RESUMO
Background and Objectives: Antimicrobial resistance (AMR) is increasing worldwide and imposes significant life-threatening risks to several different populations, especially to those in intensive care units (ICU). The most commonly isolated organisms in ICU comprise gram-negative bacilli (GNB), and these represent a leading cause of serious infections. This study was conducted to describe the prevalence of resistance in GNB isolated from patients in adults, pediatric, and neonatal ICU in a tertiary-care hospital in Mérida, Mexico. Materials and Methods: A retrospective study was done on samples collected in Neonatal (NICU), Pediatric (PICU) and Adult (AICU) ICU of Unidad Médica de Alta Especialidad, Instituto Mexicano del Seguro Social in Mérida, México. The identification of isolates and antimicrobial susceptibility testing were performed using an automated system. Results: A total of 517 GNB strains were isolated. The most common positive culture was bronchial secretions. Pseudomonas aeruginosa was the prevalent pathogen in NICU and PICU, whereas Escherichia coli was common in the AICU. Overall, GNB exhibited a high resistance rates for Ampicillin (95.85%), Cefuroxime (84.17%), Piperacillin (82.93%), Cefotaxime (78.07%), Ceftriaxone (77.41%), Aztreonam (75.23%), Cefazolin (75.00%), and Ceftazidime (73.19%). There are significant differences in the resistance rates of GNB from different ICUs for penicillins, cephalosporins, carbapenems and fluoroquinolones drugs. Escherichia coli (multidrug-resistant [MDR] = 91.57%, highly resistant microorganisms [HRMO] = 90.36%) and Acinetobacter baumannii (MDR = 86.79%, HRMO = 83.02%) exhibited the highest percentage of MDR and HRMO profiles. The prevalence of the extended-spectrum beta-lactamases (ESBL)-producing isolates was 83.13% in E. coli, 78.84% in Klebsiella pneumoniae, and 66.67% in Proteus mirabilis, respectively. Conclusions: The high resistance rates to drugs were exhibited by our GNB isolates. Continuous surveillance and control of the use of antimicrobials are urgently needed to reduce the emergence and spreading of MDR, HRMO, and/or ESBL-producing bacilli.
Assuntos
Farmacorresistência Bacteriana Múltipla , Bactérias Gram-Negativas/isolamento & purificação , Infecções por Bactérias Gram-Negativas/epidemiologia , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Criança , Pré-Escolar , Feminino , Bactérias Gram-Negativas/efeitos dos fármacos , Infecções por Bactérias Gram-Negativas/tratamento farmacológico , Infecções por Bactérias Gram-Negativas/microbiologia , Humanos , Lactente , Recém-Nascido , Unidades de Terapia Intensiva , Masculino , México/epidemiologia , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Prevalência , Estudos Retrospectivos , Fatores de Risco , Centros de Atenção Terciária , Adulto JovemRESUMO
BACKGROUND AND OBJECTIVES: Tuberculosis (TB) is one of the deadliest infectious diseases and comprises a global public health concern because co-infection with Human immunodeficiency virus (HIV) and, in particular, the continuous isolation of new Multidrug-resistant strains (MDR), rendering the discovery of novel anti-TB agents a strategic priority. One of the most effective first-line mycobactericidal drugs is Isoniazid (INH). Previously, we reported in vitro anti-mycobacterial activity against sensitive and MDR Mycobacterium tuberculosis strains of a new oxadiazole obtained from the hybridization of INH and palmitic acid. The present study evaluated the therapeutic potential of liposomes including Phosphatidylcholine (PC) and L-α Phosphatidic acid (PA) or PC and Cholesterol (Chol) containing 4-(5-pentadecyl-1,3,4-oxadiazol-2-yl)pyridine in BALB/c male mice infected by intratracheal (i.t.) route with drug-sensitive or MDR M. tuberculosis. METHODS: The lipophilic 4-(5-pentadecyl-1,3,4-oxadiazol-2-yl)pyridine was obtained to mix INH and palmitoyl chloride. The in vivo anti-TB effect of this oxadiazole derivative contained in two different liposomes was tested in BALB/c mice infected with a sensitive strain of M. tuberculosis, initiating treatment 2 months post-infection, by i.t. route, of 50 µg of oxadiazole derivative for 1 month. In a second stage, mice were infected with an MDR (resistant to first-line drugs) and treated with 150 µg of an oxadiazole derivative carried by PC + Chol liposomes for 2 months. The effect of the oxadiazole derivative in vivo was determined by the quantification of lung bacilli loads and histopathology. RESULTS: In comparison with control animals, drug-sensitive, strain-infected mice treated for 1 month with 50 µg of this oxadiazole derivative contained in the liposomes of PC + Chol showed a significant, 80% decrease of live bacilli in lungs, which correlated with the morphometric observation, and the group of MDR clinical isolate-infected mice treated with 150 µg of the oxadiazole derivative contained in the same type of liposome showed significantly lower lung bacillary loads than control mice, producing 90% of bacilli burden reduction after 2 months of treatment. CONCLUSION: These results confirm and extend the reported highly efficient anti-mycobacterial activity of this lipophilic oxidazole derivative when it is carried by liposomes in mice suffering from late progressive pulmonary TB induced by drug-sensitive, and most prominently by, MDR strains.
