Department of Biological Chemistry, Chubu University, 1200 Matsumoto, Kasugai, Aichi, 487-8501, Japan.
Cytotechnology. 2012 May;64(3):315-22. doi: 10.1007/s10616-011-9416-z. Epub 2012 Apr 24.
The dried flower buds of Magnolia sp. are widely used as herbal medicines because of their anti-inflammatory, anti-malarial and anti-platelet activities. Here, we found that veraguensin and galgravin, lignan compounds derived from Magnolia sp., dose-dependently inhibited osteoclast formation in co-cultures of bone marrow cells and osteoblastic cells. These compounds also inhibited receptor activator of nuclear factor κB ligand (RANKL)-induced osteoclast differentiation in RAW264.7 cells and bone marrow macrophages. In the RANKL-induced signaling pathway, veraguensin and galgravin reduced p38 phosphorylation and suppressed the expression of c-Fos, a key transcription factor for osteoclastogenesis. Veraguensin and galgravin also inhibited osteoclastic pit formation, which was accompanied by decreased mature osteoclast viability. In conclusion, these results indicate that veraguensin and galgravin can inhibit bone resorption and may offer novel compounds for the development of drugs to treat bone-destructive diseases such as osteoporosis.
厚朴的干花蕾因其具有抗炎、抗疟疾和抗血小板活性而被广泛用作草药。在这里，我们发现，厚朴酚和厚朴酚，这两种来源于厚朴的木脂素化合物，能够剂量依赖性地抑制骨髓细胞和成骨细胞共培养物中的破骨细胞形成。这些化合物还抑制了核因子κB 受体激活剂配体（RANKL）诱导的 RAW264.7 细胞和骨髓巨噬细胞中的破骨细胞分化。在 RANKL 诱导的信号通路中，厚朴酚和厚朴酚降低了 p38 的磷酸化，并抑制了破骨细胞生成的关键转录因子 c-Fos 的表达。厚朴酚和厚朴酚还抑制了破骨细胞陷窝的形成，同时降低了成熟破骨细胞的活力。总之，这些结果表明，厚朴酚和厚朴酚可以抑制骨吸收，可能为开发治疗骨质疏松等骨破坏性疾病的药物提供新的化合物。
