AI Article Synopsis
- Bioconjugates combining pyrrole heterocycles and peptides show potential as analgesics due to the advantages of both molecules, such as cell penetration and receptor binding.
- New bioconjugates were synthesized, and their purity and structure were confirmed using HPLC and mass spectrometry, while the analgesic activity was tested using the Paw Pressure test.
- Although free pyrrole acids demonstrated the highest analgesic effect, they are less stable; thus, incorporating peptides enhances their stability, resulting in slightly lower pain relief efficacy.
Article Abstract
Background: Bioconjugates are promising alternatives for the multiple targeting of any disease. Pyrrole heterocycle is well known with many activities and is a building block of a lot of medical drugs. On the other hand, peptides are short molecules with many advantages such as small size, ability to penetrate the cell membrane and bond-specific receptors, vectorizing potential, etc. Thus, hybrid molecules between peptide and pyrrole moiety could be a promising alternative as an anti-pain tool.
Methods: New bioconjugates with a general formula Pyrrole (α-/β-acid)-FELL-OH (NH) were synthesized using Fmoc/OtBu peptide synthesis on solid support. HPLC was used to monitor the purity of newly synthesized bioconjugates. Their structures were proven by electrospray ionization mass spectrometry. The Paw Pressure test (Randall-Selitto test) was used to examinate the analgesic activity. Hydrolytic stability of targeted structures was monitored in three model systems with pH 2.0, 7.4 and 9.0, including specific enzymes by means of the HPLC-UV method.
Results: The obtained results reveal that all newly synthesized bioconjugates have analgesic activity according to the used test but free pyrrole acids have the best analgesic activity.
Conclusions: Although free pyrrole acids showed the best analgesic activity, they are the most unstable for hydrolysis. Combination with peptide structure leads to the hydrolytic stabilization of the bioconjugates, albeit with slightly reduced activity.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10740831 | PMC |
| http://dx.doi.org/10.3390/biomedicines11123265 | DOI Listing |
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