Recently, we identified magnolol bioinspired derivatives as new Tankyrase 1/2 (TNKS1/2) inhibitors by our Inverse Virtual Screening protocol. Based on these findings, in the present contribution, we enlarged our investigation of neolignans to the natural product honokiol (1) and a group of its analogues (2-8). By integrating in silico analysis and Surface Plasmon Resonance experiments, we investigated the binding of tested compounds against biological target under investigations.
View Article and Find Full Text PDFMetformin is a widely employed drug in type 2 diabetes. In addition to warranting good short- and long-term glycemic control, metformin displays many intriguing properties as protection against cardiovascular and neurodegenerative diseases, anti-tumorigenic and longevity promotion. In addition to being a low-cost drug, metformin is generally well tolerated.
View Article and Find Full Text PDFWorkplaces cause employees to adopt sedentary behaviors for most of their daytime, negatively impacting psychophysical health. A new office concept (UP150) was designed to reduce sedentary behaviors at work through architectural changes, proactive technologies, and wellness coaches (education to active lifestyles). The present study examined the effects of the UP150 concept, previously investigated in dedicated workspaces, with a 12-month longitudinal trial in a real worksite environment.
View Article and Find Full Text PDFThe breast cancer resistance protein (BCRP/ABCG2) transporter mediates the efflux of numerous antineoplastic drugs, playing a central role in multidrug resistance related to cancer. The absence of successful clinical trials using specific ABCG2 inhibitors reveals the urge to identify new compounds to attend this critical demand. In this work, a series of 13 magnolol derivatives was tested as ABCG2 inhibitors.
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