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Salpratlactones A and B: A Pair of cis–trans Tautomeric Abietanes as Caᵥ3.1 T-Type Calcium Channel Agonists from Salvia prattii

Author:
Xia, Fan, Li, Wen-Yan, Yang, Xing-Wei, Yang, Jian, Li, Xian, Nian, Yin, Xu, Gang
Source:
Organic letters 2019 v.21 no.14 pp. 5670-5674
ISSN:
1523-7052
Subject:
Salvia, agonists, calcium channels, chemical bonding, chemical reactions, lactones, median effective concentration, tautomers
Abstract:
Salpratlactones A (1) and B (2), a pair of abietane cis–trans tautomers from Salvia prattii, were identified as the first naturally occurring agonists of T-type calcium channel (TTCC). Structurally, 1 and 2 were featured by unique 6/5 carbocyclic rings bearing a γ-lactone ring through an exocyclic double bond. Moreover, both compounds and their mixture at 10 μM potently and equally increased Caᵥ3.1 TTCC peak currents, and 1 had an EC₅₀ value of 12.48 μM.
Agid:
6539271