LC-ESI-MS/MS-based phytochemical profiling and pharmacological validation of Centaurium erythraea Rafn (Gentianaceae)
Sarra Chabane1, Amel Boudjelal2, Ibrahim Demirtas3
1Department of Veterinary, Faculty of Sciences, M'sila University, Algeria; Laboratory of Biology: Applications in Health and Environment, M'sila University, Algeria.
Ethnopharmacological Relevance:
These findings provide scientific support for the traditional use of Centaurium erythraea Rafn (Gentianaceae) in Algerian folk medicine and suggest its potential for further pharmacological exploration in the management of pain and neuroinflammatory conditions.
Aim Of The Study:
The present study aimed to scientifically validate these traditional uses through phytochemical profiling and pharmacological evaluation of the aqueous extract (C. erythraea aqueous extract, CEAE).
Materials And Methods:
The polyphenolic composition was characterized, and in vitro antioxidant and DNA protection activities, enzyme inhibitory effects, as well as in vivo analgesic activity using the acetic acid-induced writhing and hot plate tests, in addition to acute oral toxicity, and molecular docking studies were evaluated.
Results:
LC-ESI-MS/MS analysis revealed the presence of several phenolic and flavonoid constituents, including trans-ferulic acid (278.74 μg/g), syringic acid (172.81 μg/g), polydatin (33.72 μg/g), vanillin (13.05 μg/g), quercetin (12.44 μg/g), and isoquercitrin (9.32 μg/g), along with minor levels of kaempferol and trans-cinnamic acid. CEAE exhibited moderate antioxidant activity, with the strongest effect in the FRAP assay (IC50 = 148.73 ± 8.50 μg/mL). The extract showed dual inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), demonstrating stronger activity against BChE (IC50 = 31.27 ± 2.68 μg/mL) than the reference drug galantamine. In plasmid DNA protection assays, CEAE (14.69 % protection) and quercetin preserved supercoiled DNA (Form I) from oxidative damage. Oral administration of CEAE (2000 mg/kg) produced no signs of toxicity, indicating a wide safety margin. In vivo, CEAE significantly reduced acetic acid-induced writhing (51.23 % inhibition at 300 mg/kg) and increased latency times in the hot plate test, showing greater analgesic efficacy than paracetamol. The binding affinity of the trans-ferulic/syringic acid adduct (-7.1 kcal/mol) in molecular docking interactions with AChE was determined to be higher than that of the compounds (-6.7 kcal/mol) used alone.
Conclusions:
Overall, the aqueous extract of C. erythraea demonstrates notable antioxidant, cholinesterase-inhibitory, DNA-protective, and analgesic activities, consistent with its traditional use for pain and inflammation.
