In vivo and in silico evaluation of antinociceptive activities of seed extract from the Holarrhena antidysenterica plant

Abstract

The objective of the study was to investigate the analgesic activity of seeds extracted from the Holarrhena antidysenterica plant (Family: Apocynaceae). The seeds of H. antidysenterica were extracted with pure ethanol and administered to the experimental Swiss albino mice at three different doses (50, 100, and 150 mg/kg body weight) in pain models. Peripheral analgesic activity was evaluated using the acetic acid-induced writhing test, and heat-induced (hot plate and tail immersion test) pain models were applied for central anti-nociceptive activity evaluation. Formalin induced licking test was applied to evaluate both peripheral and central anti-nociceptive activity on mice. Computational studies were performed by Schr€ odinger Maestro v10.1 for molecular docking and the SwissADME online server for ADME prediction of compounds. In acetic acid-induced writhing test, dosedependent reduction of writhing response was observed with 43.94% (p < 0.001) writhing inhibition at 150 mg/ kg dose compared to standard 60.98% (p < 0.001). 150 mg/kg caused a maximum decrease in licking and biting time in both early and late phases of the formalin-induced licking test (71.2 AE 5.67, p < 0.05, and 36.6 AE 5.62, p < 0.01 respectively). In both tests of central analgesic activity, the extract also showed dose-dependent antinociceptive activity. In the hot plate method, the highest %MPE was 67.39 (p < 0.001) at 30 min at 150 mg/kg dose, which was even better than the standard drug. In the case of the tail immersion method, the highest %MPE was 69.84 at a dose of 150 mg/kg at 30 min (p < 0.001). In molecular docking study, Conimine, Conarrhimin, Conessine, and Funtudienine showed the best binding affinities against the COX-1 enzyme. The study indicates that the ethanolic seed extract of H. antidysenterica has the strong potentiality of having central analgesic activity and moderate peripheral analgesic activity due to the presence of bioactive compounds in its seeds.

In vitro and in vivo Evaluation of Pharmacological Potential of Lasia spinosa Linn.

“…Any agent that reduces the number of licking responses will reveal analgesia in animal by inhibition of prostaglandin synthesis, a peripheral mechanism of pain inhibition. 29 During formalin test, the chloroform fractions at 500 mg/kg body weight showed maximum analgesic activity with 35.44% inhibition of licking responses induced by formalin, whereas aspirin at a dose of 10 mg/kg body weight exhibited 53.22% inhibition. Our observed result showed that the analgesic effect of L. spinosa is too peripherally mediated.…”

“…Time taken by the mouse to withdraw the tail is termed as tail immersion time. 29 Centrally acting analgesics elongate this responding time. In our study, the control group showed faster tail flicks at different time intervals of the experiment (Figure 3).…”

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“…Many plant extracts and isolated compounds from these have been proved to be analgesic by evaluating through models reported for analgesic activity (Bhuiyan et al, 2020). Crude alkaloidal fractions from medicinal plants are reported to possess analgesic response (Shoaib et al, 2016).…”

Free Radical Scavenging and Analgesic Activities of 70% Ethanol Extract of Luvunga sarmentosa (BI.) Kurz from Central Kalimantan

“…The hot plate is a standard method for evaluating central analgesic activity in animal models that use thermal stimuli as pain inducers with temperature was maintained at 55°C. The principle of this method is a change in spinal cord level, which effectively describes the centrally mediated anti-nociceptive response 24 . The paw-licking or jumping are defined as pain reflex behavior [25][26][27] .…”