Next Article in Journal
Connexin 50 Expression in Ependymal Stem Progenitor Cells after Spinal Cord Injury Activation
Next Article in Special Issue
Exploring Different Strategies for Efficient Delivery of Colorectal Cancer Therapy
Previous Article in Journal
Endoplasmic Reticulum Stress Signaling in Plant Immunity—At the Crossroad of Life and Death
Previous Article in Special Issue
Improved Chemotherapeutic Activity by Morus alba Fruits through Immune Response of Toll-Like Receptor 4
Article Menu
Issue 11 (November) cover image

Export Article

Open AccessArticle
Int. J. Mol. Sci. 2015, 16(11), 26599-26607; doi:10.3390/ijms161125972

Natural Germacrane Sesquiterpenes Inhibit Osteoclast Formation, Bone Resorption, RANKL-Induced NF-κB Activation, and IκBα Degradation

1
Guangzhou Institute of Traumatic Surgery, Guangzhou Red Cross Hospital, Medical College, Jinan University, Guangzhou 510220, China
2
School of Dentistry, University of Western Australia, Perth, WA 6009, Australia
3
School of Pathology and Laboratory Medicine, the University of Western Australia, Perth, WA 6009, Australia
4
Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, China
5
Research Center for Drug Discovery (RCDD), School of Pharmaceutical Sciences, Sun Yat-Sen University, 132 East Circle at University City, Guangzhou 510006, China
6
Centre for Orthopaedic Research, School of Surgery, the University of Western Australia, Perth, WA 6009, Australia
*
Authors to whom correspondence should be addressed.
Academic Editors: Ge Zhang and Aiping Lu
Received: 7 September 2015 / Revised: 25 October 2015 / Accepted: 28 October 2015 / Published: 5 November 2015
View Full-Text   |   Download PDF [1359 KB, uploaded 5 November 2015]   |  

Abstract

Osteolytic bone diseases are commonly presented with enhanced osteoclast formation and bone resorption. Sesquiterpene lactone natural compounds have been found to possess anti-inflammatory and immune-modulation effects. Here, we identified three germacrane sesquiterpenes using computer-based virtual screening for the structural similarity with sesquiterpene lactone, parthenolide. We showed that natural germacrane sesquiterpene compounds A, B, and C inhibit osteoclast formation and bone resorption in a dose-dependent manner, with relative potency compound A > compound C > compound B based on their equimolar concentrations. Mechanistic studies by Luciferase reporter gene assay and Western blot analysis showed that germacrane sesquiterpene compound A inhibits RANKL-induced activation of NF-κB and IκBα degradation. This study reveals that natural germacrane sesquiterpene compounds are inhibitors for osteoclast formation and bone resorption, and provides evidence that naturally-occurring compounds might be beneficial as alternative medicine for the prevention and treatment of osteolysis. View Full-Text
Keywords: germacrane sesquiterpenes; osteoclastogenesis; bone resorption; RANKL; NF-κB; IκBα germacrane sesquiterpenes; osteoclastogenesis; bone resorption; RANKL; NF-κB; IκBα
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Qin, S.; Ang, E.; Dai, L.; Yang, X.; Ye, D.; Chen, H.; Zhou, L.; Yang, M.; Teguh, D.; Tan, R.; Xu, J.; Tickner, J.; Pavlos, N.J.; Xu, J. Natural Germacrane Sesquiterpenes Inhibit Osteoclast Formation, Bone Resorption, RANKL-Induced NF-κB Activation, and IκBα Degradation. Int. J. Mol. Sci. 2015, 16, 26599-26607.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top