Assuntos
Antituberculosos/farmacologia , Mycobacterium tuberculosis/isolamento & purificação , Oxidiazóis/farmacologia , Piridinas/farmacologia , Tuberculose Pulmonar/tratamento farmacológico , Animais , Antituberculosos/administração & dosagem , Colesterol/química , Modelos Animais de Doenças , Isoniazida/administração & dosagem , Isoniazida/química , Isoniazida/farmacologia , Lipossomos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Oxidiazóis/administração & dosagem , Ácidos Fosfatídicos/química , Fosfatidilcolinas/química , Piridinas/administração & dosagem , Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológicoRESUMO
BACKGROUND AND OBJECTIVES: The recent emergence of multidrug-resistant (MDR), extensively drug-resistant (XDR), and totally drug-resistant (TDR) Mycobacterium tuberculosis (MTB) strains have further complicated the control of tuberculosis (TB). There is an urgent need of new molecules candidates to be developed as novel, active, and less toxic anti-tuberculosis (anti-TB) drugs. Medicinal plants have been an excellent source of leads for the development of drugs, particularly as anti-infective agents. In previous studies, the non-polar extract of Diospyros anisandra showed potent anti-TB activity, and three monomeric and five dimeric naphthoquinones have been obtained. In this study, we performed bioguided chemical fractionation and the isolation of eight naphthoquinones from D. anisandra and their evaluation of anti-TB and cytotoxic activities against mammalian cells. METHODS: The n-hexane crude extract from the stem bark of the plant was obtained by maceration and liquid-liquid fractionation. The isolation of naphthoquinones was carried out by chromatographic methods and identified by gas chromatography and mass spectroscopy data analysis. Anti-TB activity was evaluated against two strains of MTB (H37Rv) susceptible to all five first-line anti-TB drugs and a clinical isolate that is resistant to these medications (pan-resistant, CIBIN 99) by measuring the minimal inhibitory concentration (MIC). Cytotoxicity of naphthoquinones was estimated against two mammalian cells, Vero line and primary cultures of human peripheral blood mononuclear (PBMC) cells, and their selectivity index (SI) was determined. RESULTS: Plumbagin and its dimers maritinone and 3,3'-biplumbagin showed the strongest activity against both MTB strains (MIC = 1.56-3.33 µg/mL). The bioactivity of maritinone and 3,3'-biplumbagin were 32 times more potent than rifampicin against the pan-resistant strain, and both dimers showed to be non-toxic against PBMC and Vero cells. The SI of maritinone and 3,3'-biplumbagin on Vero cells was 74.34 and 194.11 against sensitive and pan-resistant MTB strains, respectively. CONCLUSION: Maritinone and 3,3'-biplumbagin possess a very interesting potential for development as new drugs against M. tuberculosis, mainly resistant profile strains.
