With the improvement of people’s living standards,
obesity
has become a health threat, but an effective drug treatment for obesity
has not been found yet. Here, we suggest the use of celastrol, a pentacyclic
triterpenoid from the traditional Chinese medicine Tripterygium
wilfordii, which has a powerful antiobesity effect. Increasing
studies have discovered that obesity is closely related to inflammation.
In addition, MMP-2 enzyme is highly expressed in inflammatory sites.
According to the principle of the prodrug, celastrol was used as a
hydrophobic group, PVGLIG as a link, and dextran sulfate as a hydrophilic
group to form a micelle (DS-PVGLIG-Cel). Celastrol was then loaded
for the effective treatment of high-fat-diet (HFD)-induced obesity.
MMP-2-sensitive assays confirmed that PVGLIG cleavage by MMP-2 enzymes
favors the synchronous release of celastrol. A series of animal experiments
tested that the preparation group has a strong weight loss effect.
Our results suggest that this will shed light on a strategy for the
subsequent effective treatment of HFD obesity.
For the therapy attenuating
renal ischemia–reperfusion (IR)
injury, a novel drug delivery system was urgently needed, which could
precisely deliver drugs to the pathological renal tissue. Here, we
have prepared new nanomaterials with a reactive oxygen species (ROS)-responsive
hydrogen sulfide (H2S) donor and hyaluronic acid that targets
CD44 receptor. The novel material was synthesized and characterized
via related experiments. Then, rapamycin was loaded, which inhibited
kidney damage. In the in vitro study, we found that the micelles had
ROS-responsiveness, biocompatibility, and cell penetration. In addition,
the experimental results showed that the intracellular H2S concentration after administration was threefold higher than that
of the control group. The western blot assay revealed that they have
anti-inflammatory effects via H2S donor blocking the NF-κB
signaling pathway. Consequently, the rising CD44 receptor-targeting
and ROS-sensitive H2S donor micelles would provide a promising
way for renal IR injury. This work provides a strategy for improving
ischemia/reperfusion injury for pharmaceuticals.
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