Anti-inflammatory and antinociceptive activities of bufalin in rodents.
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- κ B 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.
Department of Anesthesiology, State Key Laboratory of Oncology in South China, Sun Yat-Sen University Cancer Center, 651 Dongfeng East Road, Guangzhou 510060, China.
Lili
0000-0003-3013-7289
L
Wen
Department of Anesthesiology, State Key Laboratory of Oncology in South China, Sun Yat-Sen University Cancer Center, 651 Dongfeng East Road, Guangzhou 510060, China.
Yang
Y
Huang
Department of Orthopaedic Oncology, First Affiliated Hospital of Sun Yat-Sen University, Guangzhou 510080, China.
Xianbiao
0000-0002-4212-2116
X
Xie
Department of Anesthesiology, State Key Laboratory of Oncology in South China, Sun Yat-Sen University Cancer Center, 651 Dongfeng East Road, Guangzhou 510060, China.
Wan
0000-0002-5153-3021
W
Huang
Department of Orthopaedic Oncology, First Affiliated Hospital of Sun Yat-Sen University, Guangzhou 510080, China.
Junqiang
J
Yin
Department of Anesthesiology, State Key Laboratory of Oncology in South China, Sun Yat-Sen University Cancer Center, 651 Dongfeng East Road, Guangzhou 510060, China.
Wenqian
W
Lin
The Institute of Biology, Guizhou Academy of Sciences, Guiyang 550009, China.
Qiang
0000-0001-6198-1955
Q
Jia
Department of Anesthesiology, State Key Laboratory of Oncology in South China, Sun Yat-Sen University Cancer Center, 651 Dongfeng East Road, Guangzhou 510060, China.
Weian
0000-0003-0818-402X
W
Zeng
D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use*; D002018:Bufanolides / Q000627:therapeutic use*; D002351:Carrageenan / Q000737:chemistry; D051546:Cyclooxygenase 2 / Q000378:metabolism; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D007249:Inflammation / Q000188:drug therapy; D053583:Interleukin-1beta / Q000378:metabolism; D015850:Interleukin-6 / Q000378:metabolism; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D016328:NF-kappa B / Q000378:metabolism; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism; D010146:Pain / Q000188:drug therapy*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D002018:Bufanolides; D053583:Interleukin-1beta; D015850:Interleukin-6; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D002351:Carrageenan; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2; C022777:bufalin