Abstract
Since 1970s, aplysiatoxins (ATXs), a class of biologically active dermatoxins, were identified from the marine mollusk Stylocheilus longicauda, whilst further research indicated that ATXs were originally metabolized by cyanobacteria. So far, there have been 45 aplysiatoxin derivatives discovered from marine cyanobacteria with various geographies. Recently, we isolated two neo-debromoaplysiatoxins, neo-debromoaplysiatoxin G (1) and neo-debromoaplysiatoxin H (2) from the cyanobacterium Lyngbya sp. collected from the South China Sea. The freeze-dried cyanobacterium was extracted with liquid–liquid extraction of organic solvents, and then was subjected to multiple chromatographies to yield neo-debromoaplysiatoxin G (1) (3.6 mg) and neo-debromoaplysiatoxin H (2) (4.3 mg). They were elucidated with spectroscopic methods. Moreover, the brine shrimp toxicity of the aplysiatoxin derivatives representing differential structural classifications indicated that the debromoaplysiatoxin was the most toxic compound (half inhibitory concentration (IC50) value = 0.34 ± 0.036 µM). While neo-aplysiatoxins (neo-ATXs) did not exhibit apparent brine shrimp toxicity, but showed potent blocking action against potassium channel Kv1.5, likewise, compounds 1 and 2 with IC50 values of 1.79 ± 0.22 µM and 1.46 ± 0.14 µM, respectively. Therefore, much of the current knowledge suggests the ATXs with different structure modifications may modulate multiple cellular signaling processes in animal systems leading to the harmful effects on public health.
Highlights
Marine cyanobacteria, known as blue-green algae, can yield cyanotoxins with many biologically active metabolites, which contained three major groups based largely on their primary toxicological effects: hepatotoxins, neurotoxins, and contact irritants [1,2]
The freeze-dried sample of the cyanobacterium was extracted with liquid–liquid extraction of organic solvents
The resultant extracts were subjected to multiple chromatographies to yield neodebromoaplysiatoxin G (1) (3.6 mg), neo-debromoaplysiatoxin H (2) (4.3 mg)
Summary
Known as blue-green algae, can yield cyanotoxins with many biologically active metabolites, which contained three major groups based largely on their primary toxicological effects: hepatotoxins, neurotoxins, and contact irritants [1,2]. Aplysiatoxins (ATXs), a kind of dermatoxins, which belonged to contact irritants in cyanotoxins, had attracted extensive attentions due to its series of poisoning and allergic events to public health [2,3,4,5,6]. In 2018, it was firstly reported that some ATXs exhibit potent blocking action against potassium channel Kv1.5 [20]. Our continuous study aimed to deepen the understanding of ATXs with different structural modifications that may modulate multiple cellular signaling processes in animal systems.
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