We report "pro-guest" and acyclic cucurbit[n]uril conjugated polymers as supramolecular drug delivery systems (DDSs). These supramolecular DDSs could encapsulate anti-tumor drugs. Under acidic conditions, an acid-labile "pro-guest" degraded to become a "competing guest", which displaced and released the encapsulated drug at a tunable rate.
Traumatic tracheal stenosis (TS) is a serious respiratory disease characterized by hyperplasia of airway granulation. Plumbagin (PLB) is a natural naphthoquinone component with anti-fibrotic properties. This research aimed to explore the roles of PLB in alleviating TS and the underlying mechanisms. For in vitro studies, lung fibroblasts (IMR-90 cells), with/without PLB treatment or TGF-β1 induction, were used. The viability and proliferation of IMR-90 cells were examined by CCK-8 and EdU incorporation assays. The differentiation of IMR-90 cells was assessed by detecting the mRNA and protein expression levels of collagen (COL)-1 and alpha-smooth muscle actin (α-SMA). Besides, immunofluorescence assay was conducted to evaluate the localization of α-SMA in TGF-β1-induced IMR-90 cells. Moreover, the combination of PLB with/without TβRI (SB-431,542), PI3K/Akt (Ly294002) or mTOR (rapamycin) inhibitor was pretreated on IMR-90 cells after TGF-β1 induction. For in vivo studies, a rat model of TS was established. The pathological features and severity of TS were determined by hematoxylin and eosin staining. The protein levels of TGF-β1/Smad and Akt/mTOR pathways were detected for both in vitro and in vivo models. PLB effectively inhibited the proliferation and differentiation of TGF-β1-induced IMR-90 cells, and suppressed TGF-β1/Smad and Akt/mTOR signaling pathways both in vivo and in vitro. Furthermore, PLB reduced the degree of TS in rats. Taken together, our results indicate that PLB regulates lung fibroblast activity and attenuates TS in rats by inhibiting TGF-β1/Smad and Akt/mTOR signaling pathways. In conclusion, this study implies that PLB may serve as a promising therapeutic compound for TS.
Supramolecular
fluorescent probes for the detection of reactive
oxygen species (ROSs) are designed based on a pro-guest strategy.
Nine commercially available fluorescent dyes, six host molecules,
and a pro-guest are used to rapidly generate a library of 54 potential
supramolecular probes. These potential supramolecular probes are screened
in a high-throughput fashion using a plate reader to discover seven
“hits” or workable probes. The mechanism is confirmed
to be ROS-induced conversion from a low-binding-affinity pro-guest
to a high-binding-affinity guest and the competitive displacement
of the encapsulated fluorescent dye. The response to H2O2 of four supramolecular probes is found to be concentration-dependent
and may be used for quantitative analysis of H2O2. The supramolecular probe is selectively responsive toward other
oxidative agents, such as NaClO and Na2SO3.
The cell study shows that supramolecular probes are capable of detecting
H2O2 in human cancer cells (MCF-7 or HeLa).
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