RESUMEN
BACKGROUND: We investigated the associations between the different doses of tigecycline, its efficacy and safety, and the role of tigecycline therapeutic drug monitoring for patients in the intensive care unit. METHODS: This study was a single-center cohort including patients infected with multidrug-resistant Acinetobacter baumannii (MDR-AB) and multidrug-resistant Klebsiella pneumoniae (MDR-KP) causing pulmonary infections. The steady-state plasma concentration after tigecycline administration was determined by High-Performance Liquid Chromatography (HPLC) in patients admitted to the ICU between October 2020 and December 2021. Multivariate analyses of tigecycline's clinical efficacy and safety were performed to control confounding factors. RESULTS: For this study, we included 45 patients and 45 blood samples to determine steady-state trough concentrations of tigecycline. All patients were divided into the High Dose (HD) and Standard Dose (SD) groups. The median trough concentration of tigecycline was 0.56 µg/mL in the HD group, which was higher than in the SD group (0,21 µg/mL), p = 0.000. There was no significant difference between the two groups of patients in terms of bacterial eradication rate, mortality rate, and clinical efficacy. Multiple regression analysis showed that the ICU days were correlated with mortality OR 1.030(1.005-1.056), p = 0.017. APACHE II was significantly associated with clinical efficacy OR 0.870(0.755-1.002), p = 0.045. The level of fibrinogen decline in the HD group was significantly higher than in the SD group (-3.05 ± 1.67 vs -1.75 ± 1.90), p = 0.038. We identified that age and tigecycline treatment duration influenced fibrinogen decline. CONCLUSIONS: Tigecycline plasma concentrations are significantly increased when using a high dose. However, the plasma concentration of tigecycline is not correlated with clinical efficacy and adverse reactions. Fibrinogen decline appears to be related to the patient's age and days of tigecycline. Large sample data are still needed to confirm the clinical guidance significance of tigecycline TDM.
Asunto(s)
Acinetobacter baumannii , Neumonía Bacteriana , Humanos , Tigeciclina/farmacología , Antibacterianos/uso terapéutico , Antibacterianos/farmacología , Carbapenémicos/uso terapéutico , Carbapenémicos/farmacología , Monitoreo de Drogas , Estudios Retrospectivos , Neumonía Bacteriana/tratamiento farmacológico , Resultado del Tratamiento , Bacterias Gramnegativas , Unidades de Cuidados Intensivos , Fibrinógeno , Farmacorresistencia Bacteriana Múltiple , Minociclina/uso terapéuticoRESUMEN
Chemical examination of the gum-resin of Boswellia carterii resulted in the isolation and characterization of eighteen new cembrane-type diterpenoids, named as Boscartins P-AG (1-18) and eight known ones. Their structures were established on the basis of extensive spectroscopic (2D NMR, IR, CD, MS and X-ray) analysis in combination with modified Mosher's method. All compounds featured unusual 1,12-oxygenated tetrahydrofuran functionalities, and were evaluated for hepatoprotective activity against D-galactosamine-induced HL-7702 cell damage and cytotoxic activity against MCF-7 human breast cancer cell in vitro. Compounds 1, 6-10, 12-13, 16-17 and 21-25 (10⯵M) showed some hepatoprotective activity against D-galactosamine-induced HL-7702 cell damage.
Asunto(s)
Boswellia/química , Diterpenos/farmacología , Resinas de Plantas/química , Línea Celular , China , Diterpenos/aislamiento & purificación , Humanos , Células MCF-7 , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacologíaRESUMEN
Ten tirucallane-type triterpenes named boscartene A-J and a nor-tetracyclic triterpene boscartene K, together with ten known compounds were isolated from the gum resin of Boswellia carterii Birdw. Their structures and absolute configurations were elucidated by extensive spectroscopic analysis. In vitro assay, some of these compounds (10 µM) showed moderate hepatoprotective activities against d-galactosamine-induced HL-7702 cell damage.
Asunto(s)
Boswellia/química , Hepatocitos/efectos de los fármacos , Resinas de Plantas/química , Triterpenos/química , Línea Celular , Citoprotección , Galactosamina/efectos adversos , Humanos , Estructura Molecular , Triterpenos/aislamiento & purificaciónRESUMEN
Eight new cembranoids, boscartins A-H (1, 2, and 4-9), and the known incensole oxide were isolated from the gum resin of Boswellia carterii. The absolute configurations of 1, 2, 4, and incensole oxide were unequivocally resolved using single-crystal X-ray diffraction analysis with Cu Kα radiation, and the absolute configuration of 5 was resolved via electronic circular dichroism data. The antiulcerative colitis activities of the compounds were evaluated in an in vitro x-box-binding protein 1 (XBP 1) transcriptional activity assay using dual luciferase reporter detection. At 10 µM, compounds 1, 5, 6, and 7 significantly activated XBP 1 transcription with EC50 values of 0.34, 1.14, 0.88, and 0.42 µM, respectively, compared with the pGL3-basic vector control.
