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1.
Bioorg Med Chem Lett ; 108: 129796, 2024 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-38754563

RESUMEN

In this work, we report 14 novel quinazoline derivatives as immune checkpoint inhibitors, IDO1 and PD-L1. The antitumor screening of synthesized compounds on ovarian cancer cells indicated that compound V-d and V-l showed the most activity with IC50 values of about 5 µM. Intriguingly, compound V-d emerges as a stand out, triggering cell death through caspase-dependent and caspase-independent manners. More importantly, V-d presents its ability to hinder tumor sphere formation and re-sensitized cisplatin-resistant A2780 cells to cisplatin treatment. These findings suggest that compound V-d emerges as a promising lead candidate for the future development of immuno anticancer agents.


Asunto(s)
Antineoplásicos , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Inhibidores de Puntos de Control Inmunológico , Quinazolinas , Humanos , Quinazolinas/farmacología , Quinazolinas/química , Quinazolinas/síntesis química , Relación Estructura-Actividad , Inhibidores de Puntos de Control Inmunológico/farmacología , Inhibidores de Puntos de Control Inmunológico/síntesis química , Inhibidores de Puntos de Control Inmunológico/química , Antineoplásicos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Estructura Molecular , Línea Celular Tumoral , Relación Dosis-Respuesta a Droga , Proliferación Celular/efectos de los fármacos , Indolamina-Pirrol 2,3,-Dioxigenasa/antagonistas & inhibidores , Indolamina-Pirrol 2,3,-Dioxigenasa/metabolismo , Antígeno B7-H1/antagonistas & inhibidores , Antígeno B7-H1/metabolismo
2.
Nat Prod Res ; 38(11): 1864-1873, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38739563

RESUMEN

Phytochemical studies of the stems and leaves of Stephania dielsiana Y.C.Wu yielded two new aporphine alkaloids (1 and 5), along with six known alkaloids (2-4 and 6-8). Their structures were characterised based on analyses of spectroscopic data, including one- and two-dimensional nuclear magnetic resonance (NMR) spectroscopy and high-resolution electrospray ionisation mass spectrometry (HR-ESI-MS). The cytotoxic activities of the isolated compounds against a small panel of tumour cell lines were assessed by MTS assay. Interestingly, compound 2 exhibited particularly strong cytotoxic activities against HepG2, MCF7 and OVCAR8 cancer cell lines, with IC50 values of 3.20 ± 0.18, 3.10 ± 0.06 and 3.40 ± 0.007 µM, respectively. Furthermore, molecular docking simulations were carried out to explore the interactions and binding mechanisms of the most active compound (compound 2) with proteins. Our results contribute to understanding the secondary metabolites produced by S. dielsiana and provide a scientific rationale for further investigations of cytotoxicity of this valuable medicinal plant.


Asunto(s)
Alcaloides , Antineoplásicos Fitogénicos , Aporfinas , Simulación del Acoplamiento Molecular , Hojas de la Planta , Tallos de la Planta , Stephania , Aporfinas/química , Aporfinas/farmacología , Humanos , Hojas de la Planta/química , Tallos de la Planta/química , Alcaloides/química , Alcaloides/farmacología , Stephania/química , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/química , Estructura Molecular , Línea Celular Tumoral , Células Hep G2 , Células MCF-7 , Ensayos de Selección de Medicamentos Antitumorales , Espectroscopía de Resonancia Magnética , Plantas Medicinales/química
3.
Cureus ; 16(5): e60746, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38903303

RESUMEN

Telepharmacy is receiving significant attention as an innovative approach. The objective of this study is to assess the needs and evaluate the impact of telepharmacy applications in drug consultations at Thu Duc City Hospital. We used a cross-sectional research design and conducted a survey with the participation of leaders of the Faculty of Pharmacy, clinical pharmacists, dispensing pharmacists, and patients or their caregivers who receive medication at the Pharmacy of Thu Duc Hospital. We deployed a telepharmacy application for consulting on drug use and surveyed the satisfaction of patients/family members with the telepharmacy model. 60.3% of survey subjects expressed a desire to receive drug use consultations through telepharmacy if the hospital were to offer this service. One hundred percent of the pharmacists at the pharmacy and the hospital's leadership believe that telepharmacy can address patient consultation needs and improve the current physical facilities in the dispensing area. Over 90% of telepharmacy users reported being satisfied or very satisfied with the service. Telepharmacy has garnered the attention of patients, their caregivers, and the medical staff at the Outpatient Pharmacy of Thu Duc Hospital. The majority of users are satisfied with the drug use consultation service provided by telepharmacy. By expanding the good results of Thu Duc Hospital to other hospitals, more patients across Vietnam can benefit from this innovative approach.

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