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. 2015 Mar 20:21:9.
doi: 10.1186/s40409-015-0009-8. eCollection 2015.

Antimycobacterial and cytotoxicity activity of microcystins

Daniela Fernandes Ramos  1 , Alexandre Matthiensen  2 , Wilson Colvara  3 , Ana Paula Souza de Votto  4 , Gilma Santos Trindade  4 , Pedro Eduardo Almeida da Silva  1 , João Sarkis Yunes  5
Affiliations

Antimycobacterial and cytotoxicity activity of microcystins

Daniela Fernandes Ramos et al. J Venom Anim Toxins Incl Trop Dis. .

Abstract

Background: The present work aimed to evaluate the antimycobacterial activity and cytotoxicity of Microcystis aeruginosa toxins, the MC-LR variant and purified extract of [D-Leu(1)] microcystin-LR.

Methods: The antimicrobial activity of M. aeruginosa extract and microcystin was evaluated by resazurin microtiter assay against Mycobacterium tuberculosis, M. terrae, M. chelonae and M. kansasii. The cytotoxicity assay was performed by trypan blue exclusion against the HTC cell line.

Results: Antimicrobial activity was observed in the hexanic extract of M. aeruginosa (RST 9501 strain) against M. tuberculosis, including sensitive and resistant strains with minimal inhibitory concentrations (MIC) between 1.93 μM and 0.06 μM. The high activity of M. aeruginosa hexanic extract could be attributed to the major presence of the toxins MC-LR and [D-Leu(1)] MC-LR that showed activity at MIC between 53 and 0.42 μM against tested mycobacterial strains. Even at the highest concentration tested, no toxicity of M. aeruginosa extracts was identified against HTC cells.

Conclusions: These preliminary results suggest that [D-Leu(1)] MC-LR is a promising candidate for the development of a new antimycobacterial agent.

Keywords: Antimycobacterial agents; Cytotoxic activity; Microcystins; Mycobacteria.

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Figures

Figure 1
Figure 1
General structure of microcystins (LR) with leucine (L) in the amino acid position 2 and arginine (R) in the amino acid position 4 and the structural differences in the position 1 of MC-LR (left) and [D-Leu 1 ] MC-LR (right).
Figure 2
Figure 2
Number of HTC viable cell by trypan blue exclusion test 24 hours after exposure to different concentrations of Microcystis aeruginosa strain 9501 (578.15 to 93.36 μM) which produces [D-Leu 1 ] MC-LR. Data are expressed as mean + standard error. *Indicates significant difference from the control (p < 0.05).
See this image and copyright information in PMC

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