Shao Feng, Panahipour Layla, Gruber Reinhard
Department of Oral Biology, University Clinic of Dentistry, Medical University of Vienna, Vienna, Austria.
Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang, China.
J Dent Sci. 2023 Jan;18(1):112-119. doi: 10.1016/j.jds.2022.06.026. Epub 2022 Jul 15.
BACKGROUND/PURPOSE: has been widely used in traditional medicine because of its flavonoids. This study examined which components in were capable of reducing or even stimulating the formation of bone-resorbing osteoclasts.
We have isolated subfamilies of chalcones (isoliquiritigenin, butein), flavones (7-hydroxy-6-methoxyflavone) and neoflavanoids (5-methoxylatifolin), and performed an in vitro bioassay on osteoclastogenesis. The flavonoids were tested for their potential to change the expression of tartrate-resistant acid phosphatase (TRAP) and cathepsin K (CTSK) in murine bone marrow cultures being exposed to RANKL, M-CSF and TGF-β1 using RT-PCR, histochemistry and immunoassay.
We could confirm that isoliquiritigenin and butein significantly lower the expression of TRAP and CTSK in this setting. Moreover, histochemistry supported the decrease of TRAP by the chalcones. We further observed a trend towards an increase of osteoclastogenesis in the presence of 5-methoxylatifolin and 7-hydroxy-6-methoxyflavone, particular in bone marrow cultures being exposed to RANKL and M-CSF. Consistently, the anti-inflammatory activity was restricted to isoliquiritigenin and butein in murine RAW 264.7 inflammatory macrophages stimulated by lipopolysaccharide (LPS). With respect to osteoblastogenesis, neither of the flavonoids but butyrate, a short chain fatty acid, increased the osteogenic differentiation marker alkaline phosphatase activity in ST2 murine mesenchymal cells.
We have identified two flavonoids from with a potential pro-osteoclastogenic activity and confirm the anti-osteoclastogenic activity of isoliquiritigenin and butein.
背景/目的：因其黄酮类化合物而在传统医学中被广泛使用。本研究检测了[具体物质名称未给出]中的哪些成分能够减少甚至刺激骨吸收破骨细胞的形成。
我们分离出了查耳酮亚家族（异甘草素、紫铆因）、黄酮类（7-羟基-6-甲氧基黄酮）和新黄酮类（5-甲氧基落叶松脂素），并对破骨细胞生成进行了体外生物测定。使用逆转录聚合酶链反应（RT-PCR）、组织化学和免疫测定法，检测了黄酮类化合物在暴露于核因子κB受体活化因子配体（RANKL）、巨噬细胞集落刺激因子（M-CSF）和转化生长因子-β1（TGF-β1）的小鼠骨髓培养物中改变抗酒石酸酸性磷酸酶（TRAP）和组织蛋白酶K（CTSK）表达的潜力。
我们可以证实在这种情况下，异甘草素和紫铆因显著降低了TRAP和CTSK的表达。此外，组织化学证实了查耳酮可使TRAP减少。我们还进一步观察到，在存在5-甲氧基落叶松脂素和7-羟基-6-甲氧基黄酮的情况下，尤其是在暴露于RANKL和M-CSF的骨髓培养物中，有破骨细胞生成增加的趋势。同样，在脂多糖（LPS）刺激的小鼠RAW 264.7炎性巨噬细胞中，抗炎活性仅限于异甘草素和紫铆因。关于成骨细胞生成，除了短链脂肪酸丁酸盐外，这些黄酮类化合物均未增加ST2小鼠间充质细胞中成骨分化标志物碱性磷酸酶的活性。
我们从[具体物质名称未给出]中鉴定出两种具有潜在促破骨细胞生成活性的黄酮类化合物，并证实了异甘草素和紫铆因的抗破骨细胞生成活性。
