PUBLICATION
Three New α-Pyrone Derivatives with Antiepileptic Activity from the Marine Actinomycete Nocardiopsis sp. NBUDK19
- Authors
- Li, J., Zhou, Z., Feng, F., Yuan, W., Zhang, Y., Wang, J., Zhang, B., Jin, H., He, S., Ding, L.
- ID
- ZDB-PUB-250515-25
- Date
- 2025
- Source
- Marine biotechnology (New York, N.Y.) 27: 8585 (Journal)
- Registered Authors
- Keywords
- Nocardiopsis, Antiepileptic activity, Molecular docking, Secondary metabolites, Zebrafish model
- MeSH Terms
-
- Animals
- Porifera/microbiology
- Anticonvulsants*/chemistry
- Anticonvulsants*/isolation & purification
- Anticonvulsants*/pharmacology
- Zebrafish
- Pyrones*/chemistry
- Pyrones*/isolation & purification
- Pyrones*/pharmacology
- Actinobacteria*/chemistry
- Molecular Docking Simulation
- PubMed
- 40366478 Full text @ Mar. Biotechnol.
Citation
Li, J., Zhou, Z., Feng, F., Yuan, W., Zhang, Y., Wang, J., Zhang, B., Jin, H., He, S., Ding, L. (2025) Three New α-Pyrone Derivatives with Antiepileptic Activity from the Marine Actinomycete Nocardiopsis sp. NBUDK19. Marine biotechnology (New York, N.Y.). 27:8585.
Abstract
Epilepsy is a serious brain disease that urgently needs new drugs to treat it. In this study, three new α-pyrone derivatives, nocardipones A - C (1 - 3), were isolated from the sponge-associated actinomycete Nocardiopsis sp. NBUDK19 guided by anti-epileptic bioactivity using an in vivo zebrafish model. Compounds 1 - 3 were isolated and purified by silica gel column chromatography combined with semi-preparative HPLC. The structures of 1 - 3 were elucidated by UV, HRESIMS, NMR spectroscopic analysis, optical rotation, and computational chemical calculations. Our pharmacological study showed that compounds 1 - 3 exhibited notable reductions in seizure-like locomotor activity at 5 μg/mL. The qPCR analysis showed that compounds 1 - 3 significantly regulated the mRNA expression levels of c-fos and genes associated with GABAergic-glutamatergic signaling, including gria1b and gat1. The molecular docking revealed that compounds 1 - 3 strongly binding to 4-aminobutyric acid transaminase, with binding energies of - 7.3, - 7.8, and - 7.3 kcal/mol, respectively. This work enriches bioactive drug discovery to treat epilepsy and illustrates an underlying pharmacological and molecular mechanism of these natural α-pyrones.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping