Fisetin, a flavonoid compound commonly present in fruits and vegetables, can exert anti-inflammation activities via inhibition of the NF-κB-signaling pathway. This study aims to evaluate the antiasthma activity of fisetin and investigate its possible molecular mechanisms. We found that fisetin attenuated lung inflammation, goblet cell hyperplasia, and airway hyperresponsiveness in ovalbumin-induced asthma and decreased eosinophils and lymphocytes in bronchoalveolar lavage fluid. Fisetin treatment reduced expression of the key initiators of allergic airway inflammation (eotaxin-1 and TSLP), Th2-associated cytokines (IL-4, IL-5, and IL-13) in lungs, and Th2-predominant transcription factor GATA-3 and cytokines in thoracic lymph node cells and splenocytes. Notably, fisetin treatment impaired NF-κB activation in OVA-stimulated lung tissues and TNF-α-stimulated bronchial epithelial cells. Collectively, this study demonstrated the beneficial effect of fisetin in the amelioration of asthmatic phenotypes. The antiasthma activity of fisetin is associated with reduction of Th2 responses as well as suppression of NF-κB and its downstream chemokines.

The monitoring of alkaline phosphatase (ALP) activity in different tissues is significant for disease diagnosis and therapy. However, the time-resolved in vivo sensing of ALP activity remained unresolved. Herein, a novel red–near-infrared fluorescent ALP probe (Cl2–BDCM-ALP) based on a dichloro-substituted dicyanomethylene-4H-chromene derivative was designed and synthesized with high fluorescence efficiency and stability under biological pH range. By using Cl2–BDCM-ALP, ALP activity under an acidic microenvironment such as a tumor site can be sensitively imaged, which cannot be achieved by some previously reported ALP probes. By further loading the Cl2–BDCM-ALP into a near-infrared (NIR) light-responsive nanocontainer, time-resolved long-term imaging of ALP activity was facilely achieved with noninvasive NIR light remote control. Time-resolved variation of ALP activity of the drug-induced acute liver injury mice was successfully monitored in vivo for the first time. This strategy holds great promise in the in situ ALP detection under a broad pH range with temporal resolution.

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