Anti-nociceptive and anti-inflammatory potentials of fractions from the extract of Tetracarpidium conophorum leaf in rats and mice

Tetracarpidium conophorum (TC) (Euphorbiaceae) is a perennial woody climbing shrub in low bush forest of some parts of West Africa and used among the natives for relief of ailments accompanying pain and inflammation. In this study, the analgesic and anti-inflammatory effects of the methanolic extract (METC) and fractions (ethyl acetate, F1 and n-hexane, F2) of Tetracarpidium conophorum leaf were evaluated in rat and mice. The analgesic activity was evaluated using acetic acid-induced writhing, formalin-induced paw licking and hot plate test models. Carrageenan-induced paw oedema was used to assess anti-inflammatory activity in rats. The mechanism of action of (TC) was explored by the use of naloxone, a non-selective opioid receptor blocker. The highest analgesic effect was observed in F2 extract at 57.21% inhibition and was further studied on various analgesic and anti-inflammatory models in graded doses. F2 significantly inhibited the late phase of formalin-induced paw licking and prolong hot plate latency at 55±1°C. The n-hexane fraction also significantly inhibited carrageenan-induced paw oedema in rats at 100 and 200mg/kg doses significantly (p< 0.001) and reduced paw licking response by 85.08% compared with control. Naloxone, an opioid receptor antagonist, did not significantly affect the changes observed with n-hexane fraction, thus ruling out the possibility of the involvement of opioid receptors in the analgesic actions of Tetracarpidium conophorum. Phytochemical screening showed that the leaf extracts contain alkaloids, tannins, saponins and cardenolides. The investigations showed that Tetracarpidium conophorum possesses significant anti-nociceptive and anti-inflammatory activities that should be explored.

Analgesic synergism of gabapentin and carbamazepine in rat model of diabetic neuropathic pain

Purpose: To evaluate synergy in the analgesic effects of a combination therapy of carbamazepine (CBZ) and gabapentin (GBP) in diabetic neuropathic pain. Methods: Neuropathic pain was produced in rats by a single intraperitoneal injection of streptozotocin (STZ) at 60 mg/kg. CBZ, GBP, and their combination were orally administered at varying doses (GBP 30 - 180 mg/kg; CBZ 20 - 40 mg/kg) comparable to their therapeutic doses in humans. Nociceptive responses in the diabetic rats were assessed using hot plate test. Results: Hot plate latency significantly increased with oral administration of GBP at a dose of 180 mg/kg when compared with control group (p < 0.05), while at a dose of 90 mg/kg, the increase was not significant. Oral administration of CBZ at doses of 20 and 40 mg/kg did not produce any significant impact on hot plate latency. However, a combination of GBP at 90 mg/kg and CBZ at 20 mg/kg produced significant increase in latency, compared with control group and other groups (p < 0.05), except the group that received 180 mg/kg GBP. The combination of low dose GBP 30 mg/kg and carbamazepine 30 mg/kg had no significant effect on latency (p > 0.05). Conclusion: The results obtained in this study provide useful information on the combination therapy of GBP and CBZ, which may be applied in the treatment of pain in diabetic neuropathy.

In vivo analgesic activity and safety assessment of Vitis vinifera L and Punica granatum L fruits extracts

Purpose: To investigate the analgesic properties of fruit extracts of Vitis vinifera (grape) and Punica granatum (pomegranate) in Albino mal mice. Methods: The analgesic activity of fruit extracts of V. vinifera and P. granatum were examined in vivo using thermal stimulus assays (i.e., tail immersion and hot plate) and acetic acid-induced writhing test using acetylsalicylic acid (0.1 g/kg, per os) as standard. The extracts were administered orally in doses of 1.0, 2.0 and 3.0 g/kg. Results: In acetic acid writhes test, both fruit extract pretreatments (1.0, 2.0 and 3.0 g/kg, per os) significantly decreased the number of writhes (p < 0.0001) in a dose-dependent manner compared to control. The Index of Pain Inhibition (IPI) values following V. vinifera extract treatments were 36.52 % (1.0 g/kg), 66.67 % (2.0 g/kg) and 89.71 % (3.0 g/kg) which were significantly different from those for P. granatum extracts (45.39 %, 1.0 g/kg), 70.93 %, 2.0 g/kg) and 86.88 %, 3.0 g/kg) at equivalent doses of 2.0 and 3.0 g/kg of the extracts The fruit extracts of both species increased the reaction latency time. In tail-immersion assay, only the fruit extract of P. granatum significantly increased the response to heat stimulus at doses of 2.0 g/kg (p < 0.05). Conclusion: The hydroalcohol fruit extracts of P. granatum and V. vinifera have potential analgesic effects. Further studies are needed to determine the active component responsible for this effect.