Assuntos
Antituberculosos/farmacologia , Diospyros/química , Mycobacterium tuberculosis/efeitos dos fármacos , Naftoquinonas/farmacologia , Animais , Antituberculosos/isolamento & purificação , Antituberculosos/toxicidade , Células Cultivadas , Chlorocebus aethiops , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/metabolismo , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Mycobacterium tuberculosis/isolamento & purificação , Naftoquinonas/isolamento & purificação , Naftoquinonas/toxicidade , Casca de Planta , Extratos Vegetais/farmacologia , Caules de Planta , Rifampina/farmacologia , Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológico , Tuberculose Resistente a Múltiplos Medicamentos/microbiologia , Células VeroRESUMO
The characteristics of tuberculosis (TB) patients related to a chain of recent TB transmissions were investigated. Mycobacterium tuberculosis (MTB) isolates (120) were genotyped using the restriction fragment length polymorphism-IS6110 (R), spacer oligotyping (S) and mycobacterial interspersed repetitive units-variable number of tandem repeats (M) methods. The MTB isolates were clustered and the clusters were grouped according to the similarities of their genotypes. Spearman's rank correlation coefficients between the groups of MTB isolates with similar genotypes and those patient characteristics indicating a risk for a pulmonary TB (PTB) chain transmission were ana- lysed. The isolates showing similar genotypes were distributed as follows: SMR (5%), SM (12.5%), SR (1.67%), MR (0%), S (46.67%), M (5%) and R (0%). The remaining 35 cases were orphans. SMR exhibited a significant correlation (p < 0.05) with visits to clinics, municipalities and comorbidities (primarily diabetes mellitus). S correlated with drug consumption and M with comorbidities. SMR is needed to identify a social network in metropolitan areas for PTB transmission and S and M are able to detect risk factors as secondary components of a transmission chain of TB.
Assuntos
Técnicas de Genotipagem/métodos , Mycobacterium tuberculosis/genética , Tuberculose Pulmonar/microbiologia , Tuberculose Pulmonar/transmissão , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Cidades , Comorbidade , DNA Bacteriano/isolamento & purificação , Feminino , Genótipo , Humanos , Sequências Repetitivas Dispersas/genética , Masculino , México/epidemiologia , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Epidemiologia Molecular/métodos , Mycobacterium tuberculosis/classificação , Mycobacterium tuberculosis/isolamento & purificação , Polimorfismo de Fragmento de Restrição/genética , Fatores de Risco , Fatores Sociológicos , Estatísticas não Paramétricas , Sequências de Repetição em Tandem/genética , Tuberculose Pulmonar/epidemiologia , Tuberculose Pulmonar/genética , População Urbana , Adulto JovemRESUMO
The new mulinane diterpenoids 1 and 2 were isolated from the EtOAc extract of Mulinum crassifolium, while the rearranged mulinane 5, which was isolated for the first time from a natural source, was isolated from Azorella compacta. Compounds 1-2 were prepared by semi-synthesis thorough acetylation of the diterpene 17-acetoxymulinic acid (3). A mechanism of reaction was proposed, while the structures of the new compounds were elucidated on the basis of comprehensive spectroscopic analysis and computational methods.
Assuntos
Apiaceae/química , Asteraceae/química , Diterpenos/isolamento & purificação , Diterpenos/química , Estrutura Molecular , Extratos Vegetais/químicaRESUMO
Schoepfia schreberi has been used in Mayan folk medicine to treat diarrhea and cough. This study aimed to determine the anti-growth, anti-resistance, and/or anti-virulence activities of S. schreberi extracts against Acinetobacter baumannii, a pathogen leader that causes healthcare-associated infections with high rates of drug-resistant including carbapenems, the last line of antibiotics known as superbugs, and analyze their composition using HPLC-DAD. Ethyl acetate (SSB-3) and methanol (SSB-4) bark extracts exhibit antimicrobial and biocidal effects against drug-susceptible and drug-resistant A. baumannii. Chemical analysis revealed that SSB-3 and SSB-4 contained of gallic and ellagic acids derivatives. The anti-resistance activity of the extracts revealed that SSB-3 or SSB-4, combined with imipenem, exhibited potent antibiotic reversal activity against A. baumannii by acting as pump efflux modulators. The extracts also displayed activity against surface motility of A. baumannii and its capacity to survive reactive oxygen species. This study suggests that S. schreberi can be considered a source of antibiotics, even adjuvanted compounds, as anti-resistant or anti-virulence agents against A. baumannii, contributing to ethnopharmacological knowledge and reappraisal of Mayan medicinal flora, and supporting the traditional use of the bark of the medicinal plant S. schreberi for the treatment of infectious diseases.
