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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2024-12-01
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| author | Yueyang Lu Yanguo Zhu Chengbang Ma Lei Wang Mei Zhou Tianbao Chen Xiaonan Ma Xu Zhang Zhimin Fan |
| author_facet | Yueyang Lu Yanguo Zhu Chengbang Ma Lei Wang Mei Zhou Tianbao Chen Xiaonan Ma Xu Zhang Zhimin Fan |
| author_sort | Yueyang Lu |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-92f6a1f0349844a7bbbd808c3edd3c3a |
| institution | Kabale University |
| issn | 2218-273X |
| language | English |
| publishDate | 2024-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Biomolecules |
| spelling | doaj-art-92f6a1f0349844a7bbbd808c3edd3c3a2025-01-24T13:24:55ZengMDPI AGBiomolecules2218-273X2024-12-011513010.3390/biom15010030Senegalin-2: A Novel Hexadecapeptide from <i>Kassina senegalensis</i> with Antibacterial and Muscle Relaxant Activities, and Its Derivative Senegalin-2BK as a Bradykinin AntagonistYueyang Lu0Yanguo Zhu1Chengbang Ma2Lei Wang3Mei Zhou4Tianbao Chen5Xiaonan Ma6Xu Zhang7Zhimin Fan8Jiangsu Clinical Innovation Center for Anorectal Diseases of T.C.M., Nanjing Hospital of Chinese Medicine Affiliated to Nanjing University of Chinese Medicine, Nanjing 210022, ChinaSchool of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKSchool of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKSchool of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKSchool of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKSchool of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKSchool of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKSchool of Medicine and Life Sciences, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaJiangsu Clinical Innovation Center for Anorectal Diseases of T.C.M., Nanjing Hospital of Chinese Medicine Affiliated to Nanjing University of Chinese Medicine, Nanjing 210022, ChinaThe 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.https://www.mdpi.com/2218-273X/15/1/30amphibianantimicrobial peptidessmooth musclebradykininantagonist |
| spellingShingle | Yueyang Lu Yanguo Zhu Chengbang Ma Lei Wang Mei Zhou Tianbao Chen Xiaonan Ma Xu Zhang Zhimin Fan 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 Biomolecules amphibian antimicrobial peptides smooth muscle bradykinin antagonist |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| topic | amphibian antimicrobial peptides smooth muscle bradykinin antagonist |
| url | https://www.mdpi.com/2218-273X/15/1/30 |
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