Caged polycyclic polyprenylated acylphloroglucinols as Cav3.2 low voltage-gated Ca2+ channel inhibitors from Hypericum curvisepalum

Yan-Song Ye; Rui Liu; Na-Na Jiang; Song-Yu Li; Yin Nian; Gang Xu

doi:10.1039/D2CC05396A

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Caged polycyclic polyprenylated acylphloroglucinols as Ca_v3.2 low voltage-gated Ca²⁺ channel inhibitors from Hypericum curvisepalum†

Yan-Song Ye,

‡^a Rui Liu,‡^ac Na-Na Jiang,‡^ab Song-Yu Li,^a Yin Nian

*^a and Gang Xu

*^a

Author affiliations

* Corresponding authors

^a State Key Laboratory of Phytochemistry and Plant Resources in West China and Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China
E-mail: nianyin@mail.kib.ac.cn, xugang008@mail.kib.ac.cn

^b University of Chinese Academy of Sciences, Beijing, China

^c Key Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China, College of Life Sciences, Shaanxi Normal University, Xi'an, China

Abstract

Five caged polycyclic polyprenylated acylphloroglucinols including an unprecedented octahydro-2,5-methanoindene skeleton (1) were discovered from Hypericum curvisepalum. Biologically, 1 and 2 are potent Ca_v3.2 T-type Ca²⁺ channel inhibitors with negligible effect on the cardiovascular antitarget, the human ether-à-go-go-related gene potassium channel. Additionally, 2 indicates strong antinociception in the mouse acetic acid writhing test.

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Article information

DOI: https://doi.org/10.1039/D2CC05396A
Article type: Communication
Submitted: 03 Oct 2022
Accepted: 26 Oct 2022
First published: 26 Oct 2022

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Chem. Commun., 2022,58, 13135-13138

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Caged polycyclic polyprenylated acylphloroglucinols as Ca_v3.2 low voltage-gated Ca²⁺ channel inhibitors from Hypericum curvisepalum

Y. Ye, R. Liu, N. Jiang, S. Li, Y. Nian and G. Xu, Chem. Commun., 2022, 58, 13135 DOI: 10.1039/D2CC05396A

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