RESUMEN
Zanthoxylum limoncello is a native plant from southern Mexico which is used as a timber source, condiment and as a traditional medicine. Herein, we report on the volatile content of the leaf essential oil and its biological activities. The annual essential oils (2015-2018) contained volatile organic compounds which exhibited a moderate growth inhibitory activity against H. pylori ATCC 53504 (MIC 121.4-139.7â µg mL-1 ), 26695 (MIC 85.5-94.9â µg mL-1 ) and J99 (MIC 94.7-110.4â µg mL-1 ). These hydrodistillates contained 2-undecanone (31.6-36.8 %; MIC 185.3-199.2â µg mL-1 ) and 2-undecenal (25.1-35.7 %; MIC 144.8-111.3â µg mL-1 ) as the most abundant compounds which were partially involved in the anti-H. pylori activity. The human ornithine decarboxylase enzyme (ODC1), which shows increased activity in several cancer types, was non-competitively inhibited (Vmax 2.7>0.8â Kcat s-1 ) by the essential oil of Z. limoncello as well as by 2-undecanone and 2-undecenal in accordance to inâ vitro kinetic studies. In silico calculations strongly suggest that the carbonyl group of these oxygenated hydrocarbons interacts with both Asn319 and Ala39 at the subunit A of ODC1. Considering that Ala39 is located close to Asn44, a crucial amino acid of the ODC's allosteric site, the non-competitive inhibition of the enzyme by 2-undecanone and 2-undecenal is endorsed. Finally, the essential oil of Z. limoncello and its main volatiles showed a significant (p<0.01) and prolonged repellent effect against Aedes aegypti.
Asunto(s)
Aceites Volátiles/química , Zanthoxylum/química , Aedes/efectos de los fármacos , Animales , Sitios de Unión , Alcoholes Grasos/metabolismo , Alcoholes Grasos/farmacología , Helicobacter pylori/efectos de los fármacos , Humanos , Repelentes de Insectos/aislamiento & purificación , Repelentes de Insectos/farmacología , Cetonas/metabolismo , Cetonas/farmacología , México , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/farmacología , Ornitina Descarboxilasa/efectos de los fármacos , Hojas de la Planta/químicaRESUMEN
Quinolones and fluoroquinolones are widely used to treat uropathogenic Escherichia coli infections. Bacterial resistance to these antimicrobials primarily involves mutations in gyrA and parC genes. To date, no studies have examined the potential relationship between biochemical characteristics and quinolone resistance in uropathogenic E. coli strains. The present work analyzed the quinolone sensitivity and biochemical activities of fifty-eight lactose-negative uropathogenic E. coli strains. A high percentage of the isolates (48.3%) was found to be resistant to at least one of the tested quinolones, and DNA sequencing revealed quinolone resistant determining region gyrA and parC mutations in the multi-resistant isolates. Statistical analyses suggested that the lack of ornithine decarboxylase (ODC) activity is correlated with quinolone resistance. Despite the low number of isolates examined, this is the first study correlating these characteristics in lactose-negative E. coli isolates.
Asunto(s)
Farmacorresistencia Bacteriana Múltiple/genética , Infecciones por Escherichia coli/tratamiento farmacológico , Fluoroquinolonas/uso terapéutico , Lactosa/metabolismo , Ácido Nalidíxico/uso terapéutico , Ornitina Descarboxilasa/genética , Infecciones Urinarias/tratamiento farmacológico , Escherichia coli Uropatógena/genética , Antibacterianos/uso terapéutico , Brasil , Girasa de ADN/genética , Topoisomerasa de ADN IV/genética , Descarboxilación/genética , Descarboxilación/fisiología , Infecciones por Escherichia coli/microbiología , Humanos , Pruebas de Sensibilidad Microbiana , Ornitina/metabolismo , Infecciones Urinarias/microbiología , Escherichia coli Uropatógena/efectos de los fármacos , Escherichia coli Uropatógena/enzimología , Escherichia coli Uropatógena/aislamiento & purificaciónRESUMEN
Quinolones and fluoroquinolones are widely used to treat uropathogenic Escherichia coli infections. Bacterial resistance to these antimicrobials primarily involves mutations in gyrA and parC genes. To date, no studies have examined the potential relationship between biochemical characteristics and quinolone resistance in uropathogenic E. coli strains. The present work analyzed the quinolone sensitivity and biochemical activities of fifty-eight lactose-negative uropathogenic E. coli strains. A high percentage of the isolates (48.3%) was found to be resistant to at least one of the tested quinolones, and DNA sequencing revealed quinolone resistant determining region gyrA and parC mutations in the multi-resistant isolates. Statistical analyses suggested that the lack of ornithine decarboxylase (ODC) activity is correlated with quinolone resistance. Despite the low number of isolates examined, this is the first study correlating these characteristics in lactose-negative E. coli isolates.(AU)
Asunto(s)
Humanos , Farmacorresistencia Bacteriana Múltiple/genética , Infecciones por Escherichia coli/tratamiento farmacológico , Fluoroquinolonas/uso terapéutico , Lactosa/metabolismo , Ácido Nalidíxico/uso terapéutico , Ornitina Descarboxilasa/genética , Escherichia coli Uropatógena/genética , Antibacterianos/uso terapéutico , Brasil , Girasa de ADN/genética , Topoisomerasa de ADN IV/genética , Descarboxilación/genética , Descarboxilación/fisiología , Infecciones por Escherichia coli/microbiología , Pruebas de Sensibilidad Microbiana , Ornitina/metabolismo , /microbiología , Escherichia coli Uropatógena , Escherichia coli Uropatógena/enzimología , Escherichia coli Uropatógena/aislamiento & purificaciónRESUMEN
Quinolones and fluoroquinolones are widely used to treat uropathogenic