Objective

Epilepsy is a serious neural disease that affects around 50 million people all over the world. Although for the majority patients with epilepsy, seizures are well controlled by currently available antiepileptic drugs (AEDs), there are still >30% of patients suffered from medically refractory epilepsy and approximately 30–40% of all epileptic patients affected by numerous side effects and seizure resistance to the current AEDs. Therefore, many researchers try to develop novel approaches to treat epilepsy, for example, to discover new antiepileptic constituents from herbal medicines. Although there are already several reviews on phytotherapy in epilepsy, most of them placed emphasis on the plant crude extracts or their isolated fractions, not pure active compounds derived from herbal medicines. This article aims to review components in herbal medicines that have shown antiepileptic or anticonvulsant properties.

Methods

We searched online databases and identified articles using the preset searching syntax and inclusion criteria. The active medicinal compounds that have shown anticonvulsant or antiepileptic activity were included and classified according to structural types.

Results

We have reviewed herein the active constituents including alkaloids, flavonoids, terpenoids, saponins, and coumarins. The screening models, the seizures‐inducing factors and response, the effective dose, the potential mechanisms, as well as the structure‐activity relationships in some of these active components have also been discussed.

Significance

The in vitro and in vivo experimental data reviewed in this paper would supply the basic science evidence for research and development of novel AEDs from medicinal plants.