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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-...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2020
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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. |
format | Online Article Text |
id | pubmed-7072998 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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