RESUMO
Staphylococcus aureus infections are prevalent in healthcare and community environments. Methicillin-resistant S. aureus is catalogued as a superbug of high priority among the pathogens. This Gram-positive coccus can form biofilms and produce toxins, leading to persistent infection and antibiotic resistance. Limited effective antibiotics have encouraged the development of innovative strategies, with a particular emphasis on resistance mechanisms and/or virulence factors. Medicinal aromatic plants have emerged as promising alternative sources. This study investigated the antimicrobial, antibiofilm, and antihemolysis properties of three different chemotypes of Lippia origanoides essential oil (EO) against susceptible and drug-resistant S. aureus strains. The chemical composition of the EO was analyzed using GC-MS, revealing high monoterpene concentrations, with carvacrol and thymol as the major components in two of the chemotypes. The third chemotype consisted mainly of the sesquiterpene ß-caryophyllene. The MIC values for the two monoterpene chemotypes ranged from 62.5 to 500 µg/mL for all strains, whereas the sesquiterpene chemotype showed activity against seven strains at concentrations of 125-500 µg/mL, which is the first report of its anti-S. aureus activity. The phenolic chemotypes inhibited biofilm formation in seven S. aureus strains, whereas the sesquiterpene chemotype only inhibited biofilm formation in four strains. In addition, phenolic chemotypes displayed antihemolysis activity, with IC50 values ranging from 58.9 ± 3.8 to 128.3 ± 9.2 µg/mL. Our study highlights the importance of L. origanoides EO from the Yucatan Peninsula, which has the potential for the development of anti-S. aureus agents.
RESUMO
This study aimed to determine the feasibility of applying machine-learning methods to assess the progression of chronic kidney disease (CKD) in patients with coronavirus disease (COVID-19) and acute renal injury (AKI). The study was conducted on patients aged 18 years or older who were diagnosed with COVID-19 and AKI between April 2020 and March 2021, and admitted to a second-level hospital in Mérida, Yucatán, México. Of the admitted patients, 47.92% died and 52.06% were discharged. Among the discharged patients, 176 developed AKI during hospitalization, and 131 agreed to participate in the study. The study's results indicated that the area under the receiver operating characteristic curve (AUC-ROC) for the four models was 0.826 for the support vector machine (SVM), 0.828 for the random forest, 0.840 for the logistic regression, and 0.841 for the boosting model. Variable selection methods were utilized to enhance the performance of the classifier, with the SVM model demonstrating the best overall performance, achieving a classification rate of 99.8% ± 0.1 in the training set and 98.43% ± 1.79 in the validation set in AUC-ROC values. These findings have the potential to aid in the early detection and management of CKD, a complication of AKI resulting from COVID-19. Further research is required to confirm these results.
RESUMO
The resistance of 139 Mycobacterium tuberculosis (MTB) isolates from the city of Monterrey, Northeast Mexico, to first and second-line anti-TB drugs was analysed. A total of 73 isolates were susceptible and 66 were resistant to anti-TB drugs. Monoresistance to streptomycin, isoniazid (INH) and ethambutol was observed in 29 cases. Resistance to INH was found in 52 cases and in 29 cases INH resistance was combined with resistance to two or three drugs. A total of 24 isolates were multidrug-resistant (MDR) resistant to at least INH and rifampicin and 11 MDR cases were resistant to five drugs. The proportion of MDR-TB among new TB cases in our target population was 0.72% (1/139 cases). The proportion of MDR-TB among previously treated cases was 25.18% (35/139 cases). The 13 polyresistant and 24 MDR isolates were assayed against the following seven second-line drugs: amikacin (AMK), kanamycin (KAN), capreomycin (CAP), clofazimine (CLF), ethionamide (ETH), ofloxacin (OFL) and cycloserine (CLS). Resistance to CLF, OFL or CLS was not observed. Resistance was detected to ETH (10.80%) and to AMK (2.70%), KAN (2.70%) and CAP (2.70%). One isolate of MDR with primary resistance was also resistant to three second-line drugs. Monterrey has a high prevalence of MDR-TB among previously treated cases and extensively drug-resistant-MTB strains may soon appear.
