1. Academic Validation
  2. Toddaculin, Isolated from of Toddalia asiatica (L.) Lam., Inhibited Osteoclastogenesis in RAW 264 Cells and Enhanced Osteoblastogenesis in MC3T3-E1 Cells

Toddaculin, Isolated from of Toddalia asiatica (L.) Lam., Inhibited Osteoclastogenesis in RAW 264 Cells and Enhanced Osteoblastogenesis in MC3T3-E1 Cells

  • PLoS One. 2015 May 18;10(5):e0127158. doi: 10.1371/journal.pone.0127158.
Akio Watanabe 1 Momochika Kumagai 2 Takashi Mishima 2 Junya Ito 3 Yurika Otoki 3 Teppei Harada 2 Tsuyoshi Kato 4 Mikihiko Yoshida 5 Misora Suzuki 6 Izumi Yoshida 2 Kazuhiro Fujita 2 Masatoshi Watai 2 Kiyotaka Nakagawa 3 Teruo Miyazawa 3
Affiliations

Affiliations

  • 1 Food Function Research Team, Saito Laboratory, Japan Food Research Laboratories, Ibaraki, Osaka, Japan; Food and Biodynamic Chemistry Laboratory, Graduate School of Agricultural Science, Tohoku University, Sendai, Miyagi, Japan.
  • 2 Food Function Research Team, Saito Laboratory, Japan Food Research Laboratories, Ibaraki, Osaka, Japan.
  • 3 Food and Biodynamic Chemistry Laboratory, Graduate School of Agricultural Science, Tohoku University, Sendai, Miyagi, Japan.
  • 4 Section of Applied Testing, Tama Laboratory, Japan Food Research Laboratories, Tama, Tokyo, Japan.
  • 5 Section of Nutraceutical Analysis, Saito Laboratory, Japan Food Research Laboratories, Ibaraki, Osaka, Japan.
  • 6 Section of Biological Safety Research, Tama Laboratory, Japan Food Research Laboratories, Tama, Tokyo, Japan.
Abstract

Osteoporosis with bone loss is widely recognized as a major health problem. Bone homeostasis is maintained by balancing bone formation and bone resorption. The imbalance caused by increased bone resorption over bone formation can lead to various bone-related diseases such as osteoporosis and rheumatoid arthritis. Osteoclasts are the principal cells responsible for bone resorption and the main targets of anti-resorptive therapies. However, excessive inhibition of osteoclast differentiation may lead to inhibition of osteoblast differentiation. Therefore, it is important to screen for new compounds capable of inhibiting bone resorption and enhancing bone formation. Toddalia asiatica (L.) Lam. has been utilized traditionally for medicinal purposes such as the treatment of rheumatism. Currently, the extract is considered to be a good source of pharmacological agents for the treatment of bone-related diseases, but the active compounds have yet to be identified. We investigated whether toddaculin, derived from Toddalia asiatica (L.) Lam., affects both processes by inhibiting bone resorption and enhancing bone formation. Towards this end, we used pre-osteoclastic RAW 264 cells and pre-osteoblastic MC3T3-E1 cells. We found that toddaculin not only inhibited the differentiation of osteoclasts via activation of the NF-κB, ERK 1/2, and p38 MAPK signaling pathways, but it also induced differentiation and mineralization of osteoblasts by regulating differentiation factors. Thus, toddaculin might be beneficial for the prevention and treatment of osteoporosis.

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