Analgesic effects of 1,2,3,4,6-penta-O-galloyl-β-D-glucose in an animal model of lipopolysaccharide-induced pain.

We examined the analgesic effects of 1,2,3, 4,6-penta-O-galloyl-β-D-glucose (β-PGG), a prototypical gallotannin, in an animal model of lipopolysaccharide (LPS)‑induced pain. To evaluate the analgesic activity of β-PGG, we assessed the potential of β-PGG to inhibit the generation of nitric oxide (NO) in LPS-stressed RAW 264.7 cells, and found that β-PGG inhibits NO generation in a dose-dependent manner. Furthermore, the effects of β-PGG on the voluntary movements of LPS-exposed animals were evaluated. The results showed that the voluntary movements of animals were markedly recovered after β-PGG treatment. The mRNA expression of interleukin (IL)-1β (1.33±0.38-fold) and IL-6 (0.64±0.40-fold) in the brain tissue of β-PGG-treated animals markedly decreased compared with that observed in the control groups (3.86±0.91 and 2.45±1.12-fold, respectively) and in the other LPS-administered groups. The results showed that β-PGG has potential to alleviate pain, not only by decreasing cellular NO generation in RAW 264.7 cells but also by the recovery of voluntary movement lost owing to inflammatory pain. This suggests that β-PGG is comparable to ibuprofen, which was used as a positive control in this study. Collectively, these findings suggest that β-PGG is a valuable natural compound which possesses analgesic activity.