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Characterization of Inhibitory Effectiveness in Hyperpolarization-Activated Cation Currents by a Group of ent-Kaurane-Type Diterpenoids from Croton tonkinensis

Croton is an extensive flowering plant genus in the spurge family, Euphorbiaceae. Three croton compounds with the common ent-kaurane skeleton have been purified from Croton tonkinensis. Methods: We examined any modifications of croton components (i.e., croton-01 [ent-18-acetoxy-7α-hydroxykaur-16-en-...

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Autores principales: Kuo, Ping-Chung, Liu, Yen-Chin, Lo, Yi-Ching, Wu, Sheng-Nan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7072998/
https://www.ncbi.nlm.nih.gov/pubmed/32070065
http://dx.doi.org/10.3390/ijms21041268
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author Kuo, Ping-Chung
Liu, Yen-Chin
Lo, Yi-Ching
Wu, Sheng-Nan
author_facet Kuo, Ping-Chung
Liu, Yen-Chin
Lo, Yi-Ching
Wu, Sheng-Nan
author_sort Kuo, Ping-Chung
collection PubMed
description Croton is an extensive flowering plant genus in the spurge family, Euphorbiaceae. Three croton compounds with the common ent-kaurane skeleton have been purified from Croton tonkinensis. Methods: We examined any modifications of croton components (i.e., croton-01 [ent-18-acetoxy-7α-hydroxykaur-16-en-15-one], croton-02 [ent-7α,14β-dihydroxykaur-16-en-15-one] and croton-03 [ent-1β-acetoxy-7α,14β-dihydroxykaur-16-en-15-one] on either hyperpolarization-activated cation current (I(h)) or erg-mediated K(+) current identified in pituitary tumor (GH(3)) cells and in rat insulin-secreting (INS-1) cells via patch-clamp methods. Results: Addition of croton-01, croton-02, or croton-03 effectively and differentially depressed I(h) amplitude. Croton-03 (3 μM) shifted the activation curve of I(h) to a more negative potential by approximately 11 mV. The voltage-dependent hysteresis of I(h) was also diminished by croton-03 administration. Croton-03-induced depression of I(h) could not be attenuated by SQ-22536 (10 μM), an inhibitor of adenylate cyclase, but indeed reversed by oxaliplatin (10 μM). The I(h) in INS-1 cells was also depressed effectively by croton-03. Conclusion: Our study highlights the evidence that these ent-kaurane diterpenoids might conceivably perturb these ionic currents through which they have high influence on the functional activities of endocrine or neuroendocrine cells.
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spelling pubmed-70729982020-03-19 Characterization of Inhibitory Effectiveness in Hyperpolarization-Activated Cation Currents by a Group of ent-Kaurane-Type Diterpenoids from Croton tonkinensis Kuo, Ping-Chung Liu, Yen-Chin Lo, Yi-Ching Wu, Sheng-Nan Int J Mol Sci Article Croton is an extensive flowering plant genus in the spurge family, Euphorbiaceae. Three croton compounds with the common ent-kaurane skeleton have been purified from Croton tonkinensis. Methods: We examined any modifications of croton components (i.e., croton-01 [ent-18-acetoxy-7α-hydroxykaur-16-en-15-one], croton-02 [ent-7α,14β-dihydroxykaur-16-en-15-one] and croton-03 [ent-1β-acetoxy-7α,14β-dihydroxykaur-16-en-15-one] on either hyperpolarization-activated cation current (I(h)) or erg-mediated K(+) current identified in pituitary tumor (GH(3)) cells and in rat insulin-secreting (INS-1) cells via patch-clamp methods. Results: Addition of croton-01, croton-02, or croton-03 effectively and differentially depressed I(h) amplitude. Croton-03 (3 μM) shifted the activation curve of I(h) to a more negative potential by approximately 11 mV. The voltage-dependent hysteresis of I(h) was also diminished by croton-03 administration. Croton-03-induced depression of I(h) could not be attenuated by SQ-22536 (10 μM), an inhibitor of adenylate cyclase, but indeed reversed by oxaliplatin (10 μM). The I(h) in INS-1 cells was also depressed effectively by croton-03. Conclusion: Our study highlights the evidence that these ent-kaurane diterpenoids might conceivably perturb these ionic currents through which they have high influence on the functional activities of endocrine or neuroendocrine cells. MDPI 2020-02-13 /pmc/articles/PMC7072998/ /pubmed/32070065 http://dx.doi.org/10.3390/ijms21041268 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Kuo, Ping-Chung
Liu, Yen-Chin
Lo, Yi-Ching
Wu, Sheng-Nan
Characterization of Inhibitory Effectiveness in Hyperpolarization-Activated Cation Currents by a Group of ent-Kaurane-Type Diterpenoids from Croton tonkinensis
title Characterization of Inhibitory Effectiveness in Hyperpolarization-Activated Cation Currents by a Group of ent-Kaurane-Type Diterpenoids from Croton tonkinensis
title_full Characterization of Inhibitory Effectiveness in Hyperpolarization-Activated Cation Currents by a Group of ent-Kaurane-Type Diterpenoids from Croton tonkinensis
title_fullStr Characterization of Inhibitory Effectiveness in Hyperpolarization-Activated Cation Currents by a Group of ent-Kaurane-Type Diterpenoids from Croton tonkinensis
title_full_unstemmed Characterization of Inhibitory Effectiveness in Hyperpolarization-Activated Cation Currents by a Group of ent-Kaurane-Type Diterpenoids from Croton tonkinensis
title_short Characterization of Inhibitory Effectiveness in Hyperpolarization-Activated Cation Currents by a Group of ent-Kaurane-Type Diterpenoids from Croton tonkinensis
title_sort characterization of inhibitory effectiveness in hyperpolarization-activated cation currents by a group of ent-kaurane-type diterpenoids from croton tonkinensis
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7072998/
https://www.ncbi.nlm.nih.gov/pubmed/32070065
http://dx.doi.org/10.3390/ijms21041268
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