Senegalin-2: A Novel Hexadecapeptide from <i>Kassina senegalensis</i> with Antibacterial and Muscle Relaxant Activities, and Its Derivative Senegalin-2BK as a Bradykinin Antagonist
The amphibian skin secretions are excellent sources of bioactive peptides, some of which and their derivatives exhibit multiple properties, including antibacterial and antagonism against bradykinin. A novel peptide Senegalin-2 was isolated from the skin secretions of <i>Kassina senegalensis<...
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| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2024-12-01
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| Series: | Biomolecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2218-273X/15/1/30 |
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| Summary: | The amphibian skin secretions are excellent sources of bioactive peptides, some of which and their derivatives exhibit multiple properties, including antibacterial and antagonism against bradykinin. A novel peptide Senegalin-2 was isolated from the skin secretions of <i>Kassina senegalensis</i> frog. Senegalin-2 relaxed rat bladder smooth muscle (EC<sub>50</sub> 17.94 nM) and ileum smooth muscle (EC<sub>50</sub> 135 nM), inhibited <i>S. aureus</i> and MRSA at 2 μM, and exhibited low hemolytic activity with no cytotoxicity. To design effective bradykinin antagonists, Senegalin-2 was conjugated with bradykinin to synthesize Senegalin-2BK. This modification retained potent activity against Gram-positive bacteria. Compared to Senegalin-2, Senegalin-2BK significantly reduced hemolysis and exhibited a more than threefold increase in the selectivity index. Furthermore, Senegalin-2BK contracted the bladder (EC<sub>50</sub> 2.83 μM) and ileum (EC<sub>50</sub> 56.64 nM)’s smooth muscle. The pretreatment with 10<sup>−7</sup> M Senegalin-2BK reduced the 10<sup>−6</sup> M bradykinin contraction on the bladder by over 70%. In conclusion, Senegalin-2 has dual functionalities as an antibacterial agent and muscle relaxant, positioning it as a potential therapeutic candidate for managing overactive bladder. As a synthetically derived bradykinin antagonist and myotropic peptide with antibacterial properties, Senegalin-2BK shows promise in effective therapies for relieving pain, inflammation, and addressing muscular disorders such as urinary retention, constipation, and infections. |
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| ISSN: | 2218-273X |