Int J Oral Biol.  2019 Sep;44(3):89-95. 10.11620/IJOB.2019.44.3.89.

Piperlongumine suppressed osteoclastogenesis in RAW264.7 macrophages

• Jin SM
• Kang HM
• Park DB
• Yu SB
• Kim IR
• Park BS

• KMID: 2460804
• DOI: http://doi.org/10.11620/IJOB.2019.44.3.89

Abstract

Piperlongumine (PL) is a natural product found in long pepper (Piper longum). The pharmacological effects of PL are well known, and it has been used for pain, hepatoprotection, and asthma in Oriental medicine. No studies have examined the effects of PL on bone tissue or bone-related diseases, including osteoporosis. The current study investigated for the first time the inhibitory effects of PL on osteoclast differentiation, bone resorption, and osteoclastogenesis-related factors in RAW264.7 macrophages stimulated by the receptor activator for nuclear factor-κB ligand (RANKL). Cytotoxicity was examined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and osteoclast differentiation and bone resorption were confirmed by tartrate-resistant acid phosphatase (TRAP) staining and pit formation analysis. Osteoclast differentiation factors were confirmed by western blotting. PL exhibited toxicity in RAW264.7 macrophages, inhibiting osteoclast formation and bone resorption, in addition to inhibiting the expression of osteoclastogenesis-related factors, such as tumor necrosis factor receptor-associated factor 6 (TRAF6), c-Fos, and NFATc1, in RANKL-stimulated RAW264.7 macrophages. These findings suggest that PL is suitable for the treatment of osteoporosis, and it serves as a potential therapeutic agent for various bone diseases.

Keyword

Piper longum; Osteoclastogenesis; Osteoporosis; Macrophagy

MeSH Terms

Acid Phosphatase
Asthma
Blotting, Western
Bone and Bones
Bone Diseases
Bone Resorption
Macrophages*
Medicine, East Asian Traditional
Osteoclasts
Osteoporosis
Piper
RANK Ligand
Tumor Necrosis Factor-alpha
Acid Phosphatase
RANK Ligand
Tumor Necrosis Factor-alpha