2. Academic Validation
  3. Aloperine improves osteoporosis in ovariectomized mice by inhibiting RANKL-induced NF-κB, ERK and JNK approaches

Aloperine improves osteoporosis in ovariectomized mice by inhibiting RANKL-induced NF-κB, ERK and JNK approaches

  • Int Immunopharmacol. 2021 Aug;97:107720. doi: 10.1016/j.intimp.2021.107720.
Rong Hu 1,  Libo Chen 2,  Xiaolong Chen 1,  Zhong Xie 3,  Chao Xia 3,  Yong Chen 4
Affiliations

Affiliations

  • 1 Department of Radiology, the First Affiliated Hospital, University of South China, Hengyang, Hunan 421000, China.
  • 2 Department of Urology, the First Affiliated Hospital, University of South China, Hengyang, Hunan 421000, China.
  • 3 Department of Spinal Surgery, the First Affiliated Hospital, University of South China, Hengyang, Hunan 421000, China.
  • 4 Department of Spinal Surgery, the First Affiliated Hospital, University of South China, Hengyang, Hunan 421000, China. Electronic address: yongchen110@sina.com.
PMID: 33945918 DOI: 10.1016/j.intimp.2021.107720
Abstract

Presently, postmenopausal osteoporosis mainly caused by excessive activation of in vivo osteoclasts has become a global public health burden. Natural compounds have gradually become the potential drugs for the treatment of postmenopausal osteoporosis. Aloperine is a new alkaloid extracted from the leaves and seeds of sophora bean. The current studies have proved that aloperine has many biological activities, including anti-inflammatory, Antiviral and Anticancer activities. This study shows that aloperine can inhibit activity and formation of osteoclast mediated by RANKL in a dose-dependent manner without affecting the activity of bone marrow macrophages (BMM). In addition, it is found that aloperine can inhibit the expression of osteoclast specific marker genes, including nuclear factor of activated T cells cytoplasmic 1 (NFATc1), tartrate resistant Acid Phosphatase (TRAcP), matrix metallopeptidase 9 (MMP9), Cathepsin K (Ctsk), V-ATPase d2 and Calcitonin receptor. The in vitro experiment of aloperine proved that aloperine can inhibit the degradation of IκBα and the phosphorylation of P65, ERK and JNK. Additionally, aloperine improves bone loss in ovariectomized (OVX) mice by inhibiting osteoclast activity. This project proved that aloperine can affect the formation of osteoclasts by inhibiting RANKL signaling channel, and it is indicated that aloperine has the potential to be developed as a new drug for the prevention and treatment of postmenopausal osteoporosis.

Keywords

Aloperine; NF-κB; Osteoclast; Postmenopausal osteoporosis; RANKL.

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