was also carried out to verify the suspected damage at the cellular level and determine the severity of damages produced in the homeostasis of promastigotes. BALB/c mice infected with <i>Leishmania amazonensis</i> were divided into four groups: untreated mice, mice treated with miltefosine orally and mice treated topically with 1% and 0.5% DT-Sepigel; treatment was carried out for two weeks. Treatment with DT significantly reduced the parasite load in skin, liver and spleen compared with the untreated group. In addition, DT-Sepigel at the lowest concentration (0.5%) showed the best results, reducing lesion size by 87% at 3 weeks post-treatment. DT-Sepigel has demonstrated to be a potent topical treatment that, in combined drug trials, may aim at combating cutaneous leishmaniasis.https://www.mdpi.com/1660-3397/23/1/13dehydrothyrsiferolmarine oxasqualenoid<i>Leishmania amazonensis</i>cutaneous leishmaniasis
spellingShingle Atteneri López-Arencibia
Carlos J. Bethencourt-Estrella
Desirée San Nicolás-Hernández
Rubén L. Rodríguez-Expósito
Angélica Domínguez-de-Barros
Lizbeth Salazar-Villatoro
Maritza Omaña-Molina
Francisco Cen-Pacheco
Ana R. Díaz-Marrero
José J. Fernández
Elizabeth Córdoba-Lanús
Jacob Lorenzo-Morales
José E. Piñero
Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine Model
Marine Drugs
dehydrothyrsiferol
marine oxasqualenoid
<i>Leishmania amazonensis</i>
cutaneous leishmaniasis
title Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine Model
title_full Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine Model
title_fullStr Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine Model
title_full_unstemmed Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine Model
title_short Dehydrothyrsiferol Against Cutaneous Leishmaniasis: Treatment Outcome in a Murine Model
title_sort dehydrothyrsiferol against cutaneous leishmaniasis treatment outcome in a murine model
topic dehydrothyrsiferol
marine oxasqualenoid
<i>Leishmania amazonensis</i>
cutaneous leishmaniasis
url https://www.mdpi.com/1660-3397/23/1/13
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