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1.
Chem Biodivers ; 21(3): e202301645, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38235946

RESUMEN

This study examines the potential of herniarin from tarragon, as an agent with multifaceted effects on bladder cancer cells and investigates herniarin's impact on cell viability, migration, cell cycle regulation, apoptosis induction, and Erk signaling pathways in bladder cancer cell lines, including RT-112 (grade 1, non-invasive), HTB9 (grade 2, invasive), and HT1376 (grade 3, invasive), through comprehensive in vitro experiments. The compound causes cell cycle arrest at distinct phases in different cell lines: G1/S arrest in RT112 cells, G2/M arrest in HTB9 cells, and S phase arrest in HT1376 cells. Furthermore, herniarin induces caspase-mediated apoptosis in various cell lines and simultaneously modulates protein levels of apoptotic and anti-apoptotic proteins, indicating its potential as a therapeutic agent. Herniarin's influence also extends to Erk signaling, a crucial pathway that regulates cell growth and differentiation. In conclusion, this study reveals herniarin's potential as a versatile agent in the treatment of bladder cancer.


Asunto(s)
Apoptosis , Umbeliferonas , Neoplasias de la Vejiga Urinaria , Humanos , Supervivencia Celular , Línea Celular Tumoral , Puntos de Control de la Fase G2 del Ciclo Celular , Ciclo Celular , Neoplasias de la Vejiga Urinaria/tratamiento farmacológico , Neoplasias de la Vejiga Urinaria/metabolismo , Proliferación Celular , Puntos de Control del Ciclo Celular
2.
J Enzyme Inhib Med Chem ; 34(1): 459-464, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30734593

RESUMEN

Head and neck cancer (HNC) is one of the most common malignancies in the world. HNC is a group of cancers that starts in the mouth, nose, throat, larynx, sinuses, or salivary glands. According to this section of the body parts; induction of cancer can be associated with CO2 and oxidative stress. The aim of this study is to assess the activities of carbonic anhydrase (CA), catalase (CAT), paraoxonase1 (PON1), and xanthine oxidase (XO) activities in 89 HNC patients and 115 healthy volunteers. Paraoxonase1 activity was found lower in HNC cancer patients. There is no statistically significant difference between patients and controls for catalase, carbonic anhydrase, and xanthine oxidase enzyme levels. According to this results, paraoxonase1 levels could be a candidate as an oxidative marker in HNC patients, but further studies are needed to investigate the other type of cancer related PON1 and the other enzyme levels.


Asunto(s)
Arildialquilfosfatasa/metabolismo , Biomarcadores de Tumor/metabolismo , Dióxido de Carbono/metabolismo , Anhidrasas Carbónicas/metabolismo , Catalasa/metabolismo , Neoplasias de Cabeza y Cuello/metabolismo , Xantina Oxidasa/metabolismo , Arildialquilfosfatasa/sangre , Biomarcadores de Tumor/sangre , Dióxido de Carbono/sangre , Anhidrasas Carbónicas/sangre , Catalasa/sangre , Femenino , Neoplasias de Cabeza y Cuello/sangre , Voluntarios Sanos , Humanos , Masculino , Persona de Mediana Edad , Estrés Oxidativo , Xantina Oxidasa/sangre
3.
J Enzyme Inhib Med Chem ; 31(6): 1306-11, 2016 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-26745009

RESUMEN

Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the fundamental reaction of CO2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological conditions. A series of benzothiazole-based sulfonamides were synthesized and tested as possible CA inhibitors. Their inhibitory activity was assessed against the cytosolic human isoforms hCA I and hCA II and the transmembrane hCA IX and hCA XII. Several of the investigated derivatives showed interesting inhibition activity and selectivities for inhibiting hCA IX and hCA XII over the off-target ones hCA I and hCA II. Furthermore, computational procedures were used to investigate the binding mode of this class of compounds, within the active site of hCA IX.


Asunto(s)
Benzotiazoles/química , Inhibidores de Anhidrasa Carbónica/farmacología , Anhidrasas Carbónicas/efectos de los fármacos , Isoenzimas/antagonistas & inhibidores , Sulfonamidas/química , Inhibidores de Anhidrasa Carbónica/química , Simulación del Acoplamiento Molecular
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