Activity of Semi-Synthetic Mulinanes against MDR, Pre-XDR, and XDR Strains of Mycobacterium tuberculosis

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AudienciaPúblico en generales_ES
CoberturaMéxicoes_ES
Fecha de ingreso2026-10-05T16:33:37Z
Fecha de publicación2021-01-01
ResumenTuberculosis causes more than 1.2 million deaths each year. Worldwide, it is the first cause of death by a single infectious agent. The emergence of drug-resistant strains has limited pharmacological treatment of the disease and today, new drugs are urgently needed. Semi-synthetic mulinanes have previously shown important activity against multidrug-resistant (MDR) Mycobacterium tuberculosis. In this investigation, a new set of semi-synthetic mulinanes were synthetized, characterized, and evaluated for their in vitro activity against three drug-resistant clinical isolates of M. tuberculosis: MDR, pre-extensively Drug-Resistant (pre-XDR), and extensively Drug-Resistant (XDR), and against the drug-susceptible laboratory reference strain H37Rv. Derivative 1a showed the best anti-TB activity (minimum inhibitory concentration {[}MIC] = 5.4 mu M) against the susceptible strain and was twice as potent (MIC = 2.7 mu M) on the MDR, pre-XDR, and XDR strains and also possessed a bactericidal effect. Derivative 1a was also tested for its anti-TB activity in mice infected with the MDR strain. In this case, 1a produced a significant reduction of pulmonary bacilli loads, six times lower than the control, when tested at 0.2536 mg/Kg. In addition, 1a demonstrated an adjuvant effect by shortening second-line chemotherapy. Finally, the selectivity index of >15.64 shown by 1a when tested on Vero cells makes this derivative an important candidate for future studies in the development of novel antitubercular agents.es_ES
Doihttps://doi.org/10.3390/metabo11120876es_ES
URIhttps://riuat.uat.edu.mx/handle/123456789/5422
Idiomaenes_ES
EditorialMDPIes_ES
RelaciónMetaboliteses_ES
URL relacionadohttps://doi.org/10.3390/metabo11120876es_ES
DerechosAcceso abierto (Metadatos de producción científica)es_ES
Licenciahttp://purl.org/coar/access_right/c_abf2es_ES
FuenteMetabolites
Palabra claveMDRes_ES
Palabra clavepre-XDR and XDR tuberculosises_ES
Palabra claveMycobacterium tuberculosises_ES
Palabra clavesemi-synthetic derivativeses_ES
Palabra clavemulinaneses_ES
TítuloActivity of Semi-Synthetic Mulinanes against MDR, Pre-XDR, and XDR Strains of Mycobacterium tuberculosises_ES
TipoArtículoes_ES
ArbitradoHa sido Arbitradoes_ES
AutorMartinez-Gonzalez, Maria Alejandrina
AutorPena-Rodriguez, Luis Manuel
AutorUc-Cachon, Andres Humberto
AutorBorquez, Jorge
AutorSimirgiotis, Mario J.
AutorBarrios-Garcia, Hugo Brigido
AutorHernandez-Pando, Rogelio
AutorLoyola, Luis Alberto
AutorAreche, Carlos
AutorDzul-Beh, Angel de Jesus
AutorBarrios-Payan, Jorge Alberto
AutorMata-Espinosa, Dulce
AutorEscalante-Erosa, Fabiola
AutorGarcia-Sosa, Karlina
AutorMolina-Salinas, Gloria Maria
AutorMartinez-Gonzalez, Maria Alejandrinaes_ES
AutorPena-Rodriguez, Luis Manueles_ES
AutorUc-Cachon, Andres Humbertoes_ES
AutorBorquez, Jorgees_ES
AutorSimirgiotis, Mario J.es_ES
AutorBarrios-Garcia, Hugo Brigidoes_ES
AutorHernandez-Pando, Rogelioes_ES
AutorLoyola, Luis Albertoes_ES
AutorAreche, Carloses_ES
AutorDzul-Beh, Angel de Jesuses_ES
AutorBarrios-Payan, Jorge Albertoes_ES
AutorMata-Espinosa, Dulcees_ES
AutorEscalante-Erosa, Fabiolaes_ES
AutorGarcia-Sosa, Karlinaes_ES
AutorMolina-Salinas, Gloria Mariaes_ES
InstituciónUniversidad Autónoma de Tamaulipas
InstituciónUniversidad Autónoma de Tamaulipases_ES
Número12es_ES
URL relacionadahttps://doi.org/10.3390/metabo11120876
Tipo de artículoIndexado
Tipo de artículoIndexadoes_ES
Volumen11es_ES

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