RRC ID 28821
Author Shimizu K, Sano T, Kubota R, Kobayashi N, Tahara M, Obama T, Sugimoto N, Nishimura T, Ikarashi Y.
Title Effects of the amino acid constituents of microcystin variants on cytotoxicity to primary cultured rat hepatocytes.
Journal Toxins (Basel)
Abstract Microcystins, which are cyclic heptapeptides produced by some cyanobacterial species from algal blooms, strongly inhibit serine/threonine protein phosphatase and are known as hepatotoxins. Microcystins have many structural variations, yet insufficient information is available on the differences in the cytotoxic potentials among the structural variants. In this study, the cytotoxicities of 16 microcystin variants at concentrations of 0.03-10 μg/mL to primary cultured rat hepatocytes were determined by measuring cellular ATP content, and subsequently determined by their 50% inhibitory concentration (IC50). Differences in the amino acid constituents were associated with differences in cytotoxic potential. [D-Asp3, Z-Dhb7] microcystin-LR exhibited the strongest cytotoxicity at IC50 of 0.053 μg/mL among the microcystin variants tested. Furthermore, [d-Asp3, Z-Dhb7] microcystin-HtyR was also highly cytotoxic. These results suggest that both D-Asp and Z-Dhb residues are important in determining the cytotoxic potential of microcystin variants.
Volume 6(1)
Pages 168-79
Published 2013-12-30
DOI 10.3390/toxins6010168
PII toxins6010168
PMID 24380975
PMC PMC3920255
MeSH Amino Acids / chemistry* Animals Cells, Cultured Hepatocytes / drug effects* Hepatocytes / metabolism Inhibitory Concentration 50 Marine Toxins Microcystins / chemistry Microcystins / toxicity* Phosphoprotein Phosphatases / metabolism Rats Rats, Sprague-Dawley
IF 3.531
Times Cited 23
WOS Category TOXICOLOGY
Resource
Algae NIES-90 NIES-610 NIES-928 NIES-595