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1.
Dokl Biochem Biophys ; 505(1): 145-150, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-36038679

RESUMO

A number of studies confirmed the involvement of transient receptor potential vanilloid (TRPV) and acid-sensing (ASIC) ion channels in the physiological processes associated with the development of anxiety disorders. This makes their ligands new potential anxiolytic agents. We examined the efficacy of two peptides from the sea anemone Heteractis crispa, Hcr 1b-2 and HCRG21, affecting ASIC1a and TRPV1 channels, respectively, in the open field and elevated plus maze tests. According to the obtained data, HCRG21 significantly decreases both the level of anxiety and stimulates the activity of animals at doses of 0.01-1 mg/kg, whereas Hcr 1b-2 has a weak anxiolytic effect only at a dose of 0.1 mg/kg. The pharmacodynamic study showed that the HCRG21 has an anxiolytic effect for 2 h, and its effectiveness is higher than that of the reference drug.


Assuntos
Ansiolíticos , Anêmonas-do-Mar , Canais Iônicos Sensíveis a Ácido , Animais , Ansiolíticos/farmacologia , Peptídeos/farmacologia , Canais de Cátion TRPV
2.
Dokl Biochem Biophys ; 495(1): 292-295, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33368037

RESUMO

A new neurotoxin RTX-VI that modulates the voltage-gated sodium channels (NaV) was isolated from the ethanolic extract of the sea anemone Heteractis crispa. Its amino acid sequence was determined using the combination of Edman degradation and tandem mass spectrometry. RTX-VI turned out to be an unusual natural analogue of the previously described sea anemone toxin RTX-III. The RTX-VI molecule consists of two disulfide-linked peptide chains and is devoid of Arg13, which is important for the selectivity and affinity of such peptides for the NaV channels. Electrophysiological screening of RTV-VI on NaV channel subtypes showed its selective interaction with the central nervous system (NaV1.2, NaV1.6) and insect (BgNaV1, VdNaV1) sodium channels.


Assuntos
Venenos de Cnidários/farmacologia , Proteínas de Insetos/metabolismo , Canal de Sódio Disparado por Voltagem NAV1.2/metabolismo , Canal de Sódio Disparado por Voltagem NAV1.6/metabolismo , Anêmonas-do-Mar/química , Sequência de Aminoácidos , Animais , Venenos de Cnidários/química , Ativação do Canal Iônico/efeitos dos fármacos , Homologia de Sequência , Relação Estrutura-Atividade
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