Abstract
Cyanobacterial cyclopeptides, including microcystins and nodularins, are considered a health hazard to humans due to the possible toxic effects of high consumption. From a pharmacological standpoint, microcystins are stable hydrophilic cyclic heptapeptides with a potential to cause cellular damage following uptake via organic anion-transporting polypeptides (OATP). Their intracellular biological effects involve inhibition of catalytic subunits of protein phosphatase 1 (PP1) and PP2, glutathione depletion and generation of reactive oxygen species (ROS). Interestingly, certain OATPs are prominently expressed in cancers as compared to normal tissues, qualifying MC as potential candidates for cancer drug development. In the era of targeted cancer therapy, cyanotoxins comprise a rich source of natural cytotoxic compounds with a potential to target cancers expressing specific uptake transporters. Moreover, their structure offers opportunities for combinatorial engineering to enhance the therapeutic index and resolve organ-specific toxicity issues. In this article, we revisit cyanobacterial cyclopeptides as potential novel targets for anticancer drugs by summarizing existing biomedical evidence, presenting structure-activity data and discussing developmental perspectives.
Highlights
Cyanobacteria appeared approximately 3.5 billion years ago, triggering major ecological change through photochemical release of molecular oxygen from water into the atmosphere [1,2]
We focus on microcystin (MC) as a potential anticancer compound and present relevant supporting data
It has been proposed that MCs have evolved to function as a defense mechanism of cyanobacteria against grazing, a theory that has been debated by recent findings indicating that microcystin synthetase predated the metazoan lineage [34,35]
Summary
Cyanobacteria (blue-green algae) appeared approximately 3.5 billion years ago, triggering major ecological change through photochemical release of molecular oxygen from water into the atmosphere [1,2]. The cyanobacteria population comprises 150 genera and about 2000 species of considerable diversity They are prokaryotic algae that exist as unicellular species or in colonies (Figure 1). Due to their photosynthetic capacity, they constitute the primary first level organisms in food chains in water ecosystems. These prokaryotes play a significant role in the marine nitrogen cycle and have a role in balancing nitrogen (N) and CO2 dynamics in the biosphere [3]. We focus on microcystin (MC) as a potential anticancer compound and present relevant supporting data
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