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Article

Peimine, an Anti-Inflammatory Compound from Chinese Herbal Extracts, Modulates Muscle-Type Nicotinic Receptors

by
Armando Alberola-Die
1,
José Antonio Encinar
2,
Raúl Cobo
1,
Gregorio Fernández-Ballester
2,
José Manuel González-Ros
2,
Isabel Ivorra
1 and
Andrés Morales
1,*
1
División de Fisiología, Departamento de Fisiología, Genética y Microbiología, Universidad de Alicante, Apdo. 99, E-03080 Alicante, Spain
2
Instituto de Investigación, Desarrollo e Innovación en Biotecnología Sanitaria de Elche (IDiBE), Universidad Miguel Hernández, E-03202 Elche, Spain
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2021, 22(20), 11287; https://doi.org/10.3390/ijms222011287
Submission received: 27 September 2021 / Accepted: 15 October 2021 / Published: 19 October 2021
(This article belongs to the Special Issue Cholinergic Control of Inflammation)
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Abstract

Fritillaria bulbs are used in Traditional Chinese Medicine to treat several illnesses. Peimine (Pm), an anti-inflammatory compound from Fritillaria, is known to inhibit some voltage-dependent ion channels and muscarinic receptors, but its interaction with ligand-gated ion channels remains unexplored. We have studied if Pm affects nicotinic acetylcholine receptors (nAChRs), since they play broad functional roles, both in the nervous system and non-neuronal tissues. Muscle-type nAChRs were incorporated to Xenopus oocytes and the action of Pm on the membrane currents elicited by ACh (IAChs) was assessed. Functional studies were combined with virtual docking and molecular dynamics assays. Co-application of ACh and Pm reversibly blocked IACh, with an IC50 in the low micromolar range. Pm inhibited nAChR by: (i) open-channel blockade, evidenced by the voltage-dependent inhibition of IAch, (ii) enhancement of nAChR desensitization, revealed by both an accelerated IACh decay and a decelerated IACh deactivation, and (iii) resting-nAChR blockade, deduced from the IACh inhibition elicited by Pm when applied before ACh superfusion. In good concordance, virtual docking and molecular dynamics assays demonstrated that Pm binds to different sites at the nAChR, mostly at the transmembrane domain. Thus, Pm from Fritillaria bulbs, considered therapeutic herbs, targets nAChRs with high affinity, which might account for its anti-inflammatory actions.
Keywords: peimine; traditional Chinese medicine; anti-inflammatory compound; nicotinic receptors; electrophysiological recordings; Xenopus oocytes; molecular docking; dynamics simulations peimine; traditional Chinese medicine; anti-inflammatory compound; nicotinic receptors; electrophysiological recordings; Xenopus oocytes; molecular docking; dynamics simulations

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MDPI and ACS Style

Alberola-Die, A.; Encinar, J.A.; Cobo, R.; Fernández-Ballester, G.; González-Ros, J.M.; Ivorra, I.; Morales, A. Peimine, an Anti-Inflammatory Compound from Chinese Herbal Extracts, Modulates Muscle-Type Nicotinic Receptors. Int. J. Mol. Sci. 2021, 22, 11287. https://doi.org/10.3390/ijms222011287

AMA Style

Alberola-Die A, Encinar JA, Cobo R, Fernández-Ballester G, González-Ros JM, Ivorra I, Morales A. Peimine, an Anti-Inflammatory Compound from Chinese Herbal Extracts, Modulates Muscle-Type Nicotinic Receptors. International Journal of Molecular Sciences. 2021; 22(20):11287. https://doi.org/10.3390/ijms222011287

Chicago/Turabian Style

Alberola-Die, Armando, José Antonio Encinar, Raúl Cobo, Gregorio Fernández-Ballester, José Manuel González-Ros, Isabel Ivorra, and Andrés Morales. 2021. "Peimine, an Anti-Inflammatory Compound from Chinese Herbal Extracts, Modulates Muscle-Type Nicotinic Receptors" International Journal of Molecular Sciences 22, no. 20: 11287. https://doi.org/10.3390/ijms222011287

APA Style

Alberola-Die, A., Encinar, J. A., Cobo, R., Fernández-Ballester, G., González-Ros, J. M., Ivorra, I., & Morales, A. (2021). Peimine, an Anti-Inflammatory Compound from Chinese Herbal Extracts, Modulates Muscle-Type Nicotinic Receptors. International Journal of Molecular Sciences, 22(20), 11287. https://doi.org/10.3390/ijms222011287

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