3,4,5-Trimethoxycinnamic acid, one of the constituents of Polygalae Radix exerts anti-seizure effects by modulating GABAAergic systems in mice

Abstract

Polygalae Radix is an important medicinal plant that is widely used in most of Africa. 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix. Until now, the mechanisms involved in the anti-seizure property of TMCA are still unclear. We examined the anti-seizure effect of TMCA. TMCA administered at doses of 5, 10 and 20 mg/kg and evaluated anti-seizure effects by maximal electroshock (MES) and pentylenetetrazol (PTZ) models in mice. TMCA administered at doses of 10 and 20 mg/kg significantly reduced the incidence of MES-induced tonic hindlimb extension (THE). TMCA significantly delayed the onset of myoclonic jerks (MJ), and decreased the seizure severity and mortality compared with the vehicle-treated animals in PTZ seizure model. TMCA 10 and 20 mg/kg treated groups also did not determined generalized clonic seizures (GCS). Pretreatment with a GABAA/benzodiazepine (BZ) receptor antagonist flumazenil blocked the anti-seizure effects of TMCA. These data support the further investigation of TMCA as a GABAA/BZ receptor agonist for anti-seizure therapy.

Effects of polaprezinc on gastric mucosal damage and neurotransmitters in a rat model of chemotherapy-induced vomiting

“…After activation, NF-κB regulates the expression of genes such as those encoding the inflammatory cytokines TNF-α, IL-1, and IL-6 that can directly or indirectly affect microvascular endothelial cells or blood cells to mediate their interaction, which leads to the dysfunction of microcirculation, endothelial cell, and tissue injury. 18 …”

Anticonvulsant Activity of Halogen-Substituted Cinnamic Acid Derivatives and Their Effects on Glycosylation of PTZ-Induced Chronic Epilepsy in Mice

“…In Gunia’s study, it was confirmed that the cinnamic acid derivatives have anticonvulsant activity and their study clarifies a new way to discover new potential anticonvulsants [ 18 ]. In 2015, a cinnamic acid, 3,4,5-trimethoxycinnamic acid, the main active ingredient isolated from P. tenuifolia , has been found to display anticonvulsant effect [ 19 ]. Animal models have made great contributions to the treatment of epilepsy.…”

UHPLC-MS/MS method for pharmacokinetic and bioavailability determination of five bioactive components in raw and various processed products of Polygala tenuifolia in rat plasma

“…Recent pharmacological studies have suggested that PT and its extracted fractions have significant effects regarding neuroprotection (Wang et al 2019), anti-amnesia (Zhang et al 2008), anti-depressant properties (Cao et al 2018) and relieving the symptoms of extreme fear in rats (Shin et al 2018). The main chemical components in PT include triterpenoid saponins, oligosaccharide esters and organic acids, of which oligosaccharide esters and organic acids are beneficial for the central nervous system (Liu et al 2015;Chen et al 2016). Sibiricose A5 (A5), sibiricose A6 (A6), 3,6 0 -disinapoyl sucrose (DSS) and tenuifoliside A (TFSA) are representative oligosaccharide esters in PT, while 3,4,5-trimethoxycinnamic acid (TMCA) is a representative organic acid, which showed anti-seizure (Chen et al 2016), antistroke (Li et al 2017), anti-inflammatory (Kim et al 2013), neuroprotective (Liu et al 2015) and anti-depressant-like effects (Hu et al 2010).…”

“…The main chemical components in PT include triterpenoid saponins, oligosaccharide esters and organic acids, of which oligosaccharide esters and organic acids are beneficial for the central nervous system (Liu et al 2015;Chen et al 2016). Sibiricose A5 (A5), sibiricose A6 (A6), 3,6 0 -disinapoyl sucrose (DSS) and tenuifoliside A (TFSA) are representative oligosaccharide esters in PT, while 3,4,5-trimethoxycinnamic acid (TMCA) is a representative organic acid, which showed anti-seizure (Chen et al 2016), antistroke (Li et al 2017), anti-inflammatory (Kim et al 2013), neuroprotective (Liu et al 2015) and anti-depressant-like effects (Hu et al 2010). To date, several pharmacokinetic studies about the active components of PT have been reported.…”