Assuntos
Antituberculosos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Tuberculose Resistente a Múltiplos Medicamentos/microbiologia , Tuberculose Pulmonar/microbiologia , Adolescente , Adulto , Feminino , Geografia Médica , Humanos , Masculino , México/epidemiologia , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Fatores de Risco , Fatores Socioeconômicos , Tuberculose Resistente a Múltiplos Medicamentos/epidemiologia , Tuberculose Pulmonar/epidemiologia , Adulto JovemRESUMO
A total of 82 fungal extracts were selected and screened against Mycobacterium tuberculosis and promastigotes of Leishmania mexicana strains. Results showed inhibitory activity in 29 % of the fungal strains against at least one of the targets tested. The most significant antituberculosis (antiTB) effects were presented by Cylindrocarpon sp. XH9B, Fusarium sp. TA54, Fusarium XH1Ga, Gliocladium penicillioides TH04 and TH21, Gliocladium sp. TH16, Kutilakesa sp. MR46, and Verticillium sp. TH28 strains (minimal inhibition concentration (MIC) = 1.56-25 µg/ml). Mortality of L. mexicana promastigotes was displayed by only four strains, Fusarium sp. TA50, Fusarium sp. TA54, Verticillium sp. TH28, and the unidentified 2TA2 strain (IC(50) = 14.23-100 µg/ml and IC(100) = 50-100 µg/ml). Seven of these most active strains were defatted and their corresponding fractions evaluated again. The results showed the best antiTB activity in Gliocladium sp. TH16 (MIC = 1.56 µg/ml) and the highest leishmanicidal potential in Fusarium sp. TA54 (IC(50) = 6.36 µg/ml). These results show that fungi living in the tropical regions of México have the ability to produce bioactive metabolites that could be used in the near future as natural products to control neglected tropical diseases.
Assuntos
Antiprotozoários/farmacologia , Antituberculosos/farmacologia , Fungos/química , Leishmania mexicana/efeitos dos fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Antiprotozoários/isolamento & purificação , Antituberculosos/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , México , Testes de Sensibilidade Microbiana , Clima TropicalRESUMO
BACKGROUND: Complementary and alternative medicine (CAM) is widely used for multiple reasons such as treatment of diseases and their symptoms, empowerment, self-care, disease prevention, dissatisfaction, adverse effects or cost of conventional medicine, perception of compatibility with beliefs, and idiosyncrasy. This study investigated CAM use in patients with chronic kidney disease (CKD) undergoing peritoneal dialysis (PD). METHODS: A cross-sectional survey study was conducted with 240 eligible patients with CKD in the PD program. By applying the I-CAM-Q-questionnaire, the frequency, level of satisfaction, and reasons for CAM use were explored, and the demographic and clinical data of users and non-users were analyzed. Data analysis included descriptive analysis, Student's t-test, Mann-Whitney U, chi-square, and Fisher tests. RESULTS: The main types of CAM used were herbal medicine, and chamomile was the most commonly used. To improve the state of well-being was the main reason for use, the attributable benefit of CAM was high, and only a low percentage of users reported side effects. Only 31.8% of the users informed their physicians. CONCLUSION: The use of CAM is popular among renal patients, and physicians are not adequately informed; in particular, the CAM type ingested represents a risk for drug interactions and toxicity.
RESUMO
Background: Intensive care units (ICU) are the epicenter of antimicrobial resistance (AMR), and patients' infections are mainly caused by Gram-negative bacteria (GNB). Objective: To describe the frequency and trends in AMR of GNB deriving from the clinical samples of ICU patients at a tertiary care hospital in Mérida, Yucatán. Material and methods: Study which included the review of laboratory reports of all bacteriological samples collected from patients admitted to neonatal, pediatric and adult ICU from January 1 2019 to December 31 2021. Results: 433 GNB isolates were recovered, with Klebsiella pneumoniae being the most predominant isolate (n = 117; 27.02%). The majority of GNB were recovered from bronchial secretions (n = 163). Overall, GNB showed high resistance rates to ampicillin (89.48%), ampicillin/sulbactam (66.85%), cephalosporins (58.52-93.81%), tobramycin (58.06%), and tetracycline (61.73%). Among GNB, 73.90% and 68.53% exhibited multidrug-resistant, and highly resistant microorganisms' profiles, respectively, and 47.54% of Acinetobacter baumannii exhibited an extensively drug-resistant profile. A total of 80.33% of A. baumannii was carbapenem-resistant, and 83.76% of K. pneumoniae strains were ESBL-producing. Conclusion: Our data could be helpful to improve the empirical therapy and the infection-control program.
