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

American Chemical Society (June 4, 2021)

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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Nature- biopharmadealmakers (November 30, 2020)

Biosortia is building the world’s largest library of microbiome-derived compounds for therapeutic and other applications, by leveraging the company’s microbial harvesting platform to sample and mine aquatic microbiomes at unprecedented scales with sustainable and environmentally friendly approaches. Biosortia is seeking partners interested in accessing compounds and chemistries to develop biologically relevant small molecule leads.

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NewsUSA (October 9, 2019) – 11|KTVA

More medicines may be developed faster in the near future, thanks to new technology that harnesses the tiny particles that make drug development possible. Microorganisms grown in laboratories have been the starting point for many medicines we have today. However, many more microorganisms exist in nature that can’t be grown in a lab because they are too small, too fragile, or evolve too rapidly.

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Columbus, OH (October 28, 2018) – Journal of Natural Products

Biosortia Demonstrated Products
  1. Aquatic microbiomes contain novel chemistry
  2. Novel chemistry previously undetectable & inaccessible
  3. Biosortia has proven capability of accessing previously undetectable and inaccessible chemistry in volumes sufficient for drug discovery

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Microcystins Containing Doubly Homologated Tyrosine Residues from a Microcystis aeruginosa Bloom: Structures and Cytotoxicity

American Chemical Society (May 30, 2018)

Microcystin Structure
Four new microcystin congeners are described including the first three examples of microcystins containing the rare doubly homologated tyrosine residue 2-amino-5-(4-hydroxyphenyl)pentanoic acid (Ahppa) (1–4). Large-scale harvesting and biomass processing allowed the isolation of substantial quantities of these compounds, thus enabling complete structure determination by NMR as well as cytotoxicity evaluation against selected cancer cell lines. The new Ahppa-toxins all incorporate Ahppa residues at the 2-position, and one of these also has a second Ahppa at position 4. The two most lipophilic Ahppa-containing microcystins showed 10-fold greater cytotoxic potency against human tumor cell lines (A549 and HCT-116) compared to microcystin-LR (5). The presence of an Ahppa residue in microcystin congeners is difficult to ascertain by MS methods alone, due to the lack of characteristic fragment ions derived from the doubly homologated side chain. Owing to their unexpected cytotoxic potency, the potential impact of the compounds on human health should be further evaluated.

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