RESUMO
Objective: To investigate the analgesic activity of methanolic extract of Entada phaseoloides (MEEP) along with its molecular mechanistic pathway. Methods: Swiss albino female mice and Wistar rats of either sex were administered orally with MEEP extracts (100, 200 and 400 mg/kg) and pentazocine, tramadol and diclofenac sodium, as standard drugs. Following administration, anti-nociceptive activity was evaluated using an acetic acid-induced writhing test, Eddy’s hot plate, and hot water immersion test. Serum was collected for molecular expression of various proteins and genes using Reverse Transcriptase PCR and Western Blotting. Results: Acetic acid writhing test, a frequently used method to assess peripheral analgesic activity, revealed that MEEP reduced peripherally induced pain in a dose-dependent manner. Likewise, Eddy’s hot plate and hot water immersion methods, often implicated for testing central analgesic activities, showed that MEEP is bestowed with the capability to counteract analgesia in a dose and time-dependent manner. Pro-inflammatory cytokines and factors like COX-2, IL-6, TNF-α, and NF-κB that cause inflammatory responses and pain were significantly reduced, suggesting its analgesic and anti-inflammatory potential. This analgesic and the anti-inflammatory role played by MEEP is also supported by the up-regulation of anti-inflammatory cytokine IL-10 and COMT and COX-1 enzyme demonstrated no significant difference between the groups. Conclusion: The study revealed the weak peripheral and potent central analgesic property MEEP by modulating pro-inflammatory and anti-inflammatory pathways.
RESUMO
Objective To study the chemical constituents from seed kernels of Entada phaseoloides. Methods The constituents were isolated and purified by silica gel and preparative HPLC column chromatographic methods, and their structures were identified by means of physicochemical properties and spectral analyses. Results Eight compounds were isolated from 70% ethanol extract of the seed kernels of E. phaseoloides, and identified as 4-methoxybenzyl-O-[α-L-arabinopyranosyl-(1→6)]-β-D-glucopyranoside (1), sinapyl-O-[β-D-apiofuranosyl-(1→2)]-O-β-D-glucopyranoside (2), 2-β-D-glucopyranosyloxy-5-hydroxy-phenylacetic acid (3), 2-β-D-glucopyranosyloxy-5-hydroxy-phenylacetic acid methyl ester (4), 5-O-β-D-glucopyranosyl-3-hydrobenzo [b] furan-2-one (5), dihydrophaseic acid-4'-O-β-D-glucopyranoside (6), corchoionoside C (7), and 1'S,4'S-4'-dihydroabscisic acid-4'-O-β-glucopyranoside (8). Conclusion Compound 1 is a new compound named phaseoloideside F, compound 5 is a new natural product, and compounds 2 and 4-8 are isolated from this plant for the first time.