Clerodane Diterpenes from Casearia corymbosa as Allosteric GABA_A Receptor Modulators.

ABSTRACT: An EtOAc extract of Casearia corymbosa leaves led to an allosteric potentiation of the GABA signal in a fluorometric imaging plate reader (FLIPR) assay on Chinese hamster ovary (CHO) cells stably expressing GABA_A receptors with an α₁β₂γ₂ subunit composition. The activity was tracked by HPLC-based activity profiling, and four known (2, 3, 4, and 8) and five new clerodane-type diterpenoids (1, 5-7, and 9) were isolated. Compounds 1-8 were obtained from the active time window. The absolute configuration of all compounds was established by ECD. Compounds 3, 7, and 8 exhibited EC₅₀ values of 0.5, 4.6, and 1.4 μM, respectively. To explore possib

SUBMITTER: Syafni N 

PROVIDER: S-EPMC9150179 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature