The controlled release of a molecule of interest(MOI) is useful in probe design, prodrug construction, and drugdelivery. We report herein a versatile thiol-triggeredfluorogenicrelease system using the Baylis-Hillman (BH) adducts as amodule. Common functional groups (e.g., amino, hydroxyl,carboxylic, and sulfhydryl groups) in a MOI are readily integratedinto the module. The MOI release is fast (similar to 10 min) with a nearlyquantitative yield and a >250-foldfluorescence increment. Wefurther prepared two prodrugs to release camptothecin and nitricoxide (NO) using the two-photon excitable template, and theactivation of prodrugs was visualized in live cells and mouse tissues.The therapeutic potential of the NO prodrug was also validated ina stroke model. This BH adduct-basedfluorogenic release features multiple advantages, such as easy preparation, compatibility ofvarious functional groups, fast response, high release yield, and tunable emission spectra, and is expected to have broad applications.
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