Prenylflavanones as Novel T-Type Calcium Channel Blockers Useful for Pain Therapy

Author:

Nguyen Huy Du1,Okada Takuya1,Sekiguchi Fumiko2,Tsubota Maho2,Nishikawa Hiroyuki2,Kawabata Atsufumi2,Toyooka Naoki13

Affiliation:

1. Graduate School of Innovative Life Science, University of Toyama, Japan

2. Laboratory of Pharmacology and Pathophysiology, Faculty of Pharmacy, Kindai University, Higashi-Osaka, Japan

3. Graduate School of Science and Engineering, University of Toyama, Japan

Abstract

Prenylated flavonoids have attracted much attention due to their promising and diverse bioactivities on multitarget tissues. To the best of our knowledge, our recent studies demonstrated first that (2 S)-6-prenylnaringenin (6-PNG), a hop component, blocks Cav3.2 T-type calcium channels (T-channels) and alleviates neuropathic and visceral pain with little side effects; it also indicated first that other natural prenylflavanones (PFVNs), such as sophoraflavanone G and (2 S)-8-PNG, or synthetic 6-PFVNs including (2 R/S)-6-PNG and its derivatives are capable of blocking T-channels and useful for pain therapy. Through the structure-activity relationship studies on the synthetic 6-PFVNs, we identified 6-(3-ethylpent-2-enyl)-5,7-dihydroxy-2-(2-hydroxyphenyl)chroman-4-one (8j or KTt-45) as the most potent blocker of Cav3.2 T-channels. It is interesting to recognize a prenylated flavonoid, belonging to other sub-classes, as a novel T-channel blocker. Therefore, this article will review some of our recent studies to introduce a new branch to researchers studying on prenylated flavonoids.

Publisher

SAGE Publications

Subject

Complementary and alternative medicine,Plant Science,Drug Discovery,Pharmacology,General Medicine

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