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Article

Colombian Scorpion Centruroides margaritatus: Purification and Characterization of a Gamma Potassium Toxin with Full-Block Activity on the hERG1 Channel

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Grupo de Investigaciones Herpetológicas y Toxinológicas, Centro de Investigaciones Biomédicas, Departamento de Biología, Facultad de Ciencias Naturales, Exactas y de la Educación, Universidad del Cauca, Sector Tulcan, Calle 2 N 3N-100, Popayán 190002, Cauca, Colombia
2
Grupo de Investigación Laboratorio de Herpetología y Toxinología, Departamento de Fisiología, Facultad de Salud, Universidad del Valle, Calle 4B N° 36-00, Santiago de Cali 760043, Valle del Cauca, Colombia
3
Departamento de Medicina Molecular y Bioprocesos, Instituto de Biotecnologia, Universidad Nacional Autónoma de México, Av. Universidad 2001, Cuernavaca 62210, Morelos, Mexico
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Centro de Investigación en Dinámica Celular, Research Institute in Basic and Applied Sciences (IICBA), Universidad Autónoma del Estado de Morelos, Av. Universidad 1001, Col. Chamilpa, Cuernavaca 62209, Morelos, Mexico
*
Author to whom correspondence should be addressed.
These authors contributed equally to the work.
On sabbatical leave at Departamento de Medicina Molecular y Bioprocesos, Instituto de Biotecnologia, Universidad Nacional Autónoma de México, Av. Universidad 2001, Cuernavaca 62210, Mexico.
Received: 13 May 2021 / Revised: 31 May 2021 / Accepted: 4 June 2021 / Published: 8 June 2021
(This article belongs to the Section Animal Venoms)
The Colombian scorpion Centruroides margaritatus produces a venom considered of low toxicity. Nevertheless, there are known cases of envenomation resulting in cardiovascular disorders, probably due to venom components that target ion channels. Among them, the humanether-à-go-go-Related gene (hERG1) potassium channels are critical for cardiac action potential repolarization and alteration in its functionality are associated with cardiac disorders. This work describes the purification and electrophysiological characterization of a Centruroides margaritatus venom component acting on hERG1 channels, the CmERG1 toxin. This novel peptide is composed of 42 amino acids with a MW of 4792.88 Da, folded by four disulfide bonds and it is classified as member number 10 of the γ-KTx1 toxin family. CmERG1 inhibits hERG1 currents with an IC50 of 3.4 ± 0.2 nM. Despite its 90.5% identity with toxin ɣ-KTx1.1, isolated from Centruroides noxius, CmERG1 completely blocks hERG1 current, suggesting a more stable plug of the hERG channel, compared to that formed by other ɣ-KTx. View Full-Text
Keywords: Centruroides margaritatus; CmERG1; CnERG1; Electrophysiology; ERG toxin; ERG channel Centruroides margaritatus; CmERG1; CnERG1; Electrophysiology; ERG toxin; ERG channel
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MDPI and ACS Style

Beltrán-Vidal, J.; Carcamo-Noriega, E.; Pastor, N.; Zamudio-Zuñiga, F.; Guerrero-Vargas, J.A.; Castaño, S.; Possani, L.D.; Restano-Cassulini, R. Colombian Scorpion Centruroides margaritatus: Purification and Characterization of a Gamma Potassium Toxin with Full-Block Activity on the hERG1 Channel. Toxins 2021, 13, 407. https://0-doi-org.brum.beds.ac.uk/10.3390/toxins13060407

AMA Style

Beltrán-Vidal J, Carcamo-Noriega E, Pastor N, Zamudio-Zuñiga F, Guerrero-Vargas JA, Castaño S, Possani LD, Restano-Cassulini R. Colombian Scorpion Centruroides margaritatus: Purification and Characterization of a Gamma Potassium Toxin with Full-Block Activity on the hERG1 Channel. Toxins. 2021; 13(6):407. https://0-doi-org.brum.beds.ac.uk/10.3390/toxins13060407

Chicago/Turabian Style

Beltrán-Vidal, José, Edson Carcamo-Noriega, Nina Pastor, Fernando Zamudio-Zuñiga, Jimmy A. Guerrero-Vargas, Santiago Castaño, Lourival D. Possani, and Rita Restano-Cassulini. 2021. "Colombian Scorpion Centruroides margaritatus: Purification and Characterization of a Gamma Potassium Toxin with Full-Block Activity on the hERG1 Channel" Toxins 13, no. 6: 407. https://0-doi-org.brum.beds.ac.uk/10.3390/toxins13060407

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