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1.
Spectrochim Acta A Mol Biomol Spectrosc ; 317: 124400, 2024 Sep 05.
Artículo en Inglés | MEDLINE | ID: mdl-38710139

RESUMEN

Eletriptan (ETR), a selective pharmaceutical agent agonist of the 5-hydroxytryptamine1 receptor subtype, are primarily used to treat acute migraine attacks. ETR is a triptan-class medication that works by narrowing cerebral blood vessels and reducing chemicals that produce headache pain, light and sound sensitivity, and nausea. Due to its effectiveness in reducing migraine symptoms, it is a worthwhile choice for those looking for quick and efficient treatment. A green, raid, one-pot and straightforward fluorescence spectrometric method was employed to evaluate ETR in tablets and biological samples. By introducing the ETR drug and the fluorescent ligand, Acid red 87, in an acidic buffer, a quenching of the ligand native fluorescent was promptly produced. The quenching action was simply attributed to the selective ion-pair complex generation between the cationic target and the selected ligand. An increase in ETR concentration was linearly proportional to the quenching response in the 50.0 - 500.0 ng/mL range. The optimal configurations for adjusting the system's variable parameters were determined by examining the ETR-Acid red 87 system's response. Additionally, the sensor that was developed met the standards set by the International Council for Harmonisation of Technical Requirements of Pharmaceuticals for Human Use. The sensitivity thresholds of the approach were 13.8 and 42.0 ng/mL for the detection and quantification parameters, respectively, LOD and LOQ. This approach proficiently evaluated the pharmaceutical and biological samples of ETR. Finally, the proposed approach not only simplifies the analysis process but also limits the badimpact on the environment, making it a promising technique for analytical applications.


Asunto(s)
Pirrolidinas , Espectrometría de Fluorescencia , Triptaminas , Triptaminas/análisis , Triptaminas/sangre , Triptaminas/química , Espectrometría de Fluorescencia/métodos , Humanos , Pirrolidinas/química , Tecnología Química Verde/métodos , Trastornos Migrañosos/tratamiento farmacológico , Comprimidos , Límite de Detección , Concentración de Iones de Hidrógeno
2.
Bioorg Chem ; 134: 106444, 2023 05.
Artículo en Inglés | MEDLINE | ID: mdl-36893547

RESUMEN

The present study established thirteen novel 8-hydroxyquinoline/chalcone hybrids3a-mof hopeful anticancer activity. According to NCI screening and MTT assay results, compounds3d-3f, 3i,3k,and3ldisplayed potent growth inhibition on HCT116 and MCF7 cells compared to Staurosporine. Among these compounds,3eand3fshowed outstanding superior activity against HCT116 and MCF7 cells and better safety toward normal WI-38 cells than Staurosporine. The enzymatic assay revealed that3e,3d, and3ihad goodtubulin polymerization inhibition (IC50 = 5.3, 8.6, and 8.05 µM, respectively) compared to the reference Combretastatin A4 (IC50 = 2.15 µM). Moreover,3e,3l, and3fexhibited EGFR inhibition (IC50 = 0.097, 0.154, and 0.334 µM, respectively) compared to Erlotinib (IC50 = 0.056 µM). Compounds3eand3fwere investigated for their effects on the cell cycle, apoptosis induction, andwnt1/ß-cateningene suppression. The apoptosis markers Bax, Bcl2, Casp3, Casp9, PARP1, and ß-actin were detected by Western blot. In-silico molecular docking, physicochemical, and pharmacokinetic studies were implemented for the validation of dual mechanisms and other bioavailability standards. Hence, Compounds3eand3fare promising antiproliferative leads with tubulin polymerization and EGFR kinase inhibition.


Asunto(s)
Antineoplásicos , Chalcona , Chalconas , Humanos , Simulación del Acoplamiento Molecular , Chalcona/química , Chalconas/farmacología , Tubulina (Proteína)/metabolismo , Relación Estructura-Actividad , Oxiquinolina/farmacología , Estaurosporina/farmacología , Apoptosis , Moduladores de Tubulina , Antineoplásicos/química , Receptores ErbB , Ensayos de Selección de Medicamentos Antitumorales , Proliferación Celular , Estructura Molecular
3.
J Egypt Soc Parasitol ; 46(3): 581-586, 2016 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30230755

RESUMEN

This cross sectional study in Aswan Governorate determined the prevalence of intestinal parasites and to identify the risk factors for infection in primary school children in this geographical area. The results would facilitate evaluation of the endemic level of different intestinal parasites and the determination of whether wiqespread or focal measures of parasite control are required. After obtaining official permission from the school administration, information and consent forms were given to the parents of all the schoolchildren. They were three-hundreds children aged between 6-12 year were enrolled; a detailed questionnaire, complete clinical assessment complete as well as stool analysis was done The study showed that the over-all infection was 31%, single parasitic infection was 26% and mixed one was 5%.The commonest helminthic infection was E. vermicularis 6.6% followed by H. nana 3% Ascaris lumbricoidesl%. The commonest protozoa infection was E. histolytica 8.3% followed by Giardia lamblia 3.7% and Cryptosporidium parvum 1.7%. Mixed infection was E. vernficularis plus E. histolytica (23.4%), E vermicularis plus G. lamblia (17.6%), E. vermicularis plus C. parvum (11.8%), E. histolytica plus H. nana (11.85%), A. -lumbricoides plus E. histolytica (17.6%) and G. lamblia plus E. histolytica in (11.8%). Parasitic infection was more prevalent in boys (53.8%) than girls (46.2%) and more prevalent in rural children (39.73%) than urban ones (20.13%) among age ranged from 6 to 12 years (8.97±1.72).


Asunto(s)
Helmintiasis/epidemiología , Helmintiasis/parasitología , Parasitosis Intestinales/epidemiología , Parasitosis Intestinales/parasitología , Niño , Egipto/epidemiología , Femenino , Humanos , Masculino
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