Unripe fruit of Annona muricata Linn. (Annonaceae) (soursop) is used in traditional African medicine for the treatment of neuralgia, rheumatism, and arthritic pain. This study sought to investigate the analgesic and anti-inflammatory effects of lyophilized fruit extract of Annona muricata (AM) in rodents. The analgesic activity was evaluated using the mouse writhing, formalin, and hot-plate tests while the anti-inflammatory action was investigated using the carrageenan-induced rat paw edema and xylene-induced ear edema tests. Pretreatment with AM (50, 100, and 200 mg/kg, p.o.) produced dose-dependent (P<.001) inhibition of writhes and formalin-induced pain in the late phase. AM and morphine produced time-course increase in pain threshold in hot-plate test. However, the analgesic effect elicited by AM was reversed (P<.05) by naloxone pretreatment. Similarly, the time-dependent increase in paw circumference induced by carrageenan was inhibited by AM treatment with peak effect (0.23±0.10 cm; P<.001, 200 mg/kg; 6 h), which was comparatively similar to that of diclofenac treated. Further, the xylene-induced ear edema was significantly reduced by AM (50 or 100 mg/kg) pretreatment; however, the anti-inflammatory effect elicited by AM was prevented by pretreatment of mice with N(G)-nitro-l-arginine (20 mg/kg, i.p., nitric-oxide synthase inhibitor) 15 min before AM (200 mg/kg, p.o.). The in vitro cyclooxygenase assay also showed that AM produced concentration-dependent inhibition of both cyclooxygenase (COX)-1 and COX-2 activity by 39.44%±0.05% and 55.71%±0.12%, respectively, at 100 μg/mL. In conclusion, A. muricata possesses analgesic effect through interaction with opioidergic pathway and anti-inflammatory property through inhibition of chemical mediators of inflammation.
A number of Vitex species have been investigated as a source of potential bioactive compounds such as ecdysteroids [1], diterpenoids [2], iridoids [3], flavonoids, and phenolic compounds [4] demonstrating antioxidant, anti-inflammatory, antimicrobial, hepatoprotective, analgesic, antihistaminic, anti-implantation, and antiasthmatic activities [5,6]. Generally, ecdysteroids and iridoids have been explored as chemotaxonomic markers for the plants in the family Lamiaceae including Vitex species [7]. Vitex doniana Sweet (Lamiaceae) is a small to medium sized tree growing up to 25 m tall with no phytochemical report in spite of the available ethnopharmacological significance among different African communities [8], including use of water decoctions of different parts for treatment of stomach and rheumatic pains as well as inflammatory disorders [9,10]. Antidepressant effects and potentiation of sodium thiopental sleeping time, muscle relaxant [11], anti-inflammatory, and analgesic activities [8] of V. doniana leaf extracts have been reported as well as antihypertensive effects on normative and hypertensive rats, trypanocidal and antidiarrheal activities of the stem bark [12]. Recent indication of anti-inflammatory, anticonvulsant, and antipyretic properties of ethanol extracts [13] of V. doniana stem bark prompted a phytochemical analysis of the plantʼs stem bark for potential anti-inflammatory compounds. As a result of this study, isolation of three new phytoecdysteroids [21-hydroxyshidasterone (1), 11β-hydroxy-20-deoxyshidasterone (2), and 2,3-acetonide-24-hydroxyecdysone (3)] and four known phytoecdysteroids [shidasterone (4), ajugasterone C (5), 24-hydroxyecdysone (6), and 11β,24-dihydroxyecdysone (7)] with comparable anti-inflammatory activities as diclofenac are reported. Abstract !With reference to the ethnopharmacological significance of Vitex doniana Sweet (Lamiaceae) leaves in the treatment of stomach and rheumatic pains as well as inflammatory disorders, biological studies on its stem bark extracts have also reported anti-inflammatory and analgesic activities, with no attempt to identify the active components. Chromatographic and spectroscopic procedures identified three new phytoecdysteroids: 21-hydroxyshidasterone (1), 11β-hydroxy-20-deoxyshidasterone (2), and 2,3-acetonide-24-hydroxyecdysone (3) from the stem bark methanol extracts along with known ecdysteroids shidasterone (4), ajugasterone C (5), 24-hydroxyecdysone (6), and 11β,24-hydroxyecdysone (7). The compounds (1-7) showed significant (p ≤ 0.05) inhibitory effect at 100 mg/kg dose on rat paw oedema development due to carrageenan-induced inflammation in Sprague Dawley rats. These results suggest a possible contribution of ecdysteroids to the anti-inflammatory effect of some V. doniana stem bark extracts. Abbreviations
Quercetin shows structural features that have been related to the antioxidant potency of flavonoids and also shows neuroprotection in different models of oxidative death. Because only a few studies have focused on the flavonoid structural requirements for neuroprotection, this work evaluated the protective capacity of 13 flavones structurally related to quercetin, isolated from Kenyan plants, to rescue primary cerebellar granule neurons from death induced by a treatment with 24 h of hydrogen peroxide (150 microM). Each flavone (0-100 microM) was applied 24 h prior to the oxidative insult, and neuronal viability was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results suggest that the o-dihydroxy substitution in the B-ring is not necessary to afford neuroprotection and could be partly responsible for neurotoxic effects. Furthermore, the hydroxy substitutions in the positions C3 (C-ring) in C5 and C7 (A-ring) would be important for neuroprotection in this model.
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