RESUMEN
We developed a nitroreductase responsive theranostic probe 1; it comprises biotinylated rhodol in conjunction with p-nitrobenzyl functionality. The probe 1 showed a remarkable fluorescence 'turn-on' signal in the presence of nitroreductase under physiological conditions. The probe is considerably stable within a wide biological pH range (6-8) and also is very sensitive toward a reducing micro-environment e.g. liver microsome. Further, it enables providing cellular and in vivo nematode images in a reducing microenvironment.
Asunto(s)
Biotina/análogos & derivados , Biotina/farmacología , Colorantes Fluorescentes/farmacología , Hipoxia/diagnóstico por imagen , Nitrorreductasas/metabolismo , Xantonas/farmacología , Animales , Biotina/síntesis química , Biotina/toxicidad , Caenorhabditis elegans , Línea Celular Tumoral , Fluorescencia , Colorantes Fluorescentes/síntesis química , Colorantes Fluorescentes/química , Colorantes Fluorescentes/toxicidad , Humanos , Lepidópteros , Límite de Detección , Microsomas Hepáticos/metabolismo , Piperazinas/síntesis química , Piperazinas/química , Piperazinas/farmacología , Piperazinas/toxicidad , Ratas , Nanomedicina Teranóstica , Xantonas/síntesis química , Xantonas/química , Xantonas/toxicidadRESUMEN
OBJECTIVE: To investigate the effects of Artemisia lavandulaefolia essential oil on apoptosis and necrosis of HeLa cells. METHODS: Cell viability was assayed using MTT method. The morphological and structure alterations in HeLa cells were observed by microscopy. Furthermore, cell apoptosis was measured by DNA Ladder and flow cytometry. DNA damage was measured by comet assay, and the protein expression was examined by Western blot analysis. RESULTS: MTT assay displayed essential oil from Artemisia lavandulaefolia could inhibit the proliferation of HeLa cells in a dose-dependent manner. After treated with essential oil of Artemisia lavadulaefolia for 24 h, HeLa cells in 100 and 200 microg/mL experiment groups exhibited the typical morphology changes of undergoing apoptosis, such as cell shrinkage and nucleus chromatin condensed. However, the cells in the 400 microg/mL group showed the necrotic morphology changes including cytomembrane rupture and cytoplasm spillover. In addition, DNA Ladder could be demonstrated by DNA electrophoresis in each experiment group. Apoptosis peak was also evident in flow cytometry in each experiment group. After treating the HeLa cells with essential oil of Artemisia lavadulaefolia for 6 h, comet tail was detected by comet assay. Moreover, western blotting analysis showed that caspase-3 was activated and the cleavage of PARP was inactivated. CONCLUSION: Essential oil from Artemisia lavadulaefolia can inhibit the proliferation of HeLa cells in vitro. Low concentration of essential oil from Artemisia lavadulaefolia can induce apoptosis, whereas high concentration of the compounds result in necrosis of HeLa cells. And,the mechanism may be related to the caspase-3-mediated-PARP apoptotic signal pathway.