PUBLICATION
DV21 decreases excitability of cortical pyramidal neurons and acts in epilepsy
- Authors
- Xu, M., Sun, P., Zhang, Y., Yang, C.H., Wei, X., Ma, X.X., Yang, C.R., Ni, K.M., Zhang, Y.J., Li, X.M.
- ID
- ZDB-PUB-181218-10
- Date
- 2017
- Source
- Scientific Reports 7: 1701 (Journal)
- Registered Authors
- Keywords
- none
- MeSH Terms
-
- Action Potentials/drug effects
- Animals
- Anthracenes
- Anticonvulsants/administration & dosage
- Anticonvulsants/pharmacology
- Anticonvulsants/therapeutic use
- Cerebral Cortex/pathology*
- Disease Models, Animal
- Drug Evaluation, Preclinical
- Epilepsy/blood
- Epilepsy/drug therapy*
- Epilepsy/pathology
- Epilepsy/physiopathology*
- Injections, Intraventricular
- Kainic Acid
- Mice, Inbred C57BL
- Pentylenetetrazole
- Pilocarpine
- Pyramidal Cells/drug effects
- Pyramidal Cells/pathology*
- Severity of Illness Index
- Triterpenes/administration & dosage
- Triterpenes/blood
- Triterpenes/pharmacology
- Triterpenes/therapeutic use*
- Zebrafish
- PubMed
- 28490750 Full text @ Sci. Rep.
Citation
Xu, M., Sun, P., Zhang, Y., Yang, C.H., Wei, X., Ma, X.X., Yang, C.R., Ni, K.M., Zhang, Y.J., Li, X.M. (2017) DV21 decreases excitability of cortical pyramidal neurons and acts in epilepsy. Scientific Reports. 7:1701.
Abstract
Epilepsy is one of the most common neurological disorders and the administration of antiepileptic drugs (AEDs) is the most common treatment. Although there are more than 15 AEDs available, a third of epilepsy patients remain refractory to available drugs, so novel effective drugs are needed. Here, we found that DV21, which is a natural triterpenoid compound extracted from plants of the Asclepiadaceae family, significantly decreased the incidence and stages of seizures in three classical drug-induced acute seizure models in C57BL/6 mice. Furthermore, we also found that the antiepileptic effect of DV21 might be partly mediated through reducing the excitability of cortical pyramidal neurons by increasing M current, which are low-threshold non-inactivating voltage-gated potassium currents. Moreover, the application of XE991, an inhibitor of M current, could block most the antiepileptic effect of DV21. Taken together, our results indicated that DV21 might be a novel leading compound for the treatment of epilepsy.
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