Introducción: las unidades de cuidados intensivos (UCI) son el epicentro de la resistencia a los antimicrobianos (RAM) y las infecciones en estas áreas son causadas principalmente por bacterias Gram-negativas (BGN). Objetivo: describir la frecuencia y los patrones de RAM en BGN aisladas de muestras clínicas de pacientes de las UCI de un hospital de tercer nivel en Mérida, Yucatán. Material y métodos: estudio que incluyó la revisión de los reportes de laboratorio de las muestras bacteriológicas obtenidas de pacientes ingresados en las UCI neonatal, pediátrica y adulta del 1 de enero de 2019 al 31 de diciembre de 2021. Resultados: se identificaron 433 BGN y Klebsiella pneumoniae fue el patógeno más prevalente (n = 117; 27.02%). La mayoría de las BGN aisladas se obtuvieron de secreciones bronquiales (n = 163). En general, las BGN mostraron altas tasas de resistencia a ampicilina (89.48%), ampicilina/sulbactam (66.85%), cefalosporinas (58.52-93.81%), tobramicina (58.06%) y tetraciclina (61.73%). El 73.90% y el 68.53% de las BGN exhibieron perfiles multidrogorresistentes y microorganismos altamente resistentes a fármacos, respectivamente, y 47.54% de los aislamientos de Acinetobacter baumannii mostró perfil de drogorresistencia extendida. El 80.33% de los A. baumannii fue resistente a carbapenémicos y el 83.76% de las K. pneumoniae fueron productoras de BLEE. Conclusión: nuestros datos podrían mejorar la terapia antimicrobiana empírica y el programa de control de infecciones.
Assuntos
Infecções por Bactérias Gram-Negativas , Adulto , Recém-Nascido , Humanos , Criança , Infecções por Bactérias Gram-Negativas/tratamento farmacológico , Centros de Atenção Terciária , Bactérias Gram-Negativas , Unidades de Terapia Intensiva , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Ampicilina/uso terapêutico , Testes de Sensibilidade Microbiana , Farmacorresistência Bacteriana MúltiplaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The bark of Matayba oppositifolia (A. Rich.) Britton (commonly known as "huaya" or "palo huacax") is commonly utilized in traditional Mayan medicine for treating diarrhea and for canker and other sores. AIM OF THE STUDY: The aim of this study was to investigate the in-vitro antimicrobial activity of M. oppositifolia bark extracts against drug-susceptible and -resistant ESKAPE-E pathogens. In addition, the phytochemical composition of the best antibacterial extract was analyzed. MATERIALS AND METHODS: The bark extracts were prepared with different solvents, including water, n-hexane, ethyl acetate and methanol. These were tested against ESKAPE-E (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa and Enterobacter spp., including Escherichia coli) strains using Resazurin Microtiter Assay. In addition, the composition of the most active extract was analyzed by GC-MS. RESULTS: The aqueous and organic bark extracts showed activity on drug-susceptible and -resistant ESKAPE-E microbes (MIC = 1000-31.25 µg/mL). The n-hexane bark extract was more active against the superbugs carbapenem-resistant K. pneumoniae (MIC = 500-31.25 µg/mL) and A. baumannii (MIC = 250-125 µg/mL). The GC-MS analysis of this extract allowed the identification of 12 phytochemicals as the potential antibacterial compounds. The major compounds identified were palmitic acid (1), friedelan-3-one (2) and 7-dehydrodiosgenin (3). CONCLUSION: The present study reveals the strong in-vitro antibacterial activity of the n-hexane extract from the bark of M. oppositifolia and demonstrates the potential of natural products as a source of antibacterial compounds or phytomedicines that are specifically effective against drug-resistant ESKAPE-E bugs. Additionally, our investigation contributes to the ethnopharmacological knowledge and reappraisal of Mayan medicinal flora, as well as supports the traditional use of the bark of the medicinal plant M. oppositifolia for the treatment of infectious diseases.
