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Microcystins: Toxicological Profile

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Marine and Freshwater Toxins

Part of the book series: Toxinology ((TOXI))

Abstract

Cyanobacteria are ubiquitous photosynthetic prokaryotic organisms, which can form blooms and scums in surface water, characterized by a wide morphological variability. Different cyanobacteria strains, i.e., Microcystis, Planktothrix and Anabaena spp., produce microcystins (MCs), a group of more than 100 different structural variants of toxic cyclic heptapeptides, with a common cyanobacteria-specific amino acid, Adda. MC variants differ from each other for amino acid substitutions in positions 2 and 4 (where MC-LR has leucine (L) and arginine (R), respectively) and other changes. Humans may be exposed to MCs through the oral route, by ingestion of contaminated drinking water or food (including dietary supplements) or water during recreational activities. Dermal/inhalation and parenteral exposure may also occur, the latter due to the use of contaminated water for hemodialysis, leading to fatal outcome. The acute hepatotoxicity is congener specific (range of intraperitoneal LD50 in mice: 50–1200 μg/kg body weight). Renal and neurotoxic effects have also been reported for some variants. Minimal structural changes among variants result in three- to fourfold differences in MC toxicokinetics: the active uptake and the biotransformation have been shown to be congener dependent. MC-LR mechanism of action is associated with inhibition of protein serine/threonine phosphatases (PP1 and PP2A): the altered phosphorylation of cellular proteins involved in signal transduction leads to cascade of events (lipid peroxidation, oxidative stress, apoptosis). MC-LR has been shown to be not mutagenic but has tumor-promoting activity; on this basis, IARC classified it as a 2B carcinogen. The WHO has defined a guidance value for drinking water of 1 μg MCs/L.

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Correspondence to Susanna Vichi .

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Vichi, S., Buratti, F.M., Testai, E. (2016). Microcystins: Toxicological Profile. In: Gopalakrishnakone, P., Haddad Jr., V., Tubaro, A., Kim, E., Kem, W. (eds) Marine and Freshwater Toxins. Toxinology. Springer, Dordrecht. https://doi.org/10.1007/978-94-007-6419-4_24

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