Cargando…

A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate

A long list of chemotherapeutical drugs used in the treatment of the peripheral and the central nervous systems possess anti-microbial activity. Some of these neurotropic compounds are chiral, with the one stereo isomeric form exaggerating reduced neurotropism. This is the case for the levorotatory...

Descripción completa

Detalles Bibliográficos
Autores principales: Christensen, Jørn B., Hendricks, Oliver, Chaki, Shaswati, Mukherjee, Sayanti, Das, Ayan, Pal, Tapan K., Dastidar, Sujata G., Kristiansen, Jette E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3591432/
https://www.ncbi.nlm.nih.gov/pubmed/23505431
http://dx.doi.org/10.1371/journal.pone.0057493
_version_ 1782262055886127104
author Christensen, Jørn B.
Hendricks, Oliver
Chaki, Shaswati
Mukherjee, Sayanti
Das, Ayan
Pal, Tapan K.
Dastidar, Sujata G.
Kristiansen, Jette E.
author_facet Christensen, Jørn B.
Hendricks, Oliver
Chaki, Shaswati
Mukherjee, Sayanti
Das, Ayan
Pal, Tapan K.
Dastidar, Sujata G.
Kristiansen, Jette E.
author_sort Christensen, Jørn B.
collection PubMed
description A long list of chemotherapeutical drugs used in the treatment of the peripheral and the central nervous systems possess anti-microbial activity. Some of these neurotropic compounds are chiral, with the one stereo isomeric form exaggerating reduced neurotropism. This is the case for the levorotatory form of thioridazine. The phenothiazine thioridazine is an interesting compound, characterized by exhibiting a significant growth inhibiting activity on a wide array of micro-organisms. Thioridazine is characterized by another challenging feature, because the compound is concentrated in certain human tissue cells. The present study describes a comparative study of the two enantiomers as well as the racemic form of thioridazine. The study exploits the stereochemical aspect and the in vitro and in vivo potential of these compounds, with a focus on the effects on Gram negative organism Salmonella enterica serover Typhimurium. In summary, the results of this study yielded a significant antibacterial activity of all forms of thioridazine, indicating the levorotatory (–)- form to be superior in terms of both its in vitro and in vivo efficacies.
format Online
Article
Text
id pubmed-3591432
institution National Center for Biotechnology Information
language English
publishDate 2013
publisher Public Library of Science
record_format MEDLINE/PubMed
spelling pubmed-35914322013-03-15 A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate Christensen, Jørn B. Hendricks, Oliver Chaki, Shaswati Mukherjee, Sayanti Das, Ayan Pal, Tapan K. Dastidar, Sujata G. Kristiansen, Jette E. PLoS One Research Article A long list of chemotherapeutical drugs used in the treatment of the peripheral and the central nervous systems possess anti-microbial activity. Some of these neurotropic compounds are chiral, with the one stereo isomeric form exaggerating reduced neurotropism. This is the case for the levorotatory form of thioridazine. The phenothiazine thioridazine is an interesting compound, characterized by exhibiting a significant growth inhibiting activity on a wide array of micro-organisms. Thioridazine is characterized by another challenging feature, because the compound is concentrated in certain human tissue cells. The present study describes a comparative study of the two enantiomers as well as the racemic form of thioridazine. The study exploits the stereochemical aspect and the in vitro and in vivo potential of these compounds, with a focus on the effects on Gram negative organism Salmonella enterica serover Typhimurium. In summary, the results of this study yielded a significant antibacterial activity of all forms of thioridazine, indicating the levorotatory (–)- form to be superior in terms of both its in vitro and in vivo efficacies. Public Library of Science 2013-03-07 /pmc/articles/PMC3591432/ /pubmed/23505431 http://dx.doi.org/10.1371/journal.pone.0057493 Text en © 2013 Christensen et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Christensen, Jørn B.
Hendricks, Oliver
Chaki, Shaswati
Mukherjee, Sayanti
Das, Ayan
Pal, Tapan K.
Dastidar, Sujata G.
Kristiansen, Jette E.
A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate
title A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate
title_full A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate
title_fullStr A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate
title_full_unstemmed A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate
title_short A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate
title_sort comparative analysis of in vitro and in vivo efficacies of the enantiomers of thioridazine and its racemate
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3591432/
https://www.ncbi.nlm.nih.gov/pubmed/23505431
http://dx.doi.org/10.1371/journal.pone.0057493
work_keys_str_mv AT christensenjørnb acomparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT hendricksoliver acomparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT chakishaswati acomparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT mukherjeesayanti acomparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT dasayan acomparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT paltapank acomparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT dastidarsujatag acomparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT kristiansenjettee acomparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT christensenjørnb comparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT hendricksoliver comparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT chakishaswati comparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT mukherjeesayanti comparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT dasayan comparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT paltapank comparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT dastidarsujatag comparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate
AT kristiansenjettee comparativeanalysisofinvitroandinvivoefficaciesoftheenantiomersofthioridazineanditsracemate