In vivo and in silico assessment of anti-inflammatory and analgesic activities of dulcisflavan and 3-oxo-friedelan 20α-oic acid
摘要
The present study assessed the anti-inflammatory and analgesic activities of dulcisflavan, a flavanol from Myrianthus arboreus, and 3-oxo-friedelan-20α-oic acid, a triterpenoid from Solanum torvum in a rat model. The compounds were also docked onto key enzymes and receptors that contribute to inflammatory and analgesic responses invoked by carrageenan to obtain insight into their possible mechanisms of action. Inflammation and hyperalgesia were induced in rats using the λ-carrageenan with oedema measured using a plethysmometer and hyperalgesia measured as latency time of tail withdrawal from heat source (here the heat source was water bath set at 55 °C). Simulation of the compounds’ interactions with enzymes and receptors binding sites was carried out using the Maestro software. It was observed that both compounds exhibited significant anti-inflammatory activities by reducing the oedema produced after induction with carrageenan. Whereas 3-oxo-friedelan-20α-oic acid produced a significant dose-dependent (P < 0.0001) activity, the activity of dulcisflavan doses was not statistically significant (P = 0.0680) even though there was a reasonable anti-inflammatory effect. The compounds also improve the latency time of tail withdrawal by the animals, exhibiting considerable analgesic effects, however, this analgesic affects of 3-oxo-friedelan-20α-oic acid (P = 0.0876) and dulcisflavan (p = 0.4814) were not statistically significant. The compounds, especially dulcisflavan, produced high docking scores to key mediators characterized in carrageenan-induced inflammation and hyperalgesia. Dulcisflavan and 3-oxo-friedelan-20α-oic acid exhibited significant anti-inflammatory and analgesic effects in vivo, with target binding supported by in silico docking studies.