Assuntos
Antibacterianos , Plantas Medicinais , Antibacterianos/química , Antibacterianos/farmacologia , Bactérias , Carbapenêmicos/farmacologia , Escherichia coli , Hexanos , Klebsiella pneumoniae , Metanol/farmacologia , Testes de Sensibilidade Microbiana , Ácido Palmítico , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Sapindaceae , Solventes/farmacologia , Água/farmacologiaRESUMO
Mexico's Yucatan Peninsula is an endemic area of cutaneous leishmaniasis, locally known as the chiclero's ulcer, and Mayan traditional medicine which refers to the use of Thouinia paucidentata Radlk, known as k'an chuunup. Aqueous and organic leaves extracts were evaluated against promastigotes and amastigotes of Leishmania mexicana. Toxicity tests of extracts were performed using Vero and J774A.1 macrophage cell lines. The composition of the most active extracts was analysed by GC-MS. The n-hexane and ethyl acetate extracts showed potent anti-Leishmania activity against the promastigote form, and remarkably, n-hexane extract exhibited potent activity against the amastigote form. Both extracts showed low toxicity on Vero both not on J774A.1 cells. Analysis of both bioactive extracts identified as more abundant compounds, germacrene D-4-ol and thunbergen in n-hexane, and thunbergol in ethyl acetate extracts. Our study presents T. paucidentata as anti-Leishmania phytomedicine supporting its medicinal use and contributes to the understanding of its phytochemical composition.
RESUMO
We analyzed the antimycobacterial activity of the hexane extract of rhizomes from Aristolochia elegans. Some compounds of this extract were purified and tested against a group of drug-resistant Mycobacterium tuberculosis strains. We also evaluated their antiprotozoal activities. The hexane extract was active against M. tuberculosis H37Rv at a MIC = 100 µg mL(-1); the pure compounds eupomatenoid-1, fargesin, and (8R,8'R,9R)-cubebin were active against M. tuberculosis H37Rv (MIC = 50 µg mL(-1)), while fargesin presented activity against three monoresistant strains of M. tuberculosis H37Rv and a MDR clinical isolate of M. tuberculosis (MIC < 50 µg mL(-1)). Both the extract and eupomatenoid-1 were very active against E. histolytica and G. lamblia (IC(50) < 0.624 µg mL(-1)); in contrast, fargesin and (8R,8'R,9R)-cubebin were moderately active (IC(50) < 275 µg mL(-1)). In this context, two compounds responsible for the antimycobacterial presented by A. elegans are fargesin and cubebin, although others may exert this activity also. In addition to the antimycobacterial activity, the hexane extract has important activity against E. histolytica and G. lamblia, and eupomatenoid-1 is one of the compounds responsible for the antiparasite activity.
RESUMO
Rubus liebmannii is an endemic species from Mexico used in traditional medicine primarily to treat dysentery and cough. The in vitro activity against Giardia lamblia and Entamoeba histolytica that produces the ethanolic extract of the aerial parts of the plant led us to expand the pharmacological and phytochemical research of this species. Gastrointestinal disorders including amebiasis remain one of the health problems that need to be addressed and it is of interest to find alternatives that improve their treatment. Also, it is important to emphasize that R. liebmannii grows wild in the country and is not found in abundance; therefore, alternatives that avoid overexploitation of the natural resource are mandatory. Ongoing with the evaluation of the potentialities that R. liebmannii possesses for treating infectious gastrointestinal diseases, the aim of the present study was to evaluate the biological effects and the chemical composition of the micropropagated plant.
RESUMO
Urinary tract infections (UTI) are a severe public health problem and are caused mainly by the uropathogenic Escherichia coli (UPEC). Antimicrobial resistance and limited development of new antimicrobials have led to the reuse of old antibiotics such as fosfomycin. The aim of this study was to evaluate the in vitro efficacy of fosfomycin on a collection of multidrug-resistant (MDR) UPEC and the degradative activity on biofilm producers. A total of 100 MDR UPEC clinical isolates were collected from patients at Mexican second- and third-level hospitals. Microorganism identification was performed using an automated system, the evaluation of the susceptibility of clinical isolates to fosfomycin was performed using the resazurin microtiter assay, and the identification of biofilm producers and the effect of fosfomycin in biofilms were evaluated using the crystal violet method. Among planktonic MDR UPEC, 93% were susceptible to fosfomycin. Eighty-three MDR UPEC were categorized as weak (39.8%), moderate (45.2%), and strong (14.5%) biofilm producers. Fosfomycin exhibited degradative activity ranging from 164.4 µg/mL to 1045 µg/mL. Weak producers required statistically lower concentrations of fosfomycin to destroy the biofilm, contrary to moderate and strong producers. In conclusion, fosfomycin could be an option for the treatment of infections caused by MDR UPEC, for which the antimicrobial treatment is more often becoming limited.
