RESUMO
An EBNA1-specific small molecule (JLP2) has been synthesised. As a strong binder and dimerization inhibitor of EBNA1 in vitro, JLP2 may be used as a selective luminescent agent for the imaging and inhibition of latent EBV-infected cancer cells.
Assuntos
Antígenos Nucleares do Vírus Epstein-Barr/química , Herpesvirus Humano 4/metabolismo , Compostos de Piridínio/química , Sítios de Ligação , Sobrevivência Celular/efeitos dos fármacos , Dimerização , Antígenos Nucleares do Vírus Epstein-Barr/metabolismo , Células HeLa , Humanos , Microscopia Confocal , Simulação de Acoplamento Molecular , Estrutura Terciária de Proteína , Compostos de Piridínio/metabolismo , Compostos de Piridínio/toxicidadeRESUMO
A porphyrin ytterbium complex (Yb-N) showed strong binding to phosphatidylserine and capability to differentiate cancer cells via targeting the anionic phospholipid membrane.
Assuntos
Complexos de Coordenação/química , Fosfatidilserinas/metabolismo , Porfirinas/química , Itérbio/química , Ânions/química , Células HeLa , Humanos , Microscopia ConfocalRESUMO
Endocrine disrupting chemicals (EDCs) consist of a diverse group of industrial chemicals and pharmacological agents. The use of instrumental analyses as the first screening tool might not be cost-effective to identify the existence of enormous numbers of chemical contaminants in environments. Also, knowledge of the concentration of individual residues is difficult to use to evaluate biological impacts of contaminants to wildlife and humans. The primary objective of the present study was to develop and to test the feasibility of using a battery of exposure biomarkers for the rapid-screening of various endocrine disrupting activities present in food. The measurement of the EDC-elicited activities involved various (i) receptor-mediated responses, including androgenic, estrogenic, dioxin-like, glucocorticoid-like, progesterone-like, peroxisome proliferator-like and retinoid-like as well as (ii) the non-receptor mediated responses through modulation of cellular reactive oxygen species (ROS) and ATP content. Samples of both local and imported pork, beef and chicken as well as freshwater and seawater fishes were collected. Extracts of different foods exhibited various dioxin-like and "hormonal" activities. Fish and chicken skin were found to be the major source of exogenous "hormonal" and dioxin-like substances in diets. Extracts of beef and pork contained lesser potencies of hormonally-active agents. Our data suggest that the proposed EDC-screening platform may be useful in a risk assessment for the routine monitoring of EDCs in foods. Continuous monitoring and research is warranted to assess the physiological consequences of the consumption.