RESUMEN
A series of new phenyl acetylene and isoxazole analogues of arjunolic acid were designed, synthesized and evaluated (3-8) for their tyrosinase and alpha glucosidase inhibitory potential. All the tested analogues exhibited stronger inhibitory activity than the standard drug or parent compound. Of these, compound (7) displayed the most potent tyrosinase inhibitory action with IC50 (14.3 ± 7.6) of about three folds more than the standard drug, kojic acid (41.5 ± 1.0). Further, compound (8) (14.5 ± 0.15) possessed the potent alpha glucosidase inhibitory action with IC50 value comparable to that of standard, acarbose (10.4 ± 0.06). Henceforth, compounds (7) and (8) are promising candidates for further studies.
Asunto(s)
Agaricales , Inhibidores de Glicósido Hidrolasas , Inhibidores de Glicósido Hidrolasas/farmacología , Monofenol Monooxigenasa , Estructura Molecular , Relación Estructura-Actividad , alfa-Glucosidasas/metabolismo , Simulación del Acoplamiento Molecular , Agaricales/metabolismo , Alquinos , Diseño de FármacosRESUMEN
ABSTRACT: The main aim of this study is to compare the use of non-invasive ventilation (NIV) via helmet versus face mask where different interfaces and masks can apply NIV. However, some of the limitations of the NIV face mask were air leak, face mask intolerance, and requirement of high positive end expiratory pressure, which could be resolved with the use of the helmet NIV. NIV facemask will be applied as per the facial contour of the patient. NIV helmet is a transparent hood and size will be measured as per the head size. Both groups will have a standard protocol for titration of NIV.Patients aged more than 18âyears old and diagnosed with acute respiratory distress syndrome as per Berlin definition will be enrolled in the study after signing the informed consent. Subjects who met the inclusion criteria will receive 1 of the 2 interventions; blood gases, oxygenation status [Po2/Fio2] will be monitored in both groups. The time of intubation will be the main comparison factor among the 2 groups. The primary and secondary outcomes will be measured by the number of patients requiring endotracheal intubation after application of helmet device, Improvement of oxygenation defined as PaO2/FiO2 ≥ 200 or increase from baseline by 100, duration of mechanical ventilation via an endotracheal tube, intensive care unit length of stay, death from any cause during hospitalization at the time of enrolment, need for proning during the hospital stay, intensive care unit mortality, and the degree to which overt adverse effects of a drug can be tolerated by a patient including feeding tolerance. TRIAL REGISTRATION NUMBER: NCT04507802. PROTOCOL VERSION: May 2020.
Asunto(s)
Dispositivos de Protección de la Cabeza , Máscaras , Ventilación no Invasiva/instrumentación , Síndrome de Dificultad Respiratoria/terapia , Adolescente , Adulto , Ensayos Clínicos Fase III como Asunto , Resultados de Cuidados Críticos , Femenino , Humanos , Unidades de Cuidados Intensivos , Tiempo de Internación , Masculino , Persona de Mediana Edad , Ensayos Clínicos Controlados Aleatorios como Asunto , Resultado del Tratamiento , Adulto JovenRESUMEN
The authors urge clinicians to observe for early signs of CMV reactivation in patients presenting with gastrointestinal bleeding and intestinal perforation after receiving tocilizumab or other immunosuppressive therapy as a treatment for COVID 19. Early recognition of CMV infection and treatment will prevent life-threatening bleeding and mortality.
RESUMEN
Three new isomeric corniculatolides (1, 2, and 3) with an unusual caffrane and isocorniculane framework, and five known metabolites were isolated from the chloroform extract of the stems of Xylocarpus granatum. The structures of the new metabolites were deduced as corniculatolide B (1), isocorniculatolide B (2), and corniculatolide C (3) by spectroscopic data analysis and a combination of chemical transformations and supported by single-crystal X-ray crystallographic data of 1 and 3. The isolated compounds were evaluated for their in vitro cytotoxicity and α-glucosidase (Saccharomyces cerevisiae) inhibitory potential. Compound 3 possessed α-glucosidase inhibitory activity with an IC50 value of 24.8 µM, whereas these rare macrolides showed no effect on the mammalian cancer cell lines MIAPaCa-2, DU145, MCF-7, and HTC-116.
Asunto(s)
Inhibidores de Glicósido Hidrolasas/química , Meliaceae/química , Cristalografía por Rayos X , Estructura MolecularRESUMEN
Chloral hydrate (CH) poisoning is not commonly seen in the emergency department. CH is a commonly prescribed sedative agent for various day care procedures despite its toxic profile even when other safe sedative medications are available. We report a case of CH poisoning that manifested with neurotoxicity followed by cardiotoxicity leading to cardiac arrest. With a high index of suspicion and proper management, our patient was discharged with normal neurological outcome. In this case report, we discuss CH poisoning and toxicity with highlights on specific intervention including ß-blockers. CH induced arrhythmias have been reported to be refractory to the standard antiarrhythmic medications and respond well to ß-blockers.