Asunto(s)
Antiulcerosos/aislamiento & purificación , Antiulcerosos/farmacología , Boswellia/química , Colitis/tratamiento farmacológico , Diterpenos/aislamiento & purificación , Resinas de Plantas/química , Antiulcerosos/química , Cristalografía por Rayos X , Proteínas de Unión al ADN/efectos de los fármacos , Diterpenos/química , Conformación Molecular , Estructura Molecular , Factores de Transcripción del Factor Regulador X , Factores de Transcripción/efectos de los fármacosRESUMEN
Two new benzofurans, gymnefuranols A (1) and B (2), together with six known furanolignans (3-8), were isolated from Gymnema tingens. The structures of the new compounds were elucidated by comprehensive analysis of the NMR and HR-MS data. Compounds 1, 2, 6, and 7 showed hepatoprotective activities against D-galactosamine-induced HL-7702 cell damage.
Asunto(s)
Benzofuranos/aislamiento & purificación , Benzofuranos/farmacología , Gymnema/química , Lignanos/aislamiento & purificación , Lignanos/farmacología , Hígado/efectos de los fármacos , Benzofuranos/química , Galactosamina/farmacología , Lignanos/química , Estructura Molecular , Resonancia Magnética Nuclear BiomolecularRESUMEN
Three new sesquiterpenes (1-3) and two new rutinosides (4 and 5) along with 17 known compounds (6-22) were isolated from the leaves of Murraya koenigii (L.) Spreng. The new compounds were elucidated as (3R,5S,6R)-3,5,6-trihydroxy-1,1,5-trimethylcyclohexyl-8-butyn-9-one (1), (8E,9R)-ethyl-7-(3S,5R,6S)-3,6-dihydroxy-1,1,5-trimethylcyclohexyl-9-hydroxybut-8-enoate (2), (3R)-3-O-ß-D-glucoside-6'-D-apiose-ß-ionone (3), 4-O-ß-D-rutinosyl-3-methoxyphenyl-1-propanone (4), and 1-O-ß-D-rutinosyl-2(R)-ethyl-1-pentanol (5) based on their spectroscopic data. Compounds 1, 4, 5, 18, and 21 (10 µM) exhibited moderate hepatoprotective activities.
Asunto(s)
Hepatocitos/efectos de los fármacos , Murraya/química , Extractos Vegetales/química , Sustancias Protectoras/química , Rutina/química , Sesquiterpenos/química , Línea Celular , Humanos , Estructura Molecular , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Hojas de la Planta/química , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología , Rutina/aislamiento & purificación , Rutina/farmacología , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos/farmacologíaRESUMEN
Chemical examination of the exuded gum resin of Boswellia carterii resulted in the isolation of nine new prenylaromadendrane-type diterpenes, boscartols A-I (1-9). The structures of these compounds were established by extensive 1D and 2D NMR spectroscopic analyses, mass spectrometric data, and circular dichroism spectra. Compounds 1-3, 5, 6, 8, and 9 (10 µM) showed moderate hepatoprotective activity against d-galactosamine-induced HL-7702 cell damage.
Asunto(s)
Boswellia/química , Diterpenos/aislamiento & purificación , Diterpenos/farmacología , Hígado/efectos de los fármacos , Resinas de Plantas/farmacología , Triterpenos/aislamiento & purificación , Triterpenos/farmacología , Diterpenos/química , Galactosamina/farmacología , Encía/efectos de los fármacos , Humanos , Factores Inmunológicos , Hígado/metabolismo , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Resinas de Plantas/química , Triterpenos/químicaRESUMEN
Six new phenolic diglycosides, named gymnetinosides A-F (1-6), were isolated from the ethanolic extract of Gymnema tingens, together with three known diglycosides, sequinoside K (7), khaephuoside B (8), and albibrissinoside A (9). The structures of the new compounds were determined by spectroscopic techniques including 1D-, 2D NMR, mass spectroscopy, and circular dichroism. Compounds 1, 5, and 6 showed hepatoprotective activities against D-galactosamine-induced HL-7702 cell damage.
Asunto(s)
Gymnema/química , Sustancias Protectoras/química , Sustancias Protectoras/farmacología , Línea Celular/efectos de los fármacos , Dicroismo Circular , Evaluación Preclínica de Medicamentos/métodos , Galactosamina/toxicidad , Glicósidos/química , Glicósidos/farmacología , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Fenoles/química , Extractos Vegetales/análisis , Extractos Vegetales/química , Extractos Vegetales/farmacologíaRESUMEN
OBJECTIVE: To study the chemical constituents of Balaophora polyandra. METHODS: The chemical constituents were isolated by column chromatography on silica gel, Toyopearl HW-40C and Sephadex LH-20. Their structures were elucidated on the basis of spectral analysis. RESULTS: 8 compounds have isolated from this plant, and the structure of them have identified as Gallic acid (1), Ellagic acid (2), Ferulic acid (3), Caffeic acid (4), p-hydroxylcinnamic acid (5), 1,3-di-O-galloyl-4,6-(S) - hexahydroxydiphenyl-beta-D-glucopyrannose (6),1-O-(E) - caffeoyl- 3-O-galloyl-beta-D-glucopyrannose (7), 2-O-(E) - caffeoyl-1-O-[see symbol] - (E) - coumaroyl-beta-D-glucopyrannose (8). CONCLUSION: Compounds 1 - 8 are isolated from this plant for the first time.