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. 2021 Jun 4;6(23):15472-15478.
doi: 10.1021/acsomega.1c02025. eCollection 2021 Jun 15.

New Micropeptins with Anti-Neuroinflammatory Activity Isolated from a Cyanobacterial Bloom

Riley D Kirk  1 , Haiyin He  2 , Paul G Wahome  2 , ShiBiao Wu  2 , Guy T Carter  2 , Matthew J Bertin  1
Affiliations

New Micropeptins with Anti-Neuroinflammatory Activity Isolated from a Cyanobacterial Bloom

Riley D Kirk et al. ACS Omega. .

Abstract

Metabolite mining of environmentally collected aquatic and marine microbiomes offers a platform for the discovery of new therapeutic lead molecules. Combining a prefractionated chromatography library with liquid chromatography tandem mass spectrometry (LC-MS/MS)-based molecular networking and biological assays, we isolated and characterized two new micropeptins (1 and 2) along with the previously characterized micropeptin 996. These metabolites showed potency in anti-neuroinflammatory assays using BV-2 mouse microglial cells, showing a 50% reduction in inflammation in a range from 1 to 10 μM. These results show promise for cyanobacterial peptides in the therapeutic realm apart from their impact on environmental health and provide another example of the utility of large prefractionated natural product libraries for therapeutic hit and lead identification.

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Conflict of interest statement

The authors declare no competing financial interest.

Figures

Figure 1
Figure 1
Structures of micropeptins 982 (1) and 957 (2).
Figure 2
Figure 2
Molecular networking cluster showing micropeptin 982 (1) and micropeptin 996 as nodes 1005 (M + Na+) and 1019 (M + Na+), respectively. These nodes are enlarged and in yellow.
Figure 3
Figure 3
Anti-inflammatory activity of micropeptin 982 (MP 982) 1, micropeptin 957 (MP 957) 2, and micropeptin 996 (MP 996) tested against BV-2 murine microglial cells. All data are expressed as mean ± standard error (n = 3), and the significance was reported by analysis of variance (ANOVA) followed with Dunnett’s multiple comparison procedure. Significance (α = 0.05) as compared with LPS, p ≤ 0.0002 (***) and p ≤ 0.0001 (****).
See this image and copyright information in PMC

References

    1. Ellis A.; Bennett D. L. Neuroinflammation and the generation of neuropathic pain. Br. J. Anaesth. 2013, 111, 26–37. 10.1093/bja/aet128. - DOI - PubMed
    1. DiBonaventura M. D.; Sadosky A.; Concialdi K.; Hopps M.; Kudel I.; Parsons B.; Cappelleri J. C.; Hlavacek P.; Alexander A. H.; Stacey B. R.; Markman J. D.; Farrar J. T. The prevalence of probable neuropathic pain in the US: results from a multimodal general-population health survey. J. Pain Res. 2017, 10, 2525–2538. 10.2147/JPR.S127014. - DOI - PMC - PubMed
    1. Freynhagen R.; Baron R.; Tölle T.; Stemmler E.; Gockel U.; Stevens M.; Maier C. Screening of neuropathic pain components in patients with chronic back pain associated with nerve root compression: a prospective observational pilot study (MIPORT). Curr. Med. Res. Opin. 2006, 22, 529–537. 10.1185/030079906X89874. - DOI - PubMed
    1. Khandelwal P. J.; Herman A. M.; Moussa C. E. H. Inflammation in the early stages of neurodegenerative pathology. J. Neuroimmunol. 2011, 238, 1–11. 10.1016/j.jneuroim.2011.07.002. - DOI - PMC - PubMed
    1. Stephenson J.; Nutma E.; van der Valk P.; Amor S. Inflammation in CNS neurodegenerative diseases. Immunology 2018, 154, 204–219. 10.1111/imm.12922. - DOI - PMC - PubMed