RESUMO
During the coronavirus disease 2019 (COVID-19) pandemic, the emergence and rapid increase of the B.1.1.7 (Alpha) lineage of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), first identified in the United Kingdom in September 2020, was well documented in different areas of the world and became a global public health concern because of its increased transmissibility. The B.1.1.7 lineage was first detected in Mexico during December 2020, showing a slow progressive increase in its circulation frequency, which reached its maximum in May 2021 but never became predominant. In this work, we analyzed the patterns of diversity and distribution of this lineage in Mexico using phylogenetic and haplotype network analyses. Despite the reported increase in transmissibility of the B.1.1.7 lineage, in most Mexican states, it did not displace cocirculating lineages, such as B.1.1.519, which dominated the country from February to May 2021. Our results show that the states with the highest prevalence of B.1.1.7 were those at the Mexico-U.S. border. An apparent pattern of dispersion of this lineage from the northern states of Mexico toward the center or the southeast was observed in the largest transmission chains, indicating possible independent introduction events from the United States. However, other entry points cannot be excluded, as shown by multiple introduction events. Local transmission led to a few successful haplotypes with a localized distribution and specific mutations indicating sustained community transmission. IMPORTANCE The emergence and rapid increase of the B.1.1.7 (Alpha) lineage of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) throughout the world were due to its increased transmissibility. However, it did not displace cocirculating lineages in most of Mexico, particularly B.1.1.519, which dominated the country from February to May 2021. In this work, we analyzed the distribution of B.1.1.7 in Mexico using phylogenetic and haplotype network analyses. Our results show that the states with the highest prevalence of B.1.1.7 (around 30%) were those at the Mexico-U.S. border, which also exhibited the highest lineage diversity, indicating possible introduction events from the United States. Also, several haplotypes were identified with a localized distribution and specific mutations, indicating that sustained community transmission occurred in the country.
Assuntos
COVID-19 , SARS-CoV-2 , COVID-19/epidemiologia , Genoma Viral , Humanos , México/epidemiologia , Filogenia , SARS-CoV-2/genéticaRESUMO
Bioactivity-guided fractionation of the methanolic root bark extract of Leucophyllum frutescens led to the identification of leubethanol (1), a new serrulatane-type diterpene with activity against both multi-drug-resistant and drug-sensitive strains of virulent Mycobacterium tuberculosis. Leubethanol (1) was identified by 1D/2D NMR data, as a serrulatane closely related to erogorgiane (2), and exhibited anti-TB activity with minimum inhibitory concentrations in the range 6.25-12.50 µg/mL. Stereochemical evidence for 1 was gleaned from 1D and 2D NOE experiments, from 1H NMR full spin analysis, and by comparison of the experimental vibrational circular dichroism (VCD) spectrum to density functional theory calculated VCD spectra of two diastereomers.
Assuntos
Antituberculosos/isolamento & purificação , Antituberculosos/farmacologia , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Scrophulariaceae/química , Antituberculosos/química , Dicroísmo Circular , Diterpenos/química , México , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Casca de Planta/química , Raízes de Plantas/químicaRESUMO
The efficacy of decoction in extracting mycobactericidal compounds from Flourensia cernua (Hojasé) leaves and fractionation with solvents having ascending polarity was compared with that of (i) ethanol extraction by still maceration, extraction with a Soxhlet device, shake-assisted maceration, or ultrasound-assisted maceration, followed by fractionation with n-hexane, ethyl acetate, and n-butanol; (ii) sequential extraction with n-hexane, ethyl acetate, and n-butanol, by still maceration, using a Soxhlet device, shake-assisted maceration, or ultrasound-assisted maceration. The in vitro mycobactericidal activity of each preparation was measured against drug-sensitive (SMtb) and drug-resistant (RMtb) Mycobacterium tuberculosis strains. The results of which were expressed as absolute mycobactericidal activity (AMA). These data were normalized to the ΣAMA of the decoction fraction set. Although decoction was inactive, the anti-RMtb normalized ΣAMA (NAMA) of its fractions was comparable with the anti-RMtb NAMA of the still maceration extracts and significantly higher than the anti-SMtb and anti-RMtb NAMAs of every other ethanol extract and serial extract and fraction. Hexane extracted, from decoction, material having 55.17% and 92.62% of antituberculosis activity against SMtb and RMtb, respectively. Although the mycobactericidal activity of decoction is undetectable; its efficacy in extracting F. cernua active metabolites against M. tuberculosis is substantially greater than almost all pharmacognostic methods.