AI Article Synopsis
- Apocynin is a natural compound with various biological activities, leading to the design and synthesis of new derivatives for potential therapeutic use.
- These derivatives were tested for their ability to cross the blood-brain barrier, their effects on reactive oxygen species (ROS), and their anti-glioma properties.
- The compound D31 showed promising results by effectively penetrating the BBB, increasing ROS levels, and inhibiting glioma growth through the suppression of the NF-κB pathway, suggesting its potential for future anti-glioma treatments.
Article Abstract
Apocynin (4-hydroxy-3-methoxyacetophenone) is a natural polyphenolic compound with multiple biological activities. In the present study, a series of apocynin derivatives were designed and synthesized. The ADMET prediction, blood-brain barrier (BBB) penetration assay, anti-NADPH oxidase activity, reactive oxygen species (ROS) levels, and anti-glioma effects of these apocynin derivatives were evaluated. The anti-glioma mechanisms of candidate compounds were studied by flow cytometer and Western blot. The results showed that D31 exhibited higher BBB penetration, increased ROS generations and significant anti-glioma effects both and . Further studies showed that D31 inhibited the activations of NF-κB pathway. Overall, our data demonstrated that D31 inhibited growth and induced apoptosis of glioma, which might be caused by ROS-related NF-κB activation. The current study suggested that D31 could be further explored for its potential use in anti-glioma therapy.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6733959 | PMC |
| http://dx.doi.org/10.3389/fphar.2019.00951 | DOI Listing |
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