Anti-Inflammatory and Antinociceptive Activities of Bufalin in Rodents

Abstract

The aims of this study were to evaluate the anti-inflammatory and analgesic effects of bufalin, a major component of “Chan-su.” We used a carrageenan-induced paw edema model to assess the anti-inflammatory activity of this compound, and Western blot analysis detected NF-κB signaling during this effect. The antinociceptive activities were evaluated by acetic acid-induced writhing, formalin, and hot-plate tests; open-field test investigated effects on the central nervous system. Our data showed that bufalin (0.3 and 0.6 mg/kg, i.p.) potently decreased carrageenan-induced paw edema. Bufalin down regulated the expression levels of nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) during these treatments. Further studies demonstrated that bufalin significantly inhibited the activation of NF-κB signaling. Bufalin also reduced acetic acid-induced writhing and the licking time in the formalin test and increased hot-plate reaction latencies. Naloxone pretreatment (2 mg/kg, i.p.) in the early phases of the formalin test and hot-plate test significantly attenuated the bufalin-induced antinociception effects, which suggests the involvement of the opioid system. A reduction in locomotion was not observed in the open-field test after bufalin administration. Taken together, bufalin treatment resulted in in vivo anti-inflammatory and analgesic effects, and bufalin may be a novel, potential drug for the treatment of inflammatory diseases.

Anti-tumor Activity of Bufalin by Inhibiting c-MET Mediated MEK/ERK and PI3K/AKT Signaling Pathways in Gallbladder Cancer

“…Bufalin is a kind of cardiac glycosides which is derived from the serous fluid secreted by the parotid venom glands and skin of Bufo melanostictus and Bufo bufo gargarizans [20]. Researches have showed that Bufalin has many pharmacological activities, including anti-inflammatory, anti-tumor, antiviral, cardiotonic and narcotic effects [21][22][23][24]. Among these effects, the anti-tumor activity of Bufalin has caught the attention of many researchers.…”

Bufalin Inhibits the Inflammatory Effects in Asthmatic Mice through the Suppression of Nuclear Factor-Kappa B Activity

“…In this study, our data demonstrated that bufalin treatment strongly suppressed the degradation of IκBα from NF-κB/IκBα complex, suggesting that NF-κB cannot translocate into the nucleus where it induces gene transcription by binding to the promoter of NF-κB responsive genes [39]. Similar findings indicated that bufalin significantly inhibited the activation of NF-κB in vivo by maintaining the level of IκBα, and reduced the nuclear translocation of NF-κB p65 [13]. It was reported that pretreatment with NF-κB p65 antisense significantly inhibited the established asthmatic reaction in a murine model [40].…”

“…These results suggest that bufalin may exert its anti-inflammation effects through inhibition of NF-κB activity. Recent studies have demonstrated that bufalin also exhibits a strong, dose-dependent anti-inflammatory effect on carrageenan-induced paw edema in rats by suppressing the activation of NF-κB and reducing the production of its downstream proinflammatory mediators during acute inflammation [13]. Additionally, the bufalin analogues, ouabain, and digoxin, also possess strong anti-inflammatory effects [41,42].…”

“…In recent years, bufalin was found to exert anti-inflammatory and analgesic effects in the carrageenan-induced paw edema of rodents [13]. To our knowledge, the possible benefits of bufalin in asthma treatment are still unavailable.…”

Apoptosis Inducer Capacity of Cardiotonic Steroids of <i>Urginea maritima</i> Extract on SH-SY5Y Neuroblastoma Cells, with Less Susceptibility among Neuron-Module Cells

“…Products that more effectively affect the tumorigenic cellular events than those in non-tumorigenic cells are still a critical target that is strongly needed in human neurological disorders. With their great structural diversity, natural products have offered major opportunities for the identification of novel drugs that are active against a wide range of diseases, including neurological disorders (Dunn et al, 2011;Huang et al, 2010;Wen et al, 2014). Recent significant research reported that the mechanisms by which natural extracts are powerful in promoting healing are relatively complex.…”