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Novel Labdane Diterpenes-Based Synthetic Derivatives: Identification of a Bifunctional Vasodilator That Inhibits Ca_V1.2 and Stimulates K_Ca1.1 Channels.

ABSTRACT: Sesquiterpenes such as leucodin and the labdane-type diterpene manool are natural compounds endowed with remarkably in vitro vasorelaxant and in vivo hypotensive activities. Given their structural similarity with the sesquiterpene lactone (+)-sclareolide, this molecule was selected as a scaffold to develop novel vasoactive agents. Functional, electrophysiology, and molecular dynamics studies were performed. The opening of the five-member lactone ring in the (+)-sclareolide provided a series of labdane-based small molecules, promoting a significant in vitro vasorelaxant effect. Electrophysiology data identified 7 as a Ca_V1.2 channel blocker and a K_Ca1.1 channel stimulator. These activities were also confirmed in the intact vascular tissue. The significant antago

SUBMITTER: Carullo G

PROVIDER: S-EPMC9410420 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature

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Novel Labdane Diterpenes-Based Synthetic Derivatives: Identification of a Bifunctional Vasodilator That Inhibits Ca_V1.2 and Stimulates K_Ca1.1 Channels.

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Dataset Information

Novel Labdane Diterpenes-Based Synthetic Derivatives: Identification of a Bifunctional Vasodilator That Inhibits CaV1.2 and Stimulates KCa1.1 Channels.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Novel Labdane Diterpenes-Based Synthetic Derivatives: Identification of a Bifunctional Vasodilator That Inhibits Ca_V1.2 and Stimulates K_Ca